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QuickView for Moclobemide (compound)

Name: Moclobemide
PubChem Compound ID: 4235
Description: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.
Molecular formula: C13H17ClN2O2
Molecular weight: 268.739 g/mol
SMR000012114; Moclobemide [USAN:BAN:INN]; MLS000070549; 4-Chloro-N-(2-(4-morpholinyl)ethyl)benzamide; Manerix; 4-Chlor-N-(2-morpholinoethyl)benzamid; Moclobemidum [INN-Latin]; Benzamide, 4-chloro-N-(2-(4-morpholinyl)ethyl)-; CBMicro_048319; Aurorix.
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Name: Moclobemide
Name (isomeric): DB01171
Drug Type: small molecule
Description: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.
Moclobemide [Usan:Ban:Inn]; 4-Chloro-N-(2-(4-morpholinyl)ethyl)benzamide; Moclamide; Moclaime; Moclobemid; Moclobemida [INN-Spanish]; 4-Chlor-N-(2-morpholinoethyl)benzamid; p-Chloro-N-(2-morpholinoethyl)benzamide; Moclobemidum [INN-Latin]; 4-Chloro-N-(2-morpholin-4-yl-ethyl)-benzamide.
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Brand: Manerix, Aurorix
Category: Monoamine Oxidase Inhibitors, Antidepressive Agents
CAS number: 71320-77-9
Indication: For the treatment of depression.
Moclobemide belongs to a class of MAOI antidepressants known as reversible inhibitors of monoamine oxidase type-A (RIMAs). The primary role of monoamine oxidase MAO lies in the metabolism of and regulation of the levels of monoamines (serotonin, norepinephrine, and dopamine). Within neurons, MAO appears to regulate the levels of monoamines released...
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Mechanism of Action: The mechanism of action of moclobemide involves the selective, reversible inhibition of MAO-A. This inhibition leads to a decrease in the metabolism and destruction of monoamines in the neurotransmitters. This results in an increase in the monoamines, relieving depressive symptoms.
Absorption: Well absorbed from the gastrointestinal tract (> 95%). The presence of food reduces the rate but not the extent of absorption. Hepatic first pass metabolism reduces bioavailability to 45-70% following administration of a single dose, but increases to 80% with multiple dosing as a result of saturation of the first pass effect. Peak plasma concentrations are reached within 1 - 2 hours following oral administration.
Protein binding: Approximately 50% (primarily to albumin)
Biotransformation: Moclobemide is almost completely metabolized in the liver by Cytochrome P450 2C19 and 2D6.
Half Life: 1-2 hours (4 hours in cirrhotic patients); metabolites are renally excreted
Toxicity: LD50 (mouse) is 730mg/kg and LD50 (rat) is 1,300mg/kg. Signs of toxicity include hypertension, drowsiness, dizziness, confusion, tremors, headache, agitation, muscle rigidity and seizures.
Affected organisms: Humans and other mammals
Food interaction:
Food slows absorption a little. Avoid alcohol. Take after meals in order to minimize the risk of interaction with tyramine.
Drug interaction:
RizatriptanThe MAO inhibitor, moclobemide, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, rizatriptan. Concomitant therapy is contraindicated.
ProtriptylinePossible severe adverse reaction with this combination
SelegilineDecrease in selectivity
TetrabenazineTetrabenazine may increase the adverse/toxic effects of Moclobemide. Concomitant therapy is contraindicated.
AmitriptylinePossible severe adverse reaction with this combination
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