Definition
A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.
Description
Moclobemide is only found in individuals that have used or taken this drug. It is a reversible monoamine oxidase inhibitor (MAOI) selective for isoform A (RIMA) used to treat major depressive disorder. 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.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: 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
- Uses/Sources: For the treatment of depression.
- Route of Exposure: 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.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 730mg/kg (Mouse) (A308) LD50: 1300mg/kg (Rat) (A308)
Mechanism of Action
| Target Name | Mechanism of Action | References |
|---|---|---|
| Amine oxidase [flavin-containing] A | 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. |
11752352 |
Moclobemide Interacts with Diseases
| Disease | Inference Score | References/Inference Genes |
| Brunner Syndrome | 6.59 |
|
| Drug Metabolism, Poor, CYP2C19-Related | 6.5 | |
| Fetal Nutrition Disorders | 6.04 |
|
| Antisocial Personality Disorder | 5.78 |
|
| Primary ovarian insufficiency | 5.3 |
|
| End Stage Liver Disease | 5.15 |
|
| Mental Retardation, X-Linked | 5.02 |
|
| Pheochromocytoma | 4.8 |
|
| Huntington Disease | 4.71 |
|
| Hepatic Encephalopathy | 4.28 |
|
| Kidney Failure, Chronic | 4.03 |
|
| Mental Disorders | 4.03 |
|
| Endometriosis | 4.0 |
|
| Parkinson's disease | 3.87 |
|
| Muscular Diseases | 3.81 |
|
| Thrombosis | 3.77 |
|
| Prenatal Exposure Delayed Effects | 3.76 |
|
| Cognitive impairment | 3.75 |
|
| Autism | 3.72 |
|
| Cardiovascular disease | 3.72 |
|