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Amantadine

产品号 DB00915 公司名称 DrugBank
CAS号 768-94-5 公司网站 http://www.ualberta.ca/
分子式 C10H17N 电 话 (780) 492-3111
分子量 151.24868 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 791

产品价格信息

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产品别名

标题
Amantadine
IUPAC标准名
adamantan-1-amine
IUPAC传统名
amantidine
商标名
Pk-Merz
Endantadine
Gen-Amantadine
Mantadine
Symadine
Symmetrel
别名
Amantadine HCL
1-aminoadamantane
Adamantamine
Adamantanamine
Adamantylamine
Amantadine Base
Amantidine
Aminoadamantane
Amantadine Hydrochloride

产品登记号

CAS号 768-94-5

产品性质

疏水性(logP) 2.3
溶解度 6290 mg/L (freely soluble)

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake. [PubChem]
Indication For the chemoprophylaxis, prophylaxis, and treatment of signs and symptoms of infection caused by various strains of influenza A virus. Also for the treatment of parkinsonism and drug-induced extrapyramidal reactions.
Pharmacology Amantadine is an antiviral drug which also acts as an antiparkinson agent, for which it is usually combined with L-DOPA when L-DOPA responses decline (probably due to tolerance). It is a derivate of adamantane, like a similar drug rimantadine. The mechanism of action of amantadine in the treatment of Parkinson's disease and drug-induced extrapyramidal reactions is not known. It has been shown to cause an increase in dopamine release in the animal brain, and does not possess anticholinergic activity.
Toxicity Deaths have been reported from overdose with amantadine. The lowest reported acute lethal dose was 2 grams. Drug overdose has resulted in cardiac, respiratory, renal or central nervous system toxicity. Cardiac dysfunction includes arrhythmia, tachycardia and hypertension. Pulmonary edema and respiratory distress (including ARDS) have been reported. Renal dysfunction including increased BUN, decreased creatinine clearance and renal insufficiency can occur. Central nervous system effects that have been reported include insomnia, anxiety, aggressive behavior, hypertonia, hyperkinesia, tremor, confusion, disorientation, depersonalization, fear, delirium, hallucination, psychotic reactions, lethargy, somnolence and coma. Seizures may be exacerbated in patients with prior history of seizure disorders. Hyperthermia has also been observed in cases where a drug overdose has occurred.
Affected Organisms
Humans and other mammals
Various viruses
Biotransformation No appreciable metabolism, although negligible amounts of an acetyl metabolite have been identified.
Absorption Amantadine is well absorbed orally from the gastrointestinal tract.
Half Life Mean half-lives ranged from 10 to 14 hours, however renal function impairment causes a severe increase in half life to 7 to 10 days.
Protein Binding Approximately 67% bound to plasma proteins over a concentration range of 0.1 to 2.0 µg/mL.
Elimination It is primarily excreted unchanged in the urine by glomerular filtration and tubular secretion.
Distribution * 3 to 8 L/kg [healthy subjects]
Clearance * 0.2 - 0.3 L/hr/kg
* 0.10 +/- 0.04 L/hr/kg [healthy, elderly male]
External Links
Wikipedia
RxList
Drugs.com

参考文献