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Colchicine

产品号 DB01394 公司名称 DrugBank
CAS号 64-86-8 公司网站 http://www.ualberta.ca/
分子式 C22H25NO6 电 话 (780) 492-3111
分子量 399.437 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 1205

产品价格信息

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产品别名

标题
Colchicine
IUPAC标准名
N-[(10S)-3,4,5,14-tetramethoxy-13-oxotricyclo[9.5.0.0^{2,7}]hexadeca-1(16),2(7),3,5,11,14-hexaen-10-yl]acetamide
IUPAC传统名
colchicine
商标名
Col-probenecid
Colbenemid
Condylon
Proben-C
别名
Colchicina
Colchicin
Colchicinum

产品登记号

CAS号 64-86-8

产品性质

疏水性(logP) 1.30 [HANSCH,C ET AL. (1995)]
溶解度 45 mg/mL at 25 oC [SEIDELL,A (1941)]

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description A major alkaloid from Colchicum autumnale L. and found also in other Colchicum species. Its primary therapeutic use is in the treatment of gout, but it has been used also in the therapy of familial Mediterranean fever (periodic disease). [PubChem]
Indication For treatment and relief of pain in attacks of acute gouty arthritis.
Pharmacology Colchicine is a highly poisonous alkaloid, originally extracted from plants of the genus Colchicum (Autumn crocus, also known as the "Meadow saffron"). Originally used to treat rheumatic complaints and especially gout, it was also prescribed for its cathartic and emetic effects. Its present medicinal use is mainly in the treatment of gout; as well, it is being investigated for its potential use as an anti-cancer drug. It can also be used as initial treatment for pericarditis and preventing recurrences of the condition.
Toxicity The onset of toxic effects is usually delayed for several hours or more after the ingestion of an acute overdose. Nausea, vomiting, abdominal pain, and diarrhea occur first. The diarrhea may be bloody due to hemorrhagic gastroenteritis. Burning sensations of the throat, stomach, and skin may be prominent symptoms. Extensive vascular damage may result in shock. Kidney damage, evidenced by hematuria and oliguria, may occur. Muscular weakness may be marked, and ascending paralysis of the central nervous system may develop; the patient usually remains conscious. Delirium and convulsions may occur. Death due to respiratory arrest may result. Although death from the ingestion of as little as 7 mg has been reported, much larger doses have been survived .
Affected Organisms
Humans and other mammals
Biotransformation Probably hepatic. Although colchicine metabolites have not been identified in humans, metabolism by mammalian hepatic microsomes has been demonstrated in vitro.
Absorption Colchicine is rapidly absorbed after oral administration, probably from the jejunum and ileum. However, the rate and extent of absorption are variable, depending on the tablet dissolution rate; variability in gastric emptying, intestinal motility, and pH at the absorption site; and the extent to which colchicine is bound to microtubules in gastrointestinal mucosal cells.
Half Life Elimination half-life is approximately 1 hour in healthy subjects, although a study with an extended sampling time reported mean terminal elimination half-life values of approximately 9 to 10.5 hours. Other studies have reported half-life values of approximately 2 hours in patients with alcoholic cirrhosis and approximately 2.5 hours in patients with familial Mediterranean fever.
Protein Binding Low to moderate (30 to 50%).
Elimination In healthy volunteers (n=12) 40 – 65% of 1 mg orally administered colchicine was recovered unchanged in urine.
Enterohepatic recirculation and biliary excretion are also postulated to play a role in colchicine elimination.
Distribution * 5 to 8 L/kg [healthy young volunteers]
Clearance * 0.17 L/hr/kg [familial Mediterranean fever patients with end-stage renal disease]
* 0.73 L/hr/kg [familial Mediterranean fever patients with normal renal function]
External Links
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RxList
Drugs.com

参考文献