Compounds > tolvaptan
Page last updated: 2024-11-08

tolvaptan

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Cross-References

ID SourceID
PubMed CID216237
CHEMBL ID344159
CHEBI ID32246
SCHEMBL ID242421
MeSH IDM0299851

Synonyms (88)

Synonym
HY-17000
gtpl2226
n-[4-(7-chloro-5-hydroxy2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
samsca
tolvaptan ,
opc-41061
PDSP2_001721
PDSP1_001738
150683-30-0
opc 41061
7-chloro-5-hydroxy-1-(2-methyl-4-(2-methylbenzoylamino)benzoyl)2,3,4,5-tetrahydro-1h-1-benzazepine
opc-41061(tolvaptan)
bdbm35723
chembl344159 ,
n-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-benzo[b]azepine-1-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide
benzazepine derivative, 32
L001628
(r)-n-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide
A809063
n-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
NCGC00183001-01
cas-150683-30-0
tox21_113256
dtxsid3048780 ,
dtxcid9028706
n-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide
AKOS015994735
benzamide, n-(4-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl)-3-methylphenyl)-2-methyl-
(+-)-4'-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl) carbonyl)-o-tolu-m-toluidide
hsdb 8196
tolvaptan [usan:inn:ban]
unii-21g72t1950
(+-)-4'-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl)-o-tolu-m-toluidide
21g72t1950 ,
CS-0572
S2593
SCHEMBL242421
jynarque
tolvaptan [vandf]
jinarc
tolvaptan [inn]
tolvaptan [orange book]
tolvaptan [ema epar]
tolvaptan [usan]
tolvaptan [mart.]
tolvaptan [jan]
tolvaptan [mi]
tolvaptan [who-dd]
(+/-)-4'-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl) carbonyl)-o-tolu-m-toluidide
benzamide, n-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-
AM20090726
KS-1315
7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1h-1-benzazepine
GYHCTFXIZSNGJT-UHFFFAOYSA-N
5-hydroxy-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1h-benzazepine
7-chloro-5-hydroxy-1-[2-methyl-4-(2-methyl benzoyl amino) benzoyl]-2,3,4,5-tetrahydro-1h-1-benzazepine
7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino) benzoyl]-2,3,4,5-tetrahydro-1h-1-benzazepine
n-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
h-d-phe-pro-arg-5-amido-isophthalicacid-dimethylesteracetatesalt
AC-22748
HMS3604L08
AB01565822_02
mfcd09838782
SR-01000942265-1
sr-01000942265
CHEBI:32246 ,
HMS3656K20
tolvaptan, >=98% (hplc), powder
n-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-benzamide; 1h-1-benzazepine, benzamide deriv.; 1-[4-(2-methylbenzoylamino)-2-methylbenzoyl]-7-chloro-1,2,3,4-tetrahydrobenzo[b]azepin-5-ol; opc 41061; sam
SW219182-1
FT-0675287
FT-0675288
Q426132
Z1546610480
tolvaptan (opc-41061)
n-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-benzo[b]-azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide
HMS3744A09
CCG-269223
BT164486
tolvaptan- bio-x
n-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
EN300-123019
n-(4-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1h-1-benzazepin-1-yl)carbonyl)-3-methylphenyl)-2-methyl-
tolvaptan (mart.)
n-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-1-benzazepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide
tolvaptanum
c03xa01
n-(4-(((5r)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1h-1-benzazepin-1-yl)carbonyl)-3-methylphenyl)-2-methylbenzamide

Research Excerpts

Overview

Tolvaptan (TVP) is a selective antagonist of vasopressin receptors, approved for the treatment of hyponatremia in SIADH, congestive heart failure (CHF) and cirrhosis. It slows renal deterioration rate and cysts' growth, although its acquaretic effects often impact on quality of life (QoL) and treatment adherence.

ExcerptReferenceRelevance
"Tolvaptan is an orally administered aquaretic drug indicated for patients with congestive heart failure (CHF) to remove excess fluid. "( Pharmacokinetics, Pharmacodynamics, Efficacy, and Safety of OPC-61815, a Prodrug of Tolvaptan for Intravenous Administration, in Patients With Congestive Heart Failure　- A Phase II, Multicenter, Double-Blind, Randomized, Active-Controlled Trial.
Hirano, T; Kim, S; Sato, N; Uno, S; Yamasaki, Y, 2022)		2.39
"Tolvaptan is a selective vasopressin V"( [Tolvaptan, a vasopressin V
Aihara, M; Fujiki, H; Hattori, K; Isakari, Y; Mizuguchi, H; Nagano, K; Ohmoto, K; Takeshita, Y; Yamada, Y; Yamamoto, M; Yamamura, Y, 2022)		2.35
"Tolvaptan is a consolidate option for treatment of ADPKD patients; it slows renal deterioration rate and cysts' growth, although its acquaretic effects often impact on quality of life (QoL) and treatment adherence."( [Tolvaptan in ADPKD patients at the University of Padova Nephrology Unit: impact on quality of life, efficacy and safety].
Baldini Anastasio, P; Bugnotto, B; Calò, LA; Campo, D; Carraro, G; Cirella, I; di Vico, V; Rigato, M, 2022)		2.35
"Tolvaptan (TVP) is a selective antagonist of vasopressin receptors, approved for the treatment of hyponatremia in SIADH, congestive heart failure (CHF) and cirrhosis. "( Tolvaptan in portal hypertension: real life experience.
Delgado, A; Fernández-Alonso, V; Melero, R; Rodríguez-Benítez, P; Salcedo, M; Tejedor, M, 2023)		3.8
"Tolvaptan is an effective drug for the treatment of autosomal dominant polycystic kidney disease, but its use is associated with a significant risk of T-cell-mediated liver injury in a small number of patients. "( Activation of tolvaptan-responsive T-cell clones with the structurally-related mozavaptan.
Hammond, S; Meng, X; Mosedale, M; Naisbitt, DJ, 2023)		2.71
"Tolvaptan (TLV) is a selective vasopressin receptor 2 antagonist administered for congestive heart failure (CHF) after inadequate response to other diuretics. "( Effectiveness and safety of Tolvaptan in infants with congenital heart disease.
Hirano, D; Ito, A; Miwa, S; Oishi, K; Saito, A; Sakaguchi, H; Takemasa, Y; Umeda, C, )		1.87
"Tolvaptan is an effective therapy for heart failure patients with symptomatic congestion and hyponatremia. "( Short-Term Efficacy and Safety of Tolvaptan in Patients with Left Ventricular Assist Devices.
Chung, B; Fujino, T; Imamura, T; Jeevanandam, V; Kalantari, S; Kim, G; LaBuhn, C; Narang, N; Nguyen, A; Nitta, D; Raikhelkar, J; Rodgers, D; Sarswat, N; Sayer, G; Smith, B; Uriel, N, 2020)		2.28
"Tolvaptan is an approved drug for ADPKD patients, but is also associated with multiple side effects."( Renal cyst growth is attenuated by a combination treatment of tolvaptan and pioglitazone, while pioglitazone treatment alone is not effective.
Bange, H; Dijkstra, KL; Kanhai, AA; Leonhard, WN; Peters, DJM; Price, LS; Verburg, L, 2020)		1.52
"Tolvaptan is a selective oral vasopressin V2-receptor antagonist. "( Tolvaptan therapy to treat severe hyponatremia in pediatric nephrotic syndrome.
Delbet, JD; Parmentier, C; Ulinski, T, 2020)		3.44
"Tolvaptan is an effective therapeutic option in critically ill patients with volume overload refractory to conventional diuretics. "( Vasopressin antagonist efficacy and safety in volume-overloaded critically ill patients: a new therapeutic alternative.
Broch, MJ; Castellanos-Ortega, Á; Gordon, M; Pinos, A; Ramírez, P; Ruiz-Ramos, J; Sosa, M; Villarreal, E, 2020)		2
"Tolvaptan is an effective drug for the treatment of autosomal dominant polycystic kidney disease, but its use is associated with a significant risk of liver injury in a small number of patients. "( Tolvaptan- and Tolvaptan-Metabolite-Responsive T Cells in Patients with Drug-Induced Liver Injury.
Gibson, A; Hammond, S; Jaruthamsophon, K; Mosedale, M; Naisbitt, DJ; Roth, S, 2020)		3.44
"Tolvaptan (TVP) is an effective treatment for patients with cirrhotic ascites; however, studies have indicated that a sufficient effect is difficult to obtain in patients with hepatocellular carcinoma (HCC). "( Prediction factors of tolvaptan effectiveness in patients with refractory ascites complicated with hepatocellular carcinoma.
Azumi, M; Honma, T; Imai, M; Ishikawa, T; Iwanaga, A; Kojima, Y; Nozawa, Y; Sano, T; Yoshida, T, 2021)		2.38
"Tolvaptan is an arginine vasopressin (AVP) antagonist."( Tolvaptan-induced remission of primary palmar hyperhidrosis in a patient with ADPKD: a serendipitous finding.
Cuka, E; Joli, G; Manunta, P; Sciarrone Alibrandi, TM; Vespa, M, 2022)		2.89
"Tolvaptan (TLV) is a vasopressin V2 receptor antagonist that increases free water excretion. "( Efficacy of oral tolvaptan for severe edema and hyponatremia in a patient with refractory nephrotic syndrome.
Kaku, Y; Nishimura, M; Saimiya, M, 2021)		2.4
"Tolvaptan is a recently available diuretic that blocks arginine vasopressin receptor 2 in the renal collecting duct. "( Management of Cirrhotic Ascites under the Add-on Administration of Tolvaptan.
Adachi, T; Okada, H; Onishi, H; Oyama, A; Shiraha, H; Takaki, A; Takeuchi, Y; Wada, N, 2021)		2.3
"Tolvaptan (TLV) is an oral selective vasopressin type 2 receptor antagonist. "( Experience with long-term administration of tolvaptan to patients with acute decompensated heart failure.
Dobashi, S; Fujii, T; Hisatake, S; Ikeda, T; Kabuki, T; Kiuchi, S; Takashi, O, 2017)		2.16
"Tolvaptan (TLV) is an oral selective vasopressin 2 receptor antagonist that acts on the distal nephrons, causing a loss of electrolyte-free water. "( Favorable effects of early tolvaptan administration in very elderly patients after repeat hospitalizations for acute decompensated heart failure.
Hiasa, G; Hosokawa, S; Kawada, Y; Kawamura, G; Kazatani, Y; Kinoshita, M; Kosaki, T; Matsuoka, H; Okayama, H; Shigematsu, T; Takahashi, T; Yamada, T, 2018)		2.22
"Tolvaptan is an oral non-peptide, competitive antagonist of vasopressin receptor-2."( Effects of tolvaptan on urine output in hospitalized heart failure patients with hypoalbuminemia or proteinuria.
Amitani, K; Imura, H; Ishihara, S; Ishikawa, M; Kikuchi, A; Maruyama, Y; Nakama, K; Omote, T; Sato, N; Shimizu, W; Sone, M; Takagi, K; Takahashi, N; Tokuyama, H, 2018)		1.59
"Tolvaptan is an oral vasopressin receptor antagonist that can increase serum sodium concentrations by increasing electrolyte-free water excretion."( Diagnosis and management of hyponatraemia in the older patient.
Gonski, P; Grossmann, M; Obeid, J; Scholes, R; Topliss, DJ; Woodward, M, 2018)		1.2
"Tolvaptan (TLV) is a new vasopressin type 2 receptor antagonist effective in patients with heart failure (HF). "( A case report with shock induced by tolvaptan in an elderly patient with congestive heart failure.
Liu, XM; Zhang, ZG, 2018)		2.2
"Tolvaptan (TLV) is a newly developed oral vasopressin-2 receptor antagonist that is mostly used for patients with acute decompensated heart failure (ADHF) refractory to conventional diuretic therapy. "( The effects of tolvaptan dose on cardiac mortality in patients with acute decompensated heart failure after hospital discharge.
Ehara, S; Kawase, Y; Matsumoto, K; Nakamura, Y; Otsuka, K, 2018)		2.28
"Tolvaptan (TLV) is a diuretic agent administrated for heart failure (HF) only in Japan. "( Hemodynamic and Hormonal Effects of Tolvaptan for Heart Failure.
Ikeda, T; Kiuchi, S, 2019)		2.23
"Tolvaptan is an orally active antagonist of vasopressin (antidiuretic hormone [ADH]) V2 receptors. "( An update on tolvaptan for autosomal dominant polycystic kidney disease.
Blasco, M; Molina, A; Poch, E; Quintana, L; Rodas, L, 2018)		2.29
"Tolvaptan is an orally available vasopressin V2 receptor antagonist."( Con: Tolvaptan for autosomal dominant polycystic kidney disease-do we know all the answers?
Gross, P; Paliege, A; Schirutschke, H, 2019)		1.75
"Tolvaptan is an effective treatment for polycystic kidney disease (PKD), but also causes unfortunate polyuria. "( Hydrochlorothiazide ameliorates polyuria caused by tolvaptan treatment of polycystic kidney disease in PCK rats.
Hirose, T; Ito, S; Kinugasa, S; Mori, T; Muroya, Y; Oba-Yabana, I; Ohsaki, Y; Sato, E; Takahashi, C; Wang, A, 2019)		2.21
"Tolvaptan is a non-peptide orally available arginine vasopressin V2 receptor antagonist."( Positive Response to Tolvaptan Treatment Would Be a Good Prognostic Factor for Cirrhotic Patients with Ascites.
Kida, Y, 2019)		1.55
"Tolvaptan is an orally administered selective vasopressin 2 receptor antagonist that promotes aquaresis. "( Efficacy and Safety Evaluation of Tolvaptan on Management of Fluid Balance after Cardiovascular Surgery Using Cardiopulmonary Bypass.
Hirai, H; Hosono, M; Kaku, D; Kubota, Y; Nakahira, A; Sasaki, Y; Shibata, T; Suehiro, S; Suehiro, Y, 2016)		2.16
"Tolvaptan (TLV) is a selective vasopressin type 2 receptor antagonist, which has an active effect on patients with congestive heart failure especially combined with hyponatremia. "( Hypernatremia induced by low-dose Tolvaptan in a Patient with refractory heart failure: A case report.
Li, GS; Li, T, 2019)		2.24
"Tolvaptan is an orally administered, nonpeptide, selective arginine vasopressin V(2) receptor antagonist that increases free water clearance, thereby correcting and increasing the low serum sodium levels in patients of cirrhosis, where hyponatremai is am major encountered problem."( Efficacy and Safety of Oral Tolvaptan Therapy in Hospitalized Cirrhotic Patients with Hyponatremia.
Aggarwal, S; Garg, R; Kaur, K; Singh, N, 2018)		2.22
"Tolvaptan is an orally active antagonist of arginine vasopressin type 2 receptors in the collecting duct of the kidney that inhibits water reabsorption without substantially affecting the electrolyte balance."( Tolvaptan for the treatment of hyponatremia and hypervolemia in patients with congestive heart failure.
Hori, M, 2013)		2.55
"Tolvaptan is an effective diuretic for patients with CKD."( The effects of tolvaptan on patients with severe chronic kidney disease complicated by congestive heart failure.
Murasawa, T; Ohno, D; Otsuka, T; Sakai, Y; Sato, N; Tsuruoka, S, 2013)		1.46
"Tolvaptan is a highly selective and orally effective arginine vasopressin V2 receptor antagonist, and is potentially useful for the treatment of heart failure (HF) patients. "( Renoprotective effect of vasopressin v2 receptor antagonist tolvaptan in Dahl rats with end-stage heart failure.
Ishikawa, M; Ishimitsu, T; Kobayashi, N; Onoda, S; Sugiyama, F, 2013)		2.07
"Tolvaptan is a selective V2 -receptor antagonist used to treat hypervolemic and euvolemic hyponatremia. "( Population pharmacokinetics of tolvaptan in healthy subjects and patients with hyponatremia secondary to congestive heart failure or hepatic cirrhosis.
Mager, DE; Mallikaarjun, S; Shoaf, SE; Van Wart, SA, 2013)		2.12
"Tolvaptan is a vasopressin-2 receptor antagonist, and we hypothesized that adding tolvaptan to standard diuretic therapy would be more effective in ADHF patients with renal function impairment."( Clinical effectiveness of tolvaptan in patients with acute decompensated heart failure and renal failure: design and rationale of the AQUAMARINE study.
Fujii, H; Matsue, Y; Nagahori, W; Nishioka, T; Noda, M; Okishige, K; Onishi, Y; Ono, Y; Sakurada, H; Satoh, Y; Sugi, K; Suzuki, M; Takahashi, A; Tejima, T; Torii, S; Yamaguchi, S; Yoshida, K, 2014)		1.42
"Tolvaptan is an orally active, selective arginine vasopressin V2 receptor antagonist already in use for hyponatremia."( Review of tolvaptan for autosomal dominant polycystic kidney disease.
Baur, BP; Meaney, CJ, 2014)		1.53
"Tolvaptan is a selective vasopressin receptor antagonist (V2R) that increases free water excretion. "( Effect of vasopressin antagonism on renal handling of sodium and water and central and brachial blood pressure during inhibition of the nitric oxide system in healthy subjects.
Al Therwani, S; Bech, JN; Jensen, JM; Mose, FH; Pedersen, EB, 2014)		1.85
"Tolvaptan is a competitive vasopressin V2-receptor antagonist that inhibits water reabsorption in the renal collecting ducts. "( Liquid chromatography-tandem mass spectrometry method for determining tolvaptan and its nine metabolites in rat serum: application to a pharmacokinetic study.
Furukawa, M; Himeda, Y; Hirao, Y; Kawasome, C; Koga, T; Miyata, K; Takeuchi, K; Umehara, K, 2014)		2.08
"Tolvaptan is a competitive vasopressin V2-receptor antagonist that inhibits water reabsorption in the renal collecting ducts. "( Enantioselective analysis of tolvaptan in rat and dog sera by high-performance liquid chromatography and application to pharmacokinetic study.
Furukawa, M; Hirao, Y; Umehara, K; Yamasaki, Y, 2014)		2.14
"Tolvaptan is a promising aquaretic for the treatment of refractory ascites in patients with decompensated liver cirrhosis."( Clinical efficacy of tolvaptan for treatment of refractory ascites in liver cirrhosis patients.
Ding, HG; Dong, PL; Fan, CL; Li, B; Li, L; Li, P; Wang, SZ; Zhang, X; Zhao, WM; Zheng, JF, 2014)		2.16
"Tolvaptan is a new drug used for treating ascites induced by liver cirrhosis, and it is covered by health insurance in Japan. "( Re-response to tolvaptan after furosemide dose reduction in a patient with refractory ascites.
Goto, A; Matsumoto, M; Nakamura, M; Sakaida, I; Terai, S, 2015)		2.21
"Tolvaptan is a selective, oral vasopressin-V2-receptor-antagonist that inhibits ADH-induced retention of electrolyte-free water in the connecting duct of the kidney."( [Syndrome of inadequate ADH secretion: pitfalls in diagnosis and therapy].
Lindner, U; Schäffler, A, 2015)		1.14
"Tolvaptan (TLV) is a new vasopressin type 2 receptor antagonist effective in patients with heart failure (HF). "( Acute Renal Injury Induced by Hypersensitivity to Tolvaptan in an Elderly Patient with Congestive Heart Failure.
Asada, Y; Kitamura, K; Nishihira, K; Okubo, T; Yamaguchi, M, 2015)		2.11
"Tolvaptan (Jinarc(®)) is a highly selective vasopressin V2 receptor antagonist indicated for use in patients with autosomal dominant polycystic kidney disease (ADPKD). "( Tolvaptan: A Review in Autosomal Dominant Polycystic Kidney Disease.
Blair, HA; Keating, GM, 2015)		3.3
"Tolvaptan is an oral medication used to treat SIADH-related hyponatremia patients that needs to be initiated at hospital so patients can have their serum sodium monitored."( SIADH-related hyponatremia in hospital day care units: clinical experience and management with tolvaptan.
Camps Herrero, C; Carcereny, E; De Las Peñas, R; Escobar Álvarez, Y; Henao, F; López López, R; Ponce, S; Rodríguez, CA; Virizuela, JA, 2016)		1.37
"Tolvaptan is a vasopressin V(2)-receptor antagonist that has shown promise in treating Autosomal Dominant Polycystic Kidney Disease (ADPKD). "( Inhibition of Human Hepatic Bile Acid Transporters by Tolvaptan and Metabolites: Contributing Factors to Drug-Induced Liver Injury?
Brock, WJ; Brouwer, KL; Brouwer, KR; Freeman, KM; Lu, Y; Pan, M; Slizgi, JR; St Claire, RL, 2016)		2.13
"Tolvaptan is an oral vasopressin type 2 receptor antagonist that can be used for heart failure patients with hyponatremia or symptomatic congestion. "( Effects of tolvaptan on congestive heart failure complicated with chylothorax in a neonate.
Inukai, S; Ito, K; Kato, T; Nagasaki, R; Saitoh, S; Sato, N; Sugiura, T; Suzuki, K, 2015)		2.25
"Tolvaptan is an oral selective vasopressin-2 receptor antagonist used in patients irresponsive to loop diuretics."( Early introduction of tolvaptan after cardiac surgery: a renal sparing strategy in the light of the renal resistive index measured by ultrasound.
Amano, A; Kajimoto, K; Kato, TS; Kuwaki, K; Ono, S; Yamamoto, T, 2015)		1.45
"Tolvaptan is an oral antagonist of arginine vasopressin receptor 2 that has been approved in Japan to reduce congestive symptoms in patients with heart failure refractory to loop diuretics. "( Early use of V2 receptor antagonists is associated with a shorter hospital stay and reduction in in-hospital death in patients with decompensated heart failure.
Kubota, T; Matsukawa, R; Okabe, M; Yamamoto, Y, 2016)		1.88
"Tolvaptan is a selective vasopressin receptor 2 antagonist. "( Effect of tolvaptan on acute heart failure with hyponatremia--a randomized, double blind, controlled clinical trial.
Anjaneyan, K; Doss, CR; George, M; Jena, A; Kanagesh, B; Rajaram, M; Ramaraj, B; Shanmugam, E, 2016)		2.28
"Tolvaptan is a new selective vasopression V2-receptor antagonist. "( [Preoperative Use of Tolvaptan in a Patient with Constrictive Pericarditis].
Adachi, O; Akiyama, M; Fujiwara, H; Kanda, K; Katahira, S; Kawamoto, S; Kawatsu, S; Kumagai, K; Saiki, Y; Sakatsume, K; Suzuki, T; Takahara, S, 2016)		2.2
"Tolvaptan is a vasopressin receptor antagonist that has been effective in improving hyponatremia and congestive symptoms in adults with chronic heart failure."( Use of Tolvaptan in a Patient With Palliated Congenital Heart Disease.
Busovsky-McNeal, M; Chakravarti, S, 2018)		1.66
"Tolvaptan is a selective vasopressin V2 receptor antagonist, approved in several countries for the treatment of hyponatremia and autosomal dominant polycystic kidney disease (ADPKD). "( Application of a Mechanistic Model to Evaluate Putative Mechanisms of Tolvaptan Drug-Induced Liver Injury and Identify Patient Susceptibility Factors.
Brock, WJ; Brouwer, KL; Church, R; Grammatopoulos, TN; Howell, BA; Mosedale, M; Roth, SE; Shoaf, SE; Shoda, LK; Siler, SQ; Stiles, L; Watkins, PB; Woodhead, JL, 2017)		2.13
"Tolvaptan is a very effective treatment for hypervolemic or euvolemic hyponatremia. "( Comparison of tolvaptan treatment between patients with the SIADH and congestive heart failure: a single-center experience.
Jung, MC; Kim, HJ; Kim, JK; Kim, SG; Lee, CM; Park, GH; Song, JW; Song, YR, 2018)		2.28
"Tolvaptan is a selective vasopressin receptor antagonist. "( Effect of tolvaptan on renal water and sodium excretion and blood pressure during nitric oxide inhibition: a dose-response study in healthy subjects.
Al Therwani, S; Bech, JN; Mose, FH; Pedersen, EB; Rosenbæk, JB, 2017)		2.3
"Tolvaptan is a promising pharmacological tool in the treatment of renal edema."( Tolvaptan, a selective oral vasopressin V2 receptor antagonist, ameliorates podocyte injury in puromycin aminonucleoside nephrotic rats.
Hatamura, I; Kawachi, H; Muragaki, Y; Negi, S; Okada, T; Otani, H; Saji, F; Sakaguchi, T; Shigematsu, T, 2009)		2.52
"Tolvaptan is an orally administered, nonpeptide, selective arginine vasopressin V(2) receptor antagonist that increases free water clearance, thereby correcting low serum sodium levels. "( Tolvaptan.
Plosker, GL, 2010)		3.25
"Tolvaptan is a new selective nonpeptide vasopressin V2 receptor antagonist that has shown to rapidly normalize serum sodium concentrations in hyponatremic patients."( Tolvaptan for the treatment of hyponatremia and congestive heart failure.
Ferrer, E, 2010)		2.52
"Tolvaptan is an oral nonpeptide selective vasopressin V(2)-receptor antagonist indicated for the treatment of clinically relevant hypervolemic or euvolemic hyponatremia associated with heart failure, cirrhosis, or syndrome of inappropriate antidiuretic hormone."( Treatment of hypervolemic or euvolemic hyponatremia associated with heart failure, cirrhosis, or the syndrome of inappropriate antidiuretic hormone with tolvaptan: a clinical review.
Hutchinson, DJ; Nemerovski, C, 2010)		2
"Tolvaptan is a new agent in the treatment of normovolemic and hypervolemic hyponatremia. "( Tolvaptan: a new therapeutic agent.
Alivanis, P; Aperis, G, 2011)		3.25
"Tolvaptan is a selective antagonist of the antidiuretic effect of vasopressin without primarily affecting blood pressure and depending on the dose leads to increased excretion of free water (aquaresis)."( [Treatment of hyponatremia: role of vaptans].
Hensen, J, 2010)		1.08
"Tolvaptan is an oral nonpeptide V₂-selective antagonist and has been shown to induce free water excretion without increasing urine sodium, an effect termed 'aquaresis'."( Tolvaptan for the treatment of heart failure: a review of the literature.
Ambrosy, A; Gheorghiade, M; Goldsmith, SR, 2011)		2.53
"Tolvaptan is a selective vasopressin V2 receptor antagonist that can be given orally once daily for treatment of clinically significant hypervolemic and euvolemic hyponatremia (US and Europe) or extracellular volume expansion despite taking other diuretics (Japan). "( Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		2.07
"Tolvaptan is an orally active, selective V2-receptor antagonist that blocks the effects of arginine vasopressin in the renal collecting duct to promote aquaresis without increasing sodium or potassium excretion; as a result, it increases serum sodium in a controlled manner."( Hyponatremia in hospitalized patients: the potential role of tolvaptan.
Deitelzweig, SB; McCormick, L, 2011)		1.33
"As tolvaptan is a CYP3A4 substrate, knowing the effects of inhibition and induction on CYP3A4-mediated metabolism was important for dosing recommendations."( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		1.11
"Tolvaptan is a sensitive CYP3A4 substrate with no inhibitory activity. "( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		2.04
"Tolvaptan is a vasopressin V2-receptor antagonist that improves serum sodium concentration by increasing renal solute-free water excretion. "( Tolvaptan, an oral vasopressin antagonist, in the treatment of hyponatremia in cirrhosis.
Afdhal, NH; Cárdenas, A; Czerwiec, F; Ginès, P; Guevara, M; Marotta, P; Oyuang, J, 2012)		3.26
"Tolvaptan is a selective arginine vasopressin V2-receptor antagonist that is used as an aquaretic agent. "( Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men.
Cho, JY; Jang, IJ; Jeon, H; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2012)		2.08
"Tolvaptan is a selective vasopressin V2 receptor antagonist that can be given orally once daily for treatment of clinically significant hypervolemic and euvolemic hyponatremia (US) or cardiac edema (Japan). "( Absolute bioavailability of tolvaptan and determination of minimally effective concentrations in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		2.12
"Tolvaptan is a member of a new class of drugs, called the vaptans, that antagonize receptors of the neurohormone arginine vasopressin. "( Update on tolvaptan for the treatment of hyponatremia.
Cassidy, IB; Chiong, JR; Christian, R; Dasta, JF; Friend, K; Lin, J; Lingohr-Smith, M, 2012)		2.22
"Tolvaptan is a selective vasopressin V(2)-receptor antagonist mainly used for the treatment of hyponatremia. "( Development and validation of an LC-MS/MS method for the determination of tolvaptan in human plasma and its application to a pharmacokinetic study.
Guo, C; Huang, P; Li, Z; Liu, L; Luo, M; Pei, Q; Peng, X; Tan, H; Yang, G; Zhang, B; Zuo, X, 2013)		2.06
"Tolvaptan is an oral vasopressin V2-receptor antagonist recognized as effective for fluid retention associated with congestive heart failure and liver cirrhosis. "( Tolvaptan as an alternative treatment for refractory fluid retention associated with sinusoidal obstruction syndrome after allogeneic stem cell transplantation.
Inui, Y; Kakiuchi, S; Kawamori-Iwamoto, Y; Kurata, K; Matsuoka, H; Minami, H; Miyata, Y; Murayama, T; Okamura, A; Sanada, Y; Tomioka, H; Yakushijin, K; Yamamoto, K, 2013)		3.28
"Tolvaptan at 7.5 mg/day is a clinically useful option for treating patients who do not respond well to conventional diuretics."( The pharmacokinetics and pharmacodynamics of tolvaptan in patients with liver cirrhosis with insufficient response to conventional diuretics: a multicentre, double-blind, parallel-group, phase III study.
Kobayashi, Y; Okada, M; Okita, K; Sakaida, I; Yanase, M; Yasutake, T, 2012)		1.36
"Tolvaptan is an oral vasopressin (V 2 ) antagonist that decreases body weight and increases urine volume without inducing renal dysfunction or hypokalemia."( Rationale and design of the multicenter, randomized, double-blind, placebo-controlled study to evaluate the Efficacy of Vasopressin antagonism in Heart Failure: Outcome Study with Tolvaptan (EVEREST).
Burnett, JC; Demets, D; Gheorghiade, M; Grinfeld, L; Konstam, MA; Maggioni, A; Orlandi, C; Swedberg, K; Udelson, JE; Zannad, F; Zimmer, C, 2005)		1.24
"Tolvaptan is a vasopressin V2-receptor antagonist that functions as an aquaretic (ie, it increases urine volume and serum sodium with little or no sodium loss)."( Pharmacology of new agents for acute heart failure syndromes.
Gheorghiade, M; Mebazaa, A; Teerlink, JR, 2005)		1.05
"Tolvaptan (Otsuka) is an orally administered nonpeptide vasopressin (VP) V2 receptor antagonist that inhibits water reabsorption in the kidney by competitively blocking VP binding, resulting in water diuresis without significantly changing total electrolyte excretion."( Comparison of two doses and dosing regimens of tolvaptan in congestive heart failure.
Bramer, SL; Hauptman, PJ; Mallikaarjun, S; Orlandi, C; Shoaf, SE; Udelson, J; Zimmer, C, 2005)		1.31
"Tolvaptan is an orally effective nonpeptide arginine vasopressin (AVP) V(2)-receptor antagonist synthesized by Otsuka Pharmaceutical Co., Ltd. "( Tolvaptan, an orally active vasopressin V(2)-receptor antagonist - pharmacology and clinical trials.
Fujiki, H; Miyazaki, T; Mori, T; Nakamura, S; Yamamura, Y, 2007)		3.23

Effects

Tolvaptan (TLV) has an inhibiting effect for worsening renal function (WRF) in acute decompensated heart failure (HF) patients. It is associated with an increase in adverse events at high doses when compared with the placebo.

Tovaptan has been approved for the treatment of autosomal dominant polycystic kidney disease and heart failure. Tolvaptan is associated with an increase in adverse events at high doses when compared with the placebo.

ExcerptReferenceRelevance
"Tolvaptan has a beneficial effect on ADPKD, but is associated with an increase in adverse events at high doses when compared with the placebo. "( Effectiveness of Tolvaptan in the Treatment for Patients with Autosomal Dominant Polycystic Kidney Disease: A Meta-analysis.
Bai, DH; Cai, Q; Guo, XY; Lu, AM; Sheng, HZ; Wang, BK; Wang, XR; Xie, X; Yan, K, 2020)		2.34
"Tolvaptan (TLV) has an inhibiting effect for worsening renal function (WRF) in acute decompensated heart failure (HF) patients. "( Impact of Continuous Administration of Tolvaptan on Preventing Medium-Term Worsening Renal Function and Long-Term Adverse Events in Heart Failure Patients with Chronic Kidney Disease.
Amano, T; Ando, H; Mizuno, T; Mukai, K; Murotani, K; Nakano, Y; Niwa, T; Takashima, H; Wakabayashi, H; Waseda, K; Watanabe, A, 2018)		2.19
"Tolvaptan has been used satisfactorily for managing edema in patients with heart failure and cirrhosis."( Efficacy and Safety of Combination Therapy with Tolvaptan and Furosemide in Children with Nephrotic Syndrome and Refractory Edema: A Prospective Interventional Study.
Bagga, A; Hari, P; Meena, J; Sinha, A, 2022)		1.7
"Tolvaptan has been approved for the treatment of autosomal dominant polycystic kidney disease and heart failure. "( Tolvaptan reduces angiotensin II-induced experimental abdominal aortic aneurysm and dissection.
Chang, WH; Lu, HY; Shih, CC; Wu, TC, 2022)		3.61
"Tolvaptan has been approved for the management of cirrhosis-related complications according to the Japanese and Chinese practice guidelines, but not the European or American practice guidelines in view of FDA warning about its hepatotoxicity. "( Efficacy and safety of tolvaptan in cirrhotic patients: a systematic review and meta-analysis of randomized controlled trials.
Chai, L; Cheng, G; Li, Z; Pinyopornpanish, K; Qi, X; Wang, R; Wang, T, )		1.88
"Tolvaptan has a beneficial effect on ADPKD, but is associated with an increase in adverse events at high doses when compared with the placebo. "( Effectiveness of Tolvaptan in the Treatment for Patients with Autosomal Dominant Polycystic Kidney Disease: A Meta-analysis.
Bai, DH; Cai, Q; Guo, XY; Lu, AM; Sheng, HZ; Wang, BK; Wang, XR; Xie, X; Yan, K, 2020)		2.34
"Tolvaptan has advantageous effects for immediate body weight reduction in patients with positive postoperative water balance following cardiac surgery."( Advent of New perioperative care for fluid management after cardiovascular surgery: A review of current evidence.
Nishi, H, 2020)		1.28
"Tolvaptan also has the benefit of not stimulating the renin-angiotensin and sympathetic nervous systems, which are risk factors for postoperative paroxysmal atrial fibrillation."( Tolvaptan can limit postoperative paroxysmal atrial fibrillation occurrence after open-heart surgery.
Harada, S; Horie, H; Kishimoto, Y; Nakamura, Y; Nishimura, M; Onohara, T; Otsuki, Y, 2020)		2.72
"Tolvaptan introduction has constituted the main therapeutic novelty in the management of hyponatremia in recent years."( Clinical experience with Tolvaptan outpatient use. Cost and effectiveness in 9 cases.
Barajas-Galindo, DE; Gómez-Hoyos, E; Guerra-González, M; Vidal-Casariego, A, 2020)		2.3
"Tolvaptan (TOLV) has recently been approved in many European countries for its ability to slow disease progression in patients that are eligible for treatment."( [Tolvaptan in ADPKD: a turning point or an unsustainable therapy? One year of "real life" experience].
Amicone, M; Angelucci, V; Pisani, A; Riccio, E, 2020)		2.19
"Tolvaptan has been shown to improve congestion in heart failure patients. "( Differences in pharmacological property between combined therapy of the vasopressin V2-receptor antagonist tolvaptan plus furosemide and monotherapy of furosemide in patients with hospitalized heart failure.
Amitani, K; Iha, H; Imura, H; Ishihara, S; Ishikawa, M; Ishizuka, A; Ito, Y; Kikuchi, A; Kobayashi, N; Maruyama, Y; Mitsuishi, T; Nakama, K; Nakamura, S; Nohara, T; Ohkuma, S; Omote, T; Sato, N; Shigihara, S; Shimizu, W; Sone, M; Takagi, K; Takahashi, N; Tokuyama, H; Yamamoto, E, 2020)		2.21
"Tolvaptan has been used for treating water retention associated with cirrhosis."( Durable response without recurrence to Tolvaptan improves long-term survival.
Kawagishi, N; Kitagataya, T; Kubo, A; Morikawa, K; Nakai, M; Nakamura, A; Ogawa, K; Ohara, M; Sakamoto, N; Shigesawa, T; Sho, T; Suda, G; Suzuki, K; Tokuchi, Y; Umemura, M; Yamada, R, 2020)		1.55
"Tolvaptan has been approved to slow disease progression in patients at risk of rapidly progressive disease."( Assessing Risk of Rapid Progression in Autosomal Dominant Polycystic Kidney Disease and Special Considerations for Disease-Modifying Therapy.
Chebib, FT; Torres, VE, 2021)		1.34
"Tolvaptan has been gradually spread to use as a potent diuretic for congestive heart failure in the limited country. "( Good response to tolvaptan shortens hospitalization in patients with congestive heart failure.
Hagiwara, N; Hamada, K; Jujo, K; Kogure, T; Saito, K, 2018)		2.26
"Tolvaptan (TLV) has an inhibiting effect for worsening renal function (WRF) in acute decompensated heart failure (HF) patients. "( Impact of Continuous Administration of Tolvaptan on Preventing Medium-Term Worsening Renal Function and Long-Term Adverse Events in Heart Failure Patients with Chronic Kidney Disease.
Amano, T; Ando, H; Mizuno, T; Mukai, K; Murotani, K; Nakano, Y; Niwa, T; Takashima, H; Wakabayashi, H; Waseda, K; Watanabe, A, 2018)		2.19
"Tolvaptan has been approved in Japan for the treatment of hepatic edema. "( Predictive factors of the pharmacological action of tolvaptan in patients with liver cirrhosis: a post hoc analysis.
Nakajima, K; Sakaida, I; Shibasaki, Y; Tachikawa, S; Terai, S; Tsubouchi, H, 2017)		2.15
"Tolvaptan has been proven efficient, and we believe it should be incorporated with the classical method, ECUM."( Efficacy of extracorporeal ultrafiltration in patients with diuretic-resistant heart failure.
Nakabayashi, K; Nakazawa, N; Oka, T, 2016)		1.16
"Tolvaptan has been recently approved for the treatment of hyponatremia and a marketing authorization application has been filed for the treatment of CHF."( Tolvaptan for the treatment of hyponatremia and congestive heart failure.
Ferrer, E, 2010)		2.52
"Tolvaptan has recently emerged as a promising new therapeutic option for SIADH."( [A case of venlafaxine-induced syndrome of inappropriate ADH secretion (SIADH) - treatment with tolvaptan].
Frank, D; Janssens, U; Meyer, I, 2012)		1.32
"Oral tolvaptan has been shown to be an effective and potent aquaretic to treat hyponatremia caused by SIADH as evidenced by a simultaneous increase in serum sodium and a decrease in urine osmolality."( [Hyponatremia : The water-intolerant patient].
Hensen, J, 2012)		0.83
"Tolvaptan has been shown to reduce body weight in patients with worsening heart failure without inducing renal dysfunction or causing hypokalemia. "( Rationale and design of the multicenter, randomized, double-blind, placebo-controlled study to evaluate the Efficacy of Vasopressin antagonism in Heart Failure: Outcome Study with Tolvaptan (EVEREST).
Burnett, JC; Demets, D; Gheorghiade, M; Grinfeld, L; Konstam, MA; Maggioni, A; Orlandi, C; Swedberg, K; Udelson, JE; Zannad, F; Zimmer, C, 2005)		1.96

Actions

Tovaptan slows the increase in total kidney volume in patients aged 18-24 years with ADPKD. Tolvaptan may allow for less intensification of loop diuretic therapy and a lower incidence of worsening renal function during decongestion.

ExcerptReferenceRelevance
"The tolvaptan group had a lower mean percentage of TKV growth per year compared to the placebo group (3.9% vs."( Autosomal-dominant polycystic kidney disease: tolvaptan use in adolescents and young adults with rapid progression.
Chakraborty, R; DeCoy, ME; Kline, T; Raina, R, 2021)		1.36
"Tolvaptan slows the increase in total kidney volume in patients aged 18-24 years with ADPKD. "( Autosomal-dominant polycystic kidney disease: tolvaptan use in adolescents and young adults with rapid progression.
Chakraborty, R; DeCoy, ME; Kline, T; Raina, R, 2021)		2.32
"Tolvaptan (TLV) promotes aquaresis; however, little is known about its effect on solute excretion in chronic kidney disease (CKD)."( Tolvaptan promotes urinary excretion of sodium and urea: a retrospective cohort study.
Hamano, T; Isaka, Y; Iwatani, H; Kimura, Y; Minami, S; Mizui, M, 2018)		3.37
"Tolvaptan delays the increase in total kidney volume (surrogate marker for disease progression), slows the decline in renal function, and reduces kidney pain."( Review of tolvaptan for autosomal dominant polycystic kidney disease.
Baur, BP; Meaney, CJ, 2014)		1.53
"Tolvaptan was found to cause DNA damage, as assessed by alkaline comet assays; this was confirmed by increased levels of 8-oxoguanine and phosphorylation of histone H2AX."( Mechanisms of tolvaptan-induced toxicity in HepG2 cells.
Beland, FA; Chen, S; Fang, JL; Guo, L; Liu, F; Wu, Y, 2015)		1.5
"Tolvaptan may allow for less intensification of loop diuretic therapy and a lower incidence of worsening renal function during decongestion."( Tolvaptan in Patients Hospitalized With Acute Heart Failure: Rationale and Design of the TACTICS and the SECRET of CHF Trials.
Adams, KF; Cole, RT; Egnaczyk, GF; Felker, GM; Fiuzat, M; Gregory, D; Konstam, MA; Mentz, RJ; O'Connor, CM; Patel, CB; Udelson, JE; Wedge, P, 2015)		2.58
"Tolvaptan tended to increase plasma arginine vasopressin concentrations but did not affect plasma renin activity."( Effects of tolvaptan on systemic and renal hemodynamic function in dogs with congestive heart failure.
Fujiki, H; Nakamura, S; Nakayama, S; Onogawa, T; Sakamoto, Y; Yamamura, Y, 2011)		1.48
"Tolvaptan did not cause any target organ toxicity in rats after treatment for 26 weeks or in dogs after treatment for 52 weeks at oral doses of up to 1,000 mg/kg/day."( Nonclinical safety profile of tolvaptan.
Awogi, T; Fujita, S; Hosoki, E; Ishiharada, N; Ishiyama, H; Ito, N; Miyatake, M; Morimoto, H; Morishita, K; Nakagiri, N; Oi, A; Ozaki, A; Senba, T; Shiragiku, T; Uesugi, T; Umezato, M, 2011)		1.38

Treatment

Tolvaptan-treated ADPKD patients have reduced OxSt, which might contribute to slowing down the loss of renal function. In tolvaptan treatment combined with standard therapy in ADHF patients, serum potassium level ≤ 3.8mEq/L may be a determinant factor for hypernatremia development.

ExcerptReferenceRelevance
"Mean tolvaptan treatment duration was 139.4 days, median 18.5 (range 1-1130) days; most frequent dose was 15 mg/day (used in 75% of patients)."( Using Tolvaptan to Treat Hyponatremia: Results from a Post-authorization Pharmacovigilance Study.
Estilo, A; McCormick, L; Rahman, M, 2021)		1.56
"Tolvaptan-treated ADPKD patients have reduced OxSt, which might contribute to slowing down the loss of renal function."( [Reduced oxidative stress in ADPKD patients treated with tolvaptan].
Bertoldi, G; Calò, LA; Carraro, G; Cirella, I; Di Vico, V; Dian, S; Ravarotto, V; Rigato, M, 2022)		1.69
"In tolvaptan treatment combined with standard therapy in ADHF patients, serum potassium level ≤ 3.8 mEq/L may be a determinant factor for hypernatremia development. "( Tolvaptan-induced hypernatremia related to low serum potassium level accompanying high blood pressure in patients with acute decompensated heart failure.
Fukuoka, H; Hoshida, S; Inoue, S; Inui, H; Minamisaka, T; Mine, K; Shinoda, Y; Tachibana, K; Ueda, K; Ueno, K, 2020)		2.62
"Tolvaptan treatment at 7.5 mg per day might be a good therapeutic choice for Chinese cirrhotic patients with ascites who did not achieve satisfactory clinical responses to previous treatment regimens with combination therapy with an aldosterone antagonist and an orally administered loop diuretic."( Tolvaptan therapy of Chinese cirrhotic patients with ascites after insufficient diuretic routine medication responses: a phase III clinical trial.
Chen, C; Chen, Y; Cheng, J; Ding, H; Gao, Y; Han, T; Ji, F; Jia, J; Jiang, X; Lv, N; Mao, Q; Mao, Y; Niu, J; Shang, J; Tang, J; Wang, Y; Wang, Z; Wei, Z; Zeng, M; Zhang, Q, 2020)		3.44
"Tolvaptan-treated patients were stratified into the responder group (n = 37), defined as tolvaptan-treated patients with a net decrease in TKV from baseline to year 3, and the non-responder group (n = 55), defined as tolvaptan-treated patients with a net increase in TKV."( Preservation of kidney function irrelevant of total kidney volume growth rate with tolvaptan treatment in patients with autosomal dominant polycystic kidney disease.
Horie, S; Ibuki, T; Kawano, H; Muto, S; Nakajima, K; Okada, T; Shibasaki, Y, 2021)		1.57
"Tolvaptan treatment effectiveness to reduce TKV growth was similar in all three risk categories."( Can we further enrich autosomal dominant polycystic kidney disease clinical trials for rapidly progressive patients? Application of the PROPKD score in the TEMPO trial.
Blais, JD; Chapman, AB; Cornec-Le Gall, E; Czerwiec, FS; Devuyst, O; Gansevoort, RT; Harris, PC; Heyer, CM; Irazabal, MV; Le Meur, Y; Ouyang, J; Perrone, RD; Senum, SR; Torres, VE, 2018)		1.2
"The tolvaptan-treated rats were divided into two groups: a low-dose group (0.01% tolvaptan diet; Low-Tol) and a high-dose group (0.05% tolvaptan diet; High-Tol)."( Renoprotective effects of tolvaptan in hypertensive heart failure rats depend on renal decongestion.
Aonuma, K; Chiba, H; Ishizu, T; Namekawa, M; Sai, S; Seo, Y, 2019)		1.29
"Tolvaptan treatment for 3 weeks."( Determinants of Urine Volume in ADPKD Patients Using the Vasopressin V2 Receptor Antagonist Tolvaptan.
Boertien, WE; Gansevoort, RT; Kramers, BJ; Meijer, E; van Gastel, MDA, 2019)		2.18
"In tolvaptan-treated subjects, copeptin increased from baseline to week 3 (6.3 pmol/L versus 21.9 pmol/L, respectively)."( Plasma copeptin levels predict disease progression and tolvaptan efficacy in autosomal dominant polycystic kidney disease.
Blais, JD; Chapman, AB; Czerwiec, FS; Devuyst, O; Gansevoort, RT; Higashihara, E; Lee, J; Ouyang, J; Perrone, RD; Stade, K; Torres, VE; van Gastel, MDA, 2019)		1.28
"With tolvaptan treatment, patient urine output increased dramatically to approximately 5.5 L/day and body weight decreased by 9 kg over 5 days."( Is tolvaptan indicated for refractory oedema in nephrotic syndrome?
Huh, YS; Kim, GH; Park, ES, 2015)		1.49
"Tolvaptan treatment led to delayed cell cycle progression, accompanied by decreased levels of several cyclins and cyclin-dependent kinases."( Mechanisms of tolvaptan-induced toxicity in HepG2 cells.
Beland, FA; Chen, S; Fang, JL; Guo, L; Liu, F; Wu, Y, 2015)		1.5
"Tolvaptan treatment could prevent RAAS activation in chronic heart failure patients."( Response Prediction and Influence of Tolvaptan in Chronic Heart Failure Patients Considering the Interaction of the Renin-Angiotensin-Aldosterone System and Arginine Vasopressin.
Akaike, M; Bando, M; Bando, S; Hara, T; Ise, T; Iwase, T; Kadota, M; Kawabata, Y; Matsuura, T; Ogasawara, K; Sata, M; Soeki, T; Ueno, R; Wakatsuki, T; Yagi, S; Yamada, H; Yamaguchi, K, 2016)		1.43
"Tolvaptan treatment also resulted in increased incidences of adverse events compared with control treatment (RR = 1.05, 95 % CI 1.02-1.07, Z = 3.83, P < 0.001)."( The Efficacy and Safety of Tolvaptan in Patients with Hyponatremia: A Meta-Analysis of Randomized Controlled Trials.
Fang, D; Feng, H; Li, B; Qian, C; Wang, Y, 2017)		1.47
"In tolvaptan-treated rats, nephrin and podocin expressions retained their normal linear pattern."( Tolvaptan, a selective oral vasopressin V2 receptor antagonist, ameliorates podocyte injury in puromycin aminonucleoside nephrotic rats.
Hatamura, I; Kawachi, H; Muragaki, Y; Negi, S; Okada, T; Otani, H; Saji, F; Sakaguchi, T; Shigematsu, T, 2009)		2.31
"Tolvaptan treatment increases serum sodium via aquaresis-ie, increased electrolyte-free water excretion-and thus presents an advantage in patients with syndrome of inappropriate secretion of antidiuretic hormone or other euvolemic states or hypervolemic hyponatremia."( Hyponatremia in critical care patients: frequency, outcome, characteristics, and treatment with the vasopressin V2-receptor antagonist tolvaptan.
Cirulli, J; Friedman, B, 2013)		1.31
"The tolvaptan-treated groups were found to have lower levels of left ventricular end-diastolic and systolic cardiac volumes than the vehicle group did."( Tolvaptan improves left ventricular dysfunction after myocardial infarction in rats.
Fujiki, H; Hanatani, A; Iwao, H; Izumi, Y; Nakamura, Y; Osada-Oka, M; Shimada, K; Shiota, M; Yamashita, N; Yamazaki, T; Yoshiyama, M, 2012)		2.3
"Tolvaptan treatment increased AVP levels during follow-up, but this incremental increase was not associated with worsened outcomes."( Association of arginine vasopressin levels with outcomes and the effect of V2 blockade in patients hospitalized for heart failure with reduced ejection fraction: insights from the EVEREST trial.
Ambrosy, AP; Fought, AJ; Gheorghiade, M; Goldsmith, SR; Greene, SJ; Konstam, MA; Kwasny, MJ; Lanfear, DE; Maggioni, AP; Sabbah, HN; Swedberg, K; Yancy, CW; Zannad, F, 2013)		1.11
"Treatment with tolvaptan is a consolidate option which slows renal deterioration rate, although the molecular mechanisms involved are not fully clarified."( [Reduced oxidative stress in ADPKD patients treated with tolvaptan].
Bertoldi, G; Calò, LA; Carraro, G; Cirella, I; Di Vico, V; Dian, S; Ravarotto, V; Rigato, M, 2022)		1.31
"When treated with tolvaptan, the model cohort was predicted to experience a 3.1-year delay of ESRD (95% confidence interval: 1.8 to 4.4), approximately a 23% improvement over the estimated 13.7 years for patients not receiving tolvaptan. "( A disease progression model estimating the benefit of tolvaptan on time to end-stage renal disease for patients with rapidly progressing autosomal dominant polycystic kidney disease.
Barnett, CL; Mader, G; Mladsi, D; Oberdhan, D; Purser, M; Sanon, M; Seliger, S; Watnick, T, 2022)		1.3
"A treatment by tolvaptan is currently used in adults to decelerate PKD progression."( [Autosomal dominant polycystic kidney disease : a pediatric perspective].
Collard, L; Dachy, A; Ghuysen, MS; Jouret, F; Krzesinski, JM; Mekahli, D; Seghaye, MC, 2020)		0.9
"Treatment with tolvaptan may have beneficial effects on slowing of renal function decline even in patients who have not experienced a reduction in the rate of TKV growth by treatment with tolvaptan."( Preservation of kidney function irrelevant of total kidney volume growth rate with tolvaptan treatment in patients with autosomal dominant polycystic kidney disease.
Horie, S; Ibuki, T; Kawano, H; Muto, S; Nakajima, K; Okada, T; Shibasaki, Y, 2021)		1.19
"Treatment with tolvaptan attenuated CIH-induced atrial fibrosis, reduced AF inducibility, expression levels of miR-21 and its downstream factors were also improved."( Beneficial effects of tolvaptan on atrial remodeling induced by chronic intermittent hypoxia in rats.
Li, G; Liu, R; Ma, Z; Wang, W; Yuan, M; Zhang, K; Zhang, Y, 2018)		1.14
"Treatment with tolvaptan corrected the patient's dilutional hyponatremia."( Prompt efficacy of tolvaptan in treating hyponatremia of syndrome of inappropriate secretion of antidiuretic hormone (SIADH) closely associated with rupture of a gastric artery aneurysm.
Aoki, A; Asano, T; Ikoma, A; Ishikawa, SE; Kakei, M; Kusaka, I; Yamada, H; Yamashita, T; Yoshida, M, 2014)		1.07
"Treatment with tolvaptan or pasireotide alone markedly reduced cyst progression and in combination showed a clear additive effect."( Tolvaptan plus pasireotide shows enhanced efficacy in a PKD1 model.
Harris, PC; Hommerding, CJ; Hopp, K; Torres, VE; Wang, X; Ye, H, 2015)		2.2
"Treatment with tolvaptan can often result in a rapid and controlled improvement of the symptoms."( [Syndrome of inadequate ADH secretion: pitfalls in diagnosis and therapy].
Lindner, U; Schäffler, A, 2015)		0.76
"Treatment with tolvaptan increased the urine volume, improved the dyspnea and decreased the edema."( Acute Renal Injury Induced by Hypersensitivity to Tolvaptan in an Elderly Patient with Congestive Heart Failure.
Asada, Y; Kitamura, K; Nishihira, K; Okubo, T; Yamaguchi, M, 2015)		1.01

Toxicity

Tolvaptan had no adverse effects on the central nervous, somatic nervous, autonomic nervous, smooth muscle, respiratory and cardiovascular, or digestive systems. No overcorrection of serum sodium was noted in the tolvaptan group. The main adverse events noted were dry mouth, polydipsia, and polyuria.

