Page last updated: 2024-11-04

carvedilol

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Carvedilol is a nonselective beta blocker with vasodilating properties. It is used to treat hypertension and heart failure. Carvedilol is synthesized through a multi-step process involving reactions like alkylation, condensation, and cyclization. It acts by blocking beta-adrenergic receptors in the heart and blood vessels, which reduces heart rate, blood pressure, and myocardial oxygen demand. Carvedilol's vasodilating effect is attributed to its ability to block alpha1-adrenergic receptors, leading to smooth muscle relaxation. The importance of carvedilol lies in its efficacy in treating both hypertension and heart failure, and its favorable side effect profile compared to other beta-blockers. Carvedilol is studied extensively to understand its mechanisms of action, optimize its therapeutic benefits, and explore its potential applications in other cardiovascular diseases.'

Cross-References

ID SourceID
PubMed CID2585
CHEMBL ID723
CHEBI ID3441
SCHEMBL ID22293
SCHEMBL ID10082334
SCHEMBL ID13287211
MeSH IDM0127291

Synonyms (182)

Synonym
AC-1641
CHEBI:3441 ,
carvedilolum
1-(9h-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol
AKOS005554967
HMS3269N11
HMS3393N03
BRD-A10977446-001-04-8
BRD-A10977446-045-01-1
gtpl551
artist
kredex
dibloc
dilatrend
dq-2466
dimitone
eg-p042
eucardic
coropress
sk&f-105517
querto
1-(9h-carbazol-4-yloxy)-3-[(2-{[2-(methyloxy)phenyl]oxy}ethyl)amino]propan-2-ol
dq 2466
bm-14190
bm 14190
SPECTRUM_001665
coreg
2-propanol, 1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-, (+-)-
hsdb 7044
(+-)-1-(carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol
carvedilolum [latin]
skf 105517
SPECTRUM5_001436
bdbm25759
chembl723 ,
[3-(9h-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine
MLS001424092
C06875
CARVEDILOL ,
72956-09-3
smr000449280
MLS000759508
MLS000758299
DB01136
D00255
artist (tn)
coreg (tn)
carvedilol (jp17/usp/inn)
KBIO2_004713
KBIO2_007281
KBIOGR_001252
KBIO3_002323
KBIO2_002145
KBIOSS_002145
SPECTRUM3_001182
SPECTRUM2_001673
SPBIO_001885
SPECTRUM4_000636
NCGC00167832-02
NCGC00167832-01
HMS2089B09
HMS2051N03
HMS2093E12
C2260
1-(9h-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
NCGC00167832-03
bm 14.190
skf-105517
bm-14-190
c07ag02
bm-14.190
talliton
nsc-758694
korvasan
coronis
L001243
FT-0652640
FT-0664397
1-(9h-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
STK621453
HMS3261E15
0k47ul67f2 ,
carvedilol [usan:usp:inn:ban:jan]
unii-0k47ul67f2
nsc 758694
nsc758694
pharmakon1600-01504257
BCP9000493
CCG-100917
HY-B0006
CS-1194
BCP0726000253
carvedilol-methyl-d3
FT-0603057
FT-0603055
NCGC00167832-04
LP00347
S1831
carvedilol [usan]
carvedilol [mart.]
carvedilol [ep monograph]
1-(carbazol-4-yloxy)-3-((2-(o-methoxy-phenoxy)ethyl)amino)-2-propanol
2-propanol, 1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-, (+/-)-
carvedilol [who-dd]
(+/-)-1-carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol
carvedilol [mi]
carvedilol [orange book]
carvedilol [hsdb]
carvedilol [inn]
carvedilol [jan]
carvedilol [usp monograph]
carvedilol [vandf]
carvedilol [usp-rs]
CCG-207952
AB00639903-07
OGHNVEJMJSYVRP-UHFFFAOYSA-N
1-(9h-carbazol-4-yloxy)-3-[2-(2-methoxy-phenoxy)-ethylamino]-propan-2-ol
NC00167
BBL029064
SCHEMBL22293
KS-1037
AB00639903-09
tox21_500347
NCGC00261032-01
1-((9h-carbazol-4-yl)oxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol
SCHEMBL10082334
MLS006011886
Q-200801
SCHEMBL13287211
AB00639903_11
AB00639903_10
AB00639903_12
mfcd00864692
DTXSID8022747 ,
carvedilol, >=98% (hplc), solid
SR-01000759289-5
SR-01000759289-6
sr-01000759289
SR-01000759289-9
carvedilol, united states pharmacopeia (usp) reference standard
HMS3655O14
carvedilol, european pharmacopoeia (ep) reference standard
carvedilol for system suitability, european pharmacopoeia (ep) reference standard
carvedilol, pharmaceutical secondary standard; certified reference material
carvedilol 1.0 mg/ml in methanol
SBI-0206771.P001
HMS3715D15
SW197547-3
Q412534
SY129821
F19969
HMS3677B14
107741-96-8
BCP23386
HMS3413B14
ethyl 2-(9-(pyridin-4-ylmethyl)-9h-fluoren-9-yl)acetate
BRD-A10977446-001-05-5
1-(9h-carbazol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol
EX-A5746
SB17441
SDCCGSBI-0206771.P002
HMS3884E12
NCGC00167832-19
AMY40801
HMS3750I15
bm14190
SY283162
mfcd00869664
BC164291
carvedilol - bio-x
(+/-)-carvedilol-d4
carvedilol (ep monograph)
carvedilol (usp-rs)
carvedilolum (latin)
carvedilol (usan:usp:inn:ban:jan)
carvedilol (usp monograph)
carvedilolo
carvedilol (mart.)
(2rs)-1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol
dtxcid602747
1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol
Z1515383337

Research Excerpts

Overview

Carvedilol (CAR) is a widely studied, beta and alpha-1 blocker, antihypertensive drug due to its poor water solubility and low oral bioavailability (25-35%) It is a nonspecific β-blocker clinically used for the treatment of cardiovascular diseases but has also been shown to have profound effects on excitation-contraction coupling and Ca signaling.

ExcerptReferenceRelevance
"Carvedilol is a uniquely effective drug for the treatment of cardiac arrhythmias in patients with heart failure. "( Novel carvedilol analogues that suppress store-overload-induced Ca2+ release.
Back, TG; Chen, SR; Smith, CD; Vembaiyan, K; Wang, A; Wu, G; Xie, C; Zhang, J; Zhou, Q, 2013
)
2.31
"Carvedilol (CAR) is a strategic beta-blocker agent which its application has been limited by its very low water solubility. "( Design of ultra-fine carvedilol nanococrystals: Development of a safe and stable injectable formulation.
Hadidi, M; Iman Ghetmiri, S; Mohammady, M; Yousefi, G, 2021
)
2.38
"Carvedilol (CAR) is a widely studied, beta and alpha-1 blocker, antihypertensive drug due to its poor water solubility and low oral bioavailability (25-35%). "( Mixed micelles formulation for carvedilol delivery: In-vitro characterization and in-vivo evaluation.
Arslan, FB; Çalış, S; Öztürk, K; Öztürk, SC, 2022
)
2.45
"Carvedilol is a nonspecific β-blocker clinically used for the treatment of cardiovascular diseases but has also been shown to have profound effects on excitation-contraction coupling and Ca signaling at the cellular level. "( Mechanism of carvedilol induced action potential and calcium alternans.
Blatter, LA; Kanaporis, G; Martinez-Hernandez, E, 2022
)
2.53
"Carvedilol is a commonly used antihypertensive whose oral absorption is limited by low solubility and significant first-pass metabolism. "( Chemometric optimization of salting-out assisted liquid-liquid extraction (SALLE) combined with LC-MS/MS for the analysis of carvedilol enantiomers in human plasma: Application to clinical pharmacokinetics.
de Gaitani, C; de Moraes, N; Dos Santos, J; Kemp, R; Moreira da Silva, R; Pavan, M; Salgado Junior, W; Sankarankutty, A; Yamamoto, P, 2022
)
2.37
"Carvedilol is an adrenergic receptor antagonist with pronouncedantioxidant and anti-inflammatory activity."( Carvedilol attenuates brain damage in mice with hepatic encephalopathy.
Amirshahrokhi, K; Niapour, A, 2022
)
2.89
"Carvedilol is a nonselective β & α1 blocker with additional effects as an antioxidant, anti-inflammatory and neuro protective properties."( Neuroprotective repositioning and anti-tau effect of carvedilol on rotenone induced neurotoxicity in rats: Insights from an insilico& in vivo anti-Parkinson's disease study.
Ahmed, HI; Albohy, A; Azab, SS; Kamal, RE; Menze, E, 2022
)
1.69
"Carvedilol is a non-selective beta-blocker (NSBB) acting on hyperdynamic circulation/splanchnic vasodilation and on intrahepatic resistance."( Carvedilol as the new non-selective beta-blocker of choice in patients with cirrhosis and portal hypertension.
La Mura, V; Reiberger, T; Turco, L; Vitale, G, 2023
)
3.07
"Carvedilol is an adrenergic receptor antagonist."( Remyelinating activities of Carvedilol or alpha lipoic acid in the Cuprizone-Induced rat model of demyelination.
Ahmed, KA; Ibrahim Fouad, G, 2023
)
1.93
"Carvedilol (CAR) is a third-generation β-adrenergic receptor antagonist with an α1-blocking effect."( Repurposing of carvedilol to alleviate bleomycin-induced lung fibrosis in rats: Repressing of TGF-β1/α-SMA/Smad2/3 and STAT3 gene expressions.
Abbas, NAT; Abdelmageed, AF; Afifi, R; Hassan, HA; Mohammed, HO; Nafea, OE; Samy, W, 2023
)
1.98
"Carvedilol is a poorly water-soluble drug employed to treat chronic heart failure. "( Synthesis and Characterization of Carvedilol-Etched Halloysite Nanotubes Composites with Enhanced Drug Solubility and Dissolution Rate.
Bruni, G; Capsoni, D; Conti, DM; Ferrara, C; Friuli, V; Maggi, L; Urru, C, 2023
)
2.63
"Carvedilol is a beta-adrenergic receptor antagonist primarily metabolized by cytochromes P450 (CYP) 2D6. "( Population Pharmacokinetic-Pharmacodynamic Modeling of Carvedilol to Evaluate the Effect of Cytochrome P450 2D6 Genotype on the Heart Rate Reduction.
Chung, JY; Hwang, S; Lee, S; Yoon, J, 2023
)
2.6
"Carvedilol is a poorly water-soluble drug used to treat cardiovascular problems; it is commercialized in several countries only as solid oral formulations, which are often manipulated at the point of administration to treat pediatric or geriatric patients."( Flexible New Dosage Forms Containing Carvedilol for the Treatment of Patients with Cardiovascular Disorders: Development, Stability, Palatability, and Microbiological Studies.
Leonardi, D; Maggio, R; Operto, MA; Vignaduzzo, S, 2023
)
1.9
"Carvedilol is a widely used beta-adrenoreceptor antagonist for multiple cardiovascular indications; however, it may induce cholestasis in patients, but the mechanism for this effect is unclear. "( Carvedilol impairs bile acid homeostasis in mice: implication for nonalcoholic steatohepatitis.
Alaei Faradonbeh, F; Bayer, RL; Dohnalkova, E; Dusek, J; Faistova, H; Hirsova, P; Hroch, M; Hyspler, R; Kucera, O; Lastuvkova, H; Micuda, S; Mokry, J; Nova, Z; Pavek, P; Schreiberova, J; Stefela, A, 2023
)
3.8
"Carvedilol is a nonselective beta-blocker used to reduce portal hypertension. "( Carvedilol Inhibits Angiotensin II-Induced Proliferation and Contraction in Hepatic Stellate Cells through the RhoA/Rho-Kinase Pathway.
Li, Z; Wang, S; Wu, Y; Xiu, A; Zhang, C, 2019
)
3.4
"Carvedilol is an FDA-approved β-blocker commonly used for treatment of high blood pressure, congestive heart failure, and cardiac tachyarrhythmias, including atrial fibrillation. "( Effect of carvedilol on atrial excitation-contraction coupling, Ca
Blatter, LA; Martinez-Hernandez, E, 2020
)
2.4
"Carvedilol is a third-generation β-adrenoceptor antagonist, which also stimulates β-arrestins. "( Metabolic effects of carvedilol through β-arrestin proteins: investigations in a streptozotocin-induced diabetes rat model and in C2C12 myoblasts.
Güven, B; Kara, Z; Onay-Beşikci, A, 2020
)
2.32
"Carvedilol acts as a biased ligand to promote β1AR coupling to a Gi-PI3K-Akt-nitric oxide synthase 3 (NOS3) cascade and induces robust β1AR-cGMP-PKG signal."( Carvedilol induces biased β1 adrenergic receptor-nitric oxide synthase 3-cyclic guanylyl monophosphate signalling to promote cardiac contractility.
Barbagallo, F; Deng, B; Liu, Y; Reddy, GR; Shi, Q; Wang, Q; Wang, Y; Wei, W; West, TM; Xiang, YK; Xu, B, 2021
)
2.79
"Carvedilol is a β-blocker used in the management of cardiovascular disorders, anxiety, migraine and chemotherapy-induced cardiotoxicity."( Carvedilol blocks neural regulation of breast cancer progression in vivo and is associated with reduced breast cancer mortality in patients.
Andreassen, BK; Baker, JG; Botteri, E; Chang, A; Chung, NC; Gillis, RD; Halls, ML; Pon, CK; Shackleford, DM; Sloan, EK; Ziegler, AI, 2021
)
2.79
"Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. "( Dual Activity of Hydroxypropyl-β-Cyclodextrin and Water-Soluble Carriers on the Solubility of Carvedilol.
Geng, T; Wang, B; Zoghbi, A, 2017
)
2.12
"Carvedilol is an effective additional therapy for the patients with chronic heart failure already receiving Amiodarone."( THE SAFETY AND EFFICACY OF AMIODARONE AND CARVEDILOL COMBINATION IN TREATMENT OF PATIENTS WITH SEVERE CARDIAC RHYTHM DISORDERS.
Khintibidze, I; Tsetskhladze, E, 2017
)
1.44
"Carvedilol is a β-blocker used to treat high blood pressure and heart failure."( Carvedilol abrogates hypoxia-induced oxidative stress and neuroinflammation in microglial BV2 cells.
Fu, Z; Gao, X; Wu, B; Xu, G; Zhang, Z, 2017
)
2.62
"Carvedilol is a rising nonselective beta-blocker used for reducing portal pressure with favorable outcome."( Efficacy of carvedilol versus propranolol versus variceal band ligation for primary prevention of variceal bleeding.
Abd ElRahim, AY; Elsharkawy, A; Fathalah, W; Fouad, R; Khairy, M; Khatamish, H; Khorshid, O; Moussa, M; Seyam, M, 2018
)
1.58
"Carvedilol is a good pharmaceutical alternative medicine to propranolol with lesser side-effects."( Efficacy of carvedilol versus propranolol versus variceal band ligation for primary prevention of variceal bleeding.
Abd ElRahim, AY; Elsharkawy, A; Fathalah, W; Fouad, R; Khairy, M; Khatamish, H; Khorshid, O; Moussa, M; Seyam, M, 2018
)
1.58
"Carvedilol is a non-selective, third-generation beta-blocker and is one of the cornerstones for treatment for patients with heart failure and reduced ejection fraction (HFrEF). "( Assessment of clinical effect and treatment quality of immediate-release carvedilol-IR versus SLOW release carvedilol-SR in Heart Failure patients (SLOW-HF): study protocol for a randomized controlled trial.
Choi, DJ; Hong, SJ; Hong, SK; Jeon, ES; Kang, SM; Kim, EJ; Kim, JJ; Kim, MA; Kim, SY; Lee, HY; Park, CS; Park, DG; Park, JJ; Shin, JH; Yoo, BS, 2018
)
2.16
"Carvedilol is a non-selective β-adrenoreceptor antagonist and exhibits a wide range of biological activities. "( Characterization and molecular basis for the block of Kv1.3 channels induced by carvedilol in HEK293 cells.
Cheng, N; Li, XT; Liu, XM; Ren, S; Yang, JF, 2018
)
2.15
"Carvedilol is a clinically effective β-blocker broadly used for treating congestive heart failure (CHF), and several clinical trials have demonstrated that it shows a favourable effect compared with other β-blockers in patients with CHF. "( Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels by β-blocker carvedilol.
Cao, Y; Chen, S; Liang, Y; Liu, S; Pang, J; Wu, T; Zhou, P, 2018
)
2.15
"Carvedilol is a negative gating modulator of HCN channels. "( Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels by β-blocker carvedilol.
Cao, Y; Chen, S; Liang, Y; Liu, S; Pang, J; Wu, T; Zhou, P, 2018
)
2.15
"Carvedilol (CVL) is an α-, β-blocker used to treat high blood pressure and congestive heart failure; however, some benefits beyond decreased blood pressure were observed clinically, suggesting the potential anti-inflammatory activity of CVL."( Repositioning of the β-Blocker Carvedilol as a Novel Autophagy Inducer That Inhibits the NLRP3 Inflammasome.
Chen, A; Cheng, CC; Cheng, SM; Hua, KF; Li, LH; Lin, WY; Rao, YK; Wong, WT; Yang, SP, 2018
)
1.49
"Carvedilol is a non-selective beta-blocker with additional intrinsic alpha"( Carvedilol versus traditional, non-selective beta-blockers for adults with cirrhosis and gastroesophageal varices.
Bendtsen, F; Gluud, LL; Hobolth, L; Jeyaraj, R; Morgan, MY; Zacharias, AP, 2018
)
2.64
"Carvedilol (CAR) is a β-blocker used to treat high blood pressure and heart failure."( Carvedilol (CAR) combined with carnosic acid (CAA) attenuates doxorubicin-induced cardiotoxicity by suppressing excessive oxidative stress, inflammation, apoptosis and autophagy.
Yang, JJ; Zhang, HS; Zhang, QL, 2019
)
2.68
"Carvedilol is an antioxidant that decreases inflammation in periodontitis. "( Anti-inflammatory potential of a carvedilol gel in the pulpal tissue of rats after dental bleaching: A histopathological evaluation.
Benetti, F; Briso, ALF; Cintra, LTA; de Castilho Jacinto, R; Dezan-Júnior, E; Louzada, LM; Vieira, LB, 2019
)
2.24
"Carvedilol is a first‑line pharmacological treatment of PHT."( Carvedilol improves liver cirrhosis in rats by inhibiting hepatic stellate cell activation, proliferation, invasion and collagen synthesis.
Li, G; Li, Z; Ling, L; Meng, D; Wang, G; Zhang, C, 2019
)
2.68
"Carvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris."( Bioequivalence and pharmacokinetic evaluation of two tablet formulations of carvedilol 25-mg: a single-dose, randomized-sequence, open-label, two-way crossover study in healthy Chinese male volunteers.
Chen, Q; Jia, JY; Liu, GY; Liu, Y; Lu, C; Lu, XP; Wang, W; Yu, C; Zhang, MQ, 2013
)
2.06
"Carvedilol is a β-blocker used as a multifunctional neurohormonal antagonist that has been shown to act not only as an anti-oxidant but also as an anti-inflammatory drug."( Carvedilol decrease IL-1β and TNF-α, inhibits MMP-2, MMP-9, COX-2, and RANKL expression, and up-regulates OPG in a rat model of periodontitis.
de Araújo Júnior, RF; de Araújo, AA; de Lucena, HF; de Medeiros, CA; de Souza, LB; do Socorro Costa Feitosa Alves, M; Freitas, Mde L; Souza, TO, 2013
)
2.55
"Carvedilol is a non-selective β blocker with alpha-1 adrenergic blocker activity."( Carvedilol vs. esophageal variceal band ligation in the primary prophylaxis of variceal hemorrhage: a multicentre randomized controlled trial.
Abid, S; Azam, Z; Hamid, S; Ismail, FW; Jafri, W; Khalid, A; Munir, SM; Parkash, O; Rauf, J; Shah, HA; Subhan, A, 2014
)
2.57
"Carvedilol is a nonselective beta-blocker with a mild anti-alfa-1-adrenergic activity."( Systematic review with meta-analysis: the haemodynamic effects of carvedilol compared with propranolol for portal hypertension in cirrhosis.
D'Amico, G; D'Amico, M; Perricone, G; Sinagra, E; Tinè, F, 2014
)
1.36
"Carvedilol is a non-selective β-adrenergic blocker with anti-inflammatory, antioxidant, and multiple cationic channel blocking properties."( Carvedilol for prevention of atrial fibrillation after cardiac surgery: a meta-analysis.
Wang, HS; Wang, ZW; Yin, ZT, 2014
)
2.57
"Carvedilol is a vasodilating non-selective β-blocker with alpha-1 receptor and calcium channel antagonism."( Multicentre randomised controlled study comparing carvedilol with variceal band ligation in the prevention of variceal rebleeding.
Dickson, S; Forrest, EH; Gaya, DR; Hayes, PC; Leithead, JA; MacBeth, K; Mills, PR; Smith, L; Stanley, AJ; Suzuki, H; Tripathi, D; Young, D, 2014
)
1.38
"Carvedilol is a novel β-adrenoreceptor blocker, with antioxidant properties inhibiting lipid peroxidation and preventing the depletion of endogenous antioxidants. "( Antiapoptotic and antioxidant effects of carvedilol and vitamin E protect against diabetic nephropathy and cardiomyopathy in diabetic Wistar albino rats.
Abdel-Raheem, MH; Al-Rifaay, A; Hasan-Ali, H; Mosad, E; Salama, HS; Salim, SU, 2015
)
2.13
"Carvedilol is an anti-hypertensive agent capable of blocking both alph (α) and beta (β) receptors used to preclude cardiac arrhythmias and angina. "( Assessment of sex differences in Pharmacokinetics of carvedilol in human.
Abbas, M; Khan, AM; Nawaz, HA; Riffat, S; Tipu, MY; Usman, M, 2014
)
2.09
"Carvedilol is a third-generation β-blocker indicated for congestive heart failure and high blood pressure. "( Dose proportionality and pharmacokinetics of carvedilol sustained-release formulation: a single dose-ascending 10-sequence incomplete block study.
Bae, KS; Choi, HY; Kim, C; Kim, YH; Lee, SH; Lim, HS; Noh, YH, 2015
)
2.12
"Carvedilol (CRV) is an antihypertensive drug with both alpha and beta receptor blocking activity used to preclude angina and cardiac arrhythmias. "( Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge.
Arzani, G; Bakhtiari-Kaboutaraki, H; Dadashzadeh, S; Daeihamed, M; Haeri, A, 2015
)
2.11
"Carvedilol is an antihypertensive drug with non-selective blockade (moderate selectivity for β1 and β2 adrenoceptors) and vasodilating properties due to α receptor blockade. "( Evaluation and correlation of the physicochemical properties of carvedilol.
Alves, JM; Prado, LD; Rocha, HV, 2016
)
2.12
"Carvedilol (CAR) is a potent antihypertensive drug but has poor oral bioavailability (24%). "( Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration.
Abdelbary, AA; Abdelrahim, ME; Al-mahallawi, AM; Ali, AM, 2015
)
2.09
"Carvedilol functions as a nonselective β-adrenergic receptor (AR)/α1-AR antagonist that is used for treatment of hypertension and heart failure. "( Carvedilol binding to β2-adrenergic receptors inhibits CFTR-dependent anion secretion in airway epithelial cells.
Maniak, PJ; O'Grady, SM; Peitzman, ER; Zaidman, NA, 2016
)
3.32
"Carvedilol is a drug widely used in the treatment of heart failure and associated cardiac arrhythmias. "( Suppression of store overload-induced calcium release by hydroxylated metabolites of carvedilol.
Back, TG; Chen, SR; Malig, T; Xiao, Z, 2016
)
2.1
"Carvedilol is an antihypertensive drug, which is available in clinical practice as a racemic mixture. "( Chiral analysis of carvedilol and its metabolites hydroxyphenyl carvedilol and O-desmethyl carvedilol in human plasma by liquid chromatography-tandem mass spectrometry: Application to a clinical pharmacokinetic study.
Coelho, EB; Lanchote, VL; Marques, MP; Nardotto, GHB, 2016
)
2.21
"Carvedilol (CAR) is a poorly water-soluble beta-blocker. "( Novel carvedilol paediatric nanomicelle formulation: in-vitro characterization and in-vivo evaluation.
Bernabeu, E; Bertera, FM; Buontempo, F; Cagel, M; Chiappetta, DA; Höcht, C; Moretton, MA; Parola, L; Taira, CA; Wegmann, M, 2017
)
2.38
"Carvedilol is a nonselective beta and alpha-adrenergic blocking agent that has been shown to possess powerful antioxidant and anti-inflammatory properties."( Carvedilol attenuates paraquat-induced lung injury by inhibition of proinflammatory cytokines, chemokine MCP-1, NF-κB activation and oxidative stress mediators.
Amirshahrokhi, K; Khalili, AR, 2016
)
2.6
"Carvedilol is a nonselective third generation β-blocker that does not display the negative effects of traditional β-blockers. "( Role of antioxidant property of carvedilol in mild to moderate hypertensive patients: A prospective open-label study.
Assareh, AR; Ayashi, S; Jalali, MT; Olapour, S; Yaghooti, H,
)
1.86
"Carvedilol is a drug of choice in treatment of portal hypertension. "( Antifibrotic Effects of Carvedilol and Impact of Liver Fibrosis on Carvedilol Pharmacokinetics in a Rat model.
Abdel-Sattar, SA; El-Bakly, WM; El-Demerdash, E; Mohamed, EA, 2017
)
2.2
"Carvedilol is a drug used to treat heart failure, hypertension, and coronary artery diseases . "( Carvedilol-loaded nanocapsules: Mucoadhesive properties and permeability across the sublingual mucosa.
Beck, RC; Chaves, PD; Frank, LA; Guterres, SS; Ourique, AF; Pohlmann, AR, 2017
)
3.34
"Carvedilol is an antihypertensive drug, has also been appreciated for its antioxidant and mitoprotective properties."( Carvedilol prevents functional deficits in peripheral nerve mitochondria of rats with oxaliplatin-evoked painful peripheral neuropathy.
Areti, A; Komirishetty, P; Kumar, A, 2017
)
2.62
"Carvedilol (CV) is an antagonist of alpha1 and beta1,beta2 membrane adrenoceptors and also a modulator of cardiac electrophysiological properties. "( HPLC analysis, isolation and identification of a new degradation product in carvedilol tablets.
Antoniadou-Vyza, E; Galanopoulou, O; Rozou, S, 2008
)
2.02
"Carvedilol is a non-selective beta-adrenoreceptor antagonist that is also an antagonist at the alpha(1)-adrenoreceptor. "( Carvedilol overdose with quantitative confirmation.
Bouchard, NC; Forde, J; Hoffman, RS, 2008
)
3.23
"Carvedilol is a non-selective beta-blocker which, besides its neuroprotective and vasculoprotective properties, has cardioprotective and antioxidant effects."( Carvedilol as a protector against the cardiotoxicity induced by anthracyclines (doxorubicin).
Cabral, A; Gonçalves, L; Machado, V; Monteiro, P; Providência, LA, 2008
)
2.51
"Carvedilol is a beta(1)- and beta(2)-adrenergic receptor antagonist with additional vasodilatory alpha(1)-blocking properties. "( Role of carvedilol controlled-release in cardiovascular disease.
Fonarow, GC, 2009
)
2.23
"Carvedilol is an option for primary prophylaxis in patients with high-risk esophageal varices."( Randomized controlled trial of carvedilol versus variceal band ligation for the prevention of the first variceal bleed.
Ferguson, JW; Forrest, EH; Hayes, PC; Hislop, WS; Kochar, N; Leithead, JA; McAvoy, NC; Mills, PR; Stanley, AJ; Therapondos, G; Tripathi, D, 2009
)
1.36
"Carvedilol is a potent noncardioselective beta-blocker, with weak vasodilating properties because of alpha 1 blockade. "( The role of carvedilol in the management of portal hypertension.
Hayes, PC; Tripathi, D, 2010
)
2.18
"Carvedilol is an anti-heart failure agent that is used to induce cardiac reverse remodeling, and its effect is reportedly dose-dependent."( High-dose carvedilol therapy for mechanical circulatory assisted patients.
Kyo, S; Nishimura, T, 2010
)
1.48
"Carvedilol is a third-generation beta-blocker, with the S-enantiomer being more active than the R-enantiomer. "( Proteomic profiling of cellular responses to Carvedilol enantiomers in vascular smooth muscle cells by iTRAQ-coupled 2-D LC-MS/MS.
Chen, WN; Ching, CB; Wang, M; Wang, X, 2010
)
2.06
"Carvedilol is a beta-adrenoceptor antagonist used for treating chronic heart failure (CHF). "( Population pharmacokinetics of R- and S-carvedilol in Japanese patients with chronic heart failure.
Hanada, K; Kaneko, M; Kawana, J; Mihara, K; Nagayama, M; Ogata, H; Ohno, T; Saito, M; Shiomi, M; Sumiyoshi, T, 2010
)
2.07
"Carvedilol is a β-antagonist with strong anti-oxidant effect in lipids, proteins and superoxide production protecting biological membranes from oxidative stress. "( Carvedilol treatment reduces transthyretin deposition in a familial amyloidotic polyneuropathy mouse model.
Batista, AR; Macedo, B; Magalhães, J; Saraiva, MJ, 2010
)
3.25
"Carvedilol is a nonselective β-adrenoceptor and selective α(1)-adrenoceptor blocker and is widely used in the treatment of patients with hypertensive and/or chronic heart failure because, unlike classic β-blockers, this drug has additional endothelium-dependent vasodilatory effects. "( The effects of carvedilol administration on cardiopulmonary resuscitation in a rat model of cardiac arrest induced by airway obstruction.
Kurita, A; Taniguchi, T; Yamamoto, K, 2010
)
2.16
"Carvedilol is an antihypertensive drug with potent anti-oxidant properties."( Carvedilol protects tubular epithelial cells from ischemia-reperfusion injury by inhibiting oxidative stress.
De Velasco, MA; Hayashi, T; Ishii, T; Nishioka, T; Nose, K; Saitou, Y; Uemura, H, 2010
)
2.52
"Carvedilol is a non-selective β-blocker indicated in the treatment of hypertension and heart failure. "( Metabolomic profiling of cellular responses to carvedilol enantiomers in vascular smooth muscle cells.
Bai, J; Chen, WN; Ching, CB; Wang, M, 2010
)
2.06
"Carvedilol is an antioxidant that inhibits smooth muscle cell proliferation and migration. "( Two-year clinical outcome after carvedilol-loaded stent implantation in patients with coronary artery disease.
Ahn, Y; Cho, JG; Hong, YJ; Jeong, MH; Kang, JC; Kim, HK; Kim, JH; Kim, KH; Kim, SS; Kim, W; Ko, JS; Lee, MG; Park, HW; Park, JC; Park, KH; Sim, DS; Yoon, HJ; Yoon, NS, 2011
)
2.1
"Carvedilol is an effective treatment in hypertension and chronic heart failure. "( Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics.
Brockmöller, J; Gültepe, S; Meineke, I; Sehrt, D; Tzvetkov, M, 2011
)
3.25
"Carvedilol is a drug where CYP2D6-related pharmacokinetic variation is apparently not carried forward into pharmacodynamic variation. "( Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics.
Brockmöller, J; Gültepe, S; Meineke, I; Sehrt, D; Tzvetkov, M, 2011
)
3.25
"Carvedilol is a non-selective β- and α-blocker enantiomer with antioxidant effects that are attributed to its carbazole moiety."( Novel design and synthesis of modified structure of carvedilol.
Hashemzadeh, M; Hill, DN; Movahed, MR; Russu, WA; Soroush, L, 2011
)
1.34
"Carvedilol is an antihypertensive drug available as a racemic mixture. "( Analysis of carvedilol enantiomers in human plasma using chiral stationary phase column and liquid chromatography with tandem mass spectrometry.
Bertucci, C; Coelho, EB; Da Silva, FG; Lanchote, VL; Marques, MP; Poggi, JC, 2012
)
2.2
"Carvedilol is a non-selective β-blocker with intrinsic anti-α(1)-adrenergic activity, potentially more effective than propranolol in reducing hepatic venous pressure gradient (HVPG). "( Carvedilol or propranolol in portal hypertension? A randomized comparison.
Bendtsen, F; Feldager Hansen, E; Grønbæk, H; Hobolth, L; Møller, S; Roelsgaard, K, 2012
)
3.26
"Carvedilol is a nonselective β-blocker with α1-adrenergic blocking and antioxidant properties. "( The mechanism of carvedilol in experimental viral myocarditis.
Jia-Feng, L; Li-Sha, G; Xue-Qiang, G; Yue-Chun, L, 2012
)
2.16
"Carvedilol (CRV) is an important medicament for heart arrhythmia. "( Solvent effect on the vibrational spectra of Carvedilol.
Billes, F; Marosi, G; Mikosch, H; Pataki, H; Unsalan, O; Vajna, B, 2012
)
2.08
"Carvedilol is a vasodilating noncardioselective third-generation β-blocker, without the negative hemodynamic and metabolic effects of traditional β-blockers, which can be used as a cardioprotective agent."( Use of carvedilol in hypertension: an update.
Egan, CG; Leonetti, G, 2012
)
1.56
"Carvedilol is a novel third generation non-selective β-blocker."( Combined use of direct renin inhibitor and carvedilol in heart failure with preserved systolic function.
Afonso, L; Ali Kizilbash, M; Badheka, AO; Bharadwaj, A; Rathod, A; Tuliani, TA, 2012
)
1.36
"Carvedilol is a non-selective β-blocker with α₁-adrenergic receptor antagonism properties."( A critical review of the use of carvedilol in ischemic heart disease.
Abrencillo, R; Chen-Scarabelli, C; Di Rezze, J; Faggian, G; Gardin, T; Gidwani, UK; Murad, Y; Qureshi, W; Saravolatz, L; Scarabelli, TM; Shieh, WS, 2012
)
1.38
"Carvedilol is an adrenergic antagonist which has been safely used in treatment of several cardiovascular disorders."( Carvedilol alleviates adjuvant-induced arthritis and subcutaneous air pouch edema: modulation of oxidative stress and inflammatory mediators.
Arab, HH; El-Sawalhi, MM, 2013
)
2.55
"Carvedilol is a medication with both beta-receptor and alpha-receptor blocking properties that has been approved for the treatment of heart failure in adults. "( The Pediatric Randomized Carvedilol Trial in Children with Heart Failure: rationale and design.
Boucek, MM; Burch, GH; Burr, J; Curtin, EL; Hsu, DT; LaSalle, B; Mahony, L; Pahl, E; Schlencker-Herceg, R; Shaddy, RE; Sower, B; Tani, LY, 2002
)
2.06
"Carvedilol is a nonselective beta-adrenoceptor antagonist with additional alpha 1-receptor-blocking properties."( [Hormonal hyperactivity in heart failure. Differences in beta blockers].
Beuckelmann, DJ, 2002
)
1.04
"Carvedilol is a cardiovascular drug of multifaceted therapeutic potential, with beta-blocker and vasodilatative activity. "( Carvedilol: something else than a simple betablocker?
Auteri, A; Calabria, P; Palazzuoli, A; Verzuri, MS,
)
3.02
"Carvedilol is a multiple action, non-specific, adrenergic beta-blocker, licensed for the treatment of mild, moderate and severe chronic heart failure. "( Use of carvedilol in the treatment of heart failure.
Coats, A, 2003
)
2.22
"Carvedilol is a non-selective beta-blocker with alpha-receptor blockade and antioxidant properties."( Chronic treatment with carvedilol improves ventricular function and reduces myocyte apoptosis in an animal model of heart failure.
Doye, AA; Gwathmey, JK; Hajjar, RJ; Jabbour, G; Laste, N; Lebeche, D; Lee, MX; Okafor, CC; Perreault-Micale, C; Skiroman, K, 2003
)
1.35
"Carvedilol is a combined alpha(1)- and beta-adrenoceptor antagonist. "( Carvedilol blockade of rat myocardial alpha1-adrenoceptors.
Bøkenes, J; Osnes, JB; Qvigstad, E; Sandnes, D; Schiander, I; Sjaastad, I; Skomedal, T, 2003
)
3.2
"Carvedilol is a beta/alpha1-adrenoceptor blocker. "( Measurement of carvedilol in plasma by high-performance liquid chromatography with electrochemical detection.
Kakinoki, S; Machida, M; Nomura, A; Takechi, S; Watanabe, M, 2003
)
2.11
"Carvedilol is an alpha(1)/beta-adrenoceptor antagonist with antioxidant, neuroprotective, cardioprotective and vascularprotective properties, and is used to treat hypertension, myocardial ischaemia and congestive heart failure."( Carvedilol improves energy production during acute global myocardial ischaemia.
Duarte, AI; Gonçalves, LM; Monteiro, P; Moreno, A; Providência, LA, 2003
)
2.48
"Carvedilol is a safe complement to standard therapy for heart failure in children, allowing a significant reduction of neurohormonal activation with evident benefits on both ventricular function and the clinical condition."( Modulation of neurohormonal activity after treatment of children in heart failure with carvedilol.
Bonvicini, M; Bronzetti, G; Donti, A; Formigari, R; Giardini, A; Picchio, FM; Prandstraller, D, 2003
)
1.98
"Carvedilol appears to be a potentially viable option for treating portal hypertension."( Evaluation of carvedilol for the treatment of portal hypertension.
Hemstreet, BA, 2004
)
1.41
"Carvedilol is a direct inhibitor of vascular smooth muscle cell migration and proliferation through inhibition of mitogen-activated protein kinase activity and regulation of cell cycle progression. "( Comparison between a sustained administration of carvedilol versus atenolol to reduce restenosis after coronary stenting.
Cha, KS; Kim, DI; Kim, DS; Kim, HJ; Kim, JS; Kim, JW; Kim, MH, 2004
)
2.02
"Carvedilol is a nonselective beta- and alpha(1)-receptor antagonist with additional antioxidant properties in vitro. "( Effects of carvedilol on oxidative stress in human endothelial cells and healthy volunteers.
Böger, RH; Fahlbusch, SA; Frölich, JC; Gutzki, FM; Mehls, C; Stichtenoth, DO; Tsikas, D, 2004
)
2.16
"Carvedilol is a third-generation, neurohormonal antagonist with multiple activities. "( Pharmacology of carvedilol.
Abraham, WT; Dulin, B, 2004
)
2.11
"Carvedilol is a beta-adrenoceptor blocker with a vasodilatory action that is more effective for the treatment of congestive heart failure than other beta-blockers. "( Beta-adrenoceptor blocker carvedilol provides cardioprotection via an adenosine-dependent mechanism in ischemic canine hearts.
Asakura, M; Asano, Y; Asanuma, H; Hori, M; Kim, J; Kitakaze, M; Kitamura, S; Liao, Y; Minamino, T; Mori, H; Node, K; Ogai, A; Ogita, H; Sanada, S; Shinozaki, Y; Shintani, Y; Takashima, S; Tomoike, H, 2004
)
2.07
"Carvedilol is an adrenergic antagonist with nonselective beta- and a1-receptor blocking properties that has demonstrated significant clinical benefit in the management of patients with heart failure and in the post-myocardial infarction setting. "( Carvedilol: beta-blockade and beyond.
Gheorghiade, M; Stroe, AF, 2004
)
3.21
"Carvedilol is a useful cardiovascular drug for treating heart failure, however, the in vitro effect on many cell types is unclear. "( Effect of carvedilol on Ca2+ movement and cytotoxicity in human MG63 osteosarcoma cells.
Jan, CR; Liu, CP, 2004
)
2.17
"Carvedilol is an adrenergic blocking agent with potent anti-oxidant activity."( Carvedilol prevents doxorubicin-induced free radical release and apoptosis in cardiomyocytes in vitro.
Altieri, P; Ballestrero, A; Barsotti, A; Brunelli, C; Fabbi, P; Garibaldi, S; Ghigliotti, G; Manca, V; Nasti, S; Patrone, F; Rossettin, P; Spallarossa, P, 2004
)
2.49
"Carvedilol is a nonselective beta-blocker with alpha(1)-adrenergic blocking activity."( Acute administration of carvedilol is more effective than propranolol plus isosorbide-5-mononitrate in the reduction of portal pressure in patients with viral cirrhosis.
Hou, MC; Huang, YT; Lee, FY; Lee, SD; Lin, HC; Yang, YY, 2004
)
1.35
"Carvedilol is an inherently long-acting beta-blocker while the duration of beta blockade for metoprolol is dependent on the salt and formulation, which is used."( Pharmacokinetics and pharmacodynamics of beta blockers in heart failure.
Talbert, RL, 2004
)
1.04
"Carvedilol is an antioxidant and adrenergic antagonist with demonstrated benefits in terms of mortality from heart failure (HF). "( [Effects of carvedilol on functional capacity, left ventricular function, catecholamines and oxidative stress in patients with chronic heart failure].
Castro, P; Chiong, M; Corbalán, R; Díaz-Araya, G; Greig, D; Lavandero, S; Moraga, F; Padilla, I; Pérez, O; Troncoso, R; Vukasovic, JL, 2004
)
2.15
"Carvedilol is an antioxidant that inhibits smooth muscle cell proliferation and migration, whereas probucol is a vascular protectant and reduces stent restenosis by improving the lumen dimension at the stent placement site."( Effect of anti-oxidant (carvedilol and probucol) loaded stents in a porcine coronary restenosis model.
Ahn, YK; Cha, KS; Cho, JG; Hong, YJ; Hur, SH; Hyun, DW; Jeong, MH; Kang, JC; Kim, JH; Kim, KB; Kim, MH; Kim, W; Park, HW; Park, JC; Park, JT, 2005
)
1.36
"Carvedilol is a neurohormonal antagonist of multiple action which is used in clinical practice for the treatment of congestive heart failure, mild to moderate hypertension and myocardial infarction. "( Advantages in the use of carvedilol versus propranolol for the protection of cardiac mitochondrial function.
Gonçalves, L; Monteiro, P; Moreno, AJ; Oliveira, PJ; Palmeira, CM; Providência, LA; Rolo, AP; Sardão, VA, 2004
)
2.07
"Carvedilol is a beta-adrenoceptor blocker and a potent antioxidant that improves cardiac function in patients with heart failure. "( Carvedilol effectively blocks oxidative stress-mediated downregulation of sarcoplasmic reticulum Ca2+-ATPase 2 gene transcription through modification of Sp1 binding.
Arai, M; Koitabashi, N; Kurabayashi, M; Nagai, R; Niwano, K; Periasamy, M; Takizawa, T; Tomaru, K; Watanabe, A; Wuytack, F; Yokoyama, T, 2005
)
3.21
"Carvedilol is a beta- and alpha-adrenergic-blocking drug with clinically important antiarrhythmic properties. "( Carvedilol's antiarrhythmic properties: therapeutic implications in patients with left ventricular dysfunction.
Lukas, MA; Naccarelli, GV, 2005
)
3.21
"Carvedilol is a combined alpha(1)- and beta-adrenoceptor antagonist. "( Carvedilol blockade of alpha1- and beta-adrenoceptor induced inotropic responses in rats with congestive heart failure.
Bøkenes, J; Osnes, JB; Qvigstad, E; Schiander, I; Sejersted, OM; Sjaastad, I; Skomedal, T; Solberg, L, 2005
)
3.21
"Carvedilol is a beta-blocking agent with antioxidant properties that has been shown to improve survival in chronic heart failure (CHF). "( Effects of carvedilol on myocardial sympathetic innervation in patients with chronic heart failure.
Abergel, E; Berdeaux, A; Cohen-Solal, A; Le Guludec, D; Merlet, P; Rouzet, F; Syrota, A, 2005
)
2.16
"Carvedilol (CV) is a beta-blocker with favorable effects on cardiovascular disease. "( Suppression of hyperglycemia-induced superoxide formation and endothelin-1 gene expression by carvedilol.
Haas, MJ; Horani, MH; Mooradian, AD,
)
1.79
"Carvedilol is known to be an adrenoreceptor blocker and free radical scavenger, used in hypertension and cardiac failure. "( Carvedilol action is dependent on endogenous production of nitric oxide.
Afonso, RA; Carmo, MM; Macedo, MP; Patarrao, RS, 2006
)
3.22
"Carvedilol is a nonselective beta-adrenoceptor blocker with multiple pleiotropic actions. "( Pleiotropic effects of the beta-adrenoceptor blocker carvedilol on calcium regulation during oxidative stress-induced apoptosis in cardiomyocytes.
Fukagawa, Y; Hara, M; Harada, N; Ikeda, Y; Kametani, R; Kawamura, S; Matsuzaki, M; Miura, T; Shibuya, M; Wang, R, 2006
)
2.03
"Carvedilol is a comprehensive beta(1)-, beta(2)-, and alpha(1)-adrenoreceptor blocker marketed as Dilatrend by F. "( Are generic formulations of carvedilol of inferior pharmaceutical quality compared with the branded formulation?
Merazzi, F; Salzmann, U; Smith, JC; Tarocco, G, 2006
)
2.07
"Carvedilol is a nonselective beta-blocker with alpha(1)-adrenergic blocking activity. "( Hemodynamic effects of one week of carvedilol administration on cirrhotic rats.
Hou, MC; Huang, YT; Lee, SD; Lee, TY; Lin, HC; Wang, YW; Wei, HC; Yang, YY, 2006
)
2.05
"Carvedilol is a non-selective adrenergic blocker with anti-inflammatory, antioxidant, and multiple cationic channel blocking properties."( Carvedilol versus Metoprolol for the prevention of atrial fibrillation after off-pump coronary bypass surgery: rationale and design of the Carvedilol or Metoprolol Post-Revascularization Atrial Fibrillation Controlled Trial (COMPACT).
Hayashi, Y; Kamei, M; Kanmura, Y; Kuro, M; Morita, S, 2006
)
2.5
"Carvedilol is an alpha1 and nonselective beta-adrenergic receptor antagonist with antioxidative properties known to protect endothelial function."( Carvedilol preserves endothelial junctions and reduces myocardial no-reflow after acute myocardial infarction and reperfusion.
Cui, C; Gao, R; Yang, Y; you, S; Zhao, J, 2007
)
2.5
"Carvedilol is an alpha-and beta-blocking agent with antioxidant properties. "( In vivo chronic carvedilol treatment in rats attenuates ex vivo regional infarction of the heart.
Hegna, S; Johansen, OE; Mjøs, OD; Munch-Ellingsen, J; Starkopf, J; Ytrehus, K, 2006
)
2.12
"Carvedilol is a racemic mixture of R(+) and S(-) enantiomers that combines beta(1)-, beta(2)-, and alpha(1)-adrenoceptor blockade."( Pharmacokinetic and pharmacodynamic comparison of controlled-release carvedilol and immediate-release carvedilol at steady state in patients with hypertension.
Baidoo, CA; Boyle, D; Campanile, AM; Danoff, TM; Harter, AH; Henderson, LS; Tenero, DM, 2006
)
1.29
"Carvedilol is a beta1-, beta2-, and alpha1-adrenergic blocker that is approved for the treatment of hypertension. "( Controlled-release carvedilol in the treatment of essential hypertension.
Bakris, GL; Fleck, R; Iyengar, M; Sica, DA; Tarka, EA; Weber, MA, 2006
)
2.1
"Carvedilol is a beta- and alpha(1)-adrenoceptor antagonist. "( Effects of carvedilol on transient outward and ultra-rapid delayed rectifier potassium currents in human atrial myocytes.
Deng, C; Kuang, S; Lin, S; Qian, W; Shan, Z; Wu, S; Yang, M; Yu, X; Zhang, K; Zhang, W; Zhou, Z, 2007
)
2.17
"Carvedilol is a third-generation beta(1)- and beta(2)-blocker that also possesses alpha(1)-adrenergic-blocking properties. "( Profile of carvedilol controlled-release: a new once-daily formulation of carvedilol.
Fonarow, GC, 2006
)
2.17
"Carvedilol is a beta-adrenergic antagonist with vasodilatory properties (alpha1-antagonism), which has been extensively evaluated in the treatment of patients with heart failure. "( Carvedilol: use in chronic heart failure.
Doughty, RN; White, HD, 2007
)
3.23
"Carvedilol is a beta-blocker with similar affinity for beta1- and beta2 receptors, while bisoprolol has higher beta1 affinity. "( Lung function with carvedilol and bisoprolol in chronic heart failure: is beta selectivity relevant?
Agostoni, P; Apostolo, A; Bussotti, M; Cattadori, G; Contini, M; Fiorentini, C; Palermo, P; Sciomer, S, 2007
)
2.11
"Carvedilol is a beta(1)-, beta(2)-, and alpha(1)-adrenoreceptor blocker indicated for treatment of hypertension and mild-to-severe congestive heart failure. "( Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate.
Boyle, DA; Eddington, ND; Fossler, MJ; Othman, AA; Tenero, DM, 2007
)
2.06
"Carvedilol is a nonselective ss-adrenergic receptor antagonist that also blocks alpha1-adrenergic receptors and is a potent antioxidant."( Prominent cardioprotective effects of third generation beta blocker nebivolol against anthracycline-induced cardiotoxicity using the model of isolated perfused rat heart.
Casamassimi, A; de Nigris, F; Fiorito, C; Napoli, C; Rienzo, M; Schiano, C, 2008
)
1.07
"Carvedilol (BM 14190) is a new compound with combined nonselective beta-adrenoceptor blocking activity, devoid of ISA, and a precapillary vasodilating effect. "( Acute haemodynamic effects of carvedilol (BM 14190), a new combined beta-adrenoceptor blocker and precapillary vasodilating agent, in hypertensive patients.
Andrén, L; Eggertsen, R; Hansson, L; Sivertsson, R, 1984
)
2
"Carvedilol (BM 14190) is a new antihypertensive compound which combines beta-adrenoceptor blocking and precapillary vasodilating properties but is devoid of intrinsic sympathomimetic activity. "( Haemodynamic effects of carvedilol, a new beta-adrenoceptor blocker and precapillary vasodilator in essential hypertension.
Andrén, L; Eggertsen, R; Hansson, L; Sivertsson, R, 1984
)
2.02
"Carvedilol is a safe, efficient, once/day choice as monotherapy for mild to moderate essential hypertensive patients."( [Use of carvedilol compared to nifedipine in the treatment of mild and moderate essential arterial hypertension].
Dantas, M; Freitas, AF; Furtado, MR; Kohlmann, NE; Kohlmann, O; Plavnik, FL; Portela, JE; Spritzer, N; Spritzer, T, 1994
)
2.17
"Carvedilol is a beta-adrenoceptor antagonist which also causes peripheral vasodilation primarily via alpha 1-adrenergic blockade. "( Carvedilol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Campoli-Richards, D; McTavish, D; Sorkin, EM, 1993
)
3.17
"Carvedilol is an antihypertensive agent which displays unselective beta-blocking, alpha 1-blocking and antioxidant properties. "( Antihypertensive treatment with a vasodilating beta-blocker, carvedilol, in chronic hemodialysis patients.
Deetjen, A; Heidland, A; Meyer-Sabellek, W; Pangerl, A; Schaefer, RM, 1995
)
1.98
"Carvedilol is a mildly beta 1-selective beta-adrenergic blocking agent with vasodilator properties. "( Carvedilol improves left ventricular function and symptoms in chronic heart failure: a double-blind randomized study.
Bristow, MR; Gilbert, EM; Olsen, SL; Renlund, DG; Taylor, DO; Yanowitz, FD, 1995
)
3.18
"Carvedilol is a mixed alpha- and beta-adrenergic receptor antagonist that is administered as a racemic mixture. "( Stereoselective disposition of carvedilol is determined by CYP2D6.
Wood, AJ; Zhou, HH, 1995
)
2.02
"Carvedilol is a new cardiovascular compound with the combined pharmacologic properties of nonselective beta-blockade and vasodilation. "( Comparison of a new vasodilating beta-blocker, carvedilol, with atenolol in the treatment of mild to moderate essential hypertension.
Ruilope, LM, 1994
)
1.99
"Carvedilol is an arylethanolamine that is a racemic mixture of 2 enantiomers. "( Clinical pharmacokinetics and pharmacodynamics of carvedilol.
Morgan, T, 1994
)
1.98
"Carvedilol is a nonselective beta-adrenoceptor blocking vasodilator drug that may be a promising new agent in the management of cardiovascular disease. "( A risk-benefit assessment of carvedilol in the treatment of cardiovascular disorders.
Conway, EL; Krum, H; Louis, WJ, 1994
)
2.02
"Carvedilol is a beta-adrenergic blocking agent with vasodilator activity that might be well tolerated in patients with heart failure."( Effects of short- and long-term carvedilol administration on rest and exercise hemodynamic variables, exercise capacity and clinical conditions in patients with idiopathic dilated cardiomyopathy.
Dei Cas, L; Giubbini, R; Metra, M; Nardi, M, 1994
)
2.01
"Carvedilol is a multiple action antihypertensive drug with potential use in angina and congestive heart failure. "( Myocardial protection by the novel vasodilating beta-blocker, carvedilol: potential relevance of anti-oxidant activity.
Cheng, HY; Feuerstein, GZ; Ruffolo, RR; Yue, TL, 1993
)
1.97
"Carvedilol is a nonselective beta-adrenoceptor antagonist, devoid of intrinsic sympathomimetic activity and possessing selective alpha 1-adrenoceptor-blocking activity, although this is considerably weaker than its beta-adrenoceptor antagonistic activity."( Pharmacodynamic profile of carvedilol.
van Zwieten, PA, 1993
)
1.3
"Carvedilol is a multiple-action cardiovascular agent that is a nonselective beta-adrenoceptor antagonist and a vasodilator. "( Cardioprotective potential of carvedilol.
Bril, A; Feuerstein, GZ; Ruffolo, RR, 1993
)
2.02
"Carvedilol is a beta blocker with alpha-blocking activity and its profile of action is similar to that of a combination of a beta blocker and a diuretic."( Carvedilol in hypertension.
Raftery, EB, 1993
)
2.45
"Carvedilol, which is a nonselective beta-blocking and alpha 1-blocking drug, with additional Ca(2+)-antagonistic properties, is being developed as an antihypertensive, antianginal drug and as an adjunct therapy in congestive heart failure."( Development of a multiaction beta blocker. Scientific challenges and regulatory needs.
Lessem, JN; Lukas, MA, 1993
)
1.01
"Carvedilol is a cardiovascular drug currently used for the treatment of hypertension. "( Carvedilol, a cardiovascular drug, prevents vascular smooth muscle cell proliferation, migration, and neointimal formation following vascular injury.
Arleth, A; Douglas, SA; Feuerstein, GZ; Louden, C; Ohlstein, EH; Poste, G; Ruffolo, RR; Sung, CP; Yue, TL, 1993
)
3.17
"Carvedilol is a novel multiple-action cardiovascular drug that has recently been introduced to the market for the treatment of mild to moderate hypertension. "( Preclinical and clinical pharmacology of carvedilol.
Boyle, DA; Lukas, MA; Ruffolo, RR; Venuti, RP, 1993
)
1.99
"Carvedilol is a non-selective beta-adrenoceptor antagonist with vasodilating properties which has been shown to be effective in the management both of hypertension and of stable angina pectoris. "( Vasodilating beta-blockers in heart failure.
Raftery, EB, 1995
)
1.73
"Carvedilol is a vasodilating, beta-adrenoceptor antagonist currently marketed for the treatment of mild to moderate hypertension. "( Carvedilol, a novel multiple action antihypertensive agent with antioxidant activity and the potential for myocardial and vascular protection.
Feuerstein, GZ; Ruffolo, RR, 1995
)
3.18
"Carvedilol is an adrenoceptor antagonist which modulates the activity not only of beta 1 and beta 2 but also of alpha 1 adrenergic receptors present on the cell surface membrane of the human cardiac myocyte. "( Cardiac adrenergic receptor effects of carvedilol.
Asano, K; Bouvier, M; Bristow, MR; Chidiak, P; Dutcher, D; Minobe, W; Port, JD; Roden, RL; Tremmel, KD; Yoshikawa, T, 1996
)
2.01
"Carvedilol is a vasodilating beta-blocker currently marketed for the treatment of mild to moderate hypertension and application is being filed to the FDA for treatment of congestive heart failure. "( Carvedilol, a novel vasodilating beta-blocker with the potential for cardiovascular organ protection.
Feuerstein, GZ; Ruffolo, RR, 1996
)
3.18
"Carvedilol is a new beta-adrenoceptor antagonist which also causes peripheral vasodilation primarily via alpha 1-adrenergic blockade."( [Balanced beta--alpha-blocker treatment with carvedilol in mild-moderate arterial hypertension].
Barra, M; Gigli, G; Orlandi, S; Perocchio, M; Rosolen, GA; Sacchetti, R; Vallebona, A, 1996
)
1.28
"Carvedilol is a multiple-acting compound with non-selective beta-adrenoceptor and selective alpha 1-adrenoceptor blocking activity, calcium channel blocking and anti-oxidant activity."( Carvedilol and its metabolites suppress endothelin-1 production in human endothelial cell culture.
Fyhrquist, F; Metsärinne, K; Saijonmaa, O, 1997
)
2.46
"Carvedilol is a novel, multiple-action cardiovascular drug that is currently approved in many countries for the treatment of hypertension. "( Pharmacology of carvedilol: rationale for use in hypertension, coronary artery disease, and congestive heart failure.
Feuerstein, GZ; Ruffolo, RR, 1997
)
2.09
"Carvedilol is a non selective beta-adrenoceptor antagonist which also causes peripheral vasodilation primarily via alpha 1-adrenergic blockade (Strein et al., 1987, McTavish et al., 1993). "( Carvedilol overdose.
Hantson, P; Lambermont, JY; Mahieu, P; Simoens, G, 1997
)
3.18
"Carvedilol is a novel beta blocker that is highly effective in the treatment of hypertension and congestive heart failure, and combines in one molecule a number of important pharmacologic properties."( Protective effects of carvedilol in the myocardium.
Bril, A; Feuerstein, GZ; Ruffolo, RR, 1997
)
1.33
"Carvedilol is a third-generation vasodilating beta-blocker initially approved for the treatment of hypertension. "( Recent observations with beta-adrenoceptor blockade. Beneficial effects in hypertension and heart failure.
Feuerstein, GZ; Ohlstein, EH; Ruffolo, RR, 1998
)
1.74
"Carvedilol is a new beta-blocker antihypertensive agent with vasodilating properties secondary to alpha 1-blocking activity. "( Results of therapy with carvedilol, a beta-blocker vasodilator with antioxidant properties, in hypertensive patients.
Frishman, W; Moser, M, 1998
)
2.05
"Carvedilol is a novel multiple-action neurohormonal antagonist that has been shown to be effective in the management of congestive heart failure."( Carvedilol: preclinical profile and mechanisms of action in preventing the progression of congestive heart failure.
Feuerstein, GZ; Ruffolo, RR, 1998
)
2.46
"Carvedilol is a novel antihypertensive agent. "( Carvedilol in the treatment of hypertension--a review of the clinical data base.
Hansson, L; Himmelmann, A, 1998
)
3.19
"Carvedilol is a recently introduced drug with multiple action with a non-selective beta-antiadrenergic and selective alpha1-antiadrenergic action used for treatment of mild to medium severe hypertension. "( [The effects of Carvedilol, a beta-blocker, in experimental ischemia-reperfusion kidney injury].
Bartosíková, L; Drápelová, L; Husek, K; Kuchtícková, S; Necas, J; Pavlícek, V, 1997
)
2.09
"Carvedilol is a novel cardiovascular drug of proven efficacy in the treatment of hypertension, angina, and heart failure. "( Novel mechanisms in the treatment of heart failure: inhibition of oxygen radicals and apoptosis by carvedilol.
Feuerstein, G; Ma, X; Ruffolo, RR; Yue, TL,
)
1.79
"Carvedilol is a multiple-action neurohormonal antagonist that is effective in slowing the progression of CHF."( Neurohormonal activation, oxygen free radicals, and apoptosis in the pathogenesis of congestive heart failure.
Feuerstein, GZ; Ruffolo, RR, 1998
)
1.02
"Carvedilol is a nonselective beta-receptor antagonist with vasodilating properties primarily due to selective alpha-1 antagonism. "( Effectiveness of three different doses of carvedilol for exertional angina. Carvedilol-Angina Study Group.
Dennish, G; Ferry, D; Krug-Gourley, S; Lukas, MA; Pickering, E; Smith, LK; Weiss, R, 1998
)
2.01
"Carvedilol is a non-selective beta-adrenergic blocking drug with vasodilatory properties that has been recently approved by the U.S."( Beta-blockers in heart failure. Do they improve the quality as well as the quantity of life?
Fowler, MB, 1998
)
1.02
"Carvedilol is a useful additional therapy for patients with chronic heart failure already receiving amiodarone. "( Efficacy and safety of carvedilol in patients with chronic heart failure receiving concomitant amiodarone therapy. Australia/New Zealand Heart Failure Research Collaborative Group.
Krum, H; MacMahon, S; Sharpe, N; Shusterman, N, 1998
)
2.05
"Carvedilol is a vasodilating beta-blocker and antioxidant approved for treatment of mild to moderate hypertension, angina, and congestive heart failure. "( Neuroprotective activities of carvedilol and a hydroxylated derivative: role of membrane biophysical interactions.
Feuerstein, G; Lysko, KA; Lysko, PG; Mason, PE; Mason, RP; Walter, MF; Webb, CL, 1998
)
2.03
"Carvedilol is a non-selective beta-blocker, and the only one, in recent clinical trials, to have shown a clear reduction in mortality. "( Carvedilol for heart failure: more than just a beta-blocker?
Cleland, JG,
)
3.02
"Carvedilol (CAR) is a vasodilating beta-blocker which also has antioxidant properties. "( Protective effects of carvedilol against doxorubicin-induced cardiomyopathy in rats.
Hayakawa, T; Matsui, H; Morishima, I; Numaguchi, Y; Okumura, K; Toki, Y, 1999
)
2.06
"Carvedilol is an alpha1 and nonselective beta-adrenergic receptor antagonist with antioxidative properties known to protect against reperfusion injury in the heart, brain, and kidneys. "( Carvedilol reduces ischaemic skeletal muscle necrosis.
Hvaal, K; Kirkeby, OJ; Mathisen, SR; Skjeldal, S; Svindland, A, 1999
)
3.19
"Carvedilol is an antihypertensive drug with properties that may be potentially beneficial for kidney graft recipients. "( Carvedilol treatment of kidney graft recipients with chronic rejection.
Backman, U; Fellström, B; Larsson, E; Vessby, B; Zezina, L, 1999
)
3.19
"Carvedilol is a noncompetitive inhibitor of this external NADH dehydrogenase with a K(i) of 15 microM."( Carvedilol inhibits the exogenous NADH dehydrogenase in rat heart mitochondria.
Moreno, AJ; Oliveira, PJ; Santos, DJ, 2000
)
2.47
"Carvedilol is a beta-adrenoceptor antagonist with multiple actions, which may contribute to superior cardioprotection in heart failure and myocardial infarction. "( Differential effects of carvedilol on norepinephrine release in normoxic and ischemic heart.
Görge, B; Hartmann, F; Katus, HA; Kurz, T; Richardt, D; Richardt, G; Tölg, R, 2000
)
2.06
"Carvedilol is a new-generation vasodilating beta-blocker with additional alpha1-adrenoceptor antagonism and an antiproliferative action, but it is not known if it is more beneficial than standard selective beta-blockers."( Effect of carvedilol in comparison with metoprolol on myocardial collagen postinfarction.
Chow, LT; Sanderson, JE; Wei, S, 2000
)
1.43
"Carvedilol is a relatively new drug with beta- and alpha 1-receptor blocking activity and antioxidant effects recently approved for the treatment of congestive heart failure (CHF). "( Steady-state pharmacokinetics of carvedilol and its enantiomers in patients with congestive heart failure.
Boike, S; Boyle, D; Brozena, S; Fesniak, HF; Ilson, B; Jorkasky, D; Tenero, D, 2000
)
2.03
"Carvedilol is a vasodilating beta-blocker and antioxidant approved for treatment of mild to moderate hypertension. "( A comparison of carvedilol and metoprolol antioxidant activities in vitro.
Gu, JL; Lysko, PG; Ohlstein, EH; Ruffolo, RR; Webb, CL; Yue, TL, 2000
)
2.1
"Carvedilol is a novel beta-blocker that also shows an antioxidant effect in vitro."( Carvedilol improves endothelium-dependent dilatation in patients with coronary artery disease.
Akita, H; Kanazawa, K; Matsuda, Y; Shiga, N; Terashima, M; Yokoyama, M, 2000
)
2.47
"Carvedilol is a beta-blocker with ancillary properties. "( Carvedilol versus other beta-blockers in heart failure.
Doggrell, SA, 2001
)
3.2
"Carvedilol is a unique cardiovascular drug of multifaceted therapeutic potential. "( Carvedilol: molecular and cellular basis for its multifaceted therapeutic potential.
Cheng, J; Kamiya, K; Kodama, I, 2001
)
3.2
"Carvedilol is a non-selective vasodilating beta-blocker with weak alpha1 receptor antagonism. "( Haemodynamic effects of acute and chronic administration of low-dose carvedilol, a vasodilating beta-blocker, in patients with cirrhosis and portal hypertension.
Hayes, PC; Lui, HF; Stanley, AJ; Therapondos, G; Tripathi, D, 2002
)
1.99
"Carvedilol is a relatively safe, effective portal hypotensive agent, both acutely and over 7 days, but not superior to propranolol, at least in Indians. "( Acute and 7-day portal pressure response to carvedilol and propranolol in cirrhotics.
Biswas, PK; Das, D; De, BK; Maity, AK; Majumdar, D; Mandal, SK; Sen, S, 2002
)
2.02
"Carvedilol is a novel non-selective beta-blocker without intrinsic sympathomimetic activity (ISA) and has vasodilating effect through blocking alpha 1 receptor."( [Effects of carvedilol on the hemodynamics and its tolerance in elderly patients].
Asai, T; Iguchi, A; Kanda, S; Koike, A; Kuzuya, M; Maeda, K, 2002
)
1.41
"Carvedilol is an adrenoceptor antagonist, which inhibits beta(1)-, beta(2)-, and alpha(1)-adrenergic receptors."( Rationale and design of the carvedilol or metoprolol European trial in patients with chronic heart failure: COMET.
Cleland, JG; Di Lenarda, A; Hanrath, P; J Remme, W; Komajda, M; Metra, M; Poole-Wilson, PA; Swedberg, K; Torp-Pedersen, C, 2002
)
1.33
"Carvedilol is a non-selective beta blocker with antioxidant properties approved for use in congestive heart failure."( Carvedilol: a nonselective beta blocking agent with antioxidant properties.
Book, WM,
)
2.3
"Carvedilol is a beta-blocker with additional vasodilating activity. "( Oral administration of carvedilol and prazosin inhibits the prostaglandin F2 alpha- and noradrenaline-induced contraction of human hand veins in vivo.
Beermann, C; Belz, GG; Schloos, J, 1992
)
2.04
"Carvedilol is a new multiple action agent displaying nonselective beta-blockade without intrinsic sympathicomimetic activity, alpha 1-adrenoceptor blockade (probably responsible for its vasodilator activity), and possibly also calcium antagonist properties."( Carvedilol and the kidney.
Dupont, AG, 1992
)
2.45
"Carvedilol is a new beta-blocking agent without ISA, which causes vasodilation primarily through an alpha 1-blockade."( Antihypertensive profile of carvedilol.
Agrawal, B; Meyer-Sabellek, W, 1992
)
1.3
"Carvedilol is a novel non-selective beta-blocker without intrinsic sympathomimetic activity possessing vasodilatory properties primarily due to an alpha 1-antagonism in the same dose range."( Comparison of the antihypertensive effects of carvedilol and metoprolol on resting and exercise blood pressure.
Agrawal, B; Franz, IW; Ketelhut, R; Wiewel, D, 1992
)
1.26
"Carvedilol is a vasodilating, beta-adrenoceptor blocking agent."( Carvedilol, a new antihypertensive, prevents oxidation of human low density lipoprotein by macrophages and copper.
Feuerstein, GZ; Lysko, PG; McKenna, PJ; Ruffolo, RR; Yue, TL, 1992
)
2.45
"Carvedilol is a nonselective beta-blocker with alpha-mediated vasodilating properties that has been shown to be effective in systemic hypertension, stable angina, and congestive heart failure (CHF). "( Effects of carvedilol on ventricular arrhythmias.
DasGupta, P; Lahiri, A; Müller-Beckmann, B; Senior, R; van der Does, R, 1992
)
2.12
"Carvedilol is a multiple-action cardiovascular agent that is both a beta-adrenoceptor antagonist and a vasodilator and has recently been made available for the treatment of mild-to-moderate hypertension. "( Myocardial protection with carvedilol.
Bril, A; Feuerstein, GZ; Hamburger, SA; Ruffolo, RR; Smith, EF, 1992
)
2.02
"Carvedilol is a beta-adrenergic-blocking drug with vasodilating properties. "( Alpha 1-blocking properties of carvedilol during acute and chronic administration.
Carugo, S; Cattaneo, BM; Giannattasio, C; Grassi, G; Mancia, G; Mangoni, AA; Seravalle, G; Zanchetti, A, 1992
)
2.01
"Carvedilol is an effective antihypertensive agent, and the hemodynamic mode of action reflects alpha 1- and beta 1-blocking activities."( Carvedilol in hypertension: effects on hemodynamics and 24-hour blood pressure.
Lund-Johansen, P; Nordrehaug, JE; Omvik, P; White, W, 1992
)
2.45
"Carvedilol is a dual-acting drug designed to produce two complementary effects: beta-blockade and vasodilation. "( Vasodilatory action of carvedilol.
Bartsch, W; Müller-Beckmann, B; Sponer, G; Strein, K, 1992
)
2.04
"Carvedilol is a high-affinity, slightly beta 1-selective competitive beta-blocking agent, with a KD for beta 1-receptors of approximately 4-5 nM and a selectivity of sixfold to 39-fold for beta 1-receptors rather than beta 2-receptors, depending on the method used to assess subtype potency."( Receptor pharmacology of carvedilol in the human heart.
Bristow, MR; Handwerger, D; Klein, J; Larrabee, P; Minobe, W; Müller-Beckmann, B; Port, JD; Roden, R; Skerl, L, 1992
)
1.31
"Carvedilol (Kredex) is a multiple action, antihypertensive agent that may also prove to be useful in the treatment of angina and congestive heart failure. "( Carvedilol (Kredex) reduces infarct size in a canine model of acute myocardial infarction.
Barone, FC; Feuerstein, GZ; Hamburger, SA; Ruffolo, RR, 1991
)
3.17
"Carvedilol is a new drug which possesses a balanced combination of vasodilatation and beta-blockade."( The effects of intravenous carvedilol, a new multiple action vasodilatory beta-blocker, in congestive heart failure.
Broadhurst, P; DasGupta, P; Lahiri, A, 1991
)
1.3
"Carvedilol is a novel treatment for hypertension, having a balanced pharmacology of vasodilation and beta-receptor blockade. "( A comparative study of carvedilol, slow-release nifedipine, and atenolol in the management of essential hypertension.
Ball, SG; Dixon, S; Hall, S; Hallman, RJ; Harvey, RE; Prescott, RI, 1991
)
2.03
"Carvedilol is a third-generation vasodilating beta-adrenoceptor antagonist with advantageous ancillary pharmacologic properties for the treatment of the patient with high blood pressure complicated by CAD."( Hypertension and coronary artery disease: a therapeutic challenge.
Taylor, SH, 1991
)
1
"Carvedilol is an effective antihypertensive drug that lowers blood pressure equally well in the young and the old."( The use of carvedilol in elderly hypertensive patients.
Adam, W; Anderson, A; Cripps, J; Morgan, TO, 1990
)
1.39
"Carvedilol is an alternative substance for lowering high blood pressure in elderly hypertensive patients."( Blood-pressure-lowering effect of carvedilol vs nitrendipine in geriatric hypertensives.
Hennig, M; Krönig, B; Machwirth, M; Müller-Beckmann, B; Staiger, C; Stienen, U; Widmann, L, 1990
)
1.28
"Carvedilol is a potent antihypertensive agent with a dual mechanism of action. "( The pharmacology of carvedilol.
Gellai, M; Hieble, JP; Nichols, AJ; Ruffolo, RR; Willette, RN, 1990
)
2.05
"Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. "( Assay and disposition of carvedilol enantiomers in humans and monkeys: evidence of stereoselective presystemic metabolism.
Fujimaki, M; Hakusui, H; Murakoshi, Y, 1990
)
2.03
"Carvedilol is an effective antihypertensive agent that can be used in people with essential hypertension in all age groups."( Pharmacokinetics of carvedilol in older and younger patients.
Adam, W; Anderson, A; Cripps, J; Morgan, T, 1990
)
1.32
"Carvedilol is a new beta-receptor blocking and vasodilating drug that is presently undergoing clinical trials in hypertension and coronary heart disease. "( Pharmacological profile of carvedilol as a beta-blocking agent with vasodilating and hypotensive properties.
Bartsch, W; Böhm, E; Müller-Beckmann, B; Sponer, G; Strein, K, 1987
)
2.01
"Carvedilol (BM 14190) is a new potent and well-tolerated beta-adrenoceptor antagonist with vasodilating properties. "( Circadian antihypertensive profile of carvedilol (BM 14190).
Distler, A; Gotzen, R; Meyer-Sabellek, W; Schulte, KL, 1987
)
1.99
"Carvedilol is a new compound that combines beta-receptor blockade and vasodilation in one molecule."( Antihypertensive compounds with combined actions.
Rahn, KH, 1987
)
0.99
"Carvedilol is a new substance displaying beta-sympatholytic and vasodilating activities in the same dose range. "( A new molecule with vasodilating and beta-adrenoceptor blocking properties.
Abshagen, U, 1987
)
1.72
"Carvedilol is a recently developed antihypertensive drug that combines in the same molecule a nonselective beta-adrenoceptor blocking effect and a vasodilating precapillary activity. "( Resting and postexercise hemodynamic effects of carvedilol, a beta-adrenergic blocker and precapillary vasodilator in hypertensive patients.
Boselli, L; Cuspidi, C; Leonetti, G; Rupoli, L; Sampieri, L; Terzoli, L; Zanchetti, A, 1987
)
1.97
"Carvedilol is an effective anti-anginal therapy and improves the quality of life."( Multiple action compounds in angina pectoris.
Freedman, SB; Kelly, DT, 1989
)
1
"Carvedilol (BM14190) is a new compound with combined properties of nonselective beta-adrenoceptor blockade, devoid of ISA, and precapillary vasodilatation. "( Hemodynamic effects of combined beta-adrenoceptor blockade and precapillary vasodilatation in hypertension.
Andrén, L; Eggertsen, R; Hansson, L; Sivertsson, R, 1985
)
1.71

