Page last updated: 2024-12-06

trimazosin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Trimazosin is an α1-adrenergic receptor antagonist, used to treat benign prostatic hyperplasia (BPH). It was originally developed for treatment of hypertension but has since been shown to be particularly effective in reducing the symptoms of BPH, such as difficulty urinating and frequent urination. Trimazosin is available as a capsule and is typically taken once daily. It works by relaxing the smooth muscle in the prostate gland and bladder neck, which improves urine flow. Trimazosin is generally well-tolerated, although it can cause side effects such as dizziness, lightheadedness, and fatigue. It is important to note that trimazosin can interact with other medications, so it is important to talk to your doctor about all the medications you are taking before starting trimazosin. Research into trimazosin continues to explore its potential applications in areas such as cardiovascular health and the treatment of other conditions related to smooth muscle function.'

trimazosin: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID37264
CHEMBL ID513301
CHEBI ID135710
SCHEMBL ID113671
MeSH IDM0046551

Synonyms (35)

Synonym
OPREA1_036455
trimazosinum [inn-latin]
4-(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-1-piperazinecarboxylic acid, 2-hydroxy-2-methylpropyl ester
1-piperazinecarboxylic acid, 4-(4-amino-6,7,8-trimethoxy-2-quinolinyl)-, 2-hydroxy-2-methylpropyl ester
2-hydroxy-2-methylpropyl 4-(4-amino-6,7,8-trimethoxy-2-chinazolinyl)-1-piperazinylcarboxylat
trimazosine [inn-french]
trimazosin
trimazosino [inn-spanish]
einecs 252-732-7
trimazosin [inn:ban]
L013382
CHEBI:135710
(2-hydroxy-2-methylpropyl) 4-(4-amino-6,7,8-trimethoxyquinazolin-2-yl)piperazine-1-carboxylate
trimazosin (inn)
D08212
35795-16-5
CHEMBL513301
trimazosino
trimazosine
trimazosinum
31l760807h ,
unii-31l760807h
trimazosin [who-dd]
trimazosin [inn]
trimazosin [mi]
SCHEMBL113671
DB09206
DTXSID50189319
FT-0730646
Q1324057
boc-(r)-3-amino-4-(4-bromo-phenyl)-butyricacid
CS-0026043
HY-106554
35795-16-5 (free base)
4-(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-1-piperazinecarboxylic acid 2-hydroxy-2-methylpropyl ester hydrochloride

Research Excerpts

Overview

Trimazosin is a quinazoline antihypertensive agent structurally related to the selective alpha 1-adrenoceptor blocker prazosin. It improves ventricular function in patients with left ventricular failure.

ExcerptReferenceRelevance
"Trimazosin is a quinazoline antihypertensive agent structurally related to the selective alpha 1-adrenoceptor blocker prazosin. "( The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade.
Constantine, JW; Lebel, W; Weeks, R,
)
1.87
"Trimazosin is a long-acting orally effective vasodilator which improves ventricular function in patients with left ventricular failure."( Effect of trimazosin on hemodynamics in chronic heart failure.
Aronow, WS; Danahy, DT; Lurie, M; Orlando, JR, 1978
)
1.38
"Trimazosin is a new quinazoline derivative vasodilator previously thought to act primarily on resistance vessels. "( Hemodynamic effects of trimazosin in patients with left ventricular failure.
Cohn, JN; Franciosa, JA, 1978
)
2.01

Effects

Trimazosin has the potential to cause sustained improvement in left ventricular function, both at rest and during exercise, in patients with chronic CHF. TrimazOSin has been shown previously to have less affinity for alpha 1-adrenoceptors than prazosin.

ExcerptReferenceRelevance
"Thus trimazosin has the potential to cause sustained improvement in left ventricular function, both at rest and during exercise, in patients with chronic CHF."( Trimazosin in chronic congestive heart failure: improved left ventricular function at rest and during exercise.
Avakian, D; Chatterjee, K; Parmley, WW; Ports, TA; Wilkinson, P, 1983
)
2.16
"Trimazosin has been shown previously to have less affinity for alpha 1-adrenoceptors than prazosin."( The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade.
Constantine, JW; Lebel, W; Weeks, R,
)
1.15

Actions

ExcerptReferenceRelevance
"Trimazosin did not increase plasma norepinephrine concentration at rest, suggesting that in the dosage used trimazosin caused selective alpha 1-receptor blockade.(ABSTRACT TRUNCATED AT 250 WORDS)"( Attenuation of coronary vascular resistance by selective alpha 1-adrenergic blockade in patients with coronary artery disease.
Barry, WH; Colucci, WS; Ganz, P; Gaspar, J; Horowitz, JD; Kern, MJ; Lorell, BH; Mudge, GH, 1985
)
0.99

Toxicity

ExcerptReferenceRelevance
" The side effect profile of trimazosin was comparable to placebo and significantly better than that of either methyldopa or propranolol."( Profile of trimazosin: an effective and safe antihypertensive agent.
Falkner, FC; Leader, JP; Munster, EW; O'Neil, JA; Singleton, W; Taylor, CR, 1983
)
0.95

Pharmacokinetics

Eight patients in whom the blood pressure was not normalized with a diuretic alone underwent pharmacokinetic studies and assessment of the renal function.

