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药品详细

Alverine(阿尔维林)

化学结构式图
中文名
阿尔维林
英文名
Alverine
分子式
C20H27N
化学名
ethylbis(3-phenylpropyl)amine
分子量
Average: 281.4351
Monoisotopic: 281.214349869
CAS号
150-59-4
ATC分类
A03A Drugs for Functional Bowel Disorders
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. Alverine acts directly on the muscle in the gut, causing it to relax. This prevents the muscle spasms which occur in the gut in conditions such as irritable bowel syndrome and diverticular disease. It is used to relieve cramps or spasms of the stomach and intestines. It is also useful in treating irritable bowel syndrome (IBS) and similar conditions. It can also be used to help relieve period pain. Alverine is formulated as the citrate salt (5982-87-6).

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Hayase M, Hashitani H, Suzuki H, Kohri K, Brading AF: Evolving mechanisms of action of alverine citrate on phasic smooth muscles. Br J Pharmacol. 2007 Dec;152(8):1228-38. Epub 2007 Oct 15. Pubmed
    2. Wittmann T, Paradowski L, Ducrotte P, Bueno L, Andro Delestrain MC: Clinical trial: the efficacy of alverine citrate/simeticone combination on abdominal pain/discomfort in irritable bowel syndrome—a randomized, double-blind, placebo-controlled study. Aliment Pharmacol Ther. 2010 Mar;31(6):615-24. Epub 2009 Dec 10. Pubmed
    3. Ju D, Wang X, Xie Y: Dyclonine and alverine citrate enhance the cytotoxic effects of proteasome inhibitor MG132 on breast cancer cells. Int J Mol Med. 2009 Feb;23(2):205-9. Pubmed
    4. Spasmonal Package Insert
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenylpropylamines
    Substructures
    • Benzene and Derivatives
    • Aliphatic and Aryl Amines
    • Aromatic compounds
    • Phenylpropylamines
    适应症
    药理
    Indication Used to relieve cramps or spasms of the stomach and intestines. It is also useful in treating irritable bowel syndrome (IBS) and similar conditions. It can also be used to help relieve period pain. Alverine citrate is also under investigation to increase the cytotoxic effects of the proteasome inhibitor MG132 on breast cancer cells.
    Pharmacodynamics Alverine is a smooth muscle relaxant. Smooth muscle is a type of muscle that is not under voluntary control; it is the muscle present in places such as the gut and uterus. Alverine acts directly on the muscle in the gut, causing it to relax. This prevents the muscle spasms which occur in the gut in conditions such as irritable bowel syndrome and diverticular disease. Diverticular disease is a condition in which small pouches form in the gut lining. These pouches can trap particles of food and become inflamed and painful. In irritable bowel syndrome the normal activity of the gut muscle is lost. The muscle spasms result in symptoms such as heartburn, abdominal pain and bloating, constipation or diarrhoea. By relaxing the gut muscle, alverine citrate relieves the symptoms of this condition. Alverine also relaxes the smooth muscle in the womb (uterus). It is therefore also used to treat painful menstruation, which is caused by muscle spasms in the uterus (dysmenorrhea).
    Mechanism of action Not Available
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Rapidly converted to its primary active metabolite, which is then further converted to two secondary metabolites.
    Route of elimination High renal clearance of all metabolites indicating that they are eliminated by active renal secretion.
    Half life The plasma half-life averages 0.8 hours for alverine and 5.7 hours for the active primary metabolite.
    Clearance Not Available
    Toxicity Can produce hypotension and atropine-like toxic effects. Fatality has occurred following overdose with very high doses.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point < 25 °C PhysProp
    boiling point 212.5 °C at 1.30E+01 mm Hg PhysProp
    Predicted Properties
    Property Value Source
    water solubility 9.60e-04 g/l ALOGPS
    logP 5.73 ALOGPS
    logP 5.46 ChemAxon
    logS -5.5 ALOGPS
    pKa (strongest basic) 10.44 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 1 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 3.24 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 92.67 ChemAxon
    polarizability 35.42 ChemAxon
    药物相互作用
    Drug Interaction
    Donepezil Possible antagonism of action
    Galantamine Possible antagonism of action
    食物相互作用
    Not Available

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