Effects

Carvedilol has a significant effect on alleviating the biliary cirrhosis in mice, and its relevant mechanism may be that carvedilol inhibits the endoplasmic reticulum stress through the negative regulation of ATF4-CHOP, ATF6-CHop and IRE1-pJNK signaling pathways. CarvedilOL has a powerful antiarrhythmic effect after AMI, even in patients already treated with an ACE inhibitor.

Carvedilol CR has a clinically meaningful defined dose-dependent antihypertensive effect that persists throughout a 24-hour period. It has vasodilatory, antioxidant stress and anti-inflammatory effects and poses a vital role in addressing the issue of diabetic complications.

ExcerptReferenceRelevance
"Carvedilol has a significant effect on alleviating the biliary cirrhosis in mice, and its relevant mechanism may be that carvedilol inhibits the endoplasmic reticulum stress through the negative regulation of ATF4-CHOP, ATF6-CHOP and IRE1-pJNK signaling pathways, which needs to be confirmed by further in vitro experiments."( Carvedilol alleviates the biliary cirrhosis through inhibiting the endoplasmic reticulum stress.
Gao, P; Meng, RR; Si, JY; Yang, B; Yu, HY, 2017
)
3.34
"Carvedilol has an anti-angiogenic effect on HUVECs. "( Carvedilol may attenuate liver cirrhosis by inhibiting angiogenesis through the VEGF-Src-ERK signaling pathway.
Ding, Q; Li, Y; Tian, XG; Wang, QZ; Zhang, CQ, 2015
)
3.3
"Carvedilol has a statistically significant therapeutic effect, especially on functional recovery, and we found that carvedilol reduced secondary damage by inhibiting apoptosis and regulating the oxidant and antioxidant status."( Effect of Carvedilol on Secondary Damage in Experimental Spinal Cord Injury in Rats.
Cengiz, SL; Esen, H; Karatas, Y; Savas, C; Toker, A, 2015
)
2.26
"Carvedilol has a powerful antiarrhythmic effect after AMI, even in patients already treated with an ACE inhibitor. "( Antiarrhythmic effect of carvedilol after acute myocardial infarction: results of the Carvedilol Post-Infarct Survival Control in Left Ventricular Dysfunction (CAPRICORN) trial.
Colucci, W; Dargie, H; Ford, I; Køber, L; Lopez-Sendon, J; McMurray, J; Remme, W; Robertson, M; Sharpe, DN, 2005
)
2.07
"Carvedilol has a class III antiarrhythmic effect, which may provide the rationale for a favourable clinical outcome compared with other beta-blockers as suggested in the recent COMET (Carvedilol Or Metoprolol European Trial) substudy."( Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy.
Abe, H; Anson, BD; Delisle, BP; January, CT; Kawakami, K; Kikuchi, K; Nagatomo, T; Nakashima, Y; Takemasa, H, 2006
)
1.06
"Carvedilol CR has a clinically meaningful defined dose-dependent antihypertensive effect that persists throughout a 24-hour period."( Efficacy of a once-daily formulation of carvedilol for the treatment of hypertension.
Bakris, GL; Fleck, R; Iyengar, M; Sica, DA; Tarka, EA; Weber, MA, 2006
)
1.32
"Carvedilol has a high safety profile and the clinical benefits appear maintained across a wide range of patients with comorbidities such as diabetes and renal failure."( Carvedilol: use in chronic heart failure.
Doughty, RN; White, HD, 2007
)
2.5
"Carvedilol has a neutral effect on lipids and glucose metabolism."( Results of therapy with carvedilol, a beta-blocker vasodilator with antioxidant properties, in hypertensive patients.
Frishman, W; Moser, M, 1998
)
1.33
"Carvedilol has a good metabolic profile and seems to improve insulin sensitivity."( Betablockers: old concept in a modern approach.
Hansson, BG, 1998
)
1.02
"Carvedilol (CAR) has vasodilatory, antioxidant stress and anti-inflammatory effects and poses a vital role in addressing the issue of diabetic complications."( Carvedilol activates nuclear factor E2-related factor 2/ antioxidant response element pathway to inhibit oxidative stress and apoptosis of retinal pigment epithelial cells induced by high glucose.
He, S; Li, M; Wang, W; Zhang, Y, 2022
)
2.89
"Carvedilol has been shown to protect against R-IRI."( Quercetin and lithium chloride potentiate the protective effects of carvedilol against renal ischemia-reperfusion injury in high-fructose, high-fat diet-fed Swiss albino mice independent of renal lipid signaling.
Ibrahim, IAAE; Mahmoud, AAA; Mahmoud, MF; Rezk, AM, 2021
)
1.58
"Carvedilol has been shown to be cardioprotective by reducing cardiac pro-inflammatory cytokines present in oxidative stress in certain heart diseases."( Carvedilol Inhibits Matrix Metalloproteinase-2 Activation in Experimental Autoimmune Myocarditis: Possibilities of Cardioprotective Application.
Biczysko, W; Ceremuga, I; Dziegiel, P; Haczkiewicz, K; Kobierzycki, C; Kwiatkowska, J; Piasecki, T; Podhorska-Okolow, M; Sapa, A; Skrzypiec-Spring, M; Szelag, A; Wozniak, M, 2018
)
2.64
"Carvedilol has a significant effect on alleviating the biliary cirrhosis in mice, and its relevant mechanism may be that carvedilol inhibits the endoplasmic reticulum stress through the negative regulation of ATF4-CHOP, ATF6-CHOP and IRE1-pJNK signaling pathways, which needs to be confirmed by further in vitro experiments."( Carvedilol alleviates the biliary cirrhosis through inhibiting the endoplasmic reticulum stress.
Gao, P; Meng, RR; Si, JY; Yang, B; Yu, HY, 2017
)
3.34
"Carvedilol has been identified as a promising agent for the treatment of liver fibrosis. "( Carvedilol attenuates liver fibrosis by suppressing autophagy and promoting apoptosis in hepatic stellate cells.
Li, Z; Ling, L; Meng, D; Wang, G; Wu, Y; Zhang, C, 2018
)
3.37
"Carvedilol has potential utility for treating early-stage liver cirrhosis."( Carvedilol Ameliorates Intrahepatic Angiogenesis, Sinusoidal Remodeling and Portal Pressure in Cirrhotic Rats.
Li, G; Ling, L; Meng, D; Wang, S; Zhang, C, 2018
)
2.64
"Carvedilol gel has the potential of minimizing H"( Anti-inflammatory potential of a carvedilol gel in the pulpal tissue of rats after dental bleaching: A histopathological evaluation.
Benetti, F; Briso, ALF; Cintra, LTA; de Castilho Jacinto, R; Dezan-Júnior, E; Louzada, LM; Vieira, LB, 2019
)
2.24
"Carvedilol has been shown to possess multiple biological and pharmacological properties."( Carvedilol promotes neurological function, reduces bone loss and attenuates cell damage after acute spinal cord injury in rats.
Fu, Q; Huang, Y; Jia, C; Li, B; Liang, F; Liu, D, 2015
)
2.58
"Carvedilol has an anti-angiogenic effect on HUVECs. "( Carvedilol may attenuate liver cirrhosis by inhibiting angiogenesis through the VEGF-Src-ERK signaling pathway.
Ding, Q; Li, Y; Tian, XG; Wang, QZ; Zhang, CQ, 2015
)
3.3
"Carvedilol has been shown to function as an inverse agonist, inhibiting G protein activation while stimulating β-arrestin-dependent signaling and inducing receptor desensitization."( Carvedilol binding to β2-adrenergic receptors inhibits CFTR-dependent anion secretion in airway epithelial cells.
Maniak, PJ; O'Grady, SM; Peitzman, ER; Zaidman, NA, 2016
)
2.6
"Carvedilol has a statistically significant therapeutic effect, especially on functional recovery, and we found that carvedilol reduced secondary damage by inhibiting apoptosis and regulating the oxidant and antioxidant status."( Effect of Carvedilol on Secondary Damage in Experimental Spinal Cord Injury in Rats.
Cengiz, SL; Esen, H; Karatas, Y; Savas, C; Toker, A, 2015
)
2.26
"Carvedilol has established its evidence to improve prognosis and facilitate left ventricular reverse remodeling (LVRR) in heart failure patients with reduced left ventricular ejection fraction (LVEF), and many studies have supported its dose-dependency. "( High Dose β-Blocker Therapy Triggers Additional Reverse Remodeling in Patients With Idiopathic Non-Ischemic Cardiomyopathy.
Imamura, T; Kato, NP; Kinugawa, K; Komuro, I; Nitta, D, 2016
)
1.88
"Carvedilol, which has potent antioxidant activity in addition to functioning as an adrenergic blocker, prevents nitrate tolerance by a still to be elucidated mechanism."( Coadministration of carvedilol attenuates nitrate tolerance by preventing cytochrome p450 depletion.
Funae, Y; Hirai, H; Minamiyama, Y; Nakahira, A; Okada, S; Sasaki, Y; Suehiro, S; Takemura, S, 2010
)
1.41
"Carvedilol in SHR rats has decreased blood pressure, and normalized physiological, biochemical and morphological indexes in the cardiac muscle."( [Effect of carvedilol in the combination with quercetine and tiotriazoline on the nucleus density and RNA concentration in the nucleus of cardiac myocytes of spontaneous hypertensive rats].
Zahorodnyĭ, MI,
)
1.24
"Carvedilol has theoretical advantages in patients who use cocaine, but there are no controlled studies confirming the superior efficacy of this agent. "( Carvedilol therapy after cocaine-induced myocardial infarction in patients with asthma.
Mancell, J; Rogers, ML; Self, T; Soberman, JE, 2011
)
3.25
"Carvedilol has been the most effective beta-blocker in the treatment of the systolic heart failure."( Novel design and synthesis of modified structure of carvedilol.
Hashemzadeh, M; Hill, DN; Movahed, MR; Russu, WA; Soroush, L, 2011
)
1.34
"Carvedilol has been shown to be superior to metoprolol tartrate to improve clinical outcomes in patients with heart failure (HF), yet the mechanisms responsible for these differences remain unclear. "( Endothelial function is unaffected by changing between carvedilol and metoprolol in patients with heart failure--a randomized study.
Christiansen, B; Dominguez, H; Falskov, B; Hermann, TS; Køber, L; Major-Pedersen, A; Rask-Madsen, C; Raunsø, J; Torp-Pedersen, C, 2011
)
2.06
"Carvedilol has been shown to improve endothelial cell function in vivo and to block endothelin-1 release in vitro."( Probing the mechanisms of intradialytic hypertension: a pilot study targeting endothelial cell dysfunction.
Inrig, JK; Kim, C; Povsic, TJ; Toto, R; Van Buren, P; Vongpatanasin, W, 2012
)
1.1
"Carvedilol has been shown to be more effective than propranolol in decreasing portal pressure. "( Randomized, controlled trial of carvedilol versus nadolol plus isosorbide mononitrate for the prevention of variceal rebleeding.
Chen, WC; Lo, GH; Wang, HM; Yu, HC, 2012
)
2.11
"Carvedilol has been used in a limited number of studies examining oxidative injury."( The effect of carvedilol on serum and tissue oxidative stress parameters in partial ureteral obstruction induced rat model.
Atilgan, D; Erdemir, F; Firat, F; Koseoglu, RD; Parlaktas, BS; Saylan, O; Yasar, A, 2013
)
1.47
"Carvedilol has beneficial effects on cardiac function in patients with heart failure but its effect on ovariectomy-induced myocardial contractile dysfunction remains unclear. "( Carvedilol prevents ovariectomy-induced myocardial contractile dysfunction in female rat.
Fernandes, AA; Fiorim, J; Forechi, L; Lima, FL; Pavan, BM; Potratz, FF; Ribeiro, RF; Stefanon, I; Vassallo, DV, 2013
)
3.28
"Carvedilol has hypotensive effects and inhibits agonist-induced cell proliferation of vascular smooth muscle and then prevents vascular remodeling. "( Inhibitory effects of carvedilol on calcium channels in vascular smooth muscle cells.
Iida, H; Iwasawa, K; Jo, T; Ma, J; Nagai, R; Nakajima, T; Omata, M, 2003
)
2.08
"Carvedilol has non-selective beta-adrenoceptor and selective alpha1-adrenoceptor blocking activity, calcium channel blocking, and anti-oxidant activity."( Carvedilol inhibits basal and stimulated ACE production in human endothelial cells.
Fyhrquist, F; Nyman, T; Saijonmaa, O, 2004
)
2.49
"Carvedilol has been found to prevent progressive adverse ventricular remodeling in both conditions."( Cardiac remodeling in coronary artery disease.
Sharpe, N, 2004
)
1.04
"Carvedilol has been shown to improve survival and morbidity in patients with heart failure. "( Relation of dose of carvedilol to reduction in QT dispersion in patients with mild to moderate heart failure secondary to ischemic or to idiopathic dilated cardiomyopathy.
Bristow, MR; Gill, EA; Holcslaw, TL; Pittenger, B, 2004
)
2.09
"Carvedilol has a powerful antiarrhythmic effect after AMI, even in patients already treated with an ACE inhibitor. "( Antiarrhythmic effect of carvedilol after acute myocardial infarction: results of the Carvedilol Post-Infarct Survival Control in Left Ventricular Dysfunction (CAPRICORN) trial.
Colucci, W; Dargie, H; Ford, I; Køber, L; Lopez-Sendon, J; McMurray, J; Remme, W; Robertson, M; Sharpe, DN, 2005
)
2.07
"Carvedilol has been shown to inhibit neutrophil O(2)(*-) generation in patients with stable angina."( Neutrophils superoxide anion generation during carvedilol therapy in patients with stable angina.
Błaszczyk, J; Cegliński, T; Irzmański, R; Kowalczyk, E; Kowalska, E; Kowalski, J; Pawlicki, L; Petecka, E, 2005
)
1.31
"Carvedilol has a class III antiarrhythmic effect, which may provide the rationale for a favourable clinical outcome compared with other beta-blockers as suggested in the recent COMET (Carvedilol Or Metoprolol European Trial) substudy."( Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy.
Abe, H; Anson, BD; Delisle, BP; January, CT; Kawakami, K; Kikuchi, K; Nagatomo, T; Nakashima, Y; Takemasa, H, 2006
)
1.06
"Carvedilol use has been adapted into pediatric heart failure practice although data supporting its efficacy in infants and children are scarce."( The use of carvedilol in pediatric heart failure.
Benson, LN; Greenway, SC, 2006
)
1.45
"Carvedilol CR has a clinically meaningful defined dose-dependent antihypertensive effect that persists throughout a 24-hour period."( Efficacy of a once-daily formulation of carvedilol for the treatment of hypertension.
Bakris, GL; Fleck, R; Iyengar, M; Sica, DA; Tarka, EA; Weber, MA, 2006
)
1.32
"Carvedilol has a high safety profile and the clinical benefits appear maintained across a wide range of patients with comorbidities such as diabetes and renal failure."( Carvedilol: use in chronic heart failure.
Doughty, RN; White, HD, 2007
)
2.5
"Carvedilol has been shown to possess both ROS-scavenging and ROS-suppressive effects, and its use is associated with a reduction in oxidative stress."( Antioxidant activity of carvedilol in cardiovascular disease.
Brooks, DP; Dandona, P; Ghanim, H, 2007
)
1.37
"Carvedilol has previously been demonstrated to be beneficial in patients with acute myocardial infarction (AMI) and left ventricular (LV) dysfunction. "( Randomized active-controlled study comparing effects of treatment with carvedilol versus metoprolol in patients with left ventricular dysfunction after acute myocardial infarction.
Asanin, MR; Jelena, MM; Lasica, RM; Matic, MD; Mrdovic, IB; Ostojic, MC; Perunicic, JP; Savic, LZ; Vasiljevic, ZM, 2007
)
2.02
"Carvedilol has been made into a novel osmotic pump tablet which includes Gelucire 44/14, Lutrol F68, Transcutol P, silicon dioxide, mannitol, citric acid, and sodium hydrogen carbonate. "( Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol.
Guo, L; Li, J; Liu, H; Nie, S; Pan, W; Sun, P; Wei, L, 2007
)
2.01
"Carvedilol therapy has been reported to be more effective than other beta-blockers in patients with chronic heart failure (CHF). "( Combined therapy with carvedilol and amiodarone is more effective in improving cardiac symptoms, function, and sympathetic nerve activity in patients with dilated cardiomyopathy: comparison with carvedilol therapy alone.
Adachi, H; Hoshizaki, H; Isobe, N; Kasama, S; Oshima, S; Taniguchi, K; Toyama, T; Yoshimura, Y,
)
1.89
"Carvedilol has been used in small numbers of patients with cardiac failure."( Clinical pharmacokinetics and pharmacodynamics of carvedilol.
Morgan, T, 1994
)
1.26
"Carvedilol has beneficial haemodynamic effects in patients with congestive heart failure."( A risk-benefit assessment of carvedilol in the treatment of cardiovascular disorders.
Conway, EL; Krum, H; Louis, WJ, 1994
)
1.3
"Carvedilol has been shown to improve exercise tolerance in patients with angina pectoris and reduce the occurrence of episodes of silent myocardial ischaemia."( Carvedilol in ischaemic heart disease.
Prichard, BN, 1993
)
2.45
"Carvedilol has improved the symptomatic status of patients with moderate to severe heart failure in single-center studies, but its clinical effects have not been evaluated in large, multicenter trials."( Double-blind, placebo-controlled study of the effects of carvedilol in patients with moderate to severe heart failure. The PRECISE Trial. Prospective Randomized Evaluation of Carvedilol on Symptoms and Exercise.
Cody, RJ; Colucci, WS; Freeman, I; Goldscher, DA; Gottlieb, SS; Gregory, JJ; Kantrowitz, NE; Kinhal, V; Klapholz, M; Kukin, ML; LeJemtel, TH; Liang, CS; Lukas, MA; Packer, M; Pearle, D; Sackner-Bernstein, JD; Shusterman, NH; Udelson, JE; Young, ST, 1996
)
1.98
"Carvedilol has similar efficacy to other beta-blocking agents, calcium antagonists, ACE inhibitors and hydrochlorothiazide."( Carvedilol. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disorders.
Dunn, CJ; Lea, AP; Wagstaff, AJ, 1997
)
2.46
"Carvedilol has been shown to determine a significant improvement in left ventricular function, symptoms, clinical course and prognosis of patients with chronic heart failure. "( [The effects of mid- and long-term administration (3-4 years) of carvedilol in patients with idiopathic dilated cardiomyopathy].
Boldi, E; Dei Cas, L; Garbellini, M; Giubbini, R; Metra, M; Milan, E; Nodari, S; Rosselli, F, 1997
)
1.98
"Carvedilol has a neutral effect on lipids and glucose metabolism."( Results of therapy with carvedilol, a beta-blocker vasodilator with antioxidant properties, in hypertensive patients.
Frishman, W; Moser, M, 1998
)
1.33
"Carvedilol has a good metabolic profile and seems to improve insulin sensitivity."( Betablockers: old concept in a modern approach.
Hansson, BG, 1998
)
1.02
"Carvedilol, which has beta-blocking, alpha-blocking, and antioxidant properties, is associated with a reduction in hospitalizations and symptoms and improvements in ejection fraction it also appears to reduce mortality, although confirmatory studies are needed."( Catecholamines and their blockade in congestive heart failure.
White, CM, 1998
)
1.02
"Carvedilol has been shown to be effective in systemic hypertension and coronary artery disease in patients with end-stage renal disease, on maintenance hemodialysis. "( [Complex ventricular arrhythmias and carvedilol: efficacy in hemodialyzed uremic patients].
Cice, G; Di Benedetto, A; Ferrara, L; Iacono, A; Tagliamonte, E, 1998
)
2.02
"Carvedilol has been known to combine alpha/beta-blockade with antioxidant properties."( Randomized, double-blind, placebo-controlled study of carvedilol on the prevention of nitrate tolerance in patients with chronic heart failure.
Kakihana, M; Ohtsuka, S; Sugishita, Y; Watanabe, H, 1998
)
1.27
"Carvedilol has been known to combine alpha- and beta-blockade with antioxidant properties."( Preventive effects of carvedilol on nitrate tolerance--a randomized, double-blind, placebo-controlled comparative study between carvedilol and arotinolol.
Kakihana, M; Ohtsuka, S; Sugishita, Y; Watanabe, H, 1998
)
1.34
"Carvedilol also has neuroprotective capacity with modulatory actions at N-methyl-D-aspartate (NMDA) receptors and Na+ channels."( Neuroprotective activities of carvedilol and a hydroxylated derivative: role of membrane biophysical interactions.
Feuerstein, G; Lysko, KA; Lysko, PG; Mason, PE; Mason, RP; Walter, MF; Webb, CL, 1998
)
1.31
"Carvedilol has beneficial effects on splanchnic haemodynamics following acute and chronic administration in cirrhosis, without compromising hepatic blood flow or renal function. "( Acute and chronic haemodynamic and renal effects of carvedilol in patients with cirrhosis.
Hayes, PC; Helmy, A; Stanley, AJ; Therapondos, G, 1999
)
2
"Carvedilol has been investigated in numerous in vivo studies and thus comparisons of in vitro results to in vivo observations are possible."( In vitro absorption studies with carvedilol using a new model with porcine intestine called BM-RIMO (Boehringer-Mannheim ring model).
Backfisch, G; Neidlein, R; Nolte, K, 1999
)
1.31
"Carvedilol has been shown to be beneficial for patients with heart failure, but it is not clear how it should be initiated in routine clinical practice, particularly in the elderly. "( Experience of commencing Carvedilol in elderly patients with heart failure in a routine outpatient clinic.
Owen, A, 2000
)
2.05
"Carvedilol has been shown to decrease the progression of heart failure and improve left ventricular function and survival in patients with a left ventricular ejection fraction (LVEF) less than 35%. "( Predicting response to carvedilol for the treatment of heart failure: a multivariate retrospective analysis.
Abraham, WT; Bristow, MR; Ferguson, D; Lindenfeld, JA; Lowes, BD; Schleman, KA; Wolfel, EE; Zisman, LS, 2001
)
2.06
"Carvedilol has broader antiadrenergic effects than metoprolol, but it is not clear whether this characteristic is associated with greater benefits on cardiac function during long-term treatment."( Comparative effects of carvedilol and metoprolol on left ventricular ejection fraction in heart failure: results of a meta-analysis.
Antonopoulos, GV; Berlin, JA; Chittams, J; Konstam, MA; Packer, M; Udelson, JE, 2001
)
1.34
"Carvedilol has proven to be beneficial in a majority of adult patients with congestive heart failure. "( Efficacy and safety of carvedilol in infants with dilated cardiomyopathy: a preliminary report.
Farzana, F; Gachara, N; Krishnan, U; Prabhakaran, S; Shah, MJ; Srinivas, S,
)
1.88
"Carvedilol has been shown to improve morbidity and mortality in patients with congestive heart failure (CHF). "( Carvedilol titration in patients with congestive heart failure receiving inotropic therapy.
Antonio, C; Choudhary, G; Heaney, L; Jain, A; Just, V; Kumar, A; Papp, MA, 2001
)
3.2
"Carvedilol has additional metabolic and antioxidant properties."( Rationale and design of the carvedilol or metoprolol European trial in patients with chronic heart failure: COMET.
Cleland, JG; Di Lenarda, A; Hanrath, P; J Remme, W; Komajda, M; Metra, M; Poole-Wilson, PA; Swedberg, K; Torp-Pedersen, C, 2002
)
1.33
"Carvedilol has been shown to be effective and safe in patients with essential hypertension when given as monotherapy. "( Safety and antihypertensive efficacy of carvedilol and atenolol alone and in combination with hydrochlorothiazide.
Hörrmann, M; Machwirth, M; van der Does, R; Widmann, L, 1990
)
1.99
"Carvedilol (BM 14.190) has been shown to have beta-adrenergic blocking and vasodilating activity. "( Clinical pharmacologic investigations with carvedilol, a new beta-blocker with direct vasodilator activity.
Abshagen, U; Akpan, W; Neugebauer, G; Schröter, E; von Möllendorff, E, 1986
)
1.98

Actions

Carvedilol (CAR) can inhibit cell growth and induce cell apoptosis in breast cancer in vitro. Both carvedilol and nebivolol produce hemodynamic and clinical benefits in chronic heart failure. It is unknown whether their peculiar pharmacologic properties produce different effects on LV function.

ExcerptReferenceRelevance
"Carvedilol succeeded to enhance antioxidants in gastric tissue, attenuated lipid peroxidative parameters, and suppressed the release of inflammatory mediators."( Carvedilol safeguards against aspirin-induced gastric damage in rats.
Ahmed, I; Ahmed, N; Bazarbay, AA; El-Agamy, DS; Elkablawy, MA, 2020
)
2.72
"Carvedilol (CAR) can inhibit cell growth and induce cell apoptosis in breast cancer in vitro. "( Carvedilol suppresses migration and invasion of malignant breast cells by inactivating Src involving cAMP/PKA and PKCδ signaling pathway.
Dezong, G; Qinye, F; Zhigang, Y; Zhongbing, M,
)
3.02
"Carvedilol may suppress atherosclerosis via reducing superoxide production, in addition to the hemodynamic modifications in this animal model."( Carvedilol reduces the severity of atherosclerosis in apolipoprotein E-deficient mice via reducing superoxide production.
Fujita, M; Hirano, E; Kimura, T; Kishimoto, C; Shimada, K, 2012
)
2.54
"Carvedilol did not inhibit the Ca2+ release, but significantly suppressed the sustained rise due to Ca2+ entry concentration-dependently."( Inhibitory effects of carvedilol on calcium channels in vascular smooth muscle cells.
Iida, H; Iwasawa, K; Jo, T; Ma, J; Nagai, R; Nakajima, T; Omata, M, 2003
)
1.35
"Carvedilol can inhibit this process."( [The effect of carvedilol on cardiac function and autoantibodies against the cardiac receptors].
Chen, J; Hu, DY; Li, J; Liu, XL; Wu, YF; Zhang, L, 2005
)
1.4
"Both carvedilol and nebivolol produce hemodynamic and clinical benefits in chronic heart failure, but it is unknown whether their peculiar pharmacologic properties produce different effects on LV function."( Effects of nebivolol versus carvedilol on left ventricular function in patients with chronic heart failure and reduced left ventricular systolic function.
Abrignani, MG; Braschi, A; De Castro, S; Lombardo, RM; Reina, C; Rizzo, PA, 2006
)
1.08
"Carvedilol resulted in a lower perceived burden of diabetes-related symptoms in patients with type 2 diabetes and hypertension. "( beta-blocker use and diabetes symptom score: results from the GEMINI study.
Anderson, KM; Bakris, GL; Bell, DS; Dalal, MR; Fonseca, V; Iyengar, M; Katholi, RE; Lukas, MA; McGill, JB; Messerli, FH; Phillips, RA; Raskin, P; Wright, JT, 2007
)
1.78
"Carvedilol inhibited the increase in cell number induced by foetal calf serum (FCS) in 86% (18 of 21) of human VSMC grown both from saphenous vein (17.6 +/- 3.5% inhibition, mean +/- SEM, n = 15) and restenotic lesions (31.4 +/- 5.5% inhibition, mean +/- SEM, n = 5)."( Inhibition of human vascular smooth muscle cell proliferation by the novel multiple-action antihypertensive agent carvedilol.
Betteridge, LJ; Chan, P; Patel, MK; Schachter, M; Sever, PS, 1995
)
1.22
"Carvedilol appears to increase digoxin's oral bioavailability as well as renal elimination."( Effects of long-term oral carvedilol on the steady-state pharmacokinetics of oral digoxin in patients with mild to moderate hypertension.
Boyle, DA; Chandler, MH; Clifton, GD; Field, CJ; Smith, DA; Wermeling, DP,
)
1.15
"Carvedilol reduced all-cause mortality but had no effects on the Minnesota Living With Heart Failure scale, the distance walked in 9 minutes on a self-powered treadmill, or cardiothoracic index."( Carvedilol inhibits clinical progression in patients with mild symptoms of heart failure. US Carvedilol Heart Failure Study Group.
Bowers, JA; Bristow, MR; Cohn, JN; Colucci, WS; Fowler, MB; Gilbert, EM; Hershberger, R; Holcslaw, TL; Krueger, SK; Lukas, MA; Packer, M; Sackner-Bernstein, JD; Uretsky, BF; Young, ST, 1996
)
2.46
"Carvedilol at a lower dose (7.5 mg x kg(-1) x d(-1)) and lacidipine 1 mg x kg(-1) x d(-1) had only moderate and nonsignificant effects on carotid pressure but largely prevented left ventricular hypertrophy (P<0.01) and preproendothelin-1 overexpression (P<0.05)."( Carvedilol and lacidipine prevent cardiac hypertrophy and endothelin-1 gene overexpression after aortic banding.
Donckier, J; Godfraind, T; Heyndrickx, GR; Kyselovic, J; Massart, PE; Wibo, M, 1999
)
2.47
"Carvedilol did not increase CVC, blunt the calf vasoconstrictor response to handgrip or attenuate the gain of the neuroeffector transfer function, indicating the absence of functionally important peripheral alpha(1)-adrenoceptor antagonism during long-term treatment of CHF."( Lack of evidence for peripheral alpha(1)- adrenoceptor blockade during long-term treatment of heart failure with carvedilol.
Azevedo, ER; Floras, JS; Kubo, T; Newton, GE; Parker, JD, 2001
)
1.96
"Carvedilol may cause pruritus and elevated liver function test results. "( Hepatotoxicity associated with carvedilol.
Hagmeyer, KO; Stein, J, 2001
)
2.04
"Carvedilol does not enhance the hyperkalemic effect of moderate physical exercise in anuric hemodialysis patients."( Carvedilol does not modulate moderate exercise-induced hyperkalemia in hemodialysis patients.
Klimek, D; Kokot, F; Nowicki, M; Szewczyk-Seifert, G, 2002
)
3.2
"The carvedilol-induced increase of [(3)H]STX binding was abolished by brefeldin A and H-89, inhibitors of intracellular vesicular trafficking of proteins from the trans-Golgi network and of cyclic AMP-dependent protein kinase (protein kinase A), respectively."( Differential effects of short and prolonged exposure to carvedilol on voltage-dependent Na(+) channels in cultured bovine adrenal medullary cells.
Izumi, F; Kajiwara, K; Nakashima, Y; Wada, A; Yanagihara, N; Yanagita, T, 2002
)
1.04
"Carvedilol did not cause significant changes in glomerular filtration rate, effective renal plasma flow, blood urea nitrogen, or serum creatinine."( Effect of long-term carvedilol therapy on renal function in essential hypertension.
Marumo, F; Tomita, K, 1992
)
1.33
"Carvedilol may also produce an improvement of the LV contractile status in patients with CHD and impaired LV function, mainly due to afterload reduction, in addition to its antianginal effect, which is due mainly to the beta-blocking properties of this substance."( Hemodynamic profile of carvedilol.
Eggeling, T; Haerer, W; Höher, M; Hombach, V; Kochs, M; Schmidt, A; Wieshammer, S, 1990
)
1.31

Treatment

Carvedilol treatment decreased brain levels of oxidative stress markers and induced Nrf2/HO-1 pathway. Pretreatment of carvedilol orally at a dose of 1 mg/kg body weight for 2 weeks significantly prevented initial reduction in serum electrolyte levels induced by adrenaline.