ExcerptReferenceRelevance
"The description of the relationship between different responses measured simultaneously in the same subject is commonly described in terms of specific pharmacokinetic models such as linear compartmental models."( Linear and nonlinear system approaches in pharmacokinetics: how much do they have to offer? II. The response mapping operator (RMO) approach.
Veng-Pedersen, P, 1988
)
0.27
"A general theoretical framework is constructed for the relationship between a pharmacokinetic response r (e."( A system approach to pharmacodynamics. I: Theoretical framework.
Gillespie, WR; Veng-Pedersen, P, 1988
)
0.27
" The IV and oral drug and metabolite (1-hydroxytrimazosin) concentration data are fitted simultaneously to the same pharmacokinetic model."( Modelling the pharmacokinetics and pharmacodynamics of trimazosin.
Elliott, HL; Kelman, AW; Meredith, PA; Reid, JL,
)
0.64
" Eight patients in whom the blood pressure was not normalized with a diuretic alone underwent pharmacokinetic studies and assessment of the renal function during a 10-week period of trimazosin therapy."( Pharmacokinetics of trimazosin and its effects on blood pressure, renal function and proteinuria during short-term therapy of patients with impaired renal function and hypertension.
Donker, AJ; Oe, PL; van der Meulen, J; van Kalken, CK; Vriesendorp, R, 1986
)
0.79
" Pharmacokinetic parameters were obtained by computer-assisted, nonlinear, least-squares-fitting regression analysis."( Pharmacokinetics and pharmacodynamics of trimazosin in man.
Elliott, HL; Meredith, PA; Reid, JL, 1983
)
0.53
"3 mg/L), time to peak was strongly delayed by a factor 7, and the time when plasma concentrations were higher than half of Cmax (t Cmax/2) was longer (10."( Pharmacokinetics of a sustained-release trimazosin tablet formulation.
Bianchine, JR; Flouvat, B; Fodor, F; Roux, A, 1983
)
0.53
"The pharmacokinetic and pharmacodynamic profiles of intravenous trimazosin, a postsynaptic alpha 1 antagonist, were analyzed empirically by integrated modelling techniques."( Pharmacokinetic and pharmacodynamic modelling of trimazosin and its major metabolite.
Elliott, HL; Kelman, AW; Meredith, PA; Reid, JL, 1983
)
0.76
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

Pharmacokinetics and bioavailability of a trimazosin sustained-release tablet (SRT) formulation (300 mg) were studied in healthy volunteers. The bioavailability was 61 +/- 28%.

ExcerptReferenceRelevance
" Kinetic analysis showed oral bioavailability of 63%, a clearance rate of 66 ml/min, and a terminal elimination t1/2 of approximately 3 hr."( Trimazosin in normotensive subjects.
Elliott, HL; Hughes, DM; Meredith, PA; Reid, JL; Vincent, J, 1984
)
1.71
" The bioavailability of oral trimazosin was 61 +/- 28%."( Pharmacokinetics and pharmacodynamics of trimazosin in man.
Elliott, HL; Meredith, PA; Reid, JL, 1983
)
0.82
"Pharmacokinetics and bioavailability of a trimazosin sustained-release tablet (SRT) formulation (300 mg) were studied in healthy volunteers."( Pharmacokinetics of a sustained-release trimazosin tablet formulation.
Bianchine, JR; Flouvat, B; Fodor, F; Roux, A, 1983
)
0.8

Dosage Studied

Both oral and intravenous trimazosin caused a significant rightward shift of the phenylephrine pressor dose-response curve (p less than 0.0) Trimazosins did not increase plasma norepinephrine concentration at rest, suggesting that in the dosage used it caused selective alpha 1-receptor blockade.

ExcerptRelevanceReference
" This difference in drug efficacy persisted throughout the 12-hour dosing interval."( Discrepancy between clinic and ambulatory blood pressure measurement in the evaluation of two antihypertensive agents.
Cox, JP; Fitzgerald, DJ; O'Brien, E; O'Malley, K, 1989
)
0.28
" Trimazosin did not increase plasma norepinephrine concentration at rest, suggesting that in the dosage used trimazosin caused selective alpha 1-receptor blockade."( Attenuation of coronary vascular resistance by selective alpha 1-adrenergic blockade in patients with coronary artery disease.
Barry, WH; Colucci, WS; Ganz, P; Gaspar, J; Horowitz, JD; Kern, MJ; Lorell, BH; Mudge, GH, 1985
)
1.18
" Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles."( Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat.
Buyniski, JP; Campbell, JA; Pircio, AW; Schurig, JE, 1980
)
0.54
" This hypotensive effect was maximal between 4 and 6 hr after dosing and was accompanied by a significant increase in heart rate."( Trimazosin in normotensive subjects.
Elliott, HL; Hughes, DM; Meredith, PA; Reid, JL; Vincent, J, 1984
)
1.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-arylpiperazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
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.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (64)

TimeframeStudies, This Drug (%)All Drugs %
pre-199060 (93.75)18.7374
1990's1 (1.56)18.2507
2000's3 (4.69)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.26

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.26 (24.57)
Research Supply Index4.62 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials29 (40.85%)5.53%
Reviews9 (12.68%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other33 (46.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]