ExcerptReferenceRelevance
" The most frequent adverse events--excess thirst, frequent urination, and dry mouth--appeared to be related to the pharmacological action of tolvaptan."( Pharmacokinetics, pharmacodynamics, and safety of tolvaptan, a nonpeptide AVP antagonist, during ascending single-dose studies in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE; Wang, Z, 2007)		0.79
" The most common adverse effects attributed to tolvaptan were pollakiuria, thirst, fatigue, dry mouth, polydipsia, and polyuria."( Oral tolvaptan is safe and effective in chronic hyponatremia.
Berl, T; Bichet, DG; Czerwiec, FS; Ouyang, J; Quittnat-Pelletier, F; Schrier, RW; Verbalis, JG, 2010)		1.13
" Blockade of vasopressin V2 receptor is hypothesized to inhibit cyst growth, thereby delaying additional adverse clinical outcomes."( Rationale and design of the TEMPO (Tolvaptan Efficacy and Safety in Management of Autosomal Dominant Polycystic Kidney Disease and its Outcomes) 3-4 Study.
Bae, KT; Chapman, AB; Czerwiec, FS; Devuyst, O; Gansevoort, RT; Grantham, JJ; Higashihara, E; Krasa, HB; Meijer, E; Ouyang, JJ; Perrone, RD; Torres, VE, 2011)		0.65
" The most common adverse event was mild thirst."( Pharmacokinetics, pharmacodynamics and safety of tolvaptan, a novel, oral, selective nonpeptide AVP V2-receptor antagonist: results of single- and multiple-dose studies in healthy Japanese male volunteers.
Azuma, J; Hasunuma, T; Kim, SR; Kondo, M; Okada, T; Sato, O, 2011)		0.62
" The safety profile of tolvaptan was considered acceptable for clinical use with minimal adverse effects."( Efficacy and safety of tolvaptan in heart failure patients with volume overload despite the standard treatment with conventional diuretics: a phase III, randomized, double-blind, placebo-controlled study (QUEST study).
Fukunami, M; Hori, M; Izumi, T; Matsuzaki, M, 2011)		0.99
" Neither tolvaptan increased the incidence of severe or serious adverse events when administered for 7-14 days."( Efficacy and safety of tolvaptan in heart failure patients with sustained volume overload despite the use of conventional diuretics: a phase III open-label study.
Fukunami, M; Hori, M; Izumi, T; Matsuzaki, M, 2011)		1.1
"In safety pharmacological studies, tolvaptan had no adverse effects on the central nervous, somatic nervous, autonomic nervous, smooth muscle, respiratory and cardiovascular, or digestive systems."( Nonclinical safety profile of tolvaptan.
Awogi, T; Fujita, S; Hosoki, E; Ishiharada, N; Ishiyama, H; Ito, N; Miyatake, M; Morimoto, H; Morishita, K; Nakagiri, N; Oi, A; Ozaki, A; Senba, T; Shiragiku, T; Uesugi, T; Umezato, M, 2011)		0.93
"Nonclinical toxicity that precludes the safe administration of tolvaptan to humans was not observed."( Nonclinical safety profile of tolvaptan.
Awogi, T; Fujita, S; Hosoki, E; Ishiharada, N; Ishiyama, H; Ito, N; Miyatake, M; Morimoto, H; Morishita, K; Nakagiri, N; Oi, A; Ozaki, A; Senba, T; Shiragiku, T; Uesugi, T; Umezato, M, 2011)		0.9
" Patients' weight, urine volume, sign of heart failure, heart function, blood pressure, heart rate, and all adverse events were observed."( [The efficacy and safety of tolvaptan on treating heart failure patients with hyponatremia].
Bai, H; Li, L; Zhu, WL, 2011)		0.66
" There were more drug related adverse events of thirst (11."( [The efficacy and safety of tolvaptan on treating heart failure patients with hyponatremia].
Bai, H; Li, L; Zhu, WL, 2011)		0.66
" Tolvaptan related serious adverse event was low and could be well tolerated by patients tested in this cohort."( [The efficacy and safety of tolvaptan on treating heart failure patients with hyponatremia].
Bai, H; Li, L; Zhu, WL, 2011)		1.57
" Two serious adverse events were observed."( Efficacy and safety of a 14-day administration of tolvaptan in the treatment of patients with ascites in hepatic oedema.
Kobayashi, T; Komatsu, M; Komorizono, Y; Okada, M; Okita, K; Sakai, T; Sakaida, I; Yamashita, S, 2013)		0.64
" Loop diuretics are commonly used in heart failure (HF) patients, but they are sometimes associated with insufficient response as well as adverse events."( Efficacy and safety of tolvaptan in heart failure patients with volume overload.
Inomata, T; Iwatake, N; Kinugawa, K; Mizuguchi, K; Sato, N; Shimakawa, T, 2014)		0.71
" Adverse drug reactions (ADR) were observed in 18."( Efficacy and safety of tolvaptan in heart failure patients with volume overload.
Inomata, T; Iwatake, N; Kinugawa, K; Mizuguchi, K; Sato, N; Shimakawa, T, 2014)		0.71
" No overcorrection of serum sodium (>12 mmol/L per day) was noted in the tolvaptan group, and the main adverse events noted were dry mouth, polydipsia, and polyuria, leading to 13% study withdrawal."( Tolvaptan in hospitalized cancer patients with hyponatremia: a double-blind, randomized, placebo-controlled clinical trial on efficacy and safety.
Ali, N; George, M; Lahoti, A; Palla, S; Salahudeen, AK, 2014)		2.08
" The most common adverse events occurring in the tolvaptan group were dry mouth and thirst."( Randomized, double blinded, placebo-controlled trial to evaluate the efficacy and safety of tolvaptan in Chinese patients with hyponatremia caused by SIADH.
Chen, S; Gu, F; Guo, XH; Liu, ZM; Ma, JH; Qiu, MC; Tong, NW; Yang, GY; Zhang, ZW; Zhao, JJ, 2014)		0.88
" We present a case of SIADH, heralding small cell lung cancer and persisting after apparent complete remission of primary tumor following chemotherapy/radiotherapy, in a patient who underwent long-term treatment with tolvaptan without any serious adverse effects."( Efficacy and safety of long-term tolvaptan treatment in a patient with SCLC and SIADH.
Ardizzoni, A; Bordi, P; Buti, S; Regolisti, G; Tiseo, M, 2015)		0.88
" Coadministration of tolvaptan, a selective vasopressin V2 receptor antagonist, can ameliorate such adverse events by reducing the required dose of loop diuretics; however, the safety of tolvaptan in patients with reduced renal function is not known."( Safety of add-on tolvaptan in patients with furosemide-resistant congestive heart failure complicated by advanced chronic kidney disease: a sub-analysis of a pharmacokinetics/ pharmacodynamics study.
Akashi, YJ; Kida, K; Kimura, K; Matsumoto, N; Miyake, F; Shibagaki, Y; Tominaga, N, 2015)		1.08
"In this short-term pilot study, coadministration of tolvaptan and furosemide appears to be safe in patients with heart failure and CKD."( Safety of add-on tolvaptan in patients with furosemide-resistant congestive heart failure complicated by advanced chronic kidney disease: a sub-analysis of a pharmacokinetics/ pharmacodynamics study.
Akashi, YJ; Kida, K; Kimura, K; Matsumoto, N; Miyake, F; Shibagaki, Y; Tominaga, N, 2015)		1.01
" However, it has not been fully clarified whether tolvaptan is also effective and safe for pediatric patients as well as adult."( Efficacy and safety of tolvaptan for pediatric patients with congestive heart failure. Multicenter survey in the working group of the Japanese Society of PEdiatric Circulation and Hemodynamics (J-SPECH).
Higashi, K; Honda, T; Ishikawa, S; Ishikawa, Y; Itoi, T; Kodama, Y; Masutani, S; Murakami, T; Ohuchi, H; Senzaki, H; Yamazawa, H, 2016)		1
" Adverse drug reactions were observed in 7 patients (20."( Efficacy and safety of tolvaptan for pediatric patients with congestive heart failure. Multicenter survey in the working group of the Japanese Society of PEdiatric Circulation and Hemodynamics (J-SPECH).
Higashi, K; Honda, T; Ishikawa, S; Ishikawa, Y; Itoi, T; Kodama, Y; Masutani, S; Murakami, T; Ohuchi, H; Senzaki, H; Yamazawa, H, 2016)		0.74
" No fatal adverse events were observed following tolvaptan administration."( A Safety and Efficacy Study of Tolvaptan Following Open Heart Surgery in 109 Cases.
Hori, H; Kono, T; Tanaka, H; Tayama, E; Ueda, T; Yamaki, Y, 2016)		0.97
" Tolvaptan treatment also resulted in increased incidences of adverse events compared with control treatment (RR = 1."( The Efficacy and Safety of Tolvaptan in Patients with Hyponatremia: A Meta-Analysis of Randomized Controlled Trials.
Fang, D; Feng, H; Li, B; Qian, C; Wang, Y, 2017)		1.66
"The results of this meta-analysis suggest that tolvaptan can increase serum sodium concentrations, serum sodium correction rates, 24-h urine output, net fluid balance, and total adverse event rates without significantly decreasing all-cause mortality rates or increasing serious adverse event rates in patients with hyponatremia."( The Efficacy and Safety of Tolvaptan in Patients with Hyponatremia: A Meta-Analysis of Randomized Controlled Trials.
Fang, D; Feng, H; Li, B; Qian, C; Wang, Y, 2017)		1.01
" Adverse events occurred in 46-47% of patients in both groups, and tolvaptan was not associated with worsened liver function."( Utility and safety of tolvaptan in cirrhotic patients with hyponatremia: A prospective cohort study.
Ding, HG; Gao, YQ; Ge, Y; Guo, H; Jia, JD; Li, CZ; Li, Y; Lu, W; Mao, H; Mao, Y; Wang, B; Wang, GQ; Wang, JF; Wang, X; Wong, VW; Xie, W; Zhang, Q, )		0.68
"In conclusion, short-term tolvaptan treatment is safe and can improve serum sodium level in cirrhotic patients with hyponatremia."( Utility and safety of tolvaptan in cirrhotic patients with hyponatremia: A prospective cohort study.
Ding, HG; Gao, YQ; Ge, Y; Guo, H; Jia, JD; Li, CZ; Li, Y; Lu, W; Mao, H; Mao, Y; Wang, B; Wang, GQ; Wang, JF; Wang, X; Wong, VW; Xie, W; Zhang, Q, )		0.75
" Information collected during the study included eGFR, survey scores (PKD history and outcome), adverse events, vital signs, hematology, urinalysis, and serum chemistry tests."( Rationale and Design of a Clinical Trial Investigating Tolvaptan Safety and Efficacy in Autosomal Dominant Polycystic Kidney Disease.
Blais, JD; Chapman, AB; Czerwiec, FS; Devuyst, O; Gansevoort, RT; Ouyang, J; Perrone, RD; Sergeyeva, O; Torres, VE, 2017)		0.7
"Tolvaptan appears to be effective and safe for management of postoperative fluid retention after congenital heart surgery."( Safety and effectiveness of tolvaptan for fluid management after pediatric cardiovascular surgery.
Fujii, T; Katayama, Y; Masuhara, H; Ozawa, T; Shiono, N; Watanabe, Y, 2017)		2.19
"In patients with HF and CKD, long-term administration of tolvaptan was well-tolerated, relatively safe and effective, suggesting its utility for long-term management of these conditions."( Safety and Efficacy of Long-Term Use of Tolvaptan in Patients With Heart Failure and Chronic Kidney Disease.
Imai, R; Ishikawa, S; Koyasu, M; Murohara, T; Ozaki, Y; Shibata, R; Takemoto, K; Teraoka, T; Uchikawa, T; Uemura, Y; Watanabe, T; Watarai, M, 2017)		0.97
" Adverse effects were the secondary outcomes."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		0.75
" Compared with placebo, tolvaptan of different dosage showed a non-significant higher risk of adverse effects."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		1.06
"These findings suggest that tolvaptan 30 mg and 45 mg may be the optimum dosage for CHF patients, because of its ability to provide favourable clinical results without greater adverse effects."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		1.05
"3 mg/dL, at 6 months after discharge and adverse events rate, were evaluated."( Impact of Continuous Administration of Tolvaptan on Preventing Medium-Term Worsening Renal Function and Long-Term Adverse Events in Heart Failure Patients with Chronic Kidney Disease.
Amano, T; Ando, H; Mizuno, T; Mukai, K; Murotani, K; Nakano, Y; Niwa, T; Takashima, H; Wakabayashi, H; Waseda, K; Watanabe, A, 2018)		0.75
"The result indicated a significant improvement in the serum sodium levels and no serious adverse effects after long-term use in very elderly patients."( Long-term low-dose tolvaptan treatment in hospitalized male patients aged >90 years with hyponatremia: Report on safety and effectiveness.
Fei, YH; Han, XB; Liu, YH; Xu, HT, 2017)		0.78
" No serious adverse events were reported, but in 13% of patients hyponatremia was overcorrected."( Safety and Efficacy of Tolvaptan in Korean Patients with Hyponatremia Caused by the Syndrome of Inappropriate Antidiuretic Hormone.
Choi, HY; Ha, SK; Han, SW; Jeong, KH; Kang, KP; Kim, GH; Kim, HJ; Kim, HY; Kim, SW; Kim, YW; Shin, SK; Yi, JH, 2018)		0.79
"The concomitant use of TLV and conventional diuretics is safe and effective for fluid management after TAR using cardiopulmonary bypass, selective cerebral perfusion, and hypothermic circulatory arrest."( Safety and Effectiveness of Tolvaptan Administration after Total Arch Replacement.
Iida, Y; Shimizu, H; Yoshitake, A, 2019)		0.81
"Tolvaptan exerts, a strong diuretic effect compared with conventional diuretics (furosemide and spironolactone) during the postoperative period after an operation using cardiopulmonary bypass without adverse effects on electrolyte balance and renal function."( Efficacy and Safety Evaluation of Tolvaptan on Management of Fluid Balance after Cardiovascular Surgery Using Cardiopulmonary Bypass.
Hirai, H; Hosono, M; Kaku, D; Kubota, Y; Nakahira, A; Sasaki, Y; Shibata, T; Suehiro, S; Suehiro, Y, 2016)		2.16
" The primary endpoints were adverse clinical events (death, worsening heart failure, worsening renal failure, fatal arrhythmia, cardiogenic or hypovolemic shock, and use of inotropic agents) and the volume of urine within 48 h of tolvaptan administration."( Clinical safety and efficacy of tolvaptan for acute phase therapy in patients with low-flow and normal-flow severe aortic stenosis.
Hioki, H; Kataoka, A; Kawashima, H; Kozuma, K; Mitsui, M; Nagura, F; Nakashima, M; Nara, Y; Watanabe, Y; Yokoyama, N, 2019)		0.98
" Adverse drug reactions monitored to assess safety."( Efficacy and Safety of Oral Tolvaptan Therapy in Hospitalized Cirrhotic Patients with Hyponatremia.
Aggarwal, S; Garg, R; Kaur, K; Singh, N, 2018)		0.77
" In conclusion, short-term use of tolvaptan following LVAD implantation is a safe and effective therapy to augment diuresis and improve hyponatremia."( Short-Term Efficacy and Safety of Tolvaptan in Patients with Left Ventricular Assist Devices.
Chung, B; Fujino, T; Imamura, T; Jeevanandam, V; Kalantari, S; Kim, G; LaBuhn, C; Narang, N; Nguyen, A; Nitta, D; Raikhelkar, J; Rodgers, D; Sarswat, N; Sayer, G; Smith, B; Uriel, N, 2020)		1.12
" Safety analysis included evaluation of adverse drug reactions (ADRs)."( Real-world effectiveness and safety of tolvaptan in liver cirrhosis patients with hepatic edema: results from a post-marketing surveillance study (START study).
Fukuta, Y; Hirano, T; Kurosaki, M; Okada, M; Sakaida, I; Terai, S, 2020)		0.83
" Adverse events considered related to tolvaptan (10 [62."( Open-label, multicenter, dose-titration study to determine the efficacy and safety of tolvaptan in Japanese patients with hyponatremia secondary to syndrome of inappropriate secretion of antidiuretic hormone.
Arima, H; Goto, K; Hirano, T; Ishikawa, SE; Motozawa, T; Mouri, M; Watanabe, R, 2021)		1.12
" Safety was assessed via the incidence of treatment-emergent adverse events (TEAEs)."( Efficacy and safety of oral tolvaptan in patients undergoing hemodialysis: a Phase 2, double-blind, randomized, placebo-controlled trial.
Akizawa, T; Nagamoto, H; Ogata, H; Okada, T; Shimofurutani, N, 2021)		0.92
"3%), tolvaptan was safe and well-tolerated during the study period."( Efficacy and safety of oral tolvaptan in patients undergoing hemodialysis: a Phase 2, double-blind, randomized, placebo-controlled trial.
Akizawa, T; Nagamoto, H; Ogata, H; Okada, T; Shimofurutani, N, 2021)		1.43
" The common treatment-emergent adverse events included vomiting (5 of 43 patients, 11."( Efficacy and safety of tolvaptan in patients with malignant ascites: a phase 2, multicenter, open-label, dose-escalation study.
Kojima, Y; Kudo, T; Murai, Y; Satoh, T; Uehara, K, 2021)		0.93
" In the 3-year Tolvaptan Efficacy and Safety in Management of ADPKD and Its Outcomes (TEMPO) 3:4, 2-year extension to TEMPO 3:4 (TEMPO 4:4), and 1-year Replicating Evidence of Preserved Renal Function: An Investigation of Tolvaptan Safety and Efficacy in ADPKD (REPRISE) trials, aquaretic adverse events were common."( Multicenter Study of Long-Term Safety of Tolvaptan in Later-Stage Autosomal Dominant Polycystic Kidney Disease.
Chapman, AB; Devuyst, O; Estilo, A; Gansevoort, RT; Hoke, ME; Lee, J; Perrone, RD; Sergeyeva, O; Torres, VE, 2020)		1.18
"It is not clear whether tolvaptan is safe and effective irrespective of various underlying clinical conditions including the functional ventricle morphology, chromosomal abnormalities, and renal function after complex pediatric congenital heart disease surgery."( Efficacy and safety of tolvaptan after pediatric congenital heart disease surgery.
Kanai, A; Kobayashi, T; Kojima, T; Sumitomo, N; Yoshiba, S, 2021)		1.24
" Therefore, we aimed to evaluate the clinical effectiveness and adverse events associated with tolvaptan in VE patients with ADHF."( Clinical effectiveness and adverse events associated with tolvaptan in patients above 90 years of age with acute decompensated heart failure.
Endo, A; Kagawa, Y; Morita, Y; Ouchi, T; Sato, H; Tanabe, K; Watanabe, N; Yamaguchi, K, 2021)		1.08
" No severe adverse events were reported."( Clinical Experience of the Efficacy and Safety of Low-dose Tolvaptan Therapy in a UK Tertiary Oncology Setting.
Al-Othman, S; Blackhall, F; Brabant, G; Chatzimavridou-Grigoriadou, V; Higham, CE; King, J; Kyriacou, A; Trainer, PJ, 2021)		0.86
"The use of tolvaptan in patients with acute heart failure requiring long-distance transport is safe and may show better clinical course compared with conventional therapies."( Efficacy and safety of tolvaptan in acute heart failure patients during long-distance transportation.
Iwata, S; Nakagawa, K; Nishiura, T; Okada, M; Sakai, H; Tokuno, S; Yamaki, M, 2022)		1.42
"Tolvaptan use in AS patients with heart failure is effective and safe before aortic valve intervention."( Effectiveness and Safety of Tolvaptan in Patients with Aortic Stenosis.
Fukumoto, Y; Shimozono, K, 2022)		2.46
" Most treatment-emergent adverse events were mild to moderate; one serious treatment-emergent adverse event of hyperkalaemia in the OPC-61815 group was considered treatment related."( Efficacy and safety of intravenous OPC-61815 compared with oral tolvaptan in patients with congestive heart failure.
Kim, S; Kurita, Y; Sato, N; Uno, S, 2022)		0.96
" However, tolvaptan increases the adverse effects of thirst, polyuria and hepatic injury."( Efficacy and safety of tolvaptan versus placebo in the treatment of patients with autosomal dominant polycystic kidney disease: a meta-analysis.
Ding, L; Gong, L; Jiang, W; Lu, J; Qian, X; Tang, W; Xie, F; Xu, M; Xu, W, 2023)		1.62
" The aim of the present review is to critically summarize the evidence on the effect of dietary modification on ADPKD and to offer some strategies to mitigate the adverse aquaretic effects of tolvaptan."( Dietary Aspects and Drug-Related Side Effects in Autosomal Dominant Polycystic Kidney Disease Progression.
Quiroga, B; Torra, R, 2022)		0.91
" We monitored the occurrence of adverse events, including acute kidney injury and hypernatremia, as well as laboratory data trends."( Effectiveness and safety of Tolvaptan in infants with congenital heart disease.
Hirano, D; Ito, A; Miwa, S; Oishi, K; Saito, A; Sakaguchi, H; Takemasa, Y; Umeda, C, )		0.43
" No adverse events were observed."( Effectiveness and safety of Tolvaptan in infants with congenital heart disease.
Hirano, D; Ito, A; Miwa, S; Oishi, K; Saito, A; Sakaguchi, H; Takemasa, Y; Umeda, C, )		0.43
" From the perspective of adverse effects, initiating administration at a lower dosage is preferable because this was found to be sufficiently effective."( Effectiveness and safety of Tolvaptan in infants with congenital heart disease.
Hirano, D; Ito, A; Miwa, S; Oishi, K; Saito, A; Sakaguchi, H; Takemasa, Y; Umeda, C, )		0.43
"The present study shows that long-term low-dose Tolvaptan is safe and effective in SIADH treatment."( Long-term low-dose tolvaptan efficacy and safety in SIADH.
Aliberti, L; Ambrosio, MR; Bondanelli, M; Gagliardi, I; Zatelli, MC, 2023)		1.49
" The incidence of common adverse events (AEs) was pooled."( Efficacy and safety of tolvaptan in cirrhotic patients: a systematic review and meta-analysis of randomized controlled trials.
Chai, L; Cheng, G; Li, Z; Pinyopornpanish, K; Qi, X; Wang, R; Wang, T, )		0.44

Pharmacokinetics

Tolvaptan's effect on urine excretion rate does not produce proportional changes in urine output. Following co-administration with grapefruit juice, tolv aptan concentrations were elevated compared with tolvaptAn alone for only 16 h postdose.

ExcerptReferenceRelevance
"The pharmacokinetic and pharmacodynamic interactions between tolvaptan and furosemide or hydrochlorothiazide (HCTZ) were determined in a single-center, randomized, open-label, parallel-arm, 3-period crossover study conducted in healthy white (Caucasian) men."( Pharmacokinetic and pharmacodynamic interaction between tolvaptan, a non-peptide AVP antagonist, and furosemide or hydrochlorothiazide.
Bramer, SL; Bricmont, P; Shoaf, SE; Zimmer, CA, 2007)		0.83
" Due to the saturable nature of tolvaptan's effect on urine excretion rate, changes in the pharmacokinetic profile of tolvaptan do not produce proportional changes in urine output."( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		0.88
"To evaluate the pharmacokinetic profile of tolvaptan."( Nonclinical pharmacokinetics of a new nonpeptide V2 receptor antagonist, tolvaptan.
Furukawa, M; Kashiyama, E; Umehara, K, 2011)		0.86
"The nonclinical pharmacokinetic profile of [(14)C]tolvaptan was evaluated in an absorption, distribution, and excretion study in rats after single oral administration."( Nonclinical pharmacokinetics of a new nonpeptide V2 receptor antagonist, tolvaptan.
Furukawa, M; Kashiyama, E; Umehara, K, 2011)		0.85
" Tolvaptan showed dose-linear pharmacokinetic characteristics regarding area under the concentration-time curve."( Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men.
Cho, JY; Jang, IJ; Jeon, H; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2012)		1.55
" Pharmacodynamic endpoints were urine volume and fluid balance for 0 to 24 h postdose."( Pharmacokinetics and pharmacodynamics of single-dose oral tolvaptan in fasted and non-fasted states in healthy Caucasian and Japanese male subjects.
Bricmont, P; Kim, SR; Mallikaarjun, S; Shoaf, SE, 2012)		0.62
" Twenty-four-hour urine volumes paralleled pharmacokinetic changes, but the increases were not clinically significant."( Pharmacokinetics and pharmacodynamics of single-dose oral tolvaptan in fasted and non-fasted states in healthy Caucasian and Japanese male subjects.
Bricmont, P; Kim, SR; Mallikaarjun, S; Shoaf, SE, 2012)		0.62
" This validated method was successfully applied to a pharmacokinetic study in healthy volunteers after oral administration of single-dose tolvaptan tablets."( Development and validation of an LC-MS/MS method for the determination of tolvaptan in human plasma and its application to a pharmacokinetic study.
Guo, C; Huang, P; Li, Z; Liu, L; Luo, M; Pei, Q; Peng, X; Tan, H; Yang, G; Zhang, B; Zuo, X, 2013)		0.82
"This study investigated the pharmacokinetic and pharmacodynamic profile of tolvaptan, and verified its efficacy and safety in patients with liver cirrhosis-associated ascites, with insufficient response to conventional diuretic treatment."( The pharmacokinetics and pharmacodynamics of tolvaptan in patients with liver cirrhosis with insufficient response to conventional diuretics: a multicentre, double-blind, parallel-group, phase III study.
Kobayashi, Y; Okada, M; Okita, K; Sakaida, I; Yanase, M; Yasutake, T, 2012)		0.87
" Pharmacokinetic, pharmacodynamic and efficacy variables were measured."( The pharmacokinetics and pharmacodynamics of tolvaptan in patients with liver cirrhosis with insufficient response to conventional diuretics: a multicentre, double-blind, parallel-group, phase III study.
Kobayashi, Y; Okada, M; Okita, K; Sakaida, I; Yanase, M; Yasutake, T, 2012)		0.64
"75 mg/day exerts some effects due to the pharmacokinetic profile in patients with liver cirrhosis."( The pharmacokinetics and pharmacodynamics of tolvaptan in patients with liver cirrhosis with insufficient response to conventional diuretics: a multicentre, double-blind, parallel-group, phase III study.
Kobayashi, Y; Okada, M; Okita, K; Sakaida, I; Yanase, M; Yasutake, T, 2012)		0.64
" A population pharmacokinetic (PK) analysis was performed for tolvaptan in NONMEM® based upon data obtained from three trials conducted in 93 healthy subjects and six trials conducted in 628 congestive heart failure (CHF) patients or 24 hepatic cirrhosis patients receiving oral tolvaptan (5 to 240 mg)."( Population pharmacokinetics of tolvaptan in healthy subjects and patients with hyponatremia secondary to congestive heart failure or hepatic cirrhosis.
Mager, DE; Mallikaarjun, S; Shoaf, SE; Van Wart, SA, 2013)		0.92
" The proposed method was successfully applied to a pharmacokinetic study of 15 mg and 60 mg tolvaptan tablet formulation in healthy South Indian male subjects under fasting condition."( Bioanalysis of tolvaptan, a novel AVP-V2 receptor antagonist in human plasma by a novel LC-ESI-MS/MS method: a pharmacokinetic application in healthy South Indian male subjects.
Adireddy, V; Bhukya, BR; Derangula, VR; Pilli, NR; Ponneri, V; Pulipati, CR, 2014)		0.98
"73 m(2)) by conducting a pharmacokinetic and pharmacodynamic study in these patients."( Efficacy of tolvaptan added to furosemide in heart failure patients with advanced kidney dysfunction: a pharmacokinetic and pharmacodynamic study.
Akashi, YJ; Kida, K; Kimura, K; Matsumoto, N; Miyake, F; Shibagaki, Y; Tominaga, N, 2015)		0.8

Compound-Compound Interactions

This study examined the effects of recombinant human brain natriuretic peptide (rhBNP) combined with tolvaptan on cardiac and renal function and serum inflammatory factors in patients with severe heart failure (HF) We report a case of SIADH patient treated with intermittent lower dose of toLVaptan combined with fluid restriction.

ExcerptReferenceRelevance
" Participants were assigned to receive either tolvaptan combined with torasemide (n = 20) or torasemide monotherapy (n = 20; control group)."( Short-Term Effects of Tolvaptan in Tricuspid Insufficiency Combined with Left Heart Valve Replacement-Caused Volume-Overload Patients: Results of a Prospective Pilot Study.
Jiang, L; Liu, H; Ma, L; Wu, Z; Xu, L; Yuan, F; Zhai, Z; Zhang, J; Zhou, J, 2019)		1.09
" We report a case of SIADH patient treated with intermittent lower dose of tolvaptan combined with fluid restriction."( A new method of intermittent lower dose of tolvaptan combined with fluid restriction to treat the syndrome of inappropriate antidiuresis: A case report.
Chen, S; Ke, X; Li, J; Miao, H; Pan, H; Yuan, X; Zhu, H, 2019)		1.01
"For patients with chronic SIADH, the tolvaptan dose should be individualized, and the regimen of intermittent lower dose of tolvaptan combined with fluid restriction maybe an effective choice."( A new method of intermittent lower dose of tolvaptan combined with fluid restriction to treat the syndrome of inappropriate antidiuresis: A case report.
Chen, S; Ke, X; Li, J; Miao, H; Pan, H; Yuan, X; Zhu, H, 2019)		1.05
"This study examined the effects of recombinant human brain natriuretic peptide (rhBNP) combined with tolvaptan on cardiac and renal function and serum inflammatory factors in patients with severe heart failure (HF)."( Effects of recombinant human brain natriuretic peptide combined with tolvaptan on cardiac and renal function and serum inflammatory factors in patients with severe heart failure.
Guo, M; Hao, M; Yang, J; Zhang, L, 2023)		1.36

Bioavailability

Tolvaptan absolute bioavailability was determined in a single-center, open-label, sequential administration trial. It appears that grapefruit juice increases the bioavailability of tolvaptan, but does not affect its systemic elimination.

ExcerptReferenceRelevance
"It appears that grapefruit juice increases the bioavailability of tolvaptan, but does not affect its systemic elimination."( Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		0.86
" Tolvaptan absolute bioavailability was determined in a single-center, open-label, sequential administration trial in which intravenous (i."( Absolute bioavailability of tolvaptan and determination of minimally effective concentrations in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		1.58
" Relative oral bioavailability was modeled relative to 100% for a 30 mg dose and ranged from 79."( Population pharmacokinetics of tolvaptan in healthy subjects and patients with hyponatremia secondary to congestive heart failure or hepatic cirrhosis.
Mager, DE; Mallikaarjun, S; Shoaf, SE; Van Wart, SA, 2013)		0.68
"The bioavailability of a crushed tolvaptan tablet suspended in water and administered by nasogastric (NG) tube was compared to the bioavailability from the tablet administered whole."( Relative bioavailability of tolvaptan administered via nasogastric tube and tolvaptan tablets swallowed intact.
Adams, KF; Brouwer, KL; Henry, J; Hull, JH; McNeely, EB; Patterson, JH; Simmons, B; Talameh, JA, 2013)		0.97
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

Tolvaptan was used in a higher dosage for therapy of autosomal dominant polycystic kidney disease. All subjects had tolvaptan concentrations > 20 ng/ml at 1 h postdose.

ExcerptRelevanceReference
" The study involves the physicochemical characterization of the powders using thermal analysis and dissolution testing, development and extemporaneous manufacture of liquid-filled soft gelatin capsules, and dissolution and stability testing of the final dosage form."( The preparation of soft gelatin capsules for a radioactive tracer study.
Bramer, SL; Tesconi, MS; Yalkowsky, SH, 1999)		0.3
" There were no significant clinical, pharmacokinetic, or pharmacodynamic differences between the dosing regimens over time."( Comparison of two doses and dosing regimens of tolvaptan in congestive heart failure.
Bramer, SL; Hauptman, PJ; Mallikaarjun, S; Orlandi, C; Shoaf, SE; Udelson, J; Zimmer, C, 2005)		0.59
" Dosage adjustment was based on serum Na+ changes, initially 15 mg, titratable to 30 or 60 mg."( Double-blind, placebo-controlled, multicenter trial of a vasopressin V2-receptor antagonist in patients with schizophrenia and hyponatremia.
Albazzaz, A; Czerwiec, F; Goldman, M; Jessani, M; Josiassen, RC; Lee, J; Orlandi, C; Ouyang, J; Shaughnessy, RA, 2008)		0.35
" In short and long term studies, tolvaptane has been shown to be effective in raising serum sodium levels in a predictable fashion in patients with SIADH with only few side effects, when serum sodium was frequently monitored and dosage of tolvaptans was properly adjusted."( [Treatment of hyponatremia: new developments and controversies].
Hensen, J, 2011)		0.65
" As tolvaptan is a CYP3A4 substrate, knowing the effects of inhibition and induction on CYP3A4-mediated metabolism was important for dosing recommendations."( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		1.16
" No tolvaptan accumulation was found after multiple dosing for 7 days."( Pharmacokinetics, pharmacodynamics and safety of tolvaptan, a novel, oral, selective nonpeptide AVP V2-receptor antagonist: results of single- and multiple-dose studies in healthy Japanese male volunteers.
Azuma, J; Hasunuma, T; Kim, SR; Kondo, M; Okada, T; Sato, O, 2011)		1.18
" In this study, we evaluated the dose-response effects of tolvaptan on weight loss, urine volume and electrolyte excretion in furosemide-treated Japanese HF patients exhibiting volume overload."( Effects of tolvaptan on volume overload in Japanese patients with heart failure: results of a phase II, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.
Asanoi, H; Hori, M; Izumi, T; Matsuzaki, M; Tsutamoto, T, 2011)		1
" Urine volume and fluid intake were measured for 24 hours starting the day before dosing (day -1) as baseline, and on the day of drug administration (day 1)."( Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men.
Cho, JY; Jang, IJ; Jeon, H; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2012)		0.64
" Minimally effective concentrations are rapidly achieved after oral dosing as all subjects had tolvaptan concentrations > 20 ng/ml at 1 h postdose."( Absolute bioavailability of tolvaptan and determination of minimally effective concentrations in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012)		0.89
" Model diagnostics helped to demonstrate that the population PK model reasonably predicts the rate of urinary HCTZ excretion over time using dosing history and estimated CLCR , allowing for the convenient assessment of PK-PD relationships for HCTZ when given alone or in combination with other agents used to treat fluid overload conditions."( Population-based meta-analysis of hydrochlorothiazide pharmacokinetics.
Mager, DE; Mallikaarjun, S; Shoaf, SE; Van Wart, SA, 2013)		0.39
" Predictive factors for the occurrence of hypernatremia were the starting dosage of tolvaptan (15mg/day), baseline serum sodium level (≥142mEq/L) and serum potassium level (<3."( Efficacy and safety of tolvaptan in heart failure patients with volume overload.
Inomata, T; Iwatake, N; Kinugawa, K; Mizuguchi, K; Sato, N; Shimakawa, T, 2014)		0.94
" Combination therapy using loop diuretics, tolvaptan, and carperitide with differing and complementary mechanisms of action may maximize therapeutic activity, to minimize the dosage of loop diuretics and thereby reduce the adverse effects not only for volume removal but also for the stability of cardiorenal hemodynamics."( Novel diuretic strategies for the treatment of heart failure in Japan.
Dohi, K; Ito, M, 2014)		0.67
" This study also suggests that in these patients 15 mg/day of tolvaptan should be sufficient, and increasing the dose or the frequency of dosing to overcome diuretic resistance should not be necessary, and consideration should be given to using a lower dose and/or prolonging the dosing interval."( Efficacy of tolvaptan added to furosemide in heart failure patients with advanced kidney dysfunction: a pharmacokinetic and pharmacodynamic study.
Akashi, YJ; Kida, K; Kimura, K; Matsumoto, N; Miyake, F; Shibagaki, Y; Tominaga, N, 2015)		1.04
" In turn, AVT had a dual effect on killifish opercular Isc: an immediate response (~3min) with Isc reduction in an inverted bell-shaped dose-response manner with higher current decrease (-22 μA⋅cm(-2)) at 10(-8) M AVT, and a sustained dose-dependent stimulation of Cl(-) secretion (stable up to 1h), with a threshold significant effect at 10(-8) M and maximal stimulation (~20 μA⋅cm(-2)) at 10(-6)M."( AVT and IT regulate ion transport across the opercular epithelium of killifish (Fundulus heteroclitus) and gilthead sea bream (Sparus aurata).
Fuentes, J; Mancera, JM; MartínezRodríguez, G; Martos-Sitcha, JA, 2015)		0.42
" In this study tolvaptan was used in a higher dosage for therapy of autosomal dominant polycystic kidney disease."( [Hyponatremia and tolvaptan : what is the situation 5 years after approval?].
Hensen, J, 2015)		1.1
" Moreover, the use of tolvaptan reduced the dosage of furosemide."( Effects of tolvaptan on congestive heart failure complicated with chylothorax in a neonate.
Inukai, S; Ito, K; Kato, T; Nagasaki, R; Saitoh, S; Sato, N; Sugiura, T; Suzuki, K, 2015)		1.12
" Albuminuria was measured in a spot morning urine sample prior to tolvaptan dosing and expressed as albumin-to-creatinine ratio (ACR)."( Albuminuria and tolvaptan in autosomal-dominant polycystic kidney disease: results of the TEMPO 3:4 Trial.
Chapman, AB; Czerwiec, FS; Devuyst, O; Gansevoort, RT; Grantham, JJ; Higashihara, E; Krasa, HB; Meijer, E; Ouyang, J; Perrone, RD; Torres, VE, 2016)		1.02
" Stepwise logistic regression analysis demonstrated that baseline serum sodium ≥140 mEq/L, an initial tolvaptan dosage >7."( Risk factors for hypernatremia in patients with short- and long-term tolvaptan treatment.
Hirai, K; Inoue, K; Ishii, H; Itoh, K; Kadoiri, T; Moriwaki, H; Shimomura, T; Shimoshikiryo, T; Tsuji, D, 2016)		0.88
" Dosage is 60-120 mg/day in two different doses (for instance 45/15 or 60/30 mg)."( [Treatment of autosomal dominant polycystic kidney disease (ADPKD) - Tolvaptan].
Cirillo, M, )		0.37
" In a dose-response study, we measured the effect of tolvaptan on renal handling of water and sodium and systemic hemodynamics, during baseline and NO-inhibition with L-NMMA (L-NG-monomethyl-arginine)."( Effect of tolvaptan on renal water and sodium excretion and blood pressure during nitric oxide inhibition: a dose-response study in healthy subjects.
Al Therwani, S; Bech, JN; Mose, FH; Pedersen, EB; Rosenbæk, JB, 2017)		1.11
" However, the optimal dosage remains unclear."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		0.75
" We used network meta-analysis to look for the optimal dosage in terms of effectiveness and safety."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		0.75
" Compared with placebo, tolvaptan of different dosage showed a non-significant higher risk of adverse effects."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		1.06
"These findings suggest that tolvaptan 30 mg and 45 mg may be the optimum dosage for CHF patients, because of its ability to provide favourable clinical results without greater adverse effects."( Effects and safety of oral tolvaptan in patients with congestive heart failure: A systematic review and network meta-analysis.
Chen, TT; Chen, YC; Lin, HH; Tarng, DC; Tu, YK; Wu, MY; Wu, YC, 2017)		1.05
"4) mmHg along with the increase in FeNa, leading to reduced dosage of antihypertensives in 6 patients."( Tolvaptan promotes urinary excretion of sodium and urea: a retrospective cohort study.
Hamano, T; Isaka, Y; Iwatani, H; Kimura, Y; Minami, S; Mizui, M, 2018)		1.92
" We advise caution when dosing tolvaptan in patients with both low serum sodium and SUN concentrations."( Rapidity of Correction of Hyponatremia Due to Syndrome of Inappropriate Secretion of Antidiuretic Hormone Following Tolvaptan.
Bhasin, B; Bohm, NM; Crawford, R; Kelley, D; Morris, JH; Nemecek, BD; Nietert, PJ; Velez, JCQ, 2018)		0.98
"The clinical dosing method for tolvaptan in patients with acute heart failure (HF) is still unclear."( Comparison of two dosing methods for immediate administration of tolvaptan in acute decompensated heart failure.
Ishii, H; Izumi, K; Kamiya, H; Kawamura, Y; Murohara, T; Oguri, M; Ohguchi, S; Takahara, K; Takahashi, H; Yokoi, Y, 2018)		1
"Vaptans were associated with a significant increase in urine output and serum sodium with an apparent reduction or stabilization of furosemide equivalent dosing in the early treatment period in patients with decompensated RHF."( Vasopressin antagonism for decompensated right-sided heart failure.
Chibnall, JT; Godishala, A; Goff, ZD; Hauptman, PJ; Joseph, SM; Shuster, JE; Vidic, A, 2019)		0.51
" The consequences of hepatotoxicity for the subsequent dosing of tolvaptan have not been reported."( Con: Tolvaptan for autosomal dominant polycystic kidney disease-do we know all the answers?
Gross, P; Paliege, A; Schirutschke, H, 2019)		1.27
"In Study 1, the 45 patients were divided into three groups based on changes in dosing of diuretics."( Analysis of tolvaptan non-responders and outcomes of tolvaptan treatment of ascites.
Hidaka, I; Ishikawa, T; Iwamoto, T; Maeda, M; Saeki, I; Sakaida, I; Tajima, K; Takami, T, 2019)		0.89
" What is Known: • Autosomal dominant polycystic kidney disease (ADPKD) is a genetic disorder causing the development of cysts that impede kidney function over time and eventually induce renal failure • There are few data on the effects of tolvaptan, the only treatment approved for adults to slow disease progression, in pediatric ADPKD patients with early-stage disease What is New: • A phase 3, placebo-controlled study is evaluating tolvaptan over 3 years in children and adolescents with ADPKD • This study is designed to account for challenges of tolvaptan dosing and outcome assessment specific to the pediatric population."( Tolvaptan use in children and adolescents with autosomal dominant polycystic kidney disease: rationale and design of a two-part, randomized, double-blind, placebo-controlled trial.
Bockenhauer, D; Cadnapaphornchai, MA; Dandurand, A; Emma, F; Gilbert, RD; Mekahli, D; Schaefer, F; Shi, L; Shoaf, SE; Sikes, K, 2019)		2.14
"5 mg and 15 mg dosage groups (-3."( Real-World Effectiveness and Tolerability of Tolvaptan in Patients With Heart Failure　- Final Results of the Samsca Post-Marketing Surveillance in Heart Failure (SMILE) Study.
Fukuta, Y; Inomata, T; Kinugawa, K; Sato, N; Shimakawa, T; Yasuda, M, 2019)		0.77
" The conventional therapy group continued with the original dosage regimens."( Furosemide Dose Changes Associated with Furosemide/Tolvaptan Combination Therapy in Patients with Cirrhosis.
Hidaka, H; Kako, M; Koizumi, W; Kubota, K; Nakazawa, T; Shibuya, A; Sung, JH; Tanaka, Y; Uojima, H; Wada, N, 2020)		0.81
" Dasatinib is a novel tyrosine-kinase inhibitor approved for CML with Philadelphia (Ph) chromosome and the most common adverse effects of dasatinib are peripheral edema and pleural effusion, which sometimes impose the interruption or reduction of dosage of dasatinib treatment, accompanied by diuretic and steroid use."( The efficacy of tolvaptan in treating dasatinib-induced pleural effusions in patients with chronic myelogenous leukemia.
Aoyama, R; Harada, K; Ishikawa, J, 2020)		0.9
"5 years old, and the mean dosage of dasatinib and tolvaptan were 58."( The efficacy of tolvaptan in treating dasatinib-induced pleural effusions in patients with chronic myelogenous leukemia.
Aoyama, R; Harada, K; Ishikawa, J, 2020)		1.16
" A significant negative correlation was observed between the dosage of furosemide and ΔSMI (%) (P = 0."( Management of refractory ascites attenuates muscle mass reduction and improves survival in patients with decompensated cirrhosis.
Aikata, H; Chayama, K; Fujino, H; Hiramatsu, A; Imamura, M; Kawaoka, T; Kodama, K; Morio, K; Murakami, E; Nakahara, T; Namba, M; Ohya, K; Tsuge, M; Uchikawa, S; Yamauchi, M, 2020)		0.56
" The long-term cumulative survival rates in patients who received a mean dosage of spironolactone < 23 mg/day during tolvaptan treatment were significantly higher than those receiving a mean dosage of ≥ 23 mg/day (P = 0."( Analysis of factors associated with the prognosis of cirrhotic patients who were treated with tolvaptan for hepatic edema.
Abe, H; Arai, T; Atsukawa, M; Chuma, M; Fukunishi, S; Hattori, N; Hiraoka, A; Iio, E; Ikegami, T; Itokawa, N; Iwakiri, K; Iwasa, M; Kato, K; Kondo, C; Kumada, T; Michitaka, K; Nakagawa-Iwashita, A; Nozaki, A; Okubo, H; Okubo, T; Senoh, T; Tada, T; Takaguchi, K; Takei, Y; Tanaka, Y; Tani, J; Toyoda, H; Tsubota, A; Tsutsui, A; Uojima, H; Watanabe, T; Yokohama, K; Yoshida, Y, 2020)		0.99
" Twenty-four-hour urine collections were done at baseline, day 3-4 of the dosing period, day 7-8 of the dosing period, and 3-6 days after washout."( Pharmacological Dilutional Therapy Using the Vasopressin Antagonist Tolvaptan for Young Patients With Cystinuria: A Pilot Investigation.
Baum, MA; Cilento, BG; Kurtz, MP; Nelson, CP; Venna, A, 2020)		0.79
" Further investigation should study longer term effects and safety, and determine optimal dosing to improve tolerability."( Pharmacological Dilutional Therapy Using the Vasopressin Antagonist Tolvaptan for Young Patients With Cystinuria: A Pilot Investigation.
Baum, MA; Cilento, BG; Kurtz, MP; Nelson, CP; Venna, A, 2020)		0.79
" During the follow-up period, the loop diuretic dosage significantly decreased."( Initiation and long-term use of tolvaptan for patients with worsening heart failure through hospital and clinic cooperation.
Ishikawa, S; Murohara, T; Shibata, R; Takemoto, K; Uemura, Y; Watarai, M, 2021)		0.9
" From the perspective of adverse effects, initiating administration at a lower dosage is preferable because this was found to be sufficiently effective."( Effectiveness and safety of Tolvaptan in infants with congenital heart disease.
Hirano, D; Ito, A; Miwa, S; Oishi, K; Saito, A; Sakaguchi, H; Takemasa, Y; Umeda, C, )		0.43
"001), top 50% dosage of loop diuretics (P = 0."( Risk factors of readmission and the impact of outpatient management in heart failure patients: A national study in Japan.
Fujimori, K; Fushimi, K; Miyazaki, D; Tarasawa, K, 2023)		0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
vasopressin receptor antagonistAny drug which blocks vasopressin receptors.
aquareticA class of diuretics which promote aquaresis (the excretion of water without electrolyte loss).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
benzazepineA group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.
benzenedicarboxamide
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (30)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency29.79810.007215.758889.3584AID1224835; AID624030
TDP1 proteinHomo sapiens (human)Potency21.13600.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency18.83360.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency23.91450.000221.22318,912.5098AID743035; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.60320.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency21.13170.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.91780.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.98560.000214.376460.0339AID720691
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency32.55480.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency26.83250.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.43340.001530.607315,848.9004AID1224848; AID1224849; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency23.91450.000229.305416,493.5996AID743069; AID743078
GVesicular stomatitis virusPotency27.54040.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency19.49710.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency33.48890.001024.504861.6448AID743212
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency3.79020.023723.228263.5986AID743223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.84930.001723.839378.1014AID743083
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency0.01690.057821.109761.2679AID1159526
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.15670.000323.4451159.6830AID743065; AID743067
Interferon betaHomo sapiens (human)Potency27.54040.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency22.38720.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)9.99000.11007.190310.0000AID1473738
Vasopressin V2 receptorHomo sapiens (human)IC50 (µMol)0.14860.00001.12137.0000AID1720599; AID1799335; AID1906997
Vasopressin V2 receptorHomo sapiens (human)Ki0.00140.00040.43453.9811AID1820286; AID1892238; AID1906993; AID217521
Vasopressin V1a receptorHomo sapiens (human)IC50 (µMol)0.35100.00060.38352.0000AID1799335; AID1820285
Vasopressin V1a receptorHomo sapiens (human)Ki0.16400.00020.62357.0300AID1820284; AID1892240
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (121)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of systemic arterial blood pressureVasopressin V2 receptorHomo sapiens (human)
renal water retentionVasopressin V2 receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
activation of adenylate cyclase activityVasopressin V2 receptorHomo sapiens (human)
hemostasisVasopressin V2 receptorHomo sapiens (human)
positive regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
negative regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
positive regulation of gene expressionVasopressin V2 receptorHomo sapiens (human)
telencephalon developmentVasopressin V2 receptorHomo sapiens (human)
response to cytokineVasopressin V2 receptorHomo sapiens (human)
positive regulation of intracellular signal transductionVasopressin V2 receptorHomo sapiens (human)
cellular response to hormone stimulusVasopressin V2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionVasopressin V2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinVasopressin V2 receptorHomo sapiens (human)
maternal aggressive behaviorVasopressin V1a receptorHomo sapiens (human)
positive regulation of systemic arterial blood pressureVasopressin V1a receptorHomo sapiens (human)
generation of precursor metabolites and energyVasopressin V1a receptorHomo sapiens (human)
activation of phospholipase C activityVasopressin V1a receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVasopressin V1a receptorHomo sapiens (human)
negative regulation of female receptivityVasopressin V1a receptorHomo sapiens (human)
grooming behaviorVasopressin V1a receptorHomo sapiens (human)
blood circulationVasopressin V1a receptorHomo sapiens (human)
positive regulation of cell population proliferationVasopressin V1a receptorHomo sapiens (human)
positive regulation of heart rateVasopressin V1a receptorHomo sapiens (human)
positive regulation of glutamate secretionVasopressin V1a receptorHomo sapiens (human)
myotube differentiationVasopressin V1a receptorHomo sapiens (human)
calcium-mediated signalingVasopressin V1a receptorHomo sapiens (human)
telencephalon developmentVasopressin V1a receptorHomo sapiens (human)
positive regulation of cell growthVasopressin V1a receptorHomo sapiens (human)
positive regulation of prostaglandin biosynthetic processVasopressin V1a receptorHomo sapiens (human)
positive regulation of cellular pH reductionVasopressin V1a receptorHomo sapiens (human)
social behaviorVasopressin V1a receptorHomo sapiens (human)
cellular response to water deprivationVasopressin V1a receptorHomo sapiens (human)
maternal behaviorVasopressin V1a receptorHomo sapiens (human)
sperm ejaculationVasopressin V1a receptorHomo sapiens (human)
response to corticosteroneVasopressin V1a receptorHomo sapiens (human)
negative regulation of transmission of nerve impulseVasopressin V1a receptorHomo sapiens (human)
transport across blood-brain barrierVasopressin V1a receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayVasopressin V1a receptorHomo sapiens (human)
positive regulation of vasoconstrictionVasopressin V1a receptorHomo sapiens (human)
cellular response to hormone stimulusVasopressin V1a receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinVasopressin V1a receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
vasopressin receptor activityVasopressin V2 receptorHomo sapiens (human)
protein bindingVasopressin V2 receptorHomo sapiens (human)
peptide bindingVasopressin V2 receptorHomo sapiens (human)
vasopressin receptor activityVasopressin V1a receptorHomo sapiens (human)
protein kinase C bindingVasopressin V1a receptorHomo sapiens (human)
protein bindingVasopressin V1a receptorHomo sapiens (human)
peptide hormone bindingVasopressin V1a receptorHomo sapiens (human)
V1A vasopressin receptor bindingVasopressin V1a receptorHomo sapiens (human)
peptide bindingVasopressin V1a receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endosomeVasopressin V2 receptorHomo sapiens (human)
endoplasmic reticulumVasopressin V2 receptorHomo sapiens (human)
Golgi apparatusVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
membraneVasopressin V2 receptorHomo sapiens (human)
endocytic vesicleVasopressin V2 receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneVasopressin V2 receptorHomo sapiens (human)
perinuclear region of cytoplasmVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
endosomeVasopressin V1a receptorHomo sapiens (human)
plasma membraneVasopressin V1a receptorHomo sapiens (human)
endocytic vesicleVasopressin V1a receptorHomo sapiens (human)
plasma membraneVasopressin V1a receptorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (96)

Assay IDTitleYearJournalArticle
AID1906997Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1906998Insurmountable antagonist activity at human V2 receptor expressed in CHO cells assessed as decrease in maximal response preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1907000Antagonist activity at human V2 receptor expressed in CHO cells assessed as assessed as target occupancy preincubated for 30 mins followed by vasopressin stimulation for 30 mins2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473999Drug concentration at steady state in human at 15 to 60 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1906996Inhibition of conivaptan-red binding to SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as residence time (1/koff) measured after 2 hrs by HTRF competitive binding assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892260Hepatotoxicity in wild type C57BL/6 mouse assessed as change in serum ALT level at 5 mg/kg administered once daily for 12 consecutive days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1907015Suppression of renal cyst development in Pkd1 flox/flox;Cre-Esr+ mouse model of tamoxifen induced autosomal dominant polycystic kidney disease at 2 mg/kg, sc administered once daily treatment started from postnatal day 55 to 115 days by hematoxylin and eo2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1907009Tmax in C57BL/6 mouse at 2 mg/kg, sc by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID217521Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
AID1820284Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Synthesis and Characterization of New V
AID1892251Suppression of renal cyst development in Pkd1 flox/flox;Ksp-Cre mouse model of autosomal dominant polycystic kidney disease assessed as reduction in cyst formation at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days by hematoxy2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1892250Suppression of renal cyst development in Pkd1 flox/flox;Ksp-Cre mouse model of autosomal dominant polycystic kidney disease assessed as reduction in kidney size at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days by hematoxylin2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1892247Suppression of renal cyst development in Pkd1 flox/flox;Ksp-Cre mouse model of autosomal dominant polycystic kidney disease assessed as reduction in kidney size at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1820286Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Synthesis and Characterization of New V
AID1907007Elimination rate constant in C57BL/6 mouse at 2 mg/kg, sc by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1907011AUC (0 to t) in C57BL/6 mouse at 2 mg/kg, sc by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1906995Inhibition of conivaptan-red binding to SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as binding constant (Koff) measured after 2 hrs by HTRF competitive binding assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892243Inhibition of cyst formation in MDCK cells at 1 uM treated for 8 consecutive days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1892240Displacement of [3H]-vasopressin from human V1A receptor expressed in CHO cells membrane by microbeta scintillation counter analysis2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1906999Antagonist activity at human V2 receptor expressed in CHO cells assessed as recovery of cAMP production preincubated for 30 mins followed by compound washout and subsequent vasopressin stimulation for 30 mins and measured after 1 hr2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1907012Equilibrium solubility of compound in water incubated for 24 hrs by UV-spectroscopy method2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID32545Binding affinity towards AVP receptor2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1907008Half life in C57BL/6 mouse at 2 mg/kg, sc by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1907013Ex vivo receptor occupancy at V2R in isolated perfused Sprague-Dawley rat kidney assessed as clearance rate at 0.1 uM incubated for 30 mins by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892259Drug concentration in kidney of C57BL/6 mouse at 5 mg/kg, sc measured at 1 hr by HPLC analysis2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1892253Toxicity in wild type C57BL/6 mouse assessed as change in body weight at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1906993Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1820285Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Synthesis and Characterization of New V
AID1906990Ex vivo receptor occupancy at V2R in isolated perfused Sprague-Dawley rat kidney assessed as dissociation half life at 0.1 uM incubated for 30 mins by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892242Inverse agonist activity at human V2 receptor expressed in CHO cells assessed as reduction in basal cAMP level incubated for 1 hr2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1907004Toxicity in wild type mouse assessed as effect on kidney size2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1473998AUC in human at 15 to 60 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1907016Suppression of kidney weight to body weight ratio in Pkd1 flox/flox;Cre-Esr+ mouse model of tamoxifen induced autosomal dominant polycystic kidney disease at 2 mg/kg, sc administered once daily measured at postnatal day 1152022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1906994Inhibition of conivaptan-red binding to SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as binding constant (Kon) measured after 2 hrs by HTRF competitive binding assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1892258Drug concentration in kidney of C57BL/6 mouse at 5 mg/kg, sc measured at 0.5 hr by HPLC analysis2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1892252Toxicity in wild type C57BL/6 mouse assessed as change in kidney size at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1720599Antagonist activity at human AVPR2 by PathHunter beta-arrestin assay2020Bioorganic & medicinal chemistry, 07-15, Volume: 28, Issue:14
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.
AID1907002Suppression of renal cyst development in embryonic kidney of 8-Br-cAMP induced C57BL/6 mouse mouse model of autosomal dominant polycystic kidney disease measured after 8 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892249Suppression of renal cyst development in Pkd1 flox/flox;Ksp-Cre mouse model of autosomal dominant polycystic kidney disease assessed as increase in body weight at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1907005Toxicity in wild type mouse assessed as effect on body weight2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1907006Invivo antagonist activity at V2R in Pkd1 knockout mouse model of autosomal dominant polycystic kidney disease assessed as reduction of renal cyst formation 2 mg/kg, sc administered once daily treatment started from postnatal day 6 to 12 days by hematoxyl2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1474000Ratio of drug concentration at steady state in human at 15 to 60 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1907003Invivo antagonist activity at V2R in Pkd1 knockout mouse model of autosomal dominant polycystic kidney disease assessed as reduction in kidney size at 2 mg/kg, sc administered once daily treatment started from postnatal day 6 to 12 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892254Selectivity index, ratio of Ki for human V2R expressed in HEK293 cells to Ki for human V1AR expressed in CHO cells2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1906992Suppression of renal cyst development in embryonic kidney of 8-Br-cAMP induced C57BL/6 mouse mouse model of autosomal dominant polycystic kidney disease assessed as residence time dependent measured after 8 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892248Suppression of renal cyst development in Pkd1 flox/flox;Ksp-Cre mouse model of autosomal dominant polycystic kidney disease assessed as reduction in renal cystic index at 5 mg/kg, sc administered once daily starting from postnatal day 6 to 12 days (Rvb = 2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1907010Cmax in C57BL/6 mouse at 2 mg/kg, sc by LC-MS analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1892238Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Benzodiazepine Derivatives as Potent Vasopressin V
AID1907014Reduction of kidney size in Pkd1 flox/flox;Cre-Esr+ mouse model of tamoxifen induced autosomal dominant polycystic kidney disease at 2 mg/kg, sc administered once daily treatment started from postnatal day 55 to 115 days by MRI scanner2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Long Residence Time at the Vasopressin V
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346468Rat V2 receptor (Vasopressin and oxytocin receptors)1998The Journal of pharmacology and experimental therapeutics, Dec, Volume: 287, Issue:3
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
AID1346453Human V2 receptor (Vasopressin and oxytocin receptors)1998The Journal of pharmacology and experimental therapeutics, Dec, Volume: 287, Issue:3
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
AID1346455Rat V1A receptor (Vasopressin and oxytocin receptors)1998The Journal of pharmacology and experimental therapeutics, Dec, Volume: 287, Issue:3
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
AID1346432Human V1A receptor (Vasopressin and oxytocin receptors)1998The Journal of pharmacology and experimental therapeutics, Dec, Volume: 287, Issue:3
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
AID1799335Radioligand Binding Assay to HeLa Cells from Article 10.1016/s0968-0896(99)00101-7: \\7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressi1999Bioorganic & medicinal chemistry, Aug, Volume: 7, Issue:8
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (925)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (0.32)18.2507
2000's104 (11.24)29.6817
2010's575 (62.16)24.3611
2020's243 (26.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 91.58