ExcerptReferenceRelevance
"Carvedilol treatment decreased the brain levels of oxidative stress markers and induced Nrf2/HO-1 pathway."( Carvedilol attenuates brain damage in mice with hepatic encephalopathy.
Amirshahrokhi, K; Niapour, A, 2022
)
2.89
"Carvedilol treatment decreased the detrimental effects induced by R-IRI."( Quercetin and lithium chloride potentiate the protective effects of carvedilol against renal ischemia-reperfusion injury in high-fructose, high-fat diet-fed Swiss albino mice independent of renal lipid signaling.
Ibrahim, IAAE; Mahmoud, AAA; Mahmoud, MF; Rezk, AM, 2021
)
1.58
"Carvedilol treatment led to the downregulation of phosphor-cAMP response element-binding protein (CREB)."( Carvedilol, an Adrenergic Blocker, Suppresses Melanin Synthesis by Inhibiting the cAMP/CREB Signaling Pathway in Human Melanocytes and Ex Vivo Human Skin Culture.
Chang, SE; Choi, ME; Lee, HR; Lee, WJ; Moon, IJ; Song, Y; Yoo, H, 2020
)
2.72
"Late carvedilol treatment did not lead to recovery of RV function."( [
Ahmadi, A; Beanlands, R; deKemp, RA; Mielniczuk, LM; Schock, S; Staines, WA; Stewart, DJ; Zelt, JGE, 2021
)
1.08
"Carvedilol treatment was a strong predictor for being on target dose of BB at time of implant, as was treatment with angiotensin-converting enzyme inhibitors and/or spironolactone, no history of myocardial infarction, younger age and less pronounced heart failure symptoms."( The use of guideline recommended beta-blocker therapy in primary prevention implantable cardioverter defibrillator patients: insight from Danish nationwide registers.
Gislason, GH; Johansen, JB; Jøns, C; Nielsen, JC; Petersen, HH; Riahi, S; Ruwald, AC; Torp-Pedersen, C; Vinther, M, 2018
)
1.2
"Carvedilol and vitamin E treatments were associated with better renal function and less myocardial damage, lower blood glucose, and lipid peroxidation, higher antioxidant capacity, better serum lipids, and higher expression of Bcl-2 protein in diabetic rats."( Antiapoptotic and antioxidant effects of carvedilol and vitamin E protect against diabetic nephropathy and cardiomyopathy in diabetic Wistar albino rats.
Abdel-Raheem, MH; Al-Rifaay, A; Hasan-Ali, H; Mosad, E; Salama, HS; Salim, SU, 2015
)
1.4
"Carvedilol pretreatment significantly attenuated the potassium dichromate-induced DNA damage, decreased the p53, Bax and cleaved caspase-3 expression and increased the Bcl-2 expression."( Chromium-induced nephrotoxicity and ameliorative effect of carvedilol in rats: Involvement of oxidative stress, apoptosis and inflammation.
Bijargi, SR; Koneru, M; Kota, A; Sahu, BD; Sistla, R, 2014
)
1.37
"Carvedilol treatment prevented many of these deleterious effects."( Effects of carvedilol on ventricular remodeling and the expression of β3-adrenergic receptor in a diabetic rat model subjected myocardial infarction.
Fu, L; Kang, X; Shen, J; Wang, F; Wang, Y; Yu, P; Zhang, R, 2016
)
1.55
"Carvedilol treatment also significantly reduced the levels of proinflammatory cytokines tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, transforming growth factor (TGF)-β1 and monocyte chemoattractant protein (MCP)-1 in the lung tissue."( Carvedilol attenuates paraquat-induced lung injury by inhibition of proinflammatory cytokines, chemokine MCP-1, NF-κB activation and oxidative stress mediators.
Amirshahrokhi, K; Khalili, AR, 2016
)
2.6
"Carvedilol co-treatment in CCl4-intoxicated rats for 6 weeks significantly counteracted the changes in hepatotoxicity markers and histopathological lesions induced by CCl4."( Antifibrotic Effects of Carvedilol and Impact of Liver Fibrosis on Carvedilol Pharmacokinetics in a Rat model.
Abdel-Sattar, SA; El-Bakly, WM; El-Demerdash, E; Mohamed, EA, 2017
)
1.48
"Carvedilol co-treatment in CCl4-intoxicated rats for 6 weeks recovered its pharmacokinetic profile, which is mainly attributed to the impact of pharmacodynamic antifibrotic effects of carvedilol on its own kinetics."( Antifibrotic Effects of Carvedilol and Impact of Liver Fibrosis on Carvedilol Pharmacokinetics in a Rat model.
Abdel-Sattar, SA; El-Bakly, WM; El-Demerdash, E; Mohamed, EA, 2017
)
1.48
"Carvedilol co-treatment did not reduce the anti-tumor effects of oxaliplatin in human colon cancer cells (HT-29), but exhibited free radical scavenging activity against oxaliplatin-induced oxidative stress in neuronal cells (Neuro-2a)."( Carvedilol prevents functional deficits in peripheral nerve mitochondria of rats with oxaliplatin-evoked painful peripheral neuropathy.
Areti, A; Komirishetty, P; Kumar, A, 2017
)
2.62
"Carvedilol treatment restored the IS reduction by postconditioning, possibly via other mechanism(s) of the ERK and Akt pathways."( Attenuation of cardioprotective effect by postconditioning in coronary stenosed rat heart and its restoration by carvedilol.
Maruyama, Y; Oikawa, M; Watanabe, K; Yaoita, H, 2008
)
1.28
"Carvedilol treatment also resulted in improved hemodynamics and relieved right ventricular hypertrophy."( [B-type natriuretic peptide (BNP) levels and the effects of carvedilol on BNP levels in juvenile rats with right heart failure].
An, JD; Feng, S; Liang, F, 2009
)
1.32
"Carvedilol pretreatment is associated with a reduction in both the QTd and LF/HF ratio, raising the possibility that the cardiac sympathovagal balance shift may be responsible for the impaired homogeneity of myocardial repolarization, and that beta-blocker pretreatment may decrease the mortality risk during alcoholic withdrawal."( QT interval dispersion and cardiac sympathovagal balance shift in rats with acute ethanol withdrawal.
Fujimiya, T; Hamada, K; Liu, J; Okamura, N; Shirafuji, S, 2010
)
1.08
"With carvedilol treatment, LVMI was lower (p<0.05), endothelium function of the brachial artery was higher (p<0.05), and peak diastolic coronary flow velocity at rest and at maximal vasodilation after dipyridamole infusion was significantly higher (p<0.05) than with metoprolol treatment, which led to a significantly higher CFR (p<0.05)."( Effect of carvedilol on coronary flow reserve in patients with hypertensive left-ventricular hypertrophy.
Mei, Z; Xiaozhen, H; Yu, S; Yun, Z, 2010
)
1.22
"Carvedilol treatment fully prevented damage to the heart and kidney and attenuated liver lesions induced by the Ang II infusion."( Protective effects of carvedilol on systemic vascular damage induced by angiotensin II: organ-specific effects independent of antihypertensive effects.
Matsubara, BB; Matsubara, LS; Padovani, CR; Rocha, NS; Schwartz, DS; Vailati, Mdo C, 2010
)
1.4
"Carvedilol treatment was started after establishment of pulmonary hypertension and right heart dysfunction."( Adrenergic receptor blockade reverses right heart remodeling and dysfunction in pulmonary hypertensive rats.
Abbate, A; Bogaard, HJ; Chang, PJ; Chau, VQ; Hoke, NN; Kasper, M; Kraskauskas, D; Mizuno, S; Natarajan, R; Salloum, FN; Voelkel, NF, 2010
)
1.08
"Carvedilol treatment was associated with enhancement of RV fetal gene reactivation, increased protein kinase G (PKG) activity, and a reduction in capillary rarefaction and fibrosis."( Adrenergic receptor blockade reverses right heart remodeling and dysfunction in pulmonary hypertensive rats.
Abbate, A; Bogaard, HJ; Chang, PJ; Chau, VQ; Hoke, NN; Kasper, M; Kraskauskas, D; Mizuno, S; Natarajan, R; Salloum, FN; Voelkel, NF, 2010
)
1.08
"Carvedilol treatment produced a significant increase in basal synaptic transmission and LTP in TgCRND8 mice, as compared to their vehicle-treated slices, in which basal neuronal transmission and LTP decreased."( Carvedilol reestablishes long-term potentiation in a mouse model of Alzheimer's disease.
Arrieta-Cruz, I; Pasinetti, GM; Pavlides, C; Wang, J, 2010
)
2.52
"Carvedilol treatment resulted in less left ventricular hypertrophy and dilatation."( Usefulness of carvedilol in the treatment of chronic aortic valve regurgitation.
Arsenault, M; Couet, J; Lachance, D; Roussel, E; Zendaoui, A, 2011
)
1.45
"Carvedilol treatment fully prevented diet-induced insulin resistance and hypertension, mimicking the effect of caffeine."( Chronic caffeine intake decreases circulating catecholamines and prevents diet-induced insulin resistance and hypertension in rats.
Conde, SV; Gonzalez, C; Guarino, MP; Monteiro, EC; Mota Carmo, M; Nunes da Silva, T, 2012
)
1.1
"Carvedilol treatment resulted in significant improvements in LVEF, shortening fraction, and velocity of circumferential shortening (VCF(c))."( New insights into mechanisms of action of carvedilol treatment in chronic heart failure patients--a matter of time for contractility.
Ather, S; Bolos, M; Bozkurt, B; Carabello, B; Chan, W; Deswal, A; Mann, DL, 2012
)
1.36
"Carvedilol treatment significantly attenuated the binge-induced transient increases in BP at 4 and 5 weeks."( Cardiovascular responses and differential changes in mitogen-activated protein kinases following repeated episodes of binge drinking.
Chowdhury, SA; Fink, AM; Geenen, DL; Gu, L; Piano, MR,
)
0.85
"Carvedilol treatment in the OVX animals: prevented weight gain and slight hypertrophy, restored the reduced positive inotropic responses to Ca(2+) and isoproterenol, prevented the reduction in SERCA2a expression, abolished the increase in superoxide anion production, normalized the increase in p22(phox) expression, and decreased serum angiotensin converting enzyme (ACE) activity."( Carvedilol prevents ovariectomy-induced myocardial contractile dysfunction in female rat.
Fernandes, AA; Fiorim, J; Forechi, L; Lima, FL; Pavan, BM; Potratz, FF; Ribeiro, RF; Stefanon, I; Vassallo, DV, 2013
)
2.55
"Carvedilol treatment was even cost-effective in severe disease."( [Beta blockers in heart failure therapy with special reference to the COPERNICUS Study].
Hartmann, F; Katus, HA, 2002
)
1.04
"Carvedilol treatment abolished the increase in heart rate, SVI, and CI and caused a rise, rather than a decline, in PAP, PWP, systemic vascular resistance, and pulmonary vascular resistance during dobutamine infusion."( Beta-blocker therapy influences the hemodynamic response to inotropic agents in patients with heart failure: a randomized comparison of dobutamine and enoximone before and after chronic treatment with metoprolol or carvedilol.
Bristow, MR; D'Aloia, A; Dei Cas, L; Metra, M; Muneretto, C; Nodari, S; Robertson, AD, 2002
)
1.22
"Carvedilol-treated patients were also less likely than placebo-treated patients to experience a serious adverse event (P=0.002), especially worsening heart failure, sudden death, cardiogenic shock, or ventricular tachycardia."( Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study.
Amann-Zalan, I; Coats, AJ; DeMets, DL; Fowler, MB; Holcslaw, TL; Katus, HA; Krum, H; Mohacsi, P; Packer, M; Roecker, EB; Rouleau, JL; Staiger, C; Tendera, M, 2002
)
1.44
"Carvedilol treatment reduces the mortality rate in patients with congestive heart failure. "( Carvedilol improves left ventricular function in heart failure patients with idiopathic dilated cardiomyopathy and a wide range of sympathetic nervous system function as measured by iodine 123 metaiodobenzylguanidine.
Abraham, WT; Craft, LL; Gerson, MC; McGuire, N; Suresh, DP; Wagoner, LE,
)
3.02
"Carvedilol treatment can improve cardiac function, symptoms, and cardiac sympathetic nerve activity in patients with DCM to a similar extent as metoprolol treatment. "( Efficacy of carvedilol treatment on cardiac function and cardiac sympathetic nerve activity in patients with dilated cardiomyopathy: comparison with metoprolol therapy.
Adachi, H; Hoshizaki, H; Isobe, N; Naito, S; Oshima, S; Seki, R; Taniguchi, K; Toyama, T, 2003
)
2.14
"Carvedilol treatment for CHF patients is a highly cost-effective method of therapy in the Japanese medical environment."( Cost-effectiveness analysis of carvedilol for the treatment of chronic heart failure in Japan.
Inomata, T; Izumi, T; Kobayashi, M, 2004
)
2.05
"Carvedilol treatment significantly blocked adrenoceptors during the treatment period, delayed development (eye opening), reduced growth, and reduced arterial pressure and heart rate."( Pre-weaning carvedilol treatment in spontaneously hypertensive rats.
Anderson, WP; Boesen, EI; Kett, MM; Lambert, GW, 2004
)
1.42
"Carvedilol pre-treatment blunted both the decrease of Bcl-2 (P < 0.01) and the increase of Bax-alpha mRNA expression (P < 0.01)."( Carvedilol prevents doxorubicin-induced free radical release and apoptosis in cardiomyocytes in vitro.
Altieri, P; Ballestrero, A; Barsotti, A; Brunelli, C; Fabbi, P; Garibaldi, S; Ghigliotti, G; Manca, V; Nasti, S; Patrone, F; Rossettin, P; Spallarossa, P, 2004
)
2.49
"Carvedilol treatment was started with 3.125 mg twice daily and slowly uptitrated in 2-week intervals to 2x25 mg per day."( Betablockers in heart failure: Carvedilol Safety Assessment (CASA 2-trial).
Hess, OM; Müller, K; Rickli, H; Steiner, S, 2004
)
1.33
"Carvedilol treatment in chronic heart failure (CHF) patients has been demonstrated to reduce mortality by improving cardiac systolic function and reducing left ventricular adverse remodeling. "( Left ventricular diastolic function improvement by carvedilol therapy in advanced heart failure.
Calabria, P; Gennari, L; Martini, G; Nuti, R; Palazzuoli, A; Quatrini, I; Vecchiato, L, 2005
)
2.02
"In carvedilol-treated mice, a significant improvement in left ventricular function was documented 10 days post infection."( Carvedilol improves left ventricular function in murine coxsackievirus-induced acute myocarditis association with reduced myocardial interleukin-1beta and MMP-8 expression and a modulated immune response.
Chandrasekharan, K; Li, J; Noutsias, M; Pauschinger, M; Peter Schwimmbeck, L; Poller, W; Rutschow, S; Schultheiss, HP; Tschope, C; Weitz, A; Westermann, D; Zeichhardt, H, 2005
)
2.29
"Carvedilol treatment in experimental myocarditis leads to reduced expression of proinflammatory cytokines and MMPs, which contributes to reduced matrix degradation and ultimately to improved structural integrity of the heart. "( Carvedilol improves left ventricular function in murine coxsackievirus-induced acute myocarditis association with reduced myocardial interleukin-1beta and MMP-8 expression and a modulated immune response.
Chandrasekharan, K; Li, J; Noutsias, M; Pauschinger, M; Peter Schwimmbeck, L; Poller, W; Rutschow, S; Schultheiss, HP; Tschope, C; Weitz, A; Westermann, D; Zeichhardt, H, 2005
)
3.21
"Carvedilol treatment caused a significant reduction in CANESP while metoprolol had a neutral effect (-95+/-27 vs."( Selective versus nonselective beta-adrenergic receptor blockade in chronic heart failure: differential effects on myocardial energy substrate utilization.
Al-Hesayen, A; Azevedo, ER; Floras, JS; Hollingshead, S; Lopaschuk, GD; Parker, JD, 2005
)
1.05
"Carvedilol treatment caused a 20% reduction in myocardial free fatty acid extraction while metoprolol had a neutral effect. "( Selective versus nonselective beta-adrenergic receptor blockade in chronic heart failure: differential effects on myocardial energy substrate utilization.
Al-Hesayen, A; Azevedo, ER; Floras, JS; Hollingshead, S; Lopaschuk, GD; Parker, JD, 2005
)
1.77
"Carvedilol pretreatment followed by epinephrine treatment reduced early postresuscitation ventricular ectopy (116 +/- 147 vs 834 +/- 380, P < .01) and minimized increases in arterial blood lactate at 5 minutes after resuscitation (10.9 +/- 2.1 mmol/L vs 17.4 +/- 3.5 mmol/L, P < .01)."( Carvedilol mitigates adverse effects of epinephrine during cardiopulmonary resuscitation.
Fang, X; Huang, L; Sun, S; Tang, W; Weil, MH, 2005
)
2.49
"Carvedilol treatment in chronic heart failure (CHF) demonstrated to reduce mortality and rehospitalisation, and improvement of cardiac systolic function with reduction of left ventricular volumes and remodelling. "( Effects of carvedilol on left ventricular diastolic function and chamber volumes in advanced heart failure.
De Paola, V; Iovine, F; Martini, G; Nuti, R; Palazzuoli, A; Quatrini, I; Scali, C; Vecchiato, L, 2005
)
2.16
"Carvedilol treatment improve diastolic function in CHF with severe diastolic impairment driving restrictive or pseudonormal filling pattern towards altered pattern at early time. "( Effects of carvedilol on left ventricular diastolic function and chamber volumes in advanced heart failure.
De Paola, V; Iovine, F; Martini, G; Nuti, R; Palazzuoli, A; Quatrini, I; Scali, C; Vecchiato, L, 2005
)
2.16
"Carvedilol treatment of hibernating myocardium results in improved functional recovery after revascularization compared with metoprolol tartrate, and this might partially be related to reduced cardiomyocyte degeneration."( Carvedilol improves myocardial contractility compared with metoprolol in patients with chronic hibernating myocardium after revascularization.
Diep, TP; Grohmann, B; Gupta, R; Kostin, S; Nowak, B; Schaper, J; Schwarz, ER; Uretsky, BF, 2005
)
3.21
"Carvedilol treatment in patients with CHF results in reduced oxidative stress without restoration of the chronotropic responsiveness index."( Effects of carvedilol on oxidative stress and chronotropic response to exercise in patients with chronic heart failure.
Alcaino, H; Castro, P; Chiong, M; Copaja, M; Corbalan, R; Díaz-Araya, G; Greig, D; Lavandero, S; Pérez, O; Valenzuela, R; Vukasovic, JL, 2005
)
2.16
"Carvedilol treatment did not affect serum biochemistry in either sham-operated or cirrhotic rats. "( Hemodynamic effects of one week of carvedilol administration on cirrhotic rats.
Hou, MC; Huang, YT; Lee, SD; Lee, TY; Lin, HC; Wang, YW; Wei, HC; Yang, YY, 2006
)
2.05
"Carvedilol treatment increased activities of antioxidant enzymes and expression of Bcl-2 in healthy rats as well as diabetic rats."( Carvedilol improved diabetic rat cardiac function depending on antioxidant ability.
Huang, H; Pan, XH; Qian, LB; Shan, J; Wang, HP; Xia, Q, 2007
)
2.5
"Carvedilol treatment increased activities of antioxidant enzymes and expression of Bcl-2 in healthy rats as well as diabetic rats."( Carvedilol protected diabetic rat hearts via reducing oxidative stress.
Huang, H; Pan, XH; Qian, LB; Shan, J; Wang, HP, 2006
)
2.5
"Carvedilol treatment attenuated the nicotine-induced heart rate, systolic and diastolic blood pressure increases."( Adrenergic blocker carvedilol attenuates the cardiovascular and aversive effects of nicotine in abstinent smokers.
Kosten, T; Mouratidis, M; Sofuoglu, M; Yoo, S, 2006
)
1.38
"Carvedilol pretreated patients had higher amount of serum UA (p<0.05) comparing to non-treated patients. "( Elevated serum uric acid reduce heart damage in patients undergoing opern-heart surgery.
Blagojevć, D; Davidović, B; Kastratović, D; Mijalković, D; Nikolić, A; Spasić, M, 2006
)
1.78
"Carvedilol treatment improved maximal DT and significantly decreased tension-dependent ATP consumption without altering myofibrillar Ca(2+) sensitivity."( Chronic treatment with carvedilol improves Ca(2+)-dependent ATP consumption in triton X-skinned fiber preparations of human myocardium.
Bloch, W; Boelck, B; Brixius, K; Grafweg, S; Hoyer, F; Lu, R; Mehlhorn, U; Pott, C; Schwinger, RH, 2007
)
1.37
"Carvedilol treatment reversed thyroxin induced hypertriglyceridemia, whereas propranolol treatment had no effect."( Comparative effectiveness of carvedilol and propranolol on glycemic control and insulin resistance associated with L-thyroxin-induced hyperthyroidism--an experimental study.
Bhatt, P; Goyal, R; Makwana, D; Santani, D, 2007
)
1.35
"The carvedilol group was treated with mean daily dose of 46 +/- 9 mg and metoprolol group with mean daily dose of 93 +/- 11 mg."( Optimal beta-blocker for prevention of atrial fibrillation after on-pump coronary artery bypass graft surgery: carvedilol versus metoprolol.
Alizadeh, A; Emkanjoo, Z; Fazelifar, AF; Ghafarinejad, MH; Givtaj, N; Haghjoo, M; Hashemi, MJ; Hosseini, S; Khamoushi, AJ; Sadr-Ameli, MA; Saravi, M, 2007
)
1.03
"Carvedilol treatment for 4 months resulted in a significant improvement of RVEF, which paralleled the improvement of LVEF and the decreasing of TNF-alpha and IL-6 levels in patients with systolic HF."( Effects of carvedilol on right ventricular ejection fraction and cytokines levels in patients with systolic heart failure.
Aktoz, M; Buyuklu, M; Kurum, T; Tatli, E, 2008
)
2.18
"Carvedilol treatment did not result in significant changes in neurohormonal activation, radiographic heart size, heart rate, or owner perceived quality-of-life."( Carvedilol in dogs with dilated cardiomyopathy.
Bulmer, BJ; Fuentes, VL; Luethy, MW; Oyama, MA; Prosek, R; Sisson, DD,
)
2.3
"Carvedilol treatment did not significantly alter nerve conduction in non-diabetic rats."( Neuroprotective effects of carvedilol in diabetic rats: prevention of defective peripheral nerve perfusion and conduction velocity.
Cameron, NE; Cotter, MA, 1995
)
1.31
"Carvedilol-treated patients also reported a significant lessening of heart failure symptoms (p < 0.05 vs."( Carvedilol improves left ventricular function and symptoms in chronic heart failure: a double-blind randomized study.
Bristow, MR; Gilbert, EM; Olsen, SL; Renlund, DG; Taylor, DO; Yanowitz, FD, 1995
)
2.46
"Carvedilol-treated SHR had significantly reduced systolic blood pressures and heart rates throughout the duration of the experiment, and had significantly reduced ventricle/body weights by approximately 9.0%."( Carvedilol, a novel cardiovascular agent, inhibits development of vascular and ventricular hypertrophy in spontaneously hypertensive rats.
Arleth, A; Barone, F; Camden, A; McCartney, L; Ohlstein, EH; Sung, CP; Vickery, L, 1994
)
2.45
"Carvedilol treatment, however, resulted in a small amelioration of insulin resistance and a better lipid profile [corrected]."( Differential effect of chronic treatment with two beta-blocking agents on insulin sensitivity: the carvedilol-metoprolol study.
Agrawal, B; Augustin, HJ; Dietze, GJ; Jacob, S; Rett, K; Wicklmayr, M, 1996
)
1.23
"Carvedilol treatment also reduced the extent of in vivo LDL oxidation, as reflected by the decrease in antioxidized LDL autoantibody titer."( Protective effects of carvedilol, a vasodilating beta-adrenoceptor blocker, against in vivo low density lipoprotein oxidation in essential hypertension.
Bellomo, G; Covini, D; Maggi, E; Marchesi, E; Negro, C; Perani, G, 1996
)
1.33
"Carvedilol treatment improved the impairment in the preparation from SHRSP."( Effects of chronic treatment with carvedilol on abnormalities of endothelium-dependent relaxation and structure of endothelium in resistance arteries of SHRSP.
Hashimoto, H; Sasaki, F; Shibutani, T; Shimamura, K; Sunano, S; Tanaka, M; Yamamoto, K, 1995
)
1.29
"Carvedilol treatment resulted in a significant improvement of RV ejection fraction and systolic performance, which paralleled the improvement of systolic function demonstrated in the left ventricle."( Effects of carvedilol on right ventricular function in chronic heart failure.
Bristow, MR; Christian, PE; Datz, FL; Gilbert, EM; Quaife, RA; Volkman, K, 1998
)
1.41
"Carvedilol treatment resulted in sustained reduction of pressure-rate-index and significantly smaller infarcts (22.0+/-2.5%, P < 0.01 vs."( Comparison of metoprolol and carvedilol pharmacology and cardioprotection in rabbit ischemia and reperfusion model.
Arch, JR; Cheng, HY; Feuerstein, G; Hieble, JP; Liu, GL; Ma, XL; Ruffolo, RR; Yue, TL, 1998
)
1.31
"Carvedilol treatment had a beneficial effect on lipid pattern and reduced lipid oxidation, but there was no obvious effect on progression of chronic rejection."( Carvedilol treatment of kidney graft recipients with chronic rejection.
Backman, U; Fellström, B; Larsson, E; Vessby, B; Zezina, L, 1999
)
2.47
"Carvedilol treatment improved ventricular function and reduced the incidence of arrhythmic episodes."( Efficacy of carvedilol on complex ventricular arrhythmias in dilated cardiomyopathy: double-blind, randomized, placebo-controlled study.
Cice, G; Ferrara, L; Iacono, A; Tagliamonte, E, 2000
)
1.41
"Carvedilol treatment resulted in sustained reduction of the pressure-rate-index and significantly smaller infarcts (30+/-2.9, P<0.01 vs."( Comparison of bisoprolol and carvedilol cardioprotection in a rabbit ischemia and reperfusion model.
Chen, J; Christopher, TA; Gao, F; Gu, J; Lopez, BL; Lysko, P; Ma, XL; Ohlstein, EH; Ruffolo, RR; Yue, TL, 2000
)
1.32
"Carvedilol treatment improved left ventricular (LV) function. "( Dilated cardiomyopathy in dialysis patients--beneficial effects of carvedilol: a double-blind, placebo-controlled trial.
Cice, G; Di Benedetto, A; Ferrara, L; Iacono, A; Marinelli, G; Pavese, F; Russo, PE, 2001
)
1.99
"Carvedilol treatment in patients with heart failure results in a 57% decrease in myocardial FFA use without a significant change in glucose use. "( Myocardial free fatty acid and glucose use after carvedilol treatment in patients with congestive heart failure.
DeGrado, TR; Nickles, RJ; Russell, DC; Stanko, P; Stone, CK; Taylor, M; Wallhaus, TR, 2001
)
2.01
"2. Carvedilol treatment for 11 to 18 weeks did not alter systolic blood pressure in SHR-SP rats, however, it resulted in a significant reduction in heart rate."( Renoprotective effects of carvedilol in hypertensive-stroke prone rats may involve inhibition of TGF beta expression.
Barone, F; Brooks, DP; Campbell, WG; Contino, LC; Gygielko, E; Laping, NJ; Nelson, AH; Olson, BA; Wong, VY, 2001
)
1.12
"Carvedilol-treated patients had less frequent hospital admissions and shorter lengths of stay compared with patients not receiving carvedilol."( Medical resource use and costs of congestive heart failure after carvedilol use.
Antell, L; Goldberg Arnold, RJ; Kaniecki, DJ; Najib, MM; Pettit, KG; Roth, D; Xuan, J,
)
1.09
"Carvedilol treatment reduced the rate-pressure product (8,781 +/- 2,672 vs 6,342 +/- 1,346, p <0.01) and improved ejection fraction (29 +/- 7% vs 37 +/- 11%, p <0.001), whereas no changes were observed in the control group."( Effect of carvedilol on microcirculatory and glucose metabolic regulation in patients with congestive heart failure secondary to ischemic cardiomyopathy.
Andreasen, F; Bøttcher, M; Gøtzsche, O; Nielsen, TT; Refsgaard, J, 2002
)
1.44
"Carvedilol-treated animals exhibited a 78% reduction in infarct size compared to vehicle controls, such that the percentage of the left ventricle infarcted was reduced significantly from 16.2 +/- 4.1% in control animals to 3.6 +/- 1.3% in animals treated with carvedilol (p = 0.017, n = 6)."( Carvedilol (Kredex) reduces infarct size in a canine model of acute myocardial infarction.
Barone, FC; Feuerstein, GZ; Hamburger, SA; Ruffolo, RR, 1991
)
2.45
"Carvedilol is a novel treatment for hypertension, having a balanced pharmacology of vasodilation and beta-receptor blockade. "( A comparative study of carvedilol, slow-release nifedipine, and atenolol in the management of essential hypertension.
Ball, SG; Dixon, S; Hall, S; Hallman, RJ; Harvey, RE; Prescott, RI, 1991
)
2.03
"Treatment with carvedilol and nebivolol resulted in a significant reduction in calcium handling abnormalities in the RYR2-hiPSC-CMs."( Characterization of the mechanism by which a nonsense variant in RYR2 leads to disordered calcium handling.
Arbel, G; Bates, N; Brown, B; Gepstein, A; Gepstein, L; Hopton, C; Huber, I; Kimber, SJ; Maizels, L; Newman, WG; Tijsen, AJ; Venetucci, L, 2022
)
1.06
"Treatment with carvedilol had an inverse relation with SDANN."( Heart rate variability is associated with disease severity and portal hypertension in cirrhosis.
Amodio, E; Basso, MG; Cabibbo, G; Calvaruso, V; Casuccio, A; Craxì, A; Daidone, M; Di Raimondo, D; Licata, M; Miceli, G; Pennisi, G; Petta, S; Pinto, A; Pintus, C; Simone, F; Tuttolomondo, A; Velardo, M, 2023
)
1.25
"Treatment with carvedilol blocked the effects of sympathetic nervous system activation, reducing primary tumour growth and metastasis in a mouse model of breast cancer and preventing invasion by breast cancer cell lines. "( Carvedilol blocks neural regulation of breast cancer progression in vivo and is associated with reduced breast cancer mortality in patients.
Andreassen, BK; Baker, JG; Botteri, E; Chang, A; Chung, NC; Gillis, RD; Halls, ML; Pon, CK; Shackleford, DM; Sloan, EK; Ziegler, AI, 2021
)
2.42
"Treatment with carvedilol or amlodipine completely prevented left ventricular collagen deposition and morphometric alterations in aorta."( Effects of carvedilol or amlodipine on target organ damage in L-NAME hypertensive rats: their relationship with blood pressure variability.
Berg, G; Bertera, FM; Carranza, A; Chiappetta, DA; Del Mauro, JS; Donato, M; Fernandez Machulsky, N; Gelpi, RJ; González, GE; Gorzalczany, SB; Höcht, C; Morales, C; Morettón, MA; Prince, PD; Taira, CA, 2017
)
1.18
"Treatment with carvedilol directly improved the systolic function of the right and left ventricles."( Regular Treatment Strategy with a Large Amount of Carvedilol for Heart Failure Improves Biventricular Systolic Failure in a Patient with Repaired Tetralogy of Fallot.
Hirata, Y; Inaba, T; Ishikawa, Y; Komuro, I; Saito, A; Soma, K; Yao, A, 2018
)
1.07
"Treatment with carvedilol restored VMH lactate levels and improved the adrenaline (epinephrine) responses."( Carvedilol prevents counterregulatory failure and impaired hypoglycaemia awareness in non-diabetic recurrently hypoglycaemic rats.
Chan, O; Farhat, R; Fisher, SJ; Knight, N; Sejling, AS; Su, G, 2019
)
2.3
"Treatment with carvedilol was associated with a significantly decreased risk of hospitalization for HF or death when compared with metoprolol (hazard ratio [HR]: 0.70, [95% confidence interval (CI): 0.57 to 0.87], p = 0.001)."( Effect of metoprolol versus carvedilol on outcomes in MADIT-CRT (multicenter automatic defibrillator implantation trial with cardiac resynchronization therapy).
Alexis, J; Jons, C; McNitt, S; Moss, AJ; Ruwald, AC; Ruwald, MH; Zareba, W, 2013
)
1.02
"Treatment with carvedilol is an established primary therapy for patients with heart failure (HF). "( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
1.1
"Treatment with carvedilol was associated with a significantly decreased risk of inappropriate therapy compared with metoprolol (hazard ratio [HR]: 0.64 [95% confidence interval (CI): 0.48 to 0.85]; p = 0.002)."( Impact of carvedilol and metoprolol on inappropriate implantable cardioverter-defibrillator therapy: the MADIT-CRT trial (Multicenter Automatic Defibrillator Implantation With Cardiac Resynchronization Therapy).
Abu-Zeitone, A; Jons, C; Kutyifa, V; McNitt, S; Moss, AJ; Ruwald, AC; Ruwald, MH; Zareba, W, 2013
)
1.13
"Treatment with carvedilol had no adverse events."( Effect of Carvedilol on Serum Heart-type Fatty Acid-binding Protein, Brain Natriuretic Peptide, and Cardiac Function in Patients With Chronic Heart Failure.
Li, DH; Ma, SC; Qiao, LY; Shan, RB; Sun, YP; Wei, CP; Zhang, YF, 2015
)
1.16
"Pretreatment with carvedilol attenuated LPO elevation, mucus content and sulfhydryl group inhibitions."( Carvedilol attenuates inflammatory biomarkers and oxidative stress in a rat model of ulcerative colitis.
Abuohashish, HM; Ahmed, MM; Al-Hosaini, KA; Al-Rejaie, SS; Fatani, AJ; Parmar, MY, 2015
)
2.18
"Treatment with carvedilol prevented the MI-induced decrease in total and phosphorylated Cx43 levels (91 +/- 17% and 80 +/- 20%, both P < 0.05), respectively, which were similar to the levels of sham animals."( Carvedilol ameliorates the decreases in connexin 43 and ventricular fibrillation threshold in rats with myocardial infarction.
Chen, J; He, B; Hu, X; Jiang, H; Lu, Z; Wen, H; Zhao, D, 2009
)
2.14
"Treatment with carvedilol did not change insulin-stimulated endothelial function."( Metoprolol compared to carvedilol deteriorates insulin-stimulated endothelial function in patients with type 2 diabetes - a randomized study.
Christiansen, B; Dominguez, H; Hermann, TS; Kveiborg, B; Køber, L; Major-Pedersen, A; Rask-Madsen, C; Raunsø, J; Torp-Pedersen, C, 2010
)
1.01
"Pretreatment of carvedilol orally at a dose of 1 mg/kg body weight for 2 weeks significantly prevented initial reduction in serum electrolyte levels induced by adrenaline."( Effect of carvedilol on adrenaline-induced changes in serum electrolytes in rat.
Akhter, N; Nahar, N, 2009
)
1.09
"Treatment with carvedilol significantly decreased plasma creatinine levels after IRI (up to 168 hr) compared to controls (P < 0.001), suggesting an improvement in renal function. "( Carvedilol protects tubular epithelial cells from ischemia-reperfusion injury by inhibiting oxidative stress.
De Velasco, MA; Hayashi, T; Ishii, T; Nishioka, T; Nose, K; Saitou, Y; Uemura, H, 2010
)
2.16
"Treatment with carvedilol, BM 91.0228, and tocopherol significantly improved antioxidative status of allograft kidney recipients."( Oxidative stress in chronic renal allograft nephropathy in rats: effects of long-term treatment with carvedilol, BM 91.0228, or alpha-tocopherol.
Back, WE; Braun, C; Göttmann, U; Knoll, T; Oltersdorf, J; Schaub, M; van der Woude, FJ, 2003
)
0.87
"Treatment with carvedilol resulted in a significant improvement in E:A ratio in patients with heart failure due to a LV relaxation abnormality. "( Effect of carvedilol on diastolic function in patients with diastolic heart failure and preserved systolic function. Results of the Swedish Doppler-echocardiographic study (SWEDIC).
Andersson, B; Bergström, A; Dahlström, U; Edner, M; Nylander, E; Persson, H, 2004
)
1.08
"Pre-treatment with carvedilol significantly attenuated the doxorubicin-induced increases in DCF (P < 0.001 compared to cells not pre-treated with carvedilol) and HE (P < 0.01) fluorescence."( Carvedilol prevents doxorubicin-induced free radical release and apoptosis in cardiomyocytes in vitro.
Altieri, P; Ballestrero, A; Barsotti, A; Brunelli, C; Fabbi, P; Garibaldi, S; Ghigliotti, G; Manca, V; Nasti, S; Patrone, F; Rossettin, P; Spallarossa, P, 2004
)
2.09
"The treatment of carvedilol was initiated in a majority of cases by hospital specialists (87%, n = 735), however, for most of them, further supervision of treatment was done under shared care between GPs and hospitals (70%, n = 595)."( Observational cohort study to monitor the use and safety of carvedilol in the treatment of heart failure in clinical practice in England--1st interim report.
Acharya, NV; Shakir, SA; Wilton, LV, 2005
)
0.9
"Treatment with carvedilol in the shunt group reversed the heart weight and ventricular dimension to the baseline values."( Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure.
Chang, H; Kuan, P; Lu, MJ; Shyu, KG; Sun, HY; Wang, BW, 2005
)
2.11
"Treatment with carvedilol is associated with a reversal of abnormal regulation of HIF-1alpha and VEGF in the failing ventricular myocardium."( Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure.
Chang, H; Kuan, P; Lu, MJ; Shyu, KG; Sun, HY; Wang, BW, 2005
)
2.11
"Treatment with carvedilol compared with metoprolol offers additional benefits among patients with atrial fibrillation."( Prognostic relevance of atrial fibrillation in patients with chronic heart failure on long-term treatment with beta-blockers: results from COMET.
Charlesworth, A; Cleland, J; Hanrath, P; Komajda, M; Metra, M; Olsson, LG; Poole-Wilson, P; Swedberg, K; Torp-Pedersen, C, 2005
)
0.67
"Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values."( Carvedilol prevents cardiac hypertrophy and overexpression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in pressure-overloaded rat heart.
Chang, H; Fang, WJ; Liou, JY; Shyu, KG; Wang, BW, 2005
)
2.11
"Pre-treatment with carvedilol or dexrazoxane prevented these effects."( Matrix metalloproteinase-2 and -9 are induced differently by doxorubicin in H9c2 cells: The role of MAP kinases and NAD(P)H oxidase.
Altieri, P; Ballestrero, A; Barisione, C; Barsotti, A; Brunelli, C; Fabbi, P; Garibaldi, S; Ghigliotti, G; Manca, V; Spallarossa, P, 2006
)
0.65
"Treatment with carvedilol 1) reduced the pro-inflammatory cytokines and fibrogenic cytokine TGF-beta1 levels in myocardium and was associated with the amelioration of the elevated left ventricular diastolic pressure. "( Effects of carvedilol on cardiac cytokines expression and remodeling in rat with acute myocardial infarction.
Cheng, X; Ge, H; Guo, H; Li, B; Liao, YH; Wang, M, 2006
)
1.08
"Treatment with carvedilol was associated with significant increases in total frequency power, very low frequency power, high frequency power, SDNN, the root-mean square of difference of successive RRs, and pNN50."( Changes in heart rate variability are correlated to hemodynamic improvement with chronic CARVEDILOL therapy in heart failure.
Alharethi, R; Bristow, MR; Bullinga, JR; Gilbert, EM; Schram, MS, 2005
)
0.89
"Pretreatment with carvedilol preserves endothelial junctions and reduces myocardial no-reflow after acute myocardial infarction and reperfusion. "( Carvedilol preserves endothelial junctions and reduces myocardial no-reflow after acute myocardial infarction and reperfusion.
Cui, C; Gao, R; Yang, Y; you, S; Zhao, J, 2007
)
2.12
"Treatment with carvedilol might be effective for decreasing the oxidative DNA damage."( Elevated levels of oxidative DNA damage in serum and myocardium of patients with heart failure.
Banba, K; Kimura, H; Kono, Y; Kusano, KF; Matsubara, H; Miura, A; Nagase, S; Nakamura, K; Nishii, N; Ohe, T; Sakuragi, S; Watanabe, A, 2006
)
0.67
"Treatment with carvedilol in the shunt group reversed the increase in heart weight and ventricular dimension to the baseline values."( Myostatin expression in ventricular myocardium in a rat model of volume-overload heart failure.
Chang, H; Lu, MJ; Shyu, KG; Sun, HY; Wang, BW, 2006
)
0.67
"Treatment with carvedilol is associated with a limitation of increased myostatin expression in the failing ventricular myocardium."( Myostatin expression in ventricular myocardium in a rat model of volume-overload heart failure.
Chang, H; Lu, MJ; Shyu, KG; Sun, HY; Wang, BW, 2006
)
0.67
"Treatment with carvedilol dramatically improved isometric tetanic force production at stimulus frequencies from 40 to 100 Hz (P < 0.05)."( Myofibrillar protein oxidation and contractile dysfunction in hyperthyroid rat diaphragm.
Matsunaga, S; Mishima, T; Sakamoto, M; Sugiyama, M; Wada, M; Yamada, T, 2007
)
0.68
"Treatment with carvedilol was associated with a trend toward an increase in LVEF (absolute difference between groups, 2.3%; P = .094)."( A randomized trial of carvedilol after renin-angiotensin system inhibition in chronic Chagas cardiomyopathy.
Botoni, FA; Dantas, JB; Ferreira, CS; Okonko, DO; Oliveira, BM; Pinto, AS; Poole-Wilson, PA; Reis, AM; Ribeiro, AL; Rocha, MO; Tavares, WC; Teixeira, AL; Teixeira, MM, 2007
)
0.99
"Treatment with carvedilol for 5 weeks prevented the inhibition of endothelium-dependent relaxation and the decrease of serum NO levels caused by diabetes."( Carvedilol ameliorates endothelial dysfunction in streptozotocin-induced diabetic rats.
Chen, F; Fu, GS; Huang, H; Ke, XY; Qian, LB; Wang, HP; Xia, Q, 2007
)
2.12
"Treatment with carvedilol, in comparison to that with metoprolol in patients with AMI and LV dysfunction, did not differ significantly in regard to the primary end point of t-CAE or to the secondary end point of t-CHE but resulted in better long-term quality of life and favorable early safety profile."( Randomized active-controlled study comparing effects of treatment with carvedilol versus metoprolol in patients with left ventricular dysfunction after acute myocardial infarction.
Asanin, MR; Jelena, MM; Lasica, RM; Matic, MD; Mrdovic, IB; Ostojic, MC; Perunicic, JP; Savic, LZ; Vasiljevic, ZM, 2007
)
0.93
"Treatment with carvedilol reduced IS more than did treatment with propranolol/doxazosin (p < 0.05)."( Carvedilol protects against lethal reperfusion injury through antiadrenergic mechanisms.
Berge, RK; Brunvand, H; Grong, K; Kvitting, PM; Rynning, SE, 1996
)
2.08
"Pretreatment with carvedilol retarded loss of contraction in both axes."( Carvedilol retards sudden loss of contraction during early regional myocardial ischemia in feline hearts.
Brunvand, H; Grong, K, 1997
)
2.06
"Pretreatment with carvedilol was followed by a more pronounced contrast intensity than was with metoprolol."( [The effect of carvedilol on contrast echocardiography in comparison to metoprolol in conscious dogs].
Beller, KD; Diedrich, F; Sponer, G, 1999
)
0.98
"Treatment with carvedilol resulted in significantly lower urinary protein excretion (37+/-15 mg day(-1))."( Renoprotective effects of carvedilol in hypertensive-stroke prone rats may involve inhibition of TGF beta expression.
Barone, F; Brooks, DP; Campbell, WG; Contino, LC; Gygielko, E; Laping, NJ; Nelson, AH; Olson, BA; Wong, VY, 2001
)
0.95
"Treatment with carvedilol was associated with a significant decrease in the risk of any hospitalization (adjusted odds ratio 0.35, 95% CI 0.20 to 0.63; p <0.001)."( Reimbursement claims analysis of outcomes with carvedilol and metoprolol.
Antell, LA; Chang, LL; Luzier, AB; Roth, DA; Xuan, J, 2002
)
0.91
"The treatment with carvedilol caused a significant decrease in blood pressure. "( Carvedilol does not modulate moderate exercise-induced hyperkalemia in hemodialysis patients.
Klimek, D; Kokot, F; Nowicki, M; Szewczyk-Seifert, G, 2002
)
2.09
"Treatment with carvedilol produced a significant decrease in blood pressure from 172/101 to 150/87mm Hg (p less than 0.01), but it did not cause orthostatic hypotension."( Therapeutic benefits and safety of carvedilol in the treatment of renal hypertension. An open, short term study. Carvedilol Renal Hypertension Study Group in Japan.
Fujishima, M; Fukiyama, K; Ishii, M; Kohno, M; Kubo, S; Mizuno, Y; Saruta, T; Takeda, T; Yoshimura, M, 1988
)
0.89

Toxicity

Carvedilol has been shown to be effective and safe in patients with essential hypertension when given as mono. No events were identified as new signals (according to the ID1-ID2 statistic) of adverse events associated with carvedilol.

ExcerptReferenceRelevance
" Adverse events on treatment, particularly those correlated to vasodilation, were less frequent in the carvedilol group."( Efficacy and safety of carvedilol in comparison with nifedipine sustained-release in chronic stable angina.
Derr, I; Eberhardt, R; Ehmer, B; van der Does, R, 1992
)
0.81
"Carvedilol has been shown to be effective and safe in patients with essential hypertension when given as monotherapy."( Safety and antihypertensive efficacy of carvedilol and atenolol alone and in combination with hydrochlorothiazide.
Hörrmann, M; Machwirth, M; van der Does, R; Widmann, L, 1990
)
1.99
" Nine patients experienced adverse events during combination treatment."( The safety of adding carvedilol to hypertensive patients inadequately treated with diuretics.
Dupont, AG; Schoors, DF; Venuti, RP, 1990
)
0.6
" These results suggest that carvedilol is a useful and safe drug for the treatment of renal hypertension."( Therapeutic benefits and safety of carvedilol in the treatment of renal hypertension. An open, short term study. Carvedilol Renal Hypertension Study Group in Japan.
Fujishima, M; Fukiyama, K; Ishii, M; Kohno, M; Kubo, S; Mizuno, Y; Saruta, T; Takeda, T; Yoshimura, M, 1988
)
0.85
" Beta-blockers have often been viewed as contraindicated in this group because of their potential adverse short-term effects on cardiac function."( Safety and efficacy of carvedilol in severe heart failure. The U.S. Carvedilol Heart Failure Study Group.
Bristow, MR; Cohn, JN; Colucci, WS; Fowler, MB; Gilbert, EM; Holcslaw, TL; Kinhal, V; Krueger, SK; Lejemtel, T; Lukas, MA; Narahara, KA; Packer, M; Young, ST, 1997
)
0.61
" Ten patients (8%) did not complete the open-label period because of adverse events and 11."( Safety and efficacy of carvedilol in severe heart failure. The U.S. Carvedilol Heart Failure Study Group.
Bristow, MR; Cohn, JN; Colucci, WS; Fowler, MB; Gilbert, EM; Holcslaw, TL; Kinhal, V; Krueger, SK; Lejemtel, T; Lukas, MA; Narahara, KA; Packer, M; Young, ST, 1997
)
0.61
" The main adverse events during this double-blind period were worsened heart failure, hypotension/dizziness, bradycardia/atrioventricular block, and aggravation of angina."( Efficacy and safety of carvedilol in patients with chronic heart failure receiving concomitant amiodarone therapy. Australia/New Zealand Heart Failure Research Collaborative Group.
Krum, H; MacMahon, S; Sharpe, N; Shusterman, N, 1998
)
0.61
" Carvedilol can be added to amiodarone in these patients without expectation of increased adverse effects or loss of clinical efficacy."( Efficacy and safety of carvedilol in patients with chronic heart failure receiving concomitant amiodarone therapy. Australia/New Zealand Heart Failure Research Collaborative Group.
Krum, H; MacMahon, S; Sharpe, N; Shusterman, N, 1998
)
1.52
" Carvedilol low dose/high dose was shown to be at least as safe and well tolerated as metoprolol low dose/high dose both in younger and elderly patients."( Comparison of safety and efficacy of carvedilol and metoprolol in stable angina pectoris.
Griffiths, M; Hauf-Zachariou, U; Holtbrügge, W; König, S; Lahiri, A; Pfarr, E; van der Does, R, 1999
)
1.49
" Carvedilol and verapamil (10 micromol/L) reduced the LD50 (dose which results in the death of half the number of cells) of the Hs578T-Dox subline from 200 mg/L to approx."( Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity.
Behnam-Motlagh, P; Grankvist, K; Henriksson, R; Jonsson, O; Persson, M, 1999
)
1.48
" The purpose of this study was to assess whether treatment with carvedilol is efficacious and safe for infants with dilated cardiomyopathy who do not show satisfactory clinical improvement despite treatment with conventional medications."( Efficacy and safety of carvedilol in infants with dilated cardiomyopathy: a preliminary report.
Farzana, F; Gachara, N; Krishnan, U; Prabhakaran, S; Shah, MJ; Srinivas, S,
)
0.68
" No adverse events related to carvedilol administration occurred."( Efficacy and safety of carvedilol in infants with dilated cardiomyopathy: a preliminary report.
Farzana, F; Gachara, N; Krishnan, U; Prabhakaran, S; Shah, MJ; Srinivas, S,
)
0.73
"To the best of our knowledge, the adverse reaction presented in this case report is rare."( Hepatotoxicity associated with carvedilol.
Hagmeyer, KO; Stein, J, 2001
)
0.6
"Beta-blockers substantially improve survival in patients with chronic heart failure (HF) with left ventricular systolic dysfunction, but concerns about cardiovascular adverse effects may deter physicians from prescribing this therapy."( Adverse effects of beta-blocker therapy for patients with heart failure: a quantitative overview of randomized trials.
Coffey, CS; Curtis, JP; Foody, JM; Hebert, PR; Ko, DT; Krumholz, HM; Sedrakyan, A, 2004
)
0.32
" 59 patients (41%) experienced minor and nine (6%) serious adverse events."( Betablockers in heart failure: Carvedilol Safety Assessment (CASA 2-trial).
Hess, OM; Müller, K; Rickli, H; Steiner, S, 2004
)
0.61
" Serious adverse events and hospitalisations are rare."( Betablockers in heart failure: Carvedilol Safety Assessment (CASA 2-trial).
Hess, OM; Müller, K; Rickli, H; Steiner, S, 2004
)
0.61
" The utilization of carvedilol, management of adverse events in the community and the symptomatic progression of heart failure were examined."( Observational cohort study to monitor the use and safety of carvedilol in the treatment of heart failure in clinical practice in England--1st interim report.
Acharya, NV; Shakir, SA; Wilton, LV, 2005
)
0.89
" No events were identified as new signals (according to the ID1-ID2 statistic) of adverse events associated with carvedilol."( Observational cohort study to monitor the use and safety of carvedilol in the treatment of heart failure in clinical practice in England--1st interim report.
Acharya, NV; Shakir, SA; Wilton, LV, 2005
)
0.78
"Earlier studies have implicated the adverse effects of beta- and alpha(1)-adrenergic receptors during cardiopulmonary resuscitation (CPR)."( Carvedilol mitigates adverse effects of epinephrine during cardiopulmonary resuscitation.
Fang, X; Huang, L; Sun, S; Tang, W; Weil, MH, 2005
)
1.77
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Carvedilol was well tolerated, and no serious adverse events were identified."( Safety and efficacy of carvedilol therapy for patients with dilated cardiomyopathy secondary to muscular dystrophy.
Colan, SD; Darras, BT; Geva, T; Jenkins, KJ; Margossian, R; Powell, AJ; Rhodes, J, 2008
)
1.57
"Carvedilol therapy appears to be safe for patients with DCM secondary to muscular dystrophy and produces a modest improvement in systolic and diastolic function."( Safety and efficacy of carvedilol therapy for patients with dilated cardiomyopathy secondary to muscular dystrophy.
Colan, SD; Darras, BT; Geva, T; Jenkins, KJ; Margossian, R; Powell, AJ; Rhodes, J, 2008
)
2.1
"Clozapine is contraindicated in patients who experienced cardiac adverse effects during therapy."( Beta-blocker and angiotensin-converting enzyme inhibitor may limit certain cardiac adverse effects of clozapine.
Di Norscia, G; Gensini, GF; Placidi, GF; Rostagno, C,
)
0.13
" Therefore, oral loading with propafenone (as "pill-in-the-pocket" treatment of recent-onset atrial fibrillation) in a patient on concurrent carvedilol treatment may lead to a pharmacokinetic interaction, with high plasma levels of propafenone and potential drug-related adverse effects."( Atrial fibrillation: adverse effects of "pill-in-the-pocket" treatment and propafenone-carvedilol interaction.
Biffi, M; Boriani, G; Diemberger, I; Domenichini, G; Martignani, C; Marziali, A, 2010
)
0.78
" This study retrospectively assessed the efficacy and adverse reactions based on changes of symptoms, cardiothoracic ratio (CTR), left ventricular ejection fraction (LVEF), and human atrial natriuretic peptide (hANP)/b-type natriuretic peptide (BNP) blood levels."( Efficacy and safety of carvedilol for heart failure in children and patients with congenital heart disease.
Ando, M; Hatai, Y; Mori, K; Murakami, Y; Nishiyama, M; Park, IS; Takahashi, Y; Yoshikawa, T, 2009
)
0.66
" We assessed whether treatment of systolic HF with carvedilol is efficacious and safe in adults with CKD."( Efficacy and safety of carvedilol in treatment of heart failure with chronic kidney disease: a meta-analysis of randomized trials.
Beck, GJ; Berl, T; Chartyan, DM; Cheung, AK; Chonchol, M; Cooper, C; Henrich, WL; Himmelfarb, J; Iyengar, M; Lukas, MA; Wali, RK; Weir, MR, 2011
)
0.93
" We aimed to evaluate the relation between SRH and adverse events during titration of beta-blockers in elderly patients with heart failure."( Self-rated health predicts adverse events during β-blocker treatment: the CIBIS-ELD randomised trial analysis.
Anker, SD; Apostolovic, S; Düngen, HD; Farkas, J; Gelbrich, G; Haverkamp, W; Herrmann-Lingen, C; Inkrot, S; Lainscak, M; Neskovic, AN; Rau, T; Tahirovic, E; Töpper, A, 2013
)
0.39
" Adverse events were experienced by 64% patients and 38% experienced > 1 adverse event or serious adverse event, with higher prevalence in lower SRH categories."( Self-rated health predicts adverse events during β-blocker treatment: the CIBIS-ELD randomised trial analysis.
Anker, SD; Apostolovic, S; Düngen, HD; Farkas, J; Gelbrich, G; Haverkamp, W; Herrmann-Lingen, C; Inkrot, S; Lainscak, M; Neskovic, AN; Rau, T; Tahirovic, E; Töpper, A, 2013
)
0.39
"SRH is an independent predictor of adverse events during titration of beta-blockers and correlates with the proportion and number of adverse events per patient."( Self-rated health predicts adverse events during β-blocker treatment: the CIBIS-ELD randomised trial analysis.
Anker, SD; Apostolovic, S; Düngen, HD; Farkas, J; Gelbrich, G; Haverkamp, W; Herrmann-Lingen, C; Inkrot, S; Lainscak, M; Neskovic, AN; Rau, T; Tahirovic, E; Töpper, A, 2013
)
0.39
" The two referred examples result in important take-home messages: a) drug-induced cardiac mitochondrial dysfunction is an important contributor for drug-associated organ failure, b) protection of mitochondrial function is involved in the beneficial impact of some clinically-used drugs and c) a more accurate prediction of toxic vs."( Drug-induced cardiac mitochondrial toxicity and protection: from doxorubicin to carvedilol.
Carvalho, FS; Diogo, CV; Monteiro, P; Oliveira, PJ; Pereira, GC; Silva, AM, 2011
)
0.6
"Aluminium, is a trace element available in the Earth's crust naturally and has a toxic potential for humans."( Neuroprotective effect of carvedilol against aluminium induced toxicity: possible behavioral and biochemical alterations in rats.
Dogra, S; Kumar, A; Prakash, A, 2011
)
0.67
" During the primary evaluation period, 7/19 (37%) and 4/22 (18%) patients experienced drug-related adverse events in the CR and IR groups, respectively, the characteristics of which were similar between groups."( Safety and tolerability of once-daily controlled-release carvedilol 10-80 mg in Japanese patients with chronic heart failure.
Ando, H; Kitakaze, M; Nakajima, H; Sakamoto, T; Sarai, N, 2012
)
0.62
" However, its most common adverse effects, dizziness and hypotension, often discourage continuation or dosage increase."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
0.74
"All 13 patients with dizziness (100%) and 9 of 16 with hypotension (56%) were relieved of adverse symptoms or signs."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
0.74
"Switching from carvedilol to bisoprolol may help with continuation of β-blocker treatment as well as dosage increase in HF patients with adverse symptoms or signs, allowing them to reach the target dose."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
1.1
"The use of antracycline (ANT) in breast cancer has been associated with adverse cardiac events."( Effect of carvedilol on silent anthracycline-induced cardiotoxicity assessed by strain imaging: A prospective randomized controlled study with six-month follow-up.
Bugra, Z; Ciftci, R; Cizgici, AY; Elitok, A; Kilic, L; Mercanoglu, F; Oflaz, H; Oncul, A; Oz, F; Sen, F, 2014
)
0.8
"Nephrotoxicity is a major adverse effect of chromium poisoning."( Chromium-induced nephrotoxicity and ameliorative effect of carvedilol in rats: Involvement of oxidative stress, apoptosis and inflammation.
Bijargi, SR; Koneru, M; Kota, A; Sahu, BD; Sistla, R, 2014
)
0.65
" The present data suggest that oxidative damage and genotoxicity play different roles in the toxicity of cisplatin on kidneys and tumors and therefore, some antioxidants might be safe as chemoprotectors."( Carvedilol protects the kidneys of tumor-bearing mice without impairing the biodistribution or the genotoxicity of cisplatin.
Antunes, LM; Baffa, O; Barbosa, F; Carvalho Rodrigues, MA; da Silva Faria, MC; dos Santos, AC; dos Santos, NA; Gobe, GC; Kinoshita, A; Rodrigues, JL, 2016
)
1.88
"Clinical efficacy and adverse effects of the β-blocking agents, carvedilol, bisoprolol, and metoprolol were analyzed theoretically, and then compared quantitatively, for the purpose of determining their proper use for chronic heart failure."( Analysis of Clinical Efficacy and Adverse Effects of β-Blocking Agents Used Clinically for Chronic Heart Failure.
Fujito, K; Kimura, K; Takayanagi, R; Yamada, Y, 2017
)
0.69
" Carvedilol can be added to Amiodarone in patients with severe ventricular rhythm disorders and increased risk of sudden death without expecting of increase adverse events (than either drug alone) or loss of clinical efficacy."( THE SAFETY AND EFFICACY OF AMIODARONE AND CARVEDILOL COMBINATION IN TREATMENT OF PATIENTS WITH SEVERE CARDIAC RHYTHM DISORDERS.
Khintibidze, I; Tsetskhladze, E, 2017
)
1.63
"Cadmium (Cd) is a highly toxic heavy metal with several harmful effects including cardiotoxicity."( Mechanisms mediating the cardioprotective effect of carvedilol in cadmium induced cardiotoxicity. Role of eNOS and HO1/Nrf2 pathway.
Bayoumi, AMA; El-Hussieny, M; Refaie, MMM; Shehata, S, 2019
)
0.76
" Secondary endpoints include other imaging, biomarkers and the occurrence of major adverse cardiac events during follow-up."( Prevention of doxorubicin-induced Cardiotoxicity by pharmacological non-hypoxic myocardial preconditioning based on Docosahexaenoic Acid (DHA) and carvedilol direct antioxidant effects: study protocol for a pilot, randomized, double-blind, controlled tria
Aguayo, R; Carrasco, R; Cortés, I; Erazo, M; Gormaz, JG; Hasson, D; Henriquez, P; Morales, M; Nes, K; Ramirez, MC; Ramos, C; Salas, C; Schuster, A; Sotomayor, CG, 2020
)
0.76
"Cardiac dysfunction is a major side effect of trastuzumab therapy for patients with HER2-positive breast cancer."( In Vivo Evaluation of Carvedilol Cardiac Protection Against Trastuzumab Cardiotoxicity.
Ardakani, EM; Beiranvand, E; Ostad, SN; Sardari, S; Torkashvand, F; Vaziri, B, 2020
)
0.87
" In conclusion, the NCC technology could produce the first safe soluble form of CAR for treating hypertension urgencies easy for industrial scale-up."( Design of ultra-fine carvedilol nanococrystals: Development of a safe and stable injectable formulation.
Hadidi, M; Iman Ghetmiri, S; Mohammady, M; Yousefi, G, 2021
)
0.94

Pharmacokinetics

The pharmacokinetic parameters of a single dose of carvedilol are altered in liver fibrosis, manifested as delayed clearance. The analytical method was successfully applied to a Pharmacokinetic interaction study of vortioxetine and carveilol in rats.

ExcerptReferenceRelevance
"The pharmacokinetic and acute systemic haemodynamic effects of a single oral dose of 50 mg carvedilol has been studied in 24 hypertensive patients with chronic renal failure."( Pharmacokinetic and blood pressure effects of carvedilol in patients with chronic renal failure.
Erley, CM; Krämer, BK; Ress, KM; Risler, T, 1992
)
0.76
" Clinical and pharmacokinetic responses to 12."( Pharmacokinetics of carvedilol in older and younger patients.
Adam, W; Anderson, A; Cripps, J; Morgan, T, 1990
)
0.6
" For the 50 mg capsule Cmax was 66 micrograms."( Pharmacokinetics and bioavailability of carvedilol, a vasodilating beta-blocker.
Neugebauer, G; Reiff, K; von Möllendorff, E, 1987
)
0.54
" Carvedilol and labetalol are the best known examples of such combined alpha/beta-adrenoceptor antagonists, although their pharmacodynamic profile is a result of different receptor selectivity of their component stereoisomers, rather than combined alpha/beta-blocking activity in a single chemical entity."( An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists.
van Zwieten, PA, 1993
)
1.2
"To evaluate the pharmacodynamic properties of carvedilol across a broad range of doses in relation to its enantiospecific kinetics and adrenergic receptor occupancies, relative to placebo and propranolol."( Dose-effect and pharmacokinetic-pharmacodynamic relationships of the beta 1-adrenergic receptor blocking properties of various doses of carvedilol in healthy humans.
Belz, GG; Breithaupt, K; de Mey, C; Neugebauer, G; Palm, D; Schloos, J, 1994
)
0.75
" It reaches a peak concentration 1 to 2 hours postdose and has an elimination half-life of about 4 to 7 hours."( Clinical pharmacokinetics and pharmacodynamics of carvedilol.
Morgan, T, 1994
)
0.54
"The possibility of a pharmacokinetic interaction between carvedilol and digitoxin (Study I) or phenprocoumon (Study II) has been evaluated in groups of 12 healthy volunteers."( Lack of a pharmacokinetic interaction between carvedilol and digitoxin or phenprocoumon.
Brei, R; Caspary, S; Harder, S; Merz, PG, 1993
)
0.79
" These drugs must be administered parenterally and have a half-life of only a few minutes."( Clinical pharmacokinetics of vasodilators. Part II.
Heintz, B; Kirsten, D; Kirsten, R; Nelson, K, 1998
)
0.3
" Mean with (SD) Cmax (ng x ml(-1)) for carvedilol were 53."( The pharmacokinetics of carvedilol and its metabolites after single and multiple dose oral administration in patients with hypertension and renal insufficiency.
Boyle, DA; Gehr, TW; Qian, Y; Shusterman, NH; Sica, DA; Tenero, DM, 1999
)
0.88
" Pharmacokinetic analysis was performed, using 2 conscious dogs given 160 microg of carvedilol/kg as a single IV injection."( Acute cardiovascular effects and pharmacokinetics of carvedilol in healthy dogs.
Hamlin, RL; Miyamoto, M; Nakayama, T; Sawangkoon, S, 2000
)
0.78
" Mean AUC and Cmax values for carvedilol were up to twofold higher in patients with Class IV CHF as compared to those with Class III CHF."( Steady-state pharmacokinetics of carvedilol and its enantiomers in patients with congestive heart failure.
Boike, S; Boyle, D; Brozena, S; Fesniak, HF; Ilson, B; Jorkasky, D; Tenero, D, 2000
)
0.88
"The objective of this study was to examine the pharmacokinetic and pharmacodynamic consequences of concomitant administration of fluoxetine and carvedilol in heart failure patients."( Effect of fluoxetine on carvedilol pharmacokinetics, CYP2D6 activity, and autonomic balance in heart failure patients.
Adams, KF; Carson, SW; Cascio, WE; Graff, DW; Patterson, JH; Pieper, JA; Williamson, KM, 2001
)
0.82
" Pharmacokinetic profiles of carvedilol were determined over the first 12-hour period after the initial dose in study patients, and for comparison, in 9 healthy adult volunteers."( Carvedilol therapy in pediatric patients with congestive heart failure: a study investigating clinical and pharmacokinetic parameters.
Behn, F; Eiselt, M; Läer, S; Meibohm, B; Mir, TS; Scholz, H; Venzke, A; Weil, J, 2002
)
2.05
" Elimination half-life was about 50% shorter in pediatric CHF patients compared with healthy adult volunteers (2."( Carvedilol therapy in pediatric patients with congestive heart failure: a study investigating clinical and pharmacokinetic parameters.
Behn, F; Eiselt, M; Läer, S; Meibohm, B; Mir, TS; Scholz, H; Venzke, A; Weil, J, 2002
)
1.76
" Following a single oral administration of 25-mg carvedilol to 11 healthy, male volunteers, stereoselective pharmacokinetic analysis was undertaken."( Enantioselective pharmacokinetics of carvedilol in human volunteers.
Choi, JK; Kang, JS; Kwon, KI; Lee, BJ; Phuong, NT, 2004
)
0.85
"Beta-blockers differ in their pharmacokinetic and pharmacodynamic properties."( Pharmacokinetics and pharmacodynamics of beta blockers in heart failure.
Talbert, RL, 2004
)
0.32
" The pharmacokinetic parameters in individual subjects were estimated by the Bayesian method using the nonlinear mixed effects model (NONMEM) program."( Effect of CYP2D6*10 on the pharmacokinetics of R- and S-carvedilol in healthy Japanese volunteers.
Arakawa, R; Hashimoto, Y; Honda, M; Igarashi, N; Inoue, H; Nozawa, T; Ogura, Y; Okabe, H; Taguchi, M, 2005
)
0.57
" Plasma drug concentration versus time curves were subjected to noncompartmental pharmacokinetic analysis."( Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, JR; Gordon, SG; Miller, MW; Petrikovics, I, 2005
)
0.65
"The median peak concentration (extrapolated) of carvedilol after IV administration was 476 ng/mL (range, 203 to 1,920 ng/mL), elimination half-life (t(1/2)) was 282 minutes (range, 19 to 1,021 minutes), and mean residence time (MRT) was 360 minutes (range, 19 to 819 minutes)."( Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, JR; Gordon, SG; Miller, MW; Petrikovics, I, 2005
)
0.91
"Although results suggested a 3-hour dosing interval on the basis of MRT, pharmacodynamic studies investigating the duration of beta-adrenoreceptor blockade provide a more accurate basis for determining the dosing interval of carvedilol."( Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, JR; Gordon, SG; Miller, MW; Petrikovics, I, 2005
)
0.84
" Pharmacodynamic data were evaluated in conscious, unrestrained, healthy hound dogs at baseline and after long-term oral administration of carvedilol (1."( Pharmacodynamics of carvedilol in conscious, healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, J; Gordon, SG; Longnecker, M; Miller, MW,
)
0.66
" The pharmacokinetic (PK) and pharmacodynamic (PD) profiles were compared between patients receiving carvedilol CR and carvedilol IR."( Pharmacokinetic and pharmacodynamic comparison of controlled-release carvedilol and immediate-release carvedilol at steady state in patients with hypertension.
Baidoo, CA; Boyle, D; Campanile, AM; Danoff, TM; Harter, AH; Henderson, LS; Tenero, DM, 2006
)
0.78
" The pharmacokinetic (PK)/pharmacodynamic (PD) relation between S(-)-carvedilol concentration-the enantiomer with beta-blocking activity-and change in exercise-induced heart rate was defined in healthy subjects and was best described using a direct effect inhibitory E(max) model (with E(max) being the maximum effect)."( Development of a pharmacokinetic/pharmacodynamic model for carvedilol to predict beta1-blockade in patients with congestive heart failure.
Baidoo, CA; Boyle, D; Campanile, AM; Henderson, LS; Tenero, DM, 2006
)
0.81
"We compared the pharmacokinetic (PK) profiles of repeated dosing with the currently available immediate-release (IR) carvedilol (given twice daily) and a newly developed controlled-release (CR) formulation (given once daily) in patients with left ventricular dysfunction (LVD)."( Pharmacokinetic profile of controlled-release carvedilol in patients with left ventricular dysfunction associated with chronic heart failure or after myocardial infarction.
Baidoo, CA; Greenberg, BH; Lukas, MA; Packer, M; Tenero, DM, 2006
)
0.8
" The purpose of this study was to evaluate the effects of the polymorphism on pharmacokinetics of carvedilol by population pharmacokinetic analysis."( Evaluation of effects of polymorphism for metabolic enzymes on pharmacokinetics of carvedilol by population pharmacokinetic analysis.
Kitabatake, A; Kiyokawa, M; Okamoto, H; Sugawara, M; Takekuma, Y; Takenaka, T; Tsutsui, H; Yamazaki, K, 2007
)
0.78
" The assay utility was demonstrated in the analysis of carvedilol pharmacokinetic profiles in beagle dogs following oral carvedilol administration."( Single quadrupole mass spectrometry for pre-clinical pharmacokinetic analysis: quantitation of carvedilol in dog plasma.
Carlson, BJ; McIntosh, MP; Rajewski, RA; Schorno, KS, 2007
)
0.81
" In a randomized, open-label, 4-period cross-over study, the pharmacokinetic profiles of R(+) and S(-) carvedilol were compared after a single oral dose of carvedilol controlled-release formulation (administered following a standard meal) was given alone or concomitantly with ethanol."( Ethanol does not alter the pharmacokinetic profile of the controlled-release formulation of carvedilol.
Baidoo, CA; Campanile, AM; Danoff, TM; Henderson, LS; Tenero, DM, 2007
)
0.77
"* Applying in silico tools such as population pharmacokinetic analysis and simulation will help to find adequate dosing strategies and increase the probability of success for a randomized controlled trial."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.6
" The population pharmacokinetic model was further utilized for simulations of different carvedilol dosing strategies."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.82
" 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
"Neither urethane-chloralose nor L-NAME modified estimation of pharmacokinetic parameters of carvedilol."( Is urethane-chloralose anaesthesia appropriate for pharmacokinetic-pharmacodynamic assessment? Studies with carvedilol.
Bertera, FM; Bramuglia, GF; Di Verniero, CA; Höcht, C; Mayer, MA; Taira, CA,
)
0.56
" Anaesthesia did not modify pharmacokinetic behaviour of carvedilol in both normotensive and L-NAME hypertensive rats."( Is urethane-chloralose anaesthesia appropriate for pharmacokinetic-pharmacodynamic assessment? Studies with carvedilol.
Bertera, FM; Bramuglia, GF; Di Verniero, CA; Höcht, C; Mayer, MA; Taira, CA,
)
0.59
"To compare the pharmacokinetic properties and bioavailability following oral and IV administration of bisoprolol, a second-generation beta1-adrenoceptor-selective blocking agent, with those of carvedilol, a third-generation beta1/beta2 and alpha1-adrenoceptor blocking agent, in dogs."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.78
" Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.59
" Collectively, these differences suggested that, in dogs, bisoprolol has less interindividual pharmacokinetic variability, compared with carvedilol."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.79
"The paper is aimed to investigate the pharmacokinetic (PK) and the pharmacodynamic (PD) properties of carvedilol using indirect response and effect-compartment link models, and compare the fitness of PK-PD models."( Comparison of different pharmacodynamic models for pharmacokinetic-pharmacodynamic (PK-PD) modeling of carvedilol.
Guo, RC; Liu, XY; Wang, BJ; Yuan, GY, 2009
)
0.78
"Carvedilol showed enantioselective non-linear pharmacokinetic properties in both groups."( Enantioselective pharmacokinetic-pharmacodynamic modelling of carvedilol in a N-nitro-l-arginine methyl ester rat model of secondary hypertension.
Bernabeu, E; Bertera, F; Bramuglia, GF; Buontempo, F; Chiappetta, D; Di Verniero, CA; Höcht, C; Mayer, MA; Taira, CA, 2010
)
2.04
" The data from both studies were used to estimate the population pharmacokinetic parameters and covariates using the nonlinear mixed effects model program."( Population pharmacokinetics of R- and S-carvedilol in Japanese patients with chronic heart failure.
Hanada, K; Kaneko, M; Kawana, J; Mihara, K; Nagayama, M; Ogata, H; Ohno, T; Saito, M; Shiomi, M; Sumiyoshi, T, 2010
)
0.63
"to assess the impact of paroxetine coadministration on the stereoselective pharmacokinetic (PK) properties of carvedilol."( The impact of paroxetine coadministration on stereospecific carvedilol pharmacokinetics.
Bleske, BE; Brook, R; Kerber, K; Nielsen, J; Shea, M; Stout, SM; Welage, LS, 2010
)
0.81
"After carvedilol 25 mg was administered to 110 volunteers, concentrations were enantioselectively quantified and effects on resting and exercise-induced heart rate and blood pressure were analyzed using population pharmacokinetic, pharmacodynamic and pharmacogenetic modeling."( Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics.
Brockmöller, J; Gültepe, S; Meineke, I; Sehrt, D; Tzvetkov, M, 2011
)
2.29
"Carvedilol is a drug where CYP2D6-related pharmacokinetic variation is apparently not carried forward into pharmacodynamic variation."( Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics.
Brockmöller, J; Gültepe, S; Meineke, I; Sehrt, D; Tzvetkov, M, 2011
)
3.25
" Carvedilol showed enantioselective pharmacokinetic properties with increased distribution in F rats compared with normotensive animals."( Pharmacokinetic and pharmacodynamic properties of carvedilol in fructose hypertensive rats.
Bertera, F; Buontempo, F; Chiappetta, D; Di Verniero, CA; Höcht, C; Mayer, MA; Polizio, AH; Taira, CA, 2012
)
1.07
" Tablets were evaluated for physicochemical parameters, in vitro drug release, in vivo pharmacokinetic and pharmacodynamic studies."( Mucoadhesive bilayer buccal tablet of carvedilol-loaded chitosan microspheres: in vitro, pharmacokinetic and pharmacodynamic investigations.
Dhiman, MK; Petkar, K; Sawant, K; Yedurkar, P, 2012
)
0.65
" Although pharmacokinetic properties of carvedilol remained mainly unaffected in SH rats with regard to WKY rats, hypertensive animals showed a reduction in drug clearance of R- and S-carvedilol after administration of 1 mg kg(-1) compared with WKY rats."( Enantioselective pharmacokinetic and pharmacodynamic properties of carvedilol in spontaneously hypertensive rats: focus on blood pressure variability.
Bertera, FM; Buontempo, F; Chiappetta, D; Del Mauro, JS; Höcht, C; Polizio, AH; Taira, CA, 2012
)
0.88
" The validated assay was successfully applied to the quantification of the (R)- and (S)-enantiomers of both carvedilol and its pharmacologically active 4'-hydroxyphenyl metabolite in human plasma in support of a human pharmacokinetic study."( A validated enantioselective LC-MS/MS assay for the simultaneous determination of carvedilol and its pharmacologically active 4'-hydroxyphenyl metabolite in human plasma: application to a clinical pharmacokinetic study.
Furlong, MT; He, B; Mariannino, T; Mylott, W; Shen, J; Stouffer, B; Zhao, S, 2012
)
0.82
" blood pressure, heart rate, body temperature) can be reduced, possibly due to a pharmacodynamic interaction at the serotonin reuptake transporter (SERT)."( Pharmacokinetics and pharmacodynamics of 3,4-methylenedioxymethamphetamine (MDMA): interindividual differences due to polymorphisms and drug-drug interactions.
Hondebrink, L; Meulenbelt, J; Rietjens, SJ; Westerink, RH, 2012
)
0.38
" Statistical analysis of the pharmacokinetic parameters Cmax, AUC0-24, and AUC0-∞ was conducted to determine bioequivalence."( Bioequivalence and pharmacokinetic evaluation of two tablet formulations of carvedilol 25-mg: a single-dose, randomized-sequence, open-label, two-way crossover study in healthy Chinese male volunteers.
Chen, Q; Jia, JY; Liu, GY; Liu, Y; Lu, C; Lu, XP; Wang, W; Yu, C; Zhang, MQ, 2013
)
0.62
"The aim of this study was to derive population pharmacokinetic (PK) model for clearance (CL) of carvedilol in adult patients with chronic heart failure (CHF)."( Population pharmacokinetics of carvedilol in patients with congestive heart failure.
Apostolović, S; Djuric, J; Jankovic, SM; Jevtovic-Stoimenov, T; Markovic, V; Milovanovic, JR; Nikolic, VN; Pesic, S; Stanojevic, D; Stefanovic, N; Velickovic-Radovanović, R; Zivanovic, S, 2013
)
0.89
" Plasma concentration-time curve was used for calculation of pharmacokinetic parameters using two-compartment open model."( Assessment of sex differences in Pharmacokinetics of carvedilol in human.
Abbas, M; Khan, AM; Nawaz, HA; Riffat, S; Tipu, MY; Usman, M, 2014
)
0.65
" The validated assay was successfully applied to the quantification of carvedilol and its pharmacologically active metabolites in rat pharmacokinetic study."( Simultaneous quantification of carvedilol and its metabolites in rat plasma by ultra performance liquid chromatography tandem mass spectrometry and pharmacokinetic application.
Chen, M; Ge, R; Gu, E; Hu, G; Li, J; Wang, L; Wang, S, 2015
)
0.94
"Chronic diseases are associated with pathophysiological changes that could have profound impacts on drug pharmacokinetic behaviour, with a potential need to modify the administered drug therapy."( A physiologically based pharmacokinetic drug-disease model to predict carvedilol exposure in adult and paediatric heart failure patients by incorporating pathophysiological changes in hepatic and renal blood flows.
Khalil, F; Läer, S; Rasool, MF, 2015
)
0.65
" The mean ratio(Obs/Pred) values for the pharmacokinetic parameters were not improved after incorporation of reduced blood flows in paediatric patients, except in those above 17 years of age, who were categorized according to the New York Heart Association classification of CHF, where the CL/F ratio(Obs/Pred) values in two patients were closer to unity."( A physiologically based pharmacokinetic drug-disease model to predict carvedilol exposure in adult and paediatric heart failure patients by incorporating pathophysiological changes in hepatic and renal blood flows.
Khalil, F; Läer, S; Rasool, MF, 2015
)
0.65
" The relative pharmacokinetic parameters of the optimized CVD-ODTs were compared with those of the marketed CVD tablet."( Development and optimization of carvedilol orodispersible tablets: enhancement of pharmacokinetic parameters in rabbits.
Ahmed, OA; Aljimaee, YH; El-Helw, AR; El-Say, KM, 2015
)
0.7
" The pharmacokinetic data for the optimized CVD-ODT showed a significant (P<0."( Development and optimization of carvedilol orodispersible tablets: enhancement of pharmacokinetic parameters in rabbits.
Ahmed, OA; Aljimaee, YH; El-Helw, AR; El-Say, KM, 2015
)
0.7
" Pharmacokinetic parameters including the area under the plasma concentration-time curve (AUC) from time 0 to the last measurable time (AUClast), AUC extrapolated to infinity (AUCinf), and the measured peak plasma concentration (C max) were obtained by noncompartmental analysis."( Dose proportionality and pharmacokinetics of carvedilol sustained-release formulation: a single dose-ascending 10-sequence incomplete block study.
Bae, KS; Choi, HY; Kim, C; Kim, YH; Lee, SH; Lim, HS; Noh, YH, 2015
)
0.68
"5 folds), delayed Tmax and prolonged MRT(0-∞) unraveled the dual-potential of F4 sponges for water-insoluble drugs, like CVD, in improving drug oral bioavailability and in controlling drug release kinetics via buccal mucosa."( Laminated sponges as challenging solid hydrophilic matrices for the buccal delivery of carvedilol microemulsion systems: Development and proof of concept via mucoadhesion and pharmacokinetic assessments in healthy human volunteers.
Abd-Elbary, A; Alaa-Eldin, AA; Makky, AM; Tadros, MI, 2016
)
0.66
" For such a drug, the pathophysiological changes occurring in CHF can have a profound impact on PK, and thus the resulting pharmacodynamic response, of both enantiomers."( Predicting Stereoselective Disposition of Carvedilol in Adult and Pediatric Chronic Heart Failure Patients by Incorporating Pathophysiological Changes in Organ Blood Flows-A Physiologically Based Pharmacokinetic Approach.
Khalil, F; Läer, S; Rasool, MF, 2016
)
0.7
"The study aimed at in vivo pharmacokinetic evaluation of carvedilol loaded nanocapsules (CLN) followed by in silico predictions and establishment of IVIVC."( In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus.
George, JK; Singh, SK; Verma, PR, 2016
)
0.93
"LC/MS-MS method was developed and validated to estimate the pharmacokinetic profile of CLN."( In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus.
George, JK; Singh, SK; Verma, PR, 2016
)
0.68
" In 3 separate studies, pharmacokinetic drug-drug interactions (DDIs) potential was assessed when LCZ696 was coadministered with hydrochlorothiazide (HCTZ), amlodipine, or carvedilol."( Pharmacokinetic drug-drug interaction assessment between LCZ696, an angiotensin receptor neprilysin inhibitor, and hydrochlorothiazide, amlodipine, or carvedilol.
Greeley, M; Hsiao, HL; Langenickel, TH; Pal, P; Rajman, I; Rebello, S; Roberts, J; Sunkara, G; Zhou, W, 2015
)
0.81
" The analytical method was successfully applied to a pharmacokinetic interaction study of vortioxetine and carvedilol after oral administration vortioxetine and carvedilol in rats."( Simultaneous quantification of vortioxetine, carvedilol and its active metabolite 4-hydroxyphenyl carvedilol in rat plasma by UPLC-MS/MS: Application to their pharmacokinetic interaction study.
Huang, Y; Li, T; Pan, Y; Shao, MM; Xu, ZS; Zheng, S, 2016
)
0.91
" The present study was designed to elucidate the potential role of antifibrotic effects of carvedilol in improving hepatic efficiency and the carvedilol oral pharmacokinetic changes during induction of liver fibrosis."( Antifibrotic Effects of Carvedilol and Impact of Liver Fibrosis on Carvedilol Pharmacokinetics in a Rat model.
Abdel-Sattar, SA; El-Bakly, WM; El-Demerdash, E; Mohamed, EA, 2017
)
0.98
" In addition, the pharmacokinetic parameters of a single dose of carvedilol are altered in liver fibrosis, manifested as delayed clearance."( Antifibrotic Effects of Carvedilol and Impact of Liver Fibrosis on Carvedilol Pharmacokinetics in a Rat model.
Abdel-Sattar, SA; El-Bakly, WM; El-Demerdash, E; Mohamed, EA, 2017
)
1
" The pharmacokinetic parameters of carvedilol were analyzed by the noncompartmental method."( The Pharmacokinetic Interaction Study between Carvedilol and Bupropion in Rats.
Abrudan, MB; Gheldiu, AM; Muntean, DM; Neag, MA; Vlase, L, 2017
)
0.99
" This study aims to investigate the implications of type 2 diabetes (T2DM) on the pharmacokinetics of carvedilol enantiomers using an integrated population pharmacokinetic modelling approach."( Population pharmacokinetics of carvedilol enantiomers and their metabolites in healthy subjects and type-2 diabetes patients.
Coelho, EB; Della Pasqua, O; Lanchote, VL; Nardotto, GHB, 2017
)
0.96
" The one-compartment model with first-order absorption and elimination was sufficient to explain the pharmacokinetic characters after single oral administration of carvedilol to both vehicle-pretreated and dronedarone-pretreated rats."( Effect of dronedarone on the pharmacokinetics of carvedilol following oral administration to rats.
Baek, IH; Kim, MS, 2018
)
0.93
" The present study aimed to develop a novel amorphous solid dispersion (ASD) of CAR with acidic counter ions for pH modifications in microenvironment to improve the pharmacokinetic properties under hypochlorhydric conditions."( Amorphous solid dispersions of carvedilol along with pH-modifiers improved pharmacokinetic properties under hypochlorhydoria.
Halder, S; Onoue, S; Sato, H; Seto, Y; Tabata, A, 2018
)
0.77
" The pharmacokinetic results revealed that the optimized chitosan nanoparticles formulation have higher bioavailability than marketed tablet formulation which indicates CAR-CS NPs as an effective strategy to delivery poorly water soluble drugs."( Enhancement of oral bioavailability of poorly water soluble carvedilol by chitosan nanoparticles: Optimization and pharmacokinetic study.
Jain, DK; Saraf, A; Sharma, M; Sharma, R, 2019
)
0.76
" In vivo pharmacokinetics and pharmacodynamic study parameters were compared between carvedilol loaded NLC transdermal patch and a conventional formulation (Coreg CR)."( Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies.
Kesavan, BR; Palagati, S; Selvaraj, BR; Sridhar, SK, 2020
)
1.02
"Evidence-based pharmacotherapy with carvedilol and enalapril in children suffering from heart failure is insufficient owing to limited pharmacokinetic data."( Low-volume LC-MS/MS method for the pharmacokinetic investigation of carvedilol, enalapril and their metabolites in whole blood and plasma: Application to a paediatric clinical trial.
Burckhardt, BB; Gangnus, T, 2021
)
1.13
" Method development and validation were driven for application in pharmacokinetic studies."( Chemometric optimization of salting-out assisted liquid-liquid extraction (SALLE) combined with LC-MS/MS for the analysis of carvedilol enantiomers in human plasma: Application to clinical pharmacokinetics.
de Gaitani, C; de Moraes, N; Dos Santos, J; Kemp, R; Moreira da Silva, R; Pavan, M; Salgado Junior, W; Sankarankutty, A; Yamamoto, P, 2022
)
0.93

Compound-Compound Interactions

The use of low-dose carvedilol combined with candesartan can reduce the acute and chronic cardiotoxicity of anthracycline drugs, and with tolerable toxicities.

