2-フェニルシクロプロパン-1-アミン

HEXOBARBITAL SLEEPING TIME IS PROLONGED BY PARNATE, INDICATING ITS ABILITY TO POTENTIATE OTHER DRUGS PRESUMABLY BY INTERFERING WITH THEIR DETOXIFICATION. /PARNATE/

MAO INHIBITORS ALSO ENHANCE EFFECTS OF EXOGENOUSLY ADMIN AMINES, SUCH AS 5-HT & NOREPINEPHRINE, AS WELL AS PRECURSORS, SUCH AS 3,4-HYDROXYPHENYLALANINE (DOPA) & 5-HYDROXYTRYPTOPHAN. /MAO INHIBITORS/

Meperidine should never be used for ... headaches /with the hypertensive episode/, and blood pressure should be evaluated immediately when a patient taking an MAO inhibitor reports a severe throbbing headache or a feeling of pressure in the head. /MAO INHIBITORS/

MAO INHIBITORS ... INTERFERE WITH DETOXICATION MECHANISMS FOR CERTAIN OTHER DRUGS. THEY PROLONG & INTENSIFY EFFECTS OF CENTRAL DEPRESSANT AGENTS, SUCH AS GENERAL ANESTHETICS, SEDATIVES, ANTIHISTAMINES, ALCOHOL, & POTENT ANALGESICS; OF ANTICHOLINERGIC AGENTS, PARTICULARLY THOSE USED IN THE TREATMENT OF PARKINSONISM; & OF ANTIDEPRESSANT AGENTS, ESP IMIPRAMINE & AMITRIPTYLINE. /MAO INHIBITORS/

For more Interactions (Complete) data for TRANYLCYPROMINE (37 total), please visit the HSDB record page.

Rare cases have been reported of hypertensive crisis, serotonin syndrome, myoclonus, hyperpyrexia, psychosis, and delirium, some of which progressed to coma. Additionally, in sensitive individuals or at extreme dosages, hypotension may lead to shock. [Wikipedia]

Tranylcypromine, like most monoamine oxidase inhibitors, can cause transient serum aminotransferase elevations in a proportion of patients. These elevations are usually mild, asymptomatic and self-limited and do not require dose modification. Tranylcypromine has also been associated with rare cases of acute, clinically apparent liver injury. The few cases described have resembled those caused by other MAO inhibitors. The time to clinical onset is typically 1 to 4 months and the usual pattern of serum enzyme elevations is hepatocellular (Case 1), although cholestatic injury has also been described. Immunoallergic features (rash, fever, eosinophilia) are uncommon as is autoantibody formation.

Common adverse effects of tranylcypromine include dry mouth, headaches, diarrhea, urinary hesitancy, insomnia, agitation, anxiety, nausea, and sexual dysfunction. Postural hypotension, sometimes leading to syncope, is another common adverse effect that warrants special attention for older patients on this medication. This adverse effect is dose-related and may require splitting the dose into 3 to 4 doses daily. More serious side effects include hepatotoxicity, seizures, and induction of mania. Additionally, in the United States, there is a black-box warning stating that this medication may lead to the activation of suicidal ideation and behavior in children, adolescents, and young adults aged 18 to 24 with major depressive disorder and other psychiatric disorders.

Interindividual variability in absorption. May be biphasic in some individuals. Peak plasma concentrations occur in one hour following oral administration with a secondary peak occurring within 2-3 hours. Biphasic absorption may represent different rates of absorption of the stereoisomers of the drug, though additional studies are required to confirm this.

Signs and Symptoms of Overdose

Tranylcypromine irreversibly and nonselectively inhibits monoamine oxidase (MAO). Within neurons, MAO appears to regulate the levels of monoamines released upon synaptic firing. Since depression is associated with low levels of monoamines, the inhibition of MAO serves to ease depressive symptoms, as this results in an increase in the concentrations of these amines within the CNS.

In overdosage, some patients exhibit insomnia, restlessness and anxiety, progressing in severe cases to agitation, mental confusion and incoherence. Hypotension, dizziness, weakness and drowsiness may occur, progressing in severe cases to extreme dizziness and shock. A few patients have displayed hypertension with severe headache and other symptoms. Rare instances have been reported in which hypertension was accompanied by twitching or myoclonic fibrillation of skeletal muscles with hyperpyrexia, sometimes progressing to generalized rigidity and coma.

