Name: | Moclobemide |
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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 |
Synonyms: |
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 |
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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. |
Synonyms: |
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. |
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Pharmacology: |
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: |
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