ExcerptReferenceRelevance
" The patients who received carvedilol in combination with HCTZ and were evaluated for efficacy (n = 38) showed a decrease in SBP/DBP from 156/97 at the end of monotherapy to 145/88 mmHg after 10 weeks; the combination of atenolol with HCTZ (n = 44) reduced BP from 162/97 to 147/88."( Safety and antihypertensive efficacy of carvedilol and atenolol alone and in combination with hydrochlorothiazide.
Hörrmann, M; Machwirth, M; van der Does, R; Widmann, L, 1990
)
0.84
" We report the use of a short-acting intravenous beta blocker in combination with inotropic therapy as a means to bridge five patients with advanced heart failure to chronic oral beta blockade; two of these patients had been chronically managed with intravenous inotrope."( Novel use of a short-acting intravenous beta blocker in combination with inotropic therapy as a bridge to chronic oral beta blockade in patients with advanced heart failure.
Hauptman, PJ; Prirzker, MR; Woods, D, 2002
)
0.31
"In an open prospective 16-week study we carried out assessment of clinical efficacy, vaso- and cardioprotective properties of nonselective alpha and beta-adrenoblocker carvedilol used as monotherapy and in combination with nifedipine or as combination of these drugs with metformin and simvastatin."( [Provision of complex cardioprotection with the help of carvedilol in 1-2 degree arterial hypertension combined with metabolic syndrome].
Eliseeva, IV; Gusakovskaia, LI; Matrosova, IB; Oleĭnikov, VE; Tomashevskaia, IuA, 2009
)
0.79
"Cardiac resynchronization therapy (CRT), combined with optimal medical therapy (OMT), is an established treatment for patients with advanced chronic heart failure (ACHF)."( CArdiac resynchronization in combination with beta blocker treatment in advanced chronic heart failure (CARIBE-HF): the results of the CARIBE-HF study.
Bisetti, S; Cantù, F; De Luca, A; De Santo, T; Gavazzi, A; Gori, M; Grosu, A; Iacovoni, A; Senni, M, 2011
)
0.37
"To investigate the effect of low-dose carvedilol combined with candesartan in the prevention of acute and chronic cardiotoxicity of anthracycline drugs in adjuvant chemotherapy of breast cancer."( [Preventive effect of low-dose carvedilol combined with candesartan on the cardiotoxicity of anthracycline drugs in the adjuvant chemotherapy of breast cancer].
Han, YL; Liang, XF; Liu, L; Liu, YY; Liu, ZZ; Xie, XD; Zheng, ZD, 2013
)
0.95
"Forty patients were randomly divided into two groups: the experimental group with chemotherapy plus low-dose carvedilol combined with candesartan (20 cases) and control group with chemotherapy alone (20 cases)."( [Preventive effect of low-dose carvedilol combined with candesartan on the cardiotoxicity of anthracycline drugs in the adjuvant chemotherapy of breast cancer].
Han, YL; Liang, XF; Liu, L; Liu, YY; Liu, ZZ; Xie, XD; Zheng, ZD, 2013
)
0.89
"The use of low-dose carvedilol combined with candesartan can reduce the acute and chronic cardiotoxicity of anthracycline drugs, and with tolerable toxicities."( [Preventive effect of low-dose carvedilol combined with candesartan on the cardiotoxicity of anthracycline drugs in the adjuvant chemotherapy of breast cancer].
Han, YL; Liang, XF; Liu, L; Liu, YY; Liu, ZZ; Xie, XD; Zheng, ZD, 2013
)
1
" In 3 separate studies, pharmacokinetic drug-drug interactions (DDIs) potential was assessed when LCZ696 was coadministered with hydrochlorothiazide (HCTZ), amlodipine, or carvedilol."( Pharmacokinetic drug-drug interaction assessment between LCZ696, an angiotensin receptor neprilysin inhibitor, and hydrochlorothiazide, amlodipine, or carvedilol.
Greeley, M; Hsiao, HL; Langenickel, TH; Pal, P; Rajman, I; Rebello, S; Roberts, J; Sunkara, G; Zhou, W, 2015
)
0.81
" GNPs were identified within the cell near to the nucleus when combined with carvedilol."( Apoptosis in human liver carcinoma caused by gold nanoparticles in combination with carvedilol is mediated via modulation of MAPK/Akt/mTOR pathway and EGFR/FAAD proteins.
Araújo, AA; Brito, GAC; Cavalcante, RS; Chan, AB; Cruz, LJ; De Araújo, RF; De Castro Miguel, E; Gasparotto, LHS; Guedes, PMM; Pessoa, JB; Silva, HFO, 2018
)
0.93
"After 4 months of observation, it was noted that CHF patients with IHD in combination with BPO flows less favorably."( [CLINICAL EFFICACY OF THE RECEPTOR BETA AND ALPHA BLOCKERS - CARVEDILOL AND ORNITHINE-ASPARTATE IN PATIENTS WITH CHD AND CHF COMBINED WITH ALCOHOLIC LIVER DISEASE].
Evdokimov, VV; Evdokimova, AG; Tereshchenko, OI; Tomova, AV; Zhukolenko, LV,
)
0.37
"Ivabradine combined with carvedilol improves LVDD, achieves THR more often and reduces risk of encephalopathy, acute kidney injury with improved survival in patients with cirrhosis."( Carvedilol Combined With Ivabradine Improves Left Ventricular Diastolic Dysfunction, Clinical Progression, and Survival in Cirrhosis.
Goyal, R; Khumuckham, JS; Kumar, G; Premkumar, M; Rangegowda, D; Sarin, SK; Shasthry, SM; Thomas, SS; Vyas, T, 2020
)
2.3
"This paper aims to investigate the curative effect of carvedilol combined with conventional therapy in treatment of chronic heart failure."( The curative effect of carvedilol combined with conventional therapy in treatment of chronic heart failure.
Li, X; Qu, W; Yu, Z, 2019
)
1.07
" Clinician's erythema assessment (CEA) and Demodex density were evaluated before and after topical ivermectin alone or combined with oral carvedilol."( Rosacea with persistent facial erythema and high Demodex density effectively treated with topical ivermectin alone or combined with oral carvedilol.
Hsu, CK; Huang, HP; Lee, JY, 2021
)
1.03
" This work aimed to apply chemometrics for the optimization of a salting-out assisted liquid-liquid extraction (SALLE) combined with LC-MS/MS to analyze carvedilol enantiomers in plasma samples."( Chemometric optimization of salting-out assisted liquid-liquid extraction (SALLE) combined with LC-MS/MS for the analysis of carvedilol enantiomers in human plasma: Application to clinical pharmacokinetics.
de Gaitani, C; de Moraes, N; Dos Santos, J; Kemp, R; Moreira da Silva, R; Pavan, M; Salgado Junior, W; Sankarankutty, A; Yamamoto, P, 2022
)
1.13

Bioavailability

Carvedilol in its pure state has low aqueous solubility and extremely poor bioavailability. A solidified self-nanoemulsifying drug delivery system (solidified SNEDDS) and surface-modified microspheres were developed for enhancing the oral bioavailability of carvedilol.

ExcerptReferenceRelevance
"1%) the absolute bioavailability than the S(-) form (15."( Disposition of carvedilol enantiomers in patients with liver cirrhosis: evidence for disappearance of stereoselective first-pass extraction.
Gabor, M; Neugebauer, G; Reiff, K, 1992
)
0.64
" administration, the absolute bioavailability (31."( Stereoselective disposition of carvedilol in man after intravenous and oral administration of the racemic compound.
Akpan, W; Kaufmann, B; Neugebauer, G; Reiff, K, 1990
)
0.57
" Therefore, the absolute bioavailability of 24% indicates some degree of first-pass extraction."( A new molecule with vasodilating and beta-adrenoceptor blocking properties.
Abshagen, U, 1987
)
0.27
" The absolute bioavailability reaches 24% probably due to a first-pass effect."( Pharmacokinetics and disposition of carvedilol in humans.
Akpan, W; Neubert, P; Neugebauer, G; Reiff, K; von Möllendorff, E, 1987
)
0.55
" Carvedilol was absorbed rapidly after oral administration with a bioavailability of approximately 45% and obeyed linear pharmacokinetics over the dose range 25-50 mg."( A pharmacokinetic study of carvedilol (BM 14.190) in elderly subjects: preliminary report.
Conway, EL; Drummer, OH; Louis, WJ; McNeil, JJ; Workman, BS, 1987
)
1.48
"The pharmacokinetics and absolute bioavailability of carvedilol have been studied in 20 male healthy volunteers in a randomised 4-period, cross-over trial."( Pharmacokinetics and bioavailability of carvedilol, a vasodilating beta-blocker.
Neugebauer, G; Reiff, K; von Möllendorff, E, 1987
)
0.79
" It has also proved valuable in determining the relative bioavailability of representatives of this class of drugs."( Digital pulse plethysmography--a tool for investigating vasoactive substances.
Neugebauer, G; von Möllendorff, E, 1985
)
0.27
" However, bioavailability of the oral medication is greatly increased in patients with liver disease."( Clinical pharmacokinetics and pharmacodynamics of carvedilol.
Morgan, T, 1994
)
0.54
" Carvedilol appears to increase digoxin's oral bioavailability as well as renal elimination."( Effects of long-term oral carvedilol on the steady-state pharmacokinetics of oral digoxin in patients with mild to moderate hypertension.
Boyle, DA; Chandler, MH; Clifton, GD; Field, CJ; Smith, DA; Wermeling, DP,
)
1.34
"The time course of pharmacodynamic effects allow to resolve bioavailability relevant pharmacokinetic information, provided simple assumptions can be made about their interrelation."( Inverse PK/PD: estimation and differentiation of bioavailability from effect kinetics--observations with beta-adrenoceptor antagonists.
De Mey, C, 1997
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"The aim of this study was to compare the extent and rate of absorption of two different carvedilol (CAS 72956-09-3) tablet formulations: 25 mg tablets, as the test formulation and the reference innovator product (25 mg tablets)."( Bioequivalence study of two different tablet formulations of carvedilol in healthy volunteers.
Almeida, S; Filipe, A; Portolés, A; Terleira, A; Vallée, F; Vargas, E, 2005
)
0.79
" Pharmacokinetic parameters representing the extent and/or rate of absorption (AUCinf, AUClast, and Cmax) were obtained."( Bioequivalence study of two different tablet formulations of carvedilol in healthy volunteers.
Almeida, S; Filipe, A; Portolés, A; Terleira, A; Vallée, F; Vargas, E, 2005
)
0.57
" The oral clearance was highly correlated with the apparent volume of distribution among the subjects, suggesting that the interindividual difference in bioavailability was largely responsible for the pharmacokinetic variability of carvedilol."( Effect of CYP2D6*10 on the pharmacokinetics of R- and S-carvedilol in healthy Japanese volunteers.
Arakawa, R; Hashimoto, Y; Honda, M; Igarashi, N; Inoue, H; Nozawa, T; Ogura, Y; Okabe, H; Taguchi, M, 2005
)
0.76
"A new self-emulsifying drug delivery system (SEDDS) and self-microemulsifying drug delivery system (SMEDDS) have been developed to increase the solubility, dissolution rate, and, ultimately, oral bioavailability of a poorly water soluble drug, carvedilol."( Preparation and evaluation of SEDDS and SMEDDS containing carvedilol.
Nie, S; Pan, W; Sun, P; Wei, L, 2005
)
0.75
" The oral clearance (CL/F) and also apparent volume of distribution (V/F) of both enantiomers were significantly lower in the subjects with the CYP2D6*10 allele than those with the CYP2D6*1/*1, *1/*2, or *2/*2 genotype, confirming our previous finding that the bioavailability (F) and systemic clearance (CL) of R- and S-carvedilol in the liver is significantly altered in Japanese with the CYP2D6*10 allele."( Multiple regression analysis of pharmacogenetic variability of carvedilol disposition in 54 healthy Japanese volunteers.
Hashimoto, Y; Honda, M; Inoue, H; Nozawa, T; Ogura, Y; Taguchi, M; Toyoda, W, 2006
)
0.75
" For both carvedilol CR and IR, the attenuation of exercise-induced heart rate in patients with hypertension was maintained over the entire 24-hour period, and the 2 formulations demonstrated equivalent beta(1)-blocking effects at trough (end of the dosing interval [PD(min)]), suggesting that the rate of absorption does not interfere with the PD effect."( Pharmacokinetic and pharmacodynamic comparison of controlled-release carvedilol and immediate-release carvedilol at steady state in patients with hypertension.
Baidoo, CA; Boyle, D; Campanile, AM; Danoff, TM; Harter, AH; Henderson, LS; Tenero, DM, 2006
)
0.97
" Bioavailability studies in healthy pigs reveal that carvedilol has got good buccal absorption."( Development of mucoadhesive patches for buccal administration of carvedilol.
Chandrasekhar, K; Ramesh, G; Rao, YM; Vishnu, YV, 2007
)
0.83
" The bioavailability studies in rats indicated that the carvedilol transdermal patches provided steady-state plasma concentrations with minimal fluctuations and improved bioavailability of 71% (for F3) and 62% (for F6) in comparison with oral administration."( Transdermal therapeutic system of carvedilol: effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics.
Ahmad, FJ; Khar, RK; Reddy, MV; Ruckmani, K; Ubaidulla, U, 2007
)
0.86
" It could improve the bioavailability of carvedilol by self-emulsifying drug delivery system (SEDDS), control the release rate and make the plasma concentrations more stable by elementary osmotic pump tablet."( Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol.
Guo, L; Li, J; Liu, H; Nie, S; Pan, W; Sun, P; Wei, L, 2007
)
0.84
" Co-administration with carvedilol increased ciclosporin bioavailability from 33% to 70%."( Carvedilol increases ciclosporin bioavailability by inhibiting P-glycoprotein-mediated transport.
Amioka, K; Ejiri, M; Kushihara, H; Kuzuya, T; Nabeshima, T; Nitta, A, 2007
)
2.09
" CL/F and V/F values of R- and S-carvedilol in the subjects with one UGT2B7*3 allele were similar to those without the UGT2B7*3 allele, indicating that the UGT2B7*3 allele did not significantly affect the systemic clearance (CL) and bioavailability (F) of the two enantiomers."( UGT2B7*3 did not affect the pharmacokinetics of R- and S-carvedilol in healthy Japanese.
Hashimoto, Y; Honda, M; Horiuchi, I; Inoue, H; Kayano, Y; Nozawa, T; Shimizu, T; Taguchi, M; Toyoda, W, 2007
)
0.87
" Its oral bioavailability is 25-35% because of first pass metabolism."( Design and in vivo evaluation of carvedilol buccal mucoadhesive patches.
Babu, P; Pandey, G; Thimmasetty, J, 2008
)
0.63
"To compare the pharmacokinetic properties and bioavailability following oral and IV administration of bisoprolol, a second-generation beta1-adrenoceptor-selective blocking agent, with those of carvedilol, a third-generation beta1/beta2 and alpha1-adrenoceptor blocking agent, in dogs."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.78
" Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.59
" Oral bioavailability of bisoprolol was 91."( Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Beddies, G; Fox, PR; Kanikanti, VR; Keene, BW; Krebber, R; Papich, MD, 2008
)
0.59
" Prepared self-nanoemulsifying tablet produced acceptable properties of immediate-release dosage forms and expected to increase the bioavailability of carvedilol."( Preparation and evaluation of self-nanoemulsifying tablets of carvedilol.
Bendas, ER; Mahmoud, EA; Mohamed, MI, 2009
)
0.79
"The present work aimed to investigate the effect of different concentrations of poloxamer 188, a surfactant, on lymphatic uptake of carvedilol-loaded solid lipid nanoparticles (SLNs) for oral bioavailability enhancement."( Effect of poloxamer 188 on lymphatic uptake of carvedilol-loaded solid lipid nanoparticles for bioavailability enhancement.
Alka, A; Javed, A; Sanjula, B; Shah, FM, 2009
)
0.81
"Carvedilol a poorly water soluble drug undergoes extensive first pass metabolism, which reduces its bioavailability to 25-30%."( Studies on formulation development of mouth dissolving tablets of Carvedilol.
Dhar, S; Mandpe, L; Pokharkar, V,
)
1.81
"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
" However, there is a limitation in terms of its dose due to its low bioavailability (approximately 25%)."( Clinical updates on carvedilol: a first choice beta-blocker in the treatment of cardiovascular diseases.
Chakraborty, S; Mishra, B; Shukla, D; Singh, S, 2010
)
0.68
"The aim of the present study was to develop and characterize chitosan mucoadhesive microspheres of carvedilol (CRV) for nasal delivery to improve bioavailability for treatment of hypertension and angina pectoris."( Mucoadhesive chitosan microspheres of carvedilol for nasal administration.
Babbar, A; Mathur, R; Mishra, A; Patil, S; Sawant, K, 2010
)
0.85
" It compares the bioavailability of these two study drugs from a TDDS with conventional immediate release oral tablets in healthy volunteers."( Randomised, cross-over, comparative bioavailability trial of matrix type transdermal drug delivery system (TDDS) of carvedilol and hydrochlorothiazide combination in healthy human volunteers: a pilot study.
Aggarwal, A; Agrawal, SS, 2010
)
0.57
" A one-compartment model with a first-order absorption rate was established, in which body weight and alpha(1)-acid glycoprotein were significant covariates."( Population pharmacokinetics of R- and S-carvedilol in Japanese patients with chronic heart failure.
Hanada, K; Kaneko, M; Kawana, J; Mihara, K; Nagayama, M; Ogata, H; Ohno, T; Saito, M; Shiomi, M; Sumiyoshi, T, 2010
)
0.63
" Therefore, the objective of this work was to study the enhancement in bioavailability of carvedilol phosphate (basic drug) by providing an alkaline gastric environment to drug-loaded solid lipid nanoparticles."( Effective in-vivo utilization of lipid-based nanoparticles as drug carrier for carvedilol phosphate.
Chakraborty, S; Mishra, B; Shukla, D; Singh, S; Vuddanda, PR, 2011
)
0.82
"The formulation administered orally exhibited enhanced bioavailability (∼27%) when compared with drug suspension and sustained release behaviour when compared with formulation under ideal gastric conditions."( Effective in-vivo utilization of lipid-based nanoparticles as drug carrier for carvedilol phosphate.
Chakraborty, S; Mishra, B; Shukla, D; Singh, S; Vuddanda, PR, 2011
)
0.6
"Carvedilol, a widely prescribed cardiovascular drug for hypertension and congestive heart failure, exhibits low and variable bioavailability owing to poor absorption and extensive hepatic first-pass metabolism."( Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential.
Bandyopadhyay, S; Kapil, R; Katare, OO; Khurana, L; Singh, B, 2011
)
2.04
"A multiple-unit system comprising mucoadhesive bilayer buccal tablets of carvedilol-loaded chitosan microspheres (CMs) was developed to improve bioavailability and therapeutic efficacy of carvedilol."( Mucoadhesive bilayer buccal tablet of carvedilol-loaded chitosan microspheres: in vitro, pharmacokinetic and pharmacodynamic investigations.
Dhiman, MK; Petkar, K; Sawant, K; Yedurkar, P, 2012
)
0.88
"Mucoadhesive alginate microspheres of carvedilol (CRV) for nasal administration intended to avoid first pass metabolism and to improve bioavailability were prepared and evaluated."( In vivo evaluation of alginate microspheres of carvedilol for nasal delivery.
Babbar, A; Kaul, A; Mathur, R; Mishra, A; Patil, SB; Sawant, KK, 2012
)
0.91
"As an inhibitor of CYP2C9, CYP2D6 and P-gp, myricetin might affect the bioavailability of carvedilol when myricetin and carvedilol are used concomitantly for the prevention or therapy of cardiovascular diseases as a combination therapy."( Effects of myricetin on the bioavailability of carvedilol in rats.
Choi, JS; Lee, W; Woo, ER, 2012
)
0.86
"The enhanced oral bioavailability of carvedilol may result from both inhibition of CYP2C9 or CYP2D6-mediated metabolism and P-gp-mediated efflux of carvedilol in small intestine and/or in liver by myricetin rather than reducing renal elimination."( Effects of myricetin on the bioavailability of carvedilol in rats.
Choi, JS; Lee, W; Woo, ER, 2012
)
0.91
"The transdermal drug delivery system was prepared and the bioavailability of the selected drug was enhanced by reducing first-pass metabolism."( Development and evaluation of carvedilol-loaded transdermal drug delivery system: In-vitro and in-vivo characterization study.
Bhalekar, MR; Kshirsagar, SJ; Mohapatra, SK, 2012
)
0.67
"The objective of this study was to enhance the bioavailability of carvedilol through transdermal patches."( Development and evaluation of carvedilol-loaded transdermal drug delivery system: In-vitro and in-vivo characterization study.
Bhalekar, MR; Kshirsagar, SJ; Mohapatra, SK, 2012
)
0.9
" The bioavailability studies in rats indicated that the carvedilol-loaded transdermal patches provided steady-state plasma concentration and improved bioavailability of 72% in comparison to oral administration."( Development and evaluation of carvedilol-loaded transdermal drug delivery system: In-vitro and in-vivo characterization study.
Bhalekar, MR; Kshirsagar, SJ; Mohapatra, SK, 2012
)
0.91
"The developed patch increases the efficacy of carvedilol through enhancement of bioavailability for the therapy of hypertension."( Development and evaluation of carvedilol-loaded transdermal drug delivery system: In-vitro and in-vivo characterization study.
Bhalekar, MR; Kshirsagar, SJ; Mohapatra, SK, 2012
)
0.93
"Solid lipid nanoparticles are most promising delivery systems for the enhancement of bioavailability of highly lipophilic drugs those prone to the first pass metabolism."( Design and evaluation of polymer coated carvedilol loaded solid lipid nanoparticles to improve the oral bioavailability: a novel strategy to avoid intraduodenal administration.
Adepu, L; Chede, R; Diwan, PV; Komuravelli, R; Sistla, R; Venishetty, VK, 2012
)
0.65
"2%) indicated significant enhancement in the rate and extent of bioavailability by the S-SNEDDS formulation compared to pure drug."( Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol.
Bandyopadhyay, S; Garg, B; Kapil, R; Singh, B; Singh, R, 2013
)
0.63
" Pharmacokinetic and bioavailability aspects were also discussed."( Novel chitosan-functionalized spherical nanosilica matrix as an oral sustained drug delivery system for poorly water-soluble drug carvedilol.
Jiang, T; Sun, C; Sun, J; Sun, L; Wang, S; Wang, Y; Zhang, J; Zheng, X, 2013
)
0.59
"The objective of the present investigation was to develop in situ gelling nasal spray formulation of carvedilol (CRV) nanosuspension to improve the bioavailability and therapeutic efficiency."( Nanosuspension based in situ gelling nasal spray of carvedilol: development, in vitro and in vivo characterization.
Pagar, KP; Saindane, NS; Vavia, PR, 2013
)
0.86
" The relative bioavailability of the test formulation to reference formulation was 100."( Bioequivalence and pharmacokinetic evaluation of two tablet formulations of carvedilol 25-mg: a single-dose, randomized-sequence, open-label, two-way crossover study in healthy Chinese male volunteers.
Chen, Q; Jia, JY; Liu, GY; Liu, Y; Lu, C; Lu, XP; Wang, W; Yu, C; Zhang, MQ, 2013
)
0.62
"Formulation and evaluation of nanosuspension incorporated mucoadhesive buccal films of carvedilol for bioavailability enhancement by avoiding first-pass metabolism."( Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism.
Murthy, RS; Rana, P,
)
0.59
" In vivo studies conducted in rabbit model showed 916% increase in the relative bioavailability in comparison to marketed oral tablet formulation."( Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism.
Murthy, RS; Rana, P,
)
0.36
" After loading CAR into c-MCMs, its oral bioavailability was compared with the marketed product in dogs."( Carboxylated mesoporous carbon microparticles as new approach to improve the oral bioavailability of poorly water-soluble carvedilol.
Gao, J; Li, X; Song, Y; Zhang, Y; Zhi, Z, 2013
)
0.6
"Carvedilol used in cardiovascular diseases has systemic bioavailability of 25-35%."( Novel lectin-modified poly(ethylene-co-vinyl acetate) mucoadhesive nanoparticles of carvedilol: preparation and in vitro optimization using a two-level factorial design.
Moazen, E; Varshosaz, J, 2014
)
2.07
"Present invention relates to design of nanostructured lipid carriers (NLC) to augment oral bioavailability of Carvedilol (CAR)."( Nanostructured lipid carriers as a potential vehicle for Carvedilol delivery: Application of factorial design approach.
Bari, SB; Deshmukh, PK; Patil, GB; Patil, ND; Patil, PO, 2016
)
0.89
" Overall, bioavailability of carvedilol was somewhat higher in females than in males, but these differences could be expounded by the lower body weight of female."( Assessment of sex differences in Pharmacokinetics of carvedilol in human.
Abbas, M; Khan, AM; Nawaz, HA; Riffat, S; Tipu, MY; Usman, M, 2014
)
0.94
" The in vivo test in beagle dogs demonstrated that the relative bioavailability of the novel system was 203."( Controlled delivery of carvedilol nanosuspension from osmotic pump capsule: in vitro and in vivo evaluation.
Bai, C; Ge, H; Liu, D; Lyu, C; Pan, W; Yang, X; Yu, S; Zhu, Z, 2014
)
0.71
"The nanotransfersomal vesicles were significantly more efficient in nasal delivery of carvedilol with absolute bioavailability of 63."( Nanotransfersomes of carvedilol for intranasal delivery: formulation, characterization and in vivo evaluation.
Aboud, HM; Ali, AA; El-Menshawe, SF; Elbary, AA, 2016
)
0.98
" Due to its lower aqueous solubility and extensive first-pass metabolism, the absolute bioavailability of CVD does not exceed 30%."( Development and optimization of carvedilol orodispersible tablets: enhancement of pharmacokinetic parameters in rabbits.
Ahmed, OA; Aljimaee, YH; El-Helw, AR; El-Say, KM, 2015
)
0.7
" To overcome the low, variable oral bioavailability of CRV, niosomal formulations were prepared and characterized: plain niosomes (without bile salts), bile salt-enriched niosomes (bilosomes containing various percentages of sodium cholate or sodium taurocholate), and charged niosomes (negative, containing dicetyl phosphate and positive, containing hexadecyl trimethyl ammonium bromide)."( Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge.
Arzani, G; Bakhtiari-Kaboutaraki, H; Dadashzadeh, S; Daeihamed, M; Haeri, A, 2015
)
0.67
" Consequently, the relative bioavailability (R."( Effects of cilostazol on the pharmacokinetics of carvedilol after oral and intravenous administration in rats.
Cho, YA; Choi, DH; Lim, TH, 2015
)
0.67
"Carvedilol (CAR) is a potent antihypertensive drug but has poor oral bioavailability (24%)."( Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration.
Abdelbary, AA; Abdelrahim, ME; Al-mahallawi, AM; Ali, AM, 2015
)
2.09
" Particle size reduction to form nanosized particles was found to be an efficient method for improving the oral bioavailability of carvedilol."( Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation.
He, F; Li, J; Liu, D; Pan, H; Pan, W; Wang, X; Yang, X, 2015
)
0.88
" As a consequence of these CYP2D6 metabolizer phenotypes, pharmacokinetics and bioavailability of carvedilol and metoprolol can range from therapeutically ineffective levels (in the UM patients) to excessive (overdose) and potentially toxic concentrations (in PM patients)."( Impact of CYP2D6 Genetic Variation on the Response of the Cardiovascular Patient to Carvedilol and Metoprolol.
Brill, A; Lymperopoulos, A; McCrink, KA, 2015
)
0.86
"Carvedilol (CVD) suffers from low absolute bioavailability (25%) due to its limited aqueous solubility and hepatic first-pass metabolism."( Laminated sponges as challenging solid hydrophilic matrices for the buccal delivery of carvedilol microemulsion systems: Development and proof of concept via mucoadhesion and pharmacokinetic assessments in healthy human volunteers.
Abd-Elbary, A; Alaa-Eldin, AA; Makky, AM; Tadros, MI, 2016
)
2.1
" Thus, a stable, floating, multiparticulate GMO/Eudragit E100 nanostructures having ability to release the drug in sustained manner with enhanced oral bioavailability can prove to be a promising carrier system for poorly water soluble drugs."( Fabrication of novel GMO/Eudragit E100 nanostructures for enhancing oral bioavailability of carvedilol.
Choudhary, B; Mahadik, KR; Patil, SS; Roy, K, 2016
)
0.65
"09% increase in bioavailability of carvedilol over aqueous suspension."( In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus.
George, JK; Singh, SK; Verma, PR, 2016
)
0.96
" In-vivo CAR oral bioavailability from NMs dispersions and drug control solution was evaluated in Wistar rats."( Novel carvedilol paediatric nanomicelle formulation: in-vitro characterization and in-vivo evaluation.
Bernabeu, E; Bertera, FM; Buontempo, F; Cagel, M; Chiappetta, DA; Höcht, C; Moretton, MA; Parola, L; Taira, CA; Wegmann, M, 2017
)
0.94
" The improvement on drug oral bioavailability contributes to the potential of this NMs formulation to enhance CAR paediatric treatment."( Novel carvedilol paediatric nanomicelle formulation: in-vitro characterization and in-vivo evaluation.
Bernabeu, E; Bertera, FM; Buontempo, F; Cagel, M; Chiappetta, DA; Höcht, C; Moretton, MA; Parola, L; Taira, CA; Wegmann, M, 2017
)
0.94
" However, it has low oral bioavailability (25-35%) due to its high first-pass hepatic metabolism."( Carvedilol-loaded nanocapsules: Mucoadhesive properties and permeability across the sublingual mucosa.
Beck, RC; Chaves, PD; Frank, LA; Guterres, SS; Ourique, AF; Pohlmann, AR, 2017
)
1.9
" This study provides a new successful combination of two polymers with the dual action of HPβCD and PLX/PVP on water solubility and bioavailability of CAR."( Dual Activity of Hydroxypropyl-β-Cyclodextrin and Water-Soluble Carriers on the Solubility of Carvedilol.
Geng, T; Wang, B; Zoghbi, A, 2017
)
0.67
"Carvedilol (CAR) in its pure state has low aqueous solubility and extremely poor bioavailability which largely limit its clinical application."( Comparative study on stabilizing ability of food protein, non-ionic surfactant and anionic surfactant on BCS type II drug carvedilol loaded nanosuspension: Physicochemical and pharmacokinetic investigation.
Banerjee, P; Geng, T; Li, T; Lu, Z; Wang, B; Zoghbi, A, 2017
)
2.11
"Polymer nanofibers have become increasingly important for improvement of dissolution and bioavailability of poorly soluble drugs, representing a great challenge in pharmaceutical development."( Preparation of poloxamer-based nanofibers for enhanced dissolution of carvedilol.
Kajdič, S; Kocbek, P; Vrečer, F, 2018
)
0.71
"A novel delivery system based on self-assembled liposome from multi-layered fibrous mucoadhesive membrane has been developed to improve the bioavailability of Carvedilol (Car)."( Self-assembled liposome from multi-layered fibrous mucoadhesive membrane for buccal delivery of drugs having high first-pass metabolism.
Chen, J; Duan, H; Pan, H; Pan, W; Xiong, S; Yang, X; Yang, Y, 2018
)
0.68
"The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism."( Labrasol-Enriched Nanoliposomal Formulation: Novel Approach to Improve Oral Absorption of Water-Insoluble Drug, Carvedilol.
Dadashzadeh, S; Ghassemi, S; Haeri, A; Shahhosseini, S, 2018
)
0.9
"Co-amorphous drug delivery systems are attracting increasing attention in the pharmaceutical field, due to their promising potential to improve the solubility and bioavailability of poorly water-soluble drugs."( Organic acids as co-formers for co-amorphous systems - Influence of variation in molar ratio on the physicochemical properties of the co-amorphous systems.
Grohganz, H; Löbmann, K; Rades, T; Ueda, H; Wu, W, 2018
)
0.48
" Therefore, the study aimed at developing carvedilol (CVD) in SLNs to control its release and enhance its bioavailability in the management of hypertension, and cardiac diseases."( Optimization of carvedilol solid lipid nanoparticles: An approach to control the release and enhance the oral bioavailability on rabbits.
El-Say, KM; Hosny, KM, 2018
)
1.09
"The sublingual cavity is an interesting route for administration of drugs with limited oral bioavailability due to hepatic first pass metabolism."( SCC4 cell monolayers as an alternative sublingual barrier model: influence of nanoencapsulation on carvedilol transport.
Beck, RCR; Buffon, A; Dos Santos Chaves, P; Raffin Pohlmann, A; Stanisçuaski Guterres, S; Visioli, F, 2019
)
0.73
"Mesoporous carriers have been extensively applied to improve the dissolution velocity and bioavailability of insoluble drugs."( A Comparative Study of the Use of Mesoporous Carbon and Mesoporous Silica as Drug Carriers for Oral Delivery of the Water-Insoluble Drug Carvedilol.
Dong, Y; Han, C; Huang, H; Jian, B; Sui, X; Zhu, W, 2019
)
0.72
" The pharmacokinetic results revealed that the optimized chitosan nanoparticles formulation have higher bioavailability than marketed tablet formulation which indicates CAR-CS NPs as an effective strategy to delivery poorly water soluble drugs."( Enhancement of oral bioavailability of poorly water soluble carvedilol by chitosan nanoparticles: Optimization and pharmacokinetic study.
Jain, DK; Saraf, A; Sharma, M; Sharma, R, 2019
)
0.76
"Self-(micro)emulsifying drug delivery systems (S(M)EDDS) have emerged as effective vehicles for enhancing bioavailability of poorly water soluble drugs, however solidification of the systems represents a major challenge."( Solidification of carvedilol loaded SMEDDS by swirling fluidized bed pellet coating.
Gašperlin, M; Luštrik, M; Mandić, J; Vrečer, F; Zvonar Pobirk, A, 2019
)
0.85
"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
"Coamorphous drug formulations are a promising approach to improve solubility and bioavailability of poorly water-soluble drugs."( Determination of the Optimal Molar Ratio in Amino Acid-Based Coamorphous Systems.
Grohganz, H; Liu, J; Rades, T, 2020
)
0.56
"56-fold increase in the relative bioavailability of CAR was observed for the CAR PI-SNEDDS (397."( A Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability.
Ge, L; Han, H; Li, Y; Long, K; Peng, Z; Wang, W; Webster, TJ; Zheng, C, 2020
)
0.77
" Carvedilol bioavailability was significantly increased by formulating solid dispersions, while the analysis of serum biochemical parameters excluded damage on liver and kidney function and the lipid profile of animals exposed to investigated drug delivery system."( Binary polymeric amorphous carvedilol solid dispersions: In vitro and in vivo characterization.
Krstić, M; Manić, L; Martić, N; Mračević, SĐ; Rašković, A; Vasiljević, D; Vukmirović, S, 2020
)
1.77
" After oral administration, CD is rapidly absorbed with an absolute bioavailability of 18-25% because of low solubility and extensive first-pass metabolism."(
Dudhipala, N; Krishna, VM; Kumar, VB, 2020
)
0.56
" Formulations were characterized for physical characteristics, invitro release in simulated and biorelevant dissolution media, intestinal permeability and bioavailability studies in Wistar rats."(
Dudhipala, N; Krishna, VM; Kumar, VB, 2020
)
0.56
" The results from permeability and in-vivo studies demonstrated an enhancement in permeability and bioavailability from supersaturated SEDDS in comparison with control."(
Dudhipala, N; Krishna, VM; Kumar, VB, 2020
)
0.56
" However, further development is restricted because of its poor bioavailability caused by its low solubility and high first-pass effect."( Optimization of lipid materials in the formulation of S-carvedilol self-microemulsifying drug-delivery systems.
Cai, Z; Guo, K; Huang, B; Lin, Z; Wang, X; Zhang, Q, 2020
)
0.8
"The SMEDDS using ionic lipids (oleic acid or soybean lecithin) as oil phase can increase the oral bioavailability of S-CAR by increasing the solubility and reducing the first-pass effect."( Optimization of lipid materials in the formulation of S-carvedilol self-microemulsifying drug-delivery systems.
Cai, Z; Guo, K; Huang, B; Lin, Z; Wang, X; Zhang, Q, 2020
)
0.8
"The hypothesis is to augment the bioavailability and therapeutic potential of low bioavailable Carvedilol (25-35%) through Nanostructured Lipid Carrier (NLC) loaded Transdermal patch (Nanolipid Transferosomes)."( Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies.
Kesavan, BR; Palagati, S; Selvaraj, BR; Sridhar, SK, 2020
)
1.02
" This data reveals the impact of NLC on the enhancement of bioavailability through a transdermal patch."( Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies.
Kesavan, BR; Palagati, S; Selvaraj, BR; Sridhar, SK, 2020
)
0.8
"This research data concludes that NLC loaded transdermal patch (Nanolipid Transferosomes) was a suitable candidate to enhance the bioavailability of low bioavailable drug-like Carvedilol."( Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies.
Kesavan, BR; Palagati, S; Selvaraj, BR; Sridhar, SK, 2020
)
0.99
" In this study, carvedilol and its enantiomers were compared in terms of solubility, permeability, and biliary excretion, and reasons for the poor bioavailability were discussed."( Determination and Comparison of the Solubility, Oil-Water Partition Coefficient, Intestinal Absorption, and Biliary Excretion of Carvedilol Enantiomers.
Cai, Z; Huang, B; Lin, Z; Wang, X; Xue, H; Zhang, Q, 2021
)
1.17
"In this study, a solidified self-nanoemulsifying drug delivery system (solidified SNEDDS) and surface-modified microspheres were developed for enhancing the oral bioavailability of carvedilol."( Effects of different physicochemical characteristics and supersaturation principle of solidified SNEDDS and surface-modified microspheres on the bioavailability of carvedilol.
Baek, K; Choi, HG; Choi, JE; Choi, MJ; Jin, SG; Kim, JO; Kim, JS; Woo, MR, 2021
)
1.01
"Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally."( Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect.
Alle, M; Amarachinta, PR; Chettupalli, AK; Kim, JC; Samed, N; Sharma, G, 2021
)
2.32
"Carvedilol (CAR) is a widely studied, beta and alpha-1 blocker, antihypertensive drug due to its poor water solubility and low oral bioavailability (25-35%)."( Mixed micelles formulation for carvedilol delivery: In-vitro characterization and in-vivo evaluation.
Arslan, FB; Çalış, S; Öztürk, K; Öztürk, SC, 2022
)
2.45
" Co-administration of linagliptin with either carvedilol or atorvastatin can modulate the oral bioavailability of linagliptin."( Investigation of the effect of concurrently administered carvedilol, atorvastatin and bile salts on intestinal absorption of linagliptin.
El Maghraby, GM; Embaby, MA; Osman, MA; Sultan, AA, 2023
)
1.41
"Carvedilol, a β-blocker prescribed for chronic heart failure, suffers from poor bioavailability and rapid first pass metabolism when administered orally."( Tip loaded cyclodextrin-carvedilol complexes microarray patches.
Anjani, QK; Donnelly, RF; Hamid, KA; Li, H; Moreno-Castellanos, N; Sabri, AHB, 2023
)
2.66

Dosage Studied

Carvedilol has a 3-hour dosing interval on the basis of MRT. The long acting highly selective beta1-blocker betaxolol in an adequate dosage is not inferior to carvedilol in terms of exercise tolerance and safety.

