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metopimazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1784 | 14008-44-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 15 | mg | O |
| 15 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 20 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| CL (Clearance) | 12.14 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.383 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 20.654 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 3.548 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 10.568 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 21.320 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 36.370 | % | High | 1 |
| herg | hERG pIC50 | 5.621 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.413 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 21.184 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 20.600 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MARK4,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 36 | |||
| kinase-selectivity-class | AXL,MAP2K6,PDK4,SIK2,STK33,TEK | 6 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 13.677 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 58.479 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 22.150 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 27.925 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 37.820 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 48.195 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 61.970 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 19.670 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 421.697 | uM | High | 1 |
Approvals:
None
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 |
|---|---|---|---|---|---|---|
| Acute kidney injury | 114.34 | 40.09 | 73 | 1685 | 320314 | 90306375 |
| Pancreatitis acute | 83.23 | 40.09 | 29 | 1729 | 32086 | 90594603 |
| Hyperkalaemia | 63.43 | 40.09 | 29 | 1729 | 64935 | 90561754 |
| Ischaemic stroke | 61.21 | 40.09 | 21 | 1737 | 22145 | 90604544 |
| Cholestasis | 54.55 | 40.09 | 22 | 1736 | 36277 | 90590412 |
| Hepatic cytolysis | 50.85 | 40.09 | 20 | 1738 | 30896 | 90595793 |
| Drug reaction with eosinophilia and systemic symptoms | 47.81 | 40.09 | 21 | 1737 | 42737 | 90583952 |
| Febrile bone marrow aplasia | 46.52 | 40.09 | 14 | 1744 | 9724 | 90616965 |
| Lactic acidosis | 41.42 | 40.09 | 20 | 1738 | 50443 | 90576246 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Acute kidney injury | 132.53 | 34.68 | 117 | 2698 | 635313 | 109951171 |
| Pancreatitis acute | 108.91 | 34.68 | 45 | 2770 | 60229 | 110526255 |
| Coma | 69.47 | 34.68 | 41 | 2774 | 117828 | 110468656 |
| Hepatic cytolysis | 63.46 | 34.68 | 30 | 2785 | 55023 | 110531461 |
| Cholestasis | 56.04 | 34.68 | 29 | 2786 | 64489 | 110521995 |
| Poisoning deliberate | 55.56 | 34.68 | 22 | 2793 | 26309 | 110560175 |
| Analgesic drug level increased | 55.26 | 34.68 | 14 | 2801 | 3932 | 110582552 |
| Rash maculo-papular | 54.98 | 34.68 | 30 | 2785 | 74192 | 110512292 |
| Hyperkalaemia | 52.00 | 34.68 | 36 | 2779 | 135760 | 110450724 |
| Drug reaction with eosinophilia and systemic symptoms | 49.50 | 34.68 | 29 | 2786 | 82066 | 110504418 |
| Ischaemic stroke | 49.12 | 34.68 | 23 | 2792 | 41240 | 110545244 |
| Intestinal transit time decreased | 46.56 | 34.68 | 7 | 2808 | 124 | 110586360 |
| Lactic acidosis | 43.71 | 34.68 | 28 | 2787 | 92783 | 110493701 |
| Thrombocytopenia | 42.15 | 34.68 | 48 | 2767 | 348837 | 110237647 |
| Febrile bone marrow aplasia | 41.82 | 34.68 | 16 | 2799 | 17449 | 110569035 |
| Altered state of consciousness | 39.12 | 34.68 | 22 | 2793 | 57604 | 110528880 |
| Hepatocellular injury | 36.19 | 34.68 | 20 | 2795 | 50622 | 110535862 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A04AD05 | ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Other antiemetics |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| CHEBI has role | CHEBI:50919 | antiemetic |
Related Drugs by ATC class:
A04AD Other antiemetics 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.41 | acidic |
| pKa2 | 8.95 | Basic |
| pKa3 | 3.45 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | Ki | 10.15 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | Ki | 9.21 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Ki | 8.08 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D05010 | KEGG_DRUG |
| C0066469 | UMLSCUI |
| CHEBI:135726 | CHEBI |
| CHEMBL398615 | ChEMBL_ID |
| DB13591 | DRUGBANK_ID |
| C005260 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11140 | IUPHAR_LIGAND_ID |
| 2178 | INN_ID |
| 238S75V9AV | UNII |
| 26388 | PUBCHEM_CID |
| 29954 | RXNORM |
| 005826 | NDDF |
Pharmaceutical products:
None