物质信息
ID:1037
名称和标识
商标名
FlumarcFosfomicHytrinexItrinUrodieHytrinVicardVasometBlavinHeitrinHytracin
别名
Trazosin HClTerazosin hydrochlorideTerazosinTerazosina [INN-Spanish]Abbott 45975Terazosin HClTerazosineTerazosine [INN-French]Terazosinum [INN-Latin]
IUPAC标准名
6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine
IUPAC传统名
6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine
化合物性质
理化性质
疏水性(logP)
1
溶解度
29.7mg/mL
描述信息
Drug Groups
approved
Description
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Indication
For the treatment of symptomatic BPH and mild to moderate hypertension.
Pharmacology
Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an α-adrenergic blocking agent, terazosin is used to treat hypertension and BPH. Terazosin produces vasodilation and reduces peripheral resistance but in general has only a slight effect on cardiac output. The antihypertensive effect with chronic dosing is not usually accompanied by reflex tachycardia.
Toxicity
LD50=259.3mg/kg (IV in mice)
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity.
Absorption
Essentially completely absorbed in man (90% bioavailability).
Half Life
12 hours
Protein Binding
90-94%
Elimination
Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.
References
•
Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404.
[Pubmed]
External Links
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参考文献
• Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. Pubmed