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index91.58 (24.57)
Research Supply Index7.04 (2.92)
Research Growth Index6.23 (4.65)
Search Engine Demand Index163.68 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (91.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials172 (17.79%)5.53%
Reviews193 (19.96%)6.00%
Case Studies97 (10.03%)4.05%
Observational48 (4.96%)0.25%
Other457 (47.26%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (104)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Post-Marketing Surveillance(PMS) of Safety and Efficacy of Samsca® Tablets in Korean Patients With ADPKD [NCT03406286]600 participants (Anticipated)Observational2016-07-19Recruiting
A Multi-Centre, Multi-National, Observational Post-Authorisation Safety Study to Document the Drug Utilisation of Samsca and to Collect Information on the Safety of Samsca When Used in Routine Medical Practice [NCT01228682]200 participants (Anticipated)Observational2010-10-31Active, not recruiting
Evaluating the Safety and effectivenesS in Adult KorEaN Patients Treated With Tolvaptan for Management of Autosomal domInAnt poLycystic Kidney Disease [NCT03949894]Phase 4118 participants (Actual)Interventional2019-07-01Completed
[NCT02994394]Phase 184 participants (Actual)Interventional2017-01-06Completed
A Multicenter, Double-blind, Randomized, Active-controlled, Parallel-group, Non-inferiority Trial to Evaluate the Efficacy and Safety of OPC-61815 Injection Compared With Tolvaptan 15-mg Tablet in Patients With Congestive Heart Failure [NCT03772041]Phase 3294 participants (Actual)Interventional2019-01-16Completed
A Phase 2a, Single-center Study Investigating the Short-term Renal Hemodynamic Effects, Safety and Pharmacokinetics/ Pharmacodynamics of Oral Tolvaptan in Subjects With Autosomal Dominant Polycystic Kidney Disease at Various Stages of Renal Function [NCT01336972]Phase 229 participants (Actual)Interventional2010-10-31Completed
The Effects of Tolvaptan on Renal Handling of Water and Sodium, Vasoactive Hormones and Central Hemodynamics During Baseline Conditions and After Inhibition of the Nitric Oxide System in Patients With Autosomal Dominant Polycystic Kidney Disease [NCT02527863]Phase 218 participants (Actual)Interventional2015-02-28Completed
A Clinical Study of Multiple-dose Pharmacokinetics of Tolvaptan Tablets Administered Orally (15mg Daily) for Consecutively 7 Days in Chinese Patients With Hepatocirrhosis [NCT01359462]Phase 111 participants (Actual)Interventional2009-04-30Completed
A Multicenter, Open-labeled, Dose-defining Trial to Investigate the Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Tolvaptan in Pediatric Congestive Heart Failure (CHF) Patients With Volume Overload [NCT03255226]Phase 360 participants (Anticipated)Interventional2018-02-13Recruiting
Efficacy and Safety of Low-dose Tolvaptan in Treatment of Inpatient Hyponatraemia. [NCT06171100]180 participants (Anticipated)Observational2023-12-15Recruiting
A Multicenter, Double-blind, Randomized, Active-controlled, Parallel-group Comparison Clinical Pharmacology Trial to Investigate the Dose of OPC-61815 Injection Equivalent to Tolvaptan 15-mg Tablet in Patients With Congestive Heart Failure [NCT03254108]61 participants (Actual)Interventional2017-11-06Completed
A Phase 2 Randomized, Double-blinded, Multicenter and Placebo-controlled Clinical Trial to Evaluate the Safety and Efficacy of Different Doses of Tolvaptan Tablet in Patients With Cirrhotic Ascites [NCT01349335]Phase 2180 participants (Actual)Interventional2009-04-30Completed
A Multicenter, Uncontrolled, Open-label, Dose-titration Trial to Investigate the Efficacy and Safety of Tolvaptan Tablets in Patients With Hyponatremia in Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH) [NCT03048747]Phase 316 participants (Actual)Interventional2017-03-02Completed
A Phase 2, Multi-center, Open-label Study to Determine Long-term Safety, Tolerability and Efficacy of Split-dose Oral Regimens of Tolvaptan Tablets in a Range of 30 to 120 mg/d in Patients With Autosomal Dominant Polycystic Kidney Disease [NCT00413777]Phase 246 participants (Actual)Interventional2005-12-31Completed
A Pilot Phase 3b,Multicenter,Randomized,Double-blind,Placebo-controlled Trial of the Safety,Efficacy,and Pharmacokinetics of Titrated Oral SAMSCA®(Tolvaptan) in Children and Adolescent Subjects With Euvolemic or Hypervolemic Hyponatremia [NCT02442674]Phase 30 participants (Actual)Interventional2015-11-30Withdrawn(stopped due to Trial withdrawn due to inability to meet the trial objectives (Pilot).)
A Phase 3b, Two-part, Multicenter, One Year Randomized, Double-blind, Placebo-controlled Trial of the Safety, Pharmacokinetics, Tolerability, and Efficacy of Tolvaptan Followed by a Two Year Open-label Extension in Children and Adolescent Subjects With Au [NCT02964273]Phase 391 participants (Actual)Interventional2016-09-23Completed
The Effects of Tolvaptan on Renal Handling of Water and Sodium, Vasoactive Hormones and Circulatory System, During Basal Conditions and During Inhibition of the Nitric Oxide System in Healthy Subjects. A Dose-response Study. [NCT02078973]Phase 215 participants (Actual)Interventional2014-03-01Completed
Role of Midodrine and Tolvaptan in Patients With Cirrhosis With Refractory or Recurrent Ascites [NCT02173288]Phase 2/Phase 350 participants (Actual)Interventional2013-07-31Completed
Single Administration of TOLVAptan at a Dosage Used in the Treatment of Hyponatremia: Changes in THIRST and Water Balance in Healthy Volunteers [NCT03931369]Phase 260 participants (Anticipated)Interventional2019-09-06Not yet recruiting
A Randomized, Double-blinded, Multicenter, Placebo Controlled, Parallel Designed Study, to Evaluate the Efficacy and Safety of Tolvaptan Tablet in Treatment of Patients With Cirrhosis Ascites, Using Diuretics as Initial Treatment [NCT01349348]Phase 3535 participants (Actual)Interventional2010-10-31Completed
The Role of Vasopressin Antagonism on Renal Sodium Handling [NCT03910231]Phase 130 participants (Actual)Interventional2012-02-01Completed
Metformin vs Tolvaptan for Treatment of Autosomal Dominant Polycystic Kidney Disease. A Phase 3a, Indipendent, Multicentre, Two Parallel Arms, Randomized Controlled Trial [NCT03764605]Phase 3150 participants (Anticipated)Interventional2019-01-30Not yet recruiting
Comparison of the Relative Oral Bioavailability of Tolvaptan Administered Via Nasogastric Tube to Tolvaptan Tablets Swallowed Intact [NCT01261481]Phase 129 participants (Actual)Interventional2011-01-31Completed
A Phase 3 Randomized, Double-Blind, Placebo Controlled Study of the Short Term Clinical Effects of Tolvaptan in Patients Hospitalized for Worsening Heart Failure With Challenging Volume Management [NCT01584557]Phase 3250 participants (Actual)Interventional2012-06-30Completed
A Multicenter, Open-label Extension Study to Investigate the Long-term Safety and Efficacy of Tolvaptan in Patients With Autosomal Dominant Polycystic Kidney Disease (ADPKD) [Extension of Trial 156-04-251 in Japan] [NCT01280721]Phase 3135 participants (Actual)Interventional2010-11-30Completed
Multi-center, Open-label, Extension Study to Evaluate the Long-term Efficacy and Safety of Oral Tolvaptan Tablet Regimens in Subjects With Autosomal Dominant Polycystic Kidney Disease (ADPKD) [NCT01214421]Phase 31,083 participants (Actual)Interventional2010-05-26Completed
Use of Tolvaptan to Reduce Urinary Supersaturation: a Pilot Proof of Principle Study [NCT02096965]Phase 120 participants (Actual)Interventional2014-03-31Completed
Tolvaptan add-on Therapy to Overcome Loop Diuretic Resistance in Acute Heart Failure With Renal Dysfunction [NCT04331132]128 participants (Anticipated)Interventional2021-12-01Recruiting
A Double-blind, Placebo-controlled Study of OPC-41061 in the Treatment of Cardiac Edema (Congestive Heart Failure) [NCT00462670]Phase 3110 participants (Actual)Interventional2007-04-30Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Dose Response of OPC-41061 in Congestive Heart Failure Patients With Extracellular Volume Expansion [NCT00234104]Phase 2122 participants (Actual)Interventional2004-08-31Completed
AiDing Diuresis wIth Tolvaptan (ADD-IT) [NCT02646540]Phase 114 participants (Actual)Interventional2016-01-31Completed
Randomized, Double-blind, Multicenter, Placebo-controlled (Standard Therapy + Placebo), Phase 2 Efficacy and Safety Study of the Tolvaptan Tablets in Patients With Non-hypovolemic Non-acute Hyponatremia [NCT00664014]Phase 2240 participants (Anticipated)Interventional2008-05-31Completed
[NCT02644616]Phase 440 participants (Actual)Interventional2014-11-30Completed
A Dose Block-randomized, Double-blind, Placebo-controlled, Single Dose, Dose-escalation Study to Investigate the Safety, Tolerance, Pharmacokinetics and Pharmacodynamics of Tolvaptan in Healthy Korean Male Subjects Bipolar Disorder [NCT01014416]Phase 146 participants (Anticipated)Interventional2010-01-31Completed
A Pilot Study To Evaluate The Incidence Of Hyponatremia In A Medical-Surgical Hospital And To Explore The Efficacy And Safety Of Tolvaptan In The Clinical Practice [NCT01386372]Phase 23 participants (Actual)Interventional2011-06-30Terminated(stopped due to futility)
Regional Tolvaptan Registry [NCT02666651]Phase 425 participants (Anticipated)Interventional2016-05-31Recruiting
A Long-term Administration Study of OPC-41061 in Patients With Autosomal Dominant Polycystic Kidney Disease (ADPKD) [Extension of Study 156-04-001] [NCT00841568]Phase 217 participants (Actual)Interventional2006-04-30Completed
Use of Tolvaptan to Treat SIADH-induced Hyponatremia in Selected Patients With Acute Neurological Injuries [NCT02545114]25 participants (Actual)Interventional2015-08-31Terminated(stopped due to Major protocol revision needed, current project terminated after enrollment of 25 patients.)
Randomized Placebo-Controlled Trial of Tolvaptan in Hyponatremic Patients With Cancer [NCT01199198]Phase 452 participants (Actual)Interventional2011-05-31Completed
Longitudinal Efficacy and Safety Study of Tolvaptan on Autosomal Dominant Polycystic Kidney Disease Patients (LET-PKD Study) [NCT02729662]118 participants (Actual)Interventional2016-10-01Active, not recruiting
Postoperative Tolvaptan Use in Left Ventricular Assist Device Implantation Patients [NCT05408104]28 participants (Actual)Observational2019-03-28Completed
The Targeting Acute Congestion With Tolvaptan In Congestive Heart Failure Study [NCT01644331]Phase 3257 participants (Actual)Interventional2012-10-31Completed
Phase 3 Open-label, Study of OPC-41061 in Subjects With Cardiac-induced Edema (Congestive Heart Failure) - an Investigation of the Safety of Treatment Beyond 7 Days and the Effect of Dose Escalation to 30 mg [NCT00544869]Phase 352 participants (Actual)Interventional2007-10-31Completed
Subacute Effect of Tolvaptan on Total Kidney Volume in Adult Patients With Autosomal Dominant Polycystic Kidney Disease [NCT03596957]Phase 490 participants (Anticipated)Interventional2018-09-12Recruiting
A Phase 3, Multi-center, Double-blind, Placebo-controlled, Parallel-arm Trial to Determine Long-term Safety and Efficacy of Oral Tolvaptan Tablets Regimens in Adult Subjects With Autosomal Dominant Polycystic Kidney Disease [NCT00428948]Phase 31,445 participants (Actual)Interventional2007-01-31Completed
Effect of Tolvaptan on Renal Plasma Flow (RPF) and Glomerular Filtration Rate (GFR) in ADPKD [NCT03803124]Phase 320 participants (Actual)Interventional2015-12-31Completed
Variation in the Aquaretic Efficacy of Tolvaptan in Healthy Adults [NCT01973140]Phase 417 participants (Actual)Interventional2013-11-30Completed
A Dose-defining Study of OPC-41061 in Treatment of Hepatic Edema [NCT00479336]Phase 2104 participants (Actual)Interventional2007-06-30Completed
Pharmacokinetics and Clinical Response of Tolvaptan in Neurocritical Care Patients [NCT02215148]1 participants (Actual)Observational2014-11-30Terminated(stopped due to Slow subject enrollment and contracting issues; sponsor decided to abort study)
A Long-term Administration Study of OPC-41061 in Patients With Autosomal Dominant Polycystic Kidney Disease (ADPKD) (2) [Extension of Study 156-05-002] [NCT01022424]Phase 313 participants (Actual)Interventional2009-11-30Completed
A Multi-center, Double-blind, Parallel-arm Study to Investigate Pharmacodynamics and Pharmacokinetics of OPC-41061 in Patients With Hepatic Edema [NCT01114828]Phase 340 participants (Actual)Interventional2010-02-28Completed
A Clinical Pharmacological Study of OPC-41061 in the Treatment of Cardiac Edema (Congestive Heart Failure) [NCT00525265]Phase 320 participants (Actual)Interventional2007-09-30Completed
Phase 3b, Multicenter, Randomized, Single-blind, Parallel Group Trial of the Effects of Titrated Oral SAMSCA(r) (Tolvaptan) 15, 30, or 60 mg QD Compared to Placebo Plus Fluid Restriction on Length of Hospital Stay and Symptoms in Subjects Hospitalized Wit [NCT01227512]Phase 3124 participants (Actual)Interventional2010-10-31Terminated(stopped due to Recruitment challenges and results of interim futility analysis, which showed less than likely to achieve primary endpoint goal-length of hospital stay.)
A Pilot, Phase II Study With a Prospective, Randomized, Cross-Over, Placebo-Controlled, Double-Blind Design to Assess the Short-Term Effects of Tolvaptan Plus Placebo vs Tolvaptan Plus Octreotide LAR Combination Therapy in ADPKD Patients With Normal Kidne [NCT03541447]Phase 220 participants (Actual)Interventional2018-12-12Completed
Study of Nonedematous Hyponatremia and the Utility of Fractional Urate Excretion in Hyponatremia and Suspected Renal Salt Wasting Without Hyponatremia- [NCT01425125]0 participants (Actual)Interventional2011-11-30Withdrawn
Efficacy and Safety of Tolvaptan in Cirrhotic Patients With Hyponatremia - A Multi-center Prospective Cohort Study [NCT01850940]98 participants (Actual)Observational2013-01-31Completed
Primary Mode of Therapy in Acute Decompensated Heart Failure:Comparison Between Usual Care Plus Tolvaptan and Ultrafiltration. [NCT01863511]Phase 445 participants (Actual)Interventional2013-05-31Completed
Revisiting the Human Sweat Gland - Does Arginine Vasopressin Modulate Sweat Sodium Concentration Via the V2 Receptor? [NCT02084797]10 participants (Actual)Interventional2011-06-30Completed
Samsca Post-marketing General Drug Use-results Survey in Patients With Hyponatremia in Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH) in Japan [NCT04790175]300 participants (Anticipated)Observational2021-03-29Recruiting
A Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Investigate the Efficacy of OPC-41061 Administered at a Dose of 7.5 mg in Patients With Hepatic Edema [NCT01050530]Phase 3162 participants (Actual)Interventional2009-12-31Completed
Multicenter, Randomized, Double-blind, Placebo-controlled, Efficacy and Safety Study of the Effects of Titrated Oral Tolvaptan Tablets in Patients With Hyponatremia, Study 2 [NCT00201994]Phase 3243 participants (Actual)Interventional2003-11-30Completed
A Multicenter, Uncontrolled, Open-label Phase 3 Trial of OPC-41061 in Patients With Hepatic Edema - Investigation of the Safety of Treatment at 7.5 mg Beyond 7 Days and of the Effect of Dose Escalation to 15 mg [NCT01048788]Phase 351 participants (Actual)Interventional2009-12-31Completed
Multicenter, Randomized, Double-Blind, Placebo-Controlled, Efficacy and Safety Study of the Effects of Titrated Oral Tolvaptan Tablets in Patients With Hyponatremia [NCT00072683]Phase 3240 participants Interventional2003-04-30Completed
Post-Marketing Surveillance Study of Tolvaptan in Patients With ADPKD in Japan [NCT02847624]1,672 participants (Actual)Observational2014-03-24Completed
A Phase 3b Multicenter Open-label Trial of the Safety, Tolerability, and Efficacy of Tolvaptan in Infants and Children 28 Days to Less Than 12 Weeks of Age With Autosomal Recessive Polycystic Kidney Disease (ARPKD) [NCT04786574]Phase 320 participants (Anticipated)Interventional2022-07-01Recruiting
A Multi-center, Parallel-group, Randomized, Double-blind, Placebo-masked, Multiple Dose Trial of Modified-release (MR) and Immediate-release (IR) Tolvaptan in Subjects With Autosomal Dominant Polycystic Kidney Disease (ADPKD) [NCT01210560]Phase 225 participants (Actual)Interventional2010-10-31Completed
Single Center, Open Labeled Pilot Study Evaluating the Safety and Efficacy of Tolvaptan in Patients With Cirrhotic Ascites [NCT01292304]Phase 410 participants (Actual)Interventional2012-03-31Completed
A Phase 3b, Multicenter, Extension Follow-up Trial to Evaluate the Long-term Safety of Children and Adolescent Subjects With Euvolemic or Hypervolemic Hyponatremia Who Have Previously Participated in a Trial of Titrated Oral SAMSCA® (Tolvaptan) [NCT02020278]Phase 33 participants (Actual)Interventional2016-04-22Terminated(stopped due to Issues with recruitment and enrollment made the trial impossible or highly impracticable. Termination of this trial was not due to safety reasons.)
Multi-Center, Double-Blind Study to Compare the Effects of 30mg Qd Versus 15 Mg Bid of Tolvaptan in Congestive Heart Failure Patients [NCT00043771]Phase 240 participants Interventional2002-05-31Completed
Protocol 156-03-236: Multicenter, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Long Term Efficacy and Safety of Oral Tolvaptan Tablets in Subjects Hospitalized With Worsening Congestive Heart Failure [NCT00071331]Phase 33,600 participants Interventional2003-09-30Completed
A Phase 2, Multicenter, Randomized, Placebo-controlled, Double-blind, Placebo-masked, Parallel-group Pilot Trial to Compare the Efficacy, Tolerability, and Safety of Tolvaptan Modified-release and Immediate-release Formulations in Subjects With Autosomal [NCT01451827]Phase 2178 participants (Actual)Interventional2011-10-31Completed
Multi-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Effect of Single Oral Tolvaptan Tablets on Hemodynamic Parameters in Subjects With Heart Failure [NCT00132886]Phase 2140 participants (Anticipated)Interventional2004-12-31Completed
[NCT00043758]Phase 2170 participants Interventional2002-07-31Completed
Tolvaptan Treatment to Reverse Worsening Outpatient Heart Failure: Possible Role of Copeptin In Identifying Responders (TROUPER) [NCT02476409]Phase 440 participants (Actual)Interventional2015-07-31Completed
International, Multicenter, Study of One-year, Open-label, Titrated Oral Tolvaptan Tablet Administration in Patients With Chronic Hyponatremia: Extension to Studies 156-02-235 and 156-03-238 to Assess One-year Safety [NCT02449044]Phase 3111 participants (Actual)Interventional2004-05-31Completed
Tolvaptan to Reduce Length of Stay in Hospitalized Patients With Cirrhosis and Hyponatremia [NCT01890694]Phase 42 participants (Actual)Interventional2012-03-31Terminated
A Multicenter, Randomized, Double-blind, Placebo-controlled (Standard Therapy + Placebo) Study to Evaluate the Efficacy and Safety of the Tolvaptan Tablets in Patients With Non-hypovolemic Non-acute Hyponatremia [NCT01507727]Phase 2/Phase 3240 participants (Anticipated)Interventional2012-01-31Recruiting
A Multicenter, Double-blind, Randomized, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Tolvaptan in the Treatment of Cardiac-Induced Edema in Patients With Heart Failure [NCT01618448]Phase 385 participants (Actual)Interventional2012-07-31Completed
Effect of Vasopressin Antagonism on Renal Sodium and Water Handling and Circulation During Inhibition of the Nitric Oxide System in Healthy Subjects [NCT01638663]Phase 220 participants (Actual)Interventional2012-05-31Completed
Randomized, Double-blind, Multicenter, Placebo-controlled, Parallel Phase 3 Study to Evaluate the Efficacy and Safety of Tolvaptan in the Treatment of Patients With Cardiac Edema Based on the Conventional Therapy [NCT01651156]Phase 3244 participants (Actual)Interventional2012-07-31Completed
The Use of Tolvaptan to Prevent Renal Dysfunction in High Risk Patients With Acute Decompensated Heart Failure-Pilot Study [NCT01663662]Phase 40 participants (Actual)Interventional2012-08-31Withdrawn(stopped due to Lack of eligible patients)
Efficacy and Safety Study of Tolvaptan for Liver Cirrhotic Patients With Hyponatremia and Ascites: A Multi-center, Randomized, Double-blind, Placebo-controlled 4-weeks Clinical Trial [NCT01716611]Phase 4105 participants (Anticipated)Interventional2012-11-30Not yet recruiting
Acute Heart Failure With High Copeptin Levels Treated With Tolvaptan Targets Increased AVP Activation for Treatment Efficacy [NCT01733134]Phase 3350 participants (Anticipated)Interventional2013-01-31Not yet recruiting
Aquaresis Utility for Hyponatremic Acute Heart Failure Study [NCT02183792]Phase 433 participants (Actual)Interventional2014-12-31Completed
Pilot Study of the Relationship of Ambient Copeptin to the Aquaretic Effects of Tolvaptan in Patients With Heart Failure [NCT01346072]Phase 421 participants (Actual)Interventional2011-04-30Completed
A Phase 1b, Multicenter, Pilot, Randomized, Double-blind Trial to Determine the Pharmacokinetics and Pharmacodynamics of Orally Administered Tolvaptan 3.75, 7.5, and 15 mg Tablets in Subjects With Syndrome of Inappropriate Antidiuretic Hormone Secretion [NCT02009878]Phase 1/Phase 230 participants (Actual)Interventional2013-11-30Completed
A Phase 2, Multi-center, Open-label, Dose-finding Trial to Investigate the Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of OPC-41061 in Patients With Chronic Renal Failure Undergoing Hemodialysis or Hemodiafiltration [NCT01876381]Phase 226 participants (Actual)Interventional2013-06-30Completed
A Phase 3b, Multi-center, Open-label Trial to Evaluate the Long Term Safety of Immediate-release Tolvaptan (OPC-41061, 30 mg to 120 mg/Day, Split Dose) in Subjects With Autosomal Dominant Polycystic Kidney Disease [NCT02251275]Phase 31,803 participants (Actual)Interventional2014-10-17Completed
Effects of Tolvaptan on Cognitive Function, Brain Metabolism and Quality of Life in Hyponatremic Cirrhotics With Hepatic Encephalopathy: A Prospective Clinical Trial [NCT01556646]Phase 325 participants (Actual)Interventional2011-04-30Completed
Efficacy and Safety Evaluation of Tolvaptan in the Treatment of Patients With Right Heart Failure Caused by Pulmonary Arterial Hypertension [NCT05569655]100 participants (Anticipated)Interventional2021-04-06Recruiting
Effect of Samsca on Control of Hyponatremia and Extracellular Fluid in Cirrhotic Patients With Ascites [NCT01552590]Phase 474 participants (Actual)Interventional2012-04-30Terminated
A Pilot, Phase 3B, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel Group Study of the Effects of Titrated Oral Tolvaptan 15, 30, or 60 mg QD on Cognitive and Neurological Function in Elderly Hyponatremic Patients [NCT00550459]Phase 357 participants (Actual)Interventional2007-08-31Completed
Tolvaptan for the Management of Acute Decompensated Heart Failure in Patients With Advanced or Refractory Heart Failure [NCT02959411]Phase 49 participants (Actual)Interventional2016-10-31Terminated(stopped due to Low accrual rate)
A Multicenter, Open-label, Dose-finding Trial of OPC-41061 to Investigate Efficacy, Pharmacokinetics, Pharmacodynamics, and Safety in Patients With Carcinomatous Edema (Phase 2) [NCT01684202]Phase 243 participants (Actual)Interventional2012-07-31Completed
Comparison of Oral Thiazides vs Intravenous Thiazides vs Tolvaptan in Combination With Loop Diuretics for Diuretic Resistant Decompensated Heart Failure [NCT02606253]Phase 460 participants (Actual)Interventional2016-02-29Completed
A Multi-center,_double-blind,_pararel-group Comparison Trial to Investigate the Effect of Short-term Administration of Tolvaptan on Mid- to Long-term Prognosis of Heart Failure Patients (Phase_4 Study) [NCT01439009]Phase 4100 participants (Actual)Interventional2011-09-30Completed
A Phase 3b, Multicenter, Open-label, Randomized Withdrawal Trial of the Effects of Titrated Oral SAMSCA ® (Tolvaptan) on Serum Sodium, Pharmacokinetics, and Safety in Children and Adolescent Subjects Hospitalized With Euvolemic or Hypervolemic Hyponatremi [NCT02012959]Phase 39 participants (Actual)Interventional2015-09-22Terminated(stopped due to Issues with participant recruitment & enrollment which made the trial impossible or highly impracticable. Trial termination was not due to safety reasons.)
A Phase 3b Multicenter Open-label Trial of the Safety, Tolerability, and Efficacy of Tolvaptan in Infants and Children 28 Days to Less Than 18 Years of Age With Autosomal Recessive Polycystic Kidney Disease (ARPKD) [NCT04782258]Phase 310 participants (Anticipated)Interventional2022-07-15Recruiting
A Phase 2, Multi-center, Open-label, Dose-finding Trial to Investigate the Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of OPC-41061 in Patients With Chronic Renal Failure Undergoing Peritoneal Dialysis [NCT01895322]Phase 220 participants (Actual)Interventional2013-07-31Completed
Assessment of Clinical Outcome and Treatment Quality Under Adequate Use of Tolvaptan In Correction of Hyponatremia in Patients Hospitalized With Worsening Heart Failure and Hyponatremia [NCT02352285]Phase 458 participants (Actual)Interventional2012-12-31Terminated
To Study Effect of the Combination of Midodrine and Tolvaptan Versus Tolvaptan Alone in Patients With Severe Hyponatremia in Cirrhosis(TOLMINA Trial) - An Open Label Placebo Randomized Control Trial [NCT05060523]220 participants (Anticipated)Interventional2021-09-19Recruiting
A Phase 2, Multicenter, Placebo-controlled, Double-blind, Randomized, Parallel-group Trial to Investigate the Efficacy and Safety of Orally Administered Tolvaptan (OPC-41061) in Patients With Chronic Renal Failure Undergoing Hemodialysis or Hemodiafiltrat [NCT02331680]Phase 2124 participants (Actual)Interventional2014-12-31Completed
Use of Tolvaptan, a Vasopressin Antagonist, to Increase Urine Dilution and Reduce Cystine Urolithiasis Among Patients With Homozygous Cystinuria: a Pilot Investigation [NCT02538016]4 participants (Actual)Interventional2016-10-31Completed
A Phase 3b, Multi-center, Randomized-withdrawal, Placebo-controlled, Double-blind, Parallel-group Trial to Compare the Efficacy and Safety of Tolvaptan (45 to 120 mg/Day, Split-dose) in Subjects With Chronic Kidney Disease Between Late Stage 2 to Early St [NCT02160145]Phase 31,370 participants (Actual)Interventional2014-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00234104 (1) [back to overview]Body Weight
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Bedtime.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to First Daily Dose- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to First Daily Dose.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Abdominal Girth Measurement- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Second Daily Dose- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Second Daily Dose.
NCT00413777 (21) [back to overview]Percent Change From Baseline in Renal Volume-Extension.
NCT00413777 (21) [back to overview]Percent Change From Baseline in Renal Volume.
NCT00413777 (21) [back to overview]Safety Assessments Based on Vital Signs, Electrocardiogram (ECG's), Clinical Laboratory Tests, Physical Examinations Are Reported as Adverse Events (AEs) Upon Study Physician Discretion.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Diastolic Blood Pressure (dBP) for Hypertension Assessment.
NCT00413777 (21) [back to overview]Change From Pre-dose Baseline in Renal Function Estimated by Glomerular Filtration Rate (GFR).
NCT00413777 (21) [back to overview]Change From Pre-dose Baseline in Renal Function Estimated by GFR- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Abdominal Girth Measurement.
NCT00413777 (21) [back to overview]Mean Change From Baseline in dBP for Hypertension Assessment- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in MAP for Hypertension Assessment- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Mean Arterial Pressure (MAP) for Hypertension Assessment.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Patient-assessed Renal Pain Scale- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Patient-assessed Renal Pain Scale.
NCT00413777 (21) [back to overview]Mean Change From Baseline in sBP for Hypertension Assessment- Extension.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Systolic Blood Pressure (sBP) for Hypertension Assessment.
NCT00413777 (21) [back to overview]Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Bedtime- Extension.
NCT00428948 (7) [back to overview]Change in Mean Arterial Blood Pressure Per Year in Non-hypertensive Participants From Baseline to Month 36
NCT00428948 (7) [back to overview]Area Under the Concentration-time Curve of Change in Renal Pain From Baseline to Month 36
NCT00428948 (7) [back to overview]Number of Hypertensive Events Per 100 Follow-up Years in Non-hypertensive Participants From Baseline to Month 36
NCT00428948 (7) [back to overview]Percentage of Participants With a Clinically Sustained Decrease of Blood Pressure Leading to a Sustained Reduction in Antihypertensive Therapy From Baseline to Month 36
NCT00428948 (7) [back to overview]Number of ADPKD Clinical Progression Events Per 100 Follow-up Years From Baseline to Month 36
NCT00428948 (7) [back to overview]Change in Renal Function Per Year From Week 3 to Month 36
NCT00428948 (7) [back to overview]Percentage Change Per Year in Total Kidney Volume From Baseline to Month 36
NCT00462670 (2) [back to overview]Body Weight (Percent Change)
NCT00462670 (2) [back to overview]Body Weight (Amount of Change)
NCT00479336 (2) [back to overview]Abdominal Circumference
NCT00479336 (2) [back to overview]Body Weight (Amount of Change)
NCT00525265 (1) [back to overview]Body Weight
NCT00544869 (1) [back to overview]Body Weight
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: ST Segment
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: Right Bundle Branch Block (RBBB), Left Bundle Branch Block (LBBB), Myocardial Infarction (MI)
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: QTcF Increase 30-60 Msec
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: QTcB Increase 30-60 Msec
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: QT >500 Milliseconds (Msec)
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: QRS Interval
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: Arrhythmia
NCT00550459 (29) [back to overview]Change From Baseline to Day 22 in the Individual Neurocognitive Domains Included in the Primary Endpoint: Reaction Time in Computer Tests
NCT00550459 (29) [back to overview]Change From Baseline in the Neurocognitive Composite Score of Speed Domains (NCS-SD; Sum of All Correct Speed Domain Z-Scores)
NCT00550459 (29) [back to overview]Change From Baseline in the Individual Neurocognitive Domains Included in the Primary Endpoint: Psychomotor Speed Via Morse Tapping Test
NCT00550459 (29) [back to overview]Change From Baseline in the Individual Neurocognitive Domains Included in the Primary Endpoint: Processing Speed of Rapid Visual Information Processing Test, Numeric Working Memory Test, and Word Recognition Test
NCT00550459 (29) [back to overview]Change From Baseline in Serum Sodium; ITT Population
NCT00550459 (29) [back to overview]Change From Baseline in Postural Stability Test
NCT00550459 (29) [back to overview]Change From Baseline in Overall Neurocognitive Composite Score
NCT00550459 (29) [back to overview]Change From Baseline in Gait Test (Timed Get-Up-and-Go Test)
NCT00550459 (29) [back to overview]Number of Patients With Vital Sign Abnormalities: Pulse Rate
NCT00550459 (29) [back to overview]Number of Patients With Vital Sign Abnormalities: Body Weight
NCT00550459 (29) [back to overview]Number of Patients With Vital Sign Abnormalities: Body Temperature
NCT00550459 (29) [back to overview]Number of Patients With Vital Sign Abnormalities: Blood Pressure
NCT00550459 (29) [back to overview]Number of Patients With Serum Chemistry Laboratory Abnormalities: Uric Acid
NCT00550459 (29) [back to overview]Number of Patients With Serum Chemistry Laboratory Abnormalities: Magnesium
NCT00550459 (29) [back to overview]Number of Patients With Serum Chemistry Laboratory Abnormalities: Glucose
NCT00550459 (29) [back to overview]Number of Patients With Serum Chemistry Laboratory Abnormalities: Cholesterol
NCT00550459 (29) [back to overview]Number of Patients With Serum Chemistry Laboratory Abnormalities: Blood Urea Nitrogen (BUN)
NCT00550459 (29) [back to overview]Number of Patients With Hematology Laboratory Abnormalities: Neutrophils
NCT00550459 (29) [back to overview]Number of Patients With Hematology Laboratory Abnormalities: Lymphocytes
NCT00550459 (29) [back to overview]Number of Patients With Hematology Laboratory Abnormalities: Hemoglobin
NCT00550459 (29) [back to overview]Number of Patients With Hematology Laboratory Abnormalities: Activated Partial Thromboplastin Time (aPTT)
NCT00550459 (29) [back to overview]Number of Patients With Electrocardiogram (ECG) Abnormalities: T Wave
NCT00841568 (2) [back to overview]Renal Function Test (eGFR)
NCT00841568 (2) [back to overview]Total Kidney Volume
NCT01022424 (2) [back to overview]Total Kidney Volume
NCT01022424 (2) [back to overview]Renal Function Test (eGFR)
NCT01048788 (1) [back to overview]Body Weight
NCT01050530 (2) [back to overview]Ascites Volume
NCT01050530 (2) [back to overview]Body ｗeight
NCT01114828 (2) [back to overview]Ascites Volume as Measured by CT
NCT01114828 (2) [back to overview]Body Weight
NCT01199198 (2) [back to overview]Participants Whose Serum Sodium Concentration Corrected to at Least 135 mEq/L on Day 14
NCT01199198 (2) [back to overview]Length of Stay in Hospital
NCT01210560 (20) [back to overview]Change From Baseline in Urine Volume at 24 Hours at Day 7.
NCT01210560 (20) [back to overview]Maximum (Peak) Plasma Concentration of the Drug [Cmax] and Minimum (Trough) Plasma Concentration of the Drug [Cmin] After Tolvaptan Treatment on Day 7.
NCT01210560 (20) [back to overview]Number of Participants With Urine Osmolality < 300 mOsm/kg at 23.5 Hours Postdose.
NCT01210560 (20) [back to overview]Ranking of Treatment Tolerability.
NCT01210560 (20) [back to overview]Change From Baseline in Urine Osmolality Area Under the Concentration-time Curve From Time 0 to 24 Hours Postdose (AUC0-24h) at Day 7.
NCT01210560 (20) [back to overview]Area Under the Concentration-time Curve During the Dosing Interval at Steady State and Area Under the Concentration-time Curve From Time 0 to 24 Hours Postdose (AUCT & AUC0-24h) After Tolvaptan Treatment on Day 7.
NCT01210560 (20) [back to overview]Ranking of Treatment Tolerability.
NCT01210560 (20) [back to overview]Number of Participants Experiencing Urinary Urgency Based on Urinary Urgency Questionnaire (Question 1) at Baseline and Day 6.
NCT01210560 (20) [back to overview]Number of Participants Experiencing Urinary Frequency Based on Urinary Frequency Questionnaire (Question 1) at Baseline and Day 6.
NCT01210560 (20) [back to overview]Change From Baseline in Urine Volume by Interval at Day 7.
NCT01210560 (20) [back to overview]Duration of Urine Osmolality Less Than 300 mOsm/kg at Baseline and Day 7.
NCT01210560 (20) [back to overview]Change From Baseline in Urine Osmolality at Day 7.
NCT01210560 (20) [back to overview]Change From Baseline in Urinary Urgency Questionnaire (Questions 2 to 5 and Questions 7 to 14) at Day 6.
NCT01210560 (20) [back to overview]Change From Baseline in Urinary Frequency Questionnaire (Question 2 and Questions 3 to 10) at Day 6.
NCT01210560 (20) [back to overview]Ranking of Treatment Tolerability.
NCT01210560 (20) [back to overview]Ranking of Treatment Tolerability.
NCT01210560 (20) [back to overview]Change From Baseline in Symptom Burden by Autosomal Dominant Polycystic Kidney Disease (ADPKD) Nocturia Quality of Life Questionnaire at Day 6.
NCT01210560 (20) [back to overview]Change From Baseline in Number of Urine Voids During Sleep Periods.
NCT01210560 (20) [back to overview]Change From Baseline in Number of Urine Voids During Awake Periods.
NCT01210560 (20) [back to overview]Time to Maximum (Peak) Plasma Concentration (Tmax) After Tolvaptan Treatment on Day 7.
NCT01214421 (6) [back to overview]Annualized Slope of eGFR (CKD-EPI) for Study 156-04-251 Participants Enrolled in Study 156-08-271
NCT01214421 (6) [back to overview]Percent Change From the Baseline in Total Kidney Volume (TKV) for Study 156-04-251 Participants Enrolled in This Study (156-08-271)
NCT01214421 (6) [back to overview]Annualized Slope of Renal Function (eGFRCKD-EPI) for Study 156-04-251 Placebo Participants Enrolled in Study 156-08-271
NCT01214421 (6) [back to overview]Annualized Slope of Total Kidney Volume (TKV) for Study 156-04-251 Participants Enrolled in Study 156-08-271
NCT01214421 (6) [back to overview]Annualized TKV Slope for Study 156-04-251 Placebo Participants Enrolled in Study 156-08-271
NCT01214421 (6) [back to overview]Change From the Baseline in Estimated Glomerular Filtration Rate (eGFR) as Assessed by Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) for Study 156-04-251 Participants Enrolled in This Study (156-08-271)
NCT01227512 (8) [back to overview]Change From Baseline in Serum Sodium Concentration (24 Hour Area Under the Curve [AUC]).
NCT01227512 (8) [back to overview]Change From Baseline to 48 Hours Post Dose in Clinical Global Impression - Improvement (CGI-I) Score of Hyponatremia Symptoms.
NCT01227512 (8) [back to overview]Length of Hospital Stay (LoS)
NCT01227512 (8) [back to overview]Percentage of Participants With Clinical Global Impression-Improvement (CGI-I) Score Improved to a Score of 1 or 2.
NCT01227512 (8) [back to overview]Time to First 2-point Improvement in CGI-S Score.
NCT01227512 (8) [back to overview]Change From Baseline to 24 and 72 Hours Post Dose in CGI-S of Hyponatremia Symptoms.
NCT01227512 (8) [back to overview]Percentage of Participants Requiring Rescue Therapy for Hyponatremia
NCT01227512 (8) [back to overview]Change From Baseline to 48 Hour Post Dose in Clinical Global Impression-Severity (CGI-S) of Hyponatremia Symptoms.
NCT01280721 (3) [back to overview]Renal Function Test (eGFR)
NCT01280721 (3) [back to overview]Renal Function Test (Cys-C)
NCT01280721 (3) [back to overview]Total Kidney Volume
NCT01292304 (5) [back to overview]Number of Patients With Abnormally Low Levels of Sodium (Sodium Levels Between 130 mmol/L and 135 mmol/L)
NCT01292304 (5) [back to overview]Number of Participants With Worsening Ascites (Increase in Number of Paracentesis Procedures to Remove 2 Liters of Ascites Fluid)
NCT01292304 (5) [back to overview]Time From Baseline to Worsening Ascites (Requiring 1 or More Therapeutic Paracentesis to Remove Ascites Fluid)
NCT01292304 (5) [back to overview]Number of Subjects With Worsening Ascites (Defined as Greater Than 2 kg Weight Gain)
NCT01292304 (5) [back to overview]Number of Patients With Reduction of Ascites (Weight Loss of 2 kg or More)
NCT01336972 (10) [back to overview]Mean Change From Baseline in Measured Glomerular Filtration Rate (mGFR) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01336972 (10) [back to overview]Area Under the Concentration-time Curve From 0 to 5 Hours (AUC0-5) After 3 Weeks of Tolvaptan Treatment.
NCT01336972 (10) [back to overview]Time to Peak Plasma Concentration (Cmax) After 3 Weeks of Tolvaptan Treatment.
NCT01336972 (10) [back to overview]Time to Peak Plasma Concentration (Tmax) After 3 Weeks of Tolvaptan Treatment.
NCT01336972 (10) [back to overview]Mean Change From Baseline in 2 Hour Urine Volume After 3 Weeks Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01336972 (10) [back to overview]Mean Change From Baseline in 24 Hour Urine Volume After 3 Weeks Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01336972 (10) [back to overview]Mean Change From Baseline in Effective Renal Plasma Flow (ERPF) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01336972 (10) [back to overview]Mean Change From Baseline in Filtration Fraction (GFR/ERFP) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01336972 (10) [back to overview]Mean Change From Baseline in Free Water Clearance After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment
NCT01336972 (10) [back to overview]Percentage Change From Baseline in Total Kidney Volume (TKV) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.
NCT01346072 (2) [back to overview]Body Weight
NCT01346072 (2) [back to overview]Urine Output
NCT01439009 (13) [back to overview]Plasma Brain Natriuretic Peptide (BNP) Concentration
NCT01439009 (13) [back to overview]Third Heart Sound
NCT01439009 (13) [back to overview]Pulmonary Rales
NCT01439009 (13) [back to overview]Pulmonary Congestion
NCT01439009 (13) [back to overview]Body Weight
NCT01439009 (13) [back to overview]Cardiothoracic Ratio
NCT01439009 (13) [back to overview]Change in Liver Size From Baseline
NCT01439009 (13) [back to overview]Cummulative Incidence of Events at Week 26
NCT01439009 (13) [back to overview]Dypnea
NCT01439009 (13) [back to overview]Jugular Venous Distension
NCT01439009 (13) [back to overview]Number of Subjects Whose Lower Limb Edema Severity Grading Improved by One or More Grade
NCT01439009 (13) [back to overview]Mortality （Number of Death）
NCT01439009 (13) [back to overview]Number of Subjects Whose New York Heart Association (NYHA) Classification Improved by One More Grade From Baseline
NCT01451827 (3) [back to overview]Percent Change From Baseline in TKV at Week 8.
NCT01451827 (3) [back to overview]Percent Change From Baseline in Total Kidney Volume (TKV) at Week 3
NCT01451827 (3) [back to overview]Change From Baseline in Total Score of the Autosomal Dominant Polycystic Kidney Disease Urinary Impact Scale (ADPKD-UIS)
NCT01644331 (14) [back to overview]All Cause Death or Rehospitalization
NCT01644331 (14) [back to overview]Days Hospitalized or Deceased
NCT01644331 (14) [back to overview]Development of Worsening Renal Function
NCT01644331 (14) [back to overview]Dyspnea Improvement Measured by Likert Scale at 8 and 24 Hours
NCT01644331 (14) [back to overview]Renal Function
NCT01644331 (14) [back to overview]Hospital Stay
NCT01644331 (14) [back to overview]Over-diuresis
NCT01644331 (14) [back to overview]Worsening or Persistent Heart Failure or Death
NCT01644331 (14) [back to overview]Dyspnea 11 Point NRS
NCT01644331 (14) [back to overview]Dyspnea Likert
NCT01644331 (14) [back to overview]Fluid Loss
NCT01644331 (14) [back to overview]Freedom From Congestion
NCT01644331 (14) [back to overview]Serum Sodium
NCT01644331 (14) [back to overview]Weight Loss
NCT01684202 (2) [back to overview]Change in Body Weight From Baseline at Final IMP Administration
NCT01684202 (2) [back to overview]Change in Ascites Volume From Baseline Measured by Computer Tomography (CT) at Final IMP Administration
NCT01876381 (2) [back to overview]Change From Baseline in Daily Urine Volume
NCT01876381 (2) [back to overview]Change From Baseline in Total Fluid Removal Per Week by Dialysis
NCT01895322 (4) [back to overview]Change in Body Weight From Baseline
NCT01895322 (4) [back to overview]Change in Daily Urine Volume From Baseline
NCT01895322 (4) [back to overview]Percent Change in Body Weight
NCT01895322 (4) [back to overview]Percent Change in Daily Urine Volume From Baseline
NCT02009878 (9) [back to overview]Change From Baseline in Fluid Balance (Fluid Intake Minus Urine Output) From 0-6 Hours, 0-12 Hours and 0-24 Hours.
NCT02009878 (9) [back to overview]Maximal Increase From Baseline in Serum Sodium Concentration Following Tolvaptan Administration.
NCT02009878 (9) [back to overview]Time of Maximal Increase From Baseline in Serum Sodium Concentration Following Tolvaptan Administration.
NCT02009878 (9) [back to overview]Tmax (Time to Maximum (Peak) Plasma Concentration) for Tolvaptan in Plasma
NCT02009878 (9) [back to overview]Change From Baseline in Cumulative Urine Volume at 0-6 Hours, 0-12 Hours and 0-24 Hours.
NCT02009878 (9) [back to overview]Change From Baseline in Fluid Intake From 0-6 Hours, 0-12 Hours and 0-24 Hours
NCT02009878 (9) [back to overview]Change From Baseline in Serum Sodium Concentrations
NCT02009878 (9) [back to overview]AUC Infinity (Area Under the Concentration-time Curve From Time Zero to Infinity) for Tolvaptan in Plasma
NCT02009878 (9) [back to overview]Cmax (Maximum (Peak) Plasma Concentration) for Tolvaptan in Plasma.
NCT02012959 (3) [back to overview]Change In Serum Sodium Concentration For Responders
NCT02012959 (3) [back to overview]Change In Serum Sodium Concentration During Treatment Phase A
NCT02012959 (3) [back to overview]Fluid Balance (Intake Minus Output) During Treatment Phase A
NCT02020278 (8) [back to overview]Change From Baseline In PedsQL GCS Psychosocial Health Summary Score At Month 6
NCT02020278 (8) [back to overview]Change From Baseline In PedsQL Multidimensional Fatigue Scale (MFS) Total Score At Month 6
NCT02020278 (8) [back to overview]Participants With A Tanner Staging Score Of 1 At Month 6
NCT02020278 (8) [back to overview]Change From Baseline In Alanine Aminotransferase (ALT) And Aspartate Aminotransferase (AST) For Participants On Tolvaptan At Month 2
NCT02020278 (8) [back to overview]Change From Baseline In Growth Percentiles For Body Height And Weight At Month 6
NCT02020278 (8) [back to overview]Change From Baseline In Bilirubin For Participants On Tolvaptan At Month 2
NCT02020278 (8) [back to overview]Change From Baseline In Pediatric Quality of Life Inventory (PedsQL) Generic Core Scale (GCS) Total Score At Month 6
NCT02020278 (8) [back to overview]Change From Baseline In PedsQL GCS Physical Health Summary Score At Month 6
NCT02084797 (4) [back to overview]Blood Sodium Concentration
NCT02084797 (4) [back to overview]Saliva Sodium Concentration
NCT02084797 (4) [back to overview]Sweat Sodium Concentration Obtained After the Steady-state Portion of the Trial
NCT02084797 (4) [back to overview]Urine Sodium Concentration After the Steady-state Portion of the Trial
NCT02160145 (4) [back to overview]Mean Change From Baseline in Urine Osmolality During the Double-blind Treatment Period and Post-treatment Follow-up
NCT02160145 (4) [back to overview]Mean Annualized Slope of eGFR Change
NCT02160145 (4) [back to overview]Mean Change From Baseline in Urine Specific Gravity During the Double-blind Treatment Period and Post-treatment Follow-up
NCT02160145 (4) [back to overview]The Mean Annualized Change in eGFR From Pretreatment Baseline to Post-treatment Follow-up.
NCT02183792 (2) [back to overview]Median Urine Output at 24 Hours Post Randomization
NCT02183792 (2) [back to overview]Median Change in Serum Creatinine at 24 Hours Post Randomization
NCT02251275 (1) [back to overview]Number Of Participants Reporting Treatment-Emergent Adverse Events (TEAEs)
NCT02331680 (2) [back to overview]Change in Total Volume of Fluid Removed by Dialysis Per Week
NCT02331680 (2) [back to overview]Change From Baseline in Daily Urine Volume
NCT02449044 (15) [back to overview]Number of Participants Requiring Prescription of Hypertonic Saline
NCT02449044 (15) [back to overview]Percentage of Participants Requiring Prescription of Other Medicines
NCT02449044 (15) [back to overview]Change From Baseline in Percentage of Participants With Mild Hyponatremia
NCT02449044 (15) [back to overview]Change From Baseline in Percentage of Participants With Normal Sodium Levels
NCT02449044 (15) [back to overview]Change From Baseline in Percentage of Participants With Severe Hyponatremia
NCT02449044 (15) [back to overview]Mean Change From Baseline in Serum Sodium Measurements
NCT02449044 (15) [back to overview]Mean Change From Baseline in SF-12 (Health Survey) Mental Component Summary (MCS)
NCT02449044 (15) [back to overview]Mean Change From Baseline in SF-12 (Health Survey) Physical Component Summary (PCS)
NCT02449044 (15) [back to overview]Participants With Adverse Events (AEs)
NCT02449044 (15) [back to overview]Participants With Laboratory Values Abnormalities Reported as TEAEs
NCT02449044 (15) [back to overview]Participants With Body Weight Abnormalities Reported as TEAEs
NCT02449044 (15) [back to overview]Participants With Electrocardiogram (ECG) Related Abnormalities Reported as TEAEs
NCT02449044 (15) [back to overview]Participants With Vital Signs Abnormalities Reported as Treatment Emergent Adverse Events (TEAEs)
NCT02449044 (15) [back to overview]Percentage of Participants Requiring Prescription of Fluid Restriction
NCT02449044 (15) [back to overview]Mean Change From Baseline in Body Weight by Visit for Those Participants Who Had Clinical Evidence of Hypervolemia at Baseline
NCT02476409 (7) [back to overview]Change in Loop Diuretic Score Defined Based on Change in Loop Diuretic Use
NCT02476409 (7) [back to overview]Number of Participants With a Decrease in Loop Diuretic Dosing at 48 Hours
NCT02476409 (7) [back to overview]Change in Body Weight at 48 Hours
NCT02476409 (7) [back to overview]Change in Body Weight at 48 Hours Stratified by Copeptin
NCT02476409 (7) [back to overview]Change in Body Weight at Day 8
NCT02476409 (7) [back to overview]Changes in Visual Analog Scale - Patient Dyspnea
NCT02476409 (7) [back to overview]Change in Loop Diuretic Dose (Furosemide Milligram Equivalents) at 48 Hours
NCT02538016 (2) [back to overview]Urinary Cystine Supersaturation (mg/L) at High Dose (Day7-8)
NCT02538016 (2) [back to overview]Urine Osmolality at High Dose (Day 8)
NCT02606253 (18) [back to overview]Number of Patients With Escalation of Loop Diuretic Therapy
NCT02606253 (18) [back to overview]Change in eGFR From Baseline to 48 Hours
NCT02606253 (18) [back to overview]Number of Patients With In-hospital Mortality
NCT02606253 (18) [back to overview]Number of Patients With New Inotrope Utilization
NCT02606253 (18) [back to overview]Number of Patients With Renal Replacement Therapy Utilization
NCT02606253 (18) [back to overview]Number of Patients With Symptomatic Hypotension
NCT02606253 (18) [back to overview]Potassium Supplementation
NCT02606253 (18) [back to overview]Weight Change Over 48 Hours
NCT02606253 (18) [back to overview]Change in Patient Congestion Score
NCT02606253 (18) [back to overview]Change in Serum Chloride From Baseline
NCT02606253 (18) [back to overview]Diuretic Efficiency
NCT02606253 (18) [back to overview]Mean Change in Glomerular Filtration Rate at Discharge
NCT02606253 (18) [back to overview]Mean Change in Serum Creatinine
NCT02606253 (18) [back to overview]Mean Change in Serum Potassium
NCT02606253 (18) [back to overview]Mean Change in Serum Sodium
NCT02606253 (18) [back to overview]Net Urine Output
NCT02606253 (18) [back to overview]Number of Patients With Cardiac Arrhythmias
NCT02606253 (18) [back to overview]Number of Patients With Hypokalemia
NCT02964273 (25) [back to overview]Phase A: 24-hour Sodium Clearance
NCT02964273 (25) [back to overview]Phase A: 24-hour Creatinine Clearance
NCT02964273 (25) [back to overview]Phase A: 24-hour Free Water Clearance
NCT02964273 (25) [back to overview]Phase A: 24-hour Free Water Clearance
NCT02964273 (25) [back to overview]Phase A: 24-hour Sodium Clearance
NCT02964273 (25) [back to overview]Phase B: Percentage of Each Tanner Stage by Gender and Age Compared to Normative Populations
NCT02964273 (25) [back to overview]Phase B: Percent Change From Phase B Baseline in htTKV as Measured by MRI at Month 12 and Month 24
NCT02964273 (25) [back to overview]Phase B: Change From Phase B Baseline in Renal Function (eGFR by Schwartz Formula) at Each Clinic Visit in Phase B
NCT02964273 (25) [back to overview]Phase B: Change From Baseline in Growth Percentile by Gender and Age
NCT02964273 (25) [back to overview]Phase B: Change From Baseline in Creatinine Value
NCT02964273 (25) [back to overview]Phase A: Percentage of Each Tanner Stage by Gender and Age Compared to Normative Populations
NCT02964273 (25) [back to overview]Phase A: Change From Baseline in Spot Urine Osmolality (Pre-morning Dose)
NCT02964273 (25) [back to overview]Phase A: Change From Baseline in Specific Gravity (Pre-morning Dose)
NCT02964273 (25) [back to overview]Phase A: Change From Baseline in Renal Function (Estimated Glomerular Filtration Rate [eGFR] by Schwartz Formula) at Each Clinic Visit in Phase A
NCT02964273 (25) [back to overview]Phase A and B: Mean 24-hour Fluid Balance Prior to Week 1
NCT02964273 (25) [back to overview]Phase A: Change From Baseline in Growth Percentile by Gender and Age
NCT02964273 (25) [back to overview]Phase A: Change From Baseline in Creatinine Value
NCT02964273 (25) [back to overview]Phase A: 24-hour Creatinine Clearance
NCT02964273 (25) [back to overview]Phase A and B: Percentage of Participants With Potentially Clinically Significant Abnormalities in Vital Signs
NCT02964273 (25) [back to overview]Phase A and B: Percentage of Participants With Potentially Clinically Significant Abnormalities in Laboratory Test Results Including Liver Function Tests (LFTs)
NCT02964273 (25) [back to overview]Phase A: Percent Change From Phase A Baseline in Height-Adjusted Total Kidney Volume (htTKV) as Measured by Magnetic Resonance Imaging (MRI)
NCT02964273 (25) [back to overview]Phase A: 24-hour Urine Volume
NCT02964273 (25) [back to overview]Phase A: 24-hour Fluid Intake
NCT02964273 (25) [back to overview]Phase A: 24-hour Fluid Balance
NCT02964273 (25) [back to overview]Phase A and B: Percentage of Participants With Aquaretic Adverse Events (AEs)
NCT02994394 (2) [back to overview]Area Under the Concentration-time Curve From Time Zero to the Last Observable Concentration at Time t (AUCt) of of Tolvaptan
NCT02994394 (2) [back to overview]Maximum Plasma Concentration (Cmax) of Tolvaptan
NCT03048747 (2) [back to overview]Percentage of Subjects With Normalized Serum Sodium Concentration on the Day After Final IMP Administration
NCT03048747 (2) [back to overview]Change in Serum Sodium Concentration
NCT03254108 (2) [back to overview]Area Under the Concentration-time Curve From Time Zero to 24 Hours (AUC24h) on Day 1
NCT03254108 (2) [back to overview]Maximum Plasma Concentration (Cmax) of OPC-41061 on Day 1
NCT03772041 (5) [back to overview]Improvement Rate for Lower Limb Edema and Pulmonary Congestion
NCT03772041 (5) [back to overview]Percentage of Subjects Who Achieve Resolution of Pulmonary Rales and Third Cardiac Sound
NCT03772041 (5) [back to overview]Improvement Rate for New York Heart Association (NYHA) Classification
NCT03772041 (5) [back to overview]Change From Baseline in Body Weight
NCT03772041 (5) [back to overview]Change From Baseline in Jugular Venous Distension and Hepatomegaly

Body Weight

The body weight change from baseline following final trial drug administration (NCT00234104)
Timeframe: Baseline, at the time of final trial drug administration

InterventionKg (Mean)
Placebo-0.53
15 mg of OPC-41061-1.62
30 mg of OPC-41061-1.35
45 mg of OPC-41061-1.85

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Bedtime.

"Urine osmolality at steady state (after at least 4 days of dosing) including average of troughs (the mean urine osmolality prior to bedtime).~Samples for this assessment were to be taken as closely coincident to PK blood sample as practical. During Weeks 1, 2, 3 and 4 of the Titration Period and at Month 6, additional samples were collected for the preceding day at bedtime. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration." (NCT00413777)
Timeframe: Baseline to Month 24

,
InterventionmOsm/kg (Mean)
Month 2 (N= 21, 22)Month 6 (N= 19, 23)Month 12 (16, 18)Month 24 (N= 1, 7)
Tolvaptan 45+15 mg-275.00-327.41-283.21-263.00
Tolvaptan 60+30 mg-291.09-301.83-245.83-246.00

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to First Daily Dose- Extension.

Spot urine osmolality at trough was determined for urine samples collected immediately prior to morning dosing for Day 1 (Baseline), Months 2, 6, 12, 24, 36, Extension Day 1, and Extension Month 12 for all participants. Sample was taken after the first morning's void and was provided as a mid-stream, clean catch sample. During the titration period (Weeks 1, 2, 3 and 4) and at Month 6, additional samples were collected for the preceding day immediately preceding the 2nd daily dose and at bed-time. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration. At the Month 36 visit, participants were given a urine container and brought back the specimen at Extension Day 1. All participants were fasting. (NCT00413777)
Timeframe: Baseline to Months 2, 6, 12, 24, 36, Extension Day 1, Extension Month 12

,
InterventionmOsm/kg (Mean)
Month 2 (N= 17, 17)Month 6 (N= 17, 18)Month 12 (N= 16, 17)Month 24 (N= 17, 17)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 17)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-328.06-270.94-234.56-164.06-234.71-54.59-115.59
Tolvaptan 60+30 mg-176.88-223.50-155.65-160.06-196.33-157.18-202.44

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to First Daily Dose.

Spot urine osmolality at trough was determined for urine samples collected immediately prior to morning dosing for Day 1 (Baseline), Months 2, 6, 12, 24, 36 for all participants. Sample was taken after the first morning's void and was provided as a mid-stream, clean catch sample. During the titration period (Weeks 1, 2, 3 and 4) and at Month 6, additional samples were collected for the preceding day immediately preceding the 2nd daily dose and at bed-time. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration. At the Month 36 visit, participants were given a urine container and brought back the specimen at Extension Day 1. All participants were fasting. (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionmOsm/kg (Mean)
Month 2 (N= 21, 22)Month 6 (N= 19, 23)Month 12 (N= 17, 21)Month 24 (N= 18, 20)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg-274.10-288.42-227.29-170.17-222.50
Tolvaptan 60+30 mg-228.00-263.78-178.43-189.75-208.90

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Mean Change From Baseline in Abdominal Girth Measurement- Extension.

The participant had a measurement of their abdominal girth recorded. The measurement will be taken with a tape measure extending around the abdomen at the level of the iliac crests laterally and the umbilicus anteriorly. The examiner should also palpate for each kidney and liver edge, noting presence or enlargement. (By definition if the kidneys are palpable they are enlarged, the liver edge may be palpable but not enlarged). (NCT00413777)
Timeframe: Baseline to Extension Day 1, Extension Month 12

,
Interventioncm (Mean)
Month 2 (N= 17, 18)Month 6 (N= 16, 18)Month 12 (N= 17, 18)Month 24 (N= 17, 21)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-0.80.31.12.02.54.24.6
Tolvaptan 60+30 mg-2.80.3-3.5-1.10.12.91.6

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Second Daily Dose- Extension.

"Urine osmolality at steady state (after at least 4 days of dosing) including absolute trough prior to the second daily dose.~Samples for this assessment were taken as closely coincident to PK blood sample as practical. During Weeks 1, 2, 3 and 4 of the Titration Period and at Month 6, additional samples were collected for the preceding day immediately preceding the second daily dose. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration." (NCT00413777)
Timeframe: Baseline to Month 24

,
InterventionmOsm/kg (Mean)
Month 2 (N= 17, 17)Month 6 (N= 17, 18)Month 12 (N= 16, 16)Month 24 (N= 1, 6)
Tolvaptan 45+15 mg-281.63-305.25-288.20-405.00
Tolvaptan 60+30 mg-254.82-261.61-190.69-120.50

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Second Daily Dose.

"Urine osmolality at steady state (after at least 4 days of dosing) including absolute trough prior to the second daily dose.~Samples for this assessment were taken as closely coincident to PK blood sample as practical. During Weeks 1, 2, 3 and 4 of the Titration Period and at Month 6, additional samples were collected for the preceding day immediately preceding the second daily dose. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration." (NCT00413777)
Timeframe: Baseline to Month 24

,
InterventionmOsm/kg (Mean)
Month 2 (N= 21, 21)Month 6 (N= 19, 23)Month 12 (N= 16, 20)Month 24 (N= 1, 7)
Tolvaptan 45+15 mg-263.95-321.78-288.20-405.00
Tolvaptan 60+30 mg-298.71-294.13-234.65-227.14

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Percent Change From Baseline in Renal Volume-Extension.

TKV was assessed by the central magnetic resonance imaging (MRI) rater. (NCT00413777)
Timeframe: Baseline to Months 2, 12, 24, 36, Extension Day 1, Extension Month 12

,
InterventionPercentage change per month (Mean)
Month 2 (N= 17, 18)Month 12 (N= 17, 18)Month 24 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-1.3-0.73.27.914.115.7
Tolvaptan 60+30 mg-1.41.90.23.88.410.7

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Percent Change From Baseline in Renal Volume.

Total Kidney Volume (TKV) was assessed by the central magnetic resonance imaging (MRI) rater. (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionPercentage change per month (Mean)
Month 2 (N= 21, 24)Month 12 (N= 18, 22)Month 24 (N= 18, 21)Month 36 (N= 18, 20)
Tolvaptan 45+15 mg-1.00.34.69.9
Tolvaptan 60+30 mg-1.32.41.05.3

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Safety Assessments Based on Vital Signs, Electrocardiogram (ECG's), Clinical Laboratory Tests, Physical Examinations Are Reported as Adverse Events (AEs) Upon Study Physician Discretion.

An AE was defined as any new medical problem, or exacerbation of an existing problem, experienced by a participant while enrolled in a study , whether or not it was considered drug-related by the study physician. A treatment-emergent AE (TEAE) was defined as an AE that started after start of study drug treatment; or if the event was continuous from Baseline and was serious, study drug related, or resulted in death, discontinuation. (NCT00413777)
Timeframe: AEs were recorded from screening (ICF was signed) until 7-Day follow-up

,
Interventionparticipants (Number)
Participants with serious TEAEsParticipants with severe TEAEsParticipants discontinued due to AEs
Tolvaptan 45+15 mg363
Tolvaptan 60+30 mg8101

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Mean Change From Baseline in Diastolic Blood Pressure (dBP) for Hypertension Assessment.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionmmHg (Mean)
Month 2 (N= 22, 24)Month 6 (N= 19, 23)Month 9 (N= 18, 23)Month 12 (N= 17, 23)Month 16 (N= 18, 23)Month 20 (N= 18, 21)Month 24 (N= 18, 21)Month 28 (N= 18, 21)Month 32 (N= 18, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg-4.0-3.6-4.8-9.2-5.6-7.4-3.1-5.3-4.6-5.4
Tolvaptan 60+30 mg-0.2-2.5-2.8-1.1-2.3-5.6-0.1-2.2-3.0-4.0

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Change From Pre-dose Baseline in Renal Function Estimated by Glomerular Filtration Rate (GFR).

GFR was estimated using reciprocal serum creatinine formula. The formula does not adjust for body weight or height, but this may be done to normalize to body surface area. The formula for reciprocal Serum creatinine is: 1/Pcr. (Pcr = serum creatinine concentration [mg/dL]). Clinic weight scales were calibrated at least yearly. (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventiondL/mg (Mean)
Month 2 (N= 22, 24)Month 6 (N= 19, 21)Month 9 (N= 18, 23)Month 12 (N= 17, 22)Month 16 (N= 18, 21)Month 20 (N= 18, 21)Month 24 (N= 18, 20)Month 28 (N= 18, 21)Month 32 (N= 18, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg-0.09-0.03-0.01-0.03-0.06-0.06-0.04-0.07-0.09-0.07
Tolvaptan 60+30 mg-0.05-0.01-0.03-0.01-0.02-0.03-0.02-0.02-0.06-0.06

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Change From Pre-dose Baseline in Renal Function Estimated by GFR- Extension.

