药品详细

Phenelzine(苯乙肼)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

苯乙肼

英文名

Phenelzine

分子式

C₈H₁₂N₂

化学名

(2-phenylethyl)hydrazine

分子量

Average: 136.1943
Monoisotopic: 136.100048394

CAS号

51-71-8

ATC分类

N06A 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

An irreversible non-selective inhibitor of monoamine oxidase. May be used to treat major depressive disorder.

生产厂家

Parke davis div warner lambert co

封装厂家

Farmea
Kaiser Foundation Hospital
Murfreesboro Pharmaceutical Nursing Supply
Pfizer Inc.
Professional Co.
Warner Lambert Company LLC

参考

Synthesis Reference	Not Available
General Reference	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

剂型

规格

化合物类型

Type	small molecule

Classes

Phenethylamines

Substructures

Benzene and Derivatives
Phenethylamines
Aromatic compounds
Hydrazine Derivatives

适应症

药理

Indication	For the treatment of major depressive disorder. Has also been used with some success in the management of bulimia nervosa.
Pharmacodynamics	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.
Mechanism of action	Although the exact mechanism of action has not been determined, it appears that the irreversible, nonselective inhibition of MAO by phenelzine relieves depressive symptoms by causing an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron.
Absorption	Readily absorbed after oral administration.
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	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.
Route of elimination	NARDIL ® is extensively metabolized, primarily by oxidation via monoamine oxidase.
Half life	1.2-11.6 hours following single dose administration. Multiple-dose pharmacokinetics have not been studied.
Clearance	Not Available
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
Pathways	Not Available

理化性质

Properties

State

liquid

Experimental Properties

Property	Value	Source
melting point	< 25 °C	PhysProp
boiling point	74 °C at 1.00E-01 mm Hg	PhysProp
water solubility	29.1 g/L	Not Available
logP	1.1	Not Available

Predicted Properties

Property	Value	Source
water solubility	1.11e+01 g/l	ALOGPS
logP	1.2	ALOGPS
logP	1.2	ChemAxon
logS	-1.1	ALOGPS
pKa (strongest basic)	5.55	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	2	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	38.05	ChemAxon
rotatable bond count	3	ChemAxon
refractivity	54.26	ChemAxon
polarizability	15.8	ChemAxon