ExcerptRelevanceReference
" Increasing dosages of the vasoconstrictors below their threshold of systemic activity were employed in order to obtain dose-response curves of the hand veins congested at a venous occlusion pressure of 40 mmHg."( Oral administration of carvedilol and prazosin inhibits the prostaglandin F2 alpha- and noradrenaline-induced contraction of human hand veins in vivo.
Beermann, C; Belz, GG; Schloos, J, 1992
)
0.59
" Carvedilol shifts the dose-response curve to isoprenaline to the right, as well as to alpha-stimulants such as phenylephrine."( Clinical pharmacology of carvedilol.
Graham, BR; Prichard, BN; Tomlinson, B; Walden, RJ, 1992
)
1.5
" Since ambulatory blood pressure monitoring in a cross-over trial design can reliably detect differences of 5 mmHg with less than 20 subjects, we have used this technique to assess the dose-response curve of a new beta-blocker, carvedilol."( Antihypertensive effect of carvedilol: a preliminary dose-response study.
Bird, R; Casadei, B; Coats, AJ; Conway, J, 1992
)
0.76
" As an example, this paper presents the aggregated dose-response relationship of efficacy data and a last-value analysis of laboratory data across all studies of the antihypertensive drug project carvedilol."( Hemodynamic and metabolic effects of carvedilol: a meta-analysis approach.
Meyer-Sabellek, W; Stienen, U, 1992
)
0.75
" After the administration of carvedilol on day 8, the cirazoline vasopressor response was 2 +/- 1 mmHg and the isoproterenol-induced tachycardia was 4 +/- 3 beats/min, indicating effective alpha 1- and beta-adrenergic blockade after chronic dosing with carvedilol."( Single and repeated doses of the vasodilator/beta-adrenergic antagonist, carvedilol, block cirazoline- and isoproterenol-mediated hemodynamic responses in the conscious rat.
Gagnon, R; Slivjak, MJ; Smith, EF, 1992
)
0.81
" These results indicate that carvedilol is an effective and safe agent for hypertensive patients with chronic renal failure and for hemodialysis patients with hypertension and that dosage adjustments are probably not required in these clinical situations."( Pharmacokinetics and efficacy of carvedilol in hypertensive patients with chronic renal failure and hemodialysis patients.
Abe, Y; Kaifu, Y; Kitajima, W; Masumura, H; Miki, S, 1992
)
0.86
" Oral administration of 50 mg carvedilol led to a rightward shift in the dose-response curves of angiotensin II, norepinephrine, and PGF2 alpha."( Constriction of human dorsal hand veins in vivo with several vasoconstrictors and the influence of oral administration of carvedilol.
Beermann, C; Belz, GG; Schloos, J, 1992
)
0.78
" As an example, this article presents the aggregated dose-response relationship and a subgroup analysis (by age) over all studies of the antihypertensive drug carvedilol."( The once-daily dose regimen of carvedilol: a meta-analysis approach.
Stienen, U, 1992
)
0.77
" Dosing with 25 mg carvedilol once daily or 20 mg nifedipine SR twice daily resulted in mean peak reductions in supine blood pressure of 21/11 and 20/16 mm Hg, respectively, after 1 week of treatment with each respective monotherapy."( Safety of the coadministration of carvedilol and nifedipine sustained-release in the treatment of essential hypertension.
de Vries Robles, P; Juttmann, JR; Venuti, RP, 1992
)
0.89
"The efficacy and safety of carvedilol, a beta-blocker with vasodilating properties, were compared at a dosage of 25 to 50 mg once daily with those of atenolol at a dosage of 50-100 mg once daily in a double-blind, randomized, parallel-group, multicenter study."( A comparison of carvedilol with atenolol in the treatment of mild-to-moderate essential hypertension. INT-CAR-07 (U.K.) Study Group.
Young, PH, 1992
)
0.93
" If the effect was insufficient, the dosage was successively increased to 10 or 20 mg once daily."( Effect of long-term carvedilol therapy on renal function in essential hypertension.
Marumo, F; Tomita, K, 1992
)
0.61
" Hemodynamic parameters, including supine and standing DBP, systolic blood pressure (SBP), and heart rate (HR), were measured and safety was evaluated at baseline and at days 14, 28, and 56 at the end of the dosing interval."( Safety and efficacy of once-daily carvedilol vs twice-daily labetalol in mild to moderate hypertension.
Bussiere, JL; Durier, P; Gayet, JL; Ollivier, JP, 1990
)
0.56
" This activity can be demonstrated in vivo at doses that represent the higher end of the antihypertensive dose-response curve."( The pharmacology of carvedilol.
Gellai, M; Hieble, JP; Nichols, AJ; Ruffolo, RR; Willette, RN, 1990
)
0.6
" Exercise testing, radionuclide ventriculography, and right-sided cardiac catheterization were performed and intraarterial blood pressure measured before and after 8 weeks of carvedilol therapy in a dosage of 12."( Value of carvedilol in congestive heart failure secondary to coronary artery disease.
Broadhurst, P; Das Gupta, P; Lahiri, A; Raftery, EB, 1990
)
0.89
" dosage indicating a stereoselective first-pass effect with higher extraction of the levorotatory enantiomer, which is more potent with respect to beta-adrenoceptor antagonistic activity."( Measurement of carvedilol enantiomers in human plasma and urine using S-naproxen chloride for chiral derivatization.
Henke, W; Langguth, P; Mutschler, E; Schloos, J; Spahn, H, 1990
)
0.63
" Carvedilol appears to be effective in preventing or reducing effort angina due to reduced myocardial oxygen demand, and it exhibits an important dose-response effect."( Antianginal efficacy of carvedilol, a new beta-blocker with vasodilating action.
Carter, G; Freedman, SB; Harris, PJ; Jamal, SM; Kelly, DT; Thomson, A, 1987
)
1.49
"Carvedilol, a new beta-blocker with vasodilating activity, was given orally to 9 hypertensive inpatients with impaired renal function in a dosage regimen of 5 to 20mg once daily to evaluate its clinical efficacy and safety."( Therapeutic benefits and safety of carvedilol in the treatment of renal hypertension. An open, short term study. Carvedilol Renal Hypertension Study Group in Japan.
Fujishima, M; Fukiyama, K; Ishii, M; Kohno, M; Kubo, S; Mizuno, Y; Saruta, T; Takeda, T; Yoshimura, M, 1988
)
1.99
" The patients received either carvedilol 25mg twice daily or metoprolol 50mg twice daily for a period of 4 weeks; if diastolic blood pressure was over 90mm Hg at this time, the dosage was doubled for the subsequent 4 weeks."( Influence of carvedilol on blood glucose and glycohaemoglobin A1 in non-insulin-dependent diabetics.
Ehmer, B; Rudorf, J; van der Does, R, 1988
)
0.93
" Labetalol and prazosin also significantly shifted the dose-response curve to the right for phenylephrine but not for angiotensin II."( Analysis of the mechanism underlying the vasodilator action of carvedilol in pithed spontaneously hypertensive rats.
Akashi, A; Hashimoto, H; Kanda, A; Tanaka, M, 1988
)
0.51
" Dose-response studies (required to increase heart rate or systolic blood pressure by 25 beats/min and 20mm Hg, respectively) were performed with phenylephrine, angiotensin and isoprenaline after each drug, and placebo administration and the effects of physiological pressor stimuli were compared."( Vasodilating mechanism and response to physiological pressor stimuli of acute doses of carvedilol compared with labetalol, propranolol and hydralazine.
Bompart, F; Graham, BR; Liu, JB; Prichard, BN; Tomlinson, B, 1988
)
0.5
"Indirect automatic 24-hour blood pressure monitoring has been found to be reliable and valid and thus has been introduced for the evaluation of dosage and efficacy of antihypertensive drugs."( Follow-up of a method of twenty-four-hour indirect blood pressure monitoring: evaluation of carvedilol, a new antihypertensive agent.
Distler, A; Gotzen, R; Meyer-Sabellek, W; Schulte, KL, 1987
)
0.49
" Following 4 weeks of wash-out/run-in period, patients from the carvedilol group received this drug once a day at a dosage of 25 mg/day for 8 consecutive weeks."( [Use of carvedilol compared to nifedipine in the treatment of mild and moderate essential arterial hypertension].
Dantas, M; Freitas, AF; Furtado, MR; Kohlmann, NE; Kohlmann, O; Plavnik, FL; Portela, JE; Spritzer, N; Spritzer, T, 1994
)
0.96
" After 4 weeks, the dosage was doubled if there was inadequate response."( Comparison of a new vasodilating beta-blocker, carvedilol, with atenolol in the treatment of mild to moderate essential hypertension.
Ruilope, LM, 1994
)
0.55
" dosage increased in rats with pcs due to the reduced hepatic metabolism."( Rats with portacaval shunt as a potential experimental pharmacokinetic model for liver cirrhosis: application to carvedilol stereopharmacokinetics.
Baumgartner, U; Henke, D; Mutschler, E; Schölmerich, J; Spahn-Langguth, H; Stahl, E, 1993
)
0.5
" The dose of isoprenaline required to increase heart rate by 25 beats min-1 (I25) and the dose of phenylephrine required to increase systolic and diastolic blood pressure by 20 mm Hg (PS20 and PD20) were calculated using a quadratic fit to individual dose-response curves."( The dose dependency of the alpha- and beta-adrenoceptor antagonist activity of carvedilol in man.
Guy, S; McDermott, BJ; Riddell, JG; Shanks, RG; Tham, TC, 1995
)
0.52
" During long-term treatment, adjustments in beta-blocker dosage may be required in the event of an exacerbation of heart failure."( Use of carvedilol in chronic heart failure: challenges in therapeutic management.
Sackner-Bernstein, JD,
)
0.59
"Thirty consecutive DCM patients with persistent LV dysfunction (ejection fraction < or =40%) and reduced exercise tolerance (peak oxygen consumption <25 ml/kg/min) despite chronic (>1 year) tailored treatment with metoprolol and angiotensin-converting enzyme inhibitors were enrolled in a 12-month, open-label, parallel trial and were randomized either to continue on metoprolol (n = 16, mean dosage 142+/-44 mg/day) or to cross over to maximum tolerated dosage of carvedilol (n = 14, mean dosage 74+/-23 mg/day)."( Long-term effects of carvedilol in idiopathic dilated cardiomyopathy with persistent left ventricular dysfunction despite chronic metoprolol. The Heart-Muscle Disease Study Group.
Camerini, F; Ciani, F; Di Lenarda, A; Gregori, D; Klugmann, S; Mestroni, L; Muzzi, A; Pinamonti, B; Sabbadini, G; Salvatore, L; Sinagra, G, 1999
)
0.79
" Although the present study cannot provide a final conclusion, based on the results of the present study, no changes in dosing recommendations for carvedilol are warranted in patients with moderate/severe renal insufficiency."( The pharmacokinetics of carvedilol and its metabolites after single and multiple dose oral administration in patients with hypertension and renal insufficiency.
Boyle, DA; Gehr, TW; Qian, Y; Shusterman, NH; Sica, DA; Tenero, DM, 1999
)
0.81
" It is also necessary to define the initiation and increase of dosage and the target dose of the beta-blocker."( [Beta-blockers in the treatment of chronic heart failure. How should results of clinical studies be introduced into clinical practice].
Spinar, J; Vítovec, J, 2000
)
0.31
" Plasma was collected over the 12-hour carvedilol dosing interval, and the concentrations of the R(+) and S(-) enantiomers of carvedilol were measured."( Effect of fluoxetine on carvedilol pharmacokinetics, CYP2D6 activity, and autonomic balance in heart failure patients.
Adams, KF; Carson, SW; Cascio, WE; Graff, DW; Patterson, JH; Pieper, JA; Williamson, KM, 2001
)
0.89
" Optimal timing of starting therapy, dosage and long-term effects need to be investigated with multi-institutional trials."( Efficacy and safety of carvedilol in infants with dilated cardiomyopathy: a preliminary report.
Farzana, F; Gachara, N; Krishnan, U; Prabhakaran, S; Shah, MJ; Srinivas, S,
)
0.44
" Patients who could not be dosed with up to 40 mg daily of metoprolol or 20 mg daily of carvedilol were defined as intolerant."( Comparative left ventricular functional and neurohumoral effects of chronic treatment with carvedilol versus metoprolol in patients with dilated cardiomyopathy.
Hanatani, A; Hirooka, K; Hori, M; Ishida, Y; Komamura, K; Miyatake, K; Nakatani, S; Yamagishi, M; Yasumura, Y, 2001
)
0.75
"We retrospectively evaluated patients entered into the Multicenter Oral Carvedilol Heart failure Assessment (MOCHA) trial, a 6-month, double-blind, randomized, placebo-controlled, multicenter, dose-response evaluation of carvedilol in patients with chronic stable symptomatic heart failure."( Aspirin impairs reverse myocardial remodeling in patients with heart failure treated with beta-blockers.
Bristow, MR; Lindenfeld, J; Lowes, BD; Robertson, AD, 2001
)
0.54
" Among them, only the once-daily dosing of aminoglycosides has been brought to the clinic and physicians are now increasingly adopting this approach to reduce the toxicity of these agents."( Aminoglycoside nephrotoxicity: do time and frequency of administration matter?
Beauchamp, D; Labrecque, G, 2001
)
0.31
"In this prospective, open intervention trial with blinded interpretation of selected end points, patients with CHF who did not improve on standard therapy, including digoxin, angiotensin-converting enzyme inhibitors, and diuretics, were treated with oral carvedilol in a ramped dosing scheme."( Carvedilol therapy in pediatric patients with congestive heart failure: a study investigating clinical and pharmacokinetic parameters.
Behn, F; Eiselt, M; Läer, S; Meibohm, B; Mir, TS; Scholz, H; Venzke, A; Weil, J, 2002
)
1.94
" The observed increased elimination of carvedilol in children suggests that optimal dosing strategies need to be further defined among the pediatric population."( Carvedilol therapy in pediatric patients with congestive heart failure: a study investigating clinical and pharmacokinetic parameters.
Behn, F; Eiselt, M; Läer, S; Meibohm, B; Mir, TS; Scholz, H; Venzke, A; Weil, J, 2002
)
2.03
" Little is known about its safety, efficacy, pharmacokinetics, and dosing profile in children."( The Pediatric Randomized Carvedilol Trial in Children with Heart Failure: rationale and design.
Boucek, MM; Burch, GH; Burr, J; Curtin, EL; Hsu, DT; LaSalle, B; Mahony, L; Pahl, E; Schlencker-Herceg, R; Shaddy, RE; Sower, B; Tani, LY, 2002
)
0.62
"While receiving placebo (2 months) and a full dosage of carvedilol (4 months), 15 chronic heart failure patients were evaluated by quality-of-life questionnaire, pulmonary function tests, cardiopulmonary exercise tests with constant workload, and a ramp protocol."( Carvedilol reduces the inappropriate increase of ventilation during exercise in heart failure patients.
Agostoni, P; Bussotti, M; De Vita, S; Guazzi, M; Palermo, P, 2002
)
2
"2%) and 4 others who were subsequently unable to withstand the progressive stepping up of drug dosage (8."( [Tolerance and efficacy of carvedilol prescription in patients with mild to moderated chronic heart failure].
Barnay, P; Gelisse, R; Levy, S; Maixent, JM; Paganelli, F; Saadjian, A; Sbragia, P, 2000
)
0.6
" All centres were provided with carvedilol, metoprolol, and bisoprolol at appropriate doses; the choice of the drug and dosage was left to the responsible clinician."( Treatment of chronic heart failure with beta adrenergic blockade beyond controlled clinical trials: the BRING-UP experience.
Balli, E; Geraci, E; Gorini, M; Gronda, E; Lucci, D; Maggioni, AP; Opasich, C; Sinagra, G; Tavazzi, L; Tognoni, G, 2003
)
0.6
" Starting treatment with beta blockers did not affect the prescription or dosage of other recommended drugs."( Treatment of chronic heart failure with beta adrenergic blockade beyond controlled clinical trials: the BRING-UP experience.
Balli, E; Geraci, E; Gorini, M; Gronda, E; Lucci, D; Maggioni, AP; Opasich, C; Sinagra, G; Tavazzi, L; Tognoni, G, 2003
)
0.32
" No adverse effects needing reduction or interruption in the dosage were noted in the run-in phase, nor in the period of maintenance."( Modulation of neurohormonal activity after treatment of children in heart failure with carvedilol.
Bonvicini, M; Bronzetti, G; Donti, A; Formigari, R; Giardini, A; Picchio, FM; Prandstraller, D, 2003
)
0.54
" Pharmacokinetic and pharmacodynamic analyses, however, indicate that the dosing regimen of metoprolol selected for use in the COMET trial produces a magnitude and time course of beta(1)-blockade during a 24-hour period that is similar to the dose of carvedilol targeted for use in the trial."( Do beta-blockers prolong survival in heart failure only by inhibiting the beta1-receptor? A perspective on the results of the COMET trial.
Packer, M, 2003
)
0.5
" We analyze the problems with the trial design of COMET from the standpoint of comparing 2 therapeutic agents at different positions on a common dose-response curve, and discuss the theoretical reasons why postjunctional adrenergic receptor blockade that is in addition to beta1-receptor antagonism will likely produce only minimal or no incremental benefit in chronic heart failure."( Selective versus nonselective beta-blockade for heart failure therapy: are there lessons to be learned from the COMET trial?
Adams, KF; Bristow, MR; Feldman, AM; Goldstein, S, 2003
)
0.32
" These include the choice of dose and dosage regimen of immediate-release metoprolol tartrate, a dosage form that has never been shown to reduce mortality in patients with heart failure."( Pharmacodynamics of beta-blockers in heart failure: lessons from the carvedilol or metoprolol European trial.
Bauman, JL; Talbert, RL, 2004
)
0.56
"10, NYHA III-IV 29%) to treatment with either bisoprolol or carvedilol, in order to assess and compare the maximally achievable number of patients on treatment with these BB and the maximally achieved dosage during a minimum of 2 months attendance at our out patient heart failure clinic."( Tolerability of beta-blocker initiation and titration with bisoprolol and carvedilol in congestive heart failure -- a randomized comparison.
Atar, D; Galatius, S; Gustafsson, F; Hildebrandt, PR, 2004
)
0.8
"35 +/- 1 months, the daily dosage of carvedilol was 49."( Effects of carvedilol on ventriculo-arterial coupling in patients with heart failure.
Boffa, GM; Iliceto, S; Orlando, S; Razzolini, R; Tarantini, G, 2004
)
0.99
" Results from the recently published trials are summarized to emphasize the proper selection and dosage of beta blocker therapy to optimize the care of this high risk population."( The effects of beta blockers on morbidity and mortality in heart failure.
Jafri, SM, 2004
)
0.32
" Furthermore, the dosing of metoprolol tartrate in COMET may have been inadequate based on prior studies."( Pharmacokinetics and pharmacodynamics of beta blockers in heart failure.
Talbert, RL, 2004
)
0.32
" The developed method was used for the determination of carvedilol in tablet dosage form."( Differential pulse voltammetric determination of carvedilol in tablets dosage form using glassy carbon electrode.
Elmogy, T; Radi, A, 2005
)
0.83
"Twenty chronic ischemic heart failure patients, 11 males and 9 females, aged 58 +/- 13, with the left ventricular ejection fraction (LVEF) < 45% by echocardiography and New York Heart Association (NYHA) cardiac function classification II-III, were treated with carvedilol for 6 months with a target dosage of 50 mg/d."( [The effect of carvedilol on apoptosis gene PDCD5 expression in chronic heart failure patients].
Hu, DY; Lu, PN; Luo, L; Nie, XY; Wu, Y; Zhang, GQ, 2005
)
0.86
" In 6 months maintenance treatment, 14 (70%) patients reached the dosage 50 mg/d, 4 (20%) reached 25 mg/d, and 2 (10%) reached 12."( [The effect of carvedilol on apoptosis gene PDCD5 expression in chronic heart failure patients].
Hu, DY; Lu, PN; Luo, L; Nie, XY; Wu, Y; Zhang, GQ, 2005
)
0.68
" The relationship between these two phenomena and the suitable dosage of carvedilol remains unclear."( Comparison of low and high doses of carvedilol on restoration of cardiac function and calcium-handling proteins in rat failing heart.
Hu, SJ; Hu, Y; Sun, YL; Wang, LH; Zhou, JY, 2005
)
0.83
"The Carvedilol or Metoprolol European Trial (COMET) compared the effects of a comprehensive adrenergic antagonist, carvedilol (target dosage 25 mg twice daily), with a beta-1-selective agent, metoprolol tartrate (target dosage 50 mg twice daily), in 3029 patients with chronic heart failure caused by left ventricular systolic dysfunction."( Comprehensive adrenergic receptor blockade with carvedilol is superior to beta-1-selective blockade with metoprolol in patients with heart failure: COMET.
Cleland, JG, 2004
)
1.14
" Therefore we analyzed 24-h ECG Holter recordings from a study which compared the long-term clinical efficacy of metoprolol tartrate to carvedilol in chronic heart failure patients using the same dosing regimen as in COMET."( Do metoprolol and carvedilol have equivalent effects on diurnal heart rate in patients with chronic heart failure?
Chan, SK; Fung, JW; Leung, LY; Sanderson, JE; Yip, GW; Yu, CM, 2005
)
0.87
" The dosage of beta-blockers were increased gradually to target or the tolerant dosages (bisoprolol 10 mg qd, carvedilol 25 mg bid) during 3 months in 36 patients."( [Beneficial neurohormonal profiles of beta-blockades in chronic left heart failure].
Bian, WY; Duan, B; Jia, X; Li, W; Li, YS; Wang, F; Wang, L; Xu, ZM, 2005
)
0.54
"The long acting highly selective beta1-blocker betaxolol in an adequate dosage is not inferior to carvedilol in terms of exercise tolerance, safety and effects on left ventricular function."( Betaxolol is equivalent to carvedilol in patients with heart failure NYHA II or III: result of a randomized multicenter trial (BETACAR Trial).
Chochola, J; Figulla, HR; Fridl, P; Kalmbach, C; Krzeminska-Pakula, M; Wrabec, K, 2006
)
0.85
" The target carvedilol dosage (50 mg/d) was achieved by 55."( Titration of carvedilol in elderly heart failure patients.
Creech, S; Karim, FM; Khan, E; Lawless, CE; Shah, R; Tamlyn, T,
)
0.88
"Although results suggested a 3-hour dosing interval on the basis of MRT, pharmacodynamic studies investigating the duration of beta-adrenoreceptor blockade provide a more accurate basis for determining the dosing interval of carvedilol."( Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, JR; Gordon, SG; Miller, MW; Petrikovics, I, 2005
)
0.84
"The purpose of the study reported here was to determine the magnitude and duration of beta-blocking efficacy, determine an effective dose and dosing interval, and document safety and tolerability of carvedilol given orally in clinically normal dogs."( Pharmacodynamics of carvedilol in conscious, healthy dogs.
Arsenault, WG; Boothe, DM; Chalkley, J; Gordon, SG; Longnecker, M; Miller, MW,
)
0.64
" After small and large dosage (1 or 10mg/kg/d) carvedilol-administrated for 5 weeks, hemodynamic parameters, the levels of malondialdehyde (MDA), the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px) and expression of Bcl-2 mRNA in the cardiac tissues of all six groups were measured."( Carvedilol improved diabetic rat cardiac function depending on antioxidant ability.
Huang, H; Pan, XH; Qian, LB; Shan, J; Wang, HP; Xia, Q, 2007
)
2.04
" Carvedilol is excreted by the liver and there were minimal fluctuations between hemodialysis, so, theoretically, drug dosage of the agent should be the same as in non-hemodialysis patients."( [Efficacy of additional low-dose carvedilol in maintenance hemodialysis patients with asymptomatic left ventricular systolic dysfunction].
Ishii, A; Nakano, H; Nakayama, M; Takeguchi, F, 2006
)
1.53
" After small and large dosage carvedilol-administered for 5 weeks, hemodynamic parameters, the levels of malondialdehyde, activities of antioxidant enzymes and expression of Bcl-2 mRNA in the cardiac tissues were measured."( Carvedilol protected diabetic rat hearts via reducing oxidative stress.
Huang, H; Pan, XH; Qian, LB; Shan, J; Wang, HP, 2006
)
2.07
" The availability of once-daily dosing is expected to improve treatment adherence and thereby enhance the effectiveness of carvedilol in routine clinical use."( Pharmacokinetic properties of a new controlled-release formulation of carvedilol.
Baidoo, CA; Boyle, D; Campanile, AM; Danoff, TM; Harter, AH; Henderson, LS; Tenero, DM, 2006
)
0.77
" A controlled-release (CR) formulation of carvedilol that allows once-daily dosing has recently been developed."( Pharmacokinetic and pharmacodynamic comparison of controlled-release carvedilol and immediate-release carvedilol at steady state in patients with hypertension.
Baidoo, CA; Boyle, D; Campanile, AM; Danoff, TM; Harter, AH; Henderson, LS; Tenero, DM, 2006
)
0.83
"We compared the pharmacokinetic (PK) profiles of repeated dosing with the currently available immediate-release (IR) carvedilol (given twice daily) and a newly developed controlled-release (CR) formulation (given once daily) in patients with left ventricular dysfunction (LVD)."( Pharmacokinetic profile of controlled-release carvedilol in patients with left ventricular dysfunction associated with chronic heart failure or after myocardial infarction.
Baidoo, CA; Greenberg, BH; Lukas, MA; Packer, M; Tenero, DM, 2006
)
0.8
" The currently available preparation of carvedilol needs to be taken twice daily; however, studies have shown that the need for twice-daily dosing may decrease adherence."( Profile of carvedilol controlled-release: a new once-daily formulation of carvedilol.
Fonarow, GC, 2006
)
0.99
"Bioequivalence data for two pharmaceutical formulations (solid oral dosage forms) containing carvedilol is presented for both racemic and enantiomers of the active substance."( Achiral-chiral LC/LC-FLD coupling for determination of carvedilol in plasma samples for bioequivalence purposes.
Albu, F; David, V; Galaon, T; Georgita, C; Medvedovici, A; Sora, DI; Udrescu, S, 2007
)
0.81
" Tolerability, defined as patients receiving > or =3 months of carvedilol and achieving a maintenance dosage > or =12."( The impact of baseline HR and BP on the tolerability of carvedilol in the elderly: the COLA (Carvedilol Open Label Assessment) II Study.
Hill, J; Krum, H; Macdonald, PS, 2006
)
0.82
" This analysis compares characteristics, outcomes, and carvedilol dosing of blacks and whites in COHERE."( Tolerability, safety, and efficacy of beta-blockade in black patients with heart failure in the community setting: insights from a large prospective beta-blocker registry.
Abraham, WT; Fowler, MB; Franciosa, JA; Gilbert, EM; Greenberg, B; Lottes, SR; Lukas, MA; Massie, BM; Nelson, JJ,
)
0.38
" Based on this evidence, it is now recommended to add beta-blockers such as metoprolol CR/XL with an escalating dosage regimen to the treatment of patients with symptomatic heart failure who already are receiving a stable medical regimen including angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, diuretics, vasodilators, or digitalis."( The use of metoprolol CR/XL in the treatment of patients with diabetes and chronic heart failure.
De Freitas, O; Fornoni, A; Lenz, O; Materson, BJ, 2006
)
0.33
" Beta-blocker dosages were titrated, and three patients achieved the target beta-blocker dosage established for stage A-C heart failure."( Tolerability of beta-blockers in outpatients with refractory heart failure who were receiving continuous milrinone.
Earl, GL; Fitzpatrick, JM; Narula, J; Verbos-Kazanas, MA, 2007
)
0.34
"Beta-blocker dosing in community HF appears lower than in randomized clinical trials, especially when prescribed by noncardiologists."( Beta-blocker dosing in community-based treatment of heart failure.
Abraham, WT; Fowler, MB; Franciosa, JA; Gilbert, EM; Greenberg, B; Lottes, SR; Lukas, MA; Massie, BM; Nelson, JJ, 2007
)
0.34
"5 mg/day, with the dosage titrated to 25 mg/day if tolerated."( Association of beta-blocker dose with serum procollagen concentrations and cardiac response to spironolactone in patients with heart failure.
Camp, JR; Cavallari, LH; Groo, VL; Momary, KM; Stamos, TD; Viana, MA, 2007
)
0.34
"4% for those with a reduced dosage (n."( Should beta-blocker therapy be reduced or withdrawn after an episode of decompensated heart failure? Results from COMET.
Cleland, JG; Dei Cas, L; Di Lenarda, A; Komajda, M; Metra, M; Poole-Wilson, PA; Remme, WJ; Spark, P; Swedberg, K; Torp-Pedersen, C, 2007
)
0.34
" The objective of this study was to develop and evaluate a single population model that describes S(-)-carvedilol pharmacokinetics from both the immediate-release (IR) and the new controlled-release dosage forms of the racemate."( Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate.
Boyle, DA; Eddington, ND; Fossler, MJ; Othman, AA; Tenero, DM, 2007
)
0.83
" We assessed the efficacy, tolerability and achieved dosage of carvedilol."( Treatment of chronic heart failure with carvedilol in daily practice: the SATELLITE survey experience.
Lainscak, M; Moullet, C; Schön, N; Tendera, M, 2007
)
0.85
"Patients were randomized in a 1:1:1 ratio to twice-daily dosing with placebo, low-dose carvedilol (0."( Carvedilol for children and adolescents with heart failure: a randomized controlled trial.
Blume, ED; Boucek, MM; Boucek, RJ; Burr, J; Canter, CE; Dodd, DA; Holubkov, R; Hsu, DT; LaSalle, B; Lukas, MA; Mahony, L; Pahl, E; Rosenthal, DN; Ross, RD; Shaddy, RE; Tani, LY, 2007
)
2.01
" As comparisons to metoprolol succinate as well as to optimally dosed metoprolol tartrate are missing, a definite superiority of carvedilol cannot be assumed."( [Beta-adrenoceptor antagonists and ACE-inhibitors. Carvedilol compared with metoprolol as combination partner in cases of diabetes and hypertension].
Frese, T; Sandholzer, H, 2007
)
0.8
"The concomitant ingestion of alcohol may alter the release of a drug from a modified-release dosage form, posing a potential risk to patients."( Ethanol does not alter the pharmacokinetic profile of the controlled-release formulation of carvedilol.
Baidoo, CA; Campanile, AM; Danoff, TM; Henderson, LS; Tenero, DM, 2007
)
0.56
"* Applying in silico tools such as population pharmacokinetic analysis and simulation will help to find adequate dosing strategies and increase the probability of success for a randomized controlled trial."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.6
" * Simulations revealed that an age-adjusted carvedilol dosing strategy with higher doses for younger patients with respect to body weight is preferable to a uniform one."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.86
"To investigate the ontogeny of carvedilol pharmacokinetics and to develop an age-appropriate carvedilol dosing strategy for paediatric patients."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.88
" The population pharmacokinetic model was further utilized for simulations of different carvedilol dosing strategies."( Population pharmacokinetics and dose simulation of carvedilol in paediatric patients with congestive heart failure.
Albers, S; Läer, S; Meibohm, B; Mir, TS, 2008
)
0.82
"KEOPS study suggests an improvement of usual conditions of carvedilol compared to the last investigation but the persistence of prescription outside medical authorization and less dosage of this product compared with clinical studies."( [Treating heart failure with carvedilol in private practice (initiating treatment and follow-up at one year. The KEOPS study].
Amouyel, P; Bergougnoux, L; Cohen-Solal, A; de Groote, P; Jaillon, P; Johnson, N; Komajda, M; Laperche, T, 2007
)
0.87
" Accordingly, the authors have investigated dosing equivalency by examining baseline and peak exercise heart rates and norepinephrine levels in subjects with chronic heart failure treated with carvedilol or metoprolol."( Differential effects of carvedilol and metoprolol succinate on plasma norepinephrine release and peak exercise heart rate in subjects with chronic heart failure.
Ahuja, K; Hirsh, DS; Jorde, UP; Kasper, ME; Khandwalla, RM; Tseng, CH; Vittorio, TJ; Zolty, R, 2008
)
0.84
" Patients without noticeable changes in left ventricular ejection fraction with a low to moderate carvedilol dosage show an increase in NT Pro BNP plasma levels."( N-terminal prohormone brain natriuretic peptide plasma levels in heart failure are affected both directly and indirectly by carvedilol.
Cokkinos, DV; Dritsas, A; Kallistratos, MS; Laoutaris, ID,
)
0.56
" During stability testing of CV solid dosage forms an unknown degradation product referred as UP, exceeded the identification thresholds of ICH Q3B guidelines."( HPLC analysis, isolation and identification of a new degradation product in carvedilol tablets.
Antoniadou-Vyza, E; Galanopoulou, O; Rozou, S, 2008
)
0.58
" In the first 60 to 90 days after hospital discharge, little up-titration in beta-blocker dosing occurs."( Dosing of beta-blocker therapy before, during, and after hospitalization for heart failure (from Organized Program to Initiate Lifesaving Treatment in Hospitalized Patients with Heart Failure).
Abraham, WT; Albert, NM; Fonarow, GC; Gheorghiade, M; Greenberg, BH; O'Connor, CM; Stough, WG; Sun, JL; Yancy, CW; Young, JB, 2008
)
0.35
"2% of patients were prescribed the recommended starting dosage of carvedilol (6."( Use and risk management of carvedilol for the treatment of heart failure in the community in England: results from a modified prescription-event monitoring study.
Aurich-Barrera, B; Shakir, SA; Wilton, LV, 2009
)
0.89
"The purpose of this study was to combine the advantages of self-nanoemulsifying drug delivery systems and tablets as a conventional dosage form emphasizing the excipients' effect on the development of a new dosage form."( Preparation and evaluation of self-nanoemulsifying tablets of carvedilol.
Bendas, ER; Mahmoud, EA; Mohamed, MI, 2009
)
0.59
" Dose-response relationships were determined in terms of reduction/elevation in the magnitude of renal blood flow in response to intrarenal arterial injection of dopamine, phenylephrine and isoprenaline."( Chronic treatment with losartan and carvedilol differentially modulates renal vascular responses to sympathomimetics compared to treatment with individual agents in normal Wistar Kyoto and spontaneously hypertensive rats.
Abdallah, HH; Abdulla, MH; Abdullah, NA; Johns, EJ; Khan, MA; Sattar, MA, 2009
)
0.63
" The convenience of once-daily dosing is expected to contribute to patient adherence, thereby potentially improving long-term clinical outcomes."( Role of carvedilol controlled-release in cardiovascular disease.
Fonarow, GC, 2009
)
0.79
" By simplifying the medical regimen, once-daily dosing can potentially improve compliance."( Adherence with once daily versus twice daily carvedilol in patients with heart failure: the Compliance And Quality of Life Study Comparing Once-Daily Controlled-Release Carvedilol CR and Twice-Daily Immediate-Release Carvedilol IR in Patients with Heart F
Hauptman, PJ; Lukas, MA; Massaro, J; Ordronneau, P; Pressler, SJ; Sackner-Bernstein, J; Udelson, JE, 2009
)
0.61
" Sample size estimates were based on assumptions of 75% compliance with BID dosing and 90% compliance with QD dosing."( Adherence with once daily versus twice daily carvedilol in patients with heart failure: the Compliance And Quality of Life Study Comparing Once-Daily Controlled-Release Carvedilol CR and Twice-Daily Immediate-Release Carvedilol IR in Patients with Heart F
Hauptman, PJ; Lukas, MA; Massaro, J; Ordronneau, P; Pressler, SJ; Sackner-Bernstein, J; Udelson, JE, 2009
)
0.61
"We performed a study to examine the clinical use of carvedilol, its dosage and its effects on systolic functions in children."( Treatment of dilated cardiomyopathy with carvedilol in children.
Alehan, D; Celiker, A; Erdoğan, I; Karagöz, T; Ozer, S; Ozkutlu, S,
)
0.65
" The inhibitory effect of carvedilol on I(K) was not affected by the adrenoceptor agonists phenylephrine and prazosin or the adrenoceptor antagonist isoproterenol, but propranolol was able to shift the dose-response curve of carvedilol for I(K) to the right."( Effects of carvedilol on delayed rectifier and transient inactivating potassium currents in rat hippocampal CA1 neurons.
Chen, RZ; Deng, CY; Duan, JJ; Kuang, SJ; Tao, L; Wang, Q, 2010
)
1.05
"There is an evident need for solid oral dosage forms allowing patients' tailor-made dosing due to variations in metabolization or small therapeutic indexes of drug substances."( Novel delivery device for monolithical solid oral dosage forms for personalized medicine.
Breitkreutz, J; Wening, K, 2010
)
0.36
" Prediction of exposure to free plasma carvedilol is important for dosage adjustment of beta-blocker therapy in patients with CHF."( Population pharmacokinetics of R- and S-carvedilol in Japanese patients with chronic heart failure.
Hanada, K; Kaneko, M; Kawana, J; Mihara, K; Nagayama, M; Ogata, H; Ohno, T; Saito, M; Shiomi, M; Sumiyoshi, T, 2010
)
0.9
" The validated HPLC methods were successfully applied to the analysis of their commercial tablet dosage forms, for which no interfering peaks were encountered from common pharmaceutical adjuvants."( Validated HPLC determination of the two fixed dose combinations (chlordiazepoxide hydrochloride and mebeverine hydrochloride; carvedilol and hydrochlorothiazide) in their tablets.
Belal, TS; Haggag, RS; Shaalan, RA,
)
0.34
" The number and type of antihypertensive drugs have increased dramatically from 28 diuretics in 1972 to over 125 agents today, including fixed dose combination dosage forms."( The foundation role of beta blockers across the cardiovascular disease spectrum: a year 2009 update.
Black, HR; Greenberg, BH; Weber, MA, 2010
)
0.36
" Dose-response relationships for the elevation of mean arterial pressure or change in heart rate (HR) in response to intravenous injections of noradrenaline (NA), phenylephrine (PE), methoxamine (ME) and Ang II were determined."( The effect of losartan and carvedilol on vasopressor responses to adrenergic agonists and angiotensin II in the systemic circulation of Sprague Dawley rats.
Abdulla, MH; Abdullah, NA; Anand Swarup, KR; Johns, EJ; Khan, MA; Sattar, MA,
)
0.43
" Although potentially of major public health importance, whether one agent is superior in terms of tolerability and optimal dosing has not been investigated."( Titration to target dose of bisoprolol vs. carvedilol in elderly patients with heart failure: the CIBIS-ELD trial.
Anker, SD; Apostolovic, S; Dietz, R; Doehner, W; Düngen, HD; Edelmann, F; Eschenhagen, T; Gelbrich, G; Herrmann-Lingen, C; Inkrot, S; Krotin, M; Lainscak, M; Mehrhof, F; Neskovic, AN; Prettin, C; Putnikovic, B; Rau, T; Sakac, D; Tahirovic, E; Töpper, A; Waagstein, F; Wachter, R, 2011
)
0.63
" An attempt at quantitation of carvedilol in the dosage forms was made."( Application of 13C CPMAS NMR for qualitative and quantitative characterization of carvedilol and its commercial formulations.
Pisklak, DM; Wawer, I; Zielińska-Pisklak, M, 2012
)
0.89
"During the mean 3-year follow-up, resting heart rate (HR) and BNP were significantly reduced with dose-response relations in the early period but without dose-response relations in the late period."( Minimal dose for effective clinical outcome and predictive factors for responsiveness to carvedilol: Japanese chronic heart failure (J-CHF) study.
Azuma, J; Fujio, Y; Hori, M; Izumi, T; Kitabatake, A; Matsuzaki, M; Nagai, R; Nonen, S; Ohashi, Y; Okamoto, H; Tsutsui, H; Yamazaki, T; Yoshikawa, T, 2013
)
0.61
" Carvedilol maintenance dosage was lower in patients with preserved EF (7."( Clinical status and outcome of Japanese heart failure patients with reduced or preserved ejection fraction treated with carvedilol.
Hiramatsu, K; Kobayashi, F; Mori, Y; Nishikawa, Y, 2013
)
1.51
" However, its most common adverse effects, dizziness and hypotension, often discourage continuation or dosage increase."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
0.74
"Data were retrospectively collected from 23 patients with HF [age 57±18 years, left ventricular ejection fraction (LVEF) 33±15%] who could not increase the dosage of carvedilol because of dizziness or hypotension, defined as systolic blood pressure<90 mmHg."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
0.94
"Switching from carvedilol to bisoprolol may help with continuation of β-blocker treatment as well as dosage increase in HF patients with adverse symptoms or signs, allowing them to reach the target dose."( Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension.
Asano, Y; Ichibori, Y; Kanzaki, M; Komuro, I; Minamiguchi, H; Mizote, I; Ohtani, T; Sakata, Y; Taniguchi, T, 2013
)
1.1
" The validated CE method was successfully applied to the analysis of two commercial tablet dosage forms."( Validated stability-indicating capillary electrophoresis method for the separation and determination of a fixed-dose combination of carvedilol and hydrochlorothiazide in tablets.
Al-Shehri, MM; Alzoman, NZ; Maher, HM; Olah, IV; Sultan, MA,
)
0.34
" Furthermore, if such a drug candidate is intended for the therapy of a specific group of the population, such as geriatric or pediatric, the formulation challenge is even greater, with the need to produce a dosage form that is acceptable for specific patients."( Electrospun polycaprolactone nanofibers as a potential oromucosal delivery system for poorly water-soluble drugs.
Baumgartner, S; Kocbek, P; Kristl, J; Lavrič, Z; Planinšek, O; Potrč, T; Roškar, R, 2015
)
0.42
" The dosage of carvedilol had no detectable effect and there were no unexpected safety issues."( Effect of Combining Ivabradine and β-Blockers: Focus on the Use of Carvedilol in the SHIFT Population.
Bocchi, EA; Böhm, M; Borer, JS; Ford, I; Komajda, M; Swedberg, K; Tavazzi, L, 2015
)
1.01
"There is not enough evidence to support or discourage the use of beta-blockers in children with congestive heart failure, or to propose a paediatric dosing scheme."( Beta-blockers for congestive heart failure in children.
Al Dakhoul, S; Alabed, S; Bdaiwi, Y; Frobel-Mercier, AK; Sabouni, A, 2016
)
0.43
" After adjustment for age, sex, comorbidities, and severity of HF and COPD, bisoprolol use showed a dose-response survival benefit [low dose: adjusted hazard ratio (HR) = 0."( Carvedilol, Bisoprolol, and Metoprolol Use in Patients With Coexistent Heart Failure and Chronic Obstructive Pulmonary Disease.
Chang, YS; Chen, TJ; Chou, KT; Hu, YW; Hung, MH; Lee, FY; Liu, CJ; Ou, SM; Perng, DW; Su, VY; Yang, KY, 2016
)
1.88
" However, the appropriate dosage and efficacy of carvedilol in Japanese AF patients are yet to be clarified."( Heart rate control by carvedilol in Japanese patients with chronic atrial fibrillation: The AF Carvedilol study.
Atarashi, H; Fukuzawa, M; Inoue, H; Kimura, T; Okumura, K; Shiosakai, K; Yamashita, T, 2017
)
1.02
" To evaluate the efficacy of each dosage regimen and the dose-response relationship, changes in 24-h mean HR (mHR) on Holter electrocardiograms from baseline to weeks 2, 4, and 6 were determined as primary endpoints."( Heart rate control by carvedilol in Japanese patients with chronic atrial fibrillation: The AF Carvedilol study.
Atarashi, H; Fukuzawa, M; Inoue, H; Kimura, T; Okumura, K; Shiosakai, K; Yamashita, T, 2017
)
0.77
"The findings suggested that FB is the best alternative for large-scale production of solid dosage forms containing CARV."( Development of carvedilol-cyclodextrin inclusion complexes using fluid-bed granulation: a novel solid-state complexation alternative with technological advantages.
Alonso, EC; Cunha-Filho, MS; Durig, T; Galter, D; Lima, EM; Marreto, RN; Martins, FT; Riccomini, K; Silva, LA; Taveira, SF, 2016
)
0.79
" The versatility of this method was demonstrated by different examples, including the excipients mixture and commercial solid dosage forms (e."( Application of
Pisklak, DM; Szeleszczuk, Ł; Zielińska-Pisklak, M, 2016
)
0.43
" This study highlighted the suitability of using CAR-loaded nanocapsules in the development of innovative sublingual dosage forms."( Carvedilol-loaded nanocapsules: Mucoadhesive properties and permeability across the sublingual mucosa.
Beck, RC; Chaves, PD; Frank, LA; Guterres, SS; Ourique, AF; Pohlmann, AR, 2017
)
1.9
" The present study aimed to investigate in a large database of HFrEF patients (MECKI score database) the association of β-blocker treatment with a composite outcome of cardiovascular death, urgent heart transplantation or left ventricular assist device implantation, addressing the role of β-selectivity and dosage regimens."( Prognostic role of β-blocker selectivity and dosage regimens in heart failure patients. Insights from the MECKI score database.
Agostoni, P; Apostolo, A; Badagliacca, R; Battaia, E; Belardinelli, R; Binno, S; Bonomi, A; Bussotti, M; Caravita, S; Carubelli, V; Cattadori, G; Cicoira, M; Clemenza, F; Contini, M; Corrà, U; Correale, M; Di Lenarda, A; Emdin, M; Frigerio, M; Gentile, P; Guazzi, M; Iorio, A; Lagioia, R; Limongelli, G; Lombardi, C; Magrì, D; Mapelli, M; Marchese, G; Metra, M; Mezzani, A; Minà, C; Oliva, F; Pacileo, G; Palermo, P; Paolillo, S; Parati, G; Passantino, A; Passino, C; Pastormerlo, L; Perrone Filardi, P; Piepoli, M; Raimondo, R; Re, F; Ricci, R; Salvioni, E; Scardovi, AB; Sciomer, S; Scrutino, D; Sinagra, G; Spadafora, E; Veglia, F; Zambon, E, 2017
)
0.46
"Understanding properties and mechanisms that govern drug degradation in the solid state is of high importance to ensure drug stability and safety of solid dosage forms."( Drug-Excipient Interactions in the Solid State: The Role of Different Stress Factors.
Brunsteiner, M; Davis, A; Gressl, C; Gruber-Woelfler, H; Khinast, JG; Landis, M; Paudel, A; Pencheva, K; Scrivens, G; Sluggett, GW; Wood, GPF, 2017
)
0.46
"8 months was analysed with respect to beta blocker dosing and resting HR."( Beta blockers and chronic heart failure patients: prognostic impact of a dose targeted beta blocker therapy vs. heart rate targeted strategy.
Corletto, A; Frankenstein, L; Fröhlich, H; Hochadel, M; Katus, HA; Kilkowski, C; Senges, J; Täger, T; Winkler, R; Zahn, R, 2018
)
0.48
"A PK/PD study for a single and multiple dosing of carvedilol were conducted."( Influence of
Jeong, HS; Jung, E; Kim, JM; Lee, J; Lee, JG; Oh, WY; Park, Z; Ryu, S; Seo, DW; Yi, JY, 2018
)
0.73
"With the use of the cohort of 15,205 Medicare beneficiaries hospitalized for HFrEF from 2007 to 2013 in the 5% Medicare random sample, we described prescription fills (30 days after discharge) and dosage patterns (1 year after discharge) for beta-blockers."( Low Utilization of Beta-Blockers Among Medicare Beneficiaries Hospitalized for Heart Failure With Reduced Ejection Fraction.
Brown, TM; Chen, L; Durant, RW; Kilgore, ML; Levitan, EB; Loop, MS; Safford, MM; van Dyke, MK, 2019
)
0.51
" In addition to the increased drug release rate, solid dispersions should have proper mechanical attributes in order to be successfully formulated in the final solid dosage form such as tablet."( Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions.
Dapčević, A; Djuris, J; Dobricic, V; Ibric, S; Medarevic, D; Milovanovic, S, 2019
)
0.74
" The ability for intestinal mucus to stabilize drug supersaturation and delay drug precipitation is potentially useful in enhancing the absorption of orally dosed compounds from drug delivery systems that generate supersaturation within the gastrointestinal tract (e."( Intestinal mucus is capable of stabilizing supersaturation of poorly water-soluble drugs.
Carrier, RL; Lerkvikarn, S; Lock, J; Nguyen, N; Semin, T; Yeap, YY, 2019
)
0.51
" The continuous production was accomplished using our recently developed continuous model system by controlled deposition of the nanofibers onto the carrier film strained to a wheel collector and followed by cutting into final dosage units."( Continuous manufacturing of orally dissolving webs containing a poorly soluble drug via electrospinning.
Balogh, A; Dénes, D; Domokos, A; Farkas, B; Marosi, G; Nagy, ZK; Nyerges, G; Ződi, L, 2019
)
0.51
"Oral administration of a solid dosage form requires drug dissolution in the gastrointestinal tract before absorption."( Topography of Simulated Intestinal Equilibrium Solubility.
Dunn, C; Halbert, GW; Khadra, I; Perrier, J; Wilson, CG, 2019
)
0.51
" DIF was collected from duodenal stomas after dosing of water and two levels (1 g and 2 g) of LBF."( Effect of lipids on absorption of carvedilol in dogs: Is coadministration of lipids as efficient as a lipid-based formulation?
Abrahamsson, B; Alskär, LC; Bergström, CAS; Johansson, P; Keemink, J; Parrow, A, 2019
)
0.79
"In this study, we investigate the viability of three-dimensional (3D) inkjet printing with UV curing to produce solid dosage forms containing a known poorly soluble drug, carvedilol."( Making tablets for delivery of poorly soluble drugs using photoinitiated 3D inkjet printing.
Alexander, MR; Clark, EA; Irvine, DJ; Roberts, CJ; Wallace, MJ; Wildman, RD; Yoo, J, 2020
)
0.75
"There is not enough evidence to support or discourage the use of beta-blockers in children with congestive heart failure, or to propose a paediatric dosing scheme."( Beta-blockers for congestive heart failure in children.
Al Dakhoul, S; Alabed, S; Bdaiwi, Y; Sabouni, A, 2020
)
0.56
"05) in the parameter (increased AUC0-α, MRT with decreased Cmax, Tmax) when administered through the transdermal patch and on compared to the conventional dosage form."( Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies.
Kesavan, BR; Palagati, S; Selvaraj, BR; Sridhar, SK, 2020
)
0.8
" Beta-blocker dosage groups were >0% to12."( Comparison of Metoprolol Versus Carvedilol After Acute Myocardial Infarction.
Fintel, DJ; Germano, JJ; Goldberger, JJ; Shani, J; Subacius, H; Zaatari, G, 2021
)
0.9
" The former dosage of ACEis/ARBs was continued in one group while in another group, the ACEis/ARBs were replaced by amlodipine ± carvedilol according to the dose equivalents."( Effects of Renin-Angiotensin-Aldosterone Inhibitors on Early Outcomes of Hypertensive COVID-19 Patients: A Randomized Triple-Blind Clinical Trial.
Ashraf, H; Bahreini, M; Ghoghaei, M; Najmeddin, F; Rasooli, F; Salehi, M; Soleimani, A; Solhjoo, M, 2021
)
0.83
" Carvedilol-specific experience was also influenced by the manifestation of side effects and patient dosage routine."( Exploring patients' perceptions and experiences of treatments for the prevention of variceal bleeding: a qualitative study.
Mathers, J; Poyner, C; Tripathi, D, 2021
)
1.53
" To tackle this issue, we established embryonic zebrafish models of doxorubicin-, adrenaline- and terfenadine-induced cardiotoxicity with unified dosing regimen which eventually enabled head-to-head comparison of the drugs."( Pharmacological assessment of zebrafish-based cardiotoxicity models.
Maciag, M; Mierzejewska, M; Plazinska, A; Wnorowski, A, 2022
)
0.72
" The dose-response relationship between the administered beta blockers and respiratory rates was examined using multivariable regression models."( Impact of beta blockers on resting respiratory rate in older adults: A cross-sectional study.
Nagamine, T; Takayama, A; Yoshioka, T, 2023
)
0.91
" This study assesses the impact of β-blocker type and dosing on survival in patients with DM after MI."( Impact of Diabetes Mellitus on Benefit of β-Blocker Therapy After Myocardial Infarction.
Abbott, JD; Bello, D; Blandon, C; Goldberger, JJ; Subačius, H; Zaatari, G, 2023
)
0.91
" The purpose of this work was to obtain a new dosage form of Carvedilol using safe excipients, suitable for administration to pediatric and geriatric patients."( Flexible New Dosage Forms Containing Carvedilol for the Treatment of Patients with Cardiovascular Disorders: Development, Stability, Palatability, and Microbiological Studies.
Leonardi, D; Maggio, R; Operto, MA; Vignaduzzo, S, 2023
)
1.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
beta-adrenergic antagonistAn agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
alpha-adrenergic antagonistAn agent that binds to but does not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha-adrenergic agonists. alpha-Adrenergic antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
vasodilator agentA drug used to cause dilation of the blood vessels.
cardiovascular drugA drug that affects the rate or intensity of cardiac contraction, blood vessel diameter or blood volume.
[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 (3)

ClassDescription
carbazoles
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
[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]

Pathways (1)

PathwayProteinsCompounds
Carvedilol Action Pathway488

Protein Targets (61)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency70.79460.004023.8416100.0000AID485290
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency31.44660.004110.890331.5287AID493106; AID493107
Microtubule-associated protein tauHomo sapiens (human)Potency22.38720.180013.557439.8107AID1460
EWS/FLI fusion proteinHomo sapiens (human)Potency15.40160.001310.157742.8575AID1259252; AID1259253; AID1259255
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency21.13170.001530.607315,848.9004AID1224819; AID1224820
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency44.96470.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency0.02691.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.91250.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency11.22020.036619.637650.1187AID1466; AID2242
D(1A) dopamine receptorHomo sapiens (human)Potency5.75270.02245.944922.3872AID488982; AID488983
chromobox protein homolog 1Homo sapiens (human)Potency39.81070.006026.168889.1251AID488953
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID1454
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.68920.00378.618923.2809AID2667; AID2668
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency25.11890.010323.856763.0957AID2662
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.89930.00798.23321,122.0200AID2546; AID2551
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.22023.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.22023.548118.039535.4813AID1466
D(1A) dopamine receptorSus scrofa (pig)Potency14.68920.00378.108123.2809AID2667
Ataxin-2Homo sapiens (human)Potency19.95260.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[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)
Toll-like receptor 4Homo sapiens (human)IC50 (µMol)32.22000.00240.78061.4000AID1360106
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)7.50000.40003.10009.7000AID721751
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)3.40000.21005.553710.0000AID1442001
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
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.11500.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.06000.00000.887110.0000AID625218
Potassium channel subfamily K member 2Homo sapiens (human)IC50 (µMol)10.95000.40003.92279.0000AID1307726; AID1307731
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Amyloid-beta precursor proteinHomo sapiens (human)IC50 (µMol)30.00000.00053.889510.0000AID748695
Beta-2 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00020.00020.93267.2000AID625205
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.00020.00000.66359.5499AID625205
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)0.53800.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.53300.00322.28879.3160AID625207
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)5.73330.00022.318510.0000AID681126; AID681127; AID681131
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00020.00021.46819.0000AID625204
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.00010.00011.33919.9840AID625204
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.10600.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.04000.00010.807410.0000AID625201
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)4.11930.00001.612910.0000AID625171
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.37490.00042.03378.6606AID625171
Beta-3 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00420.00233.24158.0600AID625206
Beta-3 adrenergic receptorHomo sapiens (human)Ki0.00310.00302.30986.0450AID625206
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.14600.00000.74728.0000AID625253
D(2) dopamine receptorHomo sapiens (human)Ki0.04900.00000.651810.0000AID625253
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.09400.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.04300.00020.725710.0000AID625202
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.09000.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.01300.00030.483410.0000AID625203
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.00580.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00330.00010.739610.0000AID4411; AID625190
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)1.49800.00031.84739.2250AID625252
D(1A) dopamine receptorHomo sapiens (human)Ki0.74900.00010.836310.0000AID625252
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50 (µMol)19.50000.30003.25807.3000AID1222388; AID1222389
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.53800.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.53300.00031.465610.0000AID625207
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00180.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.00090.00000.360910.0000AID625200
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.41000.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.11700.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.11500.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.06000.00010.954910.0000AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.00580.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.00330.00031.29679.2440AID625190
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.22100.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.11800.00000.70488.1930AID625222
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.57700.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.19600.00000.602010.0000AID625254
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.02300.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.01500.00030.769310.0000AID625217
5-hydroxytryptamine receptor 6Homo sapiens (human)IC50 (µMol)1.51900.00170.83815.4200AID625221
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.70500.00020.522910.0000AID625221
Potassium channel subfamily K member 10Homo sapiens (human)IC50 (µMol)15.80007.60007.60007.6000AID1307735; AID1307736
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)0.84500.00071.841946.0000AID625256
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.67100.00021.11158.0280AID625256
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)8.07870.00091.901410.0000AID161281; AID240820; AID243151; AID408340; AID576612; AID625171
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki3.37490.00211.840710.0000AID625171
Cytochrome P450 1B1Homo sapiens (human)IC50 (µMol)1.10000.00130.86969.9000AID1737231
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC50 (µMol)4.11930.10482.83988.3173AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki3.37490.08582.95428.6606AID625171
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)92.40000.01002.765610.0000AID721754
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC50 (µMol)44.67000.020020.518970.7900AID2696
Beta-2 adrenergic receptorHomo sapiens (human)Kd0.00180.00000.62888.9130AID1576808; AID1798580
Beta-1 adrenergic receptorHomo sapiens (human)Kd0.00240.00010.803910.0000AID1798580
Beta-3 adrenergic receptorHomo sapiens (human)Kd0.00240.00010.76318.9130AID1798580
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (610)

Processvia Protein(s)Taxonomy
lipopolysaccharide-mediated signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of MAP kinase activityToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayToll-like receptor 4Homo sapiens (human)
response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
wound healing involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
B cell proliferation involved in immune responseToll-like receptor 4Homo sapiens (human)
nitric oxide production involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
regulation of dendritic cell cytokine productionToll-like receptor 4Homo sapiens (human)
MyD88-dependent toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
nitric oxide biosynthetic processToll-like receptor 4Homo sapiens (human)
phagocytosisToll-like receptor 4Homo sapiens (human)
immune responseToll-like receptor 4Homo sapiens (human)
I-kappaB phosphorylationToll-like receptor 4Homo sapiens (human)
JNK cascadeToll-like receptor 4Homo sapiens (human)
gene expressionToll-like receptor 4Homo sapiens (human)
positive regulation of platelet activationToll-like receptor 4Homo sapiens (human)
positive regulation of gene expressionToll-like receptor 4Homo sapiens (human)
astrocyte developmentToll-like receptor 4Homo sapiens (human)
microglia differentiationToll-like receptor 4Homo sapiens (human)
positive regulation of smooth muscle cell migrationToll-like receptor 4Homo sapiens (human)
detection of fungusToll-like receptor 4Homo sapiens (human)
positive regulation of B cell proliferationToll-like receptor 4Homo sapiens (human)
response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
detection of lipopolysaccharideToll-like receptor 4Homo sapiens (human)
negative regulation of type II interferon productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-17 productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-23 productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-6 productionToll-like receptor 4Homo sapiens (human)
negative regulation of tumor necrosis factor productionToll-like receptor 4Homo sapiens (human)
positive regulation of chemokine productionToll-like receptor 4Homo sapiens (human)
positive regulation of interferon-alpha productionToll-like receptor 4Homo sapiens (human)
positive regulation of interferon-beta productionToll-like receptor 4Homo sapiens (human)
positive regulation of type II interferon productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-1 beta productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-1 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-10 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-12 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-6 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-8 productionToll-like receptor 4Homo sapiens (human)
positive regulation of tumor necrosis factor productionToll-like receptor 4Homo sapiens (human)
positive regulation of stress-activated MAPK cascadeToll-like receptor 4Homo sapiens (human)
toll-like receptor 4 signaling pathwayToll-like receptor 4Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusToll-like receptor 4Homo sapiens (human)
T-helper 1 type immune responseToll-like receptor 4Homo sapiens (human)
macrophage activationToll-like receptor 4Homo sapiens (human)
defense response to bacteriumToll-like receptor 4Homo sapiens (human)
positive regulation of macrophage activationToll-like receptor 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionToll-like receptor 4Homo sapiens (human)
innate immune responseToll-like receptor 4Homo sapiens (human)
MHC class II biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of MHC class II biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processToll-like receptor 4Homo sapiens (human)
negative regulation of osteoclast differentiationToll-like receptor 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIToll-like receptor 4Homo sapiens (human)
positive regulation of JNK cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of smooth muscle cell proliferationToll-like receptor 4Homo sapiens (human)
positive regulation of inflammatory responseToll-like receptor 4Homo sapiens (human)
defense response to Gram-negative bacteriumToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
stress-activated MAPK cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processToll-like receptor 4Homo sapiens (human)
intestinal epithelial structure maintenanceToll-like receptor 4Homo sapiens (human)
positive regulation of macrophage cytokine productionToll-like receptor 4Homo sapiens (human)
ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
nucleotide-binding oligomerization domain containing 1 signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of nucleotide-binding oligomerization domain containing 1 signaling pathwayToll-like receptor 4Homo sapiens (human)
nucleotide-binding oligomerization domain containing 2 signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of nucleotide-binding oligomerization domain containing 2 signaling pathwayToll-like receptor 4Homo sapiens (human)
cellular response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
cellular response to lipoteichoic acidToll-like receptor 4Homo sapiens (human)
cellular response to mechanical stimulusToll-like receptor 4Homo sapiens (human)
cellular response to type II interferonToll-like receptor 4Homo sapiens (human)
negative regulation of cold-induced thermogenesisToll-like receptor 4Homo sapiens (human)
cellular response to oxidised low-density lipoprotein particle stimulusToll-like receptor 4Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblyToll-like receptor 4Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionToll-like receptor 4Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of cellular response to macrophage colony-stimulating factor stimulusToll-like receptor 4Homo sapiens (human)
positive regulation of matrix metallopeptidase secretionToll-like receptor 4Homo sapiens (human)
cellular response to amyloid-betaToll-like receptor 4Homo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 2 productionToll-like receptor 4Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayToll-like receptor 4Homo sapiens (human)
inflammatory responseToll-like receptor 4Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
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)
cardiac ventricle developmentPotassium channel subfamily K member 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayPotassium channel subfamily K member 2Homo sapiens (human)
memoryPotassium channel subfamily K member 2Homo sapiens (human)
response to mechanical stimulusPotassium channel subfamily K member 2Homo sapiens (human)
response to axon injuryPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationPotassium channel subfamily K member 2Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 2Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of DNA biosynthetic processPotassium channel subfamily K member 2Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 2Homo 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)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
cognitionAmyloid-beta precursor proteinHomo sapiens (human)
G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglial cell activationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
suckling behaviorAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activation involved in immune responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of translationAmyloid-beta precursor proteinHomo sapiens (human)
protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
intracellular copper ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
endocytosisAmyloid-beta precursor proteinHomo sapiens (human)
response to oxidative stressAmyloid-beta precursor proteinHomo sapiens (human)
cell adhesionAmyloid-beta precursor proteinHomo sapiens (human)
regulation of epidermal growth factor-activated receptor activityAmyloid-beta precursor proteinHomo sapiens (human)
Notch signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
axonogenesisAmyloid-beta precursor proteinHomo sapiens (human)
learning or memoryAmyloid-beta precursor proteinHomo sapiens (human)
learningAmyloid-beta precursor proteinHomo sapiens (human)
mating behaviorAmyloid-beta precursor proteinHomo sapiens (human)
locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
axo-dendritic transportAmyloid-beta precursor proteinHomo sapiens (human)
cholesterol metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of cell population proliferationAmyloid-beta precursor proteinHomo sapiens (human)
adult locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
visual learningAmyloid-beta precursor proteinHomo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglia developmentAmyloid-beta precursor proteinHomo sapiens (human)
axon midline choice point recognitionAmyloid-beta precursor proteinHomo sapiens (human)
neuron remodelingAmyloid-beta precursor proteinHomo sapiens (human)
dendrite developmentAmyloid-beta precursor proteinHomo sapiens (human)
regulation of Wnt signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
extracellular matrix organizationAmyloid-beta precursor proteinHomo sapiens (human)
forebrain developmentAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection developmentAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of chemokine productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-1 beta productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-6 productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of tumor necrosis factor productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of multicellular organism growthAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of neuron differentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of glycolytic processAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of JNK cascadeAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAmyloid-beta precursor proteinHomo sapiens (human)
collateral sprouting in absence of injuryAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of inflammatory responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of synapse structure or activityAmyloid-beta precursor proteinHomo sapiens (human)
synapse organizationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular process controlling balanceAmyloid-beta precursor proteinHomo sapiens (human)
synaptic assembly at neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
neuron apoptotic processAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
neuron cellular homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAmyloid-beta precursor proteinHomo sapiens (human)
response to interleukin-1Amyloid-beta precursor proteinHomo sapiens (human)
modulation of excitatory postsynaptic potentialAmyloid-beta precursor proteinHomo sapiens (human)
NMDA selective glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of spontaneous synaptic transmissionAmyloid-beta precursor proteinHomo sapiens (human)
cytosolic mRNA polyadenylationAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionAmyloid-beta precursor proteinHomo sapiens (human)
cellular response to amyloid-betaAmyloid-beta precursor proteinHomo sapiens (human)
regulation of presynapse assemblyAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection maintenanceAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of T cell migrationAmyloid-beta precursor proteinHomo sapiens (human)
central nervous system developmentAmyloid-beta precursor proteinHomo sapiens (human)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
signal transductionPotassium channel subfamily K member 10Homo sapiens (human)
memoryPotassium channel subfamily K member 10Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 10Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 10Homo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to organic cyclic compoundCytochrome P450 1B1Homo sapiens (human)
angiogenesisCytochrome P450 1B1Homo sapiens (human)
trabecular meshwork developmentCytochrome P450 1B1Homo sapiens (human)
DNA modificationCytochrome P450 1B1Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1B1Homo sapiens (human)
nitric oxide biosynthetic processCytochrome P450 1B1Homo sapiens (human)
cell adhesionCytochrome P450 1B1Homo sapiens (human)
response to nutrientCytochrome P450 1B1Homo sapiens (human)
steroid metabolic processCytochrome P450 1B1Homo sapiens (human)
estrogen metabolic processCytochrome P450 1B1Homo sapiens (human)
negative regulation of cell population proliferationCytochrome P450 1B1Homo sapiens (human)
male gonad developmentCytochrome P450 1B1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressCytochrome P450 1B1Homo sapiens (human)
toxin metabolic processCytochrome P450 1B1Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionCytochrome P450 1B1Homo sapiens (human)
positive regulation of smooth muscle cell migrationCytochrome P450 1B1Homo sapiens (human)
sterol metabolic processCytochrome P450 1B1Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 1B1Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1B1Homo sapiens (human)
collagen fibril organizationCytochrome P450 1B1Homo sapiens (human)
adrenal gland developmentCytochrome P450 1B1Homo sapiens (human)
negative regulation of cell migrationCytochrome P450 1B1Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityCytochrome P450 1B1Homo sapiens (human)
response to follicle-stimulating hormoneCytochrome P450 1B1Homo sapiens (human)
response to estradiolCytochrome P450 1B1Homo sapiens (human)
negative regulation of cell adhesion mediated by integrinCytochrome P450 1B1Homo sapiens (human)
benzene-containing compound metabolic processCytochrome P450 1B1Homo sapiens (human)
retinol metabolic processCytochrome P450 1B1Homo sapiens (human)
retinal metabolic processCytochrome P450 1B1Homo sapiens (human)
positive regulation of apoptotic processCytochrome P450 1B1Homo sapiens (human)
blood vessel endothelial cell migrationCytochrome P450 1B1Homo sapiens (human)
endothelial cell migrationCytochrome P450 1B1Homo sapiens (human)
estrous cycleCytochrome P450 1B1Homo sapiens (human)
positive regulation of translationCytochrome P450 1B1Homo sapiens (human)
positive regulation of angiogenesisCytochrome P450 1B1Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATCytochrome P450 1B1Homo sapiens (human)
membrane lipid catabolic processCytochrome P450 1B1Homo sapiens (human)
response to arsenic-containing substanceCytochrome P450 1B1Homo sapiens (human)
blood vessel morphogenesisCytochrome P450 1B1Homo sapiens (human)
retinal blood vessel morphogenesisCytochrome P450 1B1Homo sapiens (human)
ganglion developmentCytochrome P450 1B1Homo sapiens (human)
cellular response to hydrogen peroxideCytochrome P450 1B1Homo sapiens (human)
cellular response to cAMPCytochrome P450 1B1Homo sapiens (human)
cellular response to tumor necrosis factorCytochrome P450 1B1Homo sapiens (human)
cellular response to luteinizing hormone stimulusCytochrome P450 1B1Homo sapiens (human)
cellular response to cortisol stimulusCytochrome P450 1B1Homo sapiens (human)
cellular response to progesterone stimulusCytochrome P450 1B1Homo sapiens (human)
response to dexamethasoneCytochrome P450 1B1Homo sapiens (human)
endothelial cell-cell adhesionCytochrome P450 1B1Homo sapiens (human)
response to indole-3-methanolCytochrome P450 1B1Homo sapiens (human)
cellular response to toxic substanceCytochrome P450 1B1Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1B1Homo sapiens (human)
response to 3-methylcholanthreneCytochrome P450 1B1Homo sapiens (human)
regulation of reactive oxygen species metabolic processCytochrome P450 1B1Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCytochrome P450 1B1Homo sapiens (human)
positive regulation of DNA biosynthetic processCytochrome P450 1B1Homo 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)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (152)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingToll-like receptor 4Homo sapiens (human)
amyloid-beta bindingToll-like receptor 4Homo sapiens (human)
lipopolysaccharide immune receptor activityToll-like receptor 4Homo sapiens (human)
transmembrane signaling receptor activityToll-like receptor 4Homo sapiens (human)
signaling receptor bindingToll-like receptor 4Homo sapiens (human)
protein bindingToll-like receptor 4Homo sapiens (human)
signaling receptor activityToll-like receptor 4Homo sapiens (human)
identical protein bindingToll-like receptor 4Homo sapiens (human)
protein heterodimerization activityToll-like receptor 4Homo sapiens (human)
NAD+ nucleotidase, cyclic ADP-ribose generatingToll-like receptor 4Homo sapiens (human)
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
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)
outward rectifier potassium channel activityPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 2Homo 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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
serine-type endopeptidase inhibitor activityAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
heparin bindingAmyloid-beta precursor proteinHomo sapiens (human)
enzyme bindingAmyloid-beta precursor proteinHomo sapiens (human)
identical protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
transition metal ion bindingAmyloid-beta precursor proteinHomo sapiens (human)
receptor ligand activityAmyloid-beta precursor proteinHomo sapiens (human)
PTB domain bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein serine/threonine kinase bindingAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor activator activityAmyloid-beta precursor proteinHomo sapiens (human)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
potassium channel activityPotassium channel subfamily K member 10Homo sapiens (human)
outward rectifier potassium channel activityPotassium channel subfamily K member 10Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 10Homo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
monooxygenase activityCytochrome P450 1B1Homo sapiens (human)
iron ion bindingCytochrome P450 1B1Homo sapiens (human)
protein bindingCytochrome P450 1B1Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1B1Homo sapiens (human)
heme bindingCytochrome P450 1B1Homo sapiens (human)
aromatase activityCytochrome P450 1B1Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1B1Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1B1Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, NAD(P)H as one donor, and incorporation of one atom of oxygenCytochrome P450 1B1Homo 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)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (105)