GFR was estimated using reciprocal serum creatinine formula. The formula does not adjust for body weight or height, but this may be done to normalize to body surface area. The formula for reciprocal Serum creatinine is: 1/Pcr. (Pcr = serum creatinine concentration [mg/dL]). Clinic weight scales were calibrated at least yearly. (NCT00413777)
Timeframe: Baseline to Months 2, 6, 9, 12, 16, 20, 24, 28, 32, 36, Extension Day 1, Extension Month 12

,
InterventiondL/mg (Mean)
Month 2 (N= 17, 18)Month 6 (N= 17, 16)Month 9 (N= 16, 18)Month 12 (N= 16, 17)Month 16 (N= 17, 16)Month 20 (N= 17, 18)Month 24 (N= 17, 17)Month 28 (N= 17, 18)Month 32 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-0.09-0.03-0.01-0.03-0.06-0.06-0.04-0.06-0.09-0.07-0.04-0.05
Tolvaptan 60+30 mg-0.04-0.00-0.01-0.00-0.01-0.02-0.02-0.02-0.05-0.05-0.01-0.04

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Mean Change From Baseline in Abdominal Girth Measurement.

The participant had a measurement of their abdominal girth recorded. The measurement will be taken with a tape measure extending around the abdomen at the level of the iliac crests laterally and the umbilicus anteriorly. The examiner should also palpate for each kidney and liver edge, noting presence or enlargement. (By definition if the kidneys are palpable they are enlarged, the liver edge may be palpable but not enlarged). (NCT00413777)
Timeframe: Baseline to Month 36

,
Interventioncm (Mean)
Month 2 (N= 22, 24)Month 6 (N= 18, 23)Month 12 (N= 18, 23)Month 24 (N= 17, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg0.61.41.32.03.1
Tolvaptan 60+30 mg-2.30.5-2.8-0.60.3

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Mean Change From Baseline in dBP for Hypertension Assessment- Extension.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Months 2, 6, 9, 12, 16, 20, 24, 28, 32, 36, Extension Day 1, Extension Month 4, Extension Month 8, Extension Month 12

,
InterventionmmHg (Mean)
Month 2 (N= 17, 18)Month 6 (N= 17, 18)Month 9 (N= 16, 18)Month 12 (N= 16, 18)Month 16 (N= 17, 18)Month 20 (N= 17, 18)Month 24 (N= 17, 18)Month 28 (N= 17, 18)Month 32 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 4 (N= 17, 18)Extension Month 8 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-5.5-4.5-5.3-10.1-6.9-7.5-3.9-5.6-5.4-5.7-7.9-6.8-5.0-6.0
Tolvaptan 60+30 mg0.3-2.4-2.9-1.9-2.1-6.1-0.6-2.9-3.6-4.8-4.0-6.1-6.7-5.6

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Mean Change From Baseline in MAP for Hypertension Assessment- Extension.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Months 2, 6, 9, 12, 16, 20, 24, 28, 32, 36, Extension Day 1, Extension Month 4, Extension Month 8, Extension Month 12

,
InterventionmmHg (Mean)
Month 2 (N= 17, 18)Month 6 (N= 17, 18)Month 9 (N= 16, 18)Month 12 (N= 17, 18)Month 16 (N= 17, 18)Month 20 (N= 17, 18)Month 24 (N= 17, 18)Month 28 (N= 17, 18)Month 32 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 4 (N= 17, 18)Extension Month 8 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-4.1-4.2-4.8-13.1-6.8-7.5-3.1-5.5-6.2-4.1-6.8-5.1-2.8-4.2
Tolvaptan 60+30 mg-0.6-3.4-3.4-2.3-1.9-7.20.1-2.9-4.6-5.1-4.4-6.9-6.8-6.0

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Mean Change From Baseline in Mean Arterial Pressure (MAP) for Hypertension Assessment.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionmmHg (Mean)
Month 2 (N= 22, 24)Month 6 (N= 19, 23)Month 9 (N= 18, 23)Month 12 (N= 18, 23)Month 16 (N= 18, 23)Month 20 (N= 18, 21)Month 24 (N= 18, 21)Month 28 (N= 18, 21)Month 32 (N= 18, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg-3.7-3.6-4.7-12.0-5.8-7.6-2.7-5.2-5.6-3.8
Tolvaptan 60+30 mg-1.0-3.3-3.0-1.8-2.5-7.0-0.1-2.7-4.3-4.4

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Mean Change From Baseline in Patient-assessed Renal Pain Scale- Extension.

"Participants were asked the question to assess the relative level of pain attributed to their kidneys. This question was, On a scale of 0 to 10, with zero represented no pain at all and 10 represented the worst pain ever experienced, what was the worst kidney pain experienced in the last 4 months? If the latest assessment was less than 4 months prior, the question was substituted since your last visit for in the last 4 months. The same interrogator designated to this task was used throughout the study for each participant." (NCT00413777)
Timeframe: Baseline to Months 2, 6, 12, 24, 36, Extension Day 1, Extension Month 12

,
InterventionUnits on a scale (Mean)
Month 2 (N= 17, 18)Month 6 (N=17, 18)Month 12 (N= 17, 18)Month 24 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg0.90.81.20.20.6-0.3-0.4
Tolvaptan 60+30 mg0.3-0.2-0.30.80.50.8-0.6

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Mean Change From Baseline in Patient-assessed Renal Pain Scale.

"Participants were asked the question to assess the relative level of pain attributed to their kidneys. This question was, On a scale of 0 to 10, with zero represented no pain at all and 10 represented the worst pain ever experienced, what was the worst kidney pain experienced in the last 4 months? If the latest assessment was less than 4 months prior, the question was substituted since your last visit for in the last 4 months. The same interrogator designated to this task was used throughout the study for each participant." (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionUnits on a scale (Mean)
Month 2 (N= 22, 24)Month 6 (N= 19, 23)Month 12 (N= 18, 23)Month 24 (N= 18, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg0.60.41.20.20.6
Tolvaptan 60+30 mg0.0-0.1-0.11.00.5

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Mean Change From Baseline in sBP for Hypertension Assessment- Extension.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Months 2, 6, 9, 12, 16, 20, 24, 28, 32, 36, Extension Day 1, Extension Month 4, Extension Month 8, Extension Month 12

,
InterventionmmHg (Mean)
Month 2 (N= 17, 18)Month 6 (N= 17, 18)Month 9 (N= 16, 18)Month 12 (N= 17, 18)Month 16 (N= 17, 18)Month 20 (N= 17, 18)Month 24 (N= 17, 18)Month 28 (N= 17, 18)Month 32 (N= 17, 18)Month 36 (N= 17, 18)Extension Day 1 (N= 17, 18)Extension Month 4 (N= 17, 18)Extension Month 8 (N= 17, 18)Extension Month 12 (N= 17, 18)
Tolvaptan 45+15 mg-1.6-3.4-4.1-8.9-6.5-7.7-1.8-4.9-7.6-0.6-4.4-1.11.8-0.5
Tolvaptan 60+30 mg-2.7-5.6-4.3-3.3-1.7-9.31.4-3.4-6.8-5.4-5.1-8.7-7.3-7.1

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Mean Change From Baseline in Systolic Blood Pressure (sBP) for Hypertension Assessment.

The participants were seated and resting systolic and diastolic BP for each scheduled assessment was recorded. At each assessment, participants were categorized (based on repeated blood pressure measurements as being normotensive (MAP < 100 mm Hg and off therapy), high normal (sBP > 129 and or dBP > 84 mm Hg off therapy) or hypertensive (sBP >140 and/or dBP > 90 mm Hg). The mean arterial pressure (MAP) was derived from these values and were not recorded (MAP = diastolic pressure + [1/3 x pulse pressure (ie systolic - diastolic pressure)] in mm Hg). (NCT00413777)
Timeframe: Baseline to Month 36

,
InterventionmmHg (Mean)
Month 2 (N= 22, 24)Month 6 (N= 19, 23)Month 9 (N= 18, 23)Month 12 (N= 18, 23)Month 16 (N= 18, 23)Month 20 (N= 18, 21)Month 24 (N= 18, 21)Month 28 (N= 18, 21)Month 32 (N= 18, 21)Month 36 (N= 18, 21)
Tolvaptan 45+15 mg-3.2-3.6-4.6-8.0-6.2-7.9-2.1-4.7-7.3-0.2
Tolvaptan 60+30 mg-3.0-5.0-3.5-3.5-2.9-10.0-0.1-4.1-7.2-5.4

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Mean Change From Baseline in Trough Urine Osmolality at Steady State Prior to Bedtime- Extension.

"Urine osmolality at steady state (after at least 4 days of dosing) including average of troughs (the mean urine osmolality prior to bedtime).~Samples for this assessment were to be taken as closely coincident to PK blood sample as practical. During Weeks 1, 2, 3 and 4 of the Titration Period and at Month 6, additional samples were collected for the preceding day at bedtime. These samples allowed derivation of an average nadir of spot urine osmolality concentrations at each dose level and while at steady state during extended tolvaptan administration." (NCT00413777)
Timeframe: Baseline to Month 24

,
InterventionmOsm/kg (Mean)
Month 2 (N= 17, 17)Month 6 (N= 17, 18)Month 12 (16, 15)Month 24 (N= 1, 6)
Tolvaptan 45+15 mg-322.27-309.73-283.21-263.00
Tolvaptan 60+30 mg-258.88-264.50-206.00-187.50

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Change in Mean Arterial Blood Pressure Per Year in Non-hypertensive Participants From Baseline to Month 36

For participants who were non-hypertensive (systolic BP ≤ 139 mmHg and diastolic BP ≤ 89 mmHg without taking antihypertensive medications) at baseline, mean arterial blood pressure was measured at scheduled clinic visits up to the point of exposure to antihypertensive therapy for any reason. The change in mean arterial blood pressure per year was based on the slope of blood pressure, obtained by regressing blood pressure against time by subject. (NCT00428948)
Timeframe: Baseline to Month 36

InterventionmmHg (Mean)
Tolvaptan2.561
Placebo2.592

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Area Under the Concentration-time Curve of Change in Renal Pain From Baseline to Month 36

Change from baseline in renal pain was assessed by a 0 to 10 pain scale as average area under the concentration-time curve (AUC) between baseline and the last trial visit or the last visit prior to initiating medical (eg, narcotic or anti-nociceptives [eg, tricyclic antidepressants]) or surgical therapy for pain. In the pain scale, score 0 represented no pain at all and score 10 represented the worst pain. A negative change score indicates less pain. AUC of renal pain was derived from renal pain scores within treatment period and was calculated using the trapezoidal rule, by dividing the number of days between the first and last assessment. (NCT00428948)
Timeframe: At screening, Baseline, Day 1, every 4 months up to month 36/early tremination (ET), follow-up visit 1 and 2

Interventionunits on a scale (Mean)
Tolvaptan-0.00
Placebo0.08

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Number of Hypertensive Events Per 100 Follow-up Years in Non-hypertensive Participants From Baseline to Month 36

A hypertensive event was defined as a change from non-hypertensive (systolic BP ≤ 139 mmHg and diastolic BP ≤ 89 mmHg without taking antihypertensive medications) status to 1 of 3 conditions: (1) High pre-hypertensive (systolic BP [sBP] > 129 mmHg and/or diastolic BP [dBP] > 84 mmHg), (2) hypertensive (sBP > 139 mmHg and/or dBP > 89 mmHg), or (3) requiring antihypertensive therapy. (NCT00428948)
Timeframe: Baseline to Month 36

InterventionEvents/100 follow-up years (Number)
Tolvaptan31.80
Placebo29.60

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Percentage of Participants With a Clinically Sustained Decrease of Blood Pressure Leading to a Sustained Reduction in Antihypertensive Therapy From Baseline to Month 36

(NCT00428948)
Timeframe: Baseline to Month 36

InterventionPercentage of participants (Number)
Tolvaptan6.24
Placebo5.62

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Number of ADPKD Clinical Progression Events Per 100 Follow-up Years From Baseline to Month 36

These ADPKD events in the key secondary Outcome Measure were selected on the basis of their potential relationship to progressing cystogenesis. Reducing the rate of cyst development and expansion would likely slow the progression of ADPKD. The 4 events were: (1) Onset or progression of hypertension (someone is hypertensive if they have > 139 mmHg systolic blood pressure [BP], > 89 mmHg diastolic BP, or if they are taking antihypertensive medication at any BP level); (2) severe renal pain requiring medical intervention; (3) worsening albuminuria (by category, see below); and (4) worsening renal function, defined as a 25% decrease in 1/serum creatinine from Baseline. Albuminuria was assessed using spot urine albumin/creatinine ratio measurements (all measurements in mg/mmol). Categories included normal (< 2.8 female or < 2.0 male), microalbuminuria (2.8-28 female or 2.0-20 male), and overt proteinuria (> 28 female or > 20 male. (NCT00428948)
Timeframe: Baseline to Month 36

InterventionEvents/100 follow-up years (Number)
Tolvaptan43.94
Placebo50.04

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Change in Renal Function Per Year From Week 3 to Month 36

Renal function was assessed using serum creatinine measurements and was estimated using 1/serum creatinine. The formula for 1/serum creatinine is: 1/Pcr, where Pcr = serum creatinine concentration (mg/dL). The change in renal function per year was based on the slope of change, obtained by regressing renal function data against time by subject. (NCT00428948)
Timeframe: Week 3 to Month 36

Intervention(mg/mL)^-1 per year (Mean)
Tolvaptan-2.555
Placebo-3.682

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Percentage Change Per Year in Total Kidney Volume From Baseline to Month 36

Kidney volume was assessed in T1-weighted magnetic resonance images collected at each study site and sent to a central reviewing facility. At the central reviewing facility, blinded radiologists used proprietary software to measure the volume of both kidneys. (NCT00428948)
Timeframe: Baseline to Month 36

InterventionPercentage change per year (Mean)
Tolvaptan2.777
Placebo5.608

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Body Weight (Percent Change)

Percent change in body weight from baseline at the time of final trial drug administration (NCT00462670)
Timeframe: baseline, Day 7 or at the time of final trial drug administration

Interventionpercentage of body weight (Kg) (Mean)
Placebo-0.77
OPC-41061 15mg-2.50

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Body Weight (Amount of Change)

Change in body weight from baseline at the time of final trial drug administration (NCT00462670)
Timeframe: baseline, Day 7 or at the time of final trial drug administration

InterventionKg (Mean)
Placebo-0.45
OPC-41061 15mg-1.54

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Abdominal Circumference

Change in abdominal circumference from baseline (LOCF) (NCT00479336)
Timeframe: Baseline, Day 7 or at the discontied of treatment

Interventioncm (Mean)
Placebo-1.39
OPC-41061 7.5 mg-2.98
OPC-41061 15 mg-2.42
OPC-41061 30 mg-2.62

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Body Weight (Amount of Change)

Changes in body wight from baseline at the final timepoint (LOCF). A linear regression model using changes in body weight from baseline at the final timepoint as the criterion variable and dose as the explanatory variable was fitted to the dataset. (NCT00479336)
Timeframe: Baseline, Day 7 or at the discontied of treatment

InterventionKg (Mean)
Placebo-0.68
OPC-41061 7.5 mg-2.31
OPC-41061 15 mg-1.88
OPC-41061 30 mg-1.67

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Body Weight

The body weight change from baseline at the time of final trial drug administration (NCT00525265)
Timeframe: Baseline, at the time of final trial drug administration

InterventionKg (Mean)
OPC-41061 7.5 mg-1.68
OPC-41061 15 mg-2.14

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Body Weight

The change of body weight from baseline at final observation (NCT00544869)
Timeframe: Baseline, Day 14 or at the time of final drug administration

InterventionKg (Mean)
Stopped at End of Treatment Period 1-2.05
Continued at 15 mg/Day-1.31
Dose Escalated to 30 mg/Day-2.9

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Number of Patients With Electrocardiogram (ECG) Abnormalities: ST Segment

Incidence of potentially clinically significant ECG abnormalities: ST Segment (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)2

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Number of Patients With Electrocardiogram (ECG) Abnormalities: Right Bundle Branch Block (RBBB), Left Bundle Branch Block (LBBB), Myocardial Infarction (MI)

Incidence of potentially clinically significant ECG abnormalities: Right bundle branch block (RBBB), Left bundle branch block (LBBB), myocardial infarction (MI) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)1

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Number of Patients With Electrocardiogram (ECG) Abnormalities: QTcF Increase 30-60 Msec

Incidence of potentially clinically significant ECG abnormalities (QTcF increase 30-60 msec post-baseline) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo2
Tolvaptan (15-60 mg)3

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Number of Patients With Electrocardiogram (ECG) Abnormalities: QTcB Increase 30-60 Msec

Incidence of potentially clinically significant ECG abnormalities (QTcB increase 30-60 msec) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo3
Tolvaptan (15-60 mg)4

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Number of Patients With Electrocardiogram (ECG) Abnormalities: QT >500 Milliseconds (Msec)

Incidence of potentially clinically significant ECG abnormalities (QT>500 msec) post-baseline (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)0

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Number of Patients With Electrocardiogram (ECG) Abnormalities: QRS Interval

Incidence of potentially clinically significant ECG abnormalities involving QRS interval (change > 100 msec) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)1

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Number of Patients With Electrocardiogram (ECG) Abnormalities: Arrhythmia

Incidence of potentially clinically significant ECG abnormalities: arrhythmia (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo2
Tolvaptan (15-60 mg)6

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Change From Baseline to Day 22 in the Individual Neurocognitive Domains Included in the Primary Endpoint: Reaction Time in Computer Tests

Change from baseline in the individual neurocognitive domains Z-score for Reaction Time in Computer Tests (simple reaction time test, choice reaction time test, digit vigilance test); ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo0.21
Tolvaptan (15-60 mg)0.33

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Change From Baseline in the Neurocognitive Composite Score of Speed Domains (NCS-SD; Sum of All Correct Speed Domain Z-Scores)

"Change from baseline to Day 22 in sum of all speed domain Z-scores:Reaction Time (Simple=recognize yes 50 times;Choice=recognize yes or no 50 times;Digit Vigilance=match 45 digits);Psychomotor Speed (Morse Tapping=tap button for 30 seconds with right & left hands);Processing Speed (Rapid Visual Information Processing=detect consecutive sequences of 3 odd or 3 even digits;Numeric Working Memory=recognize numbers from series of 5 digits among 30;Word Recognition=remember 15 prior learned words from 30 total;results age-matched to healthy controls from Cognitive Drug Research normative data" (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo0.20
Tolvaptan (15-60 mg)0.39

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Change From Baseline in the Individual Neurocognitive Domains Included in the Primary Endpoint: Psychomotor Speed Via Morse Tapping Test

Change from baseline to Day 22 in the individual neurocognitive domains Z-score for Psychomotor Speed (mean tap rate of Morse tapping test); ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo0.04
Tolvaptan (15-60 mg)0.31

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Change From Baseline in the Individual Neurocognitive Domains Included in the Primary Endpoint: Processing Speed of Rapid Visual Information Processing Test, Numeric Working Memory Test, and Word Recognition Test

Change from baseline to Day 22 in the individual neurocognitive domains Z-score for Processing Speed of Rapid Visual Information Processing Test, Numeric Working Memory Test, and Word Recognition Test; ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo0.24
Tolvaptan (15-60 mg)0.48

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Change From Baseline in Serum Sodium; ITT Population

Change from Baseline to Day 22 in Serum Sodium; ITT population (NCT00550459)
Timeframe: Baseline and Day 22

InterventionmEq/L (Mean)
Placebo2.23
Tolvaptan (15-60 mg)7.04

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Change From Baseline in Postural Stability Test

Change from baseline to Day 22 in Postural Stability Test Z-score (This test measures gross motor control. The ability to stand upright without moving is assessed using the SWAY meter that is modeled on the Wright Ataxiameter. A cord from the meter is attached to the subject who is required to stand as still as possible with feet apart and eyes closed for 1 minute. The test is then repeated with eyes open for 1 minute. The outcomes of these tests are combined and measured as a movement Z-score. Higher result=better postural stability); ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo1.3
Tolvaptan (15-60 mg)-0.35

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Change From Baseline in Overall Neurocognitive Composite Score

Change from Baseline to Day 22 in the overall Neurocognitive Composite Score (NCS)comprising the sum of 7 neurocognitive domain Z-scores (Reaction Time, Psychomotor Speed, Processing Speed, Continuity of Attention, Working Memory/Executive Functions, Quality of Episodic Verbal Memory, and Postural Stability); ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionZ-score (Mean)
Placebo0.19
Tolvaptan (15-60 mg)0.30

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Change From Baseline in Gait Test (Timed Get-Up-and-Go Test)

Change from baseline to Day 22 in Gait Test (Timed Get-Up-and-Go Test=time it takes for a seated subject to rise from a chair, walk 3 meters, walk around an object and return to sit in chair. Values: under 10 sec (no difficulties), 10 to 20 sec (starting to have balance difficulty), over 30 sec (at high risk for falls and dependent in most activities of daily living and mobility); test assesses risk to elderly subjects of falling and higher scores in seconds indicate higher risk of falling; ITT population (NCT00550459)
Timeframe: baseline and Day 22

InterventionSeconds (Mean)
Placebo1.06
Tolvaptan (15-60 mg)-0.43

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Number of Patients With Vital Sign Abnormalities: Pulse Rate

Incidence of abnormal pulse rate post-baseline [abnormal values: >=120 beats per minute (bpm) + increase of >=15 bpm; <=50 bpm + decrease of >=15 bpm] (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)0

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Number of Patients With Vital Sign Abnormalities: Body Weight

Incidence of clinically significant body weight change post-baseline (defined as change upward or downward of >=7%) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)1

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Number of Patients With Vital Sign Abnormalities: Body Temperature

Incidence of potentially clinically significant changes in body temperature post-baseline (defined as an increase of >=1.1 to >=38.3 degrees Celsius) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)0

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Number of Patients With Vital Sign Abnormalities: Blood Pressure

Incidence of abnormal systolic & diastolic blood pressure values post-baseline (abnormal systolic values: >=180 mmHg + increase of >=20 mmHg, <= 90 mmHg + decrease >=20 mmHg; abnormal diastolic values: >=105 mmHg+increase of >=15 mmHg, <=50 mmHg + decrease of >= 15 mmHg) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo2
Tolvaptan (15-60 mg)0

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Number of Patients With Serum Chemistry Laboratory Abnormalities: Uric Acid

Incidence of potentially clinically significant uric acid levels post-baseline (normal range=4-8.5 mg/dL) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)1

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Number of Patients With Serum Chemistry Laboratory Abnormalities: Magnesium

Incidence of potentially clinically significant magnesium levels post-baseline (normal range=1.2-2 mEq/L) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)1

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Number of Patients With Serum Chemistry Laboratory Abnormalities: Glucose

Incidence of potentially clinically significant glucose levels post-baseline (normal range=70-125 mg/dL) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo2
Tolvaptan (15-60 mg)0

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Number of Patients With Serum Chemistry Laboratory Abnormalities: Cholesterol

Incidence of potentially clinically significant cholesterol levels post-baseline (normal range=0-199 mg/dL) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)2

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Number of Patients With Serum Chemistry Laboratory Abnormalities: Blood Urea Nitrogen (BUN)

Incidence of potentially clinically significant BUN levels post-baseline (normal range=7-30 mg/dL) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)2

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Number of Patients With Hematology Laboratory Abnormalities: Neutrophils

Incidence of potentially clinically significant neutrophil count post-baseline (normal range=1.8-8 thousands/microliter) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo2
Tolvaptan (15-60 mg)0

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Number of Patients With Hematology Laboratory Abnormalities: Lymphocytes

Incidence of potentially clinically significant lymphocyte count post-baseline (normal range = 16-46%) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)2

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Number of Patients With Hematology Laboratory Abnormalities: Hemoglobin

Incidence of clinically significant hemoglobin abnormalities post-baseline (normal range=11.8-16.8 g/dL) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo0
Tolvaptan (15-60 mg)1

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Number of Patients With Hematology Laboratory Abnormalities: Activated Partial Thromboplastin Time (aPTT)

Incidence of potentially clinically significant Activated Partial Thromboplastin Time (aPTT) levels post-baseline (normal range=22-34 seconds) (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)3

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Number of Patients With Electrocardiogram (ECG) Abnormalities: T Wave

Incidence of potentially clinically significant ECG abnormalities: T wave (NCT00550459)
Timeframe: 28 days

Interventionparticipants (Number)
Placebo1
Tolvaptan (15-60 mg)1

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Renal Function Test (eGFR)

"Individual subject data on eGFR (estimated glomerular filtration rate calculated by Japanese eGFR equation) during trial period.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT00841568)
Timeframe: Baseline, Week 24, 48, 104, and 156

InterventionmL/min/1.73m2 (Median)
Baseline63.0
Week 2464.0
Week 5264.0
Week 10458.5
Week 15659.0

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Total Kidney Volume

"Individual subject data on the volumes of the total kidney volume (sum of the volumes of the left and right kidneys) measured by magnetic resonance imaging or computed tomography during trial period.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT00841568)
Timeframe: Baseline, week 24, 52, 104, and 156

InterventionmL (Median)
Baseline1500.5
Week 241573.1
Week 521567.9
Week 1041729.4
Week 1561647.7

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Total Kidney Volume

"Individual subject data on the volumes of the total kidney volume (sum of the volumes of the left and right kidneys) measured by magnetic resonance imaging or computed tomography during trial period.~Repeated oral administration at doses of 15 mg twice daily (morning and evening) until approval of the revised protocol (Edition 4.0) by the IRB of each trial site.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT01022424)
Timeframe: Baseline, Week 48, 96, 144, and 192

InterventionmL (Median)
Baseline1428
Week 481675
Week 961728
Week 1441775
Week 1921901

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Renal Function Test (eGFR)

"Individual subject data on eGFR (estimated glomerular filtration rate calculated by Japanese eGFR equation) during trial period.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT01022424)
Timeframe: Baseline, Week 48, 96, 144, and 192

InterventionmL/min/1.73 m2 (Median)
Baseline63.0
Week 4860.0
Week 9654.0
Week 14450.5
Week 19251.0

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Body Weight

Changes in body weight from baseline at the end of administration (NCT01048788)
Timeframe: Baseline, Day 14 or end of administration

InterventionKg (Mean)
Discontitued/Terminated Before Day 8-0.76
Continued Administration at 7.5 mg/Day-2.97
Dose Escalation to 15 mg/Day-0.05

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Ascites Volume

Change in ascites volume from baseline as measured by CT at end of treatment (NCT01050530)
Timeframe: Baseline, Day 7 or at the discontinued of treatment

InterventionmL (Mean)
OPC-41061-492.4
Placebo-191.8

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Body ｗeight

Change in body weight from baseline after 7-day repeated oral administration of OPC (NCT01050530)
Timeframe: Baseline, Day 7 or at the discontinued of treatment

InterventionKg (Mean)
OPC-41061-1.95
Placebo-0.44

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Ascites Volume as Measured by CT

Change from baseline (day-1) for ascites volume as measured by CT at the end of treatment (LOCF) were calculated. (NCT01114828)
Timeframe: Baseline, Day 7 or at the discontinued of treatment

InterventionmL (Mean)
OPC-41061 3.75 mg-407.5
OPC-41061 7.5 mg-514.0

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Body Weight

Changes from baseline (day-1) for body weight at the end of treatment (LOCF) were calculated. (NCT01114828)
Timeframe: Bseline, Day 7 or at the discontined of treatment

Interventionkg (Mean)
OPC-41061 3.75 mg-1.14
OPC-41061 7.5 mg-1.37

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Participants Whose Serum Sodium Concentration Corrected to at Least 135 mEq/L on Day 14

Compare proportion of hyponatremia cancer patients with a normalized serum sodium concentration at day 14 between those treated with Tolvaptan and those treated with a placebo (standard of care). Proportion of participants whose serum sodium concentration is corrected to at least 136 mEq/Lon day14. (NCT01199198)
Timeframe: 14 days

Interventionparticipants (Number)
Tolvaptan Group16
Placebo Group1

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Length of Stay in Hospital

(NCT01199198)
Timeframe: From administration of treatment to time of discharge

Interventiondays (Mean)
Tolvaptan Group21
Placebo Group26

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Change From Baseline in Urine Volume at 24 Hours at Day 7.

Urine volume was collected by 0 to 24-hour interval at Day 7. Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2 and Day 21 of Period 3. (NCT01210560)
Timeframe: Day 7

InterventionmL (Mean)
MR 20 mg1111
MR 20+20 mg2066
MR 60 mg2396
MR 120 mg3722
IR 90+30 mg3820

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Maximum (Peak) Plasma Concentration of the Drug [Cmax] and Minimum (Trough) Plasma Concentration of the Drug [Cmin] After Tolvaptan Treatment on Day 7.

Blood samples (6 mL) for determination of tolvaptan PK parameters were collected on Day 1 predose, and on Days 7, 14 and 21 at predose, and 1, 2, 4, 6, 8, 9, 10, 12, 16, and 24 hours postdose. If a sample was not drawn at the designated time, a window of ± 3 minutes for each blood draw was acceptable. Maximum and minimum plasma concentration of the drug was calculated. (NCT01210560)
Timeframe: Day 7

,,,,
Interventionng/mL (Mean)
CmaxCmin
IR 90+30 mg71657.5
MR 120 mg669139
MR 20 mg14014.7
MR 20+20 mg17550.8
MR 60 mg35051.1

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Number of Participants With Urine Osmolality < 300 mOsm/kg at 23.5 Hours Postdose.

For determination of duration of urine osmolality <300 mOsm/kg, the value was the end time of the last collection interval in which urine osmolality was <300 mOsm/kg. Day 8 in the table below was defined as Day 8 of Period 1, Day 15 of Period 2, and Day 22 of period 3. (NCT01210560)
Timeframe: 23.5 hours post-dose

,,,,
InterventionParticipants (Count of Participants)
BaselineDay 8
IR 90+30 mg011
MR 120 mg011
MR 20 mg15
MR 20+20 mg111
MR 60 mg19

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Ranking of Treatment Tolerability.

"Ranking of treatment tolerability was evaluated based on a questionnaire. At Day 22, participants were asked the following questions and their responses recorded on the eCRF: Which treatment period did you find most tolerable? and Which treatment period did you find the least tolerable?." (NCT01210560)
Timeframe: Day 22/Early Termination

,
InterventionParticipants (Number)
Most tolerable Group 1Least tolerable Group 1
IR 90+30 mg16
MR 120 mg14

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Change From Baseline in Urine Osmolality Area Under the Concentration-time Curve From Time 0 to 24 Hours Postdose (AUC0-24h) at Day 7.

The AUC0-24h for urine osmolality was determined by multiplying the concentration by the collection interval duration for each collection interval and summing all the intervals in the 24-hour period. If the urine volume for an interval is zero, the duration of that interval will be added to the next collection interval. Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2 and Day 21 of Period 3. (NCT01210560)
Timeframe: Day 7

InterventionmOsm/kg*Hour (Mean)
MR 20 mg-2546
MR 20+20 mg-3438
MR 60 mg-4209
MR 120 mg-4325
IR 90+30 mg-4620

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Area Under the Concentration-time Curve During the Dosing Interval at Steady State and Area Under the Concentration-time Curve From Time 0 to 24 Hours Postdose (AUCT & AUC0-24h) After Tolvaptan Treatment on Day 7.

Blood samples (6 mL) for determination of tolvaptan PK parameters were collected on Day 1 predose, and on Days 7, 14 and 21 at predose, and 1, 2, 4, 6, 8, 9, 10, 12, 16, and 24 hours postdose. If a sample was not drawn at the designated time, a window of ± 3 minutes for each blood draw was acceptable. Hence, both AUCT and AUC0-24h values were calculated. (NCT01210560)
Timeframe: Day 7

Interventionng·h/mL (Mean)
MR 20 mg1260
MR 20+20 mg2310
MR 60 mg3600
MR 120 mg7740
IR 90+30 mg6570

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Ranking of Treatment Tolerability.

"Ranking of treatment tolerability was evaluated based on a questionnaire. At Day 22, participants were asked the following questions and their responses recorded on the eCRF: Which treatment period did you find most tolerable? and Which treatment period did you find the least tolerable?." (NCT01210560)
Timeframe: Day 22/Early Termination

InterventionParticipants (Number)
Most tolerable Group 1Most tolerable Group 2Least tolerable Group 2
MR 60 mg336

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Number of Participants Experiencing Urinary Urgency Based on Urinary Urgency Questionnaire (Question 1) at Baseline and Day 6.

For the ADPKD Urinary Urgency Questionnaire, Question 1 (currently experiencing urgency?) was assigned 'Yes' or 'No' to measure current urine urgency status. Baseline was defined as last pre-dose evaluation; Day 6 was defined as Day 6 of Period 1, Day 13 of Period 2 and Day 20 of Period 3. (NCT01210560)
Timeframe: Baseline and Day 6

,,,,
InterventionParticipants (Number)
BaselineDay 6
IR 90+30 mg211
MR 120 mg210
MR 20 mg58
MR 20+20 mg313
MR 60 mg312

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Number of Participants Experiencing Urinary Frequency Based on Urinary Frequency Questionnaire (Question 1) at Baseline and Day 6.

"The ADPKD Urinary Frequency Questionnaire: Question 1 (currently experiencing frequency) was assigned 'Yes' or 'No' to measure current urine frequency status.~Baseline was defined as last pre-dose evaluation; Day 6 was defined as Day 6 of Period 1, Day 13 of Period 2 and Day 20 of Period 3." (NCT01210560)
Timeframe: Baseline and Day 6

,,,,
InterventionParticipants (Number)
BaselineDay 6
IR 90+30 mg412
MR 120 mg412
MR 20 mg510
MR 20+20 mg415
MR 60 mg416

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Change From Baseline in Urine Volume by Interval at Day 7.

Urine volume collected was by interval (0-4, 4-8, 8-12, 12-16, 16-24 hours). Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2 and Day 21 of Period 3. (NCT01210560)
Timeframe: 0-4, 4-8, 8-12, 12-16, 16-24 Hours at Day 7

,,,,
InterventionmL (Mean)
0-4 Hour4-8 Hour8-12 Hour12-16 Hour16-24 Hour
IR 90+30 mg2418258019101044
MR 120 mg877858879261038
MR 20 mg-87326301314257
MR 20+20 mg-118423529635598
MR 60 mg56636689667286

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Duration of Urine Osmolality Less Than 300 mOsm/kg at Baseline and Day 7.

Duration of urine osmolality remains below 300 mOsm/kg was the sum of the durations (nominal times) of all intervals where the urine concentration was < 300 mOsm/kg. Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2, and Day 21 of Period 3. (NCT01210560)
Timeframe: Baseline and Day 7

,,,,
InterventionHours (Median)
BaselineDay 7
IR 90+30 mg14.024.0
MR 120 mg14.024.0
MR 20 mg8.016.0
MR 20+20 mg8.024.0
MR 60 mg8.024.0

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Change From Baseline in Urine Osmolality at Day 7.

To determine the tolerability and nighttime urinary suppression of osmolality. The urine osmolality was summarized by collection interval (0 to 4, 4 to 8, 8 to 12, 12 to 16, and 16 to 24 hours) (NCT01210560)
Timeframe: 0-4, 4-8, 8-12, 12-16, 16-24 Hours at Day 7

,,,,
InterventionmOsm/kg (Mean)
0-4 Hour4-8 Hour8-12 Hour12-16 Hour16-24 Hour
IR 90+30 mg-123.3-191.8-166.9-178.3-239.8
MR 120 mg-59.5-186.1-167.1-176.3-246.1
MR 20 mg2.6-140.9-123.1-128.3-123.4
MR 20+20 mg-0.7-128.3-172.1-193.6-182.4
MR 60 mg-88.9-188.2-201.8-195.8-188.8

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Change From Baseline in Urinary Urgency Questionnaire (Questions 2 to 5 and Questions 7 to 14) at Day 6.

"Question 2 to Question 6 were assigned scores of 0 to 4 with higher scores indicating worse cases in experience of urinary urgency. Scores for Question 2 to Question 5 were pooled, with a maximum possible score of 16.~Question 6 was excluded from the analysis since it was only asked at screening. Question 7 to Question 14 were also assigned scores of 0 to 4 with higher scores indicating worse cases in impact of urinary urgency on life; scores for these questions were pooled, with a maximum possible score of 32.~Baseline was defined as last pre-dose evaluation; Day 6 was defined as Day 6 of Period 1, Day 13 of Period 2 and Day 20 of Period 3." (NCT01210560)
Timeframe: Day 6

,,,,
InterventionUnits on a scale (Mean)
Urinary urgency questionnaire-Question (Q) 2 to Q5Urinary urgency questionnaire-Q 7 to Q 14
IR 90+30 mg4.78.8
MR 120 mg4.610.9
MR 20 mg1.40.9
MR 20+20 mg3.24.2
MR 60 mg3.23.5

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Change From Baseline in Urinary Frequency Questionnaire (Question 2 and Questions 3 to 10) at Day 6.

"Question 2 asked, During the last 5 days, how much has urinary frequency bothered you? In order to score the response, the written answers were assigned values from 0 to 4 as follows: 0) Not at all, 1) Somewhat, 2) Moderately, 3) Quite a bit, and 4) Constantly.~Question 3 to Question 10 were assigned scores of 0 to 4 with higher scores indicating worse cases in impact of urinary frequency on life; scores for these questions were pooled, with a maximum possible score of 32.~Baseline was defined as last pre-dose evaluation; Day 6 was defined as Day 6 of Period 1, Day 13 of Period 2 and Day 20 of Period 3." (NCT01210560)
Timeframe: Day 6

,,,,
InterventionUnits on a scale (Mean)
Urinary frequency questionnaire-Question (Q) 2Urinary frequency questionnaire-Q 3 to Q 10
IR 90+30 mg1.59.1
MR 120 mg1.712.2
MR 20 mg0.41.4
MR 20+20 mg1.14.6
MR 60 mg0.94.1

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Ranking of Treatment Tolerability.

"Ranking of treatment tolerability was evaluated based on a questionnaire. At Day 22, participants were asked the following questions and their responses recorded on the eCRF: Which treatment period did you find most tolerable? and Which treatment period did you find the least tolerable?." (NCT01210560)
Timeframe: Day 22/Early Termination

InterventionParticipants (Number)
Most tolerable Group 1Most tolerable Group 2Least tolerable Group 1Least tolerable Group 2
MR 20 mg31000

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Ranking of Treatment Tolerability.

"Ranking of treatment tolerability was evaluated based on a questionnaire. At Day 22, participants were asked the following questions and their responses recorded on the eCRF: Which treatment period did you find most tolerable? and Which treatment period did you find the least tolerable?." (NCT01210560)
Timeframe: Day 22/Early Termination

InterventionParticipants (Number)
Most tolerable Group 1Least tolerable Group 2
MR 20+20 mg27

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Change From Baseline in Symptom Burden by Autosomal Dominant Polycystic Kidney Disease (ADPKD) Nocturia Quality of Life Questionnaire at Day 6.

In ADPKD Nocturia Quality of Life Questionnaire, questions 1 to 11 (with possible scores ranging from 0 to 4 and higher scores indicating better quality of life) were pooled to provide a total score (maximum of 44 points). Response scores of Question 12 (with possible scores ranging from 1 to 10, with higher scores indicating more interference (worse quality of life) with everyday life due to urination at night) were pooled separately. Day 6 was defined as Day 6 of Period 1, Day 13 of Period 2 and Day 20 of Period 3. (NCT01210560)
Timeframe: Day 6

,,,,
InterventionUnits on a scale (Mean)
Nocturia Quality of life Question (Q) 1 To Q 11Nocturia Quality of life Q 12
IR 90+30 mg-13.13.7
MR 120 mg-15.04.2
MR 20 mg-1.50.6
MR 20+20 mg-6.91.9
MR 60 mg-5.11.4

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Change From Baseline in Number of Urine Voids During Sleep Periods.

Average number of daily urine voids during sleep periods for each dose group. Day 1 was defined as Day 1 of Period 1, Day 8 of Period 2, Day 15 of Period 3; Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2 and Day 21 of Period 3; Same rule applied to Day 2 to 6. (NCT01210560)
Timeframe: Days 1, 2, 3, 4, 5, 6 and 7

,,,,
InterventionNumber of urine voids (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
IR 90+30 mg1.51.71.91.80.91.72.1
MR 120 mg2.51.81.91.71.01.11.8
MR 20 mg0.6-0.20.10.60.31.20.1
MR 20+20 mg1.10.81.40.70.91.31.0
MR 60 mg0.40.80.80.50.20.40.9

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Change From Baseline in Number of Urine Voids During Awake Periods.

Average number of daily urine voids during awake periods for each dose group. Day 1 was defined as Day1 of Period 1, Day 8 of Period 2 adn Day 15 of Period 3; Day 7 was defined as Day 7 of Period 1, Day 14 of Period 2 and Day 21 of Period 3; Same rule applied to Day 2 and Day 6. (NCT01210560)
Timeframe: Days 1, 2, 3, 4, 5, 6 and 7

,,,,
InterventionNumber of urine voids (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
IR 90+30 mg4.83.83.33.74.04.84.3
MR 120 mg5.64.83.12.83.32.32.8
MR 20 mg1.7-0.4-0.8-1.4-0.50.02.0
MR 20+20 mg1.51.20.91.50.62.93.5
MR 60 mg3.51.82.40.4-0.45.83.5

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Time to Maximum (Peak) Plasma Concentration (Tmax) After Tolvaptan Treatment on Day 7.

Blood samples (6 mL) for determination of tolvaptan PK parameters were collected on Day 1 predose, and on Days 7, 14 and 21 at predose, and 1, 2, 4, 6, 8, 9, 10, 12, 16, and 24 hours postdose. If a sample was not drawn at the designated time, a window of ± 3 minutes for each blood draw was acceptable. Time to maximum plasma concentration was calculated. (NCT01210560)
Timeframe: Day 7

InterventionHours (Median)
MR 20 mg6.00
MR 20+20 mg6.00
MR 60 mg6.00
MR 120 mg5.98
IR 90+30 mg2.00

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Annualized Slope of eGFR (CKD-EPI) for Study 156-04-251 Participants Enrolled in Study 156-08-271

Annualized slope of eGFR (CKD-EPI) is a measure of renal function and disease progression in ADPKD participants. The annualized slope of eGFR (CKD-EPI) (divided by each participant's years of participation) for all participants was calculated using MMRM analysis in participants continuing from previous study (156-04-251) at Month 24 of this study (156-08-271) comparing change in TKV for the early-treated (those previously treated with tolvaptan) to delayed-treated (those previously treated with placebo). eGFR was calculated using the Chronic Kidney Disease-Epidemiology (CKD-EPI) formula. This outcome measure was analyzed only in the participants enrolled from the previous study - 156-04-251, as pre-specified in the protocol. (NCT01214421)
Timeframe: Study Baseline (Prior to Day 1 in Study 156-08-271) to Month 24 (Study 156-08-271)

Interventionml/min/1.73m^2/participant-years (Number)
Tolvaptan, Early Treated (From Study 156-04-251: Tolvaptan)-3.255
Tolvaptan, Delayed Treated (From Study 156-04-251: Placebo)-3.142

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Percent Change From the Baseline in Total Kidney Volume (TKV) for Study 156-04-251 Participants Enrolled in This Study (156-08-271)

Total kidney volume is a measure of disease progression in the ADPKD participants. Kidney volume was assessed in T1-weighted magnetic resonance images collected at each study site and sent to a central reviewing facility. At the central reviewing facility, radiologists used proprietary software to measure the volume of both kidneys in participants continuing from previous study (156-04-251) at Month 24 of this study (156-08-271) comparing change in TKV for the early-treated (those previously treated with tolvaptan) to delayed-treated (those previously treated with placebo). The percent change in the volume of both kidneys combined was analysed using mixed-effect model repeated measures (MMRM) analysis and reported. This outcome measure was analyzed only in the participants enrolled from the previous study - 156-04-251, as pre-specified in the protocol. (NCT01214421)
Timeframe: Study Baseline (Prior to Day 1 in Study 156-04-251) to Month 24 in this study (Study 156-08-271)

Interventionpercent change (Mean)
Tolvaptan, Early Treated (From Study 156-04-251: Tolvaptan)28.66
Tolvaptan, Delayed Treated (From Study 156-04-251: Placebo)30.58

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Annualized Slope of Renal Function (eGFRCKD-EPI) for Study 156-04-251 Placebo Participants Enrolled in Study 156-08-271

Annualized slope of eGFR (CKD-EPI) is a measure of renal function and disease progression in ADPKD participants. The annualized slope of eGFR (calculated using CKD-EPI formula) divided by each participant's years of participation, using MMRM analysis to compare annualized slope of eGFR (CKD-EPI) for the participants who received placebo in previous study (156-04-251) to the annualized slope of eGFR (CKD-EPI) for the same participants who received tolvaptan in this study (156-08-271). This outcome measure was analyzed only in the participants enrolled from the previous study - 156-04-251 who received placebo in previous study and received tolvaptan in this study, as pre-specified in the protocol. (NCT01214421)
Timeframe: Tolvaptan, Delayed Treated: Baseline to Month 24 in Study 156-08-271; Placebo: Baseline to Month 36 in Study 156-04-251

Interventionml/min/1.73m^2/participant-years (Number)
Tolvaptan, Delayed Treated (In Study 156-08-271)-3.211
Placebo (In Study 156-04-251)-3.572

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Annualized Slope of Total Kidney Volume (TKV) for Study 156-04-251 Participants Enrolled in Study 156-08-271

Annualized slope of TKV is a measure of renal function and disease progression in ADPKD participants. The annualized slope is calculated as percentage of growth in TKV (measured in mL by MRI) divided by each participant's years of participation for all participants was calculated using MMRM analysis in participants continuing from previous study (156-04-251) at Month 24 of this study (156-08-271) comparing annualized slope of TKV for the early-treated (those previously treated with tolvaptan) to delayed-treated (those previously treated with placebo). This outcome measure was analyzed only in the participants enrolled from the previous study - 156-04-251, as pre-specified in the protocol. (NCT01214421)
Timeframe: Study Baseline (Prior to Day 1 in Study 156-08-271) to Month 24 in this study (Study 156-08-271)

Interventionpercent change in TKV/participant-years (Number)
Tolvaptan, Early Treated (From Study 156-04-251: Tolvaptan)6.164
Tolvaptan, Delayed Treated (From Study 156-04-251: Placebo)4.960

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Annualized TKV Slope for Study 156-04-251 Placebo Participants Enrolled in Study 156-08-271

Annualized slope of TKV is a measure of renal function and disease progression in ADPKD participants. The annualized slope is calculated as percentage of growth in TKV (measured in mL by MRI) divided by each participant's years of participation, using MMRM analysis to compare annualized slope of TKV for the participants who received placebo in previous study (156-04-251) to annualized slope of TKV for the same participants who received tolvaptan in this study (156-08-271). This outcome measure was analyzed only in the participants enrolled from the previous study - 156-04-251 and who received placebo in the previous study, as pre-specified in the protocol. (NCT01214421)
Timeframe: Tolvaptan, Delayed Treated: Baseline to Month 24 in Study 156-08-271; Placebo: Baseline to Month 36 in Study 156-04-251

Interventionpercent change in TKV/participant-years (Number)
Tolvaptan, Delayed Treated (In Study 156-08-271)4.779
Placebo (In Study 156-04-251)5.627

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Change From the Baseline in Estimated Glomerular Filtration Rate (eGFR) as Assessed by Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) for Study 156-04-251 Participants Enrolled in This Study (156-08-271)

Estimated Glomerular Filtration Rate (eGFR) according to CKD-EPI is calculated using the CKD-EPI equation, expressed as a single equation, is GFR = 141 × min (serum creatinine [Scr]/κ, 1)α × max(Scr/κ, 1)^-1.209 × 0.993 Age × 1.018 (if female) × 1.159 (if black), where Scr is serum creatinine, κ is 0.7 for females and 0.9 for males, α is -0.329 for females and -0.411 for males, min indicates the minimum of Scr/ĸ or 1, and max indicates the maximum of Scr/κ or 1 in participants continuing from previous study (156-04-251) at Month 24 of this study (156-08-271) comparing change in eGFR for the early-treated (those previously treated with tolvaptan) to delayed-treated (those previously treated with placebo). MMRM was used for the analysis. This outcome measure was analyzed only in the participants enrolled from the previous - 156-04-251, as pre-specified in the protocol. (NCT01214421)
Timeframe: Study Baseline (Prior to Day 1 in Study 156-04-251) to Month 24 in this study (Study 156-08-271)

InterventionmL/min/1.73 square meters (m^2) (Least Squares Mean)
Tolvaptan, Early Treated (From Study 156-04-251: Tolvaptan)-16.77
Tolvaptan, Delayed Treated (From Study 156-04-251: Placebo)-19.92

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Change From Baseline in Serum Sodium Concentration (24 Hour Area Under the Curve [AUC]).

"Average 24 hour AUC of serum sodium concentration change from baseline, from Day 1 Hour 0 up to 72 hours post-first dose was assessed.~A serum sodium sample was drawn at pre-treament and 8, 24, 48, and 72 hours post-first dose. Serum sodium was also assessed between 36 and 72 hours after the last dose.~Analysis of AUC was for daily average AUC, hence the units or AUC are mEq/L/24 hours." (NCT01227512)
Timeframe: 0 to 72 hours

InterventionmEq/L (Least Squares Mean)
Tolvaptan 15-60mg/Day3.90
Placebo0.13

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Change From Baseline to 48 Hours Post Dose in Clinical Global Impression - Improvement (CGI-I) Score of Hyponatremia Symptoms.

"Change in CGI-I score at 48 hours post-first dose or discharge/rescue therapy, if earlier was assessed.~The CGI-I is a one-question rating scale where the participant is asked to rate total improvement whether or not, in their judgment, it is due entirely to trial treatment. Compared to his/her condition at admission to the trial, how much has he/she changed? 0=not assessed; 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse" (NCT01227512)
Timeframe: Baseline to 48 hours post dose

InterventionUnits on a scale (Median)
Tolvaptan 15-60mg/Day2.0
Placebo2.0

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Length of Hospital Stay (LoS)

LoS was time to clinically ready to be hospital discharged (CRBD) from study treatment initiation, disregarding prolonged hospitalization due solely to social factors. (NCT01227512)
Timeframe: 45 days

InterventionDays (Median)
Tolvaptan 15-60mg/Day3.5
Placebo4.0

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Percentage of Participants With Clinical Global Impression-Improvement (CGI-I) Score Improved to a Score of 1 or 2.

Percentage of responders (defined as CGI-I score of 1 = very much improved or 2 = much improved) at 48 hours post-first dose, or at discharge/rescue therapy, if earlier. Participants given rescue therapy were given a score of 7. (NCT01227512)
Timeframe: 48 hours post dose

InterventionPercentage of participants (Number)
Tolvaptan 15-60mg/Day57.8
Placebo52.7

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Time to First 2-point Improvement in CGI-S Score.

CGI-S data up to 72 hours were used to identify 2-point improvements. Please refer to outcome measure 2 for details on the scale. For the analysis of time to first 2-point improvement in CGI-S, CGI-S data up to Hour 72 were used to identify 2-point improvements. Data for participants who received rescue therapy were censored at the time of receiving rescue therapy. For participants who were discharged before Hour 72 without reaching 2-point improvement in CGI-S, data were censored at the time of discharge. Other participants who did not reach the 2-point improvement during the 72 hours also had their data censored at their last CGI-S observations within 72 hours. (NCT01227512)
Timeframe: Up to 72 hours

InterventionHours (Median)
Tolvaptan 15-60mg/Day51
Placebo69

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Change From Baseline to 24 and 72 Hours Post Dose in CGI-S of Hyponatremia Symptoms.

"Change in CGI-S of hyponatremia symptoms from pretreatment baseline at 24 and 72 hours post-first dose, or at discharge/rescue therapy if earlier was assessed.~The CGI-S is a one-question rating scale which was as follows: Considering your total clinical experience with hyponatremia symptoms in this particular population, how symptomatic is the patient at this time? 0=not assessed; 1=normal, not at all symtpmatic; 2=borderline symptomatic; 3=mildly symptomatic; 4=moderately symptomatic; 5=markedly symptomatic; 6=severely symptomatic; 7=among the most severly symptomatic patients." (NCT01227512)
Timeframe: Baseline to 24 and 72 hours post dose

,
InterventionUnits on a scale (Median)
Baseline24 hours post-doseChange from baseline at 24 hours72 hours post-doseChange from baseline at 72 hours
Placebo4.03.0-1.02.0-1.0
Tolvaptan 15-60mg/Day4.03.0-1.02.0-2.0

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Percentage of Participants Requiring Rescue Therapy for Hyponatremia

Percentage of participants requiring rescue therapy within first 7 days of treatment for hyponatremia. (NCT01227512)
Timeframe: 7 days

InterventionPercentage of participants (Number)
Tolvaptan 15-60mg/Day3.03
Placebo9.09

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Change From Baseline to 48 Hour Post Dose in Clinical Global Impression-Severity (CGI-S) of Hyponatremia Symptoms.

"Change from baseline in blinded rater assessed CGI-S at 48 hours post-first dose or at discharge/rescue therapy, if earlier was assessed.~The CGI-S is a one-question rating scale which was as follows: Considering your total clinical experience with hyponatremia symptoms in this particular population, how symptomatic is the patient at this time? 0=not assessed; 1=normal, not at all symtpmatic; 2=borderline symptomatic; 3=mildly symptomatic; 4=moderately symptomatic; 5=markedly symptomatic; 6=severely symptomatic; 7=among the most severly symptomatic patients." (NCT01227512)
Timeframe: Baseline to 48 hours post dose

,
InterventionUnits on a scale (Median)
Baseline48 hours post doseChange from baseline
Placebo4.03.0-1.0
Tolvaptan 15-60mg/Day4.02.0-1.0

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Renal Function Test (eGFR)

"Estimated glomerular filtration rate calculated by Japanese equation for eGFR during trial period.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT01280721)
Timeframe: Baseline, Month12, Month24, and Month36

InterventionmL/min/1.73 m2 (Mean)
Baseline61.2
Month 1256.3
Month 2451.8
Month 3643.5

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Renal Function Test (Cys-C)

Measured values of serum cystatin C concentration during trial period. Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded. (NCT01280721)
Timeframe: Baseline, Month 12, Month 24, and Month 36

Interventionmg/L (Mean)
Baselime1.016
Month 121.114
Month 241.129
Month 361.281

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Total Kidney Volume

"Measured values of total kidney volume (sum of the volume of the left and right kidneys) during trial period.~Twice-daily repeated oral administration of tolvaptan at daily doses of 60 to 120 mg.~Number of participants analyzed at each time point represents number of participants with data at the specified time point. Patients who were withdrawn from trial or have no appropriate data (e.g., interruption of medication, protocol deviation, etc.) are excluded." (NCT01280721)
Timeframe: Baseline, Month12, Month24, and Month36

InterventionmL (Mean)
Baseline1812.38
Month 121878.82
Month 241934.14
Month 362214.28

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Number of Patients With Abnormally Low Levels of Sodium (Sodium Levels Between 130 mmol/L and 135 mmol/L)

Number of Patients with new episodes of hyponatremia (abnormally low levels of sodium) defined as sodium >130 mmol/L and <135 mmol/L (NCT01292304)
Timeframe: 12 weeks

Interventionparticipants (Number)
Tolvaptan1

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Number of Participants With Worsening Ascites (Increase in Number of Paracentesis Procedures to Remove 2 Liters of Ascites Fluid)

Increase in number of therapeutic paracentesis (removal of > 2 litres of ascites fluid) during 12 weeks of study drug dosing versus 12 weeks before study drug dosing (NCT01292304)
Timeframe: Week 12

Interventionparticipants (Number)
Tolvaptan0

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Time From Baseline to Worsening Ascites (Requiring 1 or More Therapeutic Paracentesis to Remove Ascites Fluid)

This outcome will describe the average time from baseline for subjects to require a therapeutic paracentesis to remove ascites fluid. (NCT01292304)
Timeframe: 12 weeks of study drug

InterventionDays (Median)
Tolvaptan27

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Number of Subjects With Worsening Ascites (Defined as Greater Than 2 kg Weight Gain)

This outcome will provide the number of subjects with a weight increase of > 2kg from baseline (worsening ascites) (NCT01292304)
Timeframe: 12 weeks of study drug

Interventionparticipants (Number)
Tolvaptan7

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Number of Patients With Reduction of Ascites (Weight Loss of 2 kg or More)

Number of patients with reduction of ascites is defined as reduction of weight by at least 2 kg during study drug dosing (NCT01292304)
Timeframe: 12 weeks

Interventionparticipants (Number)
Tolvaptan0

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Mean Change From Baseline in Measured Glomerular Filtration Rate (mGFR) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.

Renal function measurements were performed using the constant infusion method with 125I-iothalamate and 131I-hippuran. A priming solution containing 20 mL infusion solution (0.04 MBq of 125I-iothalamate and 0.03 MBq of 131I-hippuran) was given at 08:00 hours, followed by a constant infusion of 6 to 12 mL/h, with the lowest infusion rates in subjects with impaired renal function, based on previously known serum creatinine concentrations. Plasma concentrations of both tracers were allowed to stabilize during a 1.5-hour equilibration, which was followed by two 2-hour periods (09:30 to 11:30 hours and 11:30 to 13:30 hours) for simultaneous clearances of 125I-iothalamate and 131I-hippuran. Blood was drawn at 1, 2, 3, 4, and 5 hours post consumption of water/tolvaptan (08:30 hours). The mGFR was corrected for voiding errors. (NCT01336972)
Timeframe: After 3 weeks of treatment and 3 weeks post treatment

,,
InterventionmL/min (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m2-0.7-1.2
eGFR > 60 mL/Min/1.73m2-8.00.1
eGFR 30-60 mL/Min/1.73m2-6.2-1.5

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Area Under the Concentration-time Curve From 0 to 5 Hours (AUC0-5) After 3 Weeks of Tolvaptan Treatment.

"Blood sampling for determination of tolvaptan concentrations took place at the Baseline, Final Treatment, and the Post Treatment or Early Termination visits.~At the Final Treatment visit (Day 21 [+/- 1 day)]), blood samples were collected prior to the start of infusion of study treatment and at 1, 2, 3, 4, and 5 hours postdose.~At the Baseline (Day 0), and Post Treatment visit (3 weeks [+/-3 days] after last dose), a blood sample was collected prior to the start of infusion of study treatment." (NCT01336972)
Timeframe: Day 0: 0 hour, Day 21: (0, 1, 2, 3, 4 and 5 hours postdose), 3 Weeks after last dose: 0 hour

Interventionng.h/mL (Mean)
eGFR > 60 mL/Min/1.73m22850
eGFR 30-60 mL/Min/1.73m22140
eGFR <30 mL/Min/1.73m23100

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Time to Peak Plasma Concentration (Cmax) After 3 Weeks of Tolvaptan Treatment.

"Blood sampling for determination of tolvaptan concentrations took place at the Baseline, Final Treatment, and the Post Treatment or Early Termination visits.~At the Final Treatment visit (Day 21 [+/- 1 day)]), blood samples were collected prior to the start of infusion of study treatment and at 1, 2, 3, 4, and 5 hours postdose.~At the Baseline (Day 0), and Post Treatment visit (3 weeks [+/-3 days] after last dose), a blood sample was collected prior to the start of infusion of study treatment." (NCT01336972)
Timeframe: Day 0: 0 hour, Day 21: (0, 1, 2, 3, 4 and 5 hours postdose), 3 Weeks after last dose: 0 hour

Interventionng/mL (Mean)
eGFR > 60 mL/Min/1.73m2828
eGFR 30-60 mL/Min/1.73m2591
eGFR <30 mL/Min/1.73m2840

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Time to Peak Plasma Concentration (Tmax) After 3 Weeks of Tolvaptan Treatment.

