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药品详细

Phenoxybenzamine(酚苄明)

化学结构式图
中文名
酚苄明
英文名
Phenoxybenzamine
分子式
C18H22ClNO
化学名
benzyl(2-chloroethyl)(1-phenoxypropan-2-yl)amine
分子量
Average: 303.826
Monoisotopic: 303.138992038
CAS号
59-96-1
ATC分类
C04A 未知
药物类型
small molecule
阶段
approved
商品名
Bensylyt;Bensylyt Nen;Bensylyte;Benzylyt;Dibenylin;Dibenyline;Dibenzylene;Dibenzyline;Dibenzyline Hydrochloride;Dibenzyran;
同义名
Fenossibenzamina [Dcit];Fenoxibenzamina [INN-Spanish];Phenoxybenzamine Hcl;Phenoxybenzamine Hydrochloride;Phenoxybenzaminum [INN-Latin];POB HCl;
基本介绍

An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. [PubChem]

生产厂家
  • Wellspring pharmaceutical corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Caine M, Perlberg S, Meretyk S: A placebo-controlled double-blind study of the effect of phenoxybenzamine in benign prostatic obstruction. Br J Urol. 1978 Dec;50(7):551-4. Pubmed
  2. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenols and Derivatives
  • Ethers
  • Anisoles
  • Phenyl Esters
Substructures
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Alkyl Halides
  • Aromatic compounds
  • Anisoles
  • Phenyl Esters
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication For the treatment of phaeochromocytoma (malignant), benign prostatic hypertrophy and malignant essential hypertension.
Pharmacodynamics Phenoxybenzamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phenoxybenzamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phenoxybenzamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phenoxybenzamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure.
Mechanism of action Phenoxybenzamine produces its therapeutic actions by blocking alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure.
Absorption Twenty to 30 percent of orally administered phenoxybenzamine appears to be absorbed in the active form.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life 24 hours
Clearance Not Available
Toxicity Symptoms of overdose are largely the result of block of the sympathetic nervous system and of the circulating epinephrine. They may include postural hypotension resulting in dizziness or fainting, tachycardia, particularly postural, vomiting; lethargy, and shock.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 39 °C PhysProp
logP 4.7 Not Available
Predicted Properties
Property Value Source
water solubility 1.03e-02 g/l ALOGPS
logP 4.26 ALOGPS
logP 4.64 ChemAxon
logS -4.5 ALOGPS
pKa (strongest basic) 7.97 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 12.47 ChemAxon
rotatable bond count 8 ChemAxon
refractivity 88.92 ChemAxon
polarizability 34.09 ChemAxon
药物相互作用
Drug Interaction
Tadalafil Tadalafil may enhance the hypotensive effect of Phenoxybenzamine. Monitor for hypotension during concomitant therapy.
Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Phenoxybenzamine, may result in additive antihypertensive effects. Combination therapy is not recommended.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Vardenafil Additive hypotensive effects of the PDE5 inhibitor, Vardenafil, and alpha1-blocker, Phenoxybenzamine, may occur. Monitor for hypotension during concomitant therapy.
食物相互作用
Not Available

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