Page last updated: 2024-12-04

bromazepam

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Description

Bromazepam: One of the BENZODIAZEPINES that is used in the treatment of ANXIETY DISORDERS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2441
CHEMBL ID277062
CHEBI ID31302
SCHEMBL ID43933
MeSH IDM0002929

Synonyms (80)

Synonym
unii-x015l14v0o
5-26-05-00078 (beilstein handbook reference)
x015l14v0o ,
bromazepamum
2h-1, 7-bromo-1,3-dihydro-5-(2-pyridyl)-
ro 5-3350
lectopam
lekotam
lexotanil
ro 4-9253
1812-30-2
2h-1, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-
nsc-140669
7-bromo-1,4-benzodiazepin-2-one
bromazepam
lexaurin
la xvii
ro 53350
wln: t67 gmv jn ihj ce k- bt6nj
7-bromo-5-(2-pyridyl)-3h-1,4-benzodiazepin-2(1h)-one
compedium
nsc140669
lexilium
creosedin
lexotan
calmepam
lexomil
1,3-dihydro-7-bromo-5-(2-pyridyl)-2h-1,4-benzodiazepin-2-one
2h-1,4-benzodiazepin-2-one, 1,3-dihydro-7-bromo-5-(2-pyridyl)-
bromazepam [usan:inn:ban:jan]
dea no. 2748
brn 0618645
einecs 217-322-4
7-bromo-1,3-dihydro-5-(2-pyridyl)-2h-1,4-benzdiazepin-2-one
2h-1,4-benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridyl)-
bromazepamum [latin]
ultramidol
compendium
normoc
bromazepamum [inn-latin]
durazanil
nsc 140669
2h-1,4-benzodiazepin-2-one, 7-bromo-1,3-dihydro-5-(2-pyridinyl)-
DB01558
bromazepam (jp17/usan/inn)
lectopam (tn)
7-bromo-1,3-dihydro-5-(2-pyridyl)-2h-1,4-benzodiazepin-2-one
D01245
CHEMBL277062
ro-5-3350
bromazepam civ
lexatin
7-bromo-5-pyridin-2-yl-1,3-dihydro-1,4-benzodiazepin-2-one
7-bromo-5-(2-pyridyl)-3h-1,4-benzodiaxepin-2(1h)-one
MLS003899212
smr000058724
SCHEMBL43933
bromazepam [usan]
bromazepam [jan]
bromazepam civ [usp-rs]
bromazepam [inn]
bromazepam [mart.]
bromazepam [mi]
bromazepam [ep monograph]
bromazepam [who-dd]
7-bromo-5-(pyridin-2-yl)-1h-benzo[e][1,4]diazepin-2(3h)-one
7-bromo-5-(2-pyridinyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-one #
7-bromo-5-[2-pyridyl]-3h-1,4-benzodiaxepin-2[1h]-one
DTXSID40171081
7-bromo-5-(pyridin-2-yl)-2,3-dihydro-1h-1,4-benzodiazepin-2-one
bromazepam, analytical standard
bromazepam, european pharmacopoeia (ep) reference standard
bromazepam, drug standard, 1.0 mg/ml in methanol
CHEBI:31302
bromazepam, united states pharmacopeia (usp) reference standard
bromazepam 0.1 mg/ml in methanol
bromazepam 1.0 mg/ml in methanol
(e)-7-bromo-5-(pyridin-2-yl)-1h-benzo[e][1,4]diazepin-2(3h)-one
Q422435
bromazepam, 1mg/ml in methanol

Research Excerpts

Overview

Bromazepam is a benzodiazepine, widely employed in the treatment of anxiety. It appears to be a quick-acting, purely anxiolytic drug, with effects perceptible after 2 or 3 days.

ExcerptReferenceRelevance
"Bromazepam is a benzodiazepine, which has been widely employed in the treatment of anxiety. "( Absolute Theta Power in the Frontal Cortex During a Visuomotor Task: The Effect of Bromazepam on Attention.
Arias-Carrión, O; Bittencourt, J; Cagy, M; Gongora, M; Peressuti, C; Ribeiro, P; Teixeira, S; Velasques, B, 2015
)
2.08
"Bromazepam appears to be a quick-acting, purely anxiolytic drug, with effects perceptible after 2 or 3 days of the treatment."( [A clinical trial of bromazepam (author's transl)].
Kahn, JP; Laxenaire, M; Marchand, P, 1982
)
1.3
"Bromazepam appears to be a superior compound to other anxiolytic and psychovegetatively active minor tranquillisers on account of its mild hypnotic action."( [Bromazepam in the treatment of somatized psychogenic disorders (author's transl)].
Jellinger, K; Podiwinsky, F, 1979
)
1.89

