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药品详细

Papaverine(罂粟碱)

化学结构式图
中文名
罂粟碱
英文名
Papaverine
分子式
C20H21NO4
化学名
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinoline
分子量
Average: 339.385
Monoisotopic: 339.147058165
CAS号
61-25-6
ATC分类
A03A Drugs for Functional Bowel Disorders;G04B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Tang Y, Luan J, Zhang X: Accelerating tissue expansion by application of topical papaverine cream. Plast Reconstr Surg. 2004 Oct;114(5):1166-9. Pubmed
    2. Liu JK, Couldwell WT: Intra-arterial papaverine infusions for the treatment of cerebral vasospasm induced by aneurysmal subarachnoid hemorrhage. Neurocrit Care. 2005;2(2):124-32. Pubmed
    3. Takeuchi K, Sakamoto S, Nagayoshi Y, Nishizawa H, Matsubara J: Reactivity of the human internal thoracic artery to vasodilators in coronary artery bypass grafting. Eur J Cardiothorac Surg. 2004 Nov;26(5):956-9. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzylisoquinolines
    Substructures
    • Phenols and Derivatives
    • Benzylisoquinolines
    • Pyridines and Derivatives
    • Ethers
    • Benzene and Derivatives
    • Catechols
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Imines
    • (Iso)quinolines and Derivatives
    • Phenyl Esters
    适应症
    药理
    Indication For the treatment of impotence and vasospasms.
    Pharmacodynamics Papaverine is a nonxanthine phosphodiesterase inhibitor for the relief of cerebral and peripheral ischemia associated with arterial spasm and myocardial ischemia complicated by arrhythmias. The main actions of Papaverine are exerted on cardiac and smooth muscle. Like qathidine, Papaverine acts directly on the heart muscle to depress conduction and prolong the refractory period. Papaverine relaxes various smooth muscles. This relaxation may be prominent if spasm exists. The muscle cell is not paralyzed by Papaverine and still responds to drugs and other stimuli causing contraction. The antispasmodic effect is a direct one, and unrelated to muscle innervation. Papaverine is practically devoid of effects on the central nervous system. Papaverine relaxes the smooth musculature of the larger blood vessels, especially coronary, systemic peripheral, and pulmonary arteries.
    Mechanism of action Perhaps by its direct vasodilating action on cerebral blood vessels, Papaverine increases cerebral blood flow and decreases cerebral vascular resistance in normal subjects; oxygen consumption is unaltered. These effects may explain the benefit reported from the drug in cerebral vascular encephalopathy.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding ~90%
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life 0.5-2 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 226 (dec) °C PhysProp
    logP 3 Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.29e-02 g/l ALOGPS
    logP 4.19 ALOGPS
    logP 3.08 ChemAxon
    logS -4.4 ALOGPS
    pKa (strongest basic) 6.03 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 49.81 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 95.52 ChemAxon
    polarizability 36.57 ChemAxon
    药物相互作用
    Drug Interaction
    Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
    Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
    食物相互作用
    Not Available

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