Drug/Small Molecule:
isocarboxazid

2D structure

Overview

Generic Names: Isocarbonazid; Isocarbossazide [Dcit]; Isocarboxazida [INN-Spanish]; Isocarboxazide; Isocarboxazide [INN-French]; Isocarboxazidum [INN-Latin]; Isocarboxyzid
Trade Names: BMIH; Benazide; Enerzer; Maraplan; Marplan; Marplon
PharmGKB Accession Id: PA450101

Description

An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) (source: Drug Bank)

Indication

Isocarboxazid is used to treat depression, especially when the patient is excitable or suffering from phobias (fears). (source: Drug Bank)

ATC Therapeutic Category

  • N06AF:Monoamine oxidase inhibitors, non-selective

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Isocarboxazid works by irreversibly blocking the action of a chemical substance known as monoamine oxidase (MAO) in the nervous system. MAO subtypes A and B are involved in the metabolism of serotonin and catecholamine neurotransmitters such as epinephrine, norepinephrine, and dopamine. Isocarboxazid, as a nonselective MAO inhibitor, binds irreversibly to monoamine oxidase–A (MAO-A) and monoamine oxidase–B (MAO-B). The reduced MAO activity results in an increased concentration of these neurotransmitters in storage sites throughout the central nervous system (CNS) and sympathetic nervous system. This increased availability of one or more monoamines is the basis for the antidepressant activity of MAO inhibitors. (source: Drug Bank)

Pharmacology

Isocarboxazid is a non-selective hydrazine monoamine oxidase (MAO) inhibitor used to treat depression. In vivo and in vitro studies demonstrated inhibition of MAO in the brain, heart, and liver. Depression is a complicated disease that is not fully understood. It is thought that depression may be linked to an imbalance of chemicals within the brain. When depression occurs, there may be a decrease in the amount of chemicals released from nerve cells in the brain. These chemicals are called monoamines. Monoamines are broken down by a chemical called monoamine oxidase. Isocarboxazid prevents monoamine oxidase from breaking down the monoamines. This results in an increased amount of active monoamines in the brain. By increasing the amount of monoamines in the brain, the imbalance of chemicals thought to be caused by depression is altered. This helps relieve the symptoms of depression. (source: Drug Bank)

Food Interactions

Take without regard to meals, avoid tyramine, caffeine and alcohol. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic and rapid (by oxidation). (source: Drug Bank)

Absorption

Well absorbed from the gastrointestinal tract. (source: Drug Bank)

Toxicity

Signs of overdose include severe anxiety, confusion, convulsions, cool clammy skin, severe dizziness, severe drowsiness, fast and irregular pulse, fever, hallucinations, severe headache, high or low blood pressure, hyperactive reflexes, muscle stiffness, respiratory depression or failure, slowed reflexes, sweating, severe trouble in sleeping, and unusual irritability. (source: Drug Bank)

Isomeric SMILES Code:

Cc1cc(no1)C(=O)NNCc2ccccc2 (source: Drug Bank)

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
MAOA Uncurated Annotation (source: Drug Bank)
MAOB Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
almotriptan Uncurated Annotation MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)
amitriptyline Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
amoxapine Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
amphetamine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
atomoxetine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
benzphetamine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
bupropion Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
buspirone Uncurated Annotation Possible blood pressure elevation (source: Drug Bank)
chlorpropamide Uncurated Annotation The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank)
citalopram Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
clomipramine Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
desipramine Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
dextroamphetamine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
dextromethorphan Uncurated Annotation Possible severe adverse reaction (source: Drug Bank)
dobutamine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
donepezil Uncurated Annotation Possible antagonism of action (source: Drug Bank)
dopamine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
doxepin Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
duloxetine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
ephedrine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
epinephrine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
escitalopram Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
fenfluramine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
fenoterol Uncurated Annotation Increased arterial pressure (source: Drug Bank)
fluoxetine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
fluvoxamine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
galantamine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
glibenclamide Uncurated Annotation The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank)
gliclazide Uncurated Annotation The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank)
glipizide Uncurated Annotation The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank)
guanethidine Uncurated Annotation The agent decreases the effect of guanethidine (source: Drug Bank)
imipramine Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
isoproterenol Uncurated Annotation Increased arterial pressure (source: Drug Bank)
l-tryptophan Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
levodopa Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
mazindol Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
meperidine Uncurated Annotation Potentially fatal adverse effects (source: Drug Bank)
methamphetamine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
methoxamine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
methylphenidate Uncurated Annotation Possible hypertensive crisis with this combination (source: Drug Bank)
mirtazapine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
naratriptan Uncurated Annotation MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)
nefazodone Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
norepinephrine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
nortriptyline Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
orciprenaline Uncurated Annotation Increased arterial pressure (source: Drug Bank)
paroxetine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
phendimetrazine Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
phenylephrine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
pirbuterol Uncurated Annotation Increased arterial pressure (source: Drug Bank)
protriptyline Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
pseudoephedrine Uncurated Annotation Increased arterial pressure (source: Drug Bank)
rivastigmine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
rizatriptan Uncurated Annotation The MAO inhibitor increases the effect and toxicity of rizatriptan (source: Drug Bank)
salbutamol Uncurated Annotation Increased arterial pressure (source: Drug Bank)
sertraline Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
sibutramine Uncurated Annotation Possible serotoninergic syndrome with this combination (source: Drug Bank)
sumatriptan Uncurated Annotation MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)
terbutaline Uncurated Annotation Increased arterial pressure (source: Drug Bank)
tetrabenazine Uncurated Annotation CNS stimulation, hypertensive upsurge with this combination (source: Drug Bank)
tolbutamide Uncurated Annotation The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank)
tolcapone Uncurated Annotation Possible hypertensive crisis with this combination (source: Drug Bank)
tramadol Uncurated Annotation Increased risk of seizures and serotonin syndrome (source: Drug Bank)
trimipramine Uncurated Annotation Possibility of severe adverse effects (source: Drug Bank)
venlafaxine Uncurated Annotation Possible severe adverse reaction with this combination (source: Drug Bank)
zolmitriptan Uncurated Annotation MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01247
KEGG Drug ID:
D02580
PubChem Compound ID:
3759
PubChem Substance ID:
148916

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
Add New Alternate Name
Add New ATC Term
Add Cross Reference
Add a metabolite
Add a text annotation
Add a drug target
hint: enter a gene
    Add a drug interaction
    hint: enter a drug
    PharmGKB® is a registered trademark of HHS and is financially supported by NIH/NIGMS. It is managed at Stanford University (GM61374).
    ©2001-2010 PharmGKB.