Effects

ExcerptReferenceRelevance
"Bromazepam has the pharmacokinetic characteristics of benzodiazepines with half-life values between 20 and 30 hours."( Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol.
Burstein, ES; Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Ochs, HR; Shader, RI, 1987
)
2.44

Actions

ExcerptReferenceRelevance
"The bromazepam enhance the luminescence intensity of the Eu(3+) ion in Eu(3+)-bromazepam complex at lambda(ex)=390nm."( Spectrofluorimetric quantification of bromazepam using a highly selective optical probe based on Eu3+-bromazepam complex in pharmaceutical and serum samples.
Attia, MS, 2009
)
1.1

Pharmacokinetics

The time course of the pharmacodynamic effects of bromazepam on the central nervous system was assessed using a subjective rating of sedation, continuous number addition test and electroencephalography up to 21.

ExcerptReferenceRelevance
"82 ml/min/kg) and prolonged elimination half-life (29 vs."( Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol.
Burstein, ES; Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Ochs, HR; Shader, RI, 1987
)
1.72
" The pharmacokinetic parameters elimination half-life, maximum plasma concentration and area under the curve were not significantly different."( [Comparative studies on biologic availability and pharmacokinetics of bromazepam in tablets].
Barkworth, MF; Fenzl, E; Johnson, KI; Rehm, KD; von Stetten, O, 1983
)
0.5
"Large differences exist among the various benzodiazepines with regard to their pharmacokinetic properties and metabolism in man."( Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles.
Breimer, DD; Jochemsen, R, 1984
)
0.27
" Pharmacodynamic effects of bromazepam were assessed using self-rated drowsiness, continuous number addition test, and EEG."( Effect of fluconazole on the pharmacokinetics and pharmacodynamics of oral and rectal bromazepam: an application of electroencephalography as the pharmacodynamic method.
Hirose, Y; Kotegawa, T; Morimoto, T; Nakano, S; Ohtani, Y; Tsutsumi, K, 2002
)
0.83
" The time course of the pharmacodynamic effects of bromazepam on the central nervous system was assessed using a subjective rating of sedation, continuous number addition test and electroencephalography up to 21."( The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers.
Kotegawa, T; Kuwatani, K; Nakano, S; Oda, M; Ohtani, Y; Tsutsumi, K, 2003
)
0.8
" The mean (+/-SD) values of area under the plasma concentration-time curve and elimination half-life for placebo versus itraconazole were 1328+/-330 ng h/ml versus 1445+/-419 ng h/ml and 32."( The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers.
Kotegawa, T; Kuwatani, K; Nakano, S; Oda, M; Ohtani, Y; Tsutsumi, K, 2003
)
0.55
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

The relative bioavailability of a liquid oral form of 7-bromo-1,3-dihydro-5-(2-pyridyl)-2H- 1,4-benzodiazepin-2-one was investigated. The effect of food on the rate and extent ofBioavailability of bromazepam was examined in seven normal volunteers.

ExcerptReferenceRelevance
"The effect of food on the rate and extent of bioavailability of bromazepam was examined in seven normal volunteers following a single oral dose of 10 mg bromazepam with 200 ml of water in the fasting and non-fasting states."( Effect of food on the bioavailability of bromazepam following oral administration in healthy volunteers.
Fujii, J; Inotsume, N; Nakano, M, 1990
)
0.78
" The determination of cerebral bioavailability utilizing time- and dose-efficacy relations, as well as the evaluation of bioequipotency of different formulations of compounds is shown."( Topographic brain mapping of EEG in neuropsychopharmacology--Part II. Clinical applications (pharmaco EEG imaging).
Anderer, P; Grünberger, J; Kinsperger, K; Saletu, B, 1987
)
0.27
"Ten male volunteers participated in a randomized crossover trial to compare the bioavailability of bromazepam (7-bromo-1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one) from two different preparations (Normoc, the test preparation, and a commercially available standard preparation)."( [Comparative studies on biologic availability and pharmacokinetics of bromazepam in tablets].
Barkworth, MF; Fenzl, E; Johnson, KI; Rehm, KD; von Stetten, O, 1983
)
0.72
"The relative bioavailability of a liquid oral form of 7-bromo-1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one (bromazepam, Lexotan, Lexotanil) in comparison with the conventional oral form (capsules) was investigated."( Bioavailability of bromazepam in man after single administration of an oral solution.
Ascalone, V; Cisternino, M; De Palo, E; Sicolo, N, 1984
)
0.81
" Since the 90% CI for both, AUC and Cmax ratios were within the 80-125% interval proposed by the Food and Drug Administration, it is concluded that the new bromazepam slow-release formulation is therapeutic equivalent to the conventional formulation for both, the extent and the rate of absorption after single dose administration in healthy volunteers."( Comparative bioavailability of two oral formulations of bromazepam in healthy volunteers.
Batafarano, N; Casas, F; Glancszpigel, R; Lerner, FE; Schere, D, 2001
)
0.75
" The comparison of different experimental conditions for establishing a dissolution profile in vitro along with our bioavailability data further allowed us to propose rationally based experimental conditions for a dissolution test of bromazepam tablets, actually lacking a pharmacopeial monograph."( On-line solid-phase extraction coupled with high-performance liquid chromatography and tandem mass spectrometry (SPE-HPLC-MS-MS) for quantification of bromazepam in human plasma: an automated method for bioequivalence studies.
Caminha, R; Gonçalves, JC; Gonçalves, Mdo R; Gram, KR; Monteiro, TM; Neves, CS; Noël, F; Santos, FM; Silva, VA; Silveira, GE; Volpato, NM, 2005
)
0.71
"The results of this study show that the nasogastric route of administration does not appear to cause marked, clinically unsuitable alterations in the bioavailability of the tested drugs."( The bioavailability of bromazepam, omeprazole and paracetamol given by nasogastric feeding tube.
Berger-Gryllaki, M; Buclin, T; Pannatier, A; Podilsky, G; Roulet, M; Testa, B, 2009
)
0.66
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36

