moclobemide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1825 | 71320-77-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A reversible inhibitor of monoamine oxidase type A (RIMA) that has antidepressive properties.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 75 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.77 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 4 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1990 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 110.74 | 52.22 | 33 | 933 | 28649 | 63459407 |
| Drug interaction | 61.79 | 52.22 | 40 | 926 | 229091 | 63258965 |
| Apallic syndrome | 58.21 | 52.22 | 10 | 956 | 711 | 63487345 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 172.79 | 55.15 | 50 | 1005 | 19883 | 34935993 |
| Intentional overdose | 126.93 | 55.15 | 48 | 1007 | 43626 | 34912250 |
| Physical deconditioning | 104.02 | 55.15 | 20 | 1035 | 1339 | 34954537 |
| Major depression | 65.11 | 55.15 | 17 | 1038 | 4555 | 34951321 |
| Suicide attempt | 62.18 | 55.15 | 28 | 1027 | 39088 | 34916788 |
| Dissociative disorder | 55.67 | 55.15 | 10 | 1045 | 459 | 34955417 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 189.61 | 41.04 | 59 | 1539 | 44968 | 79697822 |
| Drug interaction | 86.46 | 41.04 | 69 | 1529 | 415114 | 79327676 |
| Intentional overdose | 74.14 | 41.04 | 38 | 1560 | 105922 | 79636868 |
| Dissociative disorder | 54.15 | 41.04 | 10 | 1588 | 811 | 79741979 |
| Apallic syndrome | 52.50 | 41.04 | 10 | 1588 | 958 | 79741832 |
| Depressed mood | 47.75 | 41.04 | 22 | 1576 | 48458 | 79694332 |
| Toxicity to various agents | 46.11 | 41.04 | 49 | 1549 | 421491 | 79321299 |
| Electrocardiogram QT prolonged | 45.26 | 41.04 | 26 | 1572 | 90360 | 79652430 |
| Arrhythmia | 42.85 | 41.04 | 22 | 1576 | 61250 | 79681540 |
| Serum serotonin increased | 41.77 | 41.04 | 7 | 1591 | 323 | 79742467 |
| Diabetic hyperosmolar coma | 41.77 | 41.04 | 8 | 1590 | 789 | 79742001 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AG02 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Monoamine oxidase A inhibitors |
| CHEBI has role | CHEBI:35469 | antidepressants |
| CHEBI has role | CHEBI:35703 | Xenobiotic |
| CHEBI has role | CHEBI:78298 | environmental contaminants |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D008996 | Monoamine Oxidase Inhibitors |
| MeSH PA | D011619 | Psychotropic Drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Depressive disorder | indication | 35489007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.45 | acidic |
| pKa2 | 6.83 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Amine oxidase [flavin-containing] A | Enzyme | INHIBITOR | Ki | 8.30 | CHEMBL | IUPHAR | |||
| 5-hydroxytryptamine receptor 1A | GPCR | Kd | 5.30 | CHEMBL | |||||
| Amine oxidase [flavin-containing] B | Enzyme | Ki | 5.97 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.10 | CHEMBL | |||||
| Amine oxidase [flavin-containing] B | Enzyme | Ki | 5.97 | CHEMBL | |||||
| Amine oxidase [flavin-containing] A | Enzyme | Ki | 8.30 | CHEMBL | |||||
| Amine oxidase [flavin-containing] A | Enzyme | Ki | 4.94 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166883 | NUI |
| D02561 | KEGG_DRUG |
| C0066673 | UMLSCUI |
| CHEBI:83531 | CHEBI |
| CHEMBL86304 | ChEMBL_ID |
| DB01171 | DRUGBANK_ID |
| D020912 | MESH_DESCRIPTOR_UI |
| 4235 | PUBCHEM_CID |
| 7428 | IUPHAR_LIGAND_ID |
| 4914 | INN_ID |
| PJ0Y7AZB63 | UNII |
| 30121 | RXNORM |
| 004179 | NDDF |
| 321911007 | SNOMEDCT_US |
| 395800003 | SNOMEDCT_US |
Pharmaceutical products:
None