"Blood sampling for determination of tolvaptan concentrations took place at the Baseline, Final Treatment, and the Post Treatment or Early Termination visits.~At the Final Treatment visit (Day 21 [+/- 1 day)]), blood samples were collected prior to the start of infusion of study treatment and at 1, 2, 3, 4, and 5 hours postdose.~At the Baseline (Day 0), and Post Treatment visit (3 weeks [+/-3 days] after last dose), a blood sample was collected prior to the start of infusion of study treatment." (NCT01336972)
Timeframe: Day 0: 0 hour, Day 21: (0, 1, 2, 3, 4 and 5 hours postdose), 3 Weeks after last dose: 0 hour

Interventionhours (Median)
eGFR > 60 mL/Min/1.73m22.0
eGFR 30-60 mL/Min/1.73m22.0
eGFR <30 mL/Min/1.73m22.0

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Mean Change From Baseline in 2 Hour Urine Volume After 3 Weeks Tolvaptan Treatment and at 3 Weeks Post Treatment.

The volume of urine from each 2-hour urine collection in the renal function tests at Baseline, Final Treatment, and Post Treatment was recorded. Individual voids in a collection interval were pooled before determination of total volume. (NCT01336972)
Timeframe: 2 hours

,,
InterventionmL (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m2356.727.5
eGFR > 60 mL/Min/1.73m2888.9-187.8
eGFR 30-60 mL/Min/1.73m2625.6-10.0

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Mean Change From Baseline in 24 Hour Urine Volume After 3 Weeks Tolvaptan Treatment and at 3 Weeks Post Treatment.

A 24-hour split urine sample (approximate times: 0700 to 1700 hours, 1700 hours to bedtime, and bedtime to 0700 hours) was collected beginning the day before the Baseline, Final Treatment, and Post Treatment visits and ending at admission to the renal function ward. Individual voids in a collection interval were pooled and the total volume determined. (NCT01336972)
Timeframe: 24 hours

,,
InterventionmL (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m22215.0143.1
eGFR > 60 mL/Min/1.73m24551.1-312.2
eGFR 30-60 mL/Min/1.73m23274.4-287.2

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Mean Change From Baseline in Effective Renal Plasma Flow (ERPF) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.

Renal function measurements were performed using the constant infusion method with 125I-iothalamate and 131I-hippuran. A priming solution containing 20 mL infusion solution (0.04 MBq of 125I-iothalamate and 0.03 MBq of 131I-hippuran) was given at 08:00 hours, followed by a constant infusion of 6 to 12 mL/h, with the lowest infusion rates in subjects with impaired renal function, based on previously known serum creatinine concentrations. Plasma concentrations of both tracers were allowed to stabilize during a 1.5-hour equilibration, which was followed by two 2-hour periods (09:30 to 11:30 hours and 11:30 to 13:30 hours) for simultaneous clearances of 125I-iothalamate and 131I-hippuran. Blood was drawn at 1, 2, 3, 4, and 5 hours post consumption of water/tolvaptan (08:30 hours). (NCT01336972)
Timeframe: After 3 weeks of treatment and 3 weeks post treatment

,,
InterventionmL/min (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m2-1.7-1.3
eGFR > 60 mL/Min/1.73m2-16.94.3
eGFR 30-60 mL/Min/1.73m2-11.1-8.4

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Mean Change From Baseline in Filtration Fraction (GFR/ERFP) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.

Renal function measurements were performed using the constant infusion method with 125I-iothalamate and 131I-hippuran. A priming solution containing 20 mL infusion solution (0.04 MBq of 125I-iothalamate and 0.03 MBq of 131I-hippuran) was given at 08:00 hours, followed by a constant infusion of 6 to 12 mL/h, with the lowest infusion rates in subjects with impaired renal function, based on previously known serum creatinine concentrations. Plasma concentrations of both tracers were allowed to stabilize during a 1.5-hour equilibration, which was followed by two 2-hour periods (09:30 to 11:30 hours and 11:30 to 13:30 hours) for simultaneous clearances of 125I-iothalamate and 131I-hippuran. Blood was drawn at 1, 2, 3, 4, and 5 hours post consumption of water/tolvaptan (08:30 hours). (NCT01336972)
Timeframe: After 3 weeks of treatment and 3 weeks post treatment

,,
InterventionRatios (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m2-0.010-0.016
eGFR > 60 mL/Min/1.73m2-0.005-0.003
eGFR 30-60 mL/Min/1.73m2-0.0130.005

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Mean Change From Baseline in Free Water Clearance After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment

Renal function measurements were performed using the constant infusion method with 125I-iothalamate and 131I-hippuran. A priming solution containing 20 mL infusion solution (0.04 MBq of 125I-iothalamate and 0.03 MBq of 131I-hippuran) was given at 08:00 hours, followed by a constant infusion of 6 to 12 mL/h, with the lowest infusion rates in subjects with impaired renal function, based on previously known serum creatinine concentrations. Plasma concentrations of both tracers were allowed to stabilize during a 1.5-hour equilibration, which was followed by two 2-hour periods (09:30 to 11:30 hours and 11:30 to 13:30 hours) for simultaneous clearances of 125I-iothalamate and 131I-hippuran. Blood was drawn at 1, 2, 3, 4, and 5 hours post consumption of water/tolvaptan (08:30 hours). (NCT01336972)
Timeframe: After 3 weeks of treatment and 3 weeks post treatment

,,
InterventionmL/min (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m21.7010.382
eGFR > 60 mL/Min/1.73m24.334-0.675
eGFR 30-60 mL/Min/1.73m22.822-0.195

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Percentage Change From Baseline in Total Kidney Volume (TKV) After 3 Weeks of Tolvaptan Treatment and at 3 Weeks Post Treatment.

TKV was measured using magnetic resonance imaging. (NCT01336972)
Timeframe: After 3 weeks of treatment and 3 weeks post treatment

,,
InterventionPercent (Mean)
Final treatment change from BaselinePost treatment change from Baseline
eGFR <30 mL/Min/1.73m2-1.9-0.7
eGFR > 60 mL/Min/1.73m2-4.5-1.5
eGFR 30-60 mL/Min/1.73m2-4.6-2.4

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Body Weight

Change in body weight from baseline to 24 hours after tolvaptan administration (NCT01346072)
Timeframe: Change over 24 hours

InterventionKg (Mean)
Tolvaptan High Copeptin-1.3
Tolvaptan Low Copeptin-0.4

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Urine Output

Total urine output for 24 hours following tolvaptan administration (NCT01346072)
Timeframe: 24 hours

InterventionmL (Mean)
Tolvaptan High Copeptin6498
Tolvaptan Low Copeptin5784

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Plasma Brain Natriuretic Peptide (BNP) Concentration

The comparison of the average of amount of change from baseline. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionpg/mL (Mean)
Tolvaptan-72.60
Placebo-166.96

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Third Heart Sound

Of the subjects who had third heart sound at baseline, the number of subjects whose symptom was resolved at completion of treatment. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionparticipants (Number)
Tolvaptan8
Placebo10

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Pulmonary Rales

Of the subjects who had pulmonary rales at baseline, the number of subjects whose symptom was resolved at completion of treatment. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionparticipants (Number)
Tolvaptan13
Placebo9

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Pulmonary Congestion

Of the subjects who had pulmonary congestion at baseline, the number of subjects whose pulmonary congestion severity grading showed an improvement of one grade or more (eg, moderate to mild) at completion of treatment. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionparticipants (Number)
Tolvaptan24
Placebo20

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Body Weight

The comparison of the average of amount of change from baseline. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionkg (Mean)
Tolvaptan-1.99
Placebo-1.20

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Cardiothoracic Ratio

"Investigator majored Thoracic length and Cardiac length from chest X-ray. Cardiothoracic Ratio was calculated from Cardiac length/Thoracic length*100. Lowering of Cardiothoracic Ratio suggests recovery from heart congestion.~The comparison of the average of amount of change from baseline. Statistical comparison was not done." (NCT01439009)
Timeframe: Day15

InterventionPercentage (Mean)
Tolvaptan-2.13
Placebo-0.83

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Change in Liver Size From Baseline

The comparison of the average of amount of change from baseline. Statistical comparison was not done． (NCT01439009)
Timeframe: Day15

Interventioncm (Mean)
Tolvaptan-0.20
Placebo-0.19

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Cummulative Incidence of Events at Week 26

"From start day of IMP administration to final day of follow up period, 1) and 2) below were defined as event~Death from cardiovascular events~Worsening of heart failure~The day of re-hospitalization due to worsening of heart failure~The day of medication below due to worsening of heart failure Phosphodiesterase III inhibitors (Injection), Catecholamine preparations (Injection), Colforsin preparations (Injection), Diuretics (Injection), Human atrial natriuretic peptide preparations (Injection)：Calperitide (Injection)" (NCT01439009)
Timeframe: Week 26

InterventionPercentage of events at 26 weeks (Number)
Tolvaptan35.6
Placebo43.8

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Dypnea

Of the subjects who had dyspnoea at baseline, the number of subjects whose symptom was resolved at completion of treatment. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionparticipants (Number)
Tolvaptan11
Placebo12

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Jugular Venous Distension

The comparison of the average of amount of change from baseline. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventioncm (Mean)
Tolvaptan-0.94
Placebo-1.23

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Number of Subjects Whose Lower Limb Edema Severity Grading Improved by One or More Grade

Of the subjects who had lower limb edema at baseline, the number of subjects whose lower limb edema severity grading. Statistical comparison was not done. (NCT01439009)
Timeframe: Day15

Interventionparticipants (Number)
Tolvaptan27
Placebo16

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Mortality （Number of Death）

Statistical comparison was not done. (NCT01439009)
Timeframe: Week26

Interventionparticipants (Number)
Tolvaptan2
Placebo3

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Number of Subjects Whose New York Heart Association (NYHA) Classification Improved by One More Grade From Baseline

"New York Heart Association (NYHA) Classification is below ClassI：No limitation of physical activity. Ordinary physical activity does not cause undue fatigue, palpitation, dyspnea (shortness of breath).~ClassII：Slight limitation of physical activity. Comfortable at rest. Ordinary physical activity results in fatigue, palpitation, dyspnea (shortness of breath).~ClassIII：Marked limitation of physical activity. Comfortable at rest. Less than ordinary activity causes fatigue, palpitation, or dyspnea.~ClassIV：Unable to carry on any physical activity without discomfort. Symptoms of heart failure at rest. If any physical activity is undertaken, discomfort increases." (NCT01439009)
Timeframe: The day after last IMP administration and Baseline

Interventionparticipants (Number)
Tolvaptan22
Placebo24

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Percent Change From Baseline in TKV at Week 8.

Total kidney volume is an important measure of disease progression. A 3-week time point is adequate to assess acute effects on kidney cyst shrinkage. (NCT01451827)
Timeframe: Baseline to Week 8

InterventionPercentage change (Mean)
Tolvaptan MR 50 mg-2.04
Tolvaptan MR 80 mg-2.02
Tolvaptan IR 60/30 mg-0.08
Placebo2.13

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Percent Change From Baseline in Total Kidney Volume (TKV) at Week 3

The primary endpoint was percent change from baseline in TKV at Week 3. Total kidney volume is an important measure of disease progression. A 3-week time point is adequate to assess acute effects on kidney cyst shrinkage. (NCT01451827)
Timeframe: Baseline to Week 3

InterventionPercentage change (Mean)
Tolvaptan MR 50 mg-2.46
Tolvaptan MR 80 mg-2.55
Tolvaptan IR 60/30 mg-1.17
Placebo0.09

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Change From Baseline in Total Score of the Autosomal Dominant Polycystic Kidney Disease Urinary Impact Scale (ADPKD-UIS)

The ADPKD-UIS was a self-administered questionnaire designed to measure ADPKD-related urinary symptoms in participants with ADPKD. This instrument contained 11 items in 3 domains (Urinary Frequency, Urinary Urgency, and Nocturia). Each item was scored using a scale of 1 to 5 (a higher score indicated increased difficulty/extremely bothered). The maximum total score is 55; 1: not difficult/not bothered at all; 55: extremely difficult/extremely bothered. (NCT01451827)
Timeframe: Baseline to Week 8

,,,
InterventionUnit on a scale (Mean)
Urinary FrequencyUrinary UrgencyNocturia
Placebo0.100.050.11
Tolvaptan IR 60/30 mg0.991.011.36
Tolvaptan MR 50 mg0.740.690.97
Tolvaptan MR 80 mg0.820.661.15

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All Cause Death or Rehospitalization

All cause death or rehospitalization (to include unscheduled clinic visits or ED visits) at 30 days (Kaplan-Meier and 95% confidence interval) (NCT01644331)
Timeframe: 30 days

Interventionproportion of participants (Mean)
Tolvaptan0.33
Placebo0.29

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Days Hospitalized or Deceased

Total days hospitalized or deceased during the 30 days after randomization (NCT01644331)
Timeframe: 30 days

Interventiondays (Mean)
Tolvaptan10.19
Placebo11.69

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Development of Worsening Renal Function

increase in serum creatinine ≥ 0.3mg/dl from randomization at any time point during 72 hours after randomization (NCT01644331)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Tolvaptan50
Placebo34

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Dyspnea Improvement Measured by Likert Scale at 8 and 24 Hours

The number of patients with at least moderate improvement (as reported by patient) in dyspnea Likert scale at both 8 AND 24 hours AND without the need for escalation of therapy due to worsening heart failure (rescue therapy) or death within 24 hours. (NCT01644331)
Timeframe: 8 and 24 hours

InterventionParticipants (Count of Participants)
Tolvaptan20
Placebo26

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Renal Function

Change in Serum creatinine from baseline to 24, 48 and 72 hours (NCT01644331)
Timeframe: 0, 24, 48 and 72 hours

,
Interventionmg/dL (Mean)
24 hours48 hours72 hours
Placebo0.040.050.06
Tolvaptan0.130.100.03

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Hospital Stay

Total days spent in hospital from baseline until discharge or death (NCT01644331)
Timeframe: 7 days

Interventiondays (Mean)
Tolvaptan6.46
Placebo7.35

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Over-diuresis

clinical evidence of volume depletion requiring intervention other than holding diuretics during the 72 hours after randomization (NCT01644331)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Tolvaptan7
Placebo3

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Worsening or Persistent Heart Failure or Death

Number of patients with worsening heart failure or death (NCT01644331)
Timeframe: 72 hrs

InterventionParticipants (Count of Participants)
Tolvaptan54
Placebo60

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Dyspnea 11 Point NRS

Change in NRS for assessment of dyspnea from baseline to 24, 48, and 72 hours (scale ranges from 0-No difficulty breathing to 10-Difficulty as bad as you can imagine) (NCT01644331)
Timeframe: 0, 24, 48, and 72 hours

,
Interventionunits on a scale (Mean)
24 hours48 hours72 hours
Placebo-1.84-2.29-2.42
Tolvaptan-2.20-2.85-3.07

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Dyspnea Likert

Number of patients that experience moderate or greater improvement (patient reported) in dyspnea by 7 point Likert scale at 48 and 72 hours (NCT01644331)
Timeframe: 48 and 72 hours

,
InterventionParticipants (Count of Participants)
48 hours72 hours
Placebo7448
Tolvaptan8869

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Fluid Loss

Change from baseline fluid balance at 24, 48, and 72 hours (NCT01644331)
Timeframe: 0, 24, 48, and 72 hours

,
InterventionmL (Mean)
24 hours48 hours72 hours
Placebo-1541.48-1419.09-1401.24
Tolvaptan-2182.25-1948.01-1757.09

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Freedom From Congestion

Jugular Venous Pressure (JVP) < 8 cm, no orthopnea, trace peripheral edema or less, and will be assessed at 24, 48, and 72 hours (NCT01644331)
Timeframe: 24, 48, and 72 hours

,
InterventionParticipants (Count of Participants)
24 hours48 hours72 hours
Placebo122017
Tolvaptan92427

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Serum Sodium

Change in serum sodium from baseline to 24, 48, and 72 hours (NCT01644331)
Timeframe: 0, 24, 48, and 72 hours

,
Interventionmmol/L (Mean)
24 hours48 hours72 hours
Placebo0.23-0.24-0.44
Tolvaptan3.183.342.84

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Weight Loss

Change in body weight from baseline to 24, 48, and 72 hours (NCT01644331)
Timeframe: 0, 24, 48, and 72 hours

,
Interventionlbs (Mean)
24 hours48 hours72 hours
Placebo-1.16-3.46-5.53
Tolvaptan-4.41-6.11-8.19

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Change in Body Weight From Baseline at Final IMP Administration

Body weight was measured in 100-g units before breakfast and after subjects had urinated at least once, taking care to minimize fluctuations due to defecation or clothing. (NCT01684202)
Timeframe: Baseline, at the final IMP administration (shortest:7days longest:12days)

InterventionKg (Mean)
OPC-41061 3.75 mg-0.69
OPC-41061 7.5 mg-0.34
OPC-41061 15 mg-1.13
OPC-41061 30 mg0.70

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Change in Ascites Volume From Baseline Measured by Computer Tomography (CT) at Final IMP Administration

(NCT01684202)
Timeframe: Baseline, at the final IMP administration (shortest:7days longest:12days)

InterventionmL (Mean)
OPC-41061 3.75 mg-77.20
OPC-41061 7.5 mg513.97
OPC-41061 15 mg153.72
OPC-41061 30 mg539.93

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Change From Baseline in Daily Urine Volume

The daily urine volume at each timepoint and its change and the percent change from baseline will be summarized with descriptive statistics (number, mean, standard deviation [SD], minimum, median, maximum [same for following parameters]). (NCT01876381)
Timeframe: Baseline and Day 14 (Intermittent Administration Period)

Interventionml (Mean)
OPC-41061481.0

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Change From Baseline in Total Fluid Removal Per Week by Dialysis

The total volume of fluid removed per week by dialysis at each timepoint and its change from baseline will be summarized with descriptive statistics. (NCT01876381)
Timeframe: Baseline (pretreatment observation period) and Intermittent Administration Period (Day 10 to Day 15)

Interventionml (Mean)
OPC-41061-1425.0

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Change in Body Weight From Baseline

Change in body weight from baseline during the repeated-administration period(For five days). (NCT01895322)
Timeframe: Body weight on day13 minus Body weight at baseline(day9) on the repeated-administration period

Interventionkg (Mean)
OPC-41061-0.61

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Change in Daily Urine Volume From Baseline

Change in daily urine volume from baseline during the repeated-administration period (For five days). (NCT01895322)
Timeframe: Urine Volume on day13 minus Urine Volume at baseline(day9) on the repeated-administration period.

InterventionmL (Mean)
OPC-4106118.3

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Percent Change in Body Weight

Percent change in body weight from baseline during the repeated-administration period(For five days). (NCT01895322)
Timeframe: 100%*

InterventionPercentage (Mean)
OPC-41061-0.92

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Percent Change in Daily Urine Volume From Baseline

Percent change in daily urine volume from baseline during the repeated-administration period (For five days). (NCT01895322)
Timeframe: 100%*

InterventionPercentage (Mean)
OPC-410618.89

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Change From Baseline in Fluid Balance (Fluid Intake Minus Urine Output) From 0-6 Hours, 0-12 Hours and 0-24 Hours.

Fluid intake was monitored on Day 0 (times relative to Day 1 dosing), and Day 1 at intervals of 0 to 6, 6 to 12, and 12 to 24 hours postdose. Fluid intake included fluid used for dosing (study medication and any concomitant medication); food items that included any significant amounts of water (e.g., Jello [including Gelatin and Jelly dessert] and soup) was added to the total fluid intake. Urine was collected for baseline comparison on Day 0 for the 24 hour prior to Day 1 dosing at intervals of 0 to 2, 2 to 4, 4 to 6, 6 to 8, 8 to 12 hours, and 12 to 24 hours relative to the Day 1 dosing time. Fluid balance was determined as fluid intake minus urine output. (NCT02009878)
Timeframe: 2 days

,,
InterventionmL (Mean)
Day 1 (0 to 6 hour)Day 1 (0 to 12 hour)Day 1 (0 to 24 hour)
Tolvaptan 15 mg-1478.8-1897.5-1700.6
Tolvaptan 3.75 mg-403.7-588.8-278.3
Tolvaptan 7.5 mg-856.8-839.8-537.8

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Maximal Increase From Baseline in Serum Sodium Concentration Following Tolvaptan Administration.

Maximal increase in serum sodium is summarized below by tolvaptan dose. Blood samples for determination of plasma concentrations of tolvaptan were collected predose and at 1, 2, 3, 4, 6, 8, 12, 16, and 24 hours postdose on Day 1 or at Early Termination (ET). (NCT02009878)
Timeframe: Baseline to Day 2

Interventionmmol/L (Mean)
Tolvaptan 3.75 mg3.6
Tolvaptan 7.5 mg5.3
Tolvaptan 15 mg7.9

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Time of Maximal Increase From Baseline in Serum Sodium Concentration Following Tolvaptan Administration.

Time of maximal increase in serum sodium is summarized in the table below by tolvaptan dose. Samples were taken on Day 0 (baseline) at the corresponding Day 1 predose time and 12 hours postdose time; and on Day 1 at predose and at 2, 4, 6, 8, 12, and 24 hours postdose. (NCT02009878)
Timeframe: Baseline to Day 2

Interventionhours (Median)
Tolvaptan 3.75 mg24.13
Tolvaptan 7.5 mg6.38
Tolvaptan 15 mg24.02

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Tmax (Time to Maximum (Peak) Plasma Concentration) for Tolvaptan in Plasma

Blood samples for determination of plasma concentrations of tolvaptan were collected predose and 1, 2, 3, 4, 8, 12, 16, and 24 hours postdose on Day 1 or at ET. PK parameters in participants with SIADH following tolvaptan administration for three different doses are presented below. (NCT02009878)
Timeframe: Baseline to Day 2

Interventionhours (Median)
Tolvaptan 3.75 mg1.50
Tolvaptan 7.5 mg2.00
Tolvaptan 15 mg2.00

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Change From Baseline in Cumulative Urine Volume at 0-6 Hours, 0-12 Hours and 0-24 Hours.

Urine was collected for baseline comparison on Day 0 for the 24 hour prior to Day 1 dosing at intervals of 0 to 2, 2 to 4, 4, to 6, 6, to 8, 8, to 12, and 12 to 24 hours relative to Day 1 dosing time. Urine was collected on Day 1 at intervals of 0 to 2,2 to 4, 4 to 6, 6 to 8, 8 to 12, and 12 to 24 hours postdose. For the start of the urine collection on Day 0, a window of 15 to 40 minutes prior to the assigned dosing time was acceptable, with the 0 to 24 hour collection period on Day 1 starting 24 hours after the start time on Day 0. Participants were asked to void immediately prior to the end of the collection interval. The volume of individual voids were measured and recorded prior to refrigerating. All voids in a collection interval were pooled at the end of the collection interval, at which time the volume was determined, recorded and an aliquot taken for osmolality, sodium, potassium, and creatinine assessments. (NCT02009878)
Timeframe: 2 days

,,
InterventionmL (Mean)
Day 1 (0 to 6 hour)Day 1 (0 to 12 hour)Day 1 (0 to 24 hour)
Tolvaptan 15 mg1375.62016.32226.3
Tolvaptan 3.75 mg501.2798.8639.3
Tolvaptan 7.5 mg601.8774.8666.8

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Change From Baseline in Fluid Intake From 0-6 Hours, 0-12 Hours and 0-24 Hours

Fluid intake was monitored on Day 0 (times relative to Day 1 dosing), and Day 1 at intervals of 0 to 6, 6 to 12, and 12 to 24 hours postdose. Fluid intake included fluid used for dosing (study medication and any concomitant medication); food items that included any significant amounts of water (e.g., Jello [including Gelatin and Jelly dessert] and soup) was added to the total fluid intake. Samples were taken on Day 0 (baseline) at the corresponding Day 1 predose time and 12 hours postdose time; and on Day 1 at predose and at 2, 4, 6, 8, 12, and 24 hours postdose. (NCT02009878)
Timeframe: Baseline and Day 2

,,
InterventionmL (Mean)
Day 1 (0 to 6 hour)Day 1 (0 to 12 hour)Day 1 (0 to 24 hour)
Tolvaptan 15 mg-103.0118.8525.6
Tolvaptan 3.75 mg97.5210.0361.0
Tolvaptan 7.5 mg-255.0-65.0129.0

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Change From Baseline in Serum Sodium Concentrations

Samples were taken on Day 0 (baseline) at the corresponding Day 1 predose time and 12 hours postdose time; and on Day 1 at predose and at 2, 4, 6, 8, 12, and 24 hours postdose. (NCT02009878)
Timeframe: Baseline and Day 2

,,
Interventionmmol/L (Mean)
(Day 0) 12 hour (N= 10, 9, 9)(Day 1) 2 hour (N= 10, 10, 8)(Day 1) 4 hour (N= 10, 10, 8)(Day 1) 6 hour (N= 10, 10, 8)(Day 1) 8 hour (N= 10, 10, 8)(Day 1) 12 hour (N= 9, 10, 9)(Day 1) 24 hour (N= 10, 10, 9)
Tolvaptan 15 mg-2.61.73.05.35.45.97.4
Tolvaptan 3.75 mg-2.5-2.0-1.7-0.10.0-0.62.9
Tolvaptan 7.5 mg-2.32.43.53.13.23.64.6

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AUC Infinity (Area Under the Concentration-time Curve From Time Zero to Infinity) for Tolvaptan in Plasma

Blood samples for determination of plasma concentrations of tolvaptan were collected predose and 1, 2, 3, 4, 8, 12, 16, and 24 hours postdose on Day 1 or at ET. If an indwelling catheter was utilized, saline flushes were used. PK parameters in participants with SIADH following tolvaptan administration for three different doses are presented below. (NCT02009878)
Timeframe: Baseline to Day 2

Interventionng·h/mL (Mean)
Tolvaptan 3.75 mg244
Tolvaptan 7.5 mg655
Tolvaptan 15 mg1000

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Cmax (Maximum (Peak) Plasma Concentration) for Tolvaptan in Plasma.

Blood samples for determination of plasma concentrations of tolvaptan were collected predose and 1, 2, 3, 4, 8, 12, 16, and 24 hours postdose on Day 1 or at ET. PK parameters in participants with SIADH following tolvaptan administration for three different doses are presented below. (NCT02009878)
Timeframe: Baseline to Day 2

Interventionng/mL (Mean)
Tolvaptan 3.75 mg37.7
Tolvaptan 7.5 mg107
Tolvaptan 15 mg157

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Change In Serum Sodium Concentration For Responders

Change in serum sodium concentration (mEq/L) for responders from Day 2 (or Day 2a) at the end of Treatment Phase A (where all participants received tolvaptan) to the end of Treatment Phase B for the Early compared to Late Withdrawal groups is reported. Once a participant was randomized to Treatment Phase B, any additional therapies for the purpose of raising serum sodium, including fluid restriction, were considered rescue therapy. Upon receipt of rescue therapy, a participant's endpoint data was collected and then censored from the efficacy analysis thereafter, unless specified. (NCT02012959)
Timeframe: Day 2/2a, Day 4

InterventionmEq/L (Mean)
Responder - Late Withdrawal-4.0
Responder - Early Withdrawal-1.0

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Change In Serum Sodium Concentration During Treatment Phase A

Change in serum sodium concentration (mEq/L) from baseline to the end of Day 2 (or 2a) during Treatment Phase A for all participants (responders and non-responders) is reported. (NCT02012959)
Timeframe: Baseline, Day 2/2a

InterventionmEq/L (Mean)
Day 1: 24 hours Post DoseDay 2: 24 hours Post DoseDay 2a: 24 hours Post Dose
Phase A: All Participants13.42.3

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Fluid Balance (Intake Minus Output) During Treatment Phase A

Every 6 hours and for the 24-hour daily interval on Days 1 and 2 during Treatment Phase A, fluid balance (milliliters [mL]) was determined by fluid intake (oral and intravenous) minus urine output. Improved fluid balance would be indicated through the induction of increased urine volume. Fluid balance was monitored per institutional guidelines. (NCT02012959)
Timeframe: Every 6 hours on Days 1 and 2

InterventionmL (Mean)
Day 1: 0-6 hoursDay 1: 6-12 hoursDay 1: 12-18 hoursDay 1: 18-24 hoursDay 1: 0-24 hoursDay 2: 0-6 hoursDay 2: 6-12 hoursDay 2: 12-18 hoursDay 2: 18-24 hoursDay 2: 0-24 hours
Phase A: All Participants-1-261-3631-268-1016-45-21-160

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Change From Baseline In PedsQL GCS Psychosocial Health Summary Score At Month 6

The PedsQL GCS was used for quality of life assessment. It is appropriate for at least 2 years of age, however availability may be limited for certain ages and languages. It encompasses 4 dimensions of functioning (physical, emotional, social, school). The age groups covered are: Toddler (2-4 years), Young child (5-7 years), Child (8-12 years), and Adolescent (13-18 years). Depending on the participant's age, the questionnaire may be completed by either the participant or the parent/caregiver, as appropriate. For the Toddler group, the PedsQL GCS consists of 21 items, using a 5-point Likert scale (0 to 4); for all other groups, the PedsQL GCS consists of 23 items, with a 3-point Likert scale (0, 2, 4) for the Young Child, and a 5-point Likert scale for the Child and Adolescent groups. Scores are transformed on a scale from 0 to 100 and averaged. Higher scores indicate improved quality of life. The change from baseline in summed emotional, social, and school dimensions is presented. (NCT02020278)
Timeframe: Baseline, Month 6

Interventionunits on a scale (Mean)
Core Safety Follow-up Component-13.5

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Change From Baseline In PedsQL Multidimensional Fatigue Scale (MFS) Total Score At Month 6

The PedsQL GCS was used for quality of life assessment. It is appropriate for at least 2 years of age, however availability may be limited for certain ages and languages. It encompasses 4 dimensions of functioning (physical, emotional, social, school). The age groups covered are: Toddler (2-4 years), Young child (5-7 years), Child (8-12 years), and Adolescent (13-18 years). Depending on the participant's age, the questionnaire may be completed by either the participant or the parent/caregiver, as appropriate. For the Toddler group, the PedsQL GCS consists of 21 items, using a 5-point Likert scale (0 to 4); for all other groups, the PedsQL GCS consists of 23 items, with a 3-point Likert scale (0, 2, 4) for the Young Child, and a 5-point Likert scale for the Child and Adolescent groups. Scores are transformed on a scale from 0 to 100 and averaged. Higher scores indicate improved quality of life. The change from baseline in summed emotional, social, and school dimensions is presented. (NCT02020278)
Timeframe: Baseline, Month 6

Interventionunits on a scale (Mean)
Core Safety Follow-up Component9.7

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Participants With A Tanner Staging Score Of 1 At Month 6

Tanner Staging assessment consists of 2 domains (pubic hair and breast development) for girls and 3 domains (pubic hair, penis development, and testes development) for boys. Staging was based on a single score summarizing the domains (not individual domain scores). Stages range from 1-5, with 1 indicating preadolescent and 5 adult. Participants with a Tanner staging score of 1 (preadolescent) at Month 6 are reported. (NCT02020278)
Timeframe: Month 6

InterventionParticipants (Count of Participants)
Core Safety Follow-up Component2

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Change From Baseline In Alanine Aminotransferase (ALT) And Aspartate Aminotransferase (AST) For Participants On Tolvaptan At Month 2

No enrolled participant received any investigational medicinal product during the study. Due to early study termination, efficacy data were not collected. Data reported only include assessments made for ALT and AST during the Core Safety Follow-up Component of the trial. Results are reported in units/liter (U/L). (NCT02020278)
Timeframe: Baseline, Month 2

InterventionU/L (Mean)
ALTAST
Core Safety Follow-up Component-10.00-7.50

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Change From Baseline In Growth Percentiles For Body Height And Weight At Month 6

Changes from baseline in growth percentiles for body height and weight were calculated and are reported. (NCT02020278)
Timeframe: Baseline, Month 6

Interventionpercentile (Mean)
Height PercentileWeight Percentile
Core Safety Follow-up Component19.00.7

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Change From Baseline In Bilirubin For Participants On Tolvaptan At Month 2

No enrolled participant received any investigational medicinal product during the study. Due to early study termination, efficacy data were not collected. Data reported only include assessments made for bilirubin during the Core Safety Follow-up Component of the trial. Results are reported in micromoles (umol)/L. (NCT02020278)
Timeframe: Baseline, Month 2

Interventionumol/L (Mean)
Core Safety Follow-up Component2.57

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Change From Baseline In Pediatric Quality of Life Inventory (PedsQL) Generic Core Scale (GCS) Total Score At Month 6

The PedsQL GCS was used for quality of life assessment. It is appropriate for at least 2 years of age, however availability may be limited for certain ages and languages. It encompasses 4 dimensions of functioning (physical, emotional, social, school). The age groups covered are: Toddler (2-4 years), Young child (5-7 years), Child (8-12 years), and Adolescent (13-18 years). Depending on the participant's age, the questionnaire may be completed by either the participant or the parent/caregiver, as appropriate. For the Toddler group, the PedsQL GCS consists of 21 items, using a 5-point Likert scale (0 to 4); for all other groups, the PedsQL GCS consists of 23 items, with a 3-point Likert scale (0, 2, 4) for the Young Child, and a 5-point Likert scale for the Child and Adolescent groups. Scores are transformed on a scale from 0 to 100 and averaged. Higher scores indicate improved quality of life. The change from baseline in the GCS total score is presented. (NCT02020278)
Timeframe: Baseline, Month 6

Interventionunits on a scale (Mean)
Core Safety Follow-up Component-3.5

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Change From Baseline In PedsQL GCS Physical Health Summary Score At Month 6

The PedsQL GCS was used for quality of life assessment. It is appropriate for at least 2 years of age, however availability may be limited for certain ages and languages. It encompasses 4 dimensions of functioning (physical, emotional, social, school). The age groups covered are: Toddler (2-4 years), Young child (5-7 years), Child (8-12 years), and Adolescent (13-18 years). Depending on the participant's age, the questionnaire may be completed by either the participant or the parent/caregiver, as appropriate. For the Toddler group, the PedsQL GCS consists of 21 items, using a 5-point Likert scale (0 to 4); for all other groups, the PedsQL GCS consists of 23 items, with a 3-point Likert scale (0, 2, 4) for the Young Child, and a 5-point Likert scale for the Child and Adolescent groups. Scores are transformed on a scale from 0 to 100 and averaged. Higher scores indicate improved quality of life. The change from baseline in the physical health dimension is presented. (NCT02020278)
Timeframe: Baseline, Month 6

Interventionunits on a scale (Mean)
Core Safety Follow-up Component12.5

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Blood Sodium Concentration

Measurement of blood sodium concentration will determine if normonatremia (blood sodium concentrations within the normal physiological range of 135-145mmol/L) were maintained throughout the trial with appropriate fluid intake during the V2R antagonist, agonist and placebo intervention trials. (NCT02084797)
Timeframe: 4 study trials (4 weeks)

InterventionmEq/L (Mean)
PlaceboV2R AgonistV2R Antagonist
1/Placebo, V2R Agonist, V2R Antagonist143.6144.3145.9

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Saliva Sodium Concentration

Measurement of salivary sodium concentration will allow us to determine if the V2R antagonist, agonist and placebo interventions activate aquaporin-5 (AQP5) water channels that are also located in sweat glands. If the V2R acts on the sweat glands through AQP5, there should be parallel changes in sweat, urine and saliva sodium concentrations with each pharmaceutical intervention. (NCT02084797)
Timeframe: 4 trials (4 weeks)

InterventionmEq/L (Mean)
PlaceboV2R AgonistV2R Antagonist
1/Placebo, V2R Agonist, V2R Antagonist20.528.131.0

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Sweat Sodium Concentration Obtained After the Steady-state Portion of the Trial

Changes in sweat sodium concentration will parallel changes in urine sodium concentration with use of the V2R antagonist, agonist and placebo if the primary hypothesis is true (sweat sodium is regulated by the V2R, similar to how urine sodium is regulated by principle cells located within in the kidney collecting duct) (NCT02084797)
Timeframe: 4 study trials (4 weeks)

InterventionmEq/L (Mean)
PlaceboV2R AgonistV2R Antagonist
1/Placebo, V2R Agonist, V2R Antagonist80.176.884.7

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Urine Sodium Concentration After the Steady-state Portion of the Trial

Changes in urine sodium concentration after use of the V2R antagonist, agonist and placebo interventions will verify whether or not pharmacologic activation or inhibition was successfully induced. (NCT02084797)
Timeframe: 4 study trials (4 weeks)

InterventionmEq/L (Mean)
PlaceboV2R AgonistV2R Antagonist
1/Placebo, V2R Agonist, V2R Antagonist82.089.316.4

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Mean Change From Baseline in Urine Osmolality During the Double-blind Treatment Period and Post-treatment Follow-up

The mean change from baseline in urine osmolality for the double-blind treatment period collection timepoints and post-treatment follow-up are presented. Baseline was defined as the last evaluation prior to post-randomization dosing. (NCT02160145)
Timeframe: Baseline and Months 3, 6, 9 and 12 (End of treatment visit) of the double-blind treatment period, and post-treatment follow-up.

,
Interventionmilliosmole per kilogram (mOSm/kg) (Mean)
Month 3Month 6Month 9Month12Follow-up
Placebo177.7179.1179.9180.3179.5
Tolvaptan10.222.930.436.9162.4

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Mean Annualized Slope of eGFR Change

"To compare the efficacy of tolvaptan treatment in reducing the decline of annualized eGFR slope, as compared with placebo, in subjects with late-stage CKD due to ADPKD who tolerated tolvaptan during an initial run-in period, the annualized rate of eGFR change was derived from each individual subject's eGFR slope using the CKD-EPI formula.~The annualized eGFR change slope was derived from all eGFR observations from placebo-run-in, tolvaptan run-in, double-blind treatment and post-treatment follow-up periods using the linear mixed model of analysis. The mean annualized slope of eGFR change is presented." (NCT02160145)
Timeframe: Pretreatment baseline to post-treatment follow-up (up to 61 weeks).

InterventionmL/min/1.73m^2/year (Least Squares Mean)
Tolvaptan-3.160
Placebo-4.170

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Mean Change From Baseline in Urine Specific Gravity During the Double-blind Treatment Period and Post-treatment Follow-up

The mean change from baseline in urine specific gravity for the double-blind treatment period collection timepoints and post-treatment follow up are presented. Baseline was defined as the last evaluation prior to post-randomization dosing. (NCT02160145)
Timeframe: Baseline and Months 3, 6, 9 and 12 (End of treatment visit) of the double-blind treatment period, and post-treatment follow-up.

,
Interventionunitless (Mean)
Month 3Month 6Month 9Month 12Follow-up
Placebo0.00410.00420.00400.00400.0040
Tolvaptan0.00010.00030.0040.00060.0037

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The Mean Annualized Change in eGFR From Pretreatment Baseline to Post-treatment Follow-up.

"The mean annualized change in eGFR was calculated using the Chronic Kidney Disease-Epidemiology (CKD-EPI) formula from pretreatment baseline to post-treatment follow-up, annualized (divided) by each subject's trial duration.~The baseline for the primary endpoint was defined as the average of up to 3 eGFR values observed during the screening and placebo run-in periods." (NCT02160145)
Timeframe: Pretreatment baseline to post-treatment follow-up (up to 61 weeks).

InterventionmL/min/1.73 m^2/year (Least Squares Mean)
Tolvaptan-2.339
Placebo-3.610

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Median Urine Output at 24 Hours Post Randomization

(NCT02183792)
Timeframe: 24 hours post randomization

InterventionmL (Median)
Tolvaptan2910
Furosemide3150

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Median Change in Serum Creatinine at 24 Hours Post Randomization

Comparison between baseline and 24 hours post randomization concentrations. (NCT02183792)
Timeframe: 24 hours post randomization

,
Interventionmg/dL (Median)
Median Scr at BaselineMedian Scr at 24hMedian 24h Change
Furosemide0.870.96-0.01
Tolvaptan1.151.06-0.08

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Number Of Participants Reporting Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) was as any untoward medical occurrence associated with the use of an investigational medicinal product (IMP), whether or not considered IMP related. A TEAE was an AE that started after trial drug treatment; or if the event was continuous from baseline and was serious, related to IMP, or resulted in death, discontinuation, interruption or reduction of trial therapy. A serious TEAE included any event that resulted in: death, life-threatening, persistent or significant incapacity, substantial disruption of ability to conduct normal life functions, required inpatient hospitalization, prolonged hospitalization, congenital anomaly/birth defect, or other medically significant events as per medical judgment, that jeopardized the participant and that required medical or surgical intervention. A severe TEAE was an inability to work or perform normal daily activity. A summary of serious and all other non-serious TEAEs, regardless of causality, is located in the AE section. (NCT02251275)
Timeframe: Baseline through end of treatment (up to 42 months) and follow-up 7 days posttreatment(+ 7 days)

,,,,
Interventionparticipants (Number)
Participants with TEAEsParticipants with serious TEAEsParticipants with severe TEAEsDiscontinued due to TEAEsDeaths
Tolvaptan (From 156-08-271: Tolvaptan)64010383383
Tolvaptan (From 156-13-210: Placebo)5319678655
Tolvaptan (From 156-13-210: Tolvaptan)4738774331
Tolvaptan (From Other: Placebo)32110
Tolvaptan (From Other: Tolvaptan)61200

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Change in Total Volume of Fluid Removed by Dialysis Per Week

Change in total volume of fluid removed by dialysis per week from baseline to the end of the treatment was calculated using descriptive statistics. (NCT02331680)
Timeframe: Baseline，End of the treatment

InterventionmL (Mean)
OPC-41061 15mg/Day485.9
OPC-41061 30mg/Day375.4
Placebo1099.5

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Change From Baseline in Daily Urine Volume

Change in daily urine volume from baseline to the end of the treatment was calculated using descriptive statistics. (NCT02331680)
Timeframe: Baseline，End of the treatment

InterventionmL (Mean)
OPC-41061 15mg/Day169.2
OPC-41061 30mg/Day111.8
Placebo-259.9

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Number of Participants Requiring Prescription of Hypertonic Saline

Percentage of participants requiring prescription of hypertonic saline for the express purpose of treating hyponatremia during each period of the trial, assessed descriptively at each visit. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionparticipants (Number)
Tolvaptan2

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Percentage of Participants Requiring Prescription of Other Medicines

Percentage of participants requiring prescription of other medicines for the express purpose of treating hyponatremia during each period of the trial, assessed descriptively at each visit. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionpercentage of participants (Number)
Tolvaptan0

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Change From Baseline in Percentage of Participants With Mild Hyponatremia

"Percentage of participants with varying degrees of hyponatremia (severe <130, mild 130-135, normal >135 mEq/L) at Baseline and each study visit." (NCT02449044)
Timeframe: Baseline to Week 214

Interventionpercentage of participants (Number)
Day 1 post-dose (N=99)Day 31 (N=110)Week 10 (N=110)Week 18 (N=110)Week 26 (N=110)Week 34 (N=110)Week 42 (N=110)Week 50 (N=110)Week 58 (N=110)Week 70 (N=110)Week 82 (N=110)Week 94 (N=110)Week 106 (N=110)Week 118 (N=110)Week 130 (N=110)Week 142 (N=110)Week 154 (N=110)Week 166 (N=110)Week 178 (N=110)Week 190 (N=110)Week 202 (N=110)Week 214 (N=110)
Tolvaptan53.533.628.233.630.926.426.431.826.430.931.828.227.328.229.125.525.530.930.930.930.930.9

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Change From Baseline in Percentage of Participants With Normal Sodium Levels

"Percentage of participants with varying degrees of hyponatremia (severe <130, mild 130-135, normal >135 mEq/L) at Baseline and each study visit." (NCT02449044)
Timeframe: Baseline to Week 214

Interventionpercentage of participants (Number)
Day 1 post-dose (N=99)Day 31 (N=110)Week 10 (N=110)Week 18 (N=110)Week 26 (N=110)Week 34 (N=110)Week 42 (N=110)Week 50 (N=110)Week 58 (N=110)Week 70 (N=110)Week 82 (N=110)Week 94 (N=110)Week 106 (N=110)Week 118 (N=110)Week 130 (N=110)Week 142 (N=110)Week 154 (N=110)Week 166 (N=110)Week 178 (N=110)Week 190 (N=110)Week 202 (N=110)Week 214 (N=110)
Tolvaptan26.357.360.052.752.759.160.957.360.056.457.360.960.059.159.162.762.757.357.357.358.257.3

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Change From Baseline in Percentage of Participants With Severe Hyponatremia

"Percentage of participants with varying degrees of hyponatremia (severe <130, mild 130-135, normal >135 mEq/L) at Baseline and each study visit." (NCT02449044)
Timeframe: Baseline to Week 214

Interventionpercentage of participants (Number)
Day 1 post-dose (N=99)Day 31 (N=110)Week 10 (N=110)Week 18 (N=110)Week 26 (N=110)Week 34 (N=110)Week 42 (N=110)Week 50 (N=110)Week 58 (N=110)Week 70 (N=110)Week 82 (N=110)Week 94 (N=110)Week 106 (N=110)Week 118 (N=110)Week 130 (N=110)Week 142 (N=110)Week 154 (N=110)Week 166 (N=110)Week 178 (N=110)Week 190 (N=110)Week 202 (N=110)Week 214 (N=110)
Tolvaptan20.29.111.813.616.414.512.710.913.612.710.910.912.712.711.811.811.811.811.811.811.811.8

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Mean Change From Baseline in Serum Sodium Measurements

Sodium measurements obtained at designated intervals were compared to each participant's Baseline sodium level at the beginning of placebo-controlled therapy in their original trial and from Baseline on initiation of therapy in the open-label trial. (NCT02449044)
Timeframe: Baseline of parent trial to Week 214

InterventionmEq/L (Mean)
Day 1 post-dose (N= 99)Day 14 (N= 110)Day 31 (N= 110)Week 10 (N= 110)Week 18 (N= 110)Week 26 (N= 110)Week 34 (N= 110)Week 42 (N= 110)Week 50 (N= 110)Week 58 (N= 110)Week 70 (N= 110)Week 82 (N= 110)Week 94 (N= 110)Week 106 (N= 110)Week 118 (N= 110)Week 130 (N= 110)Week 142 (N= 110)Week 154 (N= 110)Week 166 (N= 110)Week 178 (N= 110)Week 190 (N= 110)Week 202 (N= 110)Week 214 (N= 110)
Tolvaptan2.25.25.05.04.64.24.75.25.05.04.84.85.15.04.84.95.25.24.94.85.15.05.0

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Mean Change From Baseline in SF-12 (Health Survey) Mental Component Summary (MCS)

The MCS assess the physical and mental dimensions of health-related quality of life. The MCS is equal to the sum of the items of concentration activities, calculating activities, language activities, and memory activities. The MCS is a computed score with weighted function based on the 12 questions from the 8 subscales (physical functioning, role-physical, bodily pain, general health, vitality, social functioning, role-emotional, mental health) of the SF-12v1 questionnaire per instructions by the scale's publisher. The scale ranges from 0 to 100 with 0 representing the lowest level of health and 100 indicating the highest level of health. (NCT02449044)
Timeframe: Baseline to Week 214

InterventionUnits on a scale (Mean)
Day 14 (N= 102)Day 31 (N= 106)Week 10 (N= 106)Week 18 (N= 106)Week 26 (N= 106)Week 34 (N= 106)Week 42 (N= 106)Week 50 (N= 106)Week 58 (N= 106)Week 70 (N= 106)Week 82 (N= 106)Week 94 (N= 106)Week 106 (N= 106)Week 142 (N= 2)Week 166 (N= 2)Week 178 (N= 2)Week 190 (N= 6)Week 202 (N= 1)Week 214 (N= 6)
Tolvaptan-1.0-1.0-0.4-2.0-1.1-2.7-2.1-1.9-2.5-2.6-2.5-2.6-3.7-11.25.00.4-2.8-0.8-0.5

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Mean Change From Baseline in SF-12 (Health Survey) Physical Component Summary (PCS)

The PCS assess the physical and mental dimensions of health-related quality of life. The PCS is equal to the sum of the items of endurance activities, strength activities, gross coordination activities, and fine coordination activities. The PCS is a computed score with weighted function based on the 12 questions from the 8 subscales (physical functioning, role-physical, bodily pain, general health, vitality, social functioning, role-emotional, mental health) of the SF-12v1 questionnaire per instructions by the scale's publisher. The scale ranges from 0 to 100 with 0 representing the lowest level of health and 100 indicating the highest level of health. (NCT02449044)
Timeframe: Baseline to Week 214

InterventionUnits on a scale (Mean)
Day 14 (N= 102)Day 31 (N= 106)Week 10 (N= 106)Week 18 (N= 106)Week 26 (N= 106)Week 34 (N= 106)Week 42 (N= 106)Week 50 (N= 106)Week 58 (N= 106)Week 70 (N= 106)Week 82 (N= 106)Week 94 (N= 106)Week 106 (N= 106)Week 142 (N= 2)Week 166 (N= 2)Week 178 (N= 2)Week 190 (N= 6)Week 202 (N= 1)Week 214 (N= 6)
Tolvaptan1.00.40.30.4-0.9-0.3-1.1-1.1-0.9-1.1-0.9-1.6-1.7-9.14.6-11.3-2.20.64.0

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Participants With Adverse Events (AEs)

A TEAE was an AE that began after the first injection or was continuous from Baseline and was defined as any new medical problem, or exacerbation of an existing problem, whether or not it was considered drug-related by the study physician. An AE was considered serious if it was fatal; life-threatening; persistently or significantly disabling or incapacitating; required in-subject hospitalization or prolonged hospitalization; a congenital anomaly/birth defect; or other medically significant event that, based upon appropriate medical judgment, may have jeopardized the participant and may have required medical or surgical intervention to prevent the outcomes mentioned above. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionparticipants (Number)
Participants with TEAEsParticipants with serious TEAEsParticipants with severe TEAEsParticipants discontinued IMP due to TEAEParticipants discontinued IMP due to TEAE/deathDeaths
Tolvaptan1057673192819

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Participants With Laboratory Values Abnormalities Reported as TEAEs

The laboratory values were one of the primary parameters to measure the safety and tolerability of individual participants. Incidence of TEAEs of potential clinical relevance include abnormal values in serum chemistry, hematology, urinalyses and prolactin tests that were identified based on pre-defined criteria. Any value outside the normal range was flagged for the attention of the study physician who was to indicate whether the value was clinically significant for identifying laboratory values of potential clinical relevance. Participants noted with abnormal laboratory values are reported below. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionparticipants (Number)
Serum Chemistry-Blood creatinine increasedSerum Chemistry-Blood potassium increasedSerum Chemistry-Blood glucose increasedSerum Chemistry-Blood potassium decreasedSerumChemistry-Aspartate aminotransferaseincreasedSerum Chemistry-Blood cholesterol increasedSerum Chemistry-Blood sodium increasedSerum Chemistry-Hepatic enzyme increasedSerum Chemistry-Oxygen saturation decreasedSerum Chemistry-HyperglycaemiaSerum Chemistry-HyperkalaemiaSerum Chemistry-HyperlipidaemiaSerum Chemistry-HypernatraemiaSerum Chemistry-HyperuricaemiaSerum Chemistry-HypoglycaemiaSerum Chemistry-HypokalaemiaSerum Chemistry-HypomagnesaemiaSerum Chemistry-HypoatraemiaHematology-AnemiaHematology-ThrombocytopeniaHematology-International normalized ratioincreasedHematology-White blood cell count increased
Tolvaptan4433232225744351432520242

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Participants With Body Weight Abnormalities Reported as TEAEs

The body weight evaluation was one of the primary parameters to measure the safety and tolerability of individual participants. Every effort was made to ensure that body weight measurements were performed in a reproducible and consistent manner. The pre-defined criteria was change of ≥7% in body weight for both male and female. Participants were to wear the same type of clothes at each measurement, preferably a gown and no shoes. All body weight measurements were to have been taken post-void. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionparticipants (Number)
Increased weightDecreased weight
Tolvaptan51

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Participants With Vital Signs Abnormalities Reported as Treatment Emergent Adverse Events (TEAEs)

The vital signs were one of the primary parameters to measure the safety and tolerability of individual participants. Incidence of TEAEs of potential clinical relevance included abnormal values in body temperature, heart rate, systolic and diastolic blood pressure, respiratory rate and weight that were identified based on pre-defined criteria. Criteria for identifying vital signs of potential clinical relevance included: Heart rate, supine: >= 120 beats per minute (bpm) + increase of ≥15 bpm from Baseline and <=50 bpm + decrease of >= 15 bpm; Diastolic Blood Pressure, Supine: >=105 mmHg + increase of >=15 mmHg and <=50 mmHg + decrease of >=15 mmHg; Systolic Blood Pressure, Supine: >=180 mmHg + increase of >=20 mmHg and <= 90 mmHg + decrease of >=20 mmHg; Temperature (degree C): Increase of >=1.1 to >=38.3C. The vital sign abnormalities were reported as TEAEs are mentioned below. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionparticipants (Number)
HypotensionHypertensionPyrexiaIncreased body temperaturePalpitationsIncreased central venous pressureIncreased venous pressureOrthostatic hypotensionHypertensive crisisDecreased orthostatic blood pressureIncreased weightDecreased weight
Tolvaptan1386322111151

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Percentage of Participants Requiring Prescription of Fluid Restriction

Percentage of participants requiring prescription of fluid restriction for the express purpose of treating hyponatremia during each period of the trial. Assessed descriptively at each visit. (NCT02449044)
Timeframe: Baseline to Post-Week 214 follow-up visit

Interventionpercentage of participants (Number)
Mild Hyponatremia (N=76)Severe Hyponatremia (N=35)
Tolvaptan14.475.71

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Mean Change From Baseline in Body Weight by Visit for Those Participants Who Had Clinical Evidence of Hypervolemia at Baseline

Body weight at each visit (assessed only for those with clinical evidence of hypervolemia at Baseline) and was summarized using descriptive statistics. (NCT02449044)
Timeframe: Baseline to Week 214

Interventionkg (Mean)
Day 31 (N= 26)Week 10 (N= 32)Week 18 (N= 27)Week 26 (N= 27)Week 34 (N= 26)Week 42 (N= 24)Week 50 (N= 22)Week 58 (N= 22)Week 70 (N= 18)Week 82 (N= 18)Week 94 (N= 18)Week 106 (N= 15)Week 118 (N= 13)Week 130 (N= 13)Week 142 (N= 12)Week 154 (N= 11)Week 166 (N= 9)Week 178 (N= 7)Week 190 (N= 5)Week 202 (N= 2)Week 214 (N= 2)
Tolvaptan-0.5-1.10.20.40.50.31.01.71.72.03.01.42.23.03.82.72.93.2-2.4-7.1-8.5

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Change in Loop Diuretic Score Defined Based on Change in Loop Diuretic Use

Change in loop diuretic score defined by change in loop diuretic use at Visit 2. The change in loop diuretic score endpoint was calculated as follows: patients having an increase in loop diuretic use at Visit 2 were given a score of 2, patients with no change a score of 0, and patients with a decrease in loop use at Visit 2 were given a score of -1. Increases in loop diuretic use were given a higher weighting to account for their reflection of treatment failure. (NCT02476409)
Timeframe: Day 3 (48 hours)

Interventionunits on a scale (Mean)
Tolvaptan-0.47
Placebo0

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Number of Participants With a Decrease in Loop Diuretic Dosing at 48 Hours

Number of participants with a decrease in loop diuretic diuretic dosing at 48 hours in the Tolvaptan group and the Placebo group. (NCT02476409)
Timeframe: Day 3 (48 hours)

InterventionParticipants (Count of Participants)
Tolvaptan9
Placebo4

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Change in Body Weight at 48 Hours

The primary endpoint for the study will be change in body weight between patients randomized to tolvaptan versus placebo from baseline to 48 hours (NCT02476409)
Timeframe: Baseline, Day 3 (48 hours)

Interventionpounds (Mean)
Tolvaptan-3.3
Placebo-0.8

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Change in Body Weight at 48 Hours Stratified by Copeptin

The primary endpoint for the study will be change in body weight between patients randomized to tolvaptan versus placebo from baseline to 48 hours with stratification for baseline copeptin level (NCT02476409)
Timeframe: Baseline, Day 3 (48 hours)

Interventionpounds (Mean)
High Copeptin - Tolvaptan-2.9
High Copeptin - Placebo0.3
Low Copeptin - Tolvaptan-3.8
Low Copeptin - Placebo-2.4

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Change in Body Weight at Day 8

Change in body weight at 8 days will be analyzed in a similar fashion to the change in body weight at 48 hours (NCT02476409)
Timeframe: Baseline, 8 days

Interventionpounds (Mean)
Tolvaptan-1.8
Placebo-2.8

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Changes in Visual Analog Scale - Patient Dyspnea

"Changes in patient reported dyspnea scale from baseline to 48 hours based on the visual analog scale.~Visual Analog Scale (VAS) - Patient Dyspnea has a minimum value of 0 and a maximum value of 100. Higher scores mean a better outcome." (NCT02476409)
Timeframe: Baseline, Day 3 (48 hours)

Interventionscore on a scale (Mean)
Tolvaptan21
Placebo15

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Change in Loop Diuretic Dose (Furosemide Milligram Equivalents) at 48 Hours

Change in loop diuretic dose at 48 hours where doses of loop diuretic are expressed as furosemide milligram equivalents based on standard conversions of bumetanide and torsemide doses to milligram equivalents of furosemide. The formula for the conversion of doses of loop diuretics were standardized to milligram equivalents of furosemide based on 40 milligrams of furosemide for each 1 milligram of bumetanide and 2 milligrams of furosemide for each 1 milligram of torsemide. (NCT02476409)
Timeframe: Day 3 (48 hours)

Interventionfurosemide milligram equivalents (Mean)
Tolvaptan-57
Placebo-11

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Urinary Cystine Supersaturation (mg/L) at High Dose (Day7-8)

"The primary outcome was urinary cystine supersaturation as measured by cystine capacity. This proprietary test (Litholink Corp., Chicago IL) is reported as a value in mg/L above or below zero, with positive values indicating urine undersaturated with cystine, while negative values indicate that the urine is supersaturated with cystine. Four 24-hour urine samples were obtained during the study: one at baseline 3-6 days prior to the measurement, one on day 3-4 of the dosing period, one on day 7-8 of the dosing period, and one 3-6 days after the washout period. Each 24 hour urine sample was sent individually for analysis by Litholink Corp, which performs the cystine assays." (NCT02538016)
Timeframe: 23 days

Interventionmg/L (Mean)
Tolvaptan70

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Urine Osmolality at High Dose (Day 8)

Secondary outcomes included serum sodium and other electrolyte levels. Serum electrolytes for each subject before, during, and after tolvaptan treatment (Sodium/Potassium/Chloride in mmol/L). (NCT02538016)
Timeframe: 11 days

Interventionmmol/L (Mean)
SodiumPotassiumChloride
Tolvaptan1414.05102

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Number of Patients With Escalation of Loop Diuretic Therapy

Provider escalation of loop diuretic dosage at 24 hours for urine output less than 3 L at 24 hours (NCT02606253)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Metolazone4
Chlorothiazide4
Tolvaptan2

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Change in eGFR From Baseline to 48 Hours

Change in estimated glomerular filtration rate (ml/min/m2) from baseline to 48 hours (NCT02606253)
Timeframe: 48 hours

Interventionml/min/m2 (Mean)
Metolazone-6
Chlorothiazide-9
Tolvaptan2

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Number of Patients With In-hospital Mortality

Incidence of death from study enrollment to hospital discharge, an average of 5 days (NCT02606253)
Timeframe: Enrollment to hospital discharge an average of 5 days

InterventionParticipants (Count of Participants)
Metolazone0
Chlorothiazide0
Tolvaptan0

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Number of Patients With New Inotrope Utilization

Incidence of new initiation of dopamine, dobutamine, or milrinone from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

InterventionParticipants (Count of Participants)
Metolazone1
Chlorothiazide0
Tolvaptan2

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Number of Patients With Renal Replacement Therapy Utilization