Dosage Studied

In a double-blind study, fifty-five healthy, male medical students received a tranquilizer (bromazepam, 'Lexotanil') or placebo according to dosage group. Antipyrine pharmacokinetics were studied immediately before bromazepsam was administrat.

ExcerptRelevanceReference
" The prompt clinical response to bromazepam contributed to its superior safety and patient progress in that it was possible to carefully titrate dosage and thus help to control adverse reactions and allow patients to maintain alertness and productivity under therapy."( Controlled comparison of bromazepam, amitriptyline, and placebo in anxiety-depressive neurosis.
Shammas, E, 1977
)
0.84
" The optimum daily dosage was three times 3 mg; the duration of treatment ranged from 1 week to 34 months."( [Bromazepam in the treatment of somatized psychogenic disorders (author's transl)].
Jellinger, K; Podiwinsky, F, 1979
)
1.17
" After four weeks the dosage was reduced in 25% quantities until no further benzodiazepines were taken."( A double-blind comparison of the effects of gradual withdrawal of lorazepam, diazepam and bromazepam in benzodiazepine dependence.
Murphy, SM; Tyrer, P, 1991
)
0.5
" With regard to all active treatments the incidence of side effects was lower on Day 7 after the subchronic dosing period--with a third of the subchronic dose--than after the first single administration."( Placebo-controlled study on acute and subchronic effects of buspirone vs bromazepam utilizing psychomotor and cognitive assessments in healthy volunteers.
Klausnitzer, W; Schaffler, K, 1989
)
0.51
" Topographic pharmaco-EEG seems not only to confirm our previous knowledge that quantitative analysis of the human EEG in combination with certain statistical procedures ("quantitative pharmaco-EEG") is a valuable method to determine if, how, when and at which dosage a drug will be centrally effective, but also to have the potential to show effects of psychotropic drugs on the target organ--the human brain--which could not be previously picked up by single lead recordings."( Topographic brain mapping of EEG in neuropsychopharmacology--Part II. Clinical applications (pharmaco EEG imaging).
Anderer, P; Grünberger, J; Kinsperger, K; Saletu, B, 1987
)
0.27
" A control group of twelve subjects received a placebo according to the same dosage pattern."( Free fatty acids, central nervous system and bromazepam.
Kondou, I; Levis, G; Moulopoulos, S; Papageorgiou, C, 1982
)
0.52
" The mean effective dosage was 18 mg/day."( [Clinical trial of bromazepam in psychiatric hospital practice (author's transl)].
Brunner, H; Patris, MF, 1982
)
0.59
" The initial dosage (6 mg/day) was modified according to anxiolytic response and sedative effects."( [Bromazepam in the treatment of anxiety in nephrology and haemodialysis (author's transl)].
Jahn, H; Schmitt, R; Schohn, D, 1982
)
1.17
" Side-effects mostly consisted of sedation which regressed spontaneously or after dosage was reduced."( [Treatment of anxiety with bromazepam in clinical practice (author's transl)].
Benoudich, H; Bornstein, S; Kaufman, E; Konqui, M; Pigeon, P, 1982
)
0.56
" Dosage ranged from 6 to 18 mg/day."( [Clinical trial of bromazepam. Thirty-four cases (author's transl)].
Brion, S; Horseau, C, 1982
)
0.59
" Precise information was obtained concerning the optimal dosage and duration of treatment and the incidence of untoward reactions."( [Results of a cooperative study of bromazepam involving 3.401 ambulatory psychiatric patients and 8.191 patients from general practice (author's transl)].
Perrier, F, 1982
)
0.54
" From these data, significant differences of the pharmacological effects between oral and rectal administration of bromazepam were recognized in the duration of action and, in part, potencies; and therefore, rectal administration of bromazepam may be a useful dosage form for clinical use."( [Pharmacological action of bromazepam suppository].
Aida, Y; Fujii, Y; Gomita, Y; Goto, M; Ichimaru, Y; Kasama, T; Mayuzumi, K; Mayuzumi, Y; Moriyama, M, 1983
)
0.77
" Such differences may be very important clinically because pharmacokinetic data will help to optimize drug therapy with respect to the choice of the proper drug and drug preparation, as well as with the choice of a proper dose and dosage regimen."( Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles.
Breimer, DD; Jochemsen, R, 1984
)
0.27
" Antipyrine pharmacokinetics were studied immediately before bromazepam administration was started, after the dosing schedule had been completed and one week after dosing had been discontinued."( The effect of bromazepam (Lexotan) administration on antipyrine pharmacokinetics in humans.
Allen, JG; Bird, HA; Ehsanullah, RS; Galloway, DB; Ruane, RJ, 1984
)
0.87
" Its use was associated with the lowest incidence of adverse reactions and best dosage compliance."( Bromazepam, a new anxiolytic: a comparative study with diazepam in general practice. Royal College of General Practitioners Medicines Surveillance Organisation.
, 1984
)
1.71
" Although the expected anxiolytic EEG profile was not observed (increased beta and decreased alpha activity), this specific result may be related to other factors such as dosage used and the subjects' general physiological state, and not necessarily to the drug itself."( The influence of bromazepam on cortical power distribution.
Cagy, M; Piedade, R; Puga, F; Ribeiro, P; Sampaio, I; Veiga, H, 2008
)
0.69
" Information for health professionals and workers in forensic structures as well as education of the general population associated with preventive measures such as drug dosage form changes should contribute to improved care management of victims and decreased risk."( Chemical submission: results of 4-year French inquiry.
Burin, E; Dally, S; Djezzar, S; Questel, F, 2009
)
0.35
" However, this does not appear to be clinically relevant given the usual dosage range and the drug's half-life (approx."( The bioavailability of bromazepam, omeprazole and paracetamol given by nasogastric feeding tube.
Berger-Gryllaki, M; Buclin, T; Pannatier, A; Podilsky, G; Roulet, M; Testa, B, 2009
)
0.66
" The determination of BMZ in pharmaceutical dosage forms was conducted with the described method and showed mean percentage recovery of 99."( Development and validation of a stability indicating RP-HPLC-DAD method for the determination of bromazepam.
Abdelrahman, MM; Al-Hossaini, AM; Ali, NA; Darwish, HW; El Ghobashy, MR; Naguib, IA, 2021
)
0.84
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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]