Processvia Protein(s)Taxonomy
plasma membraneToll-like receptor 4Homo sapiens (human)
endosome membraneToll-like receptor 4Homo sapiens (human)
ruffleToll-like receptor 4Homo sapiens (human)
phagocytic cupToll-like receptor 4Homo sapiens (human)
cytoplasmToll-like receptor 4Homo sapiens (human)
early endosomeToll-like receptor 4Homo sapiens (human)
plasma membraneToll-like receptor 4Homo sapiens (human)
external side of plasma membraneToll-like receptor 4Homo sapiens (human)
cell surfaceToll-like receptor 4Homo sapiens (human)
endosome membraneToll-like receptor 4Homo sapiens (human)
receptor complexToll-like receptor 4Homo sapiens (human)
perinuclear region of cytoplasmToll-like receptor 4Homo sapiens (human)
lipopolysaccharide receptor complexToll-like receptor 4Homo sapiens (human)
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
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)
endoplasmic reticulum membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
cell surfacePotassium channel subfamily K member 2Homo sapiens (human)
apical plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
neuronal cell bodyPotassium channel subfamily K member 2Homo sapiens (human)
calyx of HeldPotassium channel subfamily K member 2Homo sapiens (human)
astrocyte projectionPotassium channel subfamily K member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo 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 spaceAmyloid-beta precursor proteinHomo sapiens (human)
dendriteAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionAmyloid-beta precursor proteinHomo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
nuclear envelope lumenAmyloid-beta precursor proteinHomo sapiens (human)
cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
mitochondrial inner membraneAmyloid-beta precursor proteinHomo sapiens (human)
endosomeAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum lumenAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
Golgi lumenAmyloid-beta precursor proteinHomo sapiens (human)
Golgi-associated vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cytosolAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
clathrin-coated pitAmyloid-beta precursor proteinHomo sapiens (human)
cell-cell junctionAmyloid-beta precursor proteinHomo sapiens (human)
synaptic vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
membraneAmyloid-beta precursor proteinHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleAmyloid-beta precursor proteinHomo sapiens (human)
axonAmyloid-beta precursor proteinHomo sapiens (human)
growth coneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule lumenAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
endosome lumenAmyloid-beta precursor proteinHomo sapiens (human)
trans-Golgi network membraneAmyloid-beta precursor proteinHomo sapiens (human)
ciliary rootletAmyloid-beta precursor proteinHomo sapiens (human)
dendritic spineAmyloid-beta precursor proteinHomo sapiens (human)
dendritic shaftAmyloid-beta precursor proteinHomo sapiens (human)
perikaryonAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
apical part of cellAmyloid-beta precursor proteinHomo sapiens (human)
synapseAmyloid-beta precursor proteinHomo sapiens (human)
perinuclear region of cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
presynaptic active zoneAmyloid-beta precursor proteinHomo sapiens (human)
spindle midzoneAmyloid-beta precursor proteinHomo sapiens (human)
recycling endosomeAmyloid-beta precursor proteinHomo sapiens (human)
extracellular exosomeAmyloid-beta precursor proteinHomo sapiens (human)
receptor complexAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membranePotassium channel subfamily K member 10Homo sapiens (human)
monoatomic ion channel complexPotassium channel subfamily K member 10Homo sapiens (human)
plasma membranePotassium channel subfamily K member 10Homo sapiens (human)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
mitochondrionCytochrome P450 1B1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1B1Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1B1Homo 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)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (286)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID748695Inhibition of amyloid beta (1 to 40) (unknown origin) fibril formation after 18 hrs by DELFIA2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Progress and developments in tau aggregation inhibitors for Alzheimer disease.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID416888Antiarrhythmic activity against adrenaline-induced arrhythmia in iv dosed anaesthetized Wistar rat assessed as inhibition of premature ventricular beats pretreated 60 mins prior to adrenaline challenge2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
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.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID1509206Inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in MET currents measured at -150 mV to +100 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID440287Effect on heart rate in anesthetized Wistar rat assessed as Q-T intervals time at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1057863Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1737232Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
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).
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).
AID440284Effect on heart rate in anesthetized Wistar rat assessed as QRS complex time at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
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.
AID1576811Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as dissociation rate constant measured after 90 mins by scintillation counting analysis
AID416882Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in Q-T interval at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID217926Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
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).
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).
AID440096Effect on heart rate in anesthetized Wistar rat assessed as P-Q intervals time at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1307726Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1057862Inhibition of RML prion protein infected in mouse dividing ScN2a-cl3 cells expressing full length mouse PrP assessed as reduction of PrPsc level after 5 days by ELISA2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID416877Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in QRS interval at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID440093Displacement of [3H]Clonidine from alpha2 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation counting2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID416881Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in QRS interval at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID411793Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID218994Oxidation was assessed indirectly by measuring bovine serum albumin thiol protection by using Ellman''s test at 500 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID440289Effect on heart rate in anesthetized Wistar rat assessed as Q-T intervals time at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1668034Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents.
AID218997Oxidation was assessed indirectly by measuring bovine serum albumin(BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 500 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
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.
AID218995Oxidation was assessed indirectly by measuring bovine serum albumin(BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 100 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID440097Effect on heart rate in anesthetized Wistar rat assessed as P-Q intervals time at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1509231Otoprotective activity against neomycin-induced neuromast hair cell death in 4 days post fertilized AB zebrafish larvae assessed as increase in hair cell survival incubated for 1 hr by inverted microscopic method2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509232Otoprotective activity against gentamicin-induced neuromast hair cell death in 4 days post fertilized AB zebrafish larvae assessed as increase in hair cell survival incubated for 6 hrs by inverted microscopic method2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509203Inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in size of MET currents at 10 uM measured at -160 mV to +96 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509239Effect on gentamycin-induced antibacterial activity against Pseudomonas aeruginosa at 2.2 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1668035Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents.
AID373867Hepatic clearance in human hepatocytes in absence of fetal calf serum2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
First-principle, structure-based prediction of hepatic metabolic clearance values in human.
AID440292Effect on heart rate in anesthetized Wistar rat assessed as heart beats per min at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
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.
AID13254871-octanol-water partition coefficient, log P of the compound2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID218991Oxidation was assessed indirectly by measuring bovine serum albumin (BSA) thiol protection from the formation of thiobarbituric acid reactive substances (TBARs) by TBARs test at 10 uM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID1257226Inhibition of Trichomonas vaginalis uridine ribohydrolase after 40 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1509219Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 10 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID440290Effect on heart rate in anesthetized Wistar rat assessed as heart beats per min at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1509216Binding affinity to MET in CD-1 mouse cochlear outer hair cells measured at +12.8 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509230Inhibition of MET channel in CD-1 mouse cochlea outer hair cells assessed as reduction in GTTR uptake at 100 uM preincubated for 5 mins followed by GTTR addition and measured after 24 mins by microscopic method2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID1509213Binding affinity to MET in CD-1 mouse cochlear outer hair cells measured at +16 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID440285Effect on heart rate in anesthetized Wistar rat assessed as QRS complex time at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1325485Inhibition of 15-LOX-mediated lipid oxidation in 10% C57BL/6J mouse plasma at 30 uM2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID416873Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat cerebral cortex by liquid scintillation method2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID440094Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation counting2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1509205Voltage-dependent inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in MET currents at 10 uM measured at -160 mV to +80 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
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.
AID1509234Toxicity in 3 days post fertilized AB zebrafish larvae assessed as reduction in larvae survival at 30 uM incubated for 48 hrs2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509233Toxicity in 3 days post fertilized AB zebrafish larvae assessed as reduction in larvae survival at 100 uM incubated for 48 hrs2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID416884Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in P-Q-interval at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID416885Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in QRS interval at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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.
AID1509192Cytotoxicity against CD-1 mouse cochlea assessed as induction of cell death in outer hair cell at >=30 uM after 48 hrs in presence of gentamicin by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1360120Antagonist activity at TLR4 (unknown origin) expressed in COS7 cells coexpressing HCN4 assessed as amplitude of inward current (I/I0 ratio) at 10 uM at -40 mV holding potential by pach clamp electrophysiology assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1257225Inhibition of Trichomonas vaginalis adenosine-guanosine preferring ribohydrolase after 40 mins in presence of 0.01% triton X-1002015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.
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.
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
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.
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).
AID680310TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 50 mg/L, Carvedilol: 10 uM) in Hs578T-Dox cells1999Biochemical pharmacology, Dec-01, Volume: 58, Issue:11
Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1509202Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell death in inner hair cell at >=30 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1325480Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of AAPH-derived peroxyl radicals-induced lipid hydroperoxide formation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID416876Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in P-Q interval at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID721748Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
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).
AID1509204Reversible inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in size of MET currents at 10 uM measured at -160 mV to +80 mV membrane potential measured after compound wash out by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1737231Inhibition of human CYP1B1 using 7-ethyl-O-resorufin as substrate incubated for 30 mins in presence of NADPH by EROD assay2020European journal of medicinal chemistry, May-01, Volume: 193Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
AID440286Effect on heart rate in anesthetized Wistar rat assessed as QRS complex time at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1509191Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 5 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1576812Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as residence time measured after 90 mins by scintillation counting analysis
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).
AID1307735Inhibition of of TREK2 (unknown origin) expressed in oocytes assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID416887Effect on heart rate in anaesthetized Wistar rat assessed as number of beats per minute at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID717844Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2.
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).
AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID1639037Antioxidant activity in rat brain homogenate assessed as inhibition of FeCl2/ascorbic acid-induced lipid peroxidation by measuring reduction in TBARS level at 1000 uM preincubated for 5 mins followed by FeCl2/ascorbic acid addition and measured after 30 m2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
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).
AID1307731Inhibition of of human TREK1 expressed in oocytes assessed as reversible current depression2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID1509215Binding affinity to MET in CD-1 mouse cochlear outer hair cells measured at -84 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509241Effect on gentamycin-induced antibacterial activity against Klebsiella pneumoniae at 11 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1360119Antagonist activity at TLR4 (unknown origin) expressed in COS7 cells coexpressing HCN2 assessed as amplitude of inward current (I/I0 ratio) at 10 uM at -40 mV holding potential by pach clamp electrophysiology assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID440092Displacement of [3H]Prazosin from alpha1 adrenergic receptor in Wistar rat cerebral cortex membrane by liquid scintillation counting2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1576810Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as association rate constant measured after 90 mins by scintillation counting analysis
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1509211Binding affinity to MET in CD-1 mouse cochlear outer hair cells measured at -164 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1509195Cytotoxicity in CD-1 mouse cochlea assessed as disruption of hair bundle morphology in inner hair cell at 20 uM in presence of gentamicin after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID416886Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in Q-T interval at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1509209Inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in MET currents at 1 to 10 uM measured at +96 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID416890Acute toxicity in iv dosed anaesthetized Wistar rat2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID218993Oxidation was assessed indirectly by measuring bovine serum albumin thiol protection by using Ellman''s test at 1 mM2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
New series of aryloxypropanolamines with both human beta(3)-adrenoceptor agonistic activity and free radical scavenging properties.
AID679589TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical)(Digoxin: 0.1 uM, Carvedilol: 50 uM) in MDR1-expressing LLC-PK1 cells2002Life sciences, Feb-15, Volume: 70, Issue:13
Interaction of digoxin with antihypertensive drugs via MDR1.
AID1509194Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell damage in inner hair cell at 20 uM in presence of gentamicin after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID440293Antiarrhythmic activity in Wistar rat assessed as inhibition of adrenaline-induced premature ventricular beats at 1 mg/kg, iv administered 15 mins before adrenaline challenge measured after 15 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
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).
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.
AID217930Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release)2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID1509207Voltage-dependent inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in MET currents at 1 to 10 uM measured at -150 mV to +100 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1222388Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID1325486Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of NpEP-derived singlet oxygen-induced lipid oxidation by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1509243Effect on gentamycin-induced antibacterial activity against Staphylococcus aureus at 11 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509214Binding affinity to MET in CD-1 mouse cochlear outer hair cells measured at +96 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID416883Effect on heart rate in anaesthetized Wistar rat assessed as number of beats per minute at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1495602In vivo inhibition of beta adrenoceptor in Wistar rat assessed as reduction in isoprenaline-induced tachycardia at 1 mg/kg, iv administered as single dose 10 mins prior to isoprenaline injection2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
AID1576808Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
AID1509236Toxicity in 3 days post fertilized AB zebrafish larvae assessed as effect on blood circulation at 30 uM incubated for 48 hrs by inverted microscopic method2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1325477Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of AAPH-derived peroxyl radicals-induced pyranine consumption at 50 uM2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID1509196Cytotoxicity in CD-1 mouse cochlea assessed as disruption of hair bundle morphology in outer hair cell at 20 uM in presence of gentamicin after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
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).
AID1509218Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 20 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1257224Inhibition of Trichomonas vaginalis adenosine-guanosine preferring ribohydrolase after 40 mins2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target.
AID777140Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Novel carvedilol analogues that suppress store-overload-induced Ca2+ release.
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).
AID1325483Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of NaOCl-induced lipid oxidation at 30 uM by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID416878Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in Q-T interval at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1360106Antagonist activity at human TLR4 expressed in HEK blue cells coexpressing MD-2/CD14 assessed as inhibition of LPS-induced NF-kappaB activation-mediated SEAP production after 24 hrs2018European journal of medicinal chemistry, Jun-25, Volume: 154Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents.
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.
AID1509197Cytotoxicity in CD-1 mouse cochlea assessed as disruption of hair bundle morphology in inner hair cell at 20 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID416891Therapeutic index, ratio of LD50 for Wistar rat to antiarrhythmic ED50 for Wistar rat2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID416879Effect on heart rate in anaesthetized Wistar rat assessed as number of beats per minute at 1 mg/kg, iv after 1 min by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1509228Inhibition of MET channel in CD-1 mouse cochlea outer hair bundles assessed as time constant of inward current decline at 1 uM at holding potential of -80 mV by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
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.
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.
AID721751Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1509198Cytotoxicity in CD-1 mouse cochlea assessed as disruption of hair bundle morphology in outer hair cell at 20 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1668036Inhibition of colony formation in human SK-MEL-28 cells at 5 to 100 uM supplemented with fresh medium containing compound every 72 hrs for 2 weeks by crystal violet staining based assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents.
AID1325478Antioxidant activity in 10% C57BL/6J mouse plasma assessed as inhibition of SIN-1-derived peroxynitrite-induced lipid oxidation at 50 uM by DPPP-based fluorescence assay2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
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.
AID416874Displacement of [3H]clonidine from alpha2 adrenergic receptor in rat cerebral cortex by liquid scintillation method2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1509229Inhibition of MET channel in CD-1 mouse outer hair bundles assessed as time constant of inward current decline at 3 uM at holding potential of -80 mV by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1222389Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID1509237Toxicity in 3 days post fertilized AB zebrafish larvae assessed as effect on larval movement at 100 uM incubated for 48 hrs2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1509201Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell death in inner hair cell at >=30 uM in presence of gentamicin after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
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.
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).
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.
AID1737234Inhibition of human CYP1B1 at 5 uM using 7-ethyl-O-resorufin as substrate incubated for 30 mins in presence of NADPH by EROD assay2020European journal of medicinal chemistry, May-01, Volume: 193Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
AID1325476Antioxidant activity assessed as inhibition of Meo-AMVN-derived peroxyl radicals-induced fucoxanthin consumption at 50 uM2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID389416Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID350217Octanol-water partition coefficient, log P of the cationic form of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1307736Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
AID1509242Effect on gentamycin-induced antibacterial activity against Pseudomonas aeruginosa at 11 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID440288Effect on heart rate in anesthetized Wistar rat assessed as Q-T intervals time at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1057864Ratio of LC50 for dividing mouse ScN2a-cl3 cells to EC50 for inhibition of RML prion protein2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID681131TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1325479Antioxidant activity assessed as inhibition of AAPH-derived peroxyl radicals-induced PGR consumption2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
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.
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.
AID1509235Toxicity in 3 days post fertilized AB zebrafish larvae assessed as effect on blood circulation at 100 uM incubated for 48 hrs by inverted microscopic method2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID440291Effect on heart rate in anesthetized Wistar rat assessed as heart beats per min at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1509199Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell damage in inner hair cell at 20 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1737233Cytotoxicity against human A549/Taxol cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
AID1668033Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents.
AID1325488Plasma concentration in paediatric patients with congestive heart failure2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Inhibition of plasma lipid oxidation induced by peroxyl radicals, peroxynitrite, hypochlorite, 15-lipoxygenase, and singlet oxygen by clinical drugs.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID1495685Antiarrhythmic activity in Wistar rat assessed as inhibition of adrenaline-induced premature ventricular extrasystoles administered iv 15 mins prior to adrenaline challenge2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
AID722794Antiarrhythmic activity in iv dosed Wistar rat adrenaline-induced arrhythmia model assessed as reduction of heart-rhythm disturbance administered 15 mins adrenaline-challenge2013Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.
AID416875Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID1442006Ratio of Kii for human OCT1-ASP+-inhibitor complex to Kis for human OCT1-inhibitor complex by Lineweaver-Burk plot analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID1509200Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell death in outer hair cell at >=30 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1509210Inhibition of MET in CD-1 mouse cochlear outer hair cells assessed as reduction in MET currents at 1 to 10 uM measured at -164 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID416880Effect on electrocardiogram in anaesthetized Wistar rat assessed as change in P-Q-interval at 1 mg/kg, iv after 5 mins by electrocardiography2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1.
AID302758Solubility by shake flask method2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Poorly soluble marketed drugs display solvation limited solubility.
AID440098Effect on heart rate in anesthetized Wistar rat assessed as P-Q intervals time at 1 mg/kg, iv after 15 mins by electrocardiography2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
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).
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.
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.
AID1509238Effect on gentamycin-induced antibacterial activity against Klebsiella pneumoniae at 2.2 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1495688Anti-aggregative activity in Wistar rat whole blood assessed as inhibition of collagen-induced aggregation up to 100 uM preincubated for 3 mins followed by collagen induction measured for 6 mins2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
AID1509240Effect on gentamycin-induced antibacterial activity against Staphylococcus aureus at 2.2 uM incubated for 16 to 20 hrs by BacTiter-Glo assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1495689Anti-aggregative activity in Wistar rat whole blood assessed as inhibition of collagen/adrenaline-induced aggregation up to 100 uM preincubated for 3 mins followed by collagen induction measured for 6 mins2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
AID1509193Cytotoxicity in CD-1 mouse cochlea assessed as induction of cell death in outer hair cell at 10 to 20 uM after 48 hrs by confocal microscopic analysis2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
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.
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.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC 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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
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.
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.
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.
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.
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.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
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.
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.
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.
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.
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.
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.
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.
AID17985803H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: \\The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.\\2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
AID1346297Human beta3-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
AID1346260Human beta1-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,791)

TimeframeStudies, This Drug (%)All Drugs %
pre-199064 (2.29)18.7374
1990's396 (14.19)18.2507
2000's1175 (42.10)29.6817
2010's896 (32.10)24.3611
2020's260 (9.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 123.97

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 Index123.97 (24.57)
Research Supply Index8.19 (2.92)
Research Growth Index5.37 (4.65)
Search Engine Demand Index232.75 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (123.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials680 (23.18%)5.53%
Reviews339 (11.56%)6.00%
Case Studies142 (4.84%)4.05%
Observational15 (0.51%)0.25%
Other1,757 (59.90%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (192)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Study Evaluating the Effect of Carvedilol in Patients With Active Rheumatoid Arthritis [NCT06108518]Early Phase 170 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Prevention of Left Ventricular Dysfunction With Enalapril and Carvedilol in Patients Submitted to Intensive Chemotherapy for the Treatment of Malignant Hemopathies [NCT01110824]Phase 390 participants (Actual)Interventional2008-04-30Completed
Use of Beta-blockers and Risk of New Onset Diabetes [NCT01587638]12,336 participants (Actual)Observational2009-04-30Completed
A Pilot Study: Evaluating the Anti-Cancer Effects of Carvedilol With TTFields and Standard of Care in Glioblastoma and Response of Peripheral Glioma Circulating Tumor Cells [NCT03980249]Early Phase 10 participants (Actual)Interventional2020-09-30Withdrawn(stopped due to No funding)
A Randomized, Open-label, Single-dose, Crossover Clinical Trial to Evaluate the Food Effect on the Pharmacokinetics of Dilatrend SR 64mg Capsule After Oral Administration in Healthy Male Volunteers [NCT01340248]Phase 124 participants (Anticipated)Interventional2011-07-31Completed
A Randomized, Open-label, Comparative, Non-inferiority, Multicenter Study to Compare Efficacy of Losartan Potassium Group and Carvedilol Group on Arterial Stiffness in Essential Hypertension Patients [NCT00496834]Phase 4201 participants (Actual)Interventional2008-02-01Completed
A Controlled Trial of Nadolol Plus Isosorbide Mononitrate vs. Carvedilol for the Prevention of Variceal Rebleeding [NCT01103154]Phase 4121 participants (Actual)Interventional2005-03-31Completed
Danish Trial of Beta Blocker Treatment After Myocardial Infarction Without Reduced Ejection Fraction (DANBLOCK) [NCT03778554]Phase 42,760 participants (Anticipated)Interventional2018-12-17Recruiting
A Randomized, Double-Blind, Placebo-Controlled, Flexible-Dose Study to Assess the Safety and Efficacy of Carvedilol Versus Placebo in the Treatment of Post Traumatic Stress Disorder [NCT01221792]Phase 280 participants (Anticipated)Interventional2010-10-31Active, not recruiting
A Clinical Trial to Investigate the Influence of Cytochrome P450 2D6 Polymorphism on the Pharmacokinetic/Pharmacodynamics Characteristics of Carvedilol in Healthy Korean Volunteers [NCT02286934]Phase 124 participants (Actual)Interventional2014-09-30Completed
Mechanisms of Improvement With Beta-Blocker Treatment in Heart Failure [NCT01261065]Phase 455 participants (Actual)Interventional2001-12-31Completed
A Prospective,Open Labeled, Randomized Controlled Trial Comparing Carvedilol + VSL# 3 Versus Endoscopic Variceal Ligation for Primary Prophylaxis of Esophageal Variceal Bleeding in Cirrhotic Patients Non Responder to Carvedilol. [NCT01196481]40 participants (Actual)Interventional2012-12-31Completed
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04767061]Phase 49 participants (Actual)Interventional2021-04-01Completed
WFA+M2BP in Evaluation of Portal Hypertension and Clinical Outcome in Patients With Liver Cirrhosis [NCT03195634]80 participants (Anticipated)Observational2017-06-30Not yet recruiting
Effect of Beta-blocker on Cardioprotective Effect of Remote Ischemic Conditioning [NCT03169426]Phase 411 participants (Actual)Interventional2017-05-17Completed
COR111096, A Randomized, Double-Blind, Active-Controlled, Parallel Group, Multicenter Study Comparing the Proportion of Subjects With Stage 1 or 2 Essential Hypertension Who Achieve Target Blood Pressure While Receiving Either Carvedilol CR + Lisinopril o [NCT00624065]Phase 3348 participants (Actual)Interventional2008-03-31Completed
Beta-blockers or Placebo for Primary Prophylaxis of Oesophageal Varices (BOPPP Trial). A Blinded, Multi-centre, Clinical Effectiveness and Cost-effectiveness Randomised Controlled Trial [NCT03776955]Phase 41,200 participants (Anticipated)Interventional2019-06-17Recruiting
The Effect of Carvedilol Rapid Up-Titration in Patients With Heart Failure With Reduced Ejection Fraction (Biomolecular and Clinical Study on IL-6, TNF-α, NT-ProBNP, MDA, LVEF, 6MWT, and KCCQ) [NCT05179070]Phase 426 participants (Anticipated)Interventional2021-09-10Recruiting
Comparison of Carvedilol and Atorvastatin for Prevention of Contrast-Induced Nephropathy After Cardiac Catheterization [NCT03867994]Phase 2144 participants (Actual)Interventional2016-02-01Completed
A Feasibility Study: Evaluating Carvedilol With Chemotherapy in Second Line Glioblastoma Multiforme and Response of Peripheral Glioma Circulating Tumor Cells [NCT03861598]Early Phase 14 participants (Actual)Interventional2019-07-19Terminated(stopped due to Due to Covid)
Use of Determination of Drug Levels to Optimize Pharmacotherapy of Heart Failure [NCT06035978]Phase 4100 participants (Anticipated)Interventional2023-11-30Not yet recruiting
A Randomized, Two-Way Crossover, Single-Dose, Open Label Study to Evaluate the Relative Bioavailability of a Test Tablet Formulation of Carvedilol (25 mg), Compared to an Equivalent Dose of COREG® (SmithKline Beecham Pharmaceuticals) in 24 Fed, Healthy, A [NCT00834873]Phase 124 participants (Actual)Interventional2001-12-31Completed
A Randomized, Two-Way Crossover, Single-Dose, Open Label Study to Evaluate the Relative Bioavailability of a Test Tablet Formulation of Carvedilol (25 mg), Compared to an Equivalent Dose of COREG® (SmithKline Beecham Pharmaceuticals) in 36 Fasted, Healthy [NCT00834795]Phase 136 participants (Actual)Interventional2001-12-31Completed
Assessment of Clinical Effect and Treatment Quality of Rapid Release Carvedilol Versus SLOW Release Carvedilol-SR in HEART FAILURE Patient (SLOW-HF): A Prospective Randomized, Open-label, Multicenter Study [NCT03209180]Phase 4320 participants (Anticipated)Interventional2016-10-27Recruiting
The Effect of Carvedilol Vs Propranolol in Patients With Cirrhosis Related Esophagogastric Varices After Multiple Endoscopic Treatments For Secondary Prophylaxis:A Randomized Controlled Trial [NCT02385422]Phase 4480 participants (Anticipated)Interventional2015-03-31Recruiting
Effect of Dapagliflozin on Secondary Mitral Regurgitation in Patients With Left Ventricular Dysfunction [NCT05849766]Phase 3150 participants (Anticipated)Interventional2023-04-27Recruiting
A Pilot Study of Risk-Guided Cardioprotection With Carvedilol in Breast Cancer Patients Treated With Doxorubicin and/or Trastuzumab [NCT04023110]Phase 169 participants (Actual)Interventional2019-08-09Active, not recruiting
"Efficacy and Safety of Carvedilol in Cirrhosis Patients With Uncomplicated Ascites Without High Risk Esophageal Varices- A Randomised Controlled Trial" [NCT05057572]120 participants (Anticipated)Interventional2021-10-01Recruiting
Detecting and Treating Subclinical Anthracycline Therapy Related Cardiac Dysfunction in Low Income Country [NCT03542058]Phase 350 participants (Anticipated)Interventional2018-06-30Not yet recruiting
Multicenter, Randomized, 2 x 2 Factorial, Phase 3 Study to Assess the Efficacy of Carvedilol and Empagliflozin on Improvement of Right Ventricular Remodeling in Patients With Severe Functional Tricuspid Regurgitation [NCT04345796]Phase 3180 participants (Anticipated)Interventional2021-02-15Recruiting
The Impact of Carvedilol Posology on Clinically Significant Portal Hypertension: Insights From Elastography Measurements [NCT06015373]34 participants (Actual)Interventional2023-06-01Completed
Beta-blocker Effect on Structural Remodeling and Gene Expression in the Failing Human Heart [NCT01798992]Phase 456 participants (Actual)Interventional2000-09-30Completed
A Phase 3 Study of Carvedilol vs Variceal Band Ligation vs Combination Therapy for Primary Prophylaxis of Variceal Bleeding [NCT02066649]Phase 30 participants (Actual)Interventional2018-07-31Withdrawn(stopped due to We need to revise and redesign the study)
Rate Control in Atrial Fibrillation: A Randomized, Double-Blind, Crossover Comparison of Carvedilol and Metoprolol Tartrate [NCT02251509]Phase 420 participants (Anticipated)Interventional2016-12-31Not yet recruiting
Therapeutic Approach to Diastolic Dysfunction in Chronic Liver Disease Patients and Its' Impact on Morbidity and Mortality [NCT02294292]189 participants (Actual)Interventional2014-07-01Completed
Effects of Sleep Deprivation and Adrenergic Inhibition on Glymphatic Flow in Humans [NCT03576664]Early Phase 122 participants (Actual)Interventional2018-08-28Completed
A Prospective, Double-blind, Randomized Placebo-controlled Trial of Carvedilol for Pre-primary Prophylaxis of Esophageal Varices in Cirrhosis [NCT01212250]132 participants (Anticipated)Interventional2010-09-01Recruiting
Carvedilol SR Study for Biomarkers From Blood and Urine and Safety of in Patients With Heart Failure With Preserved Ejection Fraction : a Prospective, Randomized, Double Blind, Placebo-controlled, Multicenter, Pilot Trial (CAYMUS-HFpEF) [NCT03948685]Phase 4300 participants (Anticipated)Interventional2019-05-31Not yet recruiting
A Randomized, Open-label, Single Dose, Dose-rising 10-sequence, 3-period Balanced Incomplete Blocked Clinical Trial to Evaluate Dose-proportionality of Dilatrend SR in Healthy Male Volunteers [NCT01369472]Phase 130 participants (Actual)Interventional2011-06-30Completed
Pharmacologic Reversal of Ventricular Remodeling in Childhood Cancer Survivors at Risk for Heart Failure (PREVENT-HF): A Phase 2b Randomized Placebo-Controlled (Carvedilol) Trial [NCT02717507]Phase 2196 participants (Actual)Interventional2016-04-04Active, not recruiting
Banding Ligation With Carvedilol vs. Carvedilol for the Prevention of First Bleeding in Cirrhotics With Moderate Varices [NCT01383044]Phase 465 participants (Actual)Interventional2011-07-08Terminated(stopped due to slow enrollment)
Carvedilol Post-intervention Long-term Administration in Large-scale Randomized Controlled Trial [NCT01155635]Phase 4801 participants (Actual)Interventional2010-07-31Completed
A Prospective, Double-blind, Randomized Placebo-controlled Trial of Carvedilol for Early Primary Prophylaxis of Esophageal Varices in Cirrhosis. [NCT01196507]140 participants (Actual)Interventional2010-11-30Completed
Propranolol, Carvedilol and Rosuvastatin in the Prevention of Recurrent Variceal Haemorrhage in Patients With Cirrhotic Portal Hypertension [NCT03720067]Phase 2/Phase 380 participants (Anticipated)Interventional2019-01-25Recruiting
A Nested Case-control Study of the Association Between Coreg IR and Coreg CR and Hypersensitivity Reactions: Anaphylactic Reaction/Angioedema-Updated Analysis [NCT01316952]1 participants (Actual)Observational2010-06-30Completed
Acute Hemodynamic Response to Carvedilol in Predicting Survival in Acute on Chronic Liver Failure Patients - A Pilot Study. [NCT05180292]50 participants (Anticipated)Interventional2022-01-07Recruiting
Pentoxifylline Plus Carvedilol vs Carvedilol Monotherapy in Preventing New Decompensation in Stable Cirrhotic Patients With Prior Decompensation, an Open Label Randomised Control Trial [NCT06041932]180 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Effect of Coreg CR on BP, Endothelial Function, Exhaled Nitric Oxide, and Nitric Oxide Production and Oxidation [NCT00732511]Phase 440 participants (Anticipated)Interventional2008-04-30Recruiting
An Open Label, Balanced, Randomised, Two-Treatment, Two-Period, Two-Sequence, Single-Dose, Crossover Bioavailability Study on Carvedilol Formulations Comparing Carvedilol 12.5 mg Tablets of Ranbaxy Laboratories With Coreg® 12.5 mg Tablets of Glaxosmithkli [NCT00776113]40 participants (Actual)Interventional2003-08-31Completed
A Prospective Study of Early Stage Breast Cancer Patients With Abnormal Myocardial Deformation Treated With Anthracycline and/or Trastuzumab and Pertuzumab-based Cancer Therapy [NCT02993198]Phase 2134 participants (Actual)Interventional2015-04-30Active, not recruiting
Beta-blocker Stratification Using Quantitative MRI Techniques to Assess Portal Pressure and Response to Treatment in Patients With Portal Hypertension [NCT03114813]68 participants (Anticipated)Observational2017-01-31Recruiting
An Open-label, Randomized, Crossover, Repeat-dose Study to Evaluate the Steady-State Pharmacokinetic Profile of the Final Fixed Dose Combination (FDC) Formulation of COREG CR and Lisinopril as Compared to COREG CR in Subjects With Essential Hypertension [NCT00537043]Phase 124 participants (Anticipated)Interventional2007-10-31Completed
Impact of Roux-en-Y Gastric Bypass (RYGB) Bariatric Surgery on System Pharmacology: Single-dose Cross-over Pharmacokinetic Study of Simvastatin and Carvedilol. [NCT04049786]Phase 4120 participants (Anticipated)Interventional2019-06-01Enrolling by invitation
Effects of Selective and Nonselective Beta-blockade on Platelet Aggregation in Patients With Acute Coronary Syndrome [NCT02809820]Phase 4100 participants (Actual)Interventional2016-05-31Completed
Free Fatty Acids-Induced Hypertension, Endothelial Dysfunction, Inflammation, Insulin Resistance, and Autonomic Dysfunction in Lean and Obese Subjects (Aim #2) [NCT02406586]36 participants (Actual)Interventional2009-07-31Completed
Cluster and Registry Trial of the Working Group of Heart Failure in Denmark. Are Carvedilol and Metoprolol Succinate Comparable Treatments in Heart Failure Patients With Reduced Ejection Fraction [NCT04996550]5,600 participants (Anticipated)Observational [Patient Registry]2022-01-03Not yet recruiting
Beta Blockers in Pulmonary Arterial Hypertension (PAH) A Pilot Study of Efficacy and Safety [NCT02120339]Phase 15 participants (Actual)Interventional2014-05-31Terminated(stopped due to Low enrollment)
The Cardiac Insufficiency BIsoprolol Study in Japanese Patients With Chronic Heart Failure (CIBIS-J) [NCT02137733]220 participants (Anticipated)Interventional2013-06-30Recruiting
The Effect of Adrenergic Blocker Therapy on Cardiac and Striatal Transporter Uptake in Pre-Motor and Symptomatic Parkinson's Disease: A Follow up Study [NCT04218968]Phase 215 participants (Anticipated)Interventional2019-12-30Enrolling by invitation
TREatment With Beta-blockers After myOcardial Infarction withOut Reduced Ejection fracTion [NCT03596385]Phase 48,468 participants (Anticipated)Interventional2018-10-31Recruiting
An Open Label, Balanced, Randomised, Two-Treatment, Two-Period, Two-Sequence, Single-Dose, Crossover Bioavailability Study on Carvedilol Formulations Comparing Carvedilol 12.5 mg Tablets of Ranbaxy Laboratories With Coreg® 12.5 mg Tablets of Glaxosmithkli [NCT00775619]40 participants (Actual)Interventional2003-09-30Completed
A Randomised, Single Blind, Multicentre, 9-month, Phase IV Study, Comparing Treatment Guided by Clinical Symptoms and Signs and NT-proBNP vs Treatment Guided by Clinical Symptoms and Signs Alone, in Patients With Heart Failure (HF) and Left Ventricular Sy [NCT00391846]Phase 4252 participants (Actual)Interventional2006-10-31Completed
Effects of Cardioprotective Therapy, Carvedilol vs Ramipril, in Patients Affected by Duchenne and Becker Muscular Dystrophy. Clinical Significance and Prognostic Value of Cardiac Magnetic Resonance Study. [NCT00819845]Phase 4194 participants (Anticipated)Interventional2008-12-31Recruiting
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
A Multicenter,Randomized, Double Blind, Double Dummy, Parallel Group Study to Compare Effects of Coreg CR and Coreg IR on Left Ventricular End Systolic Volume Index in Subjects With Stable Chronic Heart Failure [NCT00323037]Phase 3318 participants (Actual)Interventional2006-03-31Completed
A Study to Evaluate the Potential Incidence of Orthostatic Hypotension in Elderly Hypertensive Patients Following Administration of a Combination of COREG CR and Lisinopril [NCT00508365]Phase 162 participants (Actual)Interventional2007-09-25Completed
Oral Carvedilol in Escalating Doses in the Acute Treatment of Atrial Fibrillation [NCT02832089]Phase 330 participants (Actual)Interventional2000-12-31Completed
A Two-Way Crossover, Open-Label, Single Dose, Fed, Bioequivalence Study of Carvedilol 12.5 mg Tablets Versus Coreg® 12.5 mg Tablets in Normal, Healthy, Non-Smoking Male and Female Subjects [NCT00864149]Phase 136 participants (Actual)Interventional2005-10-31Completed
A Randomized, Double-Blind, Multi-Center Study Comparing the Effects of Carvedilol Phosphate Modified Release Formulation (COREG- MR) With Metoprolol Succinate (TOPROL XL) on the Lipid Profile in Normolipidemic, or Mildly Dyslipidemic Hypertensive Patient [NCT00273052]Phase 3514 participants (Actual)Interventional2006-01-05Completed
Effects of Carvedilol on Cocaine Use in Humans [NCT00000294]Phase 20 participants Interventional1998-09-30Completed
A Randomized, Double-Blind, Multi-Center Study Comparing the Effects of Carvedilol Modified Release Formulation (COREG MR) and Atenolol in Combination With and Compared to an Angiotensin Converting Enzyme Inhibitor (Lisinopril) on Left Ventricular Mass Re [NCT00108082]Phase 3287 participants (Actual)Interventional2005-01-31Completed
The Effect of HVPG-Guided Individualized Therapy in Patients With Cirrhosis Related Esophagogastric Variceal Hemorrhage For Secondary Prophylaxis:A Randomized Controlled Trial [NCT02638415]Phase 4500 participants (Anticipated)Interventional2015-12-31Recruiting
Effects of Spironolactone on Fibrosis Progression and Portal Pressure in Patients With Advanced Chronic Liver Disease [NCT02907749]Phase 496 participants (Actual)Interventional2018-01-01Completed
A Study to Evaluate the Safety and Tolerability of SK&F-105517-D in Patients With Chronic Heart Failure- An Open-label Study to Evaluate the Safety and Tolerability, Pharmacokinetics and Pharmacodynamics of SK&F-105517-D in Patients With Chronic Heart Fai [NCT00742508]Phase 141 participants (Actual)Interventional2008-08-28Completed
Prognostic Value of the Circadian Pattern of Ambulatory Blood Pressure for Multiple Risk Assessment [NCT00741585]Phase 421,983 participants (Actual)Interventional2008-09-01Completed
Efficacy of Nonselective Beta Blockers vs Placebo in Patients With Acute-on-chronic Liver Failure With Small/ no Esophageal Varices [NCT02583698]136 participants (Actual)Interventional2015-10-01Completed
Primary Prophylaxis of High-risk Esophageal Gastric Variceal Bleeding Comparing Carvedilol and Endoscopic Therapy: A Multicenter Randomized Controlled Trial [NCT02695732]Phase 4792 participants (Anticipated)Interventional2015-12-31Recruiting
Comparison of Carvedilol and Atenolol on Anti-anginal and Metabolic Effects in Patients With Stable Angina Pectoris [NCT02547597]Phase 499 participants (Actual)Interventional2011-04-30Completed
Single-Dose Food In Vivo Bioequivalence Study of Carvedilol Tablets (12.5 mg; Mylan) to Coreg® Tablets (12.5 mg; GSK) in Healthy Volunteers [NCT00648622]Phase 150 participants (Actual)Interventional2004-04-30Completed
A Two-Way Crossover, Open-Label, Single Dose, Fasting, Bioequivalence Study of Carvedilol 12.5 mg Tablets Versus Coreg® 12.5 mg Tablets in Normal, Healthy, Non-Smoking Male and Female Subjects [NCT00864435]Phase 136 participants (Actual)Interventional2005-10-31Completed
NT-proBNP Selected PreventiOn of Cardiac eveNts in a populaTion of dIabetic Patients Without A History of Cardiac Disease: a Prospective Randomized Trial [NCT02817360]Phase 42,400 participants (Anticipated)Interventional2016-02-29Recruiting
Vascular Benefits of Adding CarvedilolCR to Type2 Diabetic Patients on ACEI:Effects on Oxidative Stress and Inflammation. [NCT00430040]Phase 414 participants (Actual)Interventional2007-02-28Terminated
Comparative Effects of Nebivolol and Carvedilol on Diastolic Function of the Left Ventricle in the Elderly Heart Failure Patients With Preserved Ejection Fraction: Study Protocol for a Randomized Controlled Trial [NCT02619526]62 participants (Anticipated)Interventional2016-12-31Recruiting
Hepatic Vein Pressure Gradient(HVPG)-Guided Therapy vs Carvedilol Plus Endotherapy for the Prevention of Esophageal Variceal Rebleeding in Patients With Liver Cirrhosis: A Prospective Randomized Controlled Trial [NCT04254822]220 participants (Anticipated)Interventional2020-06-01Not yet recruiting
An Open-label Pilot Study Using Carvedilol-CR as a P-glycoprotein Inhibitor as Adjunct Therapy in the Treatment of Medically-refractory Epilepsy [NCT00524134]Phase 2/Phase 36 participants (Actual)Interventional2008-12-31Terminated(stopped due to PI left the institution.)
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04757584]Phase 49 participants (Actual)Interventional2021-04-01Completed
Beta Adrenergic Receptor Blockade as a Novel Therapy for Patients With Adenocarcinoma of the Prostate [NCT02944201]Phase 222 participants (Anticipated)Interventional2017-04-01Active, not recruiting
RCT of Carvedilol vs Variceal Band Ligation in the Primary Prophylaxis of Oesophageal Variceal Haemorrhage [NCT01070641]Phase 4148 participants (Anticipated)Interventional2002-06-30Recruiting
The Vascular Effects of Carvedilol Controlle Release (CR) + Lisinopril Versus Lisinopril + Hydrochlorothiazide (HCTZ) in Abdominally Obese Hypertensive Patients [NCT00459056]Phase 325 participants (Actual)Interventional2007-04-30Completed
Multicenter, Randomized, Double-blind, Placebo-controlled Study on the Effectiveness of Treatment With Beta-blockers to Prevent Decompensation of Cirrhosis With Portal Hypertension [NCT01059396]Phase 4201 participants (Actual)Interventional2010-01-28Completed
A Randomized, Double-Blind, Double-Dummy, Parallel Group, Factorial Design Trial to Assess the Efficacy and Safety of up to Six Weeks Treatment With 20mg, 40mg, or 80mg QD Doses of Carvedilol Controlled Release Formulation (COREG CR) or 10mg, 20mg, or 40m [NCT00347360]Phase 3654 participants (Actual)Interventional2006-07-31Completed
Randomized,2-way Crossover, Bioequivalence Study of Carvedilol 25 mg Film-coated Tablets and COREG® 25 mg Film-coated Tablets Administered as 1 x 25 mg Film-coated Tablet in Healthy Subjects Under Fasting Conditions [NCT01064154]Phase 136 participants (Actual)Interventional2002-05-31Completed
Randomized,2-way Crossover, Bioequivalence Study of Carvedilol 25 mg Film-coated Tablets and COREG® 25 mg Film-coated Tablets Administered as 1 x 25 mg Film-coated Tablet in Healthy Subjects Under Fed Conditions [NCT01064180]Phase 124 participants (Actual)Interventional2002-05-31Completed
CSP #2026 - Beta Blocker Dialyzability on Cardiovascular Outcomes (BRAVO) [NCT05931276]Phase 32,540 participants (Anticipated)Interventional2024-01-01Not yet recruiting
A Comparison of the Effectiveness of Carvedilol Versus Metoprolol for Atrial Fibrillation Appearing After Off-Pump Coronary Bypass Surgery in the Carvedilol or Metoprolol Post-Revascularization Atrial Fibrillation Controlled Trial (COMPACT) [NCT00198614]650 participants Interventional2005-01-31Completed
Effects of Inpatient Initiation of Carvedilol and Nurse Management on Health Outcomes in Vulnerable Heart Failure Patients (ECHO Study): a Randomized Trial [NCT00381030]Phase 4100 participants Interventional2002-10-31Completed
Efficacy and Safety Comparison of Extended-Release Carvedilol Sulfate and Sustained-release Metoprolol Succinate in Patients With Hypertension [NCT01970059]Phase 3302 participants (Anticipated)Interventional2013-10-31Recruiting
To Study the Hemodynamic Response of Early Addition of Carvedilol to Terlipressin in Acute Variceal Bleed in Child's B and C Cirrhosis- A Randomized Controlled Trial [NCT05699824]100 participants (Anticipated)Interventional2023-07-01Recruiting
Efficacy and Safety Comparison of Extended-Release Carvedilol Sulfate and Sustained-release Metoprolol Succinate in Patients With Heart Failure [NCT02012075]Phase 3316 participants (Anticipated)Interventional2013-12-31Recruiting
Carvedilol for the Prevention of Minor Cardiac Damage and Cardiac Function in Duchenne Muscular Dystrophy [NCT00606775]Phase 460 participants (Anticipated)Interventional2007-12-31Recruiting
Effects of Dapagliflozin on Hypotensive Patients With Depressed Left Ventricular Ejection Fraction After Sacubitril/Valsartan Therapy [NCT04575675]Phase 478 participants (Actual)Interventional2020-05-29Completed
Clinical Efficacy of Carvedilol for Psychostimulant Dependence [NCT01171183]Phase 232 participants (Actual)Interventional2010-08-31Completed
Collaborative Systematic Overview of Randomised Controlled Trials of Beta-Blockers in the Treatment of Heart Failure [NCT00832442]18,240 participants (Anticipated)Observational2008-08-31Enrolling by invitation
Blood Pressure, Endothelial Cell Dysfunction, and Outcomes in Dialysis Patients [NCT00827775]Phase 455 participants (Actual)Interventional2009-06-30Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Carvedilol Tablets (12.5 mg; Mylan) to Coreg® Tablets (12.5 mg; GSK) in Healthy Volunteers [NCT00650416]Phase 150 participants (Actual)Interventional2004-03-31Completed
Pilot Study of the Safety and Efficacy of Carvedilol in Pulmonary Arterial Hypertension [NCT00964678]Phase 1/Phase 210 participants (Actual)Interventional2010-06-30Completed
A Randomized, Open-label, Multiple-dose, Crossover Phase I Study to Compare the Pharmacokinetic Characteristics and Safety of Dilatrend SR Capsule 32 mg and Dilatrend Tablet 25 mg in Healthy Male Subjects [NCT01819870]Phase 148 participants (Anticipated)Interventional2013-04-30Not yet recruiting
Phase III Clinical Trial to Evaluate the Antihypertensive Effect of AGSCT101 Versus Carvedilol in Patient With Stage 1 to 2 Essential Hypertension [NCT01413048]Phase 3260 participants (Anticipated)Interventional2011-01-31Recruiting
Ischemia In Hemodialysed Patients And Outcome: Ivabradine Versus Carvedilol. A Randomized, Double Blind Study [NCT01425164]Phase 4220 participants (Anticipated)Interventional2011-01-31Recruiting
Mechanism of Increased Ambulatory Blood Pressure in Patients With Intradialytic Hypertension and Hemodialysis Controls: A Case Control Study and Crossover Trial Comparing Carvedilol and Prazosin Hydrochloride [NCT01862497]76 participants (Actual)Observational2013-01-31Completed
Carvedilol and Micro T-Wave Alternans in Hypertensives With Chronic Kidney Disease [NCT00638222]6 participants (Actual)Interventional2008-05-31Terminated(stopped due to Poor enrollment)
Extension Study of Carvedilol for the Prevention of the Esophageal Varices Progression on HBV Cirrhotic Patients With Anti-Viral Therapy [NCT05021406]240 participants (Anticipated)Interventional2021-01-08Recruiting
A Randomized, Open-label, Single-dose, Three-period, Crossover Study to Demonstrate the Bioequivalence of the Fixed Dose Combination (FDC) of COREG CR™ and Lisinopril to COREG CR and ZESTRIL [NCT00556920]Phase 150 participants (Actual)Interventional2007-10-31Completed
A Phase II, Multi-center, Multiple-dose, Double-blind, Randomized, Crossover Study Comparing the Pharmacodynamic Effects of a Once-daily Controlled-Release Carvedilol (CRC; Egalet® Formulation) and an Immediate-Release Carvedilol (IRC) Formulation in Pati [NCT00444834]Phase 214 participants (Actual)Interventional2007-04-30Terminated(stopped due to IMP supply)
Beta-blocker Uptitration in Heart Failure Patients Receiving Cardiac Resynchronization Therapy With Optivol Fluid Status Monitoring System [NCT00433043]Phase 42 participants (Actual)Interventional2007-01-31Terminated(stopped due to Insufficient enrollment)
Comparison of Effect of cARvedilol Compared To bISoprolol on cenTral Pulse Pressure in Hypertension (ARTIST) Study [NCT01243827]Phase 4200 participants (Anticipated)Interventional2010-11-30Recruiting
[NCT00497003]Phase 450 participants (Actual)Interventional2004-02-29Completed
Early Precise Diagnosis and Intervention of Cirrhotic Portal Hypertension (CPT) Based on a Noninvasive 3D-virtual-model of Hepatic Portal System (3D-vHPS) [NCT02925975]Phase 4100 participants (Actual)Interventional2015-01-31Active, not recruiting
A Prospective Multi-Center Randomized Study to Evaluate the Effects of Carvedilol on Cardiotoxicity in Cancer Patients Submitted to Anthracycline Therapy [NCT04939883]Phase 41,018 participants (Anticipated)Interventional2021-08-01Recruiting
Beta Blockers for Treatment of Pulmonary Arterial Hypertension in Children [NCT01723371]Phase 1/Phase 20 participants (Actual)Interventional2012-09-30Withdrawn(stopped due to Due to lack of enrollment.)
[NCT00004854]Phase 10 participants InterventionalCompleted
A Randomized, Open-label, Single-dose, Crossover Study to Demonstrate the Bioequivalence of the Final Fixed Dose Combination (FDC) Formulation (COREG CR & Lisinopril) to COREG CR & ZESTRIL Employed in the Phase III Factorial Study [NCT00552708]Phase 155 participants (Actual)Interventional2007-09-30Completed
Acute Hemodynamic Response to Carvedilol in Children With Clinically Significant Portal Hypertension. [NCT05767229]40 participants (Anticipated)Interventional2023-03-15Not yet recruiting
A Randomized, Double-blind, Positive-Controlled, Multicenter Study Comparing the Efficacy of Carvedilol Phosphate Modified Release Formulation (COREG MR) and Metoprolol Succinate Extended Release (TOPROL-XL) on the Reduction of Microalbuminuria in Patient [NCT00123903]Phase 31,220 participants Interventional2005-07-31Terminated
Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM)- Propranolol/Carvedilol Versus Atenolol/Bisoprolol/Sotalol [NCT05794997]817,337 participants (Actual)Observational2022-11-30Active, not recruiting
Carvedilol Effect in Preventing Chemotherapy - Induced Cardiotoxicity. A Randomized Double Blind Study. [NCT01724450]Phase 3200 participants (Actual)Interventional2013-04-30Completed
Danish Carvedilol Study in Portal Hypertension. Carvedilol in the Prevention of Bleeding in Portal Hypertension and Esophageal Varices [NCT00493480]Phase 340 participants (Anticipated)Interventional2003-09-30Completed
Carvedilol vs.Metoprolol: A Comparison of Effects on Endothelial Function and Oxidative Stress in Response to Acute Hyperglycemia in Patients With Type 2 Diabetes and Hypertension [NCT00642434]Phase 422 participants (Actual)Interventional2004-01-31Completed
AuTophagy Activation for Cardiomyopathy Due to Anthracycline tReatment (ATACAR) Trial [NCT04190433]Phase 20 participants (Actual)Interventional2020-09-01Withdrawn(stopped due to Administratively closed due to low/no accrual)
Organized Program to Initiate Lifesaving Treatment in Hospitalized Patients With Heart Failure (OPTIMIZE-HF): An Internet-based Registry and Process of Care Improvement Program for Heart Failure Patients [NCT00344513]Phase 450,000 participants Interventional2002-12-16Completed
Nebivolol Versus Bisoprolol Versus Carvedilol in Heart Failure: Effects on Exercise Capacity and Hypoxia, Chemoreceptor Response, Pulmonary Function [NCT00517725]Phase 460 participants (Actual)Interventional2007-07-31Completed
A Randomized, Placebo-Controlled, Open-label, Multi-Center Study to Assess the Efficacy and Safety of Fuzheng Huayu Combined With Entecavir and Carvedilol in Moderate and Severe Cirrhotic Portal Hypertension Due to Hepatitis B Virus [NCT02945982]Phase 4184 participants (Anticipated)Interventional2018-04-05Recruiting
The Use of Low-Dose Carvedilol to Improve Hypoglycemia Awareness in Patients With Type 1 Diabetes Mellitus [NCT03538015]Phase 21 participants (Actual)Interventional2019-04-22Terminated(stopped due to Sponsor was impacted by COVID-19 and did not have sufficient funds to continue.)
Action to Control Cardiovascular Risk in Diabetes (ACCORD) [NCT00000620]Phase 310,251 participants (Actual)Interventional1999-09-30Completed
Beta-blockers Or Placebo for Primary Prophylaxis of Oesophageal Varices (BOPPP Trial). A Blinded, UK Multi-centre, Clinical Effectiveness and Cost-effectiveness Randomised Controlled Trial. [NCT05872698]Phase 41,200 participants (Anticipated)Interventional2019-06-01Recruiting
A Randomized, Double-Blind, Multicenter Study Comparing the Effects of Carvedilol and Metoprolol on Glycemic Control in Hypertensive Patients With Type II Diabetes Mellitus. [NCT00060931]Phase 4501 participants (Actual)Interventional2001-06-30Completed
A Multicenter, Open Label Extension Study to Evaluate the Safety of Twice Daily Oral Carvedilol in Pediatric Patients With Chronic Heart Failure [NCT00129363]Phase 375 participants (Actual)Interventional2002-01-31Completed
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Crossover, Bioequivalence Study of Carvedilol Tablets USP 12.5 mg With Coreg® 12.5 mg in Normal, Healthy, Adult, Human Subjects Under Fasting Condition. [NCT01577914]Phase 142 participants (Actual)Interventional2011-07-31Completed
A Multicenter, Placebo-Controlled, 8-Month Study of the Effect of Twice Daily Carvedilol in Children With Congestive Heart Failure Due to Systemic Ventricular Systolic Dysfunction [NCT00052026]Phase 3161 participants (Actual)Interventional2000-05-31Completed
A Randomized, Double-Blind, Multicenter Study Comparing the Glycemic Control Characteristics of Carvedilol and Metoprolol in Hypertensive Patients With Type II Diabetes Mellitus. [NCT00060918]Phase 41,210 participants Interventional2001-06-30Completed
The Effects of ß2 Polymorphisms on Beta Selectivity After ß-adrenergic Blockade in Patients With Heart Failure [NCT00214318]25 participants Interventional2005-01-31Completed
Effects of Combined Ventricular Unloading and Pharmacological Therapy on Left Ventricular Metabolic Dysfunction in Heart Failure [NCT00402376]Phase 420 participants (Anticipated)Interventional2007-04-30Terminated
Efficacy of Coreg CR and Lisinopril on Markers for Cardiovascular Functional and Structural Disease. DETECT (DEtection and Treatment of Early Cardiovascular Disease Trial) [NCT00553969]Phase 1/Phase 2101 participants (Actual)Interventional2007-11-30Completed
Effects of Carvedilol on Suppressing the Premature Ventricular Complex/Ventricular Tachycardia From Outflow Tract [NCT03587558]Phase 4104 participants (Anticipated)Interventional2017-09-05Recruiting
Efficacy and Tolerability of Nebivolol Compared With Carvedilol in Patients With Coronary Artery Disease and Stage I or II Hypertension [NCT00673075]Phase 439 participants (Actual)Interventional2008-05-31Completed
Cocaine Withdrawal and Pharmacotherapy Response [NCT00566969]106 participants (Actual)Interventional2007-09-30Completed
Official Title: Spironolactone Combined With Captopril and Carvedilol for the Treatment of Patients With Pulmonary Arterial Hypertension Associated With Congenital Heart Disease-Focus on Pulmonary Artery Remodeling [NCT00240656]Phase 10 participants Interventional2005-10-31Completed
Prospective, Randomized, Controlled Assessment of Once-Daily Controlled Release COREG CR vs Twice-Daily COREG Immediate Release(IR)on Measures of Compliance and Quality of Life in Patients With Heart Failure and Left Ventricular Systolic Dysfunction [NCT00272805]Phase 3400 participants Interventional2005-10-31Completed
Prognostic Value of Ambulatory Blood Pressure Monitoring in the Prediction of Cardiovascular Events and Effects of Chronotherapy in Relation to Risk (the MAPEC Study). [NCT00295542]Phase 43,344 participants (Actual)Interventional2000-03-31Completed
"Effects of Carvedilol on the Cardiovascular and Subjective Response to MDMA (3,4-Methylenedioxymethamphetamine, Ecstasy)" [NCT01270672]16 participants (Actual)Interventional2011-01-31Completed
Rate Control in Atrial Fibrillation [NCT00313157]Phase 380 participants (Actual)Interventional2006-04-30Completed
Evaluation of Effects of Chronic Dose Exposure to Cardioselective and Non-cardioselective Beta Blockers on Measures of Cardiopulmonary Function in Moderate to Severe COPD. [NCT01656005]Phase 418 participants (Actual)Interventional2012-08-31Completed
A Prospective Randomized Controlled Trial Comparing Non-selective Beta Blockers Versus EVL for Primary Prophylaxis of Esophageal Variceal Bleeding in Patients With Hepatocellular Carcinoma With Portal Vein Tumour Thrombosis [NCT01659346]0 participants (Actual)Interventional2016-02-29Withdrawn(stopped due to Due to high mortality)
Effects of Carvedilol and Metoprolol on Endothelial Function in Hypertensive Patients With Type 2 Diabetes Mellitus [NCT00123604]Phase 436 participants (Actual)Interventional2004-06-30Completed
A Randomized, Double-blind, Multi-center, Phase 3 Trial to Evaluate the Efficacy and Safety of Carvedilol SR Versus Carvedilol IR in Patients With Essential Hypertension [NCT01756430]Phase 3238 participants (Actual)Interventional2012-12-31Completed
Effect of Ivabradine, Carvedilol or Their Combination in Patients With Heart Failure [NCT01178528]Phase 3121 participants (Actual)Interventional2009-09-30Completed
Non-Invasive Determination of Central Aortic Blood Pressure in Hypertensive Patients Treated With Controlled-Release Carvedilol or Atenolol [NCT00669279]Phase 441 participants (Actual)Interventional2008-04-30Completed
Pulmonary Artery Catheterization and Carvedilol Early Initiation in Cardiogenic SHOCK Caused by Heart Failure With Reduced Ejection Fraction [NCT06078436]160 participants (Anticipated)Interventional2023-10-31Not yet recruiting
Cardioprotective Benefits of Carvedilol-CR or Valsartan Added to Lisinopril [NCT00657241]Phase 330 participants (Actual)Interventional2008-04-30Completed
Clinical Study of Carvedilol for the Prevention of the Progression of Esophageal Varices in Hepatitis B Related Cirrhotic Patients With Anti-Viral Therapy [NCT03736265]240 participants (Actual)Interventional2017-10-09Active, not recruiting
Carvedilol for Prevention of Paroxysmal Atrial Fibrillation [NCT01608893]300 participants (Anticipated)Interventional2012-05-31Active, not recruiting
Slow-release CArvedilol in Patients With REduced Strain and Preserved Ejection Fraction Heart Failure (CARE-preserved HF): A Prospective Randomized, Double-Blinded, Multicenter Study [NCT05553314]Phase 4100 participants (Anticipated)Interventional2021-11-17Recruiting
Multicentre, Open-label, Non-interventional Observational Clinical Study Lasting 48 Weeks in Patients With Heart Failure or Reduced Left Ventricular Ejection Fraction Following Acute Myocardial Infarction Who Are Treated With Carvedilol [NCT01484327]415 participants (Actual)Observational2009-01-31Completed
A Randomized Trial of Carvedilol After Renin-angiotensin System Inhibition in Chronic Chagas Cardiomyopathy [NCT01557140]Phase 442 participants (Actual)Interventional2003-05-31Completed
A Pilot Study of Treatment of Adults With Sickle Cell Disease Associated Pulmonary Hypertension Based on Hemodynamic Stratification: Safety and Tolerability Study of Imatinib and Carvedilol [NCT01568645]Phase 10 participants (Actual)Interventional2012-03-02Withdrawn
Effect of Carvedilol on Exercise Performance in Fontan Patients [NCT02946892]Phase 426 participants (Actual)Interventional2016-11-30Completed
Pilot Trial of Carvedilol in Alzheimer's Disease [NCT01354444]Phase 429 participants (Actual)Interventional2011-06-30Completed
The CAMERA Study: CArvedilol MEtoprolol Respiratory Assessment Investigator Trial [NCT00384566]Phase 40 participants (Actual)Interventional2005-06-30Withdrawn(stopped due to In order to join forces with another study already running which aims to answer the same question.)
Conditioned Pharmacotherapeutic Effects in Hypertension [NCT02056626]Phase 444 participants (Actual)Interventional2011-03-31Completed
Carvedilol Plus Endoscopic Cyanoacrylate Injection Versus Endoscopic Cyanoacrylate Injection for Secondary Prophylaxis of Gastric Variceal Bleeding [NCT02504723]Phase 4121 participants (Actual)Interventional2011-12-31Completed
Randomized Controlled Trial of Carvedilol Versus Endoscopic Band Ligation for Primary Prophylaxis of Oesophageal Variceal Bleeding in Cirrhotic Patients With Arterial Hypertension [NCT04499898]Phase 2/Phase 3306 participants (Anticipated)Interventional2018-10-01Recruiting
Prospective, Randomized Comparison of Therapy With Verapamil or Carvedilol on Long-Term Outcomes of Patients With Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy [NCT00374465]Phase 4100 participants Interventional2006-01-31Recruiting
Doppler Ultrasound Hepatic Vein Waveform as a Non-invasive Tool in the Assessment of Severity of Portal Hypertension (DPH Trial) [NCT02975323]Phase 350 participants (Anticipated)Interventional2014-12-31Recruiting
Beta-blockers in Pulmonary Arterial Hypertension - A Phase 2 Double-Blind, Placebo-Controlled, Crossover Study Evaluating the Efficacy, and Safety of Carvedilol for Right Ventricular Dysfunction in Pulmonary Arterial Hypertension [NCT02507011]Phase 22 participants (Actual)Interventional2016-01-31Terminated(stopped due to Recruitment)
[NCT02357004]0 participants (Actual)Interventional2015-02-28Withdrawn(stopped due to Change in priority of interventional protocols)
Pulmonary Arterial Hypertension Treatment With Carvedilol for Heart Failure [NCT01586156]30 participants (Actual)Interventional2012-12-31Completed
Carvedilol, Endoscopic Variceal Ligation or Combination of Both for Prevention of First Variceal Bleed in Child's B & C Cirrhosis: A Randomized Controlled Trial [NCT03069339]330 participants (Actual)Interventional2017-03-15Active, not recruiting
A Prospective Randomized Study to Compare the Efficacy and Safety of Carvedilol With or Without Simvastatin in Patients With Portal Hypertension and Esophageal Varices [NCT02465645]220 participants (Actual)Interventional2015-06-01Completed
Clinical Study Evaluating the Gastroprotective Effect of Carvedilol in Patients With Ischemic Heart Disease on Aspirin Therapy [NCT05553717]66 participants (Anticipated)Interventional2022-10-31Not yet recruiting
Endoscopic and Microbiological Assessment of the Effect of Carvedilol Combined With Berberine on GOV in Cirrhosis: a Prospective Cohort Study [NCT04543643]Phase 3288 participants (Anticipated)Interventional2021-11-01Not yet recruiting
Prospective Evaluation of Carvedilol in Prevention of Cardiac Toxicity in Patients With Metastatic HER-2+ Breast Cancer, Phase III [NCT03418961]Phase 3817 participants (Anticipated)Interventional2017-11-01Recruiting
TrAstuzumab Cardiomyopathy Therapeutic Intervention With Carvedilol (TACTIC) Trial [NCT03879629]Phase 2450 participants (Anticipated)Interventional2019-08-21Recruiting
A Four Way Crossover Study in Healthy Volunteers to Evaluate the Application of Stable Isotope Approach to Reduce Number of Subjects Needed for PK Studies [NCT01793870]Phase 117 participants (Actual)Interventional2013-01-15Completed
The Effect of Adrenergic Blocker Therapy on Cardiac and Striatal Transporter Uptake in Pre-Motor and Symptomatic Parkinson's Disease [NCT03775096]Phase 215 participants (Anticipated)Interventional2019-04-04Recruiting
Radiofrequency Ablation for Atrial Fibrillation in Advanced Chronic Heart Failure [NCT00292162]41 participants (Actual)Interventional2007-01-31Completed
Phase II Placebo-controlled Trial of Lisinopril and Coreg CR® to Reduce Cardiotoxicity in Patients With Breast Cancer Receiving (Neo)Adjuvant Chemotherapy With Trastuzumab (Herceptin®) [NCT01009918]Phase 2468 participants (Actual)Interventional2010-03-31Completed
Mechanism of Masked Hypertension - Intervention [NCT04121299]Phase 30 participants (Actual)Interventional2021-07-31Withdrawn(stopped due to lack of funding)
Comparison of the Cardiovascular, Metabolic and Respiratory Effects of Nebivolol and Carvedilol at High Altitude in Healthy Subjects. [NCT00924833]Phase 427 participants (Actual)Interventional2006-05-31Completed
Randomized Open-Label Crossover Trial Comparing Tolerability of a Cardioselective Beta-Blocker (Metoprolol-Succinate-ER) and a Non-Cardioselective Beta-Blocker (Carvedilol) in Patients With Chronic Obstructive Pulmonary Disease [NCT03370835]Phase 421 participants (Actual)Interventional2004-06-30Completed
Carvedilol for the Prevention of Anthracycline/Anti-HER2 Therapy Associated Cardiotoxicity Among Women With HER2-Positive Breast Cancer Using Myocardial Strain Imaging for Early Risk Stratification [NCT02177175]Phase 282 participants (Actual)Interventional2014-06-24Completed
Biomarker Guided Therapies in Stage A/B Heart Failure [NCT02230891]Phase 258 participants (Actual)Interventional2014-10-01Completed
Randomized Controlled Trial on the Effectiveness and Safety of Carvedilol vs. Propranolol Combined With Endoscopic Treatment in Second Prophylaxis of Variceal Bleeding in Cirrhosis [NCT05651789]160 participants (Anticipated)Interventional2023-01-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00000620 (6) [back to overview]First Occurrence of MCE or Revascularization or Hospitalization for Congestive Heart Failure (CHF) in Lipid Trial.
NCT00000620 (6) [back to overview]First Occurrence of a Major Cardiovascular Event (MCE); Specifically Nonfatal Heart Attack, Nonfatal Stroke, or Cardiovascular Death (Measured Throughout the Study) in the Glycemia Trial.
NCT00000620 (6) [back to overview]Death From Any Cause in the Glycemia Trial.
NCT00000620 (6) [back to overview]Stroke in the Blood Pressure Trial.
NCT00000620 (6) [back to overview]First Occurrence of Major Cardiovascular Event (MCE) in the Lipid Trial.
NCT00000620 (6) [back to overview]First Occurrence of Major Cardiovascular Event (MCE) in the Blood Pressure Trial.
NCT00108082 (14) [back to overview]Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed C-Reactive Protein (CRP) at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed B-type Natriuretic Peptide (BNP) at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed Albumin Creatinine Ratio (ACR) at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in LV Mass as Measured by Echocardiography at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed by Height (LVMIH) as Measured by Echocardiography at Month 12
NCT00108082 (14) [back to overview]Mean Change From Baseline in LV Filling Parameters as Measured by MRI at Month 12
NCT00108082 (14) [back to overview]Percentage Change From Baseline in Log Transformed Lipid Parameters at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed (LVMI) by Body Surface Area as Measured by Magnetic Resonance Imaging (MRI) at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed (LVMI) by Body Surface Area as Measured by Echocardiography at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Systolic and Diastolic Blood Pressure (BP) at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in LV End Systolic and Diastolic Volumes and Ejection Fraction as Measured by MRI at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in LV End Systolic and Diastolic Volumes and Ejection Fraction as Measured by Echocardiography at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Left Ventricular (LV) Mass as Measured by MRI at Month 12
NCT00108082 (14) [back to overview]Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed by Height (LVMIH) as Measured by MRI at Month 12
NCT00123604 (1) [back to overview]Flow Mediated Dilation
NCT00273052 (14) [back to overview]Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) Levels by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Hemoglobin A1c (HbA1c) (Glycemic Parameter) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Heart Rate by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Fasting Plasma Glucose (FPG) (Glycemic Parameter) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Additional Lipid Parameters by Treatment Group With Unit of Measures of mg/dL at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in c-Peptide (Glycemic Parameter) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Triglycerides Levels by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Blood Pressure by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Fasting Insulin (Glycemic Parameter) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Additional Lipid Parameters by Treatment Group With Unit of Measures of g/L at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Weight by Treatment Group at Maintenance Month
NCT00273052 (14) [back to overview]Change From Baseline in Log Transformed Lipoprotein-associated Phospholipase A2 (LpPLA2) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Log Transformed High Sensitivity C-reactive Protein (Hs-CRP) by Treatment Group at Maintenance Month 6
NCT00273052 (14) [back to overview]Change From Baseline in Homeostasis Model Assessment (Glycemic Parameter) by Treatment Group at Maintenance Month 6
NCT00292162 (6) [back to overview]Plasma B-type Natriuretic Peptide (BNP) at 6 Months
NCT00292162 (6) [back to overview]Plasma B-type Natriuretic Peptide (BNP) at Baseline
NCT00292162 (6) [back to overview]Baseline Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)
NCT00292162 (6) [back to overview]Change in Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)%
NCT00292162 (6) [back to overview]Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)at 6 Months
NCT00292162 (6) [back to overview]Plasma B-type Natriuretic Peptide (BNP)
NCT00323037 (16) [back to overview]Change From Baseline in Early to Late Atrial Ratio (E:A Ratio)
NCT00323037 (16) [back to overview]Change From Baseline in Deceleration Time
NCT00323037 (16) [back to overview]Change From Baseline in BNP Levels
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular End Diastolic Volume (LVEDV)
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular End Systolic Volume Index (LVESVI) Characterized by 2-D Echocardiography
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular End Diastolic Volume Index (LVEDVI)
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular Ejection Fraction (LVEF)
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular End Systolic Volume (LVESV)
NCT00323037 (16) [back to overview]Incidence of Hospitalizations
NCT00323037 (16) [back to overview]Drug Dose Tolerability
NCT00323037 (16) [back to overview]Safety and Tolerability of Coreg CR
NCT00323037 (16) [back to overview]Change From Baseline in Posterior Wall Thickness (PWT)
NCT00323037 (16) [back to overview]Change From Baseline in Left Ventricular Mass (LVM)
NCT00323037 (16) [back to overview]Change From Baseline in End Diastolic Dimension (EDD)
NCT00323037 (16) [back to overview]Change From Baseline in End Systolic Dimension (ESD)
NCT00323037 (16) [back to overview]Change From Baseline in Intraventricular Septal Thickness (IVST)
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Mean SBP and DBP Measured in Morning by 24 Hour ABPM
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Mean SBP and DBP Measured at Night by 24hr ABPM
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in 24 Hour (hr) Mean Diastolic Blood Pressure
NCT00347360 (11) [back to overview]Dose-response Treatment Estimates: Change From Baseline to Week 6 in 24 Hour Mean DBP by ABPM (Ambulatory Blood Pressure Monitoring)
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Mean SBP and DBP Measured in Afternoon by 24hr ABPM
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Trough to Peak Ratios of DBP by 24 Hour ABPM (Ambulatory Blood Pressure Monitoring)
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Trough Diastolic Blood Pressure
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in 24 Hour Mean Systolic Blood Pressure
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Trough Systolic Blood Pressure
NCT00347360 (11) [back to overview]Change From Baseline to Week 6 in Mean Trough Sitting SBP and Sitting DBP by Cuff Assessment
NCT00347360 (11) [back to overview]Diastolic Responders, Defined as ≥ 10 mmHg Sitting (s)DBP Reduction From Baseline or a sDBP of <90 / 80 Millimeters (mm) of Mercury (Hg) for Non Diabetic / Diabetic Subjects Respectively (Based on Cuff Trough Measures)
NCT00391846 (8) [back to overview]Changes in Health-related Quality of Life
NCT00391846 (8) [back to overview]Changes in Heart Failure Symptoms
NCT00391846 (8) [back to overview]Changes in NT-proBNP Values Over Time in All Patients
NCT00391846 (8) [back to overview]Composite Value of 3 Variables After 9 Months: Cardiovascular Death (Days Alive), Cardiovascular Hospitalization (Days Out of Hospital), Heart Failure Symptoms (Symptom Score Subset of the Kansas City Cardiomyopathy Questionnaire - Questions 3,5,7,9)
NCT00391846 (8) [back to overview]Discontinuations
NCT00391846 (8) [back to overview]Number of CV Deaths
NCT00391846 (8) [back to overview]Number of Days in Hospital for CV Reason
NCT00391846 (8) [back to overview]Total Number of Titration Steps in Prescribed Heart Failure Treatment
NCT00459056 (1) [back to overview]Change in Reactive Hyperemic Index by Period (Carvedilol CR + Lisinopril vs. Lisinopril + HCTZ)
NCT00496834 (4) [back to overview]Pulse Wave Velocity (PWV) Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug
NCT00496834 (4) [back to overview]Diastolic Blood Pressure (DBP) Mean Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug
NCT00496834 (4) [back to overview]Systolic Blood Pressure (SBP) Mean Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug
NCT00496834 (4) [back to overview]PWV Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug
NCT00553969 (1) [back to overview]Change in Disease Score (DS) Among the Treatment Groups
NCT00566969 (1) [back to overview]Percent Days Abstinent From Cocaine - Self Report
NCT00624065 (2) [back to overview]Number of Participants With Mean Sitting Cuff Blood Pressure <140/90 mmHg at the End of 6 Weeks of Treatment
NCT00624065 (2) [back to overview]Mean Change From Baseline in Sitting Systolic Blood Pressure (sSBP) and Sitting Diastolic Blood Pressure (sDBP) at Week 6
NCT00642434 (1) [back to overview]Number of Participants Assessed for Change in Markers of Inflammation (PAI-1) Following Treatment Compared to Baseline
NCT00657241 (6) [back to overview]Stroke Volume (SV)
NCT00657241 (6) [back to overview]Cardiac Output
NCT00657241 (6) [back to overview]Central Systolic Blood Pressure
NCT00657241 (6) [back to overview]Difference in Resting CTTI Between Carvedilol CR (Beta-blocker) and Valsartan (ARB) in Combination With Lisinopril.
NCT00657241 (6) [back to overview]Heart Rate (Beats/Min)
NCT00657241 (6) [back to overview]Systemic Vascular Resistance
NCT00669279 (1) [back to overview]Central Aortic Blood Pressure
NCT00673075 (4) [back to overview]Left Ventricular Ejection Fraction (LVEF) (%) at Week 18
NCT00673075 (4) [back to overview]Peripheral Systolic Blood Pressure (SBP)
NCT00673075 (4) [back to overview]Proportion of Patients With Peripheral SBP <140 mm Hg and DBP <90 mm Hg at Week 18
NCT00673075 (4) [back to overview]Peripheral Diastolic Blood Pressure (DBP)
NCT00742508 (29) [back to overview]Mean Change From Baseline in Alkaline Phosphatase, Alanine Aminotransferase, Aspartate Aminotransferase, Creatine Kinase, and Gamma Glutamyl Transferase at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Calcium, Chloride, Glucose, Potassium, Sodium, and Urea/Blood Urea Nitrogen at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Creatine Kinase BB Percentage, Creatine Kinase MB Percentage, and Creatine Kinase MM Percentage at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Each Type of White Blood Cell (WBC) (Basophils, Eosinophils, Lymphocytes, Monocytes, and Total Neutrophils) at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Hemoglobin and Mean Corpuscular Hemoglobin Concentration at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Platelet Count and White Blood Cell Count at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Weight at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at Week 8
NCT00742508 (29) [back to overview]Mean Plasma Brain Natriuretic Peptide Concentration at Baseline and Week 8
NCT00742508 (29) [back to overview]Number of Participants With Adverse Events by Severity From Week 0 Through Week 8 (CRV-IR) or Week 14 (SK&F-105517-D)
NCT00742508 (29) [back to overview]Number of Participants With the Indicated Change From Baseline New York Heart Association (NYHA) Functional Class at Week 8
NCT00742508 (29) [back to overview]Number of Participants With the Indicated Electrocardiogram Findings at Baseline and Week 8
NCT00742508 (29) [back to overview]Number of Participants With the Indicated Urinalysis Dipstick Results at Baseline and Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Hematocrit at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Heart Rate at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Amylase at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Mean Corpuscular Hemoglobin at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Mean Corpuscular Volume at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Red Blood Cell Count at Week 8
NCT00742508 (29) [back to overview]Adjusted Mean Change From Baseline in Diastolic Blood Pressure at Week 8
NCT00742508 (29) [back to overview]Time of Maximal Plasma Concentration (Tmax) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8
NCT00742508 (29) [back to overview]Adjusted Mean Change From Baseline in Mean Heart Rate at Week 8
NCT00742508 (29) [back to overview]Adjusted Mean Change From Baseline in Systolic Blood Pressure at Week 8
NCT00742508 (29) [back to overview]Area Under the Plasma Concentration Versus Time Curve From Time Zero to 24 Hours (AUC0-24) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8
NCT00742508 (29) [back to overview]Cardiothoracic Ratio at Baseline and Week 8
NCT00742508 (29) [back to overview]Echocardiogram Results: Left Ventricular Ejection Fraction at Baseline and Week 8
NCT00742508 (29) [back to overview]Maximum Plasma Concentration (Cmax) and Trough Plasma Concentration (Cmin) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Albumin and Total Protein at Week 8
NCT00742508 (29) [back to overview]Mean Change From Baseline in Total Bilirubin, Creatinine, and Uric Acid at Week 8
NCT00827775 (4) [back to overview]Endothelial Progenitor Cells
NCT00827775 (4) [back to overview]Endothelial Progenitor Cells
NCT00827775 (4) [back to overview]Flow Mediated Vasodilation
NCT00827775 (4) [back to overview]Flow Mediated Vasodilation
NCT00834795 (3) [back to overview]AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated) - Carvedilol in Plasma
NCT00834795 (3) [back to overview]Cmax - Maximum Observed Concentration - Carvedilol in Plasma
NCT00834795 (3) [back to overview]AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Carvedilol in Plasma
NCT00834873 (3) [back to overview]Cmax - Maximum Observed Concentration - Carvedilol in Plasma
NCT00834873 (3) [back to overview]AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Carvedilol in Plasma
NCT00834873 (3) [back to overview]AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated) - Carvedilol in Plasma
NCT00924833 (4) [back to overview]Peak Exercise Oxygen Consumption
NCT00924833 (4) [back to overview]Delta Peak Exercise Minute Ventilation Time 1 Versus Time 3.
NCT00924833 (4) [back to overview]Delta Peak Exercise Oxygen Consumption Time 1 Versus Time 3
NCT00924833 (4) [back to overview]Peak Exercise Minute Ventilation
NCT00964678 (4) [back to overview]Absolute Change in Right Ventricular Ejection Fraction
NCT00964678 (4) [back to overview]Change in 6 Minute Walk Distance
NCT00964678 (4) [back to overview]Change in Right Ventricular End Systolic Volume
NCT00964678 (4) [back to overview]Change in Tricuspid Annular Plane Systolic Excursion
NCT01009918 (5) [back to overview]Number of Participants With Cardiotoxicity-free Survival at 750 Days From Baseline
NCT01009918 (5) [back to overview]Number of Participants With LVEF Decrease to <50%
NCT01009918 (5) [back to overview]Number of Participants With Trastuzumab-Induced Cardiotoxicity After 52 Weeks of Treatment
NCT01009918 (5) [back to overview]Number of Patients With Trastuzumab Course Interruption
NCT01009918 (5) [back to overview]Quality-of-life Changes Between Baseline and 52-weeks
NCT01171183 (2) [back to overview]Retention
NCT01171183 (2) [back to overview]Urine Toxicology Screens
NCT01178528 (4) [back to overview]Exercise Tolerance Assessed by 6 Minute Walking Test
NCT01178528 (4) [back to overview]Maximal Oxygen Consumption
NCT01178528 (4) [back to overview]New York Heart Association (NYHA) Class
NCT01178528 (4) [back to overview]Quality of Life
NCT01354444 (3) [back to overview]Effect of Carvedilol Treatment in Cerebrospinal Fluid (CSF) Levels of Amyloid-beta Oligomers
NCT01354444 (3) [back to overview]Hopkins Verbal Learning Test (HVLT) Scores at Baseline, 3, and 6 Months
NCT01354444 (3) [back to overview]Effect of Carvedilol Treatment in Cerebrospinal Fluid (CSF) Levels of Amyloid-beta Oligomers
NCT01586156 (7) [back to overview]Beta-Adrenergic Receptor (Alprenolol Binding Assay)
NCT01586156 (7) [back to overview]Cardiac Glucose Uptake in FDG-PET (Fluorodeoxyglucose-Positron Emission Tomography)
NCT01586156 (7) [back to overview]Echocardiogram Left Ventricular Cardiac Output
NCT01586156 (7) [back to overview]Echocardiogram Right Ventricular Systolic Pressure (RVSP)
NCT01586156 (7) [back to overview]NT-proBNP (N-terminal Pro-B Type Natriuretic Peptide)
NCT01586156 (7) [back to overview]Urinary cAMP (Cyclic Adenosine Monophosphate)/Creatinine
NCT01586156 (7) [back to overview]6 Minute Walk Test
NCT01798992 (3) [back to overview]Improvement in Left Ventricular Ejection Fraction (LVEF) at 12 Months
NCT01798992 (3) [back to overview]Improvement in LVEF at 3 Months
NCT01798992 (3) [back to overview]Composite of All-cause Mortality, Need for Heart Transplant or Need for Ventricular Assist Device.
NCT02056626 (3) [back to overview]Mean Systolic Blood Pressure
NCT02056626 (3) [back to overview]Mean Systolic Blood Pressure
NCT02056626 (3) [back to overview]Mean Systolic Blood Pressure
NCT02177175 (4) [back to overview]Maximum Change in LVEF at 12 Months
NCT02177175 (4) [back to overview]Maximum Change in LVEF at 3 Months
NCT02177175 (4) [back to overview]Maximum Change in LVEF at 6 Months
NCT02177175 (4) [back to overview]Maximum Change in LVEF at 9 Months
NCT02230891 (4) [back to overview]Change in Pulse Wave Velocity
NCT02230891 (4) [back to overview]Change in Troponin T Measured Using a High Sensitivity Assay
NCT02230891 (4) [back to overview]Change in Cardiac Global Longitudinal Strain
NCT02230891 (4) [back to overview]Change in NTproBNP (Biomarker)
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Flow-mediated Dilation
NCT02406586 (20) [back to overview]Change in Flow-mediated Dilation
NCT02406586 (20) [back to overview]Change in FFA (Free Fatty Acid) Levels From Baseline to 6 Weeks
NCT02406586 (20) [back to overview]Change in Expression of Inflammatory Biomarker Interleukin-6 (IL-6)
NCT02406586 (20) [back to overview]Change in Expression of Inflammatory Biomarker C-Reactive Protein (CRP)
NCT02406586 (20) [back to overview]Change in Diastolic Blood Pressure From Baseline to 6 Weeks
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure.
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Flow-mediated Dilation
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Systolic Blood Pressure
NCT02406586 (20) [back to overview]Change in Flow-mediated Dilation
NCT02504723 (4) [back to overview]All Cause Mortality or Liver Transplantation
NCT02504723 (4) [back to overview]All Adverse Effects
NCT02504723 (4) [back to overview]Rebleeding From Gastric Varices
NCT02504723 (4) [back to overview]All Upper Gastrointestinal Bleeding
NCT02507011 (1) [back to overview]Mean Change in Right Ventricular Ejection Fraction as Measured by Cardiac MRI
NCT02717507 (20) [back to overview]Average Left Ventricular End-diastolic Dimension
NCT02717507 (20) [back to overview]Average Left Ventricular End-diastolic Dimension
NCT02717507 (20) [back to overview]Average Galectin-3
NCT02717507 (20) [back to overview]Average Fractional Shortening
NCT02717507 (20) [back to overview]Average Ejection Fraction
NCT02717507 (20) [back to overview]Average Cardiac Troponin I
NCT02717507 (20) [back to overview]Average Cardiac N-terminal Pro B-type Natriuretic Peptide
NCT02717507 (20) [back to overview]Average Bilirubin
NCT02717507 (20) [back to overview]"Proportion of Patients Who Responded Moderately, Quite a Bit, or Extremely to How Bothersome the Symptom of DIARRHEA Was at Any Post-day 0 Assessment Time Point."
NCT02717507 (20) [back to overview]Proportion of Patients With Reportable Adverse Events as Described in the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE).
NCT02717507 (20) [back to overview]Proportion of Participants With Average Adherence > 90%
NCT02717507 (20) [back to overview]Average Aspartate Aminotransferase
NCT02717507 (20) [back to overview]Average Alanine Aminotransferase
NCT02717507 (20) [back to overview]Average Peak Early Atrial Divided by Peak Late Atrial Velocities
NCT02717507 (20) [back to overview]Average Left-Ventricular Wall Thickness-Dimension Ratio Z-score (LVWT/Dz)
NCT02717507 (20) [back to overview]Average Left Ventricular Mass
NCT02717507 (20) [back to overview]Average Left Ventricular End-systolic Wall Stress
NCT02717507 (20) [back to overview]Average N-terminal Pro B-type Natriuretic Peptide
NCT02717507 (20) [back to overview]Average Left Ventricular End-systolic Volume
NCT02717507 (20) [back to overview]Average Left Ventricular End-systolic Volume
NCT02946892 (3) [back to overview]Change in Peak Heart Rate
NCT02946892 (3) [back to overview]Change in Oxygen Uptake at Anaerobic Threshold
NCT02946892 (3) [back to overview]Change in Peak Oxygen Uptake From Baseline Peak Oxygen Uptake
NCT04767061 (10) [back to overview]Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)
NCT04767061 (10) [back to overview]Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device
NCT04767061 (10) [back to overview]Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)
NCT04767061 (10) [back to overview]Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)
NCT04767061 (10) [back to overview]Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)