Incidence of Renal replacement therapy utilization (hemodialysis, ultrafiltration) from enrollment to hospital discharge, an average of 5 days (NCT02606253)
Timeframe: enrollment to hospital discharge an average of 5 days

InterventionParticipants (Count of Participants)
Metolazone0
Chlorothiazide0
Tolvaptan0

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Number of Patients With Symptomatic Hypotension

SBP < 85 mmHg plus medical intervention for symptomatic hypotension (NCT02606253)
Timeframe: 48 hours

InterventionParticipants (Count of Participants)
Metolazone2
Chlorothiazide0
Tolvaptan2

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Potassium Supplementation

Cumulative dose of potassium supplementation (mEq) administered from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

InterventionmEq (Mean)
Metolazone103
Chlorothiazide63
Tolvaptan58

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Weight Change Over 48 Hours

The primary outcome will be 48-hour standing scale weight change (kg) from enrollment among the metolazone, intravenous chlorothiazide, and tolvaptan arms, using metolazone group as the comparator group for all other groups. (NCT02606253)
Timeframe: 48 hours

Interventionkg (Mean)
Metolazone-4.6
Chlorothiazide-5.8
Tolvaptan-4.1

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Change in Patient Congestion Score

"Participants will score their congestion on a 10cm scale ranging from Best (10cm) to Worst (0cm). Change in score (units in centimeters) from baseline to 48 hours." (NCT02606253)
Timeframe: 48 hours

Interventioncm of dyspena analog scale (Median)
Metolazone4.0
Chlorothiazide3.0
Tolvaptan3.0

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Change in Serum Chloride From Baseline

Change in serum chloride (mEq/L) from baseline to 48 hrs (NCT02606253)
Timeframe: 48 hours

InterventionmEq/L (Mean)
Metolazone-7
Chlorothiazide-7
Tolvaptan2

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Diuretic Efficiency

Diuretic Efficiency is calculated as 48hr urine output/ 48hr Furosemide equivalents in milligrams (NCT02606253)
Timeframe: 48 hours

InterventionUOP / 40mg IV furosemide (Mean)
Metolazone217
Chlorothiazide294
Tolvaptan326

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Mean Change in Glomerular Filtration Rate at Discharge

Mean change in glomerular filtration rate from enrollment to end of study at hospital discharge, an average of 5 days (NCT02606253)
Timeframe: hospital discharge an average of 5 days

Interventionml/min/m2 (Mean)
Metolazone-2
Chlorothiazide-2
Tolvaptan-6

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Mean Change in Serum Creatinine

Mean change in serum creatinine (mg/dl) from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

Interventionmg/dl (Mean)
Metolazone0.3
Chlorothiazide0.5
Tolvaptan0.03

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Mean Change in Serum Potassium

Mean change in serum potassium (mEq/L) from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

InterventionmEq/L (Mean)
Metolazone-0.1
Chlorothiazide-0.2
Tolvaptan0.1

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Mean Change in Serum Sodium

Mean change in serum sodium (mEq/L) from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

InterventionmEq/L (Mean)
Metolazone-1
Chlorothiazide-1
Tolvaptan4

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Net Urine Output

Net urine output from enrollment to the end of study at 48 hours measured in liters (NCT02606253)
Timeframe: 48 hours

Interventionliters (Median)
Metolazone-7.8
Chlorothiazide-8.8
Tolvaptan-9.8

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Number of Patients With Cardiac Arrhythmias

Incidence of new atrial or ventricular arrhythmias from enrollment to end of study at 48 hours (NCT02606253)
Timeframe: 48 hours

InterventionParticipants (Count of Participants)
Metolazone0
Chlorothiazide0
Tolvaptan0

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Number of Patients With Hypokalemia

Incidence of hypokalemia (serum potassium less than 3.5mEq/L ) from enrollment to end of study (NCT02606253)
Timeframe: 48 hours

InterventionParticipants (Count of Participants)
Metolazone3
Chlorothiazide2
Tolvaptan2

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Phase A: 24-hour Sodium Clearance

Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

Interventionmilliliter per minute (mL/min) (Mean)
Total Daily Dose: 37.5 mgTotal Daily Dose: 45 mgTotal Daily Dose: 60 mg
Phase A: Tolvaptan0.80.70.9

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Phase A: 24-hour Creatinine Clearance

Creatinine is produced from the metabolism of protein, when muscles burn energy. Most creatinine is filtered out of the blood by the kidneys and excreted in urine. The creatinine clearance value is determined by measuring the concentration of endogenous creatinine (that which is produced by the body) in both plasma and urine. Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

InterventionmL/min (Mean)
Total Daily Dose: 22.5 mgTotal Daily Dose: 37.5 mgTotal Daily Dose: 45 mgTotal Daily Dose: 60 mg
Phase A: Tolvaptan124.6148.595.0123.7

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Phase A: 24-hour Free Water Clearance

Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

InterventionmL/min (Mean)
Total Daily Dose: Placebo
Phase A: Placebo0.1

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Phase A: 24-hour Free Water Clearance

Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

InterventionmL/min (Mean)
Total Daily Dose: 37.5 mgTotal Daily Dose: 45 mgTotal Daily Dose: 60 mg
Phase A: Tolvaptan2.32.63.0

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Phase A: 24-hour Sodium Clearance

Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

Interventionmilliliter per minute (mL/min) (Mean)
Total Daily Dose: Placebo
Phase A: Placebo0.7

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Phase B: Percentage of Each Tanner Stage by Gender and Age Compared to Normative Populations

Tanner stages is a scale that defines physical measurements of development based on external primary and secondary sex characteristics. It was used in this study to assess pubertal development with values ranging from Stage 1 (pre-pubertal characteristics) to Stage 5 (adult or mature characteristics). Only those categories with at least one participant with event are reported. (NCT02964273)
Timeframe: At Baseline, Months 6, 12, 18, and 24 of Phase B

,
Interventionpercentage of participants (Number)
Female (>=4 to <12 Years): Phase B Baseline- Stage 1Female (>=4 to <12 Years): Phase B Baseline- Stage 2Female (>=4 to <12 Years): Phase B Baseline- Stage 4Female (>=4 to <12 Years): Month 6, Phase B- Stage 1Female (>=4 to <12 Years): Month 6, Phase B- Stage 2Female (>=4 to <12 Years): Month 6, Phase B- Stage 4Female (>=4 to <12 Years): Month 12, Phase B- Stage 1Female (>=4 to <12 Years): Month 12, Phase B- Stage 2Female (>=4 to <12 Years): Month 12, Phase B- Stage 3Female (>=4 to <12 Years): Month 12, Phase B- Stage 4Female (>=4 to <12 Years): Month 18, Phase B- Stage 1Female (>=4 to <12 Years): Month 18, Phase B- Stage 2Female (>=4 to <12 Years): Month 18, Phase B- Stage 4Female (>=4 to <12 Years): Month 24, Phase B- Stage 1Female (>=4 to <12 Years): Month 24, Phase B- Stage 2Female (>=4 to <12 Years): Month 24, Phase B- Stage 3Female (>=4 to <12 Years): Month 24, Phase B- Stage 4Male (>=4 to <12 Years): Phase B Baseline- Stage 1Male (>=4 to <12 Years): Phase B Baseline- Stage 2Male (>=4 to <12 Years): Phase B Baseline- Stage 3Male (>=4 to <12 Years): Phase B Baseline- Stage 4Male (>=4 to <12 Years): Month 6, Phase B- Stage 1Male (>=4 to <12 Years): Month 6, Phase B- Stage 2Male (>=4 to <12 Years): Month 6, Phase B- Stage 3Male (>=4 to <12 Years): Month 6, Phase B- Stage 4Male (>=4 to <12 Years): Month 12, Phase B- Stage 1Male (>=4 to <12 Years): Month 12, Phase B- Stage 2Male (>=4 to <12 Years): Month 12, Phase B- Stage 3Male (>=4 to <12 Years): Month 12, Phase B- Stage 4Male (>=4 to <12 Years): Month 18, Phase B- Stage 1Male (>=4 to <12 Years): Month 18, Phase B- Stage 2Male (>=4 to <12 Years): Month 18, Phase B- Stage 3Male (>=4 to <12 Years): Month 18, Phase B- Stage 4Male (>=4 to <12 Years): Month 18, Phase B- Stage 5Male (>=4 to <12 Years): Month 24, Phase B- Stage 1Male (>=4 to <12 Years): Month 24, Phase B- Stage 2Male (>=4 to <12 Years): Month 24, Phase B- Stage 3Male (>=4 to <12 Years): Month 24, Phase B- Stage 4Male (>=4 to <12 Years): Month 24, Phase B- Stage 5Female (>=12 to <15 Years): Phase B Baseline- Stage 2Female (>=12 to <15 Years): Phase B Baseline- Stage 3Female (>=12 to <15 Years): Phase B Baseline- Stage 4Female (>=12 to <15 Years): Phase B Baseline- Stage 5Female (>=12 to <15 Years): Month 6, Phase B- Stage 3Female (>=12 to <15 Years): Month 6, Phase B- Stage 4Female (>=12 to <15 Years): Month 6, Phase B-Stage 5Female (>=12 to <15 Years): Month 12, Phase B- Stage 4Female (>=12 to <15 Years): Month 12, Phase B- Stage 5Female (>=12 to <15 Years): Month 18, Phase B- Stage 4Female (>=12 to <15 Years): Month 18, Phase B- Stage 5Female (>=12 to <15 Years): Month 24, Phase B- Stage 4Female (>=12 to <15 Years): Month 24, Phase B- Stage 5Female (>=12 to <15 Years): End of Treatment, Phase B- Stage 4Female (>=12 to <15 Years): End of Treatment, Phase B- Stage 5Male (>=12 to <15 Years): Phase B Baseline- Stage 2Male (>=12 to <15 Years): Phase B Baseline- Stage 3Male (>=12 to <15 Years): Phase B Baseline- Stage 4Male (>=12 to <15 Years): Phase B Baseline- Stage 5Male (>=12 to <15 Years): Month 6, Phase B- Stage 2Male (>=12 to <15 Years): Month 6, Phase B- Stage 3Male (>=12 to <15 Years): Month 6, Phase B- Stage 4Male (>=12 to <15 Years): Month 6, Phase B- Stage 5Male (>=12 to <15 Years): Month 12, Phase B- Stage 2Male (>=12 to <15 Years): Month 12, Phase B- Stage 4Male (>=12 to <15 Years): Month 12, Phase B- Stage 5Male (>=12 to <15 Years): Month 18, Phase B- Stage 2Male (>=12 to <15 Years): Month 18, Phase B- Stage 4Male (>=12 to <15 Years): Month 18, Phase B- Stage 5Male (>=12 to <15 Years): Month 24, Phase B- Stage 2Male (>=12 to <15 Years): Month 24, Phase B- Stage 4Male (>=12 to <15 Years): Month 24, Phase B- Stage 5Male (>=12 to <15 Years): End of Treatment, Phase B- Stage 5Female (>=15 to <18 Years): Phase B Baseline- Stage 4Female (>=15 to <18 Years): Phase B Baseline- Stage 5Female (>=15 to <18 Years): Month 6, Phase B- Stage 4Female (>=15 to <18 Years): Month 6, Phase B- Stage 5Female (>=15 to <18 Years): Month 12, Phase B- Stage 4Female (>=15 to <18 Years): Month 12, Phase B- Stage 5Female (>=15 to <18 Years): Month 18, Phase B- Stage 4Female (>=15 to <18 Years): Month 18, Phase B- Stage 5Female (>=15 to <18 Years): Month 24, Phase B- Stage 4Female (>=15 to <18 Years): Month 24, Phase B- Stage 5Female (>=15 to <18 Years): End of Treatment, Phase B- Stage 5Male (>=15 to <18 Years): Phase B Baseline- Stage 4Male (>=15 to <18 Years): Phase B Baseline- Stage 5Male (>=15 to <18 Years): Month 6, Phase B- Stage 5Male (>=15 to <18 Years): Month 12, Phase B- Stage 5Male (>=15 to <18 Years): Month 18, Phase B- Stage 5Male (>=15 to <18 Years): Month 24, Phase B- Stage 5Male (>=15 to <18 Years): End of Treatment, Phase B- Stage 5
Phase B: Prior Placebo10.32.62.67.72.62.67.72.62.62.62.67.72.62.65.12.62.65.12.65.10.02.62.62.62.62.60.05.12.62.60.05.10.02.60.00.05.10.02.62.62.65.110.35.15.110.35.110.32.610.35.110.32.62.62.60.07.72.62.60.05.12.62.65.15.12.60.07.72.60.010.32.60.015.40.012.80.012.80.012.80.012.85.10.020.517.917.915.412.87.7
Phase B: Prior Tolvaptan7.10.00.04.80.00.04.80.00.00.04.80.00.02.42.40.00.011.94.80.02.49.52.42.42.49.52.42.42.44.82.40.04.80.04.84.82.42.42.40.00.00.016.70.00.016.70.014.30.011.90.09.50.07.10.02.49.54.80.02.44.84.80.07.17.10.04.89.50.04.89.50.02.416.72.416.72.416.72.416.72.416.70.02.416.719.016.716.716.74.8

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Phase B: Percent Change From Phase B Baseline in htTKV as Measured by MRI at Month 12 and Month 24

htTKV is used in participants with autosomal dominant polycystic kidney disease to predict the onset of renal insufficiency. (NCT02964273)
Timeframe: Phase B Baseline, Months 12 and 24

,
Interventionpercent change (Mean)
Percent Change From Phase B Baseline at Month 12, Phase BPercent Change From Phase B Baseline at Month 24 Phase B
Phase B: Prior Placebo3.097.35
Phase B: Prior Tolvaptan7.6813.55

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Phase B: Change From Phase B Baseline in Renal Function (eGFR by Schwartz Formula) at Each Clinic Visit in Phase B

Renal function was assessed by estimated eGFR calculated by the Schwartz formula (eGFR = 0.413 × height [cm] /serum creatinine mg/dL), expressed as mean change in eGFR at the specified time points. (NCT02964273)
Timeframe: Phase B Baseline, Week 1, Months 1, 6, 12, 18, and 24

,
InterventionmL/min/1.73 m^2 (Mean)
Phase B BaselineChange From Phase B Baseline at Week 1, Phase BChange From Phase B Baseline at Month 1, Phase BChange From Phase B Baseline at Month 6, Phase BChange From Phase B Baseline at Month 12, Phase BChange From Phase B Baseline at Month 18, Phase BChange From Phase B Baseline at Month 24, Phase B
Phase B: Prior Placebo98.5-6.7-4.8-6.4-7.2-9.0-10.3
Phase B: Prior Tolvaptan97.0-1.7-0.9-4.2-5.6-3.5-5.2

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Phase B: Change From Baseline in Growth Percentile by Gender and Age

The growth percentile was based on the assessment of height and weight. (NCT02964273)
Timeframe: At Baseline, Months 6, 12, 18, and 24 of Phase B

,
Interventiongrowth percentile (Mean)
Female Participants with Age >=15 to <18 Years - Phase B BaselineChange From Baseline Female Participants with Age >=15 to <18 Years - Month 6, Phase BChange From Baseline Female Participants with Age >=15 to <18 Years - Month 12, Phase BChange From Baseline Female Participants with Age >=15 to <18 Years - Month 18, Phase BChange From Baseline Female Participants with Age >=15 to <18 Years - Month 24, Phase BMale Participants with Age >=15 to <18 Years - Phase B BaselineChange From Baseline Male Participants with Age >=15 to <18 Years - Month 6, Phase BChange From Baseline Male Participants with Age >=15 to <18 Years - Month 12, Phase BChange From Baseline Male Participants with Age >=15 to <18 Years - Month 18, Phase BChange From Baseline Male Participants with Age >=15 to <18 Years - Month 24, Phase BFemale Participants with Age >=12 to <15 Years - Phase B BaselineChange From Baseline Female Participants with Age >=12 to <15 Years - Month 6, Phase BChange From Baseline Female Participants with Age >=12 to <15 Years - Month 12, Phase BChange From Baseline Female Participants with Age >=12 to <15 Years - Month 18, Phase BChange From Baseline Female Participants with Age >=12 to <15 Years - Month 24, Phase BMale Participants with Age >=12 to <15 Years - Phase B BaselineChange From Baseline Male Participants with Age >=12 to <15 Years - Month 6, Phase BChange From Baseline Male Participants with Age >=12 to <15 Years - Month 12, Phase BChange From Baseline Male Participants with Age >=12 to <15 Years - Month 18, Phase BChange From Baseline Male Participants with Age >=12 to <15 Years - Month 24, Phase BFemale Participants with Age 4 to <=11 Years - Phase B BaselineChange From Baseline Female Participants with Age 4 to <=11 Years - Month 6, Phase BChange From Baseline Female Participants with Age 4 to <=11 Years - Month 12, Phase BChange From Baseline Female Participants with Age 4 to <=11 Years - Month 18, Phase BChange From Baseline Female Participants with Age 4 to <=11 Years - Month 24, Phase BMale Participants with Age 4 to <=11 Years - Phase B BaselineChange From Baseline Male Participants with Age 4 to <=11 Years - Month 6, Phase BChange From Baseline Male Participants with Age 4 to <=11 Years - Month 12, Phase BChange From Baseline Male Participants with Age 4 to <=11 Years - Month 18, Phase BChange From Baseline Male Participants with Age 4 to <=11 Years - Month 24, Phase B
Phase B: Prior Placebo46122010166918-4-11541312101377-15-23-22-1859212106414221
Phase B: Prior Tolvaptan69-70-2660-13-816-262312516714-4-878-25-5-46503-40

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Phase B: Change From Baseline in Creatinine Value

Phase B Baseline is the last evaluation prior to the first dose in Phase B. The Last Visit is the last available post-baseline evaluation including early term. As prespecified in the protocol, data for safety is reported by the treatment group (Phase B: Prior Tolvaptan and Phase B: Prior Placebo). (NCT02964273)
Timeframe: Baseline, Week 1, Months 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, Follow Up Day 7, End of Treatment, and Last Visit

,
Interventionmg/dL (Mean)
BaselineChange From Baseline at Week 1Change From Baseline at Month 1Change From Baseline at Month 2Change From Baseline at Month 3Change From Baseline at Month 4Change From Baseline at Month 5Change From Baseline at Month 6Change From Baseline at Month 7Change From Baseline at Month 8Change From Baseline at Month 9Change From Baseline at Month 10Change From Baseline at Month 11Change From Baseline at Month 12Change From Baseline at Month 13Change From Baseline at Month 14Change From Baseline at Month 15Change From Baseline at Month 16Change From Baseline at Month 17Change From Baseline at Month 18Change From Baseline at Month 19Change From Baseline at Month 20Change From Baseline at Month 21Change From Baseline at Month 22Change From Baseline at Month 23Change From Baseline at Month 24Change From Baseline at Follow Up Day 7Change From Baseline at End of TreatmentChange From Baseline at Last Visit
Phase B: Prior Placebo0.690.040.040.040.040.050.070.060.060.070.090.060.080.070.080.080.060.080.080.090.090.110.090.090.120.120.140.020.10
Phase B: Prior Tolvaptan0.730.010.010.020.020.040.030.030.040.050.070.060.050.060.040.080.060.050.070.050.060.040.090.060.070.07-0.01-0.010.05

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Phase A: Percentage of Each Tanner Stage by Gender and Age Compared to Normative Populations

Tanner stages is a scale that defines physical measurements of development based on external primary and secondary sex characteristics. It was used in this study to assess pubertal development with values ranging from Stage 1 (pre-pubertal characteristics) to Stage 5 (adult or mature characteristics). Only those categories with at least one participant with event are reported. (NCT02964273)
Timeframe: At Baseline, Months 6 and 12 of Phase A

,
Interventionpercentage of participants (Number)
Female (>=4 to <12 Years): Baseline- Stage 1Female (>=4 to <12 Years): Baseline- Stage 3Female (>=4 to <12 Years): Month 6, Phase A- Stage 1Female (>=4 to <12 Years): Month 6, Phase A- Stage 2Female (>=4 to <12 Years): Month 6, Phase A- Stage 4Female (>=4 to <12 Years): Month 12, Phase A- Stage 1Female (>=4 to <12 Years): Month 12, Phase A- Stage 2Female (>=4 to <12 Years): Month 12, Phase A- Stage 4Male (>=4 to <12 Years): Baseline- Stage 1Male (>=4 to <12 Years): Baseline- Stage 2Male (>=4 to <12 Years): Baseline- Stage 3Male (>=4 to <12 Years): Month 6, Phase A- Stage 1Male (>=4 to <12 Years): Month 6, Phase A- Stage 2Male (>=4 to <12 Years): Month 6, Phase A- Stage 3Male (>=4 to <12 Years): Month 12, Phase A- Stage 1Male (>=4 to <12 Years): Month 12, Phase A- Stage 2Male (>=4 to <12 Years): Month 12, Phase A- Stage 3Male (>=4 to <12 Years): Month 12, Phase A- Stage 4Female (>=12 to <15 Years): Baseline- Stage 1Female (>=12 to <15 Years): Baseline- Stage 2Female (>=12 to <15 Years): Baseline- Stage 3Female (>=12 to <15 Years): Baseline- Stage 4Female (>=12 to <15 Years): Baseline- Stage 5Female (>=12 to <15 Years): Month 6, Phase A- Stage 2Female (>=12 to <15 Years): Month 6, Phase A- Stage 3Female (>=12 to <15 Years): Month 6, Phase A- Stage 4Female (>=12 to <15 Years): Month 6, Phase A- Stage 5Female (>=12 to <15 Years): Month 12, Phase A- Stage 2Female (>=12 to <15 Years): Month 12, Phase A- Stage 3Female (>=12 to <15 Years): Month 12, Phase A- Stage 4Female (>=12 to <15 Years): Month 12, Phase A- Stage 5Male (>=12 to <15 Years): Baseline- Stage 2Male (>=12 to <15 Years): Baseline- Stage 3Male (>=12 to <15 Years): Baseline- Stage 4Male (>=12 to <15 Years): Baseline- Stage 5Male (>=12 to <15 Years): Month 6, Phase A- Stage 2Male (>=12 to <15 Years): Month 6, Phase A- Stage 3Male (>=12 to <15 Years): Month 6, Phase A- Stage 4Male (>=12 to <15 Years): Month 6, Phase A- Stage 5Male (>=12 to <15 Years): Month 12, Phase A- Stage 2Male (>=12 to <15 Years): Month 12, Phase A- Stage 3Male (>=12 to <15 Years): Month 12, Phase A- Stage 4Male (>=12 to <15 Years): Month 12, Phase A- Stage 5Male (>=12 to <15 Years): End of Treatment- Stage 5Female (>=15 to <18 Years): Baseline- Stage 4Female (>=15 to <18 Years): Baseline- Stage 5Female (>=15 to <18 Years): Month 6, Phase A- Stage 4Female (>=15 to <18 Years): Month 6, Phase A- Stage 5Female (>=15 to <18 Years): Month 12, Phase A- Stage 4Female (>=15 to <18 Years): Month 12, Phase A- Stage 5Female (>=15 to <18 Years): End of Treatment- Stage 5Male (>=15 to <18 Years): Baseline- Stage 4Male (>=15 to <18 Years): Baseline- Stage 5Male (>=15 to <18 Years): Month 6, Phase A- Stage 4Male (>=15 to <18 Years): Month 6, Phase A- Stage 5Male (>=15 to <18 Years): Month 12, Phase A- Stage 4Male (>=15 to <18 Years): Month 12, Phase A- Stage 5Male (>=15 to <18 Years): End of Treatment- Stage 5
Phase A: Placebo11.62.39.32.32.37.02.32.34.74.70.07.00.04.74.72.34.70.00.04.72.30.07.02.32.30.07.02.32.34.79.34.74.74.72.32.32.34.72.32.30.07.02.32.30.018.60.016.30.016.32.34.714.02.316.30.018.60.0
Phase A: Tolvaptan6.30.06.30.00.04.20.00.016.70.02.116.72.12.114.64.20.02.12.10.02.14.210.40.00.02.112.50.00.00.014.66.34.22.12.14.24.24.22.10.02.18.34.22.12.112.52.112.52.114.60.02.116.72.114.62.114.62.1

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Phase A: Change From Baseline in Spot Urine Osmolality (Pre-morning Dose)

Urine osmolality is a measure of urine concentration, measured by osmometer, which evaluates the freezing point depression of a solution and supplies results as milliosmoles per kilogram of water. Spot urine osmolality was determined for urine samples collected immediately prior to morning dosing for Day 1 (Baseline), and Week 1 for all participants. Sample was taken after the first morning's void and was provided as a mid-stream, clean catch sample. All participants were fasting. (NCT02964273)
Timeframe: Baseline, and Week 1 of Phase A

,
Interventionmilliosmoles per kilogram (mOsm/kg) (Mean)
BaselineChange From Baseline at Week 1, Phase A
Phase A: Placebo646-93
Phase A: Tolvaptan635-386

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Phase A: Change From Baseline in Specific Gravity (Pre-morning Dose)

Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. Spot urine sample for determination of specific gravity was collected immediately prior to morning dosing for Day 1 (Baseline), and Week 1 for all participants. Sample was taken after the first morning's void and was provided as a mid-stream, clean catch sample. All participants were fasting. (NCT02964273)
Timeframe: Baseline, and Week 1 of Phase A

,
Interventionratio (Mean)
BaselineChange From Baseline at Week 1, Phase A
Phase A: Placebo1.017-0.002
Phase A: Tolvaptan1.017-0.009

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Phase A: Change From Baseline in Renal Function (Estimated Glomerular Filtration Rate [eGFR] by Schwartz Formula) at Each Clinic Visit in Phase A

Renal function was assessed by estimated eGFR calculated by the Schwartz formula (eGFR = 0.413 × height [cm] /serum creatinine mg/dL), expressed as mean change in eGFR at the specified time points. The units for the data reported are milliliter per minute per 1.73 meter square (mL/min/1.73 m^2). The baseline was the evaluation done at Week 1 in Phase A for this outcome measure. (NCT02964273)
Timeframe: Phase A Baseline, Months 1, 6, and 12

,
InterventionmL/min/1.73 m^2 (Mean)
BaselineChange From Baseline at Month 1, Phase AChange From Baseline at Month 6, Phase AChange From Baseline at Month 12, Phase A
Phase A: Placebo102.1-1.9-2.5-3.2
Phase A: Tolvaptan93.92.84.62.6

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Phase A and B: Mean 24-hour Fluid Balance Prior to Week 1

Participants were instructed to record all fluid taken and all urine output for the 24-hour period. (NCT02964273)
Timeframe: Prior to Week 1 in Phase A and B

Interventionmilliliter (Mean)
Phase A: Tolvaptan31
Phase A: Placebo241
Phase B: Prior Tolvaptan138
Phase B: Prior Placebo207

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Phase A: Change From Baseline in Growth Percentile by Gender and Age

The growth percentile was based on the assessment of height and weight. (NCT02964273)
Timeframe: At Baseline, Months 6 and 12 of Phase A

,
Interventiongrowth percentile (Mean)
Female Participants with Age >=15 to <18 Years - Baseline, Phase AChange From Baseline in Female Participants with Age >=15 to <18 Years - Month 6, Phase AChange From Baseline in Female Participants with Age >=15 to <18 Years - Month 12, Phase AMale Participants with Age >=15 to <18 Years - Baseline, Phase AChange From Baseline in Male Participants with Age >=15 to <18 Years - Month 6, Phase AChange From Baseline in Male Participants with Age >=15 to <18 Years - Month 12, Phase AFemale Participants with Age >=12 to <15 Years - Baseline, Phase AChange From Baseline in Female Participants with Age >=12 to <15 Years - Month 6, Phase AChange From Baseline in Female Participants with Age >=12 to <15 Years - Month 12, Phase AMale Participants with Age >=12 to <15 Years - Baseline, Phase AChange From Baseline in Male Participants with Age >=12 to <15 Years - Month 6, Phase AChange From Baseline in Male Participants with Age >=12 to <15 Years - Month 12, Phase AFemale Participants with Age 4 to <=11 Years - Baseline, Phase AChange From Baseline in Female Participants with Age 4 to <=11 Years - Month 6, Phase AChange From Baseline in Female Participants with Age 4 to <=11 Years - Month 12, Phase AMale Participants with Age 4 to <=11 Years - Baseline, Phase AChange From Baseline in Male Participants with Age 4 to <=11 Years - Month 6, Phase AChange From Baseline in Male Participants with Age 4 to <=11 Years - Month 12, Phase A
Phase A: Placebo60-2-573-1-372-20-1876-13857426301
Phase A: Tolvaptan62275612271-2-1170-7071-175741

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Phase A: Change From Baseline in Creatinine Value

Phase A Baseline is the last pre-dose evaluation. The Last Visit is the last available post-baseline evaluation including early term. As prespecified in the protocol, data for safety is reported by the treatment group (Phase A: Tolvaptan and Phase A: Placebo) (NCT02964273)
Timeframe: Baseline, Week 1, Months 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, Follow Up Day 7, End of Treatment, and Last Visit

,
Interventionmilligrams per deciliter (mg/dL) (Mean)
BaselineChange From Baseline at Week 1Change From Baseline at Month 1Change From Baseline at Month 2Change From Baseline at Month 3Change From Baseline at Month 4Change From Baseline at Month 5Change From Baseline at Month 6Change From Baseline at Month 7Change From Baseline at Month 8Change From Baseline at Month 9Change From Baseline at Month 10Change From Baseline at Month 11Change From Baseline at Month 12Change From Baseline at Follow Up Day 7Change From Baseline at End of TreatmentChange From Baseline at Last Visit
Phase A: Placebo0.67-0.010.010.000.01-0.010.010.020.020.020.010.030.040.02-0.020.030.02
Phase A: Tolvaptan0.700.040.010.010.000.000.010.010.010.010.040.010.020.020.090.030.03

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Phase A: 24-hour Creatinine Clearance

Creatinine is produced from the metabolism of protein, when muscles burn energy. Most creatinine is filtered out of the blood by the kidneys and excreted in urine. The creatinine clearance value is determined by measuring the concentration of endogenous creatinine (that which is produced by the body) in both plasma and urine. Data was categorized and reported based on the total daily dose for the given time point of 0-24 hours. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

InterventionmL/min (Mean)
Total Daily Dose: Placebo
Phase A: Placebo105.1

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Phase A and B: Percentage of Participants With Potentially Clinically Significant Abnormalities in Vital Signs

Vital sign measurements included measurements of respiratory rate, blood pressure, body temperature and pulse. Any value outside the normal range was flagged for the attention of the investigator who assessed whether or not a flagged value is of clinical significance. Only those categories with at least one participant with event are reported. As prespecified in the protocol, data for safety is reported by the treatment group (Phase A: Tolvaptan, Phase A: Placebo, Phase B: Prior Tolvaptan and Phase B: Prior Placebo). (NCT02964273)
Timeframe: From first dose of study drug up to 14 days post last dose (up to approximately 37 months)

,,,
Interventionpercentage of participants (Number)
Pulse Rate (Beats per Minute [BPM]) <=50 and Decrease from Baseline >=15Systolic Blood Pressure (millimetre of mercury [mmHg]) >=130 and Increase from Baseline >=20Systolic Blood Pressure (mmHg) <=120 and Decrease from Baseline >=20Systolic Blood Pressure (mmHg) >=144 and Increase from Baseline >=20Diastolic Blood Pressure (mmHg) <=50 and Decrease from Baseline >=15Diastolic Blood Pressure (mmHg) >=86 and Increase from Baseline >=15Diastolic Blood Pressure (mmHg) <=80 and Decrease from Baseline >=15Diastolic Blood Pressure (mmHg) >=92 and Increase from Baseline >=15
Phase A: Placebo2.30.07.02.37.00.018.64.7
Phase A: Tolvaptan0.02.14.22.14.20.012.50.0
Phase B: Prior Placebo5.30.010.32.60.00.012.82.6
Phase B: Prior Tolvaptan0.00.09.50.09.57.116.74.8

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Phase A and B: Percentage of Participants With Potentially Clinically Significant Abnormalities in Laboratory Test Results Including Liver Function Tests (LFTs)

Laboratory parameters=haematology,chemistry,urinalysis,& LFTs.Criteria for laboratory abnormalities along with their test result grade=Increased creatinine level: Baseline(BSL):Grade 0,>BSL-1.5xBSL:1,>1.5-3xBSL:2,>3-6xBSL:3,>6xBSL:4.Decreased glucose level: <30:-4,30-<40:-3, 40-<55:-2, 55-<65:-1,>=65:0; Increased:<=115:0,>115-160:1,>160-250:2,>250-500:3,>500:4.Decreased potassium level: <2.5:-4,2.5-<3:-3,3-ULN-5.5:1,>5.5-6:2,>6-7:3,>7:4.Decreased sodium level: <120:-4,120-124:-3,125-129:-2,130-135:-1,>=136:0; Increased:<=145:0,146-150:1,151-155:2,156-160:3,>160:4. Increased triglyceride level:ULN:0,>ULN-2.5xULN:1,>2.5-5xULN:2,>5-6xULN:3,>6xULN:4. Decreased Neutrophils:<0.5:-4,0.5-<1:-3,1-<1.5:-2,1.5-1, <-1 or Baseline grade >1,<-1 and post-baseline grade >orNCT02964273)
Timeframe: From first dose of study drug up to 14 days post last dose (up to approximately 37 months)

,,,
Interventionpercentage of participants (Number)
Increase in Creatinine Level (mg/dL)Decrease in Glucose Level (mg/dL)Increase in Potassium Level (milliequivalents per deciliter [mEq/dL])Increase in Sodium Level (mEq/dL)Increase in Triglyceride Level (mg/dL)Decrease in Neutrophils (10^9/L)
Phase A: Placebo0.02.60.00.00.04.9
Phase A: Tolvaptan8.30.02.10.00.00.0
Phase B: Prior Placebo7.72.92.62.60.02.6
Phase B: Prior Tolvaptan7.10.00.00.03.15.0

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Phase A: Percent Change From Phase A Baseline in Height-Adjusted Total Kidney Volume (htTKV) as Measured by Magnetic Resonance Imaging (MRI)

htTKV is used in participants with autosomal dominant polycystic kidney disease to predict the onset of renal insufficiency. (NCT02964273)
Timeframe: Baseline, and Month 12 of Phase A

Interventionpercent change (Mean)
Phase A: Tolvaptan2.28
Phase A: Placebo6.11

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Phase A: 24-hour Urine Volume

Urine volume refers to the quantity of urine produced per unit of time. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

Interventionmilliliter per 24 hours post dose (Mean)
Phase A: Tolvaptan7171
Phase A: Placebo2529

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Phase A: 24-hour Fluid Intake

Daily fluid intake (total water) is defined as the amount of water consumed from foods, plain drinking water, and other beverages. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

Interventionmilliliter (Mean)
Phase A: Tolvaptan7486
Phase A: Placebo3156

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Phase A: 24-hour Fluid Balance

Fluid balance is a term used to describe the balance of the input and output of fluids in the body to allow metabolic processes to function correctly. (NCT02964273)
Timeframe: 24 hours post dose after Month 1 on study medication in Phase A

Interventionmilliliter (Mean)
Phase A: Tolvaptan53
Phase A: Placebo230

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Phase A and B: Percentage of Participants With Aquaretic Adverse Events (AEs)

An AE was defined as any untoward medical occurrence in a participant administered a medicinal product and which does not necessarily have a causal relationship with this treatment. Aquaretic AEs included Medical Dictionary for Regulatory Activities [MedDRA] preferred terms of thirst, polyuria (production of large volumes of dilute urine), nocturia (need to wake up to urinate at night), pollakiuria (abnormally frequent urination), and polydipsia (excessive thirst). As prespecified in the protocol, data for safety is reported by the treatment group (Phase A: Tolvaptan, Phase A: Placebo, Phase B: Prior Tolvaptan and Phase B: Prior Placebo). (NCT02964273)
Timeframe: From first dose of study drug up to 14 days post last dose (up to approximately 37 months)

Interventionpercentage of participants (Number)
Phase A: Tolvaptan64.6
Phase A: Placebo16.3
Phase B: Prior Tolvaptan14.3
Phase B: Prior Placebo48.7

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Area Under the Concentration-time Curve From Time Zero to the Last Observable Concentration at Time t (AUCt) of of Tolvaptan

Blood sampling for plasma tolvaptan concentration before IMP administration and 1, 2, 3, 4, 5, 6, 8, 10, 12, and 16 hours postdose in each period in Cohort 1 and 2 was performed for pharmacokinetic evaluation. (NCT02994394)
Timeframe: Pre-dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16 hours post-dose

Interventionng*h/mL (Mean)
Cohort 1: 15 mg Conventional Tablet697
Cohort 1: 15 mg OD Tablet Without Water674
Cohort 1: 15 mg OD Tablet With Water685
Cohort 2: 30 mg Conventional Tablet1120
Cohort 2: 30 mg OD Tablet Without Water1130
Cohort 2: 30 mg OD Tablet With Water1110

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Maximum Plasma Concentration (Cmax) of Tolvaptan

Blood sampling for plasma tolvaptan concentration before IMP administration and 1, 2, 3, 4, 5, 6, 8, 10, 12, and 16 hours postdose in each period in Cohort 1 and 2 was performed for pharmacokinetic evaluation. (NCT02994394)
Timeframe: Pre-dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16 hours post-dose

Interventionng/mL (Mean)
Cohort 1: 15 mg Conventional Tablet131
Cohort 1: 15 mg OD Tablet Without Water149
Cohort 1: 15 mg OD Tablet With Water125
Cohort 2: 30 mg Conventional Tablet203
Cohort 2: 30 mg OD Tablet Without Water218
Cohort 2: 30 mg OD Tablet With Water198

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Percentage of Subjects With Normalized Serum Sodium Concentration on the Day After Final IMP Administration

The percentage of subjects with normalized serum sodium concentration, defined as ≥135 mEq/L, on the day after final IMP administration will be calculated versus the number of subjects with serum sodium concentration of <135 mEq/L at baseline on Day 1 of the treatment period. (NCT03048747)
Timeframe: Baseline, Day2, Day3, Day4, Day5, Day7, Day14, Day21, Day after final study medication

Interventionpercentage of participants (Number)
Day2Day3Day4Day5Day7Day14Day21Day after final study medication
Tolvaptan43.8808085.792.983.381.881.3

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Change in Serum Sodium Concentration

"The mean and standard error of measured values for serum sodium concentration on the day of fixing the maintenance dose and on the day after final IMP administration were calculated.~The day of fixing the maintenance dose: Day2, Day3, Day4, Day5, Day7, Day14, and Day21" (NCT03048747)
Timeframe: Day2, Day3, Day4, Day5, Day7, Day14, Day21 and the day after final IMP administration

InterventionmEq/L (Mean)
Day2Day3Day4Day5Day7Day14Day21Day after final study medication
Tolvaptan6.98.18.58.810.010.810.411.0

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Area Under the Concentration-time Curve From Time Zero to 24 Hours (AUC24h) on Day 1

(NCT03254108)
Timeframe: Baseline, 1, 1.5, 2, 4, 6, 12 24 hours after the start of administration of investigational drug

Interventionng*h/mL (Mean)
OPC-61815 Injection 2mg356
OPC-61815 Injection 4mg983
OPC-61815 Injection 8mg1340
OPC-61815 Injection 16mg2400
Tolvaptan Tablet 15mg2850

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Maximum Plasma Concentration (Cmax) of OPC-41061 on Day 1

(NCT03254108)
Timeframe: Baseline, 1, 1.5, 2, 4, 6, 12 24 hours after the start of administration of investigational drug

Interventionng/mL (Mean)
OPC-61815 Injection 2mg41.4
OPC-61815 Injection 4mg98.6
OPC-61815 Injection 8mg149
OPC-61815 Injection 16mg282
Tolvaptan Tablet 15mg325

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Improvement Rate for Lower Limb Edema and Pulmonary Congestion

"The improvement rate was defined as the percentage of subjects in whom the symptom was present at baseline and it markedly improved or improved after IMP administration. Improvement category is a 4-point scale below:~Markedly improved~Improved~Unchanged~Deteriorated" (NCT03772041)
Timeframe: Baseline, Day 6

,
Interventionpercentage of participants (Number)
Lower Limb EdemaPulmonary Congestion
OPC-61815 Injection 16 mg68.956.1
Tolvaptan Tablet 15mg75.764.7

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Percentage of Subjects Who Achieve Resolution of Pulmonary Rales and Third Cardiac Sound

"Percentage of subjects in whom the symptom was present at baseline and disappeared after IMP administration was provided.~The presence of pulmonary rales was checked by auscultation.~The presence of cardiac third sound was checked by auscultation." (NCT03772041)
Timeframe: Baseline, Day 6

,
Interventionpercentage of participants (Number)
Pulmonary RalesThird Cardiac Sound
OPC-61815 Injection 16 mg74.331.7
Tolvaptan Tablet 15mg78.931.0

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Improvement Rate for New York Heart Association (NYHA) Classification

"NYHA classification assesses the severity of heart failure based on subjective symptoms as follows.~Class I: No limitations of physical activity. Ordinary physical activity caused no undue fatigue, palpitation, dyspnea or anginal pain.~Class II: Slight limitation of physical activity, comfortable at rest. Ordinary physical activity resulted in fatigue, palpitation, dyspnea or anginal pain.~Class III: Marked limitation of physical activity, comfortable at rest. Less than ordinary physical activity caused fatigue, palpitation, dyspnea or anginal pain.~Class IV: Inability to carry on any physical activity without discomfort. heart failure or anginal syndrome may have been present even at rest. If any physical activity was undertaken, discomfort was increased.~Of the subjects with Class II or higher at baseline, the percentage of subjects whose NYHA classification stage at the time of final IMP administration improved by 1 or more grades was provided." (NCT03772041)
Timeframe: Baseline, Day 6

Interventionpercentage of participants (Number)
OPC-61815 Injection 16 mg44.9
Tolvaptan Tablet 15mg42.5

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Change From Baseline in Body Weight

Change in body weight from baseline (before investigational medicinal product [IMP] administration on Day 1) at time of final IMP administration (day after final IMP administration). A negative change from baseline indicates improvement. (NCT03772041)
Timeframe: Baseline, Day 6

Interventionkg (Least Squares Mean)
OPC-61815 Injection 16 mg-1.67
Tolvaptan Tablet 15mg-1.36

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Change From Baseline in Jugular Venous Distension and Hepatomegaly

"Jugular Venous Distension: the presence of Jugular Venous Distension was checked, and if present, the height (in cm) from the sternal angle to the highest point of pulsation in the internal Jugular vein was measured with the subject in a semi-upright position. A negative change from baseline indicates improvement.~Hepatomegaly: the presence of a palpable liver was checked, and if present, the width (distance from the right costal arch of the right chest, in cm) was measured. A negative change from baseline indicates improvement." (NCT03772041)
Timeframe: Baseline, Day 6

,
Interventioncm (Least Squares Mean)
Jugular Venous DistensionHepatomegaly
OPC-61815 Injection 16 mg-2.89-0.93
Tolvaptan Tablet 15mg-3.15-0.88