Bioassays (54)

Assay IDTitleYearJournalArticle
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1147966CNS activity in po dosed unanesthesized cat assessed as muscle relaxant activity1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID29344Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1147963CNS activity in po dosed mouse assessed as reduction in fighting behaviour1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1147965Anticonvulsant activity in po dosed mouse assessed as protection against maximal electroshock-induced seizures1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID27575HPLC capacity factor (k)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID1261691Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.
AID29421Partition coefficient (logP) (HPLC)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1147962CNS activity in po dosed mouse assessed as reduction in muscle relaxant activity by inclined screening method1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID27580Partition coefficient (logP)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1660982Inhibition of Escherichia coli Stx2 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation at 30 uM incubated with cells for 4 hrs prior to Stx2 addition and further incubated for 20 hrs and s2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1147964Anticonvulsant activity in po dosed mouse assessed as protection against pentylenetetrazole-induced seizures1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26380Dissociation constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (337)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990171 (50.74)18.7374
1990's45 (13.35)18.2507
2000's66 (19.58)29.6817
2010's43 (12.76)24.3611
2020's12 (3.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 109.38

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 Index109.38 (24.57)
Research Supply Index6.20 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index201.43 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (109.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials112 (29.55%)5.53%
Reviews6 (1.58%)6.00%
Case Studies71 (18.73%)4.05%
Observational1 (0.26%)0.25%
Other189 (49.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Trimebutine Maleate (NEWBUTIN SR 300 mg Tab) as a Prophylactic Anti-emetic Drug for Patients Who Underwent Arthroscopic Rotator Cuff Repair: a Randomized Controlled Study [NCT01984931]Phase 345 participants (Anticipated)Interventional2013-10-31Recruiting
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]