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Phenelzine

产品号 DB00780 公司名称 DrugBank
CAS号 51-71-8 公司网站 http://www.ualberta.ca/
分子式 C8H12N2 电 话 (780) 492-3111
分子量 136.19428 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 660

产品价格信息

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产品别名

标题
Phenelzine
IUPAC标准名
(2-phenylethyl)hydrazine
IUPAC传统名
phenelzine
商标名
Fenelzyne
Nardil
Fenelzina [INN-Spanish]
Beta-phenylethylhydrazine
Phenylethylhydrazine
Stinerval
Fenelzyna
Phenalzine
Phenelezine
Phenelzinum [INN-Latin]
Phenethylhydrazine
Phenylethyl hydrazine-HCl

产品登记号

PubChem CID 3675
PubChem SID 46507348
CAS号 51-71-8

产品性质

疏水性(logP) 1.1
溶解度 29.1 g/L

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description An irreversible non-selective inhibitor of monoamine oxidase. May be used to treat major depressive disorder.
Indication For the treatment of major depressive disorder. Has also been used with some success in the management of bulimia nervosa.
Pharmacology Phenelzine belongs to a class of antidepressants called monoamine oxidase inhibitors (MAOIs). MAO is an enzyme that catalyzes the oxidative deamination of a number of amines, including serotonin, norepinephrine, epinephrine, and dopamine. Two isoforms of MAO, A and B, are found in the body. MAO-A is mainly found within cells located in the periphery and catalyzes the breakdown of serotonin, norepinephrine, epinephrine, dopamine and tyramine. MAO-B acts on phenylethylamine, norepinephrine, epinephrine, dopamine and tyramine, is localized extracellularly and is found predominantly in the brain. While the mechanism of MAOIs is still unclear, it is thought that they act by increasing free serotonin and norepinephrine concentrations and/or by altering the concentrations of other amines in the CNS. It has been postulated that depression is caused by low levels of serotonin and/or norepinephrine and that increasing serotonergic and norepinephrinergic neurotransmission results in relief of depressive symptoms. MAO A inhibition is thought to be more relevant to antidepressant activity than MAO B inhibition. Selective MAO B inhibitors, such as selegiline, have no antidepressant effects. Response to therapy generally occurs 2 - 4 weeks following onset though some patients may not experience symptom relief for up to 8 weeks.
Toxicity Symptoms of overdose include drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions and coma, rapid and irregular pulse, hypertension, hypotension and vascular collapse, precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin. Hypertensive crisis may occur with the ingestion of tyramine-rich foods such as cured meats, poultry or fish, aged cheeses, concentrated soy products, tap beer and wine, yeast extracts, broad bean pods and fava beans and sauerkraut.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic. Acetylation of phenelzine appears to be a minor metabolic pathway. Beta-phenylethylamine is a metabolite of phenelzine, and there is indirect evidence that phenelzine may also be ring-hydroxylated and N-methylated.
Absorption Readily absorbed after oral administration.
Half Life 1.2-11.6 hours following single dose administration. Multiple-dose pharmacokinetics have not been studied.
Elimination NARDIL ? is extensively metabolized, primarily by oxidation via monoamine oxidase.
References
Nolen WA: [Classical monoamine oxidase inhibitor: not registered for, but still a place in the treatment of depression] Ned Tijdschr Geneeskd. 2003 Oct 4;147(40):1940-3. [Pubmed]
Sowa BN, Holt A, Todd KG, Baker GB: Monoamine oxidase inhibitors, their structural analogues, and neuroprotection. Indian J Exp Biol. 2004 Sep;42(9):851-7. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Nolen WA: [Classical monoamine oxidase inhibitor: not registered for, but still a place in the treatment of depression] Ned Tijdschr Geneeskd. 2003 Oct 4;147(40):1940-3. Pubmed
  • Sowa BN, Holt A, Todd KG, Baker GB: Monoamine oxidase inhibitors, their structural analogues, and neuroprotection. Indian J Exp Biol. 2004 Sep;42(9):851-7. Pubmed