用户名： 密   码：
注册 | 忘记密码？
药品详细

Terazosin(特拉唑嗪)

化学结构式图
中文名
特拉唑嗪
英文名
Terazosin
分子式
C19H25N5O4
化学名
6,7-dimethoxy-2-{4-[(oxolan-2-yl)carbonyl]piperazin-1-yl}quinazolin-4-amine
分子量
Average: 387.4329
Monoisotopic: 387.190654313
CAS号
63590-64-7
ATC分类
G04C 未知
药物类型
small molecule
阶段
approved
商品名
Blavin (Baliarda (Argentina));Flumarc (Raffo (Argentina));Fosfomic (Finadiet (Argentina));Heitrin (Abbott (Germany; discontinued));Hytracin;Hytrin (Abbott);Hytrinex (Amdipharm (Sweden));Itrin (Keryos (Italy));Urodie (Keryos (Italy));Vasomet;Vicard (Amdipharm (Austria));
同义名
Abbott 45975;Terazosin HCl;Terazosin hydrochloride;Terazosina [INN-Spanish];Terazosine;Terazosine [INN-French];Terazosinum [INN-Latin];Trazosin HCl;
基本介绍

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.

生产厂家
  • Abbott laboratories pharmaceutical products div
  • Apotex inc
  • Cadista pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan laboratories inc
  • Mylan technologies inc
  • Ranbaxy laboratories ltd
  • Sandoz inc
  • Teva pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. 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
剂型
规格
化合物类型
Type small molecule
Classes
  • Quinazolines
Substructures
  • Quinazolines
  • Phenols and Derivatives
  • Amino Ketones
  • Aliphatic and Aryl Amines
  • Piperazines
  • Ethers
  • Benzene and Derivatives
  • Pyrimidines and Derivatives
  • Catechols
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Carboxamides and Derivatives
  • Furans
  • Cyanamides
  • Phenyl Esters
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication For the treatment of symptomatic BPH and mild to moderate hypertension.
Pharmacodynamics 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.
Mechanism of action In general, α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α1-Receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (chromosome 20). Terazosin is the first α1-receptor antagonist to demonstrate selectivity for the α1A-receptor. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of α1-receptors activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Terozosin produces its pharmacological effects by inhibiting α1A-receptor activation. Inhibition of these receptors in the vasculature and prostate results in muscle relaxation, decreased blood pressure and improved urinary outflow in symptomatic benign prostatic hyperplasia.
Absorption Essentially completely absorbed in man (90% bioavailability).
Volume of distribution Not Available
Protein binding 90-94%
Metabolism
Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity.
Route of elimination Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.
Half life 12 hours
Clearance Not Available
Toxicity LD50=259.3mg/kg (IV in mice)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 273 °C PhysProp
water solubility 29.7mg/mL Not Available
logP 1 Not Available
Predicted Properties
Property Value Source
water solubility 1.50e+00 g/l ALOGPS
logP 1.12 ALOGPS
logP 1.18 ChemAxon
logS -2.4 ALOGPS
pKa (strongest acidic) 19.93 ChemAxon
pKa (strongest basic) 7.24 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 103.04 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 105.18 ChemAxon
polarizability 41.26 ChemAxon
药物相互作用
Drug Interaction
Acebutolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Alfuzosin Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
Amifostine Terazosin may increase the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Terazosin should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
Atenolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Betaxolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Bisoprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Carteolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Carvedilol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Celiprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Esmolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Labetalol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Metoprolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Nadolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Nebivolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Oxprenolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Penbutolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Pindolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Propranolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Rituximab Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Terazosin for 12 hours prior to administration of Rituximab.
Sildenafil Increased risk of hypotension.
Silodosin Additive antihypertensive effects may occur. Increase risk of orthostatic hypotension and syncope. Concomitant therapy should be avoided.
Sotalol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Tadalafil Tadalafil may enhance the hypotensive effect of Terazosin. Monitor for hypotension during concomitant therapy.
Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Terazosin, may result in additive antihypertensive effects. Combination therapy is not recommended.
Timolol Increased risk of hypotension. Initiate concomitant therapy cautiously.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Terazosin, may occur. Monitor for hypotension during concomitant therapy.
食物相互作用
Not Available

返回 | 收藏