EFFECTS OF OVERDOSAGE INCL AGITATION, HALLUCINATIONS, HYPERREFLEXIA, HYPERPYREXIA, & CONVULSIONS. BOTH HYPOTENSION & HYPERTENSION ALSO OCCUR. /MAO INHIBITORS/

CHRONIC TOXICITY. ... MOST DANGEROUS ARE THOSE INVOLVING LIVER, BRAIN, & CARDIOVASCULAR SYSTEM. ... HYPERSENSITIVITY MAY BE RESPONSIBLE MECHANISM... /MAO INHIBITORS/

...HAS EXHIBITED NO SPECIFIC OR SELECTIVE OCULAR TOXIC EFFECT IN USUAL DOSAGE OF 20 MG/DAY, BUT LARGE OVERDOSAGE TAKEN WITH SUICIDAL INTENT APPEARS TO HAVE RESULTED IN OCULAR & VISUAL DISTURBANCES IN 2 CASES.

66-YR-OLD MAN TREATED FOR DEPRESSION (TRANYLCYPROMINE SULFATE 10 MG 3 TIMES/DAY FOR 6 DAYS) DEVELOPED INAPPROPRIATE ANTIDIURETIC HORMONE SECRETION WHICH DISAPPEARED AFTER DISCONTINUATION.

For more Human Toxicity Excerpts (Complete) data for TRANYLCYPROMINE (8 total), please visit the HSDB record page.

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

tranylcypromine

DILI Positive

Oral

DOI:10.1016/j.drudis.2019.09.022

IN ANIMALS IT PRODUCES IRRITABILITY, RESTLESSNESS, HYPERREFLEXIA, HYPERTONIA, SALIVATION, LACRIMATION, MYDRIASIS, & MILD ELEVATIONS IN BLOOD PRESSURE. IT SUPPRESSES APPETITE...

TRANYLCYPROMINE 20 MG/KG PARENTERAL TO RATS INCR BRAIN SEROTONIN CONCN & DECR BRAIN GLYCOGEN; NO EFFECT ON BRAIN PHOSPHORYLASE A & B ACTIVITIES OR ON BRAIN ABILITY TO PRODUCE LACTATE ANAEROBICALLY FROM GLYCOGEN (THESE CONSIDERED INDICATORS OF GLYCOGENOLYSIS).

Hepatic.

Hepatic. Half Life: 1.5-3.2 hours in patients with normal renal and hepatic function

3E3V44J4Z9

TRANYLCYPROMINE

Established Pharmacologic Class [EPC] - Monoamine Oxidase Inhibitor

Mechanisms of Action [MoA] - Monoamine Oxidase Inhibitors

Tranylcypromine is a Monoamine Oxidase Inhibitor. The mechanism of action of tranylcypromine is as a Monoamine Oxidase Inhibitor.

TRANYLCYPROMINE

Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems.

A chemically heterogeneous group of drugs that have in common the ability to block oxidative deamination of naturally occurring monoamines. (From Gilman, et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p414)

Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here.

Interindividual variability in absorption. May be biphasic in some individuals. Peak plasma concentrations occur in one hour following oral administration with a secondary peak occurring within 2-3 hours. Biphasic absorption may represent different rates of absorption of the stereoisomers of the drug, though additional studies are required to confirm this.

1.1-5.7 L/kg

THE MAO INHIBITORS ARE ABSORBED READILY WHEN GIVEN BY MOUTH. THESE DRUGS PRODUCE MAXIMAL INHIBITION OF MAO WITHIN 5-10 DAYS. ... ALTHOUGH THEIR BIOLOGICAL ACTIVITY IS PROLONGED BECAUSE OF THE CHARACTERISTICS OF THEIR INTERACTION WITH THE ENZYME, THEIR CLINICAL EFFICACY APPEARS TO BE REDUCED WHEN THE DRUG IS GIVEN LESS FREQUENTLY THAN ONCE DAILY. /MAO INHIBITORS/