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.02106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
ammonium hydroxide
azane : Saturated acyclic nitrogen hydrides having the general formula NnHn+2.		2.1710azane;
gas molecular entity;
mononuclear parent hydride		EC 3.5.1.4 (amidase) inhibitor;
metabolite;
mouse metabolite;
neurotoxin;
NMR chemical shift reference compound;
nucleophilic reagent;
refrigerant
benzyl alcohol
Benzyl Alcohol: A colorless liquid with a sharp burning taste and slight odor. It is used as a local anesthetic and to reduce pain associated with LIDOCAINE injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring.. hydroxytoluene : Any member of the class of toluenes carrying one or more hydroxy substituents.. benzyl alcohol : An aromatic alcohol that consists of benzene bearing a single hydroxymethyl substituent.. aromatic alcohol : Any alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring.. aromatic primary alcohol : Any primary alcohol in which the alcoholic hydroxy group is attached to a carbon which is itself bonded to an aromatic ring.		2.0510benzyl alcoholsantioxidant;
fragrance;
metabolite;
solvent
betaine
glycine betaine : The amino acid betaine derived from glycine.		3.2310amino-acid betaine;
glycine derivative		fundamental metabolite
chlorine
chloride : A halide anion formed when chlorine picks up an electron to form an an anion.		2.7730halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite
bupropion
Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.		3.2310aromatic ketone;
monochlorobenzenes;
secondary amino compound		antidepressant;
environmental contaminant;
xenobiotic
aminocaproic acid
Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator.		3.2310amino acid zwitterion;
epsilon-amino acid;
omega-amino fatty acid		antifibrinolytic drug;
hematologic agent;
metabolite
creatine
[no description available]		3.4711glycine derivative;
guanidines;
zwitterion		geroprotector;
human metabolite;
mouse metabolite;
neuroprotective agent;
nutraceutical
hydrogen carbonate
Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.. hydrogencarbonate : The carbon oxoanion resulting from the removal of a proton from carbonic acid.		3.3510carbon oxoanioncofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
histamine
[no description available]		2.0610aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
iodine
Iodine: A nonmetallic element of the halogen group that is represented by the atomic symbol I, atomic number 53, and atomic weight of 126.90. It is a nutritionally essential element, especially important in thyroid hormone synthesis. In solution, it has anti-infective properties and is used topically.. diiodine : Molecule comprising two covalently bonded iodine atoms with overall zero charge..		4.411diatomic iodinenutrient
melatonin
[no description available]		2.0810acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		2.0510pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		3.2310pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		3.6120monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
pyridoxine
4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms).		3.2310hydroxymethylpyridine;
methylpyridines;
monohydroxypyridine;
vitamin B6		cofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
thiamine
thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively.		3.2310primary alcohol;
vitamin B1		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
thymine
[no description available]		2.0210pyrimidine nucleobase;
pyrimidone		Escherichia coli metabolite;
human metabolite;
mouse metabolite
trimethyloxamine
trimethyloxamine: used in manufacture of quaternary ammonium cpds; insect attractant; warming agent for gas; oxidant; structure. trimethylamine N-oxide : A tertiary amine oxide resulting from the oxidation of the amino group of trimethylamine.		2.2110tertiary amine oxideEscherichia coli metabolite;
metabolite;
osmolyte
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		8.8194uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		9.91163isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
1-(3-chlorophenyl)piperazine
1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.		2.0810monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
1-aminobenzotriazole
[no description available]		2.1510
phenytoin
[no description available]		3.2310imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
tacrine
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.		2.0810acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		3.2310aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		3.9330acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		3.6120monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		3.2310acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
alaproclate
alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer		3.2310alpha-amino acid ester
albendazole
[no description available]		3.6120aryl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
albuterol
Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).		3.8730phenols;
phenylethanolamines;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
environmental contaminant;
xenobiotic
alendronate
alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.		3.23101,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
alfuzosin
alfuzosin: structure given in first source		3.2310monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
alosetron
alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.		3.2310imidazoles;
pyridoindole		antiemetic;
gastrointestinal drug;
serotonergic antagonist
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.2310organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		2.0810secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
altretamine
Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.		3.2310triamino-1,3,5-triazine
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		3.2310adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
ambenonium
ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens.		3.2310quaternary ammonium ionEC 3.1.1.8 (cholinesterase) inhibitor
diatrizoic acid
Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.		3.6120acetamides;
benzoic acids;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
amifostine anhydrous
Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy.		3.2310diamine;
organic thiophosphate		antioxidant;
prodrug;
radiation protective agent
aminoglutethimide
Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.		2.0810dicarboximide;
piperidones;
substituted aniline		adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
p-aminohippuric acid
p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow.		5.921N-acylglycineDaphnia magna metabolite
theophylline
[no description available]		3.6120dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		4.3501-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
dan 2163
[no description available]		2.0810aromatic amide;
aromatic amine;
benzamides;
pyrrolidines;
sulfone		environmental contaminant;
second generation antipsychotic;
xenobiotic
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		3.6120carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amlexanox
amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position.		2.0810monocarboxylic acid;
pyridochromene		anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		3.6120dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		3.6120dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.0810acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
anastrozole
[no description available]		3.6120nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
anthralin
Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9.		2.0810anthracenesantipsoriatic
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		2.0810pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		3.8830benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.0810benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		3.6120ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		3.6120aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
baclofen
[no description available]		3.6120amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
bendazac
bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts.		3.2310indazoles;
monocarboxylic acid		non-steroidal anti-inflammatory drug;
radical scavenger
bendroflumethiazide
Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group.		3.2310benzothiadiazine;
sulfonamide		antihypertensive agent;
diuretic
benzbromarone
Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.		3.61201-benzofurans;
aromatic ketone		uricosuric drug
benzocaine
Benzocaine: A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.. dextran sulfate sodium : An organic sodium salt of dextran sulfate. It induces colitis in mice.. benzocaine : A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.		2.0810benzoate ester;
substituted aniline		allergen;
antipruritic drug;
sensitiser;
topical anaesthetic
betaxolol
[no description available]		3.2310propanolamineantihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bethanechol
Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention.		3.2310carbamate ester;
quaternary ammonium ion		muscarinic agonist
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		3.6120(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
bay h 4502
bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1.		2.0810biphenyls;
imidazoles
biperiden
Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease.		3.2310piperidines;
tertiary alcohol;
tertiary amino compound		antidote to sarin poisoning;
antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist;
parasympatholytic
bisacodyl
Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)		3.6120diarylmethane
bisoprolol
Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.		3.2310secondary alcohol;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bromopride
bromopride: RN given refers to parent cpd; structure		2.0810benzamides
bronopol
[no description available]		2.0810nitro compound
bumetanide
[no description available]		3.930amino acid;
benzoic acids;
sulfonamide		diuretic;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		3.2310azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
busulfan
[no description available]		3.6120methanesulfonate esteralkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent
secbutabarbital
secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital		3.2310barbiturates
caffeine
[no description available]		3.6120purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		3.6120aromatic ether;
nitrile;
polyether;
tertiary amino compound
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		3.2310benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		3.6120dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carbinoxamine
carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease.		3.2310monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist
carisoprodol
Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.		3.2310carbamate estermuscle relaxant
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.0810N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
carprofen
carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.		2.0810carbazoles;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
photosensitizing agent
carvedilol
[no description available]		3.6120carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
celecoxib
[no description available]		3.6120organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		3.2310ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		3.6120aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chlorcyclizine
chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness		3.2310diarylmethane
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		3.6120benzodiazepine
chlormezanone
Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.		3.23101,3-thiazine;
lactam;
monochlorobenzenes;
sulfone		antipsychotic agent;
anxiolytic drug;
muscle relaxant
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		3.6120aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
chlorothiazide
Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension.		5.9821benzothiadiazineantihypertensive agent;
diuretic
chlorpheniramine
Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.		3.6120monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		3.6120organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
chlorpropamide
Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.		3.6120monochlorobenzenes;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
chlorthalidone
Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.		3.6120isoindoles;
monochlorobenzenes;
sulfonamide
chlorzoxazone
Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.		3.61201,3-benzoxazoles;
heteroaryl hydroxy compound;
organochlorine compound		muscle relaxant;
sedative
cifenline
[no description available]		2.0810diarylmethane
ciclopirox
[no description available]		2.0810cyclic hydroxamic acid;
hydroxypyridone antifungal drug;
pyridone		antibacterial agent;
antiseborrheic
ciglitazone
ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.		2.0810aromatic ether;
thiazolidinone		antineoplastic agent;
insulin-sensitizing drug
cilostazol
[no description available]		3.6120lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		3.6120aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
ciprofibrate
[no description available]		2.0810cyclopropanes;
monocarboxylic acid;
organochlorine compound		antilipemic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		3.6120aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		8.88302-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
clioquinol
Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease.		2.0810monohydroxyquinoline;
organochlorine compound;
organoiodine compound		antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antiprotozoal drug;
chelator;
copper chelator
clobazam
Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.		2.08101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		2.0810monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		3.6120aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clomiphene
[no description available]		3.6120tertiary amineestrogen antagonist;
estrogen receptor modulator
clomipramine
Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.		3.6120dibenzoazepineanticoronaviral agent;
antidepressant;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
serotonergic antagonist;
serotonergic drug;
serotonin uptake inhibitor
clonazepam
Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.		3.23101,4-benzodiazepinone;
monochlorobenzenes		anticonvulsant;
anxiolytic drug;
GABA modulator
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		3.2310clonidine;
imidazoline
4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide
[no description available]		2.0810sulfonamide
chlorazepate
clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.		3.23101,4-benzodiazepinoneanticonvulsant;
anxiolytic drug;
GABA modulator;
prodrug
clotrimazole
[no description available]		3.2310conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
cyclobenzaprine
cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm.		3.2310carbotricyclic compoundantidepressant;
muscle relaxant;
tranquilizing drug
cyclofenil
Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE.		3.2310organic molecular entity
cyproheptadine
Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.		3.2310piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
dapsone
[no description available]		3.6120substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug
deferoxamine
Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator.		3.2310acyclic desferrioxaminebacterial metabolite;
ferroptosis inhibitor;
iron chelator;
siderophore
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		3.6120dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		3.2310primary amine
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		3.61201,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		3.6120benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		3.2310amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
dichlorphenamide
Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma.		3.2310dichlorobenzene;
sulfonamide		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
ophthalmology drug
dicyclomine
Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.		3.2310carboxylic ester;
tertiary amine		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
pentetic acid
Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium.		3.2310pentacarboxylic acidcopper chelator
diflunisal
Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position.		3.2310monohydroxybenzoic acid;
organofluorine compound		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
dimercaprol
Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury.		3.2310dithiol;
primary alcohol		chelator
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		3.2310ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
dipyridamole
Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.		3.6120piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol		adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
disopyramide
Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.		3.6120monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
disulfiram
[no description available]		3.6120organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		4.120branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		2.0810benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
donepezil
Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.		3.6120aromatic ether;
indanones;
piperidines;
racemate		EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
doxapram
Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.		3.2310morpholines;
pyrrolidin-2-ones		central nervous system stimulant
doxazosin
Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.		3.2310aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines		alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
doxepin
Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.		3.6120dibenzooxepine;
tertiary amino compound		antidepressant
doxylamine
Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM.		3.2310pyridines;
tertiary amine		anti-allergic agent;
antiemetic;
antitussive;
cholinergic antagonist;
H1-receptor antagonist;
histamine antagonist;
sedative
droperidol
Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.		3.2310aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
dyphylline
Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs.		3.2310oxopurine;
propane-1,2-diols		bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
muscle relaxant;
vasodilator agent
ebastine
[no description available]		2.0810organic molecular entity
edrophonium
Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.		3.2310phenols;
quaternary ammonium ion		antidote;
diagnostic agent;
EC 3.1.1.8 (cholinesterase) inhibitor
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.08101,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
estazolam
Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.		3.2310triazoles;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA modulator
ethacrynic acid
Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor.		3.6120aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid		EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic
ethosuximide
Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures.		3.6120dicarboximide;
pyrrolidinone		anticonvulsant;
geroprotector;
T-type calcium channel blocker
ethotoin
ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective.		3.2310imidazolidine-2,4-dioneanticonvulsant
etidronate
Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces.		3.23101,1-bis(phosphonic acid)antineoplastic agent;
bone density conservation agent;
chelator
etodolac
Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active.		3.2310monocarboxylic acid;
organic heterotricyclic compound		antipyretic;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
brl 42810
[no description available]		3.61202-aminopurines;
acetate ester		antiviral drug;
prodrug
felbamate
Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy.		3.2310carbamate esteranticonvulsant;
neuroprotective agent
4-biphenylylacetic acid
biphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis.		2.0810biphenyls;
monocarboxylic acid		non-steroidal anti-inflammatory drug
felodipine
Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.		3.6120dichlorobenzene;
dihydropyridine;
ethyl ester;
methyl ester		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		3.6120aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
fenoldopam
Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.		3.2310benzazepinealpha-adrenergic agonist;
antihypertensive agent;
dopamine agonist;
dopaminergic antagonist;
vasodilator agent
fenoprofen
Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding.		3.2310monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		3.2310piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
fipexide
fipexide: regulates dopaminergic systems at macromolecular level		3.2310benzodioxoles
flavoxate
Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol.		3.2310carboxylic ester;
flavones;
piperidines;
tertiary amino compound		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		3.2310aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		2.0810difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		4.4430conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		3.6120aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluphenazine
[no description available]		3.2310N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		3.6120ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
fluorescite
fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer.		3.6120benzoic acids;
cyclic ketone;
hydroxy monocarboxylic acid;
organic heterotricyclic compound;
phenols;
xanthene dye		fluorescent dye;
radioopaque medium
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		3.6120nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		3.6120(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
flurazepam
Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia.		3.23101,4-benzodiazepinone;
monofluorobenzenes;
organochlorine compound;
tertiary amino compound		anticonvulsant;
anxiolytic drug;
GABAA receptor agonist;
sedative
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		3.2310fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		3.6120(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
fomepizole
Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4.		3.2310pyrazolesantidote;
EC 1.1.1.1 (alcohol dehydrogenase) inhibitor;
protective agent
foscarnet
Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		3.7320carboxylic acid;
one-carbon compound;
phosphonic acids		antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		15.246432chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
gabapentin
Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.		3.2310gamma-amino acidanticonvulsant;
calcium channel blocker;
environmental contaminant;
xenobiotic
gemfibrozil
[no description available]		3.6120aromatic etherantilipemic drug
glafenine
Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market.		3.2310aminoquinoline;
carboxylic ester;
glycol;
organochlorine compound;
secondary amino compound		inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gliclazide
Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.		2.0810N-sulfonylureahypoglycemic agent;
insulin secretagogue;
radical scavenger
glimepiride
glimepiride: structure given in first source		3.6120sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		3.6120aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		3.6120monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester
[no description available]		3.2310benzenes
granisetron
[no description available]		3.2310aromatic amide;
indazoles
guaifenesin
Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations.		3.2310methoxybenzenes
guanethidine
Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.		3.2310azocanes;
guanidines		adrenergic antagonist;
antihypertensive agent;
sympatholytic agent
guanfacine
Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.		3.6120acetamides
guanidine
Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines.		3.2310carboxamidine;
guanidines;
one-carbon compound
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		3.6120aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
hydralazine
Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent.		4.0720azaarene;
hydrazines;
ortho-fused heteroarene;
phthalazines		antihypertensive agent;
vasodilator agent
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		6.4162benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroflumethiazide
Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide.		3.6120benzothiadiazine;
thiazide		antihypertensive agent;
diuretic
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		3.2310aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
hydroxyurea
[no description available]		3.6120one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		3.2310hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		3.2310monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
phenelzine
Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.		3.2310primary amine
lidocaine
Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.		3.6120benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
ifosfamide
[no description available]		3.8930ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		3.6120dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
amrinone
Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.		3.6120bipyridinesEC 3.1.4.* (phosphoric diester hydrolase) inhibitor
indapamide
Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.		3.6120indoles;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		3.6120aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
iohexol
Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position.		2.0810benzenedicarboxamide;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
iothalamic acid
Iothalamic Acid: A contrast medium in diagnostic radiology with properties similar to those of diatrizoic acid. It is used primarily as its sodium and meglumine (IOTHALAMATE MEGLUMINE) salts.		4.3711organic molecular entity
ioversol
[no description available]		3.2310amidobenzoic acid
iproniazid
[no description available]		3.6120carbohydrazide;
pyridines
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		3.6120azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
isocarboxazid
Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311)		3.2310benzenes
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		3.6120carbohydrazideantitubercular agent;
drug allergen
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		3.2310catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
isoxsuprine
Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.		3.2310alkylbenzene
isradipine
Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.		3.6120benzoxadiazole;
dihydropyridine;
isopropyl ester;
methyl ester
itraconazole
[no description available]		3.6120piperazines
ketamine
Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.		3.6120cyclohexanones;
monochlorobenzenes;
secondary amino compound		analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
ketanserin
Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.		2.0810aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		5.2731dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketoprofen
Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.		3.2310benzophenones;
oxo monocarboxylic acid		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketorolac
Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.		3.2310amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate		analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
labetalol
Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5.		3.2310benzamides;
benzenes;
phenols;
primary carboxamide;
salicylamides;
secondary alcohol;
secondary amino compound
lamotrigine
[no description available]		3.61201,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		3.6120benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		3.6120(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
letrozole
[no description available]		3.6120nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
lofepramine
Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.		2.0810aromatic ketone;
dibenzoazepine;
monochlorobenzenes;
tertiary amino compound		antidepressant
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		3.2310fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
lomustine
[no description available]		3.6120N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
loperamide
Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		3.2310monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol		anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		3.6120benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
lorazepam
Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.		3.2310benzodiazepine
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		3.2310biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
loxapine
Loxapine: An antipsychotic agent used in SCHIZOPHRENIA.		3.2310dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
maprotiline
Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.		3.6120anthracenes
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		3.6120aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
mecamylamine
Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.		3.2310primary aliphatic amine
mechlorethamine
nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.		3.2310nitrogen mustard;
organochlorine compound		alkylating agent
meclizine
Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.		3.2310diarylmethane
meclofenamic acid
Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.		3.2310aminobenzoic acid;
organochlorine compound;
secondary amino compound		analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		3.6120aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
memantine
[no description available]		3.2310adamantanes;
primary aliphatic amine		antidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
mepenzolate
mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure		3.2310diarylmethane
meperidine
Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.		3.2310ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
mephenytoin
Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism.		3.2310imidazolidine-2,4-dioneanticonvulsant
mepivacaine
Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic.		3.2310piperidinecarboxamidedrug allergen;
local anaesthetic
meprobamate
Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603)		3.2310organic molecular entity
mesalamine
Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.		3.2310amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols		non-steroidal anti-inflammatory drug
mesoridazine
Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group.		3.2310phenothiazines;
sulfoxide;
tertiary amino compound		dopaminergic antagonist;
first generation antipsychotic
metaproterenol
Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself.		3.2310aralkylamino compound;
phenylethanolamines;
resorcinols;
secondary alcohol;
secondary amino compound
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		4.9540guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methadone
Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.		3.2310benzenes;
diarylmethane;
ketone;
tertiary amino compound
methazolamide
Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.		3.2310sulfonamide;
thiadiazoles
methocarbamol
Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester.		3.2310aromatic ether;
carbamate ester;
secondary alcohol
methoxsalen
Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis.		3.2310aromatic ether;
psoralens		antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite
methyclothiazide
Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825)		3.2310benzothiadiazine
methylphenidate
Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group.		3.2310beta-amino acid ester;
methyl ester;
piperidines
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		3.6120benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
metolazone
Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics.		5.9821organochlorine compound;
quinazolines;
sulfonamide		antihypertensive agent;
diuretic;
ion transport inhibitor
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		3.8930aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		3.6120C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
metyrapone
Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency.		3.2310aromatic ketoneantimetabolite;
diagnostic agent;
EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		3.6120aromatic ether;
primary amino compound		anti-arrhythmia drug
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		3.6120imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
midodrine
Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.		10.9421amino acid amide;
aromatic ether;
secondary alcohol		alpha-adrenergic agonist;
prodrug;
sympathomimetic agent;
vasoconstrictor agent
milrinone
[no description available]		3.2310bipyridines;
nitrile;
pyridone		cardiotonic drug;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
minoxidil
Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.		3.6120dialkylarylamine;
tertiary amino compound
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		3.6120benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
mitotane
Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.		3.2310diarylmethane
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		3.2310dihydroxyanthraquinoneanalgesic;
antineoplastic agent
moclobemide
Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression.		2.0810benzamides;
monochlorobenzenes;
morpholines		antidepressant;
environmental contaminant;
xenobiotic
modafinil
Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.		3.2310monocarboxylic acid amide;
sulfoxide
moxisylyte
Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312)		3.2310monoterpenoid
acecainide
Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine.		2.0810acetamides;
benzamides		anti-arrhythmia drug
nabumetone
Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.		3.2310methoxynaphthalene;
methyl ketone		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
nadolol
[no description available]		3.6120tetralins
nalidixic acid
[no description available]		3.61201,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
naratriptan
naratriptan: structure given in first source		3.2310heteroarylpiperidine;
sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
nefazodone
nefazodone: may be useful as an opiate adjunct		3.6120aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles		alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor
nefopam
Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26). nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain.. 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively.		2.0810benzoxazocine;
tertiary amino compound
neostigmine
Neostigmine: A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.. neostigmine : A quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor.		2.0810quaternary ammonium ionantidote to curare poisoning;
EC 3.1.1.7 (acetylcholinesterase) inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		3.6120cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nialamide
Nialamide: An MAO inhibitor that is used as an antidepressive agent.		3.2310organonitrogen compound;
organooxygen compound
nicardipine
Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.		3.6120benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		3.6120C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
nilutamide
[no description available]		3.2310(trifluoromethyl)benzenes;
C-nitro compound;
imidazolidinone		androgen antagonist;
antineoplastic agent
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		3.6120aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
nimodipine
Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.		3.61202-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester		antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
nisoldipine
Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris.		3.6120C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
methyl ester
nitrazepam
Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome).		2.08101,4-benzodiazepinone;
C-nitro compound		anticonvulsant;
antispasmodic drug;
drug metabolite;
GABA modulator;
sedative
nitrendipine
Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension.		2.0810C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
nitroglycerin
Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.		3.2310nitroglycerolexplosive;
muscle relaxant;
nitric oxide donor;
prodrug;
tocolytic agent;
vasodilator agent;
xenobiotic
nizatidine
[no description available]		3.23101,3-thiazoles;
C-nitro compound;
carboxamidine;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
cholinergic drug;
H2-receptor antagonist
nomifensine
Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.		3.2310isoquinolinesdopamine uptake inhibitor
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		3.6120fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
nortriptyline
Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.		3.6120organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		3.61203-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		3.6120aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		3.6120carbazoles
orphenadrine
Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.		3.2310ether;
tertiary amino compound		antidyskinesia agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
oxaprozin
Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis.		3.61201,3-oxazoles;
monocarboxylic acid		analgesic;
non-steroidal anti-inflammatory drug
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		3.23101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
oxybutynin
oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.		3.6120acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound		antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic
aminosalicylic acid
Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.		3.2310aminobenzoic acid;
phenols		antitubercular agent
pamidronate
[no description available]		3.2310phosphonoacetic acid
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		3.2310aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
papaverine
Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.		3.6120benzylisoquinoline alkaloid;
dimethoxybenzene;
isoquinolines		antispasmodic drug;
vasodilator agent
pemoline
Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.		3.61201,3-oxazolescentral nervous system stimulant
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		3.6120aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
pentobarbital
Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		3.2310barbituratesGABAA receptor agonist
pentoxifylline
[no description available]		3.6120oxopurine
perhexiline
Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis.		3.2310piperidinescardiovascular drug
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		3.6120N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
phenacetin
Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione		2.0810acetamides;
aromatic ether		cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		3.2310barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
phenoxybenzamine
Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.		3.2310aromatic amine
phentermine
Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity.		3.2310primary amineadrenergic agent;
appetite depressant;
central nervous system drug;
central nervous system stimulant;
dopaminergic agent;
sympathomimetic agent
4-phenylbutyric acid
4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation.		3.2310monocarboxylic acidantineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		3.6120indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		8.9330aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
piracetam
Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent.		2.520organonitrogen compound;
organooxygen compound
piribedil
Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.		2.0810N-arylpiperazine
polythiazide
[no description available]		3.2310benzothiadiazine
duodote
duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents		3.2310pyridinium ionantidote to organophosphate poisoning;
antidote to sarin poisoning;
cholinergic drug;
cholinesterase reactivator
ono 1078
pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist		2.0810chromones
pyranoprofen
pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source		2.0810pyridochromene
praziquantel
azinox: Russian drug		3.6120isoquinolines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		3.6120aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		3.6120aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
primidone
Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures.		3.6120pyrimidoneanticonvulsant;
environmental contaminant;
xenobiotic
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		3.6120benzoic acids;
sulfonamide		uricosuric drug
probucol
Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.		2.0310dithioketal;
polyphenol		anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		3.6120benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
procarbazine
Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		3.2310benzamides;
hydrazines		antineoplastic agent
prochlorperazine
Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.		3.6120N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines		alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
procyclidine
Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.		3.6120pyrrolidines;
tertiary alcohol		antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist
promethazine
Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.		3.6120phenothiazines;
tertiary amine		anti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
sedative
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		3.6120aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propantheline
Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.		3.2310xanthenes
propofol
Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.		3.2310phenolsanticonvulsant;
antiemetic;
intravenous anaesthetic;
radical scavenger;
sedative
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		3.6120naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
protriptyline
Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.		3.2310carbotricyclic compoundantidepressant
pyridostigmine
[no description available]		3.2310pyridinium ion
pyrimethamine
Maloprim: contains above 2 cpds		3.2310aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sch 16134
quazepam: structure given in first source		3.2310benzodiazepine
quetiapine
[no description available]		3.2310dibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine		adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
rabeprazole
Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.		3.2310benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
raloxifene
raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.		3.23101-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols		bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
ranitidine
[no description available]		2.0810aralkylamine
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		3.6120benzothiazoles
rimantadine
Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.		3.2310alkylamine
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		3.61201,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
rizatriptan
rizatriptan: structure given in first source; RN given refers to benzoate		3.2310tryptaminesanti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rofecoxib
[no description available]		2.4520butenolide;
sulfone		analgesic;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
ropinirole
[no description available]		3.2310indolones;
tertiary amine		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
dopamine agonist
salicylsalicylic acid
salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes.		3.2310benzoate ester;
benzoic acids;
phenols;
salicylates		antineoplastic agent;
antirheumatic drug;
EC 3.5.2.6 (beta-lactamase) inhibitor;
hypoglycemic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
secobarbital
Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups.		3.2310barbituratesanaesthesia adjuvant;
GABA modulator;
sedative
sibutramine
sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride		3.2310organochlorine compound;
tertiary amino compound		anti-obesity agent;
serotonin uptake inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		3.6120pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
risedronic acid
Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION.		3.2310pyridines
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		3.6120ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
imatinib
[no description available]		3.6120aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		3.6120dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
succinylcholine
Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid.		3.2310quaternary ammonium ion;
succinate ester		drug allergen;
muscle relaxant;
neuromuscular agent
sulfamethizole
Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2.		3.2310sulfonamide antibiotic;
sulfonamide;
thiadiazoles		antiinfective agent;
antimicrobial agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		2.0810isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfanitran
[no description available]		2.0810sulfonamide
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		3.6120
sulfathiazole
Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position.		3.23101,3-thiazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sulfisoxazole
Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.. sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms.		2.0810isoxazoles;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
drug allergen
2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol
[no description available]		3.2310alkylbenzene
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		3.6120sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		2.0810N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		2.0810acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
temazepam
Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.		3.2310benzodiazepine
temozolomide
[no description available]		3.6120imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		3.6120furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
terbutaline
Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.		3.6120phenylethanolamines;
resorcinols		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hypoglycemic agent;
sympathomimetic agent;
tocolytic agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		2.0810diarylmethane
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		3.2310phthalimides;
piperidones
thiabendazole
Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate		3.23101,3-thiazoles;
benzimidazole fungicide;
benzimidazoles		antifungal agrochemical;
antinematodal drug
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		3.2310phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
thiotepa
Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed).		3.6120aziridines
tiapride
[no description available]		2.0810benzamides
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		3.8730monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
tilorone
Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.. tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug.		2.0810aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound		anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist
tinidazole
Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent.		3.6120imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
tiopronin
Tiopronin: Sulfhydryl acylated derivative of GLYCINE.		3.2310N-acyl-amino acid
tizanidine
tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.		3.6120benzothiadiazole;
imidazoles		alpha-adrenergic agonist;
muscle relaxant
nikethamide
Nikethamide: A central nervous system stimulant. It was formerly used in the treatment of barbiturate overdose but is now considered to be of no value for such purposes and may be dangerous. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1229)		2.0810pyridinecarboxamide
tolazamide
Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.		3.2310N-sulfonylureahypoglycemic agent;
potassium channel blocker
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		3.6120N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
tolmetin
Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.		3.2310aromatic ketone;
monocarboxylic acid;
pyrroles		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
tolnaftate
[no description available]		2.0810monothiocarbamic esterantifungal drug
ultram
2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively.		3.2310aromatic ether;
tertiary alcohol;
tertiary amino compound
tranexamic acid
Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage.		3.2310amino acid
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		3.6120monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
triamterene
Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.		3.6120pteridinesdiuretic;
sodium channel blocker
triazolam
Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.		3.2310triazolobenzodiazepinesedative
trichlormethiazide
Trichlormethiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830). trichlormethiazide : A benzothiadiazine, hydrogenated at positions 2, 3 and 4 and substituted with an aminosulfonyl group at C-7, a chloro substituent at C-6 and a dichloromethyl group at C-3 and with S-1 as an S,S-dioxide. A sulfonamide antibiotic, it is used as a diuretic to treat oedema (including that associated with heart failure) and hypertension.		8.9421benzothiadiazine;
sulfonamide antibiotic		antihypertensive agent;
diuretic
trifluoperazine
[no description available]		3.2310N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
trihexyphenidyl
Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic.		3.2310amine
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		3.2310oxazolidinoneanticonvulsant;
geroprotector
trimethobenzamide
trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans.		3.2310benzamides;
tertiary amino compound		antiemetic
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		3.6120aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		3.2310
trimipramine
Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant.		3.2310dibenzoazepine;
tertiary amino compound		antidepressant;
environmental contaminant;
xenobiotic
troglitazone
Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.		4.4230chromanes;
thiazolidinone		anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
thenoyltrifluoroacetone
Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration.		2.0810
tyramine
[no description available]		3.2310monoamine molecular messenger;
primary amino compound;
tyramines		EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
delavirdine
Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		3.2310aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
undecylenic acid
undecylenic acid: a fatty acid with a terminal double bond. 10-undecenoic acid : An undecenoic acid having its double bond in the 10-position. It is derived from castor oil and is used for the treatment of skin problems.. undecenoic acid : A C11, straight-chain fatty acid carrying a C=C double bond at any position.		2.0810undecenoic acidantifungal drug;
plant metabolite
urapidil
[no description available]		2.0810piperazines
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		3.6120cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
vigabatrin
[no description available]		3.6120gamma-amino acidanticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor
pirinixic acid
pirinixic acid: structure		2.0810aryl sulfide;
organochlorine compound;
pyrimidines
ici 204,219
zafirlukast: a leukotriene D4 receptor antagonist		3.6120carbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
zaleplon
zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.		3.6120nitrile;
pyrazolopyrimidine		anticonvulsant;
anxiolytic drug;
central nervous system depressant;
sedative
zolpidem
Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.		3.2310imidazopyridinecentral nervous system depressant;
GABA agonist;
sedative
zonisamide
Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.		3.61201,2-benzoxazoles;
sulfonamide		anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
zopiclone
zopiclone: S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position.		2.0810monochloropyridine;
pyrrolopyrazine		central nervous system depressant;
sedative
cortisone acetate
Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.		3.2310corticosteroid hormone
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		3.2310mitomycinalkylating agent;
antineoplastic agent
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		3.893011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		3.6120alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		3.2310imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		3.2310glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		3.23102-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
dextroamphetamine
Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.		3.23101-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
spironolactone
Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.		12.51123-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester		aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
aldosterone
[no description available]		3.568011beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
penicillamine
Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group.		3.6120non-proteinogenic alpha-amino acid;
penicillamine		antirheumatic drug;
chelator;
copper chelator;
drug allergen
cysteine
[no description available]		3.2310cysteine zwitterion;
cysteine;
L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid		EC 4.3.1.3 (histidine ammonia-lyase) inhibitor;
flour treatment agent;
human metabolite
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		3.231011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		3.231017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
oxandrolone
Oxandrolone: A synthetic hormone with anabolic and androgenic properties.		3.231017beta-hydroxy steroid;
3-oxo steroid;
anabolic androgenic steroid;
oxa-steroid		anabolic agent;
androgen
penicillin g
Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.		3.2310penicillin allergen;
penicillin		antibacterial drug;
drug allergen;
epitope
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		3.2310pilocarpineantiglaucoma drug
triiodothyronine
Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.		3.23102-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine		human metabolite;
mouse metabolite;
thyroid hormone
carbon tetrachloride
Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.		2.5120chlorocarbon;
chloromethanes		hepatotoxic agent;
refrigerant
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		3.6120C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		3.2310amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
vincristine
[no description available]		3.2310acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		3.2310carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		2.081017-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
tubocurarine
Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.. tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.. isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine.		2.0810bisbenzylisoquinoline alkaloiddrug allergen;
muscle relaxant;
nicotinic antagonist
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		3.6120aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
methyltestosterone
Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position.		3.231017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
enone		anabolic agent;
androgen;
antineoplastic agent
tetrabenazine
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7.		3.2310benzoquinolizine;
cyclic ketone;
tertiary amino compound
puromycin aminonucleoside
3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine: structure in first source. 3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine : Puromycin derivative that lacks the methoxyphenylalanyl group on the amine of the sugar ring.		7.05103'-deoxyribonucleoside;
adenosines
kanamycin a
Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components.		3.6120kanamycinsbacterial metabolite
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.1110monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.0810amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
edetic acid
Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.		3.2310ethylenediamine derivative;
polyamino carboxylic acid;
tetracarboxylic acid		anticoagulant;
antidote;
chelator;
copper chelator;
geroprotector
cysteamine
Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2.		3.2310amine;
thiol		geroprotector;
human metabolite;
mouse metabolite;
radiation protective agent
acetylcholine chloride
acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug.		3.2310quaternary ammonium salt
mepazine
mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position.		3.2310phenothiazines
cloxacillin
Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6.		3.2310penicillin allergen;
penicillin;
semisynthetic derivative		antibacterial agent;
antibacterial drug
calcium acetate
calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces.		3.2310calcium saltchelator
methionine
Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.		3.2310aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid		antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		3.6120alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
mebanazine
mebanazine: RN given refers to parent cpd without isomeric designation; structure		3.2310benzenes
oxacillin
Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.		3.2310penicillinantibacterial agent;
antibacterial drug
triamcinolone diacetate
triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone		2.0810corticosteroid hormone
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		3.23104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
benziodarone
benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74)		3.2310aromatic ketone
ampicillin
Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.		3.2310beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
mannitol
[no description available]		3.2310mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
cytarabine
[no description available]		3.6120beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
medroxyprogesterone acetate
[no description available]		2.081020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester		adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		3.6320arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
perflutren
Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines.		3.2310fluoroalkane;
fluorocarbon
triamcinolone acetonide
Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections.		2.081011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
cyclic ketal;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
fluoxymesterone
Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women.		3.231011beta-hydroxy steroid;
17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
anabolic androgenic steroid;
fluorinated steroid		anabolic agent;
antineoplastic agent
methsuximide
methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation		3.2310organic molecular entity
tromethamine
Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)		3.2310primary amino compound;
triol		buffer
taurocholic acid
Taurocholic Acid: The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.. taurocholate : An organosulfonate oxoanion that is the conjugate base of taurocholic acid.. taurocholic acid : A bile acid taurine conjugate of cholic acid that usually occurs as the sodium salt of bile in mammals.		2.1310amino sulfonic acid;
bile acid taurine conjugate		human metabolite
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		3.61206-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.0810organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
brompheniramine
Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310organobromine compound;
pyridines		anti-allergic agent;
H1-receptor antagonist
penicillin v
Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain.		3.2310penicillin allergen;
penicillin
isosorbide dinitrate
Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action.		4.0720glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
penicillanic acid
Penicillanic Acid: A building block of penicillin, devoid of significant antibacterial activity. (From Merck Index, 11th ed). penicillanic acid : A penam that consists of 3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane bearing a carboxy group at position 2 and having (2S,5R)-configuration.		2.1310penicillanic acids
pseudoephedrine
Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group.		3.2310phenylethanolamines;
secondary alcohol;
secondary amino compound		anti-asthmatic drug;
bronchodilator agent;
central nervous system drug;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
diethylpropion
Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity.		3.2310aromatic ketone;
tertiary amine		appetite depressant
benzonatate
benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant.		3.2310benzoate ester;
secondary amino compound;
substituted aniline		anaesthetic;
antitussive
cyclohexanol
Cyclohexanols: Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.. cyclohexanols : An alcohol in which one or more hydroxy groups are attached to a cyclohexane skeleton.		2.0710cyclohexanols;
secondary alcohol		solvent
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		10.76330pyrrole;
secondary amine
methylergonovine
Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed)		3.2310ergoline alkaloid
phenformin
Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.		2.0810biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent
cinchophen
cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94		3.2310quinolines
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		2.2510methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
nafcillin
Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group.		3.2310penicillin allergen;
penicillin		antibacterial drug
methohexital
Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups.		3.2310acetylenic compound;
barbiturates		drug allergen;
intravenous anaesthetic
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		3.1710indazole
thiazoles
[no description available]		2.05101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
ephedrine
Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively.		3.2310phenethylamine alkaloid;
phenylethanolamines		bacterial metabolite;
environmental contaminant;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
aminophylline
Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio.		3.6120mixturebronchodilator agent;
cardiotonic drug
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		3.2310N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
galantamine
Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils.		3.6120benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound		antidote to curare poisoning;
cholinergic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant metabolite
nandrolone decanoate
Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS.		3.2310steroid ester
procarbazine hydrochloride
procarbazine hydrochloride : A hydrochloride obtained by combining procarbazine with one equivalent of hydrochloric acid. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.0810hydrochlorideantineoplastic agent
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.081011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
dextropropoxyphene
Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene.		3.23101-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoatemu-opioid receptor agonist;
opioid analgesic
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		3.2310bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.0810isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
4-hydroxybutyric acid
4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group.		3.23104-hydroxy monocarboxylic acid;
hydroxybutyric acid		general anaesthetic;
GHB receptor agonist;
neurotoxin;
sedative
dihydroergotamine
Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension.		3.2310ergot alkaloid;
semisynthetic derivative		dopamine agonist;
non-narcotic analgesic;
serotonergic agonist;
sympatholytic agent;
vasoconstrictor agent
medroxyprogesterone
[no description available]		3.231017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		contraceptive drug;
progestin;
synthetic oral contraceptive
dimenhydrinate
gravinol: has antioxidant and ant-inflammatory activities; structure in first source		3.6120diarylmethane
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		3.2310amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
levocarnitine
(R)-carnitine : The (R)-enantiomer of carnitine.		3.2310carnitineantilipemic drug;
nootropic agent;
nutraceutical;
Saccharomyces cerevisiae metabolite;
water-soluble vitamin (role)
sulfanilylurea
sulfanilylurea: antimicrobial agent; structure		3.2310benzenes;
sulfonamide
1-naphthylisothiocyanate
1-Naphthylisothiocyanate: A tool for the study of liver damage which causes bile stasis and hyperbilirubinemia acutely and bile duct hyperplasia and biliary cirrhosis chronically, with changes in hepatocyte function. It may cause skin and kidney damage.		2.0810isothiocyanateinsecticide
lithium carbonate
Lithium Carbonate: A lithium salt, classified as a mood-stabilizing agent. Lithium ion alters the metabolism of BIOGENIC MONOAMINES in the CENTRAL NERVOUS SYSTEM, and affects multiple neurotransmission systems.		3.1510carbonate salt;
lithium salt		antimanic drug
lactulose
[no description available]		3.2310glycosylfructosegastrointestinal drug;
laxative
megestrol acetate
[no description available]		2.081020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
pamabrom
[no description available]		3.2310
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		3.2310acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		3.6120cyclic ketone;
erythromycin
hydroxychloroquine sulfate
[no description available]		2.0810
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		3.612017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
diphenoxylate
Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin.		3.2310ethyl ester;
nitrile;
piperidinecarboxylate ester;
tertiary amine		antidiarrhoeal drug
deoxycytidine
[no description available]		2.0810pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
ethambutol hydrochloride
ethambutol dihydrochloride : The dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone.		2.0810hydrochlorideantitubercular agent
ethambutol
Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.		3.2310ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
antimycin a
[no description available]		2.0810benzamides;
formamides;
macrodiolide;
phenols		antifungal agent;
mitochondrial respiratory-chain inhibitor;
piscicide
vancomycin
Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.		3.2310glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		3.2310alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
pregnenolone carbonitrile
Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.		2.0810aliphatic nitrile
ibufenac
ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects.		3.2310monocarboxylic acidEC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
metylperon
metylperon: RN given refers to parent cpd		2.0810aromatic ketone
metaxalone
[no description available]		3.2310aromatic ether
spectinomycin
Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis.		3.2310cyclic acetal;
cyclic hemiketal;
cyclic ketone;
pyranobenzodioxin;
secondary alcohol;
secondary amino compound		antibacterial drug;
antimicrobial agent;
bacterial metabolite
dronabinol
Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.		3.2310benzochromene;
diterpenoid;
phytocannabinoid;
polyketide		cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
amiloride
Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.		3.5920aromatic amine;
guanidines;
organochlorine compound;
pyrazines		diuretic;
sodium channel blocker
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		3.2310benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
dexbrompheniramine
dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310brompheniramineanti-allergic agent;
H1-receptor antagonist
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		3.6120dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
dicloxacillin
Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group.		3.6120dichlorobenzene;
penicillin		antibacterial drug
fluorescein-5-isothiocyanate
Fluorescein-5-isothiocyanate: Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.. fluorescein 5-isothiocyanate : The 5-isomer of fluorescein isothiocyanate. Acts as a fluorescent probe capable of being conjugated to tissue and proteins; used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.		2.0310fluorescein isothiocyanate
megestrol
Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17.		3.231017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
streptomycin
[no description available]		3.2310antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor
cladribine
[no description available]		3.6120organochlorine compound;
purine 2'-deoxyribonucleoside		antineoplastic agent;
immunosuppressive agent
carbenicillin
Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain.		3.2310penicillin allergen;
penicillin		antibacterial drug
metocurine
metocurine: from Chinese herb Cyclea hainanensis Mrr		2.0810isoquinolines
clomacran
clomacran: RN given refers to parent cpd; structure		3.2310acridines
methenamine hippurate
methenamine hippurate: both parts of molecule contribute to its antibacterial action		3.2310N-acylglycine
olsalazine
olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease.		3.2310azobenzenes;
dicarboxylic acid		non-steroidal anti-inflammatory drug;
prodrug
etidronate disodium
etidronate disodium : An organic sodium salt resulting from the replacement of two protons from etidronic acid (one from from each of the phosphonic acid groups) by sodium ions.		2.0810organic sodium saltantineoplastic agent;
bone density conservation agent;
chelator
palladium
Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.		2.0310metal allergen;
nickel group element atom;
platinum group metal atom
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		2.0810pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.0810delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
ferrous sulfate
ferrous sulfate: Ferro-Gradumet is ferrous sulfate in controlled release form; RN given refers to Fe(+2)[1:1] salt. iron(2+) sulfate (anhydrous) : A compound of iron and sulfate in which the ratio of iron(2+) to sulfate ions is 1:1. Various hydrates occur naturally - most commonly the heptahydrate, which loses water to form the tetrahydrate at 57degreeC and the monohydrate at 65degreeC.		2.1310iron molecular entity;
metal sulfate		reducing agent
tricalcium phosphate
tricalcium phosphate: a form of tricalcium phosphate used as bioceramic bone replacement material; see also records for alpha-tricalcium phosphate, beta-tricalcium phosphate, calcium phosphate; apatitic tricalcium phosphate Ca9(HPO4)(PO4)5(OH) is the calcium orthophosphate leading to beta tricalcium phosphate Ca3(PO4)2 (b-TCP). calcium phosphate : A calcium salt composed of calcium and phosphate/diphosphate ions; present in milk and used for the mineralisation of calcified tissues.		3.5111calcium phosphate
sodium thiosulfate
sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio.		3.2310inorganic sodium saltantidote to cyanide poisoning;
antifungal drug;
nephroprotective agent
chlorine
Chlorine: An element with atomic symbol Cl, atomic number 17, and atomic weight 35, and member of the halogen family.		2.1510diatomic chlorine;
gas molecular entity		bleaching agent
vasotocin
Vasotocin: A nonapeptide that contains the ring of OXYTOCIN and the side chain of ARG-VASOPRESSIN with the latter determining the specific recognition of hormone receptors. Vasotocin is the non-mammalian vasopressin-like hormone or antidiuretic hormone regulating water and salt metabolism.. vasotocin : A heterodetic cyclic peptide that is homologous to oxytocin and vasopressin. It is a pituitary hormone that acts as an endocrine regulator for water balance, osmotic homoeostasis and is involved in social and sexual behavior in non-mammalian vertebrates.		2.1110
mafenide acetate
[no description available]		2.0810carboxylic acid
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		2.0810anthraquinone
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		3.2310selegiline;
terminal acetylenic compound		geroprotector
selegiline hydrochloride, (r)-isomer
[no description available]		2.0810hydrochloride;
terminal acetylenic compound		antiparkinson drug;
dopaminergic agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor
clemastine
Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		3.2310monochlorobenzenes;
N-alkylpyrrolidine		anti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
thiamphenicol
[no description available]		2.0810monocarboxylic acid amide;
sulfone		antimicrobial agent;
immunosuppressive agent
pancuronium bromide
pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication.		2.0810bromide saltcholinergic antagonist;
muscle relaxant;
nicotinic antagonist
cephalexin
Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
semisynthetic derivative		antibacterial drug
ornidazole
Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.		2.0810C-nitro compound;
imidazoles;
organochlorine compound;
secondary alcohol		antiamoebic agent;
antibacterial drug;
antiinfective agent;
antiprotozoal drug;
antitrichomonal drug;
epitope
danazol
Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.		3.612017beta-hydroxy steroid;
terminal acetylenic compound		anti-estrogen;
estrogen antagonist;
geroprotector
fenclozic acid
fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd		3.2310
laxagetten 4,4'-diacetoxydiphenylpyridylemethane
[no description available]		3.2310
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		3.2310aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
fludarabine phosphate
fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas.		3.6120nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate		antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug
alclofenac
alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash.		3.2310aromatic ether;
monocarboxylic acid;
monochlorobenzenes		drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		3.2310indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
oxyphenisatin
[no description available]		3.2310indoles
fludrocortisone
Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity.		3.231011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
fluorinated steroid;
mineralocorticoid		adrenergic agent;
anti-inflammatory drug
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		3.2310bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		2.0810C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
calcium oxalate
Calcium Oxalate: The calcium salt of oxalic acid, occurring in the urine as crystals and in certain calculi.. calcium oxalate : The calcium salt of oxalic acid, which in excess in the urine may lead to formation of oxalate calculi (kidney stones).		4.0221organic calcium salt
dexchlorpheniramine
dexchlorpheniramine: RN given refers to parent cpd(S)-isomer		3.2310chlorphenamine
clometacin
clometacin: structure		3.2310N-acylindole
cefazolin
Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
tetrazoles;
thiadiazoles		antibacterial drug
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		3.6120penicillin allergen;
penicillin		antibacterial drug
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		3.6120timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
indoramin
Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.		2.0810tryptamines
oxcarbazepine
Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.		3.6120cyclic ketone;
dibenzoazepine		anticonvulsant;
drug allergen
carbidopa
carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		3.6120catechols;
hydrazines;
monocarboxylic acid		antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
moricizine
Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group.		3.2310carbamate ester;
morpholines;
phenothiazines		anti-arrhythmia drug
amineptin
amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne.		3.2310amino acid;
carbocyclic fatty acid;
carbotricyclic compound;
secondary amino compound		antidepressant;
dopamine uptake inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		3.6120azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
feprazone
Feprazone: A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15)		2.0810organic molecular entity
pirprofen
pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure		3.2310pyrroline
tobramycin
Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.		2.0810amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		3.8930taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		3.6120beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
dobutamine
Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.		4.1320catecholamine;
secondary amine		beta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
penbutolol
Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.		3.2310ethanolamines
ribavirin
Rebetron: Rebetron is tradename		3.61201-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
amikacin
Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group.		3.6120alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin
cephradine
Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton.		3.2310beta-lactam antibiotic allergen;
cephalosporin		antibacterial drug
ticrynafen
Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis.		3.2310aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid;
thiophenes		antihypertensive agent;
hepatotoxic agent;
loop diuretic
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		3.2310L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		3.61205-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
lonidamine
lonidamine: structure. lonidamine : A member of the class of indazoles that is 1H-indazole that is substituted at positions 1 and 3 by 2,4-dichlorobenzyl and carboxy groups, respectively.		3.1710dichlorobenzene;
indazoles;
monocarboxylic acid		antineoplastic agent;
antispermatogenic agent;
EC 2.7.1.1 (hexokinase) inhibitor;
geroprotector
vecuronium bromide
Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent;
nicotinic antagonist
vecuronium
vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents.		3.2310acetate ester;
androstane;
quaternary ammonium ion		drug allergen;
muscle relaxant;
neuromuscular agent;
nicotinic antagonist
benoxaprofen
benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals.		3.23101,3-benzoxazoles;
monocarboxylic acid;
monochlorobenzenes		antipsoriatic;
antipyretic;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
hepatotoxic agent;
nephrotoxin;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
protein kinase C agonist
exifone
[no description available]		3.2310benzophenones
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		3.2310[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
nitazoxanide
nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug		3.6120benzamides;
carboxylic ester
sufentanil
Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid.		3.2310anilide;
ether;
piperidines;
thiophenes		anaesthesia adjuvant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
acarbose
[no description available]		3.6120tetrasaccharide derivativeEC 3.2.1.1 (alpha-amylase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
geroprotector;
hypoglycemic agent
torsemide
Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.		6.2831aminopyridine;
N-sulfonylurea;
secondary amino compound		antihypertensive agent;
loop diuretic
epirubicin
Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA.		3.2310aminoglycoside;
anthracycline antibiotic;
anthracycline;
deoxy hexoside;
monosaccharide derivative;
p-quinones;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		antimicrobial agent;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
lorcainide
[no description available]		2.0810acetamides
idarubicin
Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.		3.2310anthracycline antibiotic;
deoxy hexoside;
monosaccharide derivative
piperacillin
Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.		3.6320penicillin allergen;
penicillin		antibacterial drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		3.2310aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		3.8630alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
cefoperazone
Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance.		3.2310cephalosporinantibacterial drug
staurosporine
[no description available]		2.0810indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
foscarnet sodium
trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.0810one-carbon compound;
organic sodium salt		antiviral drug
atracurium
Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups.		3.2310diester;
quaternary ammonium ion		muscle relaxant;
nicotinic antagonist
atracurium besylate
atracurium besylate : The bisbenzenesulfonate salt of atracurium.		2.0810organosulfonate salt;
quaternary ammonium salt		muscle relaxant;
nicotinic antagonist
nicorandil
Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris.		2.0810nitrate ester;
pyridinecarboxamide		potassium channel opener;
vasodilator agent
pergolide
Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		3.2310diamine;
methyl sulfide;
organic heterotetracyclic compound		antiparkinson drug;
dopamine agonist
pergolide mesylate
pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.0810methanesulfonate saltantiparkinson drug;
dopamine agonist;
geroprotector
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.6620acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
cefadroxil anhydrous
Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.6120cephalosporinantibacterial drug
talniflumate
talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma		2.0810benzofurans
fenoldopam mesylate
[no description available]		2.0810benzazepine
fialuridine
[no description available]		3.6920
cefaclor anhydrous
Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.6120cephalosporinantibacterial drug;
drug allergen
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		2.0810fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
alfentanil
Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.		3.2310monocarboxylic acid amide;
piperidines		central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
miglustat
miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group.		3.2310piperidines;
tertiary amino compound		anti-HIV agent;
EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor
haloperidol decanoate
[no description available]		3.2310organic molecular entity
cefotetan
Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms.		3.6120
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		3.6120delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
flupirtine
flupirtine: RN given refers to parent cpd without isomeric designation		2.0810aminopyridine
tolrestat
tolrestat: RN & structure given in first source		3.2310naphthalenesEC 1.1.1.21 (aldehyde reductase) inhibitor
enoximone
Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.		2.0810aromatic ketone
stepronin
[no description available]		2.0810N-acyl-amino acid
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		3.6120delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
idazoxan
Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.		2.0810benzodioxine;
imidazolines		alpha-adrenergic antagonist
remoxipride
Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.		2.0810dimethoxybenzene
balsalazide
balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond.		3.2310
pravastatin
Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		3.23103-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic)		anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic
cabergoline
Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.		3.6120N-acylureaantineoplastic agent;
antiparkinson drug;
dopamine agonist
atomoxetine hydrochloride
Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine.		2.0810hydrochlorideadrenergic uptake inhibitor;
antidepressant
atomoxetine
atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.		3.2310aromatic ether;
secondary amino compound;
toluenes		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
quinapril
Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.		3.6120dicarboxylic acid monoester;
ethyl ester;
isoquinolines;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
alpidem
[no description available]		3.2310imidazoles
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		3.61203-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
fosphenytoin
fosphenytoin: structure given in first & second source		3.2310imidazolidine-2,4-dione
salmeterol xinafoate
Salmeterol Xinafoate: A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.		2.4620naphthoic acid
ranolazine
Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina.		4.3530aromatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		3.61203-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		2.0810imidazoquinolineantineoplastic agent;
interferon inducer
esmolol
methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure.		3.2310aromatic ether;
ethanolamines;
methyl ester;
secondary alcohol;
secondary amino compound
sertindole
sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.		2.0810heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
adapalene
Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.		2.0810adamantanes;
monocarboxylic acid;
naphthoic acid		dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
adefovir
adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection.		3.23106-aminopurines;
ether;
phosphonic acids		antiviral drug;
DNA synthesis inhibitor;
drug metabolite;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent
aromasil
[no description available]		3.612017-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor;
environmental contaminant;
xenobiotic
sparfloxacin
[no description available]		2.0810fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
zileuton
[no description available]		3.61201-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		3.8730methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
cidofovir anhydrous
Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients.		3.6120phosphonic acids;
pyrimidone		anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent
tiagabine
Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy.		3.2310beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes		anticonvulsant;
GABA reuptake inhibitor
topotecan
Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.		3.2310pyranoindolizinoquinolineantineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
bromfenac
bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.		3.6120aromatic amino acid;
benzophenones;
organobromine compound;
substituted aniline		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gemcitabine hydrochloride
[no description available]		2.0810hydrochloride;
organofluorine compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		3.6120organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
ibutilide
ibutilide: RN & structure in first source; RN refers to the fumarate salt		3.2310benzenes;
organic amino compound
aripiprazole
Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.		3.6120aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
remifentanil
Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline.		3.2310alpha-amino acid ester;
anilide;
monocarboxylic acid amide;
piperidinecarboxylate ester		intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
sedative
atorvastatin calcium anhydrous
[no description available]		2.0810organic calcium salt
atorvastatin
[no description available]		3.2310aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
lamivudine
[no description available]		3.6120monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
duloxetine hydrochloride
Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration.		2.0810duloxetine hydrochlorideantidepressant
duloxetine
[no description available]		3.2310duloxetine
irinotecan
[no description available]		3.2310carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		8.9430biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
ibandronic acid
Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS.		3.2310
ziprasidone
ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.		3.23101,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
zolmitriptan
zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.		3.6120oxazolidinone;
tryptamines		anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
3-iodobenzylguanidine
3-Iodobenzylguanidine: A guanidine analog with specific affinity for tissues of the sympathetic nervous system and related tumors. The radiolabeled forms are used as antineoplastic agents and radioactive imaging agents. (Merck Index, 12th ed) MIBG serves as a neuron-blocking agent which has a strong affinity for, and retention in, the adrenal medulla and also inhibits ADP-ribosyltransferase.		3.6411organoiodine compound
simendan
Simendan: A hydrazone and pyridazine derivative; the levo-form is a phosphodiesterase III inhibitor, calcium-sensitizing agent, and inotropic agent that is used in the treatment of HEART FAILURE.		5.1740
adefovir dipivoxil
bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.		2.08106-aminopurines;
carbonate ester;
ether;
organic phosphonate		antiviral drug;
DNA synthesis inhibitor;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		3.6120monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		3.2310biphenyls
tiludronic acid
tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source		3.2310organochlorine compound
relcovaptan
relcovaptan: a nonpeptide vasopressin V1 receptor antagonist; structure given in first source		5.1150proline derivative
tirofiban
Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.		3.2310L-tyrosine derivative;
piperidines;
sulfonamide		anticoagulant;
fibrin modulating drug;
platelet glycoprotein-IIb/IIIa receptor antagonist
capecitabine
Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.		3.2310carbamate ester;
cytidines;
organofluorine compound		antimetabolite;
antineoplastic agent;
prodrug
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		3.6120adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
paroxetine hydrochloride
paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug.		2.0810hydrochlorideantidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
bupropion hydrochloride
[no description available]		2.0810aromatic ketone
venlafaxine hydrochloride
Venlafaxine Hydrochloride: A cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT.		2.0710hydrochloride
trazodone hydrochloride
Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.		2.0810hydrochlorideadrenergic antagonist;
antidepressant;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
trovafloxacin
trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure.		3.2310
cefprozil
[no description available]		3.2310cephalosporin;
semisynthetic derivative		antibacterial drug
doxazosin mesylate
Cardura: Trade name in United States.		2.0810methanesulfonate saltgeroprotector
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		3.6120acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		3.6120aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
rolofylline
rolofylline: selective antagonist for adenosine receptors; a cardiovascular agent		8.1443oxopurine
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		2.2110D-glucopyranoseepitope;
mouse metabolite
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2.08102-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
bupivacaine hydrochloride
bupivacaine hydrochloride (anhydrous) : A racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride : A hydrochloride obtained by combining 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide with one molar equivalent of hydrochloric acid.		2.0810hydrochloride;
racemate		adrenergic antagonist;
amphiphile;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
local anaesthetic
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		3.2310aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		3.8730azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
amprenavir
[no description available]		3.6120carbamate ester;
sulfonamide;
tetrahydrofuryl ester		antiviral drug;
HIV protease inhibitor
oseltamivir
Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.		3.2310acetamides;
amino acid ester;
cyclohexenecarboxylate ester;
primary amino compound		antiviral drug;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
environmental contaminant;
prodrug;
xenobiotic
ticlopidine hydrochloride
[no description available]		2.0810hydrochloride
epirubicin hydrochloride
[no description available]		2.0810
histamine phosphate
histamine phosphate : A phosphate salt that is the diphosphate salt of histamine.		3.2310phosphate salthistamine agonist
tilbroquinol
[no description available]		3.2310organohalogen compound;
quinolines
bendamustine
[no description available]		3.2310benzimidazoles
droxicam
droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.		3.2310organic heterotricyclic compound;
pyridines		cyclooxygenase 1 inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
prodrug
milnacipran
Milnacipran: A cyclopropanecarboxamide serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of FIBROMYALGIA.		2.0510acetamides
ebrotidine
ebrotidine: an H2-receptor antagonist and gastric mucosa protector		3.2310sulfonamide
pazufloxacin
[no description available]		2.0810quinolines
repaglinide
[no description available]		3.6120piperidines
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		3.6120benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.49201,2,3-triazole
miconazole nitrate
miconazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-miconazole nitrate. An antifungal used for the treatment of athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.		2.0810
sertraline
Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		3.2310dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor
zoledronic acid
Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.		3.61201,1-bis(phosphonic acid);
imidazoles		bone density conservation agent
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
brinzolamide
brinzolamide: an antiglaucoma agent		2.0810sulfonamide;
thienothiazine		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
drospirenone
drospirenone: a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source		2.08103-oxo-Delta(4) steroid;
steroid lactone		aldosterone antagonist;
contraceptive drug;
progestin
artemether
Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810artemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid		antimalarial
acamprosate
Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3.		3.2310acetamides;
organosulfonic acid		environmental contaminant;
neurotransmitter agent;
xenobiotic
isaxonine
isaxonine: promotes nerve growth		3.2310aminopyrimidine
nebivolol
2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group.		3.2310chromanes;
diol;
organofluorine compound;
secondary alcohol;
secondary amino compound
uk 68798
[no description available]		3.6120aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
hp 873
iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.		3.61201,2-benzoxazoles;