First Occurrence of MCE or Revascularization or Hospitalization for Congestive Heart Failure (CHF) in Lipid Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, cardiovascular death, revascularization procedure or hospitalization for CHF in Lipid Trial participants. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
Lipid Trial: Fenofibrate641
Lipid Trial: Placebo667

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First Occurrence of a Major Cardiovascular Event (MCE); Specifically Nonfatal Heart Attack, Nonfatal Stroke, or Cardiovascular Death (Measured Throughout the Study) in the Glycemia Trial.

"Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death. This was the primary outcome measure in all three trials: Glycemia (all participants), Blood Pressure (subgroup of participants not in Lipid Trial), and Lipid (subgroup of participants not in Blood Pressure Trial).~In the Glycemia Trial, a finding of higher mortality in the intensive arm group led to an early discontinuation of therapy after a mean of 3.5 years of follow-up. Intensive arm participants were transitioned to standard arm strategy over a period of 0.2 year and followed for an additional 1.2 years to the planned end of the Glycemia Trial while participating in one of the other sub-trials (BP or Lipid) to their planned completion." (NCT00000620)
Timeframe: 4.9 years

Interventionparticipants (Number)
Glycemia Trial: Intensive Control503
Glycemia Trial: Standard Control543

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Death From Any Cause in the Glycemia Trial.

"Time to death from any cause. Secondary measure for Glycemia Trial.~A finding of higher mortality in the intensive-therapy group led to an early discontinuation of therapy after a mean of 3.5 years of follow-up. Intensive arm participants were transitioned to standard arm strategy over a period of 0.2 year and followed for an additional 1.2 years to the planned end of the Glycemia Trial while participating in one of the other sub-trials (BP or Lipid)." (NCT00000620)
Timeframe: 4.9 years

Interventionparticipants (Number)
Glycemia Trial: Intensive Control391
Glycemia Trial: Standard Control327

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Stroke in the Blood Pressure Trial.

Time to first occurrence of nonfatal or fatal stroke among participants in the BP Trial. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
BP Trial: Intensive Control36
BP Trial: Standard Control62

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First Occurrence of Major Cardiovascular Event (MCE) in the Lipid Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death in Lipid Trial participants. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
Lipid Trial: Fenofibrate291
Lipid Trial: Placebo310

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First Occurrence of Major Cardiovascular Event (MCE) in the Blood Pressure Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death. Primary outcome for Blood Pressure Trial. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
BP Trial: Intensive Control208
BP Trial: Standard Control237

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Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed C-Reactive Protein (CRP) at Month 12

CRP concentration (milligrams per deciliter) was measured at Baseline and after 12 months of treatment/Month 12. Percentage change from Baseline was based on log transformed data and calculated as 100 x (exponent (mean change on log scale) - 1). [Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value.] (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF was used)

Interventionpercentage of change (Geometric Mean)
Carvedilol CR-10.63
Atenolol-3.22
Lisinopril2.70

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Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed B-type Natriuretic Peptide (BNP) at Month 12

BNP concentration (picagram per milliter) was measured at Baseline and after 12 months of treatment/Month 12. Percentage change from Baseline was based on log transformed data and was calculated as 100 x (exponent (mean change on log scale) -1) [Change is the Month 12 value (or value after 12 months of treatment) minus the Baseline value]. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF was used

Interventionpercentage of change (Geometric Mean)
Carvedilol CR51.7
Atenolol48.3
Lisinopril-39.1

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Model-adjusted Ratio to Baseline as Percentage Change From Baseline in Log Transformed Albumin Creatinine Ratio (ACR) at Month 12

Urinary ACR (micrograms per milligram) was determined at Baseline and after 12 months of treatment/Month 12. Percentage change from Baseline was based on log transformed data and was calculated as 100 x (exponent (exponent (mean change on log scale) - 1. [Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value.] (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF was used)

Interventionpercentage of change (Geometric Mean)
Carvedilol CR-27.1
Atenolol-20.1
Lisinopril-21.5

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Model-adjusted Mean Change From Baseline in LV Mass as Measured by Echocardiography at Month 12

LV Mass was measured by echocardiography at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

Interventiongrams (Mean)
Carvedilol CR-45.76
Atenolol-40.56
Lisinopril-38.58

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Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed by Height (LVMIH) as Measured by Echocardiography at Month 12

LVMIH was measured by echogradiography at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was available)

Interventiong/m raised to 2.7 (g/(m^2.7)) (Mean)
Carvedilol CR-11.78
Atenolol-12.51
Lisinopril-11.61

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Mean Change From Baseline in LV Filling Parameters as Measured by MRI at Month 12

LV filling parameters, LV E-Volume and LV A-Volume, were measured by MRI at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. These filling parameters represent the volumes of blood filling the ventricle during the passive filling phase (E-volume) and the active filling phase caused by atrial contraction (A-volume). (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

,,
Interventionmilliliters (mL) (Mean)
LV E-volumeLV A-volume
Atenolol6.763-0.565
Carvedilol CR0.364-0.513
Lisinopril-3.4061.088

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Percentage Change From Baseline in Log Transformed Lipid Parameters at Month 12

Plasma lipid concentrations (milligrams per deciliter) were measured at Baseline and after 12 months of treatment/Month 12. Percentage change from Baseline was based on log transformed data and calculated as 100 x (exponent(mean change on log scale) - 1). [Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value.] (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF was used)

,,
Interventionpercentage of change (Geometric Mean)
Total cholesterolLow-density lipid cholesterolHigh-density lipid cholesterolTriglycerides
Atenolol-1.3-4.0-4.77.1
Carvedilol CR0.70.0-4.311.0
Lisinopril-1.7-2.7-1.56.2

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Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed (LVMI) by Body Surface Area as Measured by Magnetic Resonance Imaging (MRI) at Month 12

LVMI was measured by MRI at Baseline and after 12 months of treatment/Month 12. A reduction in left ventricular mass, calculated as LVMI, of 5 g/m^2 was assumed to be clinically meaningful. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the Last Observation Carried Forward [LOCF] analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

Interventiongrams per meters squared (g/m^2) (Mean)
Carvedilol CR-6.34
Atenolol-6.67
Lisinopril-7.94

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Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed (LVMI) by Body Surface Area as Measured by Echocardiography at Month 12

LVMI was measured by echogradiography at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

Interventiongrams per meters squared (g/m^2) (Mean)
Carvedilol CR-20.35
Atenolol-20.06
Lisinopril-18.48

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Model-adjusted Mean Change From Baseline in Systolic and Diastolic Blood Pressure (BP) at Month 12

Systolic and Diastolic BP were measured at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

,,
InterventionmmHg (millimeters of mercury) (Mean)
Systolic blood pressureDiastolic blood pressure
Atenolol-21.12-14.05
Carvedilol CR-21.32-12.77
Lisinopril-22.53-11.13

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Model-adjusted Mean Change From Baseline in LV End Systolic and Diastolic Volumes and Ejection Fraction as Measured by MRI at Month 12

LV End Systolic and Diastolic Volumes and Ejection Fraction were measured by MRI at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. The ejection fraction is the fraction of the blood volume available at the end of diastole that is pumped out of the ventricules during systole. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

,,
Interventionmilliliters (mL) (Mean)
LV End Systolic VolumeLV End Diastolic VolumeLV Ejection Fraction
Atenolol-4.29-2.452.16
Carvedilol CR-1.44-2.860.08
Lisinopril-3.04-7.45-0.01

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Model-adjusted Mean Change From Baseline in LV End Systolic and Diastolic Volumes and Ejection Fraction as Measured by Echocardiography at Month 12

LV End Systolic and Diastolic Volumes and Ejection Fraction were measured by echocardiography at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

,,
Interventionmilliliters (mL) (Mean)
LV End Systolic VolumeLV End Diastolic VolumeLV Ejection Fraction
Atenolol-4.74-3.642.33
Carvedilol CR-3.38-3.071.03
Lisinopril-5.34-9.370.63

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Model-adjusted Mean Change From Baseline in Left Ventricular (LV) Mass as Measured by MRI at Month 12

LV Mass was measured by MRI at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

Interventiongrams (g) (Mean)
Carvedilol CR-13.74
Atenolol-14.17
Lisinopril-17.17

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Model-adjusted Mean Change From Baseline in Left Ventricular Mass Indexed by Height (LVMIH) as Measured by MRI at Month 12

LVMIH was measured by MRI at Baseline and after 12 months of treatment/Month 12. Change in Baseline was calculated as Month 12 value (or value after 12 months of treatment) minus the Baseline value. LV mass depends on body size. One method of determining whether an individual has LV hypertrophy relates LV mass to height raised to a power of 2.7. (NCT00108082)
Timeframe: Baseline and Month 12 (If Month 12 data were not available, the LOCF analysis, which includes data collected on or after Month 9 of treatment to Month 12 of treatment, was used)

Interventiong/m raised to 2.7 (g/(m^2.7)) (Mean)
Carvedilol CR-3.19
Atenolol-3.37
Lisinopril-3.98

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Flow Mediated Dilation

Flow mediated dilation is a measure of endothelial function. It is measured by the percent change in artery diameter (i.e. dilation), pre and post manual artery occlusion. (NCT00123604)
Timeframe: change from baseline to 5 months

Interventionpercentage of change in dilation (Mean)
Carvedilol6.2
Metoprolol4.1

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Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C) Levels by Treatment Group at Maintenance Month 6

Blood draw for HDL-C levels. Full beta Quant test performed with HDL subclasses. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionmg/dL (Number)
Coreg CR-4.4
Toprol XL-5.1

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Change From Baseline in Hemoglobin A1c (HbA1c) (Glycemic Parameter) by Treatment Group at Maintenance Month 6

Blood draw for glycemia levels. Full beta Quant test performed. Test for Fasting plasma glucose, HbA1c, fasting insulin. Homeostasis model Assessment (HOMA) is a computer-generated model consisting of non-linear empirical equations solved numerically to predict glucose, Insulin and C-peptide concentrations in fasting subjects for insulin sensitivity (%S). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

InterventionPercent Change (Number)
Coreg CR0.01
Toprol XL0.04

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Change From Baseline in Heart Rate by Treatment Group at Maintenance Month 6

Manual physical examination. Change = Month 6 value minus Baseline value. (BPM=beats per minute) (NCT00273052)
Timeframe: Baseline and Month 6

Interventionbpm (Number)
Coreg CR-5.98
Toprol XL-6.07

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Change From Baseline in Fasting Plasma Glucose (FPG) (Glycemic Parameter) by Treatment Group at Maintenance Month 6

Blood draw for glycemia levels. Full beta Quant test performed. Test for Fasting plasma glucose, HbA1c, fasting insulin. Homeostasis model Assessment (HOMA) is a computer-generated model consisting of non-linear empirical equations solved numerically to predict glucose, Insulin and C-peptide concentrations in fasting subjects for insulin sensitivity (%S). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionmg/dL (Number)
Coreg CR0.94
Toprol XL1.20

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Change From Baseline in Additional Lipid Parameters by Treatment Group With Unit of Measures of mg/dL at Maintenance Month 6

Blood draw for lipid levels. Full beta Quant test performed with HDL subclasses and IDL. IDL=Intermediate density lipoproteins, LDL=Low-density lipoprotein, VLDL=Very Low density lipoprotein, HDL=High-density lipoprotein. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

,
Interventionmg/dL (Number)
Total Serum CholesterolLow-Density Lipoprotein (LDL)Low+Very Low Density LipoproteinHigh-Density Lipoprotein 2 (HDL2)High-Density Lipoprotein 3 (HDL3)Low-Density Lipoprotein-Relative FlotationIntermediate Density Lipoproteins+VLDL
Coreg CR0.1-1.10.9-1.45-4.00.1662.0
Toprol XL-0.7-1.70.4-6.5-3.5-1.3605.6

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Change From Baseline in c-Peptide (Glycemic Parameter) by Treatment Group at Maintenance Month 6

Blood draw for glycemia levels. Full beta Quant test performed. Test for Fasting plasma glucose, HbA1c, fasting insulin. Homeostasis model Assessment (HOMA) is a computer-generated model consisting of non-linear empirical equations solved numerically to predict glucose, Insulin and C-peptide concentrations in fasting subjects for insulin sensitivity (%S). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionng/mL (Number)
Coreg CR-0.23
Toprol XL0.20

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Change From Baseline in Triglycerides Levels by Treatment Group at Maintenance Month 6

Blood draw for triglyceride levels. Full beta quantification test performed which uses ultracentrifugation to partially separate lipoprotein classes and is the basis for the reference methods. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionmg/dL (Number)
Coreg CR2.65
Toprol XL10.39

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Change From Baseline in Blood Pressure by Treatment Group at Maintenance Month 6

Manual physical examination (cuff blood pressure). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

,
Interventionmm Hg (Number)
Systolic Blood PressureDiastolic Blood Pressure
Coreg CR-15.90-10.89
Toprol XL-16.23-11.06

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Change From Baseline in Fasting Insulin (Glycemic Parameter) by Treatment Group at Maintenance Month 6

Blood draw for glycemia levels. Full beta Quant test performed. Test for Fasting plasma glucose, HbA1c, fasting insulin. Homeostasis model Assessment (HOMA) is a computer-generated model consisting of non-linear empirical equations solved numerically to predict glucose, Insulin and C-peptide concentrations in fasting subjects for insulin sensitivity (%S). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

InterventionuIU/mL (Number)
Coreg CR-1.21
Toprol XL1.35

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Change From Baseline in Additional Lipid Parameters by Treatment Group With Unit of Measures of g/L at Maintenance Month 6

Blood draw for lipid levels. Full beta Quant test performed. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

,
Interventiong/L (Number)
Apolipoprotein A-1 (Apo-A1)Apolipoprotein B (Apo-B)
Coreg CR-1.82-1.16
Toprol XL-3.450.81

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Change From Baseline in Weight by Treatment Group at Maintenance Month

Manual physical examination. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionkg (Number)
Coreg CR1.01
Toprol XL0.73

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Change From Baseline in Log Transformed Lipoprotein-associated Phospholipase A2 (LpPLA2) by Treatment Group at Maintenance Month 6

Blood draw for LpPLA2 activity. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionmcmol/min/L (Number)
Coreg CR-2.38
Toprol XL-2.23

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Change From Baseline in Log Transformed High Sensitivity C-reactive Protein (Hs-CRP) by Treatment Group at Maintenance Month 6

Blood draw for hs-CRP. Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

Interventionmg/dL (Number)
Coreg CR-1.76
Toprol XL0.49

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Change From Baseline in Homeostasis Model Assessment (Glycemic Parameter) by Treatment Group at Maintenance Month 6

Blood draw for glycemia levels. Full beta Quant test performed. Test for Fasting plasma glucose, HbA1c, fasting insulin. Homeostasis model Assessment (HOMA) is a computer-generated model consisting of non-linear empirical equations solved numerically to predict glucose, Insulin and C-peptide concentrations in fasting subjects for insulin sensitivity (%S). Change = Month 6 value minus Baseline value. (NCT00273052)
Timeframe: Baseline and Month 6

InterventionPercent Change (Number)
Coreg CR2.05
Toprol XL-4.14

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Plasma B-type Natriuretic Peptide (BNP) at 6 Months

Plasma B-type Natriuretic Peptide (BNP) (NCT00292162)
Timeframe: 6 months

Interventionpicograms per millilitre (Mean)
Medical Therapy1931
Radiofrequency Ablation2354

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Plasma B-type Natriuretic Peptide (BNP) at Baseline

Plasma B-type Natriuretic Peptide (BNP) measured at basline (NCT00292162)
Timeframe: Baseline

Interventionpicograms per millilitre (Mean)
Medical Therapy1846
Radiofrequency Ablation2550

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Baseline Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)

Baseline Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)in % (NCT00292162)
Timeframe: Baseline

Interventionpercentage of blood ejected in one beat (Mean)
Medical Therapy43
Radiofrequency Ablation36

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Change in Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)%

left ventricular ejection fraction (LVEF) is a measure of the % of blood ejected from the ventricle in one heart beat. It is a measure of cardiac function. We measured LVEF at baseline and at 6 months, to assess whether there had been a change in the patients cardiac function over time. (NCT00292162)
Timeframe: baseline and 6 months

Interventionpercentage of blood ejected in one beat (Mean)
Medical Therapy2.8
Radiofrequency Ablation4.5

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Left Ventricular Ejection Fraction by Magnetic Resonance Imaging (MRI)at 6 Months

Left Ventricular Ejection Fraction as measured by Magnetic Resonance Imaging (MRI)at 6 months (NCT00292162)
Timeframe: 6 months

Interventionpercentage of blood ejected in one beat (Mean)
Medical Therapy46
Radiofrequency Ablation41

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Plasma B-type Natriuretic Peptide (BNP)

venous blood taken to assess levels of the above peptide. High evels of the peptide are associated with adverse prognosis. Blood levels are taken at baseline and 6 months. The change over 6 months is assessed, thereore it is possible to have a negative number if the level falls. (NCT00292162)
Timeframe: baseline and 6 months

Interventionpicograms per millilitre (Mean)
Medical Therapy85
Radiofrequency Ablation-196

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Change From Baseline in Early to Late Atrial Ratio (E:A Ratio)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-0.20
Carvedilol Controlled Release-0.45

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Change From Baseline in Deceleration Time

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release24.00
Carvedilol Controlled Release53.37

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Change From Baseline in BNP Levels

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-0.88
Carvedilol Controlled Release-0.86

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Change From Baseline in Left Ventricular End Diastolic Volume (LVEDV)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-36.61
Carvedilol Controlled Release-42.22

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Change From Baseline in Left Ventricular End Systolic Volume Index (LVESVI) Characterized by 2-D Echocardiography

Maintenance Visit 3 minus Baseline. Maintenance Visit 3 occurred 24 weeks after entry into the maintenance period. The maintenance period started after completion of a titration period of variable duration. (NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

InterventionmL/m^2 (Mean)
Coreg Immediate Release-18.36
Coreg Controlled Release-20.81

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Change From Baseline in Left Ventricular End Diastolic Volume Index (LVEDVI)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-18.29
Carvedilol Controlled Release-20.57

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Change From Baseline in Left Ventricular Ejection Fraction (LVEF)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release.08
Carvedilol Controlled Release.08

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Change From Baseline in Left Ventricular End Systolic Volume (LVESV)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-36.61
Carvedilol Controlled Release-43.00

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Incidence of Hospitalizations

(NCT00323037)
Timeframe: Up to 32 weeks (titration and maintenance phases)

,
Interventionparticipants in each treatment group (Number)
Hospitalization for Heart FailureHospitalization Due to Any CauseHospitalization or Death
Carvedilol Controlled Release62929
Carvedilol Immediate Release63132

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Drug Dose Tolerability

(NCT00323037)
Timeframe: Up to 32 weeks (titration and maintenance phases)

,
Interventionsubjects in each treatment group (Number)
Study Entry (10mg Coreg CR, 3.125mg Coreg IR)Maintenance Entry (10mg Coreg CR, 3.125mg Coreg IR)End of Study (10mg Coreg CR, 3.125mg Coreg IR)Study Entry (20mg Coreg CR, 6.25mg Coreg IR)Maintenance Entry (20mg Coreg CR, 6.25mg Coreg IR)End of Study (20mg Coreg CR, 6.25mg Coreg IR)Study Entry (40mg Coreg CR, 12.5mg Coreg IR)Maintenance Entry (40mg Coreg CR, 12.5mg Coreg IR)End of Study (40mg Coreg CR, 12.5mg Coreg IR)Study Entry (80mg Coreg CR, 25mg Coreg IR)Maintenance Entry (80mg Coreg CR, 25mg Coreg IR)End of Study (80mg Coreg CR, 25mg Coreg IR)
Carvedilol Controlled Release8304399162716224114111
Carvedilol Immediate Release79076113162112214116121

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Safety and Tolerability of Coreg CR

SAEs experienced (NCT00323037)
Timeframe: 24 weeks after entry into the maintenance phase (after unblinding)

Interventionnumber of SAEs (Number)
Carvedilol Immediate Release40
Carvedilol Controlled Release35

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Change From Baseline in Posterior Wall Thickness (PWT)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release.07
Carvedilol Controlled Release.05

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Change From Baseline in Left Ventricular Mass (LVM)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release9.5
Carvedilol Controlled Release-9.29

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Change From Baseline in End Diastolic Dimension (EDD)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-0.33
Carvedilol Controlled Release-0.36

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Change From Baseline in End Systolic Dimension (ESD)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release-0.76
Carvedilol Controlled Release-0.83

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Change From Baseline in Intraventricular Septal Thickness (IVST)

(NCT00323037)
Timeframe: 24 weeks after entry into the maintenance period

Interventionpercentage of change (Mean)
Carvedilol Immediate Release.08
Carvedilol Controlled Release.05

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Change From Baseline to Week 6 in Mean SBP and DBP Measured in Morning by 24 Hour ABPM

Mean changes from Baseline to Week 6 in DBP and SBP measured by 24hr ABPM at the end of up-titration recorded in the morning. The morning assessment period started at or after 6 am and ended immediately before 12 noon. (NCT00347360)
Timeframe: Morning BP, Baseline, Week 6

,,,,,,,,,,,,,,
InterventionmmHg (Mean)
Change in Morning SBP from Baseline to Week 6Change in Morning DBP from Baseline to Week 6
Carvedilol Controlled Release 20-6.23-5.01
Carvedilol Controlled Release 20 Lisinopril 10-13.89-9.21
Carvedilol Controlled Release 20 Lisinopril 20-10.22-7.86
Carvedilol Controlled Release 20 Lisinopril 40-14.50-10.04
Carvedilol Controlled Release 40-10.42-6.82
Carvedilol Controlled Release 40 Lisinopril 10-12.78-8.79
Carvedilol Controlled Release 40 Lisinopril 20-14.29-11.15
Carvedilol Controlled Release 40 Lisinopril 40-14.84-9.96
Carvedilol Controlled Release 80-13.70-7.53
Carvedilol Controlled Release 80 Lisinopril 10-17.09-11.95
Carvedilol Controlled Release 80 Lisinopril 20-14.52-10.71
Carvedilol Controlled Release 80 Lisinopril 40-17.12-12.46
Lisinopril 10-9.37-6.12
Lisinopril 20-14.53-9.20
Lisinopril 40-10.76-7.62

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Change From Baseline to Week 6 in Mean SBP and DBP Measured at Night by 24hr ABPM

Mean changes from Baseline to Week 6 in DBP and SBP measured by 24hr ABPM at the end of up-titration recorded in the night. The night-time assessment period started at the time of the first reading at or after 6 pm and ended immediately before 6 am on the following day. (NCT00347360)
Timeframe: Night BP, Baseline, Week 6

,,,,,,,,,,,,,,
InterventionmmHg (Mean)
Change in Night SBP from Baseline to Week 6Change in Night DBP from Baseline to Week 6
Carvedilol Controlled Release 20-4.28-3.20
Carvedilol Controlled Release 20 Lisinopril 10-10.37-8.11
Carvedilol Controlled Release 20 Lisinopril 20-9.94-7.03
Carvedilol Controlled Release 20 Lisinopril 40-12.64-9.36
Carvedilol Controlled Release 40-7.70-6.49
Carvedilol Controlled Release 40 Lisinopril 10-10.02-8.23
Carvedilol Controlled Release 40 Lisinopril 20-11.87-9.34
Carvedilol Controlled Release 40 Lisinopril 40-11.25-9.09
Carvedilol Controlled Release 80-7.71-5.34
Carvedilol Controlled Release 80 Lisinopril 10-12.08-8.27
Carvedilol Controlled Release 80 Lisinopril 20-14.12-9.88
Carvedilol Controlled Release 80 Lisinopril 40-13.06-10.14
Lisinopril 10-9.01-5.83
Lisinopril 20-11.58-6.78
Lisinopril 40-10.38-7.49

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Change From Baseline to Week 6 in 24 Hour (hr) Mean Diastolic Blood Pressure

Ambulatory blood pressure monitoring (ABPM) was completed at Baseline and at the end of treatment/Week 6 or early withdrawal by standard electronic ABPM equipment worn by the subject for 24-hr of ambulatory activity. The 24 hr assessment period started at the time of the first reading and ended exactly 24 hr later on the following day. Data collected included mean diastolic blood pressure (DBP). (NCT00347360)
Timeframe: Baseline, Week 6.

InterventionmmHg (Mean)
Lisinopril 10-5.79
Lisinopril 20-8.11
Lisinopril 40-7.37
Carvedilol Controlled Release 20-4.40
Carvedilol Controlled Release 40-7.61
Carvedilol Controlled Release 80-6.52
Carvedilol Controlled Release 20 Lisinopril 10-9.29
Carvedilol Controlled Release 20 Lisinopril 20-8.57
Carvedilol Controlled Release 20 Lisinopril 40-10.19
Carvedilol Controlled Release 40 Lisinopril 10-9.36
Carvedilol Controlled Release 40 Lisinopril 20-10.96
Carvedilol Controlled Release 40 Lisinopril 40-10.37
Carvedilol Controlled Release 80 Lisinopril 10-10.93
Carvedilol Controlled Release 80 Lisinopril 20-11.09
Carvedilol Controlled Release 80 Lisinopril 40-11.92

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Dose-response Treatment Estimates: Change From Baseline to Week 6 in 24 Hour Mean DBP by ABPM (Ambulatory Blood Pressure Monitoring)

Evaluation of the dose-response relationship between incremental doses of carvedilol CR and lisinopril and mean 24-hr ABPM DBP. (NCT00347360)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
Lisinopril 10-5.77
Lisinopril 20-7.55
Lisinopril 40-7.49
Carvedilol Controlled Release 20-5.11
Carvedilol Controlled Release 40-6.61
Carvedilol Controlled Release 80-7.13
Carvedilol Controlled Release 20 Lisinopril 10-8.08
Carvedilol Controlled Release 20 Lisinopril 20-9.83
Carvedilol Controlled Release 20 Lisinopril 40-9.71
Carvedilol Controlled Release 40 Lisinopril 10-9.55
Carvedilol Controlled Release 40 Lisinopril 20-11.3
Carvedilol Controlled Release 40 Lisinopril 40-11.1
Carvedilol Controlled Release 80 Lisinopril 10-10.0
Carvedilol Controlled Release 80 Lisinopril 20-11.7
Carvedilol Controlled Release 80 Lisinopril 40-11.4

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Change From Baseline to Week 6 in Mean SBP and DBP Measured in Afternoon by 24hr ABPM

Mean changes from Baseline to Week 6 in SBP and DBP measured by 24hr ABPM at the end of up-titration recorded in the afternoon. The afternoon assessment period started at or after 12 noon and ended immediately before 6 pm. (NCT00347360)
Timeframe: Afternoon BP, Baseline, Week 6

,,,,,,,,,,,,,,
InterventionmmHg (Mean)
Change in Afternoon SBP from Baseline to Week 6Change in Afternoon DBP from Baseline to Week 6
Carvedilol Controlled Release 20-9.69-6.27
Carvedilol Controlled Release 20 Lisinopril 10-13.96-11.28
Carvedilol Controlled Release 20 Lisinopril 20-15.54-12.04
Carvedilol Controlled Release 20 Lisinopril 40-16.38-11.59
Carvedilol Controlled Release 40-13.34-10.12
Carvedilol Controlled Release 40 Lisinopril 10-14.51-12.18
Carvedilol Controlled Release 40 Lisinopril 20-17.97-14.03
Carvedilol Controlled Release 40 Lisinopril 40-17.82-12.54
Carvedilol Controlled Release 80-13.76-8.38
Carvedilol Controlled Release 80 Lisinopril 10-20.91-15.12
Carvedilol Controlled Release 80 Lisinopril 20-20.46-13.87
Carvedilol Controlled Release 80 Lisinopril 40-19.36-15.02
Lisinopril 10-9.68-5.62
Lisinopril 20-17.21-10.25
Lisinopril 40-10.53-6.67

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Change From Baseline to Week 6 in Trough to Peak Ratios of DBP by 24 Hour ABPM (Ambulatory Blood Pressure Monitoring)

Trough (20-24 hr) to peak (3-7 hr) ratios of DBP were examined in order to evaluate the extent to which once-daily criteria were met (ie trough:peak > 50%). Trough to peak ratios were calculated from change trough mean/change peak mean x 100. (NCT00347360)
Timeframe: Baseline, Week 6

Interventiontrough:peak ratio x 100% (Number)
Lisinopril 10133.33
Lisinopril 2061.04
Lisinopril 40114.45
Carvedilol Controlled Release 2034.11
Carvedilol Controlled Release 4071.00
Carvedilol Controlled Release 8049.67
Carvedilol Controlled Release 20 Lisinopril 1044.50
Carvedilol Controlled Release 20 Lisinopril 2049.46
Carvedilol Controlled Release 20 Lisinopril 4059.47
Carvedilol Controlled Release 40 Lisinopril 1054.71
Carvedilol Controlled Release 40 Lisinopril 2052.86
Carvedilol Controlled Release 40 Lisinopril 4037.93
Carvedilol Controlled Release 80 Lisinopril 1041.95
Carvedilol Controlled Release 80 Lisinopril 2053.54
Carvedilol Controlled Release 80 Lisinopril 4052.07

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Change From Baseline to Week 6 in Trough Diastolic Blood Pressure

Trough ABPM was the average across 20-24 hr after dosing for each subject. (NCT00347360)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
Lisinopril 10-6.40
Lisinopril 20-6.08
Lisinopril 40-8.16
Carvedilol Controlled Release 20-2.34
Carvedilol Controlled Release 40-7.76
Carvedilol Controlled Release 80-5.26
Carvedilol Controlled Release 20 Lisinopril 10-5.14
Carvedilol Controlled Release 20 Lisinopril 20-6.36
Carvedilol Controlled Release 20 Lisinopril 40-7.22
Carvedilol Controlled Release 40 Lisinopril 10-6.79
Carvedilol Controlled Release 40 Lisinopril 20-7.76
Carvedilol Controlled Release 40 Lisinopril 40-4.90
Carvedilol Controlled Release 80 Lisinopril 10-6.54
Carvedilol Controlled Release 80 Lisinopril 20-7.26
Carvedilol Controlled Release 80 Lisinopril 40-8.42

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Change From Baseline to Week 6 in 24 Hour Mean Systolic Blood Pressure

Ambulatory blood pressure monitoring (ABPM) was completed at Baseline and at the end of treatment/Week 6 or early withdrawal by standard electronic ABPM equipment worn by the subject for 24-hr of ambulatory activity. The 24 hr assessment period started at the time of the first reading and ended exactly 24 hr later on the following day. Data collected included mean systolic blood pressure (SBP). (NCT00347360)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
Lisinopril 10-9.19
Lisinopril 20-13.58
Lisinopril 40-10.60
Carvedilol Controlled Release 20-6.15
Carvedilol Controlled Release 40-9.84
Carvedilol Controlled Release 80-10.38
Carvedilol Controlled Release 20 Lisinopril 10-12.06
Carvedilol Controlled Release 20 Lisinopril 20-11.58
Carvedilol Controlled Release 20 Lisinopril 40-14.16
Carvedilol Controlled Release 40 Lisinopril 10-11.68
Carvedilol Controlled Release 40 Lisinopril 20-14.03
Carvedilol Controlled Release 40 Lisinopril 40-13.90
Carvedilol Controlled Release 80 Lisinopril 10-15.60
Carvedilol Controlled Release 80 Lisinopril 20-15.93
Carvedilol Controlled Release 80 Lisinopril 40-15.59

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Change From Baseline to Week 6 in Trough Systolic Blood Pressure

Trough ABPM was the average across 20-24 hr after dosing for each subject. (NCT00347360)
Timeframe: Baseline, Week 6

InterventionmmHg (Mean)
Lisinopril 10-9.47
Lisinopril 20-7.52
Lisinopril 40-9.54
Carvedilol Controlled Release 20-0.96
Carvedilol Controlled Release 40-9.27
Carvedilol Controlled Release 80-5.68
Carvedilol Controlled Release 20 Lisinopril 10-6.44
Carvedilol Controlled Release 20 Lisinopril 20-9.27
Carvedilol Controlled Release 20 Lisinopril 40-9.88
Carvedilol Controlled Release 40 Lisinopril 10-8.87
Carvedilol Controlled Release 40 Lisinopril 20-8.11
Carvedilol Controlled Release 40 Lisinopril 40-5.82
Carvedilol Controlled Release 80 Lisinopril 10-9.80
Carvedilol Controlled Release 80 Lisinopril 20-10.74
Carvedilol Controlled Release 80 Lisinopril 40-10.00

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Change From Baseline to Week 6 in Mean Trough Sitting SBP and Sitting DBP by Cuff Assessment

Analysis of Change from Baseline to Week 6 in Mean sSBP and sDBP by Cuff Assessments at Drug Trough (20-24 hr) at End of Treatment Titration (NCT00347360)
Timeframe: Baseline, Week 6

,,,,,,,,,,,,,,
InterventionmmHg (Mean)
Change in sSBP by Cuff from Baseline to Week 6Change in sDBP by Cuff from Baseline to Week 6
Carvedilol Controlled Release 20-5.68-6.87
Carvedilol Controlled Release 20 Lisinopril 10-9.54-5.66
Carvedilol Controlled Release 20 Lisinopril 20-11.84-10.02
Carvedilol Controlled Release 20 Lisinopril 40-13.43-10.28
Carvedilol Controlled Release 40-5.07-5.70
Carvedilol Controlled Release 40 Lisinopril 10-9.79-8.73
Carvedilol Controlled Release 40 Lisinopril 20-11.26-10.89
Carvedilol Controlled Release 40 Lisinopril 40-13.49-9.63
Carvedilol Controlled Release 80-8.88-7.54
Carvedilol Controlled Release 80 Lisinopril 10-6.42-8.22
Carvedilol Controlled Release 80 Lisinopril 20-9.00-9.45
Carvedilol Controlled Release 80 Lisinopril 40-14.58-10.95
Lisinopril 10-11.97-7.45
Lisinopril 20-10.85-5.32
Lisinopril 40-13.09-10.35

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Diastolic Responders, Defined as ≥ 10 mmHg Sitting (s)DBP Reduction From Baseline or a sDBP of <90 / 80 Millimeters (mm) of Mercury (Hg) for Non Diabetic / Diabetic Subjects Respectively (Based on Cuff Trough Measures)

(NCT00347360)
Timeframe: Week 6

Interventionparticipants (Number)
Lisinopril 1022
Lisinopril 2023
Lisinopril 4027
Carvedilol Controlled Release 2020
Carvedilol Controlled Release 4018
Carvedilol Controlled Release 8017
Carvedilol Controlled Release 20 Lisinopril 1020
Carvedilol Controlled Release 20 Lisinopril 2028
Carvedilol Controlled Release 20 Lisinopril 4025
Carvedilol Controlled Release 40 Lisinopril 1030
Carvedilol Controlled Release 40 Lisinopril 2022
Carvedilol Controlled Release 40 Lisinopril 4027
Carvedilol Controlled Release 80 Lisinopril 1028
Carvedilol Controlled Release 80 Lisinopril 2024
Carvedilol Controlled Release 80 Lisinopril 4028

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Changes in Heart Failure Symptoms

Changes from baseline in the symptom score subset (question 3, 5, 7 and 9) of KCCQ (swelling, fatigue, shortness of breath, shortness of breath night time). KCCQ is a self-administered by patient symptom score, where higher score reflect better health status. Scale scores are transformed to a 0 to 100 range by subtracting the lowest possible scale score, dividing by the range of the scale and multiplying by 100. This mean that the KCCQ scale is from 0 to 100 with the higher value showing a better health status. (NCT00391846)
Timeframe: 9 months and baseline

InterventionCategorial scale (Mean)
Guided by NT-proBNP3.67
Not Guided by NT-proBNP6.11

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Changes in NT-proBNP Values Over Time in All Patients

The 95% confidential interval (CI) is given as measure of dispersion (NCT00391846)
Timeframe: 9 months and baseline

Interventionng/L (Geometric Mean)
Guided by NT-proBNP2332.1
Not Guided by NT-proBNP2063

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Composite Value of 3 Variables After 9 Months: Cardiovascular Death (Days Alive), Cardiovascular Hospitalization (Days Out of Hospital), Heart Failure Symptoms (Symptom Score Subset of the Kansas City Cardiomyopathy Questionnaire - Questions 3,5,7,9)

The non-parametric scale is constructed from 3 variables, modified after Cleland. Each patient receives a rank score from 1 to 246 (246-number of patients in the study). The lowest score receive patients who die (due to CV event), next patients still alive at end-of-study with the worst composite score, the best alive patients with 0 days in hospital and the largest improvement in the KCCQ (self-administered by patient symptom score, where the higher score reflect better health status). Scores will be summarized using non-parametric calculations. The mean of non-parametric scores is presented (NCT00391846)
Timeframe: 9 months

InterventionScores on a scale (Mean)
Guided by NT-proBNP118.6
Not Guided by NT-proBNP128.4

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Discontinuations

Number of patients discontinued due to adverse events' (NCT00391846)
Timeframe: 9 months

InterventionParticipants (Number)
Guided by NT-proBNP8
Not Guided by NT-proBNP6

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Number of CV Deaths

Number of deaths (NCT00391846)
Timeframe: 9 months

InterventionParticipants (Number)
Guided by NT-proBNP4
Not Guided by NT-proBNP5

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Number of Days in Hospital for CV Reason

Each overnight stay is counted as one day. The lower the better (NCT00391846)
Timeframe: 9 months

InterventionDays in hospital (Mean)
Guided by NT-proBNP5.79
Not Guided by NT-proBNP5.94

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Total Number of Titration Steps in Prescribed Heart Failure Treatment

Each titration step in prescribed medication is counted as one step, either up or down. One step up indicates an increase of dose in prescribed medication and one step down indicates a decrease of dose in prescribed medication. The sum of steps is given as a score. Score is given for each arm as a total number of titration steps for all patients in arm. (NCT00391846)
Timeframe: 9 months

InterventionTitration steps (Number)
Guided by NT-proBNP517
Not Guided by NT-proBNP485

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Change in Reactive Hyperemic Index by Period (Carvedilol CR + Lisinopril vs. Lisinopril + HCTZ)

Reactive hyperemic index is a measure of endothelial function. This is measured by the ratio of post-occlusion blood volume flow versus the baseline blood volume flow. The outcome reported is the change in this ratio after the first intervention phase compared to after the second intervention phase. (NCT00459056)
Timeframe: Change from three months to seven months

InterventionRatio (Mean)
Carvedilol CR + Lisinopril, Then Lisinopril +HCTZ-0.26
Lisinopril + HCTZ, Then Carvedilol CR + Lisinopril-0.14

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Pulse Wave Velocity (PWV) Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug

Analysis was performed in the modified intention to treat (mITT) population. (NCT00496834)
Timeframe: Baseline and 24 Weeks

Interventionmeters/second (Mean)
Losartan0.28
Carvedilol-0.12

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Diastolic Blood Pressure (DBP) Mean Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug

(NCT00496834)
Timeframe: Baseline and 24 weeks

Interventionmm Hg (Mean)
Losartan-8.43
Carvedilol-7.81

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Systolic Blood Pressure (SBP) Mean Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug

(NCT00496834)
Timeframe: Baseline and 24 weeks

Interventionmm Hg (Mean)
Losartan-15.08
Carvedilol-14.81

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PWV Changes From Baseline (Visit 2) to 24 Weeks (Visit 6) After the Administration of the Study Drug

Analysis was performed in the per protocol (PP) population which additionally excludes certain protocol violations as described in the analysis plan. (NCT00496834)
Timeframe: Baseline and 24 Weeks

Interventionmeters/second (Mean)
Losartan0.16
Carvedilol-0.20

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Change in Disease Score (DS) Among the Treatment Groups

Rasmussen Disease Score (RDS) Change From Baseline to 9 Months A score of six or higher on these tests means the patient likely has plaque build-up in the arteries, or atherosclerosis, while a score of three to five suggests that such a problem may be developing. A score of two or less signals a patient is fine but should return in the future for another test. The method detects disease at the earliest moment, before the traditionally used calcium score would show any signs of trouble. (NCT00553969)
Timeframe: Baseline and nine months

InterventionOverall Rasmussen Disease Score Change (Mean)
1 Coreg CR + Lisinopril-2.48
2 Coreg CR + Placebo-2.29
3 Lisinopril + Placebo-2.38
4 Placebo + Placebo-0.96

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Percent Days Abstinent From Cocaine - Self Report

Percent Self reported days of abstinence from any cocaine use during the 11 week trial. (NCT00566969)
Timeframe: 11 weeks

Interventionpercentage of days (Mean)
Sugar Pill72.9
Carvedilol 25 mg72.9
Carvedilol 50 mg59.3

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Number of Participants With Mean Sitting Cuff Blood Pressure <140/90 mmHg at the End of 6 Weeks of Treatment

Sitting cuff blood pressure was calculated as the mean of three measurements taken approximately 2 minutes apart, and before the morning dose. (NCT00624065)
Timeframe: Week 6

,
InterventionParticipants (Number)
Responders (mean BP <140/90 mmHg)Non-responders (SBP >/=140 mmHg or DBP >/=90 mmHg)
Carvedilol CR + Lisinopril13764
Lisinopril13964

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Mean Change From Baseline in Sitting Systolic Blood Pressure (sSBP) and Sitting Diastolic Blood Pressure (sDBP) at Week 6

Mean change was calculated as Week 6 values minus Baseline values. (NCT00624065)
Timeframe: Baseline and Week 6

,
InterventionmmHg (Mean)
sSBP (mmHg)sDBP (mmHg)
Carvedilol CR + Lisinopril-16.07-9.14
Lisinopril-17.05-10.15

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Number of Participants Assessed for Change in Markers of Inflammation (PAI-1) Following Treatment Compared to Baseline

Reporting the number of participants with a change in markers of inflammation (PAI-1) following treatment compared to baseline. (NCT00642434)
Timeframe: 5 months

Interventionparticipants (Number)
Metoprolol0
Carvedilol0

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Stroke Volume (SV)

Hemodynamic variable (volume pumped per heart beat) in mL per beat. Clinically, SV is reported simply as mL (NCT00657241)
Timeframe: End of each treatment period (4 weeks on ARB or beta-blocker)

InterventionmL or mL/beat (Mean)
Lisinopril Plus Valsartan77
Lisinopril Plus Carvedilol76

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Cardiac Output

Hemodynamic variable representing whole-body blood flow (the product of heart rate and stroke volume) (NCT00657241)
Timeframe: End of each 4-week treatment period (valsartan vs. carvedilol CR)

InterventionL/min (Mean)
Lisinopril Plus Valsartan5.7
Lisinopril Plus Carvedilol5.1

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Central Systolic Blood Pressure

Aortic SBP derived non-invasively from radial arterial tonometry, pulse wave analysis, and a generalized transfer function algorithm within the SphygmoCor device. Aortic SBP is different from brachial SBP and is variably lower than brachial SBP due to pulse wave transmission differences between individuals. It is expressed in mmHg. (NCT00657241)
Timeframe: End of each treatment period (4 weeks of valsartan or carvedilol CR)

InterventionmmHg (Mean)
Lisinopril Plus Valsartan130
Lisinopril Plus Carvedilol141

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Difference in Resting CTTI Between Carvedilol CR (Beta-blocker) and Valsartan (ARB) in Combination With Lisinopril.