药物相互作用

Drug	Interaction
Almotriptan	The MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, almotriptan. Concomitant therapy is contraindicated.
Altretamine	Risk of severe hypotension
Amitriptyline	Possibility of severe adverse effects
Amoxapine	Possibility of severe adverse effects
Amphetamine	Possible hypertensive crisis
Atomoxetine	Possible severe adverse reaction with this combination
Benzphetamine	MAO Inhibitors may enhance the hypertensive effect of Amphetamines. Concomitant use of amphetamines and monoamine oxidase inhibitors (MAOI) should be avoided. If used concomitantly, careful monitoring of blood pressure must occur. It may take up to 2 weeks after the discontinuation of an MAOI for the effects to dissipate enough to afford safety to the administration of interacting agents.
Bezafibrate	MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like phenelzine.
Brimonidine	MAO Inhibitors like phenelzine may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Buprenorphine	Buprenorphine may enhance the adverse/toxic effect of MAO Inhibitors like phenelzine. When possible, avoid use of buprenorphine in patients who have used a monoamine oxidase inhibitor within the past 14 days due to possible severe adverse effects.
Bupropion	Possible severe adverse reaction with this combination
Buspirone	Possible blood pressure elevation
Citalopram	Possible severe adverse reaction with this combination
Clomipramine	Possibility of severe adverse effects
Desipramine	Possibility of severe adverse effects
Desvenlafaxine	Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
Dexfenfluramine	Possible hypertensive crisis
Dextroamphetamine	Possible hypertensive crisis
Dextromethorphan	Possible severe adverse reaction
Diethylpropion	Possible hypertensive crisis
Dobutamine	Increased arterial pressure
Donepezil	Possible antagonism of action
Dopamine	Increased arterial pressure
Doxepin	Possibility of severe adverse effects
Duloxetine	Possible severe adverse reaction with this combination
Entacapone	Possible hypertensive crisis with this combination
Ephedra	Increased arterial pressure
Ephedrine	Increased arterial pressure
Epinephrine	Increased arterial pressure
Escitalopram	Possible severe adverse reaction with this combination
Fenfluramine	Possible hypertensive crisis
Fenoterol	Increased arterial pressure
Fluoxetine	Possible severe adverse reaction with this combination
Fluvoxamine	Possible severe adverse reaction with this combination
Galantamine	Possible antagonism of action
Guanethidine	Phenelzine may decrease the effect of guanethidine.
Imipramine	Possibility of severe adverse effects
Isoproterenol	Increased arterial pressure
Levodopa	Possible hypertensive crisis
Mazindol	Possible hypertensive crisis
Meperidine	Potentially fatal adverse effects
Mephentermine	Increased arterial pressure
Metaraminol	Increased arterial pressure
Methamphetamine	Possible hypertensive crisis
Methotrimeprazine	Possible severe adverse reaction with this combination
Methoxamine	Increased arterial pressure
Methylphenidate	Possible hypertensive crisis with this combination
Midodrine	Possible hypertensive crisis with this combination
Milnacipran	Increase serotonin levels. Combination therapy is contraindicated.
Mirtazapine	Possible severe adverse reaction with this combination
Naratriptan	The use of two serotonin modulators increases the risk of serotonin syndrome. Consider alternate therapy or monitor for signs and symptoms of serotonin syndrome.
Nefazodone	Possible severe adverse reaction with this combination
Norepinephrine	Increased arterial pressure
Nortriptyline	Possibility of severe adverse effects
Orciprenaline	Increased arterial pressure
Paroxetine	Possible severe adverse reaction with this combination
Phendimetrazine	Possible hypertensive crisis
Phentermine	Possible hypertensive crisis
Phenylephrine	Increased arterial pressure
Phenylpropanolamine	Increased arterial pressure
Pirbuterol	Increased arterial pressure
Procaterol	Increased arterial pressure
Protriptyline	Possibility of severe adverse effects
Pseudoephedrine	Increased arterial pressure
Rivastigmine	Possible antagonism of action
Rizatriptan	The MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, rizatriptan. Concomitant therapy is contraindicated.
Salbutamol	Increased arterial pressure
Sertraline	Possible severe adverse reaction with this combination
Sibutramine	Possible serotoninergic syndrome with this combination
Sumatriptan	The MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, sumatriptan. Concomitant therapy is contraindicated.
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Phenelzine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Terbutaline	Increased arterial pressure
Tetrabenazine	Tetrabenazine may increase the adverse/toxic effects of Phenelzine. Concomitant therapy is contraindicated.
Tolcapone	Tolcapone and Phenelzine decrease the metabolism of endogenous catecholamines. Concomitant therapy may result in increased catecholamine effects. Consider alternate therapy or use cautiously and monitor for increased catecholamine effects.
Tramadol	Tramadol may increase the risk of serotonin syndrome and seizure induction by the MAO inhibitor, phenelzine.
Tranylcypromine	Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
Trazodone	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Trimethobenzamide	Trimethobenzamide and Phenelzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimipramine	Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Avoid combination or monitor for symptoms of serotonin syndrome and/or hypertensive crisis.
Triprolidine	Triprolidine and Phenelzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium	Trospium and Phenelzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tryptophanyl-5'amp	Possible severe adverse reaction with this combination
Venlafaxine	Increased risk of serotonin syndrome. Ensure adequate washout period between therapies to avoid toxicity. Concurrent therapy should be avoided.
Vilazodone	MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome.
Zolmitriptan	The MAO inhibitor, phenelzine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing phenelzine are contraindicated.

食物相互作用

Avoid aged foods (cheese, red wine), pickled foods, cured foods (bacon/ham), chocolate, fava beans, beer, unless approved by your physician.
Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Avoid St.John's Wort.
Take without regard to meals.

返回 | 收藏