aromatic ether;
aromatic ketone;
methyl ketone;
monoamine;
organofluorine compound;
piperidines;
tertiary amino compound		dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist
dexrazoxane
Dexrazoxane: The (+)-enantiomorph of razoxane.		3.2310razoxaneantineoplastic agent;
cardiovascular drug;
chelator;
immunosuppressive agent
loxapine succinate
[no description available]		2.0810succinate saltgeroprotector
fenoxypropazine
[no description available]		3.2310aromatic ether
voriconazole
Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.		3.6120conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug		P450 inhibitor
betamipron
[no description available]		2.0810organonitrogen compound;
organooxygen compound
uroxatral
[no description available]		2.0810hydrochloride
aceclofenac
[no description available]		3.6120amino acid;
carboxylic ester;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
nitrefazole
[no description available]		3.2310imidazoles
thiocolchicoside
[no description available]		2.0810glycoside
doripenem
Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.		3.6120carbapenems
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		3.2310hydroxy-1,2-naphthoquinone
rivastigmine
[no description available]		3.2310carbamate ester;
tertiary amino compound		cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent
frovatriptan
[no description available]		3.2310carbazoles
eletriptan
eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.		3.2310indoles;
N-alkylpyrrolidine;
sulfone		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rosiglitazone
[no description available]		3.8730aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
tamiflu
[no description available]		2.0810phosphate salt
bexarotene
[no description available]		3.6120benzoic acids;
naphthalenes;
retinoid		antineoplastic agent
s20098
[no description available]		2.0810acetamides
flunisolide
flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones		2.081011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
primary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug;
immunosuppressive agent
ketorolac tromethamine
Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.		2.0810organoammonium saltanalgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor
clarithromycin
Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.		3.6120macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
cholest-5-ene-3,4-diol
cholest-5-ene-3,4-diol: RN given refers to (3beta,4beta)-isomer		2.2510
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.08103-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
moexipril
[no description available]		3.2310peptide
gliquidone
gliquidone: structure; RN given refers to parent cpd		2.0810isoquinolines
mci 9038
[no description available]		3.2310peptide
lopinavir
[no description available]		2.0810amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
moxifloxacin hydrochloride
moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride.		2.0810hydrochlorideantibacterial drug
fulvestrant
Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.		3.612017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
mizoribine
[no description available]		2.0810imidazolesanticoronaviral agent
sr141716
[no description available]		2.4520amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
bosentan anhydrous
Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.		4.3930primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
racecadotril
racecadotril: parenterally active enkephalinase inhibitor		2.0810N-acyl-amino acid
perindopril
Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline		3.2310alpha-amino acid ester;
dicarboxylic acid monoester;
ethyl ester;
organic heterobicyclic compound		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
benzamil
[no description available]		2.0610guanidines;
pyrazines
tadalafil
[no description available]		3.6120benzodioxoles;
pyrazinopyridoindole		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
opc 21268
OPC 21268: structure given in first source; vasopressin V1 receptor antagonist		2.4420
paliperidone
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia.		3.23101,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol
nitisinone
[no description available]		3.2310(trifluoromethyl)benzenes;
C-nitro compound;
cyclohexanones;
mesotrione		EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor
plavix
[no description available]		2.0810azaheterocycle sulfate salt;
organoammonium sulfate salt		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
clofarabine
[no description available]		3.6120adenosines;
organofluorine compound		antimetabolite;
antineoplastic agent
mozavaptan
mozavaptan: aquaretic agent; vasopressin V2 receptor antagonist; structure given in first source		11.47120benzamidesaquaretic
pramipexole
Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.		3.6120benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
valdecoxib
[no description available]		3.6120isoxazoles;
sulfonamide		antipyretic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
almotriptan
almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.		3.2310indoles;
sulfonamide;
tertiary amine		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
mk 0663
[no description available]		2.0810bipyridines;
organochlorine compound;
sulfone		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
gefitinib
[no description available]		3.6120aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
desloratadine
desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.		3.6120benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
desvenlafaxine
O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine.		3.2310cyclohexanols;
phenols;
tertiary amino compound		antidepressant;
drug metabolite;
marine xenobiotic metabolite
methotrexate
[no description available]		3.6120dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
tamsulosin
[no description available]		3.23105-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent
rufinamide
rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source		3.5920aromatic amide;
heteroarene
sulbactam
[no description available]		2.0810penicillanic acids
olmesartan medoxomil
Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.		3.6120biphenyls
dexpanthenol
dexpanthenol: The alcohol of pantothenic acid		3.2310amino alcohol;
monocarboxylic acid amide		cholinergic drug;
provitamin
fosamprenavir
fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir.		3.2310sulfonamideprodrug
omega-n-methylarginine
omega-N-Methylarginine: A competitive inhibitor of nitric oxide synthetase.. N(omega)-methyl-L-arginine : A L-arginine derivative with a N(omega)-methyl substituent.		5.3922amino acid zwitterion;
arginine derivative;
guanidines;
L-arginine derivative;
non-proteinogenic L-alpha-amino acid
abiraterone
[no description available]		2.08103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines		antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
febuxostat
Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout.		3.87301,3-thiazolemonocarboxylic acid;
aromatic ether;
nitrile		EC 1.17.3.2 (xanthine oxidase) inhibitor
escitalopram
Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram.		3.23101-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrileantidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
lexapro
Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram.		2.0810
10-propargyl-10-deazaaminopterin
10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.		3.2310N-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		3.6120secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
atazanavir
atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).		3.2310carbohydrazideantiviral drug;
HIV protease inhibitor
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		3.61209-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		3.6120azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
ertapenem
Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.		3.2310carbapenemcarboxylic acid;
pyrrolidinecarboxamide		antibacterial drug
cox 189
lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity.		3.6120amino acid;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
secondary amino compound		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
conivaptan
conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH).		16.32560benzazepineaquaretic;
vasopressin receptor antagonist
tezosentan
tezosentan: structure in first source		4.6830
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.2310aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
pralnacasan
pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source		3.2310
clevidipine
clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source		3.2310dihydropyridine
solifenacin
[no description available]		3.2310isoquinolines
dexmethylphenidate
dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate.		3.2310methyl phenyl(piperidin-2-yl)acetateadrenergic agent
xamoterol
Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.		2.0810morpholines
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		3.6120methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
cinacalcet
cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.		3.2310(trifluoromethyl)benzenes;
naphthalenes;
secondary amino compound		calcimimetic;
P450 inhibitor
lubiprostone
[no description available]		3.2310
satavaptan
satavaptan: a vasopressin V2 receptor antagonist; structure given in first source		16.88192
telbivudine
[no description available]		3.6120pyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		3.17102,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
paromomycin
Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis.		3.2310amino cyclitol glycoside;
aminoglycoside antibiotic		anthelminthic drug;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
anidulafungin
Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis.		3.2310antibiotic antifungal drug;
azamacrocycle;
echinocandin;
heterodetic cyclic peptide;
semisynthetic derivative
17 alpha-hydroxyprogesterone caproate
17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS.		3.2310corticosteroid hormone
varenicline
Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.		3.2310
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		8.6320amino acid zwitterion;
angiotensin II		human metabolite
fiduxosin
fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source		3.2310
lixivaptan
[no description available]		15.76330
atropine
tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.		3.6120
erlotinib
[no description available]		3.2310aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
oxytocin, asp(5)-
[no description available]		2.110
etravirine
[no description available]		3.2310aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
dronedarone
Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias.		3.23101-benzofurans;
aromatic ether;
aromatic ketone;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
environmental contaminant;
xenobiotic
ramelteon
ramelteon: melatonin MT1/MT2 receptor agonist		3.6120indanes
lapatinib
[no description available]		3.2310furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
darunavir
Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.		3.2310carbamate ester;
furofuran;
sulfonamide		antiviral drug;
HIV protease inhibitor
deferasirox
Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions.		3.6120benzoic acids;
monocarboxylic acid;
phenols;
triazoles		iron chelator
bms204352
BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source		2.0810
tbc-11251
sitaxsentan: endothelin A receptor antagonist; structure in first source		3.6120benzodioxoles
sorafenib
[no description available]		3.5920(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
succinobucol
succinobucol: monosuccinic acid ester of probucol; a metabolically stable modification of probucol, an equipotent antioxidant to probucol but is pharmacologically distinct		2.0310benzoate ester;
phenols
lenalidomide
[no description available]		3.6120aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
regadenoson
[no description available]		3.2310purine nucleoside
lacosamide
Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES.		3.8730N-acyl-amino acid
vincaleukoblastine
[no description available]		3.6120acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
vincristine sulfate
[no description available]		2.0810organic sulfate saltantineoplastic agent;
geroprotector
benzarone
benzarone: antihemorrhagic agent; structure		3.23101-benzofurans
estramustine
Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.		3.231017beta-hydroxy steroid;
carbamate ester;
organochlorine compound		alkylating agent;
antineoplastic agent;
radiation protective agent
wortmannin
[no description available]		2.0810acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
bortezomib
[no description available]		3.6120amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		3.61201,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		3.930heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
pentostatin
Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.		3.6120coformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		3.6120cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		3.6120alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
griseofulvin
Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment.		3.23101-benzofurans;
antibiotic antifungal drug;
benzofuran antifungal drug;
organochlorine compound;
oxaspiro compound		antibacterial agent;
Penicillium metabolite
cefoxitin
Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
cephamycin;
semisynthetic derivative		antibacterial drug
digitoxin
Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain.		2.0810cardenolide glycosideEC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		3.6120L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
pancuronium
Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant.		3.2310acetate ester;
steroid ester		cholinergic antagonist;
muscle relaxant;
nicotinic antagonist
abacavir
abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection.		3.23102,6-diaminopurinesantiviral drug;
drug allergen;
HIV-1 reverse transcriptase inhibitor
perindopril erbumine
[no description available]		2.0810addition compoundantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
miglitol
[no description available]		3.6120piperidines
metyrosine
alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma.		3.2310L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		antihypertensive agent;
EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor
rocuronium bromide
rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent
linezolid
[no description available]		3.6120acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
bq 123
cyclo(Trp-Asp-Pro-Val-Leu): derived from the modification of a natural lead of BE-18257B, an endothelin A receptor antagonist; has neuroprotective activity; amino acid sequence given in first source		3.1510cyclic peptide
clindamycin phosphate
[no description available]		3.2310
pemirolast potassium salt
[no description available]		2.0810
eplerenone
Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.		3.61203-oxo-Delta(4) steroid;
epoxy steroid;
gamma-lactone;
methyl ester;
organic heteropentacyclic compound;
oxaspiro compound;
steroid acid ester		aldosterone antagonist;
antihypertensive agent
tolterodine
[no description available]		3.2310tertiary amineantispasmodic drug;
muscarinic antagonist;
muscle relaxant
ao 128
AO 128: alpha-glucosidase inhibitor; structure given in first source		2.0810organic molecular entity
loteprednol etabonate
Loteprednol Etabonate: An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
etabonate ester;
organochlorine compound;
steroid acid ester;
steroid ester		anti-inflammatory drug
darifenacin
darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.		3.23101-benzofurans;
monocarboxylic acid amide;
pyrrolidines		antispasmodic drug;
muscarinic antagonist
fluticasone propionate
fluticasone propionate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
propanoate ester;
steroid ester;
thioester		adrenergic agent;
anti-allergic agent;
anti-asthmatic drug;
anti-inflammatory drug;
bronchodilator agent;
dermatologic drug
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		3.6120retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
retinol
Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).		3.2310retinol;
vitamin A		human metabolite;
mouse metabolite;
plant metabolite
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		3.8630macrolide lactambacterial metabolite;
immunosuppressive agent
rosuvastatin
rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer).		3.2310dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrimidines;
statin (synthetic);
sulfonamide		anti-inflammatory agent;
antilipemic drug;
cardioprotective agent;
CETP inhibitor;
environmental contaminant;
xenobiotic
mycophenolic acid
Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.		3.23102-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols		anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
mupirocin
Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.		2.0810alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor
clindamycin
Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.		3.2310
fosfomycin
Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus.		3.2310epoxide;
phosphonic acids		antimicrobial agent;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		3.6120macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
octreotide
[no description available]		3.2310
eptifibatide
[no description available]		3.2310homodetic cyclic peptide;
macrocycle;
organic disulfide		anticoagulant;
platelet aggregation inhibitor
decitabine
[no description available]		3.61202'-deoxyribonucleoside
teniposide
[no description available]		3.6120aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
valrubicin
[no description available]		2.0810anthracycline;
trifluoroacetamide
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		3.2310actinomycinmutagen
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		3.6120L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		3.2310nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
posaconazole
[no description available]		3.6120aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
rubitecan
rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.		2.0810C-nitro compound;
delta-lactone;
pyranoindolizinoquinoline;
semisynthetic derivative;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
micafungin
Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy.		3.2310antibiotic antifungal drug;
echinocandin		antiinfective agent
riboflavin
vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms).		3.2310flavin;
vitamin B2		anti-inflammatory agent;
antioxidant;
cofactor;
Escherichia coli metabolite;
food colouring;
fundamental metabolite;
human urinary metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite
sodium bicarbonate
Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.		3.2310one-carbon compound;
organic sodium salt		antacid;
food anticaking agent
arsenic trioxide
Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius.		3.2310arsenic oxideantineoplastic agent;
insecticide
sr 90107
fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux.		3.2310
meglumine iodipamide
[no description available]		3.2310organoammonium saltradioopaque medium
thyrotropin-releasing hormone
PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence.		3.2310peptide hormone;
tripeptide		human metabolite
arginine vasopressin
Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.		14.59638vasopressincardiovascular drug;
hematologic agent;
mitogen
s 1033
[no description available]		3.2310(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
trilostane
trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions.		2.081017beta-hydroxy steroid;
3-hydroxy steroid;
androstanoid;
epoxy steroid;
nitrile		abortifacient;
antineoplastic agent;
EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor
leuprolide acetate
leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0810acetate saltantineoplastic agent;
gonadotropin releasing hormone agonist
propylthiouracil
Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.		3.6120pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
etomidate
Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.		3.2310ethyl ester;
imidazoles		intravenous anaesthetic;
sedative
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		3.6120aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
levosulpiride
(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).		2.0810sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
pyrantel
Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'.		3.23101,4,5,6-tetrahydropyrimidines;
carboxamidine;
thiophenes		antinematodal drug
thiothixene
[no description available]		3.2310N-methylpiperazineanticoronaviral agent
eszopiclone
Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use.		3.6120zopiclonecentral nervous system depressant;
sedative
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		3.1710aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
benztropine
Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		3.2310diarylmethane
methimazole
Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen.		3.61201,3-dihydroimidazole-2-thionesantithyroid drug
cinnarizine
Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.		2.0810diarylmethane;
N-alkylpiperazine;
olefinic compound		anti-allergic agent;
antiemetic;
calcium channel blocker;
geroprotector;
H1-receptor antagonist;
histamine antagonist;
muscarinic antagonist
sulindac
Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.		3.6120monocarboxylic acid;
organofluorine compound;
sulfoxide		analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
terbinafine
[no description available]		3.2310acetylenic compound;
allylamine antifungal drug;
enyne;
naphthalenes;
tertiary amine		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor;
sterol biosynthesis inhibitor
epalrestat
epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.		2.0810monocarboxylic acid;
thiazolidines		EC 1.1.1.21 (aldehyde reductase) inhibitor
drotaverin
drotaverin: Hungarian drug; RN given refers to parent cpd; structure		2.0810isoquinolines
thioguanine anhydrous
Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.		3.23102-aminopurinesanticoronaviral agent;
antimetabolite;
antineoplastic agent
D-fructopyranose
[no description available]		2.2110cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
succimer
Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning.		3.2310dicarboxylic acid;
dithiol;
sulfur-containing carboxylic acid		chelator
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		10.8232cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
streptozocin
[no description available]		3.2310
tamoxifen
[no description available]		3.6120stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		3.2310pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
cancidas
[no description available]		3.2310
fusidic acid
Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.		2.081011alpha-hydroxy steroid;
3alpha-hydroxy steroid;
alpha,beta-unsaturated monocarboxylic acid;
steroid acid;
steroid antibiotic;
sterol ester		EC 2.7.1.33 (pantothenate kinase) inhibitor;
Escherichia coli metabolite;
protein synthesis inhibitor
lincomycin
Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis.		3.2310carbohydrate-containing antibiotic;
L-proline derivative;
monocarboxylic acid amide;
pyrrolidinecarboxamide;
S-glycosyl compound		antimicrobial agent;
bacterial metabolite
valinomycin
Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains.		2.0810cyclodepsipeptide;
macrocycle		antimicrobial agent;
antiviral agent;
bacterial metabolite;
potassium ionophore
ranitidine
Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease.		3.2310C-nitro compound;
furans;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
drug allergen;
environmental contaminant;
H2-receptor antagonist;
xenobiotic
aplaviroc
aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source		3.2310
hmr 3647
[no description available]		3.6120
latoconazole
latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source		2.0810conazole antifungal drug;
imidazole antifungal drug
maraviroc
[no description available]		3.6120tropane alkaloid
toremifene citrate
[no description available]		2.0810stilbenoidanticoronaviral agent
toremifene
Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.		3.2310aromatic ether;
organochlorine compound;
tertiary amine		antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
nelarabine
nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G).		3.6120beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside		antineoplastic agent;
DNA synthesis inhibitor;
prodrug
lithium
Lithium: An element in the alkali metals family. It has the atomic symbol Li, atomic number 3, and atomic weight [6.938; 6.997]. Salts of lithium are used in treating BIPOLAR DISORDER.		4.120alkali metal atom
dermatan sulfate
Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units.		3.2310amino disaccharide;
glycosylgalactose derivative;
iduronic acids;
oligosaccharide sulfate
dolasetron
[no description available]		3.2310indolyl carboxylic acid
gestodene
Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer		2.0810steroidestrogen
orlistat
Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.		3.6120beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative		anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor
quinine
[no description available]		3.6120cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
cystine
[no description available]		7.3110
fospropofol
[no description available]		3.2310alkylbenzene
azilect
[no description available]		2.0810
rasagiline
[no description available]		3.2310indanes;
secondary amine;
terminal acetylenic compound		EC 1.4.3.4 (monoamine oxidase) inhibitor;
neuroprotective agent
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		8.93301,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		3.6120triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		3.61202-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
quercetin
[no description available]		2.08107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
bilirubin
[no description available]		4.9421biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		3.0120prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		3.6120D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
alprostadil
[no description available]		2.0810prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
vitamin d 2
Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa.		3.6120hydroxy seco-steroid;
seco-ergostane;
vitamin D		bone density conservation agent;
nutraceutical;
plant metabolite;
rodenticide
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		3.2310antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
pulmicort
Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.		3.612011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen
oxymetholone
Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects.		3.6120
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		3.6120dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
montelukast
montelukast: a leukotriene D4 receptor antagonist		3.2310aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
mivacurium
Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent.		3.2310isoquinolines
brompheniramine maleate
brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810maleate saltanti-allergic agent
dexchlorpheniramine maleate
[no description available]		2.0810organic molecular entity
hemabate
carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy.		3.2310
mycophenolate mofetil
mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.		3.6120carboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound		anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug
entacapone
entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.		3.61202-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
paricalcitol
[no description available]		3.2310hydroxy seco-steroid;
seco-cholestane		antiparathyroid drug
l 660,711
[no description available]		2.0810quinolines
travoprost
Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.		2.0810(trifluoromethyl)benzenes;
isopropyl ester;
prostaglandins Falpha		antiglaucoma drug;
antihypertensive agent;
ophthalmology drug;
prodrug;
prostaglandin receptor agonist
tranilast
tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.		2.0810amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide		anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
7432 s
Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections.		3.2310cephalosporin;
dicarboxylic acid		antibacterial drug
imipenem
[no description available]		2.0810carbapenems
etretinate
retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.		2.0810enoate ester;
ethyl ester;
retinoid		keratolytic drug
isotretinoin
Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases.		3.6120retinoic acidantineoplastic agent;
keratolytic drug;
teratogenic agent
ketotifen fumarate
ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.		2.0810organoammonium saltanti-asthmatic drug;
H1-receptor antagonist
epoprostenol
[no description available]		3.2310prostaglandins Imouse metabolite
indocyanine green
[no description available]		3.23101,1-diunsubstituted alkanesulfonate;
benzoindole;
cyanine dye
dinoprost tromethamine
[no description available]		2.0810organic molecular entity
triprolidine
Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders.		3.2310N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
pitavastatin
pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.		3.2310cyclopropanes;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
quinolines;
statin (synthetic)		antioxidant
rosuvastatin calcium
S 4522: structure in first source		2.0810N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine;
organic calcium salt		anti-inflammatory agent;
cardioprotective agent;
CETP inhibitor
terbinafine hydrochloride
terbinafine hydrochloride : A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride.		2.0810allylamine antifungal drug;
hydrochloride		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor
ethamolin
monoethanolamine oleate: used for treatment of pyogenic granuloma		3.2310long-chain fatty acid
alatrofloxacin mesylate
[no description available]		3.2310
codeine
[no description available]		3.2310morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		3.6120homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
natamycin
[no description available]		2.0810antibiotic antifungal drug;
dicarboxylic acid monoester;
epoxide;
macrolide antibiotic;
monosaccharide derivative;
polyene antibiotic		antifungal agrochemical;
antimicrobial food preservative;
apoptosis inducer;
bacterial metabolite;
ophthalmology drug
acitretin
Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9.		3.6120acitretin;
alpha,beta-unsaturated monocarboxylic acid;
retinoid		keratolytic drug
estropipate
estropipate: used therapeutically in menopausal patients		3.2310piperazinium salt;
steroid sulfate
hydromorphone
Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class.		3.2310morphinane alkaloid;
organic heteropentacyclic compound		mu-opioid receptor agonist;
opioid analgesic
levetiracetam
Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine.		8.930pyrrolidin-2-onesanticonvulsant;
environmental contaminant;
xenobiotic
ly 163892
loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.		3.2310carbacephem;
zwitterion		antibacterial drug;
antimicrobial agent
nabilone
nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure		3.2310
nalmefene
nalmefene: RN given refers to 5-alpha isomer		2.0810morphinane alkaloid
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		3.6120morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
oxycodone
Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain.		3.2310organic heteropentacyclic compound;
semisynthetic derivative		antitussive;
mu-opioid receptor agonist;
opioid analgesic
oxymorphone
Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)		3.2310morphinane alkaloid
vitamin k 1
Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones.		3.2310phylloquinones;
vitamin K		cofactor;
human metabolite;
plant metabolite
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		5.4270antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		3.6120cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
trospium chloride
trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder.		3.2310
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		3.2310morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
demycarosylturimycin h
[no description available]		2.0810
acipimox
acipimox: lipolysis inhibitor		2.0810pyrazinecarboxylic acid
atosiban
[no description available]		2.0810oligopeptide
benzphetamine
Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity.		3.2310amphetamines;
tertiary amine		adrenergic uptake inhibitor;
appetite depressant;
dopamine uptake inhibitor;
sympathomimetic agent
bimatoprost
Bimatoprost: A cloprostenol-derived amide that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.		2.0810monocarboxylic acid amideantiglaucoma drug;
antihypertensive agent
deamino arginine vasopressin
Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR.		8.0891heterodetic cyclic peptidediagnostic agent;
renal agent;
vasopressin receptor agonist
dexmedetomidine
[no description available]		3.2310medetomidinealpha-adrenergic agonist;
analgesic;
non-narcotic analgesic;
sedative
goserelin
Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer.		3.2310organic molecular entity
latanoprost
Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.		2.0810isopropyl ester;
prostaglandins Falpha;
triol		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
nalbuphine
Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.		3.2310organic heteropentacyclic compoundmu-opioid receptor antagonist;
opioid analgesic
nateglinide
Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.		3.6120phenylalanine derivative
vinorelbine
[no description available]		3.2310acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
silodosin
silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source		3.5920indolecarboxamide
fluvoxamine
Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder.		3.2310(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
serotonin uptake inhibitor
bosutinib
4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source		3.1710aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
su 11248
[no description available]		3.2310monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.		3.6120dihydroxy monocarboxylic acid;
indoles;
organofluorine compound
molsidomine
[no description available]		2.0810ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
levorphanol
Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.		3.2310morphinane alkaloid
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		3.2310cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
dextromethorphan
Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.		3.23106-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
butorphanol
Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.		3.6120morphinane alkaloidantitussive;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
cefixime
[no description available]		3.6120cephalosporinantibacterial drug;
drug allergen
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		3.6120dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
benazepril
benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.		3.2310benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		3.6120azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
verteporfin
(2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid.		3.2310
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		3.6120dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
zimeldine
Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385)		3.2310styrenes
enalapril maleate
enalapril maleate : The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.		2.0810maleate saltantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		3.2310dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
trientine hydrochloride
[no description available]		3.2310
n-methylscopolamine bromide
scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide.		3.2310
fumarates
Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)		3.8430butenedioate;
C4-dicarboxylate		human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
bleomycin
[no description available]		3.2310bleomycinantineoplastic agent;
metabolite
enalaprilat anhydrous
Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.		3.6120dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ximelagatran
ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.		3.2310amidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide		anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor
cefuroxime
[no description available]		3.23103-(carbamoyloxymethyl)cephalosporin;
furans;
oxime O-ether		drug allergen
ceftriaxone
[no description available]		3.23101,2,4-triazines;
1,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 3.5.2.6 (beta-lactamase) inhibitor
cefepime
Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.2310cephalosporin;
oxime O-ether		antibacterial drug
pafuramidine
pafuramidine: a prodrug of furamidine		3.2310
ceftazidime
[no description available]		3.2310cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
trandolapril
trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.		3.6120dicarboxylic acid monoester;
dipeptide;
ethyl ester;
organic heterobicyclic compound;
secondary amino compound;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
pregabalin
Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.		3.6120gamma-amino acidanticonvulsant;
calcium channel blocker
alvimopan anhydrous
alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain		3.6120peptide
aliskiren
aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.		4.5940monocarboxylic acid amide;
monomethoxybenzene		antihypertensive agent
famotidine
[no description available]		3.61201,3-thiazoles;
guanidines;
sulfonamide		anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
cefotaxime
Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.		3.23101,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen
aztreonam
[no description available]		3.2310beta-lactam antibiotic allergen;
monobactam		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
cci 15641
[no description available]		2.0810cephalosporin
cefpodoxime
[no description available]		3.2310carboxylic acid;
cephalosporin		antibacterial drug
palonosetron
Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.		3.2310azabicycloalkane;
delta-lactam;
organic heterotricyclic compound		antiemetic;
serotonergic antagonist
tenofovir disoproxil fumarate
tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.		2.0810fumarate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
dexbrompheniramine maleate
dexbrompheniramine maleate : The maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810brompheniramine maleateanti-allergic agent;
H1-receptor antagonist
rifaximin
[no description available]		3.6120acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterohexacyclic compound;
rifamycins;
semisynthetic derivative		antimicrobial agent;
gastrointestinal drug;
orphan drug
everolimus
[no description available]		4.6140cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
ixabepilone
[no description available]		3.23101,3-thiazoles;
beta-hydroxy ketone;
epoxide;
lactam;
macrocycle		antineoplastic agent;
microtubule-destabilising agent
cgp-56697
Artemether, Lumefantrine Drug Combination: Drug combination of artemether and lumefantrine that is used to treat PLASMODIUM FALCIPARUM MALARIA.		2.0510
cefpodoxime proxetil
cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.		2.0810carboxylic acid;
carboxylic ester;
cephalosporin		antibacterial drug;
prodrug
ceftizoxime
[no description available]		3.2310cephalosporinantibacterial drug
1-methyl-d-lysergic acid butanolamide
[no description available]		3.2310ergot alkaloid;
monocarboxylic acid amide		serotonergic antagonist;
sympatholytic agent;
vasoconstrictor agent
fluphenazine
[no description available]		2.0810
nitrofurantoin
Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA.		3.6120imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
dantrolene
[no description available]		3.2310
roxithromycin
(E)-roxithromycin : A major geometrical isomer of roxithromycin.		2.0810roxithromycinenvironmental contaminant;
xenobiotic
cefdinir
[no description available]		3.6120cephalosporin;
ketoxime		antibacterial drug
etonogestrel
[no description available]		3.231017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin
bisoprolol, fumarate (1:1) salt
[no description available]		2.0810
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		2.0810artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
etoposide phosphate
[no description available]		2.0810furonaphthodioxole
ciclesonide
ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis		2.0810organic molecular entity
temsirolimus
[no description available]		3.6120macrolide lactam
dutasteride
Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.		3.6120(trifluoromethyl)benzenes;
aza-steroid;
delta-lactam		antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
tekturna
[no description available]		2.0810fumarate saltantihypertensive agent
lu 208075
ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension		3.2310diarylmethane
bibx 1382bs
BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001		3.2310substituted aniline
vildagliptin
[no description available]		2.0810amino acid amide
fesoterodine
fesoterodine: a muscarinic antagonist for treatment of overactive bladder		3.5920diarylmethane
sgd 301-76
[no description available]		2.0810conazole antifungal drug;
imidazole antifungal drug;
organic nitrate salt		antiinfective agent
fluvoxamine maleate
[no description available]		2.0810(trifluoromethyl)benzenes
thioacetazone
Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives.		2.0810
gemifloxacin
Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position.		3.23101,8-naphthyridine derivative;
fluoroquinolone antibiotic;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
topoisomerase IV inhibitor
dexlansoprazole
Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE.		3.6120benzimidazoles;
sulfoxide
gemifloxacin mesylate
gemifloxacin mesylate : The mesylate salt of gemifloxacin.		2.0810methanesulfonate saltantimicrobial agent;
topoisomerase IV inhibitor
fosinopril
[no description available]		3.2310
armodafinil
armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.		3.23102-[(diphenylmethyl)sulfinyl]acetamidecentral nervous system stimulant;
eugeroic
amoxicillin-potassium clavulanate combination
Amoxicillin-Potassium Clavulanate Combination: A fixed-ratio combination of amoxicillin trihydrate and potassium clavulanate.		2.2110
sincalide
Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.		3.2310oligopeptide
vasopressin, 1-(1-mercaptocyclohexaneacetic acid)-2-(o- methyl-l-tyrosine)-8-l-arginine-
vasopressin, 1-(1-mercaptocyclohexaneacetic acid)-2-(O- methyl-L-tyrosine)-8-L-arginine-: highly potent antagonist of vasopressor response to arginine-vasopressin; structure in first source		2.0310
tapentadol
Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.		3.5920alkylbenzene
pentagastrin
Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.		3.2310organic molecular entity
cefditoren
cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections.		3.2310carboxylic acid;
cephalosporin		antibacterial drug
ticagrelor
Ticagrelor: An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION.. ticagrelor : A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.		2.110aryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines		P2Y12 receptor antagonist;
platelet aggregation inhibitor
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		2.0810aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
dapagliflozin
[no description available]		7.2110aromatic ether;
C-glycosyl compound;
monochlorobenzenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
hki 272
[no description available]		2.0810nitrile;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		2.0810N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
pasireotide
pasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease.		7.1110homodetic cyclic peptide;
peptide hormone		antineoplastic agent
pazopanib
pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.		3.6120aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
prasugrel hydrochloride
Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels.		3.2310
besifloxacin
[no description available]		2.0510quinolines
bibw 2992
[no description available]		2.1710aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
amg 009
AMG 009: an anti-inflammatory agent; structure in first source		2.5520
isotocin
isotocin: hormone found in some teleosts; Gln in position 4 of oxytocin replaced by Ser & Leu in position 8 by Ile; structure		2.1110
cefotaxime sodium
[no description available]		2.0810organic sodium salt
baci-im
[no description available]		3.2310homodetic cyclic peptide;
polypeptide;
zwitterion		antibacterial agent;
antimicrobial agent
bms 477118
[no description available]		3.2310adamantanes;
azabicycloalkane;
monocarboxylic acid amide;
nitrile;
tertiary alcohol		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
nystatin a1
Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.		3.2310nystatins
milnacipran
[no description available]		3.2310acetamides
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		2.7430
d-arg-dmt-lys-phe-nh2
[no description available]		2.4110
scopolamine hydrobromide
[no description available]		3.2310
dactolisib
dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.		2.0810imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
pituitrin
Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR).		14.42619
arabinofuranosyluracil
Arabinofuranosyluracil: A pyrimidine nucleoside formed in the body by the deamination of CYTARABINE.		2.3110
rabeprazole sodium
[no description available]		2.0810organic sodium salt
bivalirudin
bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.		3.8630polypeptideanticoagulant;
EC 3.4.21.5 (thrombin) inhibitor
somatostatin
[no description available]		2.0810heterodetic cyclic peptide;
peptide hormone
atrial natriuretic factor
Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.		6.5953polypeptide
enfuvirtide
Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes.		3.2310
ganirelix
[no description available]		3.2310polypeptide
teriparatide
[no description available]		3.2310polypeptide
salmon calcitonin
[no description available]		3.2310heterodetic cyclic peptide;
peptide hormone;
polypeptide		bone density conservation agent;
metabolite
ly-146032
[no description available]		3.6120heterodetic cyclic peptide;
lipopeptide antibiotic;
lipopeptide;
macrocycle;
macrolide		antibacterial drug;
bacterial metabolite;
calcium-dependent antibiotics
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt		3.5920polypeptide
exenatide
[no description available]		3.2310
warfarin sodium
warfarin sodium : A racemate comprising equal amounts of (R)- and (S)-warfarin sodium. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.		2.0810
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		3.1510
pravastatin sodium
pravastatin sodium : An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.0810organic sodium salt;
statin (semi-synthetic)		anticholesteremic drug
alendronate sodium
[no description available]		2.0810
sl 80.0750
[no description available]		2.0810
mesna
Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE.		3.6120organosulfonic acid
clavulanate potassium
potassium clavulanate : A potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases.		2.0810potassium saltantibacterial drug;
antimicrobial agent;
EC 3.5.2.6 (beta-lactamase) inhibitor
sodium lactate
Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion.		3.2310lactate salt;
organic sodium salt		food acidity regulator;
food preservative
piperacillin sodium
[no description available]		2.0810organic sodium salt
sodium iothalamate
[no description available]		3.2310
oxacillin sodium
[no description available]		2.0810organic sodium salt
cefazolin sodium
cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.		2.0810organic sodium salt
azlocillin sodium
[no description available]		2.0810organic sodium salt
piperacillin, tazobactam drug combination
Piperacillin, Tazobactam Drug Combination: An antibiotic combination product of piperacillin and tazobactam, a penicillanic acid derivative with enhanced beta-lactamase inhibitory activity, that is used for the intravenous treatment of intra-abdominal, pelvic, and skin infections and for community-acquired pneumonia of moderate severity. It is also used for the treatment of PSEUDOMONAS AERUGINOSA INFECTIONS.		2.1310
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		121811
cetrorelix
cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.		3.2310oligopeptideantineoplastic agent;
GnRH antagonist
piperidines
Piperidines: A family of hexahydropyridines.		2.4620
natriuretic peptide, brain
Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.		8.03142polypeptide
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		3.2310ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
raltegravir
[no description available]		3.23101,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		3.6120
oxytetracycline, anhydrous
Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.		3.2310
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		3.6120
piroxicam
[no description available]		3.6120benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
roquinimex
roquinimex: structure in first source		2.0810aromatic amide
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		3.61201,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
mobiflex
tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.		2.0810heteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
isoxicam
isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome.		2.0810benzothiazine;
isoxazoles;
monocarboxylic acid amide		antirheumatic drug;
non-steroidal anti-inflammatory drug
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		3.9730benzenes;
hydroxycoumarin;
methyl ketone
demeclocycline
Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		6.9361
tipranavir
tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor.		3.2310sulfonamideantiviral drug;
HIV protease inhibitor
minocycline hydrochloride
[no description available]		2.0810
tigecycline
[no description available]		3.6120
lornoxicam
lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.		2.0810heteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine		antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.1110
(6-chloro-1-(2-(dimethylamino)ethyl)indol-3-yl)-spiro(1h-isobenzofuran-3,4'-piperidine)-1'-yl-methanone
(6-chloro-1-(2-(dimethylamino)ethyl)indol-3-yl)-spiro(1H-isobenzofuran-3,4'-piperidine)-1'-yl-methanone: a vasopressin 1a receptor antagonist; structure in first source		2.3110
hirudin
Hirudin: A 65-residue polypeptide from LEECHES.		2.0310
fertinex
[no description available]		3.2310
nephrin
nephrin: gene nephrin is mutated in congenital nephrotic syndrome; amino acid sequence in first source; GenBank F19541; RefSeq NM_019459 (mouse), NM_004646 (human), NM_022628 (rat)		2.0510
transforming growth factor alpha
Transforming Growth Factor alpha: An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR.		2.1110
entecavir
entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B.		3.61202-aminopurines;
oxopurine;
primary alcohol;
secondary alcohol		antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
acyclovir
Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.		3.61202-aminopurines;
oxopurine		antimetabolite;
antiviral drug
guanosine triphosphate
Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.		2.0210guanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		3.6320folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		5.4941cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		4.3930benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		3.8930dacarbazine
didanosine
Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.		3.6120purine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor;
geroprotector;
HIV-1 reverse transcriptase inhibitor
ganciclovir
[no description available]		3.61202-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
valtrex
[no description available]		2.0810organic molecular entity
valacyclovir
Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES.		3.2310L-valyl esterantiviral drug
sildenafil
sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position.		3.2310piperazines;
pyrazolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
olanzapine
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		3.6120benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
raltitrexed
[no description available]		2.0810N-acyl-amino acid
vardenafil
vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine.		3.2310imidazotriazine;
N-alkylpiperazine;
N-sulfonylpiperazine		EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		3.6120nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
citrovorum factor
[no description available]		3.6120tetrahydrofolic acid
leucovorin
5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5.		3.2310formyltetrahydrofolic acidEscherichia coli metabolite;
mouse metabolite
rifapentine
rifapentine: cyclopentyl derivative of rifampicin		3.6120N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug
bl 4162a
anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions.		3.2310imidazoquinazolineanticoagulant;
antifibrinolytic drug;
cardiovascular drug;
platelet aggregation inhibitor
tegaserod
tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source		3.2310carboxamidine;
guanidines;
hydrazines;
indoles		gastrointestinal drug;
serotonergic agonist
pemetrexed
pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).		3.2310N-acyl-L-glutamic acid;
pyrrolopyrimidine		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
sildenafil citrate
Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.		2.0810citrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
valganciclovir
Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine.		3.2310L-valyl ester;
purines		antiviral drug;
prodrug
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		3.6120(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
fosaprepitant
fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid.		3.2310(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
phosphoramide;
triazoles		antiemetic;
neurokinin-1 receptor antagonist;
prodrug
tegaserod maleate
[no description available]		2.0810maleate saltserotonergic agonist
rifabutin
[no description available]		3.6120
levomefolate calcium
levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid.		3.2310organic calcium saltantidepressant
ConditionIndicatedRelationship StrengthStudiesTrials
Acute Liver Injury, Drug-Induced
[description not available]		09.88231
Adverse Drug Event
[description not available]		06.7481
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		09.88231
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		06.7481
Benign Neoplasms
[description not available]		08.42142
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		08.42142
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		06.89270
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
ADPKD
[description not available]		020.4120560
Polycystic Kidney, Autosomal Dominant
Kidney disorders with autosomal dominant inheritance and characterized by multiple CYSTS in both KIDNEYS with progressive deterioration of renal function.		122.4120560
Cyst
[description not available]		05.2590
Cardiac Failure
[description not available]		027.64404123
Mitral Incompetence
[description not available]		02.5820
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		127.4808246
Mitral Valve Insufficiency
Backflow of blood from the LEFT VENTRICLE into the LEFT ATRIUM due to imperfect closure of the MITRAL VALVE. This can lead to mitral valve regurgitation.		02.5820
Ascites
Accumulation or retention of free fluid within the peritoneal cavity.		015.296023
Acute Disease
Disease having a short and relatively severe course.		015.716324
Tricuspid Incompetence
[description not available]		04.0840
Antidiuretic Hormone, Inappropriate Secretion
[description not available]		018.4214728
Hyponatremia
Deficiency of sodium in the blood; salt depletion. (Dorland, 27th ed)		123.5229063
Inappropriate ADH Syndrome
A condition of HYPONATREMIA and renal salt loss attributed to overexpansion of BODY FLUIDS resulting from sustained release of ANTIDIURETIC HORMONES which stimulates renal resorption of water. It is characterized by normal KIDNEY function, high urine OSMOLALITY, low serum osmolality, and neurological dysfunction. Etiologies include ADH-producing neoplasms, injuries or diseases involving the HYPOTHALAMUS, the PITUITARY GLAND, and the LUNG. This syndrome can also be drug-induced.		120.4214728
Chronic Kidney Failure
[description not available]		013.473112
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		013.473112
Disease Exacerbation
[description not available]		016.537126
Chronic Kidney Diseases
[description not available]		013.24610
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		115.24610
Cirrhosis, Liver
[description not available]		017.89842
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		119.89842
Aortic Stenosis
[description not available]		03.3250
Aortic Valve Stenosis
A pathological constriction that can occur above (supravalvular stenosis), below (subvalvular stenosis), or at the AORTIC VALVE. It is characterized by restricted outflow from the LEFT VENTRICLE into the AORTA.		08.3250
Kidney, Polycystic
[description not available]		07.61220
Polycystic Kidney Diseases
Hereditary diseases that are characterized by the progressive expansion of a large number of tightly packed CYSTS within the KIDNEYS. They include diseases with autosomal dominant and autosomal recessive inheritance.		111.39440
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		03.0340
Anasarca
[description not available]		07.4212
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		07.4212
Nephrotic Syndrome
A condition characterized by severe PROTEINURIA, greater than 3.5 g/day in an average adult. The substantial loss of protein in the urine results in complications such as HYPOPROTEINEMIA; generalized EDEMA; HYPERTENSION; and HYPERLIPIDEMIAS. Diseases associated with nephrotic syndrome generally cause chronic kidney dysfunction.		03.85100
Cancer of Pancreas
[description not available]		02.4110
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		02.4110
Acute Kidney Failure
[description not available]		07.98142
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		07.98142
Liver Dysfunction
[description not available]		03.3650
Liver Diseases
Pathological processes of the LIVER.		03.3650
Abdominal Aortic Aneurysm
[description not available]		07.4920
Aortic Aneurysm, Abdominal
An abnormal balloon- or sac-like dilatation in the wall of the ABDOMINAL AORTA which gives rise to the visceral, the parietal, and the terminal (iliac) branches below the aortic hiatus at the diaphragm.		02.4920
Breathlessness
[description not available]		012.741811
Dyspnea
Difficult or labored breathing.		114.741811
Water-Electrolyte Imbalance
Disturbances in the body's WATER-ELECTROLYTE BALANCE.		011.48206
Adenoma Sebaceum
Facial ANGIOFIBROMA in tuberous sclerosis		02.610
Tuberous Sclerosis
Autosomal dominant neurocutaneous syndrome classically characterized by MENTAL RETARDATION; EPILEPSY; and skin lesions (e.g., adenoma sebaceum and hypomelanotic macules). There is, however, considerable heterogeneity in the neurologic manifestations. It is also associated with cortical tuber and HAMARTOMAS formation throughout the body, especially the heart, kidneys, and eyes. Mutations in two loci TSC1 and TSC2 that encode hamartin and tuberin, respectively, are associated with the disease.		07.610
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		019.625131
Hyperpotassemia
[description not available]		05.3441
Hyperkalemia
Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)		05.3441
Hematuria
Presence of blood in the urine.		03.5210
Blood Pressure, High
[description not available]		08.98163
Colicky Pain
[description not available]		03.5120
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		08.98163
Polyuria
Urination of a large volume of urine with an increase in urinary frequency, commonly seen in diabetes (DIABETES MELLITUS; DIABETES INSIPIDUS).		012.2162
Abdominal Pain
Sensation of discomfort, distress, or agony in the abdominal region.		03.5120
Cruveilhier-Baumgarten Syndrome
Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS.		03.6820
Hypertension, Portal
Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.		03.6820
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		08.4820
Hypernatremia
Excessive amount of sodium in the blood. (Dorland, 27th ed)		06.31121
Viremia
The presence of viruses in the blood.		02.610
Infections, Roseolovirus
[description not available]		02.610
Cirrhosis
[description not available]		05.0280
Innate Inflammatory Response
[description not available]		04.2130
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		010.0280
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		04.2130
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		18.394
Pulmonary Hypertension
[description not available]		03.4860
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		03.4860
ARPKD
[description not available]		02.7630
Polycystic Kidney, Autosomal Recessive
A genetic disorder with autosomal recessive inheritance, characterized by multiple CYSTS in both KIDNEYS and associated LIVER lesions. Serious manifestations are usually present at BIRTH with high PERINATAL MORTALITY.		02.7630
Auricular Fibrillation
[description not available]		03.0740
Aortic Dissection
[description not available]		07.610
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		08.0740
Cancer of Lung
[description not available]		06.5992
Local Neoplasm Recurrence
[description not available]		02.6620
Lung Neoplasms
Tumors or cancer of the LUNG.		06.5992
Chronic Liver Failure
[description not available]		05.3941
End Stage Liver Disease
Final stage of a liver disease when the liver failure is irreversible and LIVER TRANSPLANTATION is needed.		05.3941
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		013.881911
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		08.881911
Absence Seizure
[description not available]		02.610
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		02.610
Calcification, Pathologic
[description not available]		02.610
Oxaluria, Primary
[description not available]		02.610
Calcinosis
Pathologic deposition of calcium salts in tissues.		02.610
Hyperoxaluria, Primary
A genetic disorder characterized by excretion of large amounts of OXALATES in urine; NEPHROLITHIASIS; NEPHROCALCINOSIS; early onset of RENAL FAILURE; and often a generalized deposit of CALCIUM OXALATE. There are subtypes classified by the enzyme defects in glyoxylate metabolism.		02.610
Canine Diseases
[description not available]		02.610
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		02.8330
Pleural Effusion
Presence of fluid in the pleural cavity resulting from excessive transudation or exudation from the pleural surfaces. It is a sign of disease and not a diagnosis in itself.		02.9330
Granulocytic Leukemia, Chronic
[description not available]		02.2510
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		02.2510
Left Ventricular Dysfunction
[description not available]		013.7145
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		08.7145
Sarcopenia
Progressive decline in muscle mass due to aging which results in decreased functional capacity of muscles.		02.2510
Adenocarcinoma Of Kidney
[description not available]		03.5520
Cancer of Kidney
[description not available]		03.7730
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		03.5520
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		03.7730
Complication, Postoperative
[description not available]		06.22162
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		06.22162
Alloxan Diabetes
[description not available]		02.2510
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.4820
Urinary Lithiasis
[description not available]		02.3110
Urinary Calculi
Low-density crystals or stones in any part of the URINARY TRACT. Their chemical compositions often include CALCIUM OXALATE, magnesium ammonium phosphate (struvite), CYSTINE, or URIC ACID.		02.3110
Cystinuria
An inherited disorder due to defective reabsorption of CYSTINE and other BASIC AMINO ACIDS by the PROXIMAL RENAL TUBULES. This form of aminoaciduria is characterized by the abnormally high urinary levels of cystine; LYSINE; ARGININE; and ORNITHINE. Mutations involve the amino acid transport protein gene SLC3A1.		02.8630
Urolithiasis
Formation of stones in any part of the URINARY TRACT, usually in the KIDNEY; URINARY BLADDER; or the URETER.		07.3110
Chronic Illness
[description not available]		013.832912
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		013.832912
Critical Illness
A disease or state in which death is possible or imminent.		04.1350
Kidney Stones
[description not available]		05.3641
Kidney Calculi
Stones in the KIDNEY, usually formed in the urine-collecting area of the kidney (KIDNEY PELVIS). Their sizes vary and most contains CALCIUM OXALATE.		17.3641
Diabetic Glomerulosclerosis
[description not available]		03.2450
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		03.2450
Urinary Tract Infections
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.		02.3110
Recrudescence
[description not available]		08.275
Adenocarcinoma, Basal Cell
[description not available]		02.2510
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.2510
Acquired Nephrogenic Diabetes Insipidus
[description not available]		06.2571
Weight Reduction
[description not available]		09.1114
Weight Loss
Decrease in existing BODY WEIGHT.		09.1114
Genetic Predisposition
[description not available]		03.6420
Acute-On-Chronic Liver Failure (ACLF)
[description not available]		03.1710
Encephalopathy, Hepatic
[description not available]		03.9320
Hepatic Encephalopathy
A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5)		03.9320
Hepatorenal Syndrome
Functional KIDNEY FAILURE in patients with liver disease, usually LIVER CIRRHOSIS or portal hypertension (HYPERTENSION, PORTAL), and in the absence of intrinsic renal disease or kidney abnormality. It is characterized by intense renal vasculature constriction, reduced renal blood flow, OLIGURIA, and sodium retention.		03.9320
Acute-On-Chronic Liver Failure
Sudden liver failure in the presence of underlying compensated chronic LIVER DISEASE (e.g., LIVER CIRRHOSIS; HEPATITIS; and liver injury and failure) due to a precipitating acute hepatic insult.		03.1710
Hepatocellular Carcinoma
[description not available]		03.1240
Cancer of Liver
[description not available]		03.1240
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		03.1240
Liver Neoplasms
Tumors or cancer of the LIVER.		03.1240
Abnormality, Heart
[description not available]		02.8930
Heart Defects, Congenital
Developmental abnormalities involving structures of the heart. These defects are present at birth but may be discovered later in life.		02.8930
Electrolytes
Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)		011.0552
47,XX,+21
[description not available]		02.3110
Down Syndrome
A chromosome disorder associated either with an extra chromosome 21 or an effective trisomy for chromosome 21. Clinical manifestations include hypotonia, short stature, brachycephaly, upslanting palpebral fissures, epicanthus, Brushfield spots on the iris, protruding tongue, small ears, short, broad hands, fifth finger clinodactyly, Simian crease, and moderate to severe INTELLECTUAL DISABILITY. Cardiac and gastrointestinal malformations, a marked increase in the incidence of LEUKEMIA, and the early onset of ALZHEIMER DISEASE are also associated with this condition. Pathologic features include the development of NEUROFIBRILLARY TANGLES in neurons and the deposition of AMYLOID BETA-PROTEIN, similar to the pathology of ALZHEIMER DISEASE. (Menkes, Textbook of Child Neurology, 5th ed, p213)		02.3110
Hyperidrosis
[description not available]		02.4110
Hyperhidrosis
Excessive sweating. In the localized type, the most frequent sites are the palms, soles, axillae, inguinal folds, and the perineal area. Its chief cause is thought to be emotional. Generalized hyperhidrosis may be induced by a hot, humid environment, by fever, or by vigorous exercise.		07.4110
Cardiac Output, Low
A state of subnormal or depressed cardiac output at rest or during stress. It is a characteristic of CARDIOVASCULAR DISEASES, including congenital, valvular, rheumatic, hypertensive, coronary, and cardiomyopathic. The serious form of low cardiac output is characterized by marked reduction in STROKE VOLUME, and systemic vasoconstriction resulting in cold, pale, and sometimes cyanotic extremities.		03.4420
Cardiovascular Stroke
[description not available]		03.5880
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		03.5880
Hemorrhage, Subarachnoid
[description not available]		02.6120
Subarachnoid Hemorrhage
Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.		02.6120
Bile Duct Obstruction
[description not available]		02.1510
Cholestasis
Impairment of bile flow due to obstruction in small bile ducts (INTRAHEPATIC CHOLESTASIS) or obstruction in large bile ducts (EXTRAHEPATIC CHOLESTASIS).		02.1510
Carcinoma, Oat Cell
[description not available]		03.4220
Cancer of Prostate
[description not available]		02.1510
Symptom Cluster
[description not available]		04.0950
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.1510
Syndrome
A characteristic symptom complex.		09.0950
Carcinoma, Small Cell
An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)		03.4220
Ventricular Septal Perforation
Presence of a hole or holes in the ventricular septum.		02.1510
Hepatic Failure
[description not available]		02.1510
Liver Failure
Severe inability of the LIVER to perform its normal metabolic functions, as evidenced by severe JAUNDICE and abnormal serum levels of AMMONIA; BILIRUBIN; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; LACTATE DEHYDROGENASES; and albumin/globulin ratio. (Blakiston's Gould Medical Dictionary, 4th ed)		02.1510
Carcinoma, Small Cell Lung
[description not available]		05.4572
Lung Adenocarcinoma
[description not available]		02.1710
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		02.1710
Paraneoplastic Syndromes
In patients with neoplastic diseases a wide variety of clinical pictures which are indirect and usually remote effects produced by tumor cell metabolites or other products.		04.1250
Cancer, Second Primary
[description not available]		02.1710
Adenocarcinoma of Lung
A carcinoma originating in the lung and the most common lung cancer type in never-smokers. Malignant cells exhibit distinct features such as glandular epithelial, or tubular morphology. Mutations in KRAS, EGFR, BRAF, and ERBB2 genes are associated with this cancer.		02.1710
Small Cell Lung Carcinoma
A form of highly malignant lung cancer that is composed of small ovoid cells (SMALL CELL CARCINOMA).		05.4572
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		07.1710
Hypoalbuminemia
A condition in which albumin level in blood (SERUM ALBUMIN) is below the normal range. Hypoalbuminemia may be due to decreased hepatic albumin synthesis, increased albumin catabolism, altered albumin distribution, or albumin loss through the urine (ALBUMINURIA).		04.4441
Genetic Diseases, X-Chromosome Linked
[description not available]		02.5420
Delirium of Mixed Origin
[description not available]		02.1510
Delirium
A disorder characterized by CONFUSION; inattentiveness; disorientation; ILLUSIONS; HALLUCINATIONS; agitation; and in some instances autonomic nervous system overactivity. It may result from toxic/metabolic conditions or structural brain lesions. (From Adams et al., Principles of Neurology, 6th ed, pp411-2)		02.1510
Circulatory Collapse
[description not available]		02.1710
Shock
A pathological condition manifested by failure to perfuse or oxygenate vital organs.		07.1710
Muscular Weakness
[description not available]		02.2510
Acute Autoimmune Neuropathy
[description not available]		02.2510
Muscle Weakness
A vague complaint of debility, fatigue, or exhaustion attributable to weakness of various muscles. The weakness can be characterized as subacute or chronic, often progressive, and is a manifestation of many muscle and neuromuscular diseases. (From Wyngaarden et al., Cecil Textbook of Medicine, 19th ed, p2251)		02.2510
Guillain-Barre Syndrome
An acute inflammatory autoimmune neuritis caused by T cell- mediated cellular immune response directed towards peripheral myelin. Demyelination occurs in peripheral nerves and nerve roots. The process is often preceded by a viral or bacterial infection, surgery, immunization, lymphoma, or exposure to toxins. Common clinical manifestations include progressive weakness, loss of sensation, and loss of deep tendon reflexes. Weakness of respiratory muscles and autonomic dysfunction may occur. (From Adams et al., Principles of Neurology, 6th ed, pp1312-1314)		02.2510
Cardio-Renal Syndrome
Condition where a primary dysfunction of either heart or kidney results in failure of the other organ (e.g., HEART FAILURE with worsening RENAL INSUFFICIENCY).		011.1261
Arteriosclerosis, Coronary
[description not available]		03.9421
Oliguria
Decreased URINE output that is below the normal range. Oliguria can be defined as urine output of less than or equal to 0.5 or 1 ml/kg/hr depending on the age.		07.5320
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		03.9421
Cardiac Arrest, Sudden
[description not available]		03.5611
Death, Sudden, Cardiac
Unexpected rapid natural death due to cardiovascular collapse within one hour of initial symptoms. It is usually caused by the worsening of existing heart diseases. The sudden onset of symptoms, such as CHEST PAIN and CARDIAC ARRHYTHMIAS, particularly VENTRICULAR TACHYCARDIA, can lead to the loss of consciousness and cardiac arrest followed by biological death. (from Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine, 7th ed., 2005)		03.5611
Left Ventricular Hypertrophy
[description not available]		03.4620
Diastolic Heart Failure
[description not available]		03.0910
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		03.4620
Heart Failure, Diastolic
Heart failure caused by abnormal myocardial relaxation during DIASTOLE leading to defective cardiac filling.		03.0910
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		16.3740
Shingles
[description not available]		02.1710
Herpes Zoster
An acute infectious, usually self-limited, disease believed to represent activation of latent varicella-zoster virus (HERPESVIRUS 3, HUMAN) in those who have been rendered partially immune after a previous attack of CHICKENPOX. It involves the SENSORY GANGLIA and their areas of innervation and is characterized by severe neuralgic pain along the distribution of the affected nerve and crops of clustered vesicles over the area. (From Dorland, 27th ed)		02.1710
Atrial Remodeling
Long-term changes in the electrophysiological parameters and/or anatomical structures of the HEART ATRIA that result from prolonged changes in atrial rate, often associated with ATRIAL FIBRILLATION or long periods of intense EXERCISE.		07.1710
Anoxemia
[description not available]		02.1710
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		07.1710
Dehydration
The condition that results from excessive loss of water from a living organism.		03.0910
Heart Valve Diseases
Pathological conditions involving any of the various HEART VALVES and the associated structures (PAPILLARY MUSCLES and CHORDAE TENDINEAE).		03.7430
Cancer of Pituitary
[description not available]		02.2110
Craniopharyngioma, Adamantinous
[description not available]		02.2110
Craniopharyngioma
A benign pituitary-region neoplasm that originates from Rathke's pouch. The two major histologic and clinical subtypes are adamantinous (or classical) craniopharyngioma and papillary craniopharyngioma. The adamantinous form presents in children and adolescents as an expanding cystic lesion in the pituitary region. The cystic cavity is filled with a black viscous substance and histologically the tumor is composed of adamantinomatous epithelium and areas of calcification and necrosis. Papillary craniopharyngiomas occur in adults, and histologically feature a squamous epithelium with papillations. (From Joynt, Clinical Neurology, 1998, Ch14, p50)		07.2110
Pituitary Neoplasms
Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA.		02.2110
Aneurysm, Thoracic Aortic
[description not available]		02.2110
Aortic Aneurysm, Thoracic
An abnormal balloon- or sac-like dilatation in the wall of the THORACIC AORTA. This proximal descending portion of aorta gives rise to the visceral and the parietal branches above the aortic hiatus at the diaphragm.		02.2110
Cardiomyopathies, Primary
[description not available]		02.2110
Cardiomyopathies
A group of diseases in which the dominant feature is the involvement of the CARDIAC MUSCLE itself. Cardiomyopathies are classified according to their predominant pathophysiological features (DILATED CARDIOMYOPATHY; HYPERTROPHIC CARDIOMYOPATHY; RESTRICTIVE CARDIOMYOPATHY) or their etiological/pathological factors (CARDIOMYOPATHY, ALCOHOLIC; ENDOCARDIAL FIBROELASTOSIS).		02.2110
Brain Swelling
[description not available]		06.9971
Brain Hemorrhage, Cerebral
[description not available]		02.5820
Brain Edema
Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)		011.9971
Cerebral Hemorrhage
Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.		07.5820
Capillary Leak Syndrome
A condition characterized by recurring episodes of fluid leaking from capillaries into extra-vascular compartments causing hematocrit to rise precipitously. If not treated, generalized vascular leak can lead to generalized EDEMA; SHOCK; cardiovascular collapse; and MULTIPLE ORGAN FAILURE.		07.2110
Cardiomyopathy, Hypertrophic Obstructive
[description not available]		02.2110
Cardiomyopathy, Hypertrophic
A form of CARDIAC MUSCLE disease, characterized by left and/or right ventricular hypertrophy (HYPERTROPHY, LEFT VENTRICULAR; HYPERTROPHY, RIGHT VENTRICULAR), frequent asymmetrical involvement of the HEART SEPTUM, and normal or reduced left ventricular volume. Risk factors include HYPERTENSION; AORTIC STENOSIS; and gene MUTATION; (FAMILIAL HYPERTROPHIC CARDIOMYOPATHY).		02.2110
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		03.1710
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		03.1710
Pulmonary Consumption
[description not available]		02.0810
Tuberculosis, Pulmonary
MYCOBACTERIUM infections of the lung.		02.0810
Hypertension, Renal
Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.		03.8820
Multiple Primary Neoplasms
[description not available]		02.0810
Acute Brain Injuries
[description not available]		02.7730
Bewilderment
[description not available]		02.0810
Injuries, Multiple
[description not available]		02.4920
Agitation, Psychomotor
[description not available]		02.0810
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		02.7730
Psychomotor Agitation
A feeling of restlessness associated with increased motor activity. This may occur as a manifestation of nervous system drug toxicity or other conditions.		02.0810
Rhabdomyolysis
Necrosis or disintegration of skeletal muscle often followed by myoglobinuria.		02.0810
Psychoses
[description not available]		05.341
Psychotic Disorders
Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994)		010.341
Nephrosclerosis
Hardening of the KIDNEY due to infiltration by fibrous connective tissue (FIBROSIS), usually caused by renovascular diseases or chronic HYPERTENSION. Nephrosclerosis leads to renal ISCHEMIA.		02.0810
Systolic Heart Failure
[description not available]		012.1154
Heart Failure, Systolic
Heart failure caused by abnormal myocardial contraction during SYSTOLE leading to defective cardiac emptying.		07.1154
Adenohypophyseal Hyposecretion
[description not available]		02.0810
Hypopituitarism
Diminution or cessation of secretion of one or more hormones from the anterior pituitary gland (including LH; FOLLICLE STIMULATING HORMONE; SOMATOTROPIN; and CORTICOTROPIN). This may result from surgical or radiation ablation, non-secretory PITUITARY NEOPLASMS, metastatic tumors, infarction, PITUITARY APOPLEXY, infiltrative or granulomatous processes, and other conditions.		02.0810
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		05.6563
Cardiac Remodeling, Ventricular
[description not available]		06.6771
Acute-Phase Reaction
An early local inflammatory reaction to insult or injury that consists of fever, an increase in inflammatory humoral factors, and an increased synthesis by hepatocytes of a number of proteins or glycoproteins usually found in the plasma.		02.0810
Hypovolemic
[description not available]		06.6561
Hypovolemia
An abnormally low volume of blood circulating through the body. It may result in hypovolemic shock (see SHOCK).		06.6561
Central Diabetes Insipidus
[description not available]		02.110
Diabetes Insipidus, Neurogenic
A genetic or acquired polyuric disorder caused by a deficiency of VASOPRESSINS secreted by the NEUROHYPOPHYSIS. Clinical signs include the excretion of large volumes of dilute URINE; HYPERNATREMIA; THIRST; and polydipsia. Etiologies include HEAD TRAUMA; surgeries and diseases involving the HYPOTHALAMUS and the PITUITARY GLAND. This disorder may also be caused by mutations of genes such as ARVP encoding vasopressin and its corresponding neurophysin (NEUROPHYSINS).		02.110
Adenohypophyseal Diseases
[description not available]		03.0110
Pituitary Diseases
Disorders involving either the ADENOHYPOPHYSIS or the NEUROHYPOPHYSIS. These diseases usually manifest as hypersecretion or hyposecretion of PITUITARY HORMONES. Neoplastic pituitary masses can also cause compression of the OPTIC CHIASM and other adjacent structures.		03.0110
Central Hypothyroidism
[description not available]		03.0110
Hypothyroidism
A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.		03.0110
Fusiform Aneurysm
Elongated, spindle-shaped dilation in the wall of blood vessels, usually large ARTERIES with ATHEROSCLEROSIS.		02.110
Aneurysm
Pathological outpouching or sac-like dilatation in the wall of any blood vessel (ARTERIES or VEINS) or the heart (HEART ANEURYSM). It indicates a thin and weakened area in the wall which may later rupture. Aneurysms are classified by location, etiology, or other characteristics.		07.110
Brain Hemorrhage
[description not available]		02.110
Clinically Isolated CNS Demyelinating Syndrome
[description not available]		04.1430
Demyelinating Diseases
Diseases characterized by loss or dysfunction of myelin in the central or peripheral nervous system.		04.1430
Intracranial Hemorrhages
Bleeding within the SKULL, including hemorrhages in the brain and the three membranes of MENINGES. The escape of blood often leads to the formation of HEMATOMA in the cranial epidural, subdural, and subarachnoid spaces.		02.110
Apoplexy
[description not available]		02.110
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		07.110
Acute Coronary Syndrome
An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION.		02.4620
Glomerulonephritis, Minimal Change
[description not available]		02.1110
Nephrosis, Lipoid
A kidney disease with no or minimal histological glomerular changes on light microscopy and with no immune deposits. It is characterized by lipid accumulation in the epithelial cells of KIDNEY TUBULES and in the URINE. Patients usually show NEPHROTIC SYNDROME indicating the presence of PROTEINURIA with accompanying EDEMA.		02.1110
Hypokalemia
Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed)		04.1631
Blood Pressure, Low
[description not available]		04.4422
Hypotension
Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.		09.4422
Endotoxin Shock
[description not available]		02.1110
Shock, Septic
Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.		02.1110
Aura
[description not available]		02.1110
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.1110
Allergy, Drug
[description not available]		02.1110
Drug Hypersensitivity
Immunologically mediated adverse reactions to medicinal substances used legally or illegally.		02.1110
Exanthem
[description not available]		02.1110
Itching
[description not available]		02.1110
Cutaneous T-Cell Lymphoma
[description not available]		02.1110
Exanthema
Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.		02.1110
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		02.1110
Lymphoma, T-Cell, Cutaneous
A group of lymphomas exhibiting clonal expansion of malignant T-lymphocytes arrested at varying stages of differentiation as well as malignant infiltration of the skin. MYCOSIS FUNGOIDES; SEZARY SYNDROME; LYMPHOMATOID PAPULOSIS; and PRIMARY CUTANEOUS ANAPLASTIC LARGE CELL LYMPHOMA are the best characterized of these disorders.		02.1110
Airflow Obstruction, Chronic
[description not available]		03.511
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		03.511
Mediastinitis
Inflammation of the mediastinum, the area between the pleural sacs.		07.1110
Cardiac Edema
[description not available]		08.1785
Edema, Cardiac
Abnormal fluid retention by the body due to impaired cardiac function or heart failure. It is usually characterized by increase in venous and capillary pressure, and swollen legs when standing. It is different from the generalized edema caused by renal dysfunction (NEPHROTIC SYNDROME).		110.1785
Dextro-Looped Transposition of the Great Arteries
[description not available]		02.1110
Chylothorax
The presence of chyle in the thoracic cavity. (Dorland, 27th ed)		07.1110
Transposition of Great Vessels
A congenital cardiovascular malformation in which the AORTA arises entirely from the RIGHT VENTRICLE, and the PULMONARY ARTERY arises from the LEFT VENTRICLE. Consequently, the pulmonary and the systemic circulations are parallel and not sequential, so that the venous return from the peripheral circulation is re-circulated by the right ventricle via aorta to the systemic circulation without being oxygenated in the lungs. This is a potentially lethal form of heart disease in newborns and infants.		02.1110
Albuminuria
The presence of albumin in the urine, an indicator of KIDNEY DISEASES.		011.0133
Complications of Diabetes Mellitus
[description not available]		04.4522
Endolymphatic Hydrops
An accumulation of ENDOLYMPH in the inner ear (LABYRINTH) leading to buildup of pressure and distortion of intralabyrinthine structures, such as COCHLEA and SEMICIRCULAR CANALS. It is characterized by SENSORINEURAL HEARING LOSS; TINNITUS; and sometimes VERTIGO.		02.1310
Auditory Vertigo
[description not available]		02.1310
Meniere Disease
A disease of the inner ear (LABYRINTH) that is characterized by fluctuating SENSORINEURAL HEARING LOSS; TINNITUS; episodic VERTIGO; and aural fullness. It is the most common form of endolymphatic hydrops.		02.1310
Blast Phase
[description not available]		02.1110
Dysmyelopoietic Syndromes
[description not available]		02.1110
Blast Crisis
An advanced phase of chronic myelogenous leukemia, characterized by a rapid increase in the proportion of immature white blood cells (blasts) in the blood and bone marrow to greater than 30%.		07.1110
Myelodysplastic Syndromes
Clonal hematopoietic stem cell disorders characterized by dysplasia in one or more hematopoietic cell lineages. They predominantly affect patients over 60, are considered preleukemic conditions, and have high probability of transformation into ACUTE MYELOID LEUKEMIA.		02.1110
Cognitive Decline
[description not available]		03.5111
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		03.5111
Ache
[description not available]		06.0233
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		011.0233
Heart Disease, Ischemic
[description not available]		02.1310
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		02.1310
Cirrhoses, Experimental Liver
[description not available]		02.1310
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		02.1310
Constrictive Pericarditis
[description not available]		07.1310
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.1310
Pneumonia
Infection of the lung often accompanied by inflammation.		02.1310
Disease, Pulmonary
[description not available]		02.1310
Lung Diseases
Pathological processes involving any part of the LUNG.		02.1310
Cardiac Diseases
[description not available]		02.4820
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		02.4820
Diathesis
[description not available]		02.1510
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.1310
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.1310
Alarm Clock Headache
[description not available]		03.5311
Blood Poisoning
[description not available]		02.1310
Tungiasis
An infestation with the flea TUNGA PENETRANS causing inflammation, pruritus, and pain, in both humans and other mammals. There is a high incidence of secondary infections such as BACTEREMIA and TETANUS.		02.1310
Ectoparasitic Infestations
Infestations by PARASITES which live on, or burrow into, the surface of their host's EPIDERMIS. Most ectoparasites are ARTHROPODS.		02.1310
Sepsis
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.		02.1310
Encephalopathy, Traumatic
[description not available]		02.1510
Brain Injuries, Traumatic
A form of acquired brain injury which occurs when a sudden trauma causes damage to the brain.		02.1510
Extramembranous Glomerulopathy
[description not available]		02.1510
Glomerulonephritis, Membranous
A type of glomerulonephritis that is characterized by the accumulation of immune deposits (COMPLEMENT MEMBRANE ATTACK COMPLEX) on the outer aspect of the GLOMERULAR BASEMENT MEMBRANE. It progresses from subepithelial dense deposits, to basement membrane reaction and eventual thickening of the basement membrane.		02.1510
Nervous System Disorders
[description not available]		02.1510
Nervous System Diseases
Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.		02.1510
Brain Disorders
[description not available]		02.9610
Brain Diseases
Pathologic conditions affecting the BRAIN, which is composed of the intracranial components of the CENTRAL NERVOUS SYSTEM. This includes (but is not limited to) the CEREBRAL CORTEX; intracranial white matter; BASAL GANGLIA; THALAMUS; HYPOTHALAMUS; BRAIN STEM; and CEREBELLUM.		02.9610
Dementia Praecox
[description not available]		04.7521
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		04.7521
Weight Gain
Increase in BODY WEIGHT over existing weight.		03.4311
Nephrosis
Pathological processes of the KIDNEY without inflammatory or neoplastic components. Nephrosis may be a primary disorder or secondary complication of other diseases. It is characterized by the NEPHROTIC SYNDROME indicating the presence of PROTEINURIA and HYPOALBUMINEMIA with accompanying EDEMA.		02.0510
Atelectasis
[description not available]		04.3511
Central Pontine Myelinolysis
[description not available]		02.9610
Alcoholic Cirrhosis
[description not available]		07.4720
Liver Cirrhosis, Alcoholic
FIBROSIS of the hepatic parenchyma due to chronic excess ALCOHOL DRINKING.		02.4720
Cardiomyopathy, Congestive
[description not available]		03.8520
Cardiomyopathy, Dilated
A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.		03.8520
Age-Related Memory Disorders
[description not available]		02.0510
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		02.0510
Water Intoxication
A condition resulting from the excessive retention of water with sodium depletion.		03.8520
Ventricular Dysfunction
A condition in which HEART VENTRICLES exhibit impaired function.		02.9710
Dizzyness
[description not available]		03.4511
Dizziness
An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness.		03.4511
Secondary Hyperparathyroidism
[description not available]		02.0610
Hyperparathyroidism, Secondary
Abnormally elevated PARATHYROID HORMONE secretion as a response to HYPOCALCEMIA. It is caused by chronic KIDNEY FAILURE or other abnormalities in the controls of bone and mineral metabolism, leading to various BONE DISEASES, such as RENAL OSTEODYSTROPHY.		02.0610
Ectopic Hormone Syndromes
[description not available]		03.4511
Foot Diseases
Anatomical and functional disorders affecting the foot.		02.0610
Skin Diseases, Vascular
Skin diseases affecting or involving the cutaneous blood vessels and generally manifested as inflammation, swelling, erythema, or necrosis in the affected area.		02.0610
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.0610
Cerebromeningitis
[description not available]		02.0710
Infection
[description not available]		02.9910
Infections
Invasion of the host organism by microorganisms or their toxins or by parasites that can cause pathological conditions or diseases.		02.9910
Depression, Endogenous
[description not available]		02.0710
Convulsive Generalized Seizure Disorder
[description not available]		02.0710
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		02.0710
Drop Attack
[description not available]		02.0710
Syncope
A transient loss of consciousness and postural tone caused by diminished blood flow to the brain (i.e., BRAIN ISCHEMIA). Presyncope refers to the sensation of lightheadedness and loss of strength that precedes a syncopal event or accompanies an incomplete syncope. (From Adams et al., Principles of Neurology, 6th ed, pp367-9)		02.0710
Embolus
[description not available]		02.0710
Bleeding
[description not available]		02.0710
Hematochezia
The passage of bright red blood from the rectum. The blood may or may not be mixed with formed stool in the form of blood, blood clots, bloody stool or diarrhea.		02.0710
Drug Withdrawal Symptoms
[description not available]		02.0710
Embolism
Blocking of a blood vessel by an embolus which can be a blood clot or other undissolved material in the blood stream.		02.0710
Hemorrhage
Bleeding or escape of blood from a vessel.		02.0710
Gastrointestinal Hemorrhage
Bleeding in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.		02.0710
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		02.0710
Hepatic Veno Occlusive Disease
[description not available]		02.0810
Hepatic Veno-Occlusive Disease
Liver disease that is caused by injuries to the ENDOTHELIAL CELLS of the vessels and subendothelial EDEMA, but not by THROMBOSIS. Extracellular matrix, rich in FIBRONECTINS, is usually deposited around the HEPATIC VEINS leading to venous outflow occlusion and sinusoidal obstruction.		02.0810
Cardiomyopathy, Restrictive
A form of CARDIAC MUSCLE disease in which the ventricular walls are excessively rigid, impeding ventricular filling. It is marked by reduced diastolic volume of either or both ventricles but normal or nearly normal systolic function. It may be idiopathic or associated with other diseases (ENDOMYOCARDIAL FIBROSIS or AMYLOIDOSIS) causing interstitial fibrosis.		02.110
Cystic Kidney Diseases
[description not available]		02.0210
Kidney Diseases, Cystic
A heterogeneous group of hereditary and acquired disorders in which the KIDNEY contains one or more CYSTS unilaterally or bilaterally (KIDNEY, CYSTIC).		02.0210
Arrhythmia
[description not available]		07.0210
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		02.0210
Angor Pectoris
[description not available]		02.0210
Angina Pectoris
The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.		02.0210
Hypothermia, Accidental
[description not available]		03.4111
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		03.4111
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		02.4420
Dilatation, Pathologic
The condition of an anatomical structure's being dilated beyond normal dimensions.		04.3411
Chronic Bronchitis
[description not available]		02.0410
Bacterial Endocarditides
[description not available]		02.0410
Endocarditis, Bacterial
Inflammation of the ENDOCARDIUM caused by BACTERIA that entered the bloodstream. The strains of bacteria vary with predisposing factors, such as CONGENITAL HEART DEFECTS; HEART VALVE DISEASES; HEART VALVE PROSTHESIS IMPLANTATION; or intravenous drug use.		02.0410
Thromboembolism
Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.		02.0410
Bronchitis, Chronic
A subcategory of CHRONIC OBSTRUCTIVE PULMONARY DISEASE. The disease is characterized by hypersecretion of mucus accompanied by a chronic (more than 3 months in 2 consecutive years) productive cough. Infectious agents are a major cause of chronic bronchitis.		02.0410