"Cardiac time-tension index (CTTI) is a refined version of the rate-pressure product (RPP, historically systolic [S] BP x heart rate) reported by the SphygmoCor pulse wave analysis system used in this trial. CTTI is preferable to RPP because the latter overestimates the contribution of systolic BP to cardiac work (the formula intrinsically assumes maximum SBP throughout the entire heart period [RR interval]). In contrast, CTTI represents cardiac work during the actual systolic time interval (STI, the period of active contraction, which is about 320 ms, inversely related to HR). Thus, CTTI = [mean systolic BP during STI, mmHg] x [STI/RR] x [HR, beats/min] and is expressed as CTTI units or as mmHg*beats/min. Mean resting CTTI for SBP 150, HR 60 = about 2500 units (corresponding RPP = 9000 units). In this crossover study, the principal dependent variable is the mean within-subjects difference in supine CTTI between valsartan and carvedilol CR after 4 weeks of each treatment." (NCT00657241)
Timeframe: End of each treatment period (4 weeks on ARB or beta-blocker)

InterventionCTTI units (mmHg*beats/min) (Mean)
Carvedilol CR2447
Valsartan2500

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Heart Rate (Beats/Min)

Hemodynamic variable (cardiac rate) (NCT00657241)
Timeframe: End of each treatment period (4 weeks on ARB or beta-blocker)

Interventionbeats per minute (Mean)
Lisinopril Plus Valsartan75
Lisinopril Plus Carvedilol68

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Systemic Vascular Resistance

Hemodynamic variable measured as mean arterial pressure (mmHg) / cardiac output (L/min) *80 in units of dyne-sec-cm[-5] (NCT00657241)
Timeframe: End of each treatment period (4 weeks of valsartan or carvedilol CR)

Interventiondyne sec cm-5 (Mean)
Lisinopril Plus Valsartan1407
Lisinopril Plus Carvedilol1591

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Central Aortic Blood Pressure

(NCT00669279)
Timeframe: Measured at baseline and 4 weeks.

InterventionmmHg (Mean)
Carvedilol CR-16.1
Atenolol-16.0

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Left Ventricular Ejection Fraction (LVEF) (%) at Week 18

Left ventricular ejection fraction (LVEF) (%) at Week 18 (NCT00673075)
Timeframe: 18 weeks post-treatment

,
Interventionpercentage (Mean)
BaselinePost baseline
Carvedilol60.44260.775
Nebivolol61.4361.93

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Peripheral Systolic Blood Pressure (SBP)

Peripheral systolic blood pressure (SBP) at visit 13 (week 18) (NCT00673075)
Timeframe: 18 weeks post initiation of randomized treatment

,
InterventionmmHg (Mean)
BaselinePost-Baseline
Carvedilol136.9137.3
Nebivolol135.1129.6

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Proportion of Patients With Peripheral SBP <140 mm Hg and DBP <90 mm Hg at Week 18

Proportion of Patients with Peripheral SBP <140 mm Hg and DBP <90 mm Hg at Week 18 (NCT00673075)
Timeframe: 18 weeks post-treatment

Interventionparticipants (Number)
Nebivolol11
Carvedilol5

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Peripheral Diastolic Blood Pressure (DBP)

Peripheral diastolic blood pressure (DBP) at post-baseline (visit 13, week 18) (NCT00673075)
Timeframe: 18 weeks post initiation of randomized treatment

,
InterventionmmHg (Mean)
BaselinePost-baseline
Carvedilol78.279.3
Nebivolol81.178.0

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Mean Change From Baseline in Alkaline Phosphatase, Alanine Aminotransferase, Aspartate Aminotransferase, Creatine Kinase, and Gamma Glutamyl Transferase at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventioninternational units per liter (IU/L) (Mean)
Alkaline PhosphataseAlanine AminotransferaseAspartate AminotransferaseCreatine KinaseGamma Glutamyl Transferase
CRV-IR-10.9-0.20.834.4-0.8
SK&F-105517-D-5.03.81.4-0.12.4

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Mean Change From Baseline in Calcium, Chloride, Glucose, Potassium, Sodium, and Urea/Blood Urea Nitrogen at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionmillimoles per liter (mmol/L) (Mean)
CalciumChlorideGlucosePotassiumSodiumUrea/Blood Urea Nitrogen
CRV-IR-0.0272180.2-0.136252-0.070.50.61339
SK&F-105517-D-0.0561382.4-1.9567280.071.6-0.58013

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Mean Change From Baseline in Creatine Kinase BB Percentage, Creatine Kinase MB Percentage, and Creatine Kinase MM Percentage at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (BB, brain-derived; MB=cardiac muscle-derived; MM=skeletal muscle-derived. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionpercentage of Total Creatine Kinase (Mean)
Creatine Kinase BB percentageCreatine Kinase MB percentageCreatine Kinase MM percentage
CRV-IR-0.2-0.31.1
SK&F-105517-D0.5-0.10.8

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Mean Change From Baseline in Each Type of White Blood Cell (WBC) (Basophils, Eosinophils, Lymphocytes, Monocytes, and Total Neutrophils) at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionpercentage of each WBC type in WBC count (Mean)
BasophilsEosinophilsLymphocytesMonocytesTotal Neutrophils
CRV-IR-0.060.150.050.19-0.41
SK&F-105517-D-0.060.762.211.28-4.31

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Mean Change From Baseline in Hemoglobin and Mean Corpuscular Hemoglobin Concentration at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventiongrams per liter (g/L) (Mean)
HemoglobinMean Corpuscular Hemoglobin Concentration
CRV-IR-2.31.3
SK&F-105517-D-3.9-1.9

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Mean Change From Baseline in Platelet Count and White Blood Cell Count at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventiongibi (2 to the power of 30)/liter (Gi/L) (Mean)
Platelet CountWhite Blood Cell Count
CRV-IR-6.90.297
SK&F-105517-D-11.1-0.498

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Mean Change From Baseline in Weight at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventionkilograms (kg) (Mean)
CRV-IR0.29
SK&F-105517-D-0.11

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Mean Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionmillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
CRV-IR-5.70.6
SK&F-105517-D10.02.8

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Mean Plasma Brain Natriuretic Peptide Concentration at Baseline and Week 8

Brain natriuretic peptide is a surrogate marker of the severity of heart failure and was measured by a central laboratory. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionng/L (nanogram per Liter) (Mean)
Baseline, n=20, 19Week 8, n=11, 8
CRV-IR108.9364.88
SK&F-105517-D226.46111.93

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Number of Participants With Adverse Events by Severity From Week 0 Through Week 8 (CRV-IR) or Week 14 (SK&F-105517-D)

Drug-related adverse events (AEs) were defined as AEs that were judged to have a relationship with the investigational product by the investigator (or subinvestigator) with the use of clinical judgment and the Clinical Investigator Brochure to determine the relationship. Refer to adverse event information for type and frequency of adverse events. (NCT00742508)
Timeframe: Treatment Period from Week 0 (Baseline) to Week 8 and 1-week Follow-up Period (Week 9) for CRV-IR; Treatment Period from Week 0 (Baseline) to Week 14 and 1-week Follow-up Period (Week 15) for SK&F-105517-D

,
Interventionparticipants (Number)
SevereModerateMildSevere (drug-related)Moderate (drug-related)Mild (drug-related)
CRV-IR029023
SK&F-105517-D1510134

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Number of Participants With the Indicated Change From Baseline New York Heart Association (NYHA) Functional Class at Week 8

The NYHA classification assesses the severity of symptoms of heart failure as judged by the investigator and is comprised of. 4 classes: I, no resulting limitations on physical activity (PA); II, slight limitations on PA; III, marked limitations on PA; IV, inability to carry out any PA without discomfort. The number of participants with any change from Baseline in the NYHA Functional Class at Week 8 was calculated. Improved=class at the visit is decreased compared to baseline class, Unchanged=class at the visit is stable, Worsened=class at the visit is increased compared to baseline class. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionparticipants (Number)
ImprovedUnchangedWorse
CRV-IR0110
SK&F-105517-D170

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Number of Participants With the Indicated Electrocardiogram Findings at Baseline and Week 8

There are 3 categories for electrocardiogram (ECG) findings: normal; abnormal, not clinically significant; and abnormal, clinically significant. Each of the findings was classified by the investigator according to whether it was normal. Abnormal ECGs were further classified according to whether they were felt to be clinically significant in the medical and scientific judgment of the investigator. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionparticipants (Number)
Normal, Baseline (BL), n=22, 19Abnormal-Not clinically significant, BL, n=22, 19Abnormal-Clinically significant, BL, n=22, 19Normal, Week (W) 8, n=11, 8Abnormal-Not clinically significant, W8, n=11, 8Abnormal-Clinically significant, W8, n=11, 8
CRV-IR2128254
SK&F-105517-D199116

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Number of Participants With the Indicated Urinalysis Dipstick Results at Baseline and Week 8

Dipstick test values: Negative (-), Traces (+-), +1, +2, +3. +4. Normal ranges (qualitative): protein, - or +-; glucose, - or +-; occult blood, -; ketones, -. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionparticipants (Number)
Urine Glucose, Negative, Baseline, n=22, 19Urine Glucose, Traces, Baseline, n=22, 19Urine Glucose, 1+, Baseline, n=22, 19Urine Glucose, 2+, Baseline, n=22, 19Urine Glucose, 3+, Baseline, n=22, 19Urine Glucose, 4+, Baseline, n=22, 19Urine Ketones, Negative, Baseline, n=22, 19Urine Ketones, Traces, Baseline, n=22, 19Urine Ketones, 1+, Baseline, n=22, 19Urine Ketones, 2+, Baseline, n=22, 19Urine Ketones, 3+, Baseline, n=22, 19Urine Ketones, 4+, Baseline, n=22, 19Urine Occult Blood, Negative, Baseline, n=22, 19Urine Occult Blood, Traces, Baseline, n=22, 19Urine Occult Blood, 1+, Baseline, n=22, 19Urine Occult Blood, 2+, Baseline, n=22, 19Urine Occult Blood, 3+, Baseline, n=22, 19Urine Occult Blood, 4+, Baseline, n=22, 19Urine Protein, Negative, Baseline, n=22, 19Urine Protein, Traces, Baseline, n=22, 19Urine Protein, 1+, Baseline, n=22, 19Urine Protein, 2+, Baseline, n=22, 19Urine Protein, 3+, Baseline, n=22, 19Urine Protein, 4+, Baseline, n=22, 19Urine Glucose, Negative, Week 8, n=11, 8Urine Glucose, Traces, Week 8, n=11, 8Urine Glucose, 1+, Week 8, n=11, 8Urine Glucose, 2+, Week 8, n=11, 8Urine Glucose, 3+, Week 8, n=11, 8Urine Glucose, 4+, Week 8, n=11, 8Urine Ketones, Negative, Week 8, n=11, 8Urine Ketones, Traces, Week 8, n=11, 8Urine Ketones, 1+, Week 8, n=11, 8Urine Ketones, 2+, Week 8, n=11, 8Urine Ketones, 3+, Week 8, n=11, 8Urine Ketones, 4+, Week 8, n=11, 8Urine Occult Blood, Negative, Week 8, n=11, 8Urine Occult Blood, Traces, Week 8, n=11, 8Urine Occult Blood, 1+, Week 8, n=11, 8Urine Occult Blood, 2+, Week 8, n=11, 8Urine Occult Blood, 3+, Week 8, n=11, 8Urine Occult Blood, 4+, Week 8, n=11, 8Urine Protein, Negative, Week 8, n=11, 8Urine Protein, Traces, Week 8, n=11, 8Urine Protein 1+, Week 8, n=11, 8Urine Protein, 2+, Week 8, n=11, 8Urine Protein, 3+, Week 8, n=11, 8Urine Protein, 4+, Week 8, n=11, 8
CRV-IR20100102200000181210021001001100000110000011000001010000
SK&F-105517-D1900000190000016111001801000800000800000800000800000

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Mean Change From Baseline in Hematocrit at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventionproportion of 1 (SI) (Mean)
CRV-IR-0.0085
SK&F-105517-D-0.0095

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Mean Change From Baseline in Heart Rate at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventionbeats per minute (Mean)
CRV-IR-10.4
SK&F-105517-D-10.6

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Mean Change From Baseline in Amylase at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value (NCT00742508)
Timeframe: Baseline and Week 8

Interventionunits per liter (U/L) (Mean)
CRV-IR-10.2
SK&F-105517-D-0.1

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Mean Change From Baseline in Mean Corpuscular Hemoglobin at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventionpicograms (pg) (Mean)
CRV-IR0.12
SK&F-105517-D-0.21

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Mean Change From Baseline in Mean Corpuscular Volume at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventionfemtoliters (fL) (Mean)
CRV-IR0.1
SK&F-105517-D-0.1

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Mean Change From Baseline in Red Blood Cell Count at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

Interventiontebi (2 to the power of 40)/liter (Ti/L) (Mean)
CRV-IR-0.091
SK&F-105517-D-0.087

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Adjusted Mean Change From Baseline in Diastolic Blood Pressure at Week 8

Pharmacodynamic (PD) assessment points were 24 hours (h) (from time of first reading to time of last reading), morning (6 am-12 pm), afternoon (12-6 pm), night (6 pm-6 am on following day), waking (8 am-9 pm), sleeping (0-5 am), PDmax (maximal value obtained with each participant during the 0-24 h interval), PDmin (minimal value obtained with each participant during the 0-24 h interval), and PDmax/PDmin. PDmax/PDmim was calculated as the ratio of the PDmax to PDmin, and it showed the degree of change during the 0-24 h interval. The mean was adjusted for Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionmillimeters of mercury (mmHg) (Mean)
24 hMorningAfternoonNightWakingSleepingPDmaxPDminPDmax/PDmin
CRV-IR-7.10-7.68-5.32-9.01-5.11-12.68-10.45-1.34-0.24
SK&F-105517-D-4.89-8.24-10.250.73-8.565.38-17.91-0.24-0.36

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Time of Maximal Plasma Concentration (Tmax) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8

Time of maximal plasma concentration (tmax) of S-carvedilol, R-carvedilol, and M4 active metabolite (SB-203231) was measured. Participants in each treatment group were divided into 3 groups by pharmacokinetic sampling timing: Groups A, B, and C in the SK&F-105517-D group and Groups D, E, and F in the CRV-IR group. Carvedilol is a racemic mixture. Non-selective β-blocking activity is shown by S-carvedilol, while α1-blocking activity is shown by both S-carvedilol and R-carvedilol. (NCT00742508)
Timeframe: Week 8

,
Interventionhours (Median)
S-carvedilolR-carvedilolSB-203231
CRV-IR1.9831.9831.983
SK&F-105517-D5.9585.9585.958

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Adjusted Mean Change From Baseline in Mean Heart Rate at Week 8

Pharmacodynamic (PD) assessment points were 24 hours (h) (from time of first reading to time of last reading), morning (6 am-12 pm), afternoon (12-6 pm), night (6 pm-6 am on following day), waking (8 am-9 pm), sleeping (0-5 am), PDmax (maximal value obtained with each participant during the 0-24 h interval), PDmin (minimal value obtained with each participant during the 0-24 h interval), and PDmax/PDmin. PDmax/PDmim was calculated as the ratio of the PDmax to PDmin, and it showed the degree of change during the 0-24 h interval. The mean was adjusted for Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionbeats per minute (Mean)
24 hMorningAfternoonNightWakingSleepingPDmaxPDminPDmax/PDmin
CRV-IR-11.38-9.59-13.96-11.12-12.53-11.16-13.43-2.04-0.93
SK&F-105517-D-15.37-14.87-15.93-15.26-15.53-14.28-23.43-3.47-1.27

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Adjusted Mean Change From Baseline in Systolic Blood Pressure at Week 8

Pharmacodynamic (PD) assessment points were 24 hours (h) (from time of first reading to time of last reading), morning (6 am-12 pm), afternoon (12-6 pm), night (6 pm-6 am on following day), waking (8 am-9 pm), sleeping (0-5 am), PDmax (maximal value obtained with each participant during the 0-24 h interval), PDmin (minimal value obtained with each participant during the 0-24 h interval), and PDmax/PDmin. PDmax/PDmim was calculated as the ratio of the PDmax to PDmin, and it showed the degree of change during the 0-24 h interval. The mean was adjusted for Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionmillimeters of mercury (mmHg) (Mean)
24 hMorningAfternoonNightWakingSleepingPDmaxPDminPDmax/PDmin
CRV-IR-10.84-12.34-10.14-9.04-10.39-11.85-9.74-6.890.07
SK&F-105517-D-1.45-4.78-12.065.17-9.9913.20-10.191.42-0.17

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Area Under the Plasma Concentration Versus Time Curve From Time Zero to 24 Hours (AUC0-24) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8

Area under the plasma concentration versus time curve from time zero to 24 hours (AUC0-24) of S-carvedilol, R-carvedilol, and M4 active metabolite (SB-203231) was measured. Participants in each treatment group were divided into 3 groups by pharmacokinetic sampling timing: Groups A, B, and C in the SK&F-105517-D group and Groups D, E, and F in the CRV-IR group. The analysis was performed on log-transformed data. Carvedilol is a racemic mixture. Non-selective β-blocking activity is shown by S-carvedilol, while α1-blocking activity is shown by both S-carvedilol and R-carvedilol. (NCT00742508)
Timeframe: Week 8

,
Interventionhours * nanograms per milliliter (ng/mL) (Geometric Mean)
S-carvedilolR-carvedilolSB-203231
CRV-IR60.040170.72828.113
SK&F-105517-D155.109284.31364.687

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Cardiothoracic Ratio at Baseline and Week 8

Cardiothoracic ratio is a marker of the degree of heart enlargement and was measured by chest X-ray. It is shown as the ratio of the transverse diameter of the heart to the transverse diameter of the thorax, and is measured as a percentage. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionpercentage (Mean)
Baseline, n=22, 19Week 8, n=11, 8
CRV-IR53.7050.91
SK&F-105517-D53.5852.35

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Echocardiogram Results: Left Ventricular Ejection Fraction at Baseline and Week 8

Left ventricular ejection fraction (LVEF) is a marker of left ventricular systolic function and was measured by echocardiogram. It is shown as the ratio of left ventricular stroke volume (LVSV) to left ventricular end-diastolic volume (LVEDV), and is measured as a percentage. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionpercentage (Mean)
Baseline, n=20, 19Week 8, n=11, 8
CRV-IR34.042.0
SK&F-105517-D32.237.6

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Maximum Plasma Concentration (Cmax) and Trough Plasma Concentration (Cmin) of S-carvedilol, R-carvedilol, and M4 Active Metabolite (SB-203231) at Week 8

Maximum Plasma Concentration (Cmax) and Trough Plasma Concentration (Cmin) of S-carvedilol, R-carvedilol, and M4 active Metabolite (SB-203231) were measured. Participants in each treatment group were divided into 3 groups by pharmacokinetic sampling timing: Groups A, B, and C in the SK&F-105517-D group and Groups D, E, and F in the CRV-IR group. The analysis was performed on log-transformed data. Carvedilol is a racemic mixture. Non-selective β-blocking activity is shown by S-carvedilol, while α1-blocking activity is shown by both S-carvedilol and R-carvedilol. (NCT00742508)
Timeframe: Week 8

,
Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
S-carvedilol, CmaxS-carvedilol, CminR-carvedilol, CmaxR-carvedilol, CminSB-203231, CmaxSB-203231, Cmin
CRV-IR6.79521.207219.18642.94453.16650.4843
SK&F-105517-D12.81713.379627.13064.25656.39371.2386

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Mean Change From Baseline in Albumin and Total Protein at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value. (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventiongrams per liter (g/L) (Mean)
AlbuminTotal Protein
CRV-IR0.70.4
SK&F-105517-D-1.9-1.6

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Mean Change From Baseline in Total Bilirubin, Creatinine, and Uric Acid at Week 8

Mean change from baseline was calculated as the Week 8 value minus the Baseline value (NCT00742508)
Timeframe: Baseline and Week 8

,
Interventionmicromoles per liter (umol/L) (Mean)
Total BilirubinCreatinineUric Acid
CRV-IR1.5555.545130.8215
SK&F-105517-D-4.489-4.530514.1265

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Endothelial Progenitor Cells

"ALDH bright cells reported as percentage of mononuclear cells. These were assayed using flow cytometry~CD34/CD133 endothelial progenitor cells reported as percentage of mononuclear cells. These were assayed using flow cytometry" (NCT00827775)
Timeframe: 12 weeks

Intervention% of mononuclear cells (Median)
Baseline ALDH brightBaseline CD34/CD133 endothelial progenitor cells
Control0.0520.059

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Endothelial Progenitor Cells

"ALDH bright cells reported as percentage of mononuclear cells. These were assayed using flow cytometry~CD34/CD133 endothelial progenitor cells reported as percentage of mononuclear cells. These were assayed using flow cytometry" (NCT00827775)
Timeframe: 12 weeks

Intervention% of mononuclear cells (Median)
Baseline ALDH brightFollow up ALDH brightBaseline CD34/CD133 endothelial progenitor cellsFollow up CD34/CD133
Intervention0.0340.0270.0330.029

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Flow Mediated Vasodilation

Measured as percent change in brachial artery diameter from baseline to post shear stress for an individual measurement. Follow up measurements were obtained in intervention subjects 12 weeks later (NCT00827775)
Timeframe: 12 weeks

Intervention% dilation from baseline (Mean)
Baseline FMD
Control1.67

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Flow Mediated Vasodilation

Measured as percent change in brachial artery diameter from baseline to post shear stress for an individual measurement. Follow up measurements were obtained in intervention subjects 12 weeks later (NCT00827775)
Timeframe: 12 weeks

Intervention% dilation from baseline (Mean)
Baseline FMDFollow Up FMD
Intervention1.031.4

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AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated) - Carvedilol in Plasma

Bioequivalence based on AUC0-inf (NCT00834795)
Timeframe: Blood samples collected over 60 hour period

Interventionng*h/mL (Mean)
Carvedilol465.29
Coreg®468.81

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Cmax - Maximum Observed Concentration - Carvedilol in Plasma

Bioequivalence based on Cmax (NCT00834795)
Timeframe: Blood samples collected over 60 hour period

Interventionng/mL (Mean)
Carvedilol104.98
Coreg®107.47

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AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Carvedilol in Plasma

Bioequivalence based on AUC0-t (NCT00834795)
Timeframe: Blood samples collected over 60 hour period

Interventionng*h/mL (Mean)
Carvedilol454.24
Coreg®456.05

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Cmax - Maximum Observed Concentration - Carvedilol in Plasma

Bioequivalence based on Cmax (NCT00834873)
Timeframe: Blood samples collected over 60 hour period

Interventionng/mL (Mean)
Carvedilol89.91
Coreg®97.05

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AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant) - Carvedilol in Plasma

Bioequivalence based on AUC0-t (NCT00834873)
Timeframe: Blood samples collected over 60 hour period

Interventionng*h/mL (Mean)
Carvedilol455.91
Coreg®478.61

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AUC0-inf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated) - Carvedilol in Plasma

Bioequivalence based on AUC0-inf (NCT00834873)
Timeframe: Blood samples collected over 60 hour period

Interventionng*h/mL (Mean)
Carvedilol467.57
Coreg®490.16

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Peak Exercise Oxygen Consumption

Oxygen consumption at peak of exercise (NCT00924833)
Timeframe: Time 1: sea level, baseline, no treatment. Time 2: sea level, after three weeks of allocated treatment. Time 3: within the first two days of high altitude exposure, under treatment.

,,
Interventionml/Kg/min (Mean)
Time 1Time 2Time 3
Carvedilol37.636.224.0
Nebivolol38.039.728.8
Placebo33.933.922.9

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Delta Peak Exercise Minute Ventilation Time 1 Versus Time 3.

"Difference in peak exercise minute ventilation between Time 1 and Time 3 (Time 3 - Time 1.~Minute ventilation = tidal volume (ml) multiplied by the respiratory rate (breaths/min)." (NCT00924833)
Timeframe: Time 1: sea level, baseline, no treatment. Time 3: within the first two days of high altitude exposure, under treatment.

InterventionL/min (Mean)
Placebo0.7
Carvedilol-9.3
Nebivolol15.2

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Delta Peak Exercise Oxygen Consumption Time 1 Versus Time 3

Difference in peak exercise oxygen consumption between Time 1 and Time 3 (Time 3 - Time 1) (NCT00924833)
Timeframe: Time 1: sea level, baseline, no treatment. Time 3: within the first two days of high altitude exposure, under treatment.

Interventionml/Kg/min (Mean)
Placebo-32.7
Carvedilol-37.6
Nebivolol-22.5

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Peak Exercise Minute Ventilation

Minute ventilation at peak of exercise. Minute ventilation = tidal volume (ml) multiplied by the respiratory rate (breaths/min) (NCT00924833)
Timeframe: Time 1: sea level, baseline, no treatment. Time 2: sea level, after three weeks of allocated treatment. Time 3: within the first two days of high altitude exposure, under treatment.

,,
InterventionL/min (Mean)
Time 1Time 2Time 3
Carvedilol90.389.684.5
Nebivolol81.883.892.0
Placebo93.995.690.3

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Absolute Change in Right Ventricular Ejection Fraction

Change in right ventricular ejection fraction is measured by cardiac magnetic resonance imaging, using the method of disks with the reading radiologist being blinded to before and after images. Cardiac magnetic resonance imaging was done at baseline and 6 months only (NCT00964678)
Timeframe: baseline, 6 months

Intervention% RVEF (Mean)
Carvedilol10.4

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Change in 6 Minute Walk Distance

(NCT00964678)
Timeframe: baseline and 6 months

Interventionfeet (Number)
Participant 1Participant 2Participant 3Participant 5Participant 6
Carvedilol4516035596

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Change in Right Ventricular End Systolic Volume

right ventricular end systolic volume determined by MRI (NCT00964678)
Timeframe: baseline and 6 months

InterventionmL (Number)
Participant 1Participant 2Participant 3Participant 4Participant 5Participant 6
Carvedilol31456112725

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Change in Tricuspid Annular Plane Systolic Excursion

Higher values indicate a better outcome. (NCT00964678)
Timeframe: baseline and 6 months

Interventioncentimeters (Number)
Participant 1Participant 2Participant 4Participant 5Participant 6
Carvedilol0.4-0.08-0.120.450.08

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Number of Participants With Cardiotoxicity-free Survival at 750 Days From Baseline

Number of Participants with cardiotoxicity-free survival at 750 days from baseline (NCT01009918)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Arm I Lisinopril15
Arm II Coreg CR®24
Arm III Placebo17

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Number of Participants With LVEF Decrease to <50%

Number of Participants with Left Ventricular Ejection Fraction (LVEF) drop to <50% (NCT01009918)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Arm I Lisinopril5
Arm II Coreg CR®9
Arm III Placebo15

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Number of Participants With Trastuzumab-Induced Cardiotoxicity After 52 Weeks of Treatment

Reduction in incidence of trastuzumab-induced cardiotoxicity after 52 weeks of treatment as measured by preservation of Left Ventricular Ejection Fraction (LVEF). Number of Patients who experienced a cardiotoxicity. (NCT01009918)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Arm I Lisinopril45
Arm II Coreg CR®43
Arm III Placebo46

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Number of Patients With Trastuzumab Course Interruption

Measure indicates the number of patients who had an interruption of trastuzumab for any reason (NCT01009918)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Arm I Lisinopril27
Arm II Coreg CR®24
Arm III Placebo40

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Quality-of-life Changes Between Baseline and 52-weeks

Quality-of-life changes as assessed by North European Organisation for Research and Treatment of Cancer Quality of Life Questionnaire (EORTC-QLQ-C30), which measures the quality of life of cancer patients. Higher score indicates higher quality of life. Score range is 0-100. The questionnaire was administered at baseline and at 52 weeks. (NCT01009918)
Timeframe: 52 weeks

InterventionScores on a scale (Mean)
Arm I Lisinopril1
Arm II Coreg CR®2
Arm III Placebo5

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Retention

number of weeks each participant is on study protocol (NCT01171183)
Timeframe: 12 weeks

InterventionWeeks (Mean)
Placebo5.70
Carvedilol Controlled Release5.28

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Urine Toxicology Screens

Treatment Effectiveness Score, defined by the # of cocaine negative urines during the outpatient phase of the study divided by the total number of urine samples (30) and then multiplied by 100. (NCT01171183)
Timeframe: based on thrice weekly urine results during the 10-week outpatient phase

Interventionpercentage of cocaine negative urines (Mean)
Placebo38.33
Carvedilol Controlled Release41.85

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Exercise Tolerance Assessed by 6 Minute Walking Test

"Distance measured at 6 minute walking test. The 6 minute walking test was performed according to standardised procedure at baseline, before inclusion (at least 1 week after baseline evaluation), and at the end of the study. Patients who had not done at least two tests in the past underwent two practice 6 minute walking tests at least 3 days apart. Results are expressed in terms of distance walked (metres). The test was supervised by a physical therapist.~Patients were asked to walk at their own maximal pace a 100 m long hospital corridor. At the beginning of the last (6th) minute of the test a standard phrase of encouragement was told. Patients were allowed to stop if signs or symptoms of significant distress occurred (dyspnea, angina), through they were instructed to resume walking as soon as possible." (NCT01178528)
Timeframe: 3 months

Interventionmeters (Mean)
Ivabradine474.8
Carvedilol435.7
Carvedilol and Ivabradine453.1

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Maximal Oxygen Consumption

Functional capacity was assessed by means of a cardiopulmonary exercise test with a bicycle ergometer with gas exchange monitoring (Vmax 29 C, SensorMedics). Peak oxygen consumption was defined as the maximal oxygen consumption (MVO2) observed during exercise. (NCT01178528)
Timeframe: 3 months

InterventionmL/Kg/min (Mean)
Ivabradine15.8
Carvedilol12.9
Carvedilol and Ivabradine14.7

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New York Heart Association (NYHA) Class

"The 1994 NYHA Classification system is a measure of functional status. It was designed for clinical assessment of patients by physicians as NYHA class I, II, III, or IV, on the basis of patient's limitations in physical activities caused by cardiac symptoms.~Class I describes patients with cardiovascular disease (CVD) but without resulting limitation of physical activity. There is no objective evidence of CVD.~Class II describes patients with CVD resulting in slight limitation of physical activity. There is objective evidence of minimal CVD.~Class III describes patients with CVD resulting in marked limitation of physical activity. There is objective evidence of moderately severe CVD.~Class IV describes patients with CVD resulting in inability to carry on any physical activity without discomfort. There is objective evidence of severe CVD.~Here we report data on number of patients showing an improvement by at least one NYHA class according to treatment allocation." (NCT01178528)
Timeframe: 3 months

Interventionparticipants (Number)
Ivabradine30
Carvedilol5
Carvedilol and Ivabradine20

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Quality of Life

Quality of life (QoL) was evaluated using the Visual Analogue Scale (VAS) which is a global measurement of QoL, allowing a subjective assessment of the impact of the disease and treatment. Patients are asked to indicate their current state in a line from 0 (worst state) to 10 (best state), with higher values therefore representing a better outcome. (NCT01178528)
Timeframe: 3 months

Interventionunits on a scale (Mean)
Ivabradine6.7
Carvedilol4.1
Carvedilol and Ivabradine6.1

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Effect of Carvedilol Treatment in Cerebrospinal Fluid (CSF) Levels of Amyloid-beta Oligomers

The investigators will measure CSF Abeta oligomer levels before and after 6 months randomized placebo-controlled double-blind treatment with carvedilol at a target dose of 25 mg daily, comparing the change in levels in 6 AD participants taking carvedilol vs. 10 AD participants taking placebo. These 16 participants had both baseline and 6 month CSF collected (of the entire study population). (NCT01354444)
Timeframe: 6 months

,
Interventionng/mL (Mean)
Baseline Oligomeric ABeta (ng/mL)Six month oligomeric ABeta (ng/mL)
Carvedilol3.833.895
Placebo0.1290.117

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Hopkins Verbal Learning Test (HVLT) Scores at Baseline, 3, and 6 Months

The investigators measured episodic memory (as evidence by the Hopkins Verbal Learning Test (HVLT)) before and after 6 months randomized placebo-controlled double-blind treatment with carvedilol at a target dose of 25 mg daily. Changes in HVLT Immediate and Delayed Recall score in 14 Alzheimer's Disease (AD) participants taking carvedilol vs. 15 AD participants taking placebo were compared. HVLT test score ranges are as follows: immediate recall (0-24) delayed recall (0-12). Higher scores indicate better episodic memory recall. (NCT01354444)
Timeframe: Baseline, 3 months, and 6 months

,
InterventionScores on a scale (Mean)
HVLT score at Baseline (immediate recall)HVLT score at 3 months (immediate recall)HVLT score at 6 months (immediate recall)HVLT score at Baseline (delayed recall)HVLT score at 3 months (delayed recall)HVLT score at 6 months (delayed recall)
HVLT Score in Placebo Group131212111
HVLT Score in Treatment Group121313110

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Effect of Carvedilol Treatment in Cerebrospinal Fluid (CSF) Levels of Amyloid-beta Oligomers

The investigators will measure CSF Abeta oligomer levels before and after 6 months randomized placebo-controlled double-blind treatment with carvedilol at a target dose of 25 mg daily, comparing the change in levels in 6 AD participants taking carvedilol vs. 10 AD participants taking placebo. These 16 participants had both baseline and 6 month CSF collected (of the entire study population). CSF was collected at the baseline visit and 6 months later. (NCT01354444)
Timeframe: 6 months

,
Interventionpg/mL (Mean)
Baseline Tau (pg/mL)Baseline ABeta42 (pg/mL)Baseline P tau (pg/mL)Six month Tau (pg/mL)Six month ABeta42 (pg/mL)Six month P tau (pg/mL)
Carvedilol169.476396.98542.666222.461499.32556.003
Placebo169.484379.40666.133171.757361.56364.331

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Beta-Adrenergic Receptor (Alprenolol Binding Assay)

We hypothesize that use of carvedilol in patients with PAH will increase beta- adrenergic receptor availability, and this will be measurable as a increase in alprenolol binding over time of drug use. (NCT01586156)
Timeframe: 6 months

,,
Interventionabritrary units (Mean)
baseline6 months
Escalation-dose Carvedilol8277983730
Low-fixed-dose Carvedilol8523084554
Placebo Arm9225479083

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Cardiac Glucose Uptake in FDG-PET (Fluorodeoxyglucose-Positron Emission Tomography)

We hypothesize that use of carvedilol in patients with PAH (Pulmonary Arterial Hypertension) will decrease the cardiac glucose utilization, and this will be measurable as a drop in fasting FDG-PET standardized uptake values of the heart at 6 months as compared to baseline (NCT01586156)
Timeframe: 6 months

,,
Interventionstandardized uptake value (SUV) (Median)
baseline FDG-PET6 month FDG-PET
Escalation-dose Carvedilol0.90.7
Low-fixed-dose Carvedilol0.60.6
Placebo Arm1.00.8

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Echocardiogram Left Ventricular Cardiac Output

We hypothesized that carvedilol would be safe and tolerable and thus that Left ventricular cardiac output, a measure of heart function, would not decrease in participants on carvedilol. (NCT01586156)
Timeframe: 6 months

,,
InterventionL/min (Mean)
baseline3 months6 months
Escalation-dose Carvedilol4.54.84.9
Low-fixed-dose Carvedilol5.24.64.7
Placebo Arm4.74.74.5

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Echocardiogram Right Ventricular Systolic Pressure (RVSP)

We hypothesized that RVSP might decrease in participants on carvedilol. (NCT01586156)
Timeframe: 6 months

,,
Interventionmm Hg (Mean)
baseline3 months6 months
Escalation-dose Carvedilol635464
Low-fixed-dose Carvedilol635951
Placebo Arm767866

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NT-proBNP (N-terminal Pro-B Type Natriuretic Peptide)

We hypothesized that carvedilol would be safe and tolerable and thus that NT-BNP, a measure of heart failure, would not increase in participants on carvedilol. (NCT01586156)
Timeframe: 6 months

,,
Interventionpg/ml (Median)
baseline1 month3 months6 months
Escalation-dose Carvedilol127120169146
Low-fixed-dose Carvedilol57927952
Placebo Arm170183152293

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Urinary cAMP (Cyclic Adenosine Monophosphate)/Creatinine

We hypothesize that use of carvedilol in patients with PAH will increase beta adrenergic receptor function and this will be measurable as an increase in cAMP measured in the urine at 6 months in participants in dose escalation carvedilol. (NCT01586156)
Timeframe: 6 months

,,
Interventionumol/g (Median)
baseline1 month3 months6 months
Escalation-dose Carvedilol1.00.71.51.0
Low-fixed-dose Carvedilol0.60.80.60.7
Placebo Arm1.41.31.21.4

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6 Minute Walk Test

We hypothesized that carvedilol would not worsen 6 minute walk distance. (NCT01586156)
Timeframe: 6 months

,,
Interventionmeters (Mean)
baseline3 months6 months
Escalation-dose Carvedilol438438450
Low-fixed-dose Carvedilol504504486
Placebo Arm404412453

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Improvement in Left Ventricular Ejection Fraction (LVEF) at 12 Months

The primary clinical outcome will be LVEF response at 12 months defined as an improvement in LVEF of ≥ 8% at 12 months or if not available, ≥5% at 3 months in the absence of an adverse clinical outcome. Data are not presented for non-failing controls, who only went baseline evaluation and did not undergo treatment, given that they did not have heart failure. (NCT01798992)
Timeframe: 12 months

InterventionLVEF responders (Number)
Metoprolol Succinate12
Metoprolol Succinate + Doxazosin10
Carvedilol9

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Improvement in LVEF at 3 Months

A secondary outcome will be LVEF response at 3 months, defined as an improvement of ≥ 5% Data are not presented for non-failing controls, who only went baseline evaluation and did not undergo treatment, given that they did not have heart failure. (NCT01798992)
Timeframe: 3 months

InterventionLVEF responders (Number)
Metoprolol Succinate16
Metoprolol Succinate + Doxazosin10
Carvedilol10

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Composite of All-cause Mortality, Need for Heart Transplant or Need for Ventricular Assist Device.

Clinical status at 18 months will be assessed at time of study completion, specifically for the composite outcome of all-cause mortality, need for heart transplant, or need for ventricular assist device. Outcomes are not presented for non-failing controls, who only went baseline evaluation and did not undergo treatment, given that they did not have heart failure. (NCT01798992)
Timeframe: 18 months

Interventionparticipants (Number)
Metoprolol Succinate1
Metoprolol Succinate + Doxazosin0
Carvedilol0

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Mean Systolic Blood Pressure

(NCT02056626)
Timeframe: day 0

InterventionmmHg (Mean)
Partial Reinforcement151.59
Controlled Dosing, Daily152.64
Controlled Dosing, Every Other Day155.42
Standard Therapy151.74

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Mean Systolic Blood Pressure

(NCT02056626)
Timeframe: day 30

InterventionmmHg (Mean)
Partial Reinforcement138.90
Controlled Dosing, Daily136.38
Controlled Dosing, Every Other Day139.27
Standard Therapy134.94

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Mean Systolic Blood Pressure

(NCT02056626)
Timeframe: day 14

InterventionmmHg (Mean)
Partial Reinforcement133.64
Controlled Dosing, Daily132.92
Controlled Dosing, Every Other Day133.12
Standard Therapy135.00

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Maximum Change in LVEF at 12 Months

Value at 12 months minus value at baseline (NCT02177175)
Timeframe: 12 months

Interventionchange in percent ejection fraction (Median)
Carvedilol-2.5
Placebo-2

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Maximum Change in LVEF at 3 Months

Value at 3 months minus value at baseline (NCT02177175)
Timeframe: 3 months

Interventionchange in percent ejection fraction (Median)
Carvedilol1
Placebo-5

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Maximum Change in LVEF at 6 Months

Value at 6 months minus value at baseline (NCT02177175)
Timeframe: 6 months

Interventionchange in percent ejection fraction (Median)
Carvedilol-2
Placebo-5

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Maximum Change in LVEF at 9 Months

Value at 9 months minus value at baseline (NCT02177175)
Timeframe: 9 months

Interventionchange in percent ejection fraction (Median)
Carvedilol-3.5
Placebo-5.5

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Change in Pulse Wave Velocity

Changes in arterial stiffness between baseline and 18 months after therapy with carvedilol, spironolactone or usual care. Arterial stiffness was measured by pulse wave velocity (Sphygmocor device) (NCT02230891)
Timeframe: 18 months

Interventionm/sec (Mean)
Carvedilol-0.71
Spironolactone-0.77
Usual Care-0.59

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Change in Troponin T Measured Using a High Sensitivity Assay

Change in levels of troponin T (measured with a high sensitivity assay in blood samples) between baseline and 18 months after therapy with carvedilol or spironolactone or usual care (NCT02230891)
Timeframe: 18 months

Interventionng/L (Mean)
Carvedilol-0.2
Spironolactone1.4
Usual Care0.35

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Change in Cardiac Global Longitudinal Strain

Change in myocardial speckle tracked strain (global longitudinal strain) after 18 months (baseline vs. 18 months) of therapy with carvedilol or spironolactone or usual care. The myocardial global longitudinal strain was measured using echocardiography (NCT02230891)
Timeframe: 18 months

Intervention% systolic deformation (Mean)
Carvedilol-1.4
Spironolactone-1.74
Usual Care-1.14

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Change in NTproBNP (Biomarker)

Change in levels of NT-proBNP (measured in blood samples) between baseline and 18 months after therapy with carvedilol or spironolactone or usual care (NCT02230891)
Timeframe: 18 months

Interventionpg/ml (Mean)
Carvedilol87.9
Spironolactone-16.5
Usual Care3.65

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at Week 6 from pre-dosing with Intralipid to 12 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 12 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate9.50
Carvedilol8.14
Placebo0.38

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 24 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 24 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate13.93
Carvedilol13.21
Placebo10.27

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 20 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 20 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate13.27
Carvedilol9.39
Placebo11.4

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 16 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 16 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate15.78
Carvedilol8.05
Placebo3.6

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 12 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 12 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate20.55
Carvedilol1.74
Placebo5.25

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at Week 6 from pre-dosing with Intralipid to 4 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 4 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate11.50
Carvedilol14.32
Placebo4.26

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Change in Flow-mediated Dilation

The change in endothelium-dependent vascular reactivity will be measured by flow-mediated dilation (FMD) of the brachial artery using a high-resolution vascular ultrasound with a 10-MHz linear array transducer. FMD is expressed as the percentage increase in diameter at the baseline visit from pre-dosing with Intralipid to 24 hours during Intralipid infusion (NCT02406586)
Timeframe: Pre-dose (Baseline), within 24 hours at Baseline visit

Interventionpercent change in diameter (Mean)
Salsalate0.35
Carvedilol0.53
Placebo0.47

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Change in Flow-mediated Dilation

The change in endothelium-dependent vascular reactivity will be measured by flow-mediated dilation (FMD) of the brachial artery using a high-resolution vascular ultrasound with a 10-MHz linear array transducer. FMD is expressed as the percentage increase in diameter at the baseline visit from pre-dosing with Intralipid to 12 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 12 hours at Baseline visit

Interventionpercent change in diameter (Mean)
Salsalate0.14
Carvedilol0.24
Placebo0.26

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Change in FFA (Free Fatty Acid) Levels From Baseline to 6 Weeks

Blood samples were collected for measurement of free fatty acids at baseline and 6 weeks after the Intralipid 20% infusion. FFA levels were determined by colorimetric method. Current guidelines identify normal range of FFA level as less than 0.72 mmol/L. Elevated plasma levels of FFA indicate a greater rate of insulin resistance. Change is the difference between 6-week FFA levels from baseline FFA levels. (NCT02406586)
Timeframe: Baseline, 6 weeks

Interventionmmol/L (Mean)
Salsalate-0.08
Carvedilol0.04
Placebo0.03

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Change in Expression of Inflammatory Biomarker Interleukin-6 (IL-6)

It is measured by using microsphere-based flow cytometric immunoassay. Change is the difference between 6-week level from baseline level. (NCT02406586)
Timeframe: Baseline, 6 weeks

Interventionpg/ml (Mean)
Salsalate-0.29
Carvedilol-1.84
Placebo-0.36

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Change in Expression of Inflammatory Biomarker C-Reactive Protein (CRP)

It is measured by using microsphere-based flow cytometric immunoassay. Change is the difference between 6-week inflammatory biomarker level from baseline level. (NCT02406586)
Timeframe: Baseline, 6 weeks

Interventionmg/dL (Mean)
Salsalate2.55
Carvedilol-7.08
Placebo-0.20

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Change in Diastolic Blood Pressure From Baseline to 6 Weeks

Diastolic blood pressure is the amount of pressure in the arteries when the heart is at rest between beats. Current guidelines identify normal diastolic blood pressure as lower than 80 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 8 hour infusion with subjects in supine position. Change is the difference between 6-week diastolic blood pressure from baseline diastolic blood pressure. (NCT02406586)
Timeframe: Baseline, 6 weeks

InterventionmmHg (Mean)
Salsalate1.00
Carvedilol-1.50
Placebo2.22

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at Week 6 from pre-dosing with Intralipid to 16 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 16 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate7.85
Carvedilol7.55
Placebo-0.04

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Change in Systolic Blood Pressure.

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 4 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 4 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate15.37
Carvedilol10.04
Placebo10.25

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. from Change is the difference in systolic blood pressure at the baseline visit from pre-dosing with Intralipid to 8 hours during Intralipid. (NCT02406586)
Timeframe: Pre-dose (Baseline), within 8 hours at Baseline visit

InterventionmmHg (Mean)
Salsalate13.02
Carvedilol2.03
Placebo5.47

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure from at Week 6 from pre-dosing with Intralipid to 8 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 8 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate10.1
Carvedilol11.62
Placebo4.14

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Change in Flow-mediated Dilation

The change in endothelium-dependent vascular reactivity will be measured by flow-mediated dilation (FMD) of the brachial artery using a high-resolution vascular ultrasound with a 10-MHz linear array transducer. FMD is expressed as the percentage increase in diameter at the Week 6 visit from pre-dosing with Intralipid to 24 hours during Intralipid infusion (NCT02406586)
Timeframe: Pre-dose (Week 6), within 24 hours at Week 6 visit

Interventionpercent change in diameter (Mean)
Salsalate0.39
Carvedilol0.70
Placebo0.48

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at Week 6 from pre-dosing with Intralipid to 24 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 24 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate11.23
Carvedilol9.92
Placebo3.04

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Change in Systolic Blood Pressure

Systolic blood pressure is the amount of pressure the heart generates when pumping blood through the arteries to the body. Current guidelines identify normal systolic blood pressure as lower than 120 mmHg. Blood pressure was measured in triplicate with a manual cuff prior to and every 4 hours during the 24-hour infusion with subjects in supine position. Change is the difference in systolic blood pressure at Week 6 from pre-dosing with Intralipid to 20 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 20 hours at Week 6 visit

InterventionmmHg (Mean)
Salsalate12.88
Carvedilol8.84
Placebo6.6

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Change in Flow-mediated Dilation

The change in endothelium-dependent vascular reactivity will be measured by flow-mediated dilation (FMD) of the brachial artery using a high-resolution vascular ultrasound with a 10-MHz linear array transducer. FMD is expressed as the percentage increase in diameter at the Week 6 visit from pre-dosing with Intralipid to 12 hours during Intralipid infusion. (NCT02406586)
Timeframe: Pre-dose (Week 6), within 12 hours at Week 6 visit

Interventionpercent change in diameter (Mean)
Salsalate0.22
Carvedilol0.42
Placebo0.20

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All Cause Mortality or Liver Transplantation

All cause mortality or liver transplantation during the study period (NCT02504723)
Timeframe: Within 6 years

InterventionParticipants (Count of Participants)
Cyanoacrylate Injection Plus Carvedilol13
Cyanoacrylate Injection20

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All Adverse Effects

All adverse effects during the study period (NCT02504723)
Timeframe: Within 6 years

InterventionParticipants (Count of Participants)
Cyanoacrylate Injection Plus Carvedilol32
Cyanoacrylate Injection9

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Rebleeding From Gastric Varices

Rebleeding from gastric varices during the follow-up period (NCT02504723)
Timeframe: Within 6 years

InterventionParticipants (Count of Participants)
Cyanoacrylate Injection Plus Carvedilol14
Cyanoacrylate Injection21

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All Upper Gastrointestinal Bleeding

All upper gastrointestinal bleeding during the follow-up period (NCT02504723)
Timeframe: Within 6 years

InterventionParticipants (Count of Participants)
Cyanoacrylate Injection Plus Carvedilol17
Cyanoacrylate Injection29

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Mean Change in Right Ventricular Ejection Fraction as Measured by Cardiac MRI

(NCT02507011)
Timeframe: 6 months

Interventionpercent (Mean)
Carvedilol10
Placebo2.5

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Average Left Ventricular End-diastolic Dimension

Thickness of cardiac muscle (in ml) of the left ventricle at the end of diastole. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionml (Mean)
BL6m12m18m24
Arm I (Carvedilol)4.58364.60354.6364.60324.5147
Arm II (Placebo)4.52694.5650.05564.54624.5976

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Average Left Ventricular End-diastolic Dimension

The amount of blood (in ml) in the heart's left ventricle just before the heart contracts. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionml (Mean)
BL6m12m18m24m
Arm I (Carvedilol)99.750799.3216102.378101.174100.659
Arm II (Placebo)93.315595.743496.500299.465698.9602

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Average Galectin-3

A protein produced by activated macrophages, and a member of a family of β-galactoside-binding lectings and promotes cardiac fibroblast proliferation and collagen synthesis following myocadial injury (in ng/ml). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionng/mL (Mean)
BL6m12m18m24m
Arm I (Carvedilol)4.44644.32523.73453.45483.8073
Arm II (Placebo)5.25384.37354.34154.02144.0791

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Average Fractional Shortening

A measure to assess preload and afterload (in %). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionpercent (Mean)
BL6m12m18m24
Arm I (Carvedilol)28.536228.540929.612127.821928.0302
Arm II (Placebo)28.433927.686628.108527.889128.5953

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Average Ejection Fraction

The percentage of blood leaving the heart at the end of diastole. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
InterventionPercent (Mean)
BL6m12m18m24
Arm I (Carvedilol)57.658.1658.0757.3558.16
Arm II (Placebo)57.4256.8456.6157.657.5

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Average Cardiac Troponin I

Troponin I is a biomarker for myocardial cell injury (in ng/ml). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionng/mL (Mean)
BL6m12m18m24m
Arm I (Carvedilol)0.004460.002650.004670.007370.01111
Arm II (Placebo)0.00110.001740.007420.006840.01132

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Average Cardiac N-terminal Pro B-type Natriuretic Peptide

N-terminal pro b-type natriuretic peptide- a biomarker for heart failure (in pg/ml). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionpg/mL (Mean)
BL6m12m18m24m
Arm I (Carvedilol)85.630190.753687.716799.4912101.8333
Arm II (Placebo)115.7222128.9565115.636493.2105107.849

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Average Bilirubin

A liver function measurement (in mg/dL). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionmg/dL (Mean)
BL6m12m18m24m
Arm I (Carvedilol)0.56340.59730.5630.5930.5561
Arm II (Placebo)0.49890.49420.49690.5070.5449

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"Proportion of Patients Who Responded Moderately, Quite a Bit, or Extremely to How Bothersome the Symptom of DIARRHEA Was at Any Post-day 0 Assessment Time Point."

"In a questionnaire, patients responded Yes/No to certain symptoms. If answered Yes, they selected slightly, moderately, quite a bit, or extremely regarding how bothersome the symptom was. The proportion of participants responding with any of these three categories was calculated by arm, and corresponding 95% confidence intervals are reported." (NCT02717507)
Timeframe: responses at days 14 to 730 were combined

,
InterventionProportion of patients (Number)
DiarrheaSkin rashItchy skinDry MouthEasy bruisingNosebleedsSunburn easilyWeight gainFluid retentionSwollen feetIncreased sweatingFeeling weak in parts of your bodyShortness of breath or wheezingChest pain or heavinessHeart racing or skipping beatsFeeling shaky or having tremorsDecreased bodily movementFeeling nervousFeeling downhearted, sad, and/or tearfulMood swingsDizziness and/or lightheadednessDizziness upon standing (from sitting or lying down)InsomniaDifficulty concentratingInterrupted sleepTendency to take napsTiredwheezingFeeling unusually tiredFalling asleep at inappropriate timesRinging in the earsDifficulty breathingSensation that I have to urinate much of the timeDiscoloration of urine (ie, bloody)Decreased libidoUnusually heavy menstrual flows (N/A if postmenopausal or male)
Arm I (Carvedilol)0.05330.09330.14670.06670.01330.06670.09330.05330.026700.09330.09330.09330.080.080.05330.01330.14670.20.120.160.14670.17330.10670.20.120.22670.02670.05330.02670.066700.06670.2
Arm II (Placebo)0.13160.07890.14470.17110.09210.05260.05260.07890.03950.09210.07890.13160.03950.09210.03950.07890.03950.17110.11840.09210.13160.15790.17110.13160.21050.10530.22370.03950.092100.07890.03950.05260.111

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Proportion of Patients With Reportable Adverse Events as Described in the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE).

Patients with toxicities reported via CTEP-AERS and all Grade ≥ 2 adverse events (AEs) that can be attributed probably or definitely to the study drug are considered to have AEs. The proportion of patients with AEs are reported by arm with corresponding 95% confidence intervals. (NCT02717507)
Timeframe: From baseline to month 24 since baseline

InterventionProportion of patients with AE (Number)
Arm I (Carvedilol)0.0267
Arm II (Placebo)0

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Proportion of Participants With Average Adherence > 90%

The number of pills taken out of the total prescribed in a 3-month period, averaged across all study time points. The proportion of participants with average adherence rate >90% is computed by arm and corresponding 95% confidence intervals are reported. (NCT02717507)
Timeframe: Average adherence across 6 months, 12 months, 18 months, 24 months after treatment initiation are calculated.

Interventionproportion of participants (Number)
Arm I (Carvedilol)0.483
Arm II (Placebo)0.517

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Average Aspartate Aminotransferase

A liver function measurement (in U/L). Normal range is 14-20 for men, 10-36 for women. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
InterventionIU/L (Mean)
BL6m12m18m24m
Arm I (Carvedilol)26.60824.06825.42624.37524.561
Arm II (Placebo)25.77326.34227.01428.41127.038

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Average Alanine Aminotransferase

A liver function measurement (in U/L). Normal range is 8-48 IU/L. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
InterventionIU/L (Mean)
BL6m12m18m24m
Arm I (Carvedilol)29.12228.01430.14827.19629.86
Arm II (Placebo)30.46732.15831.15530.53629.245

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Average Peak Early Atrial Divided by Peak Late Atrial Velocities

"Ratio of peak velocity blood flow from left ventricular relaxation in early diastole (E wave) to peak velocity flow in late diastole caused by atrial contraction (A wave). Number shown for Unit of Measure refers to this ratio. Normal: >1. Impaired: <1. The mean is reported by arm at each timepoint with corresponding standard errors." (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionratio (Mean)
BL6m12m18m24m
Arm I (Carvedilol)1.7281.6421.7231.7321.603
Arm II (Placebo)1.7320.0711.7221.7321.64

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Average Left-Ventricular Wall Thickness-Dimension Ratio Z-score (LVWT/Dz)

Z-score of the ratio of left ventricular (LV) posterior wall dimension of systole to internal LV dimension in diastole, calculated for each subject by subtracting the reference healthy population mean, then dividing by the standard deviation. The Z-score indicates the number of standard deviations away from the mean of the reference population. Negative Z- score indicates worse outcome. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionz-score (Mean)
BL6m12m18m24m
Arm I (Carvedilol)-0.1372-0.2167-0.2416-0.23750.0213
Arm II (Placebo)-0.08930.3215-0.2367-0.19740.1834

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Average Left Ventricular Mass

The weight of the left ventricle adjusted for body surface area (in g/m2). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventiong/m2 (Mean)
BL6m12m18m24m
Arm I (Carvedilol)57.486258.283960.211657.705358.3315
Arm II (Placebo)57.932257.092459.450859.179359.1026

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Average Left Ventricular End-systolic Wall Stress

Echocardiographic measure of left ventricular (LV) afterload based on LV pressure (P), volume (V), and wall thickness (T), calculated by the formula (P x V)/T, which equals the number referred to below in the Measure Type. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventiong/cm^2 (Mean)
BL6m12m18m24m
Arm I (Carvedilol)93.289290.308888.98493.926789.2513
Arm II (Placebo)90.613596.835696.061691.645894.0647

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Average N-terminal Pro B-type Natriuretic Peptide

B-type natriuretic peptide- a biomarker for heart failure (in pg/ml). The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionpg/mL (Mean)
BL6m12m18m24m
Arm I (Carvedilol)27.383631.840626.820335.80734.625
Arm II (Placebo)31.432434.185733.294132.280733.3774

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Average Left Ventricular End-systolic Volume

The amount of blood (in ml) in the heart's left ventricle just after the heart contracts. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventionml (Mean)
BL6m12m18m24m
Arm I (Carvedilol)42.219341.612842.843743.145342.0086
Arm II (Placebo)39.735441.383941.81131.60542.442

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Average Left Ventricular End-systolic Volume

The amount of blood (in ml) in the heart's left ventricle just after the heart contracts. The mean is reported by arm at each timepoint with corresponding standard errors. (NCT02717507)
Timeframe: Baseline before treatment, 6 months, 12 months, 18 months, 24 months after treatment initiation

,
Interventioncentimeter (Mean)
BL6m12m18m24m
Arm I (Carvedilol)03.27653.29013.2623.323.2441
Arm II (Placebo)3.23963.30233.29643.27983.286

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Change in Peak Heart Rate

during exercise test on week 12 and week 30 (NCT02946892)
Timeframe: on week 12 and week 30 of the study

Interventionbeats per minute (Mean)
Carvedilol-32.3
Placebo1.9

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Change in Oxygen Uptake at Anaerobic Threshold

during exercise test on week 12 and week 30 (NCT02946892)
Timeframe: on week 12 and week 30 of the study

Interventionml/kg/min (Mean)
Carvedilol-1.02
Placebo-1.78

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Change in Peak Oxygen Uptake From Baseline Peak Oxygen Uptake

during exercise test on week 12 and week 30 (NCT02946892)
Timeframe: on week 12 and week 30 of the study

Interventionml/kg/min (Mean)
Carvedilol-2.01
Placebo-1.01

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Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)

"The PROMIS-29 assesses 7 domains with 4 questions with an additional pain intensity numeric rating scale. The patients' answers to the PROMIS-29 are scored from 1-5 (except for the pain numeric rating scale). The sum of the PROMIS-29 is the raw score transformed into a final T-score metric. Scores are mapped so that the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the PROMIS-29 raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse health compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker before enrollment, therefore, each subject's respective period for the OFF and ON periods could range between 3 - 6 weeks. The values measured over the time points were averaged." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

,
Interventionscore on a scale (Mean)
Physical Health ComponentMental Health Component
OFF Beta Blockers40.047.9
ON Beta Blockers39.846.8

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Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device

"The wearable activity monitoring device measures daily step count. Due to the nature of N-of-1 trials, the duration of a subject's periods varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 and 6 weeks. We will compare average step counts over 2-week periods, which will be the final 2 weeks of each period when subjects are either on their home (ON Beta Blockers) or minimally tolerated (OFF Beta Blockers) dose. The outcome measure data is the mean collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 8-weeks (last 2 weeks of each period for up to 4 periods).

InterventionCount of Steps (Mean)
ON Beta Blockers2790.5
OFF Beta Blockers3167.3

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Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)

"The EuroQol-5D Visual Analogue System (EQ-5D VAS) indicates patient-perceived health on a vertical visual analogue scale. The scale ranges from 0, indicating poorest health, to 100, indicating the best health. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers68.9
OFF Beta Blockers67.8

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Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)

"The Kansas City Cardiomyopathy Questionnaire (KCCQ-12) is a heart failure-specific health status survey. Questions are ranked on 5- to 7-point Likert scales, with higher scores indicating better health status. KCCQ scores are scaled from 0 to 100 and frequently summarized in 25-point ranges, where scores represent health status as follows: 0 to 24: very poor to poor; 25 to 49: poor to fair; 50 to 74: fair to good; and 75 to 100: good to excellent. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The max amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, bi-weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers58.7
OFF Beta Blockers66.0

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Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The chair rise portion of the SPPB assesses core strength. When comparing the number of seconds it takes to complete 5 chair rises, quicker speeds indicate better core strength. Our research team has chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers16
OFF Beta Blockers15.1

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Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)

"Cardiopulmonary exercise testing (CPET) measures breath-by-breath oxygen production during symptom-limited exercise on a stationary bike. This permits the calculation of peak oxygen consumption (VO2). Percent predicted peak VO2 for body weight will also be calculated. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 6-weeks. This outcome was measured at the end of the first and second visit.

Interventionml/kg/min (Mean)
ON Beta Blockers10.0
OFF Beta Blockers11.4

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Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The balance test portion of the SPPB assesses the subject's ability to stand unassisted without the use of a cane or walker. Balance test scores range from 0 - 4 with higher scores indicating better ability to stand unassisted. Our research team conducted the balance test according to SPPB standards. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers3.9
OFF Beta Blockers3.6

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Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The gait speed portion of the SPPB assesses the subject's lower extremity function. When comparing the number of seconds it takes to complete the 4-meter gait speed test, quicker speeds indicate better lower extremity function. Our research team conducted the 4-meter gait speed test according to SPPB standards, but have chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers4.3
OFF Beta Blockers4.6

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Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)

"Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a) is a survey of patient-perceived cognitive deficits. Questions are ranked on a 5-point Likert scale, with higher scores indicating better cognitive function. Scores are mapped so the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse cognitive function compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3-6 weeks. The outcome measure data is the mean of the data collected during the span of the measured time points." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers53.8
OFF Beta Blockers52.4

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Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)

"Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function) measures self-reported sexual function and satisfaction. Questions are ranked on a 6-point Likert scale, with higher scores indicating poorer sexual function and satisfaction. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame. The score ranges from 0-10 with higher scores meaning worsened sexual function." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers1.8
OFF Beta Blockers2.1

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