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trimethobenzamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2754 | 138-56-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.909 | High | 0.83 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 11.858 | High | 0.83 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 3.436 | 10^-6 cm/s | High | 0.83 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.821 | uL/min/10^6 cells | High | 0.83 |
| dppb | Dog plasma protein binding (% unbound) | 45.410 | % | High | 0.83 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 66.770 | % | High | 0.83 |
| herg | hERG pIC50 | 4.333 | pIC50 | High | 0.83 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.581 | uL/min/10^6 cells | High | 0.83 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.140 | uL/min/mg protein | High | 0.83 |
| hppb | Human plasma protein binding (% unbound) | 23.240 | % | High | 0.83 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPK9,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 49 | |||
| kinase-selectivity-class | AXL,EIF2AK3,EPHB4,ERBB2,GRK2,PDK4,SIK2 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 8.054 | High | 0.83 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.715 | High | 0.83 | |
| mppb | Mouse plasma protein binding (% unbound) | 44.500 | High | 0.83 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 18.750 | High | 0.83 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 60.490 | % | High | 0.83 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.842 | uL/min/10^6 cells | High | 0.83 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 79.700 | % | High | 0.83 |
| rppb | Rat plasma protein binding (% unbound) | 39.340 | % | High | 0.83 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 883.080 | uM | High | 0.83 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 12, 1974 | FDA | PAR STERILE PRODUCTS |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 53.75 | 30.49 | 39 | 762 | 463570 | 90164076 |
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 |
|---|---|---|---|---|---|---|
| Nausea | 37.73 | 25.50 | 51 | 966 | 1235639 | 109352643 |
| Drug hypersensitivity | 29.74 | 25.50 | 28 | 989 | 454062 | 110134220 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R06AA10 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers |
| FDA PE | N0000009034 | Emesis Suppression |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| FDA EPC | N0000178372 | Antiemetic |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
Related Drugs by ATC class:
R06AA Aminoalkyl ethers 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Nausea and vomiting | indication | 16932000 | |
| Vomiting | indication | 422400008 | |
| Nausea | indication | 422587007 | |
| Dehydration | contraindication | 34095006 | |
| Encephalitis | contraindication | 45170000 | DOID:9588 |
| Bleeding hemorrhoids | contraindication | 51551000 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disorder of mucous membrane | contraindication | 95351003 | |
| Disorder of electrolytes | contraindication | 237840007 | |
| Fever greater than 100.4 Fahrenheit | contraindication | 426000000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.61 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D02733 | KEGG_DRUG |
| 554-92-7 | SECONDARY_CAS_RN |
| 4018405 | VANDF |
| 4019961 | VANDF |
| CHEBI:27796 | CHEBI |
| CHEMBL1201256 | ChEMBL_ID |
| CHEMBL1200887 | ChEMBL_ID |
| C100146 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7614 | IUPHAR_LIGAND_ID |
| DB00662 | DRUGBANK_ID |
| W2X096QY97 | UNII |
| 227528 | RXNORM |
| 2183 | MMSL |
| 3031 | MMSL |
| 5632 | MMSL |
| d00862 | MMSL |
| 001679 | NDDF |
| 001680 | NDDF |
| 14814001 | SNOMEDCT_US |
| 24261009 | SNOMEDCT_US |
| 372657005 | SNOMEDCT_US |
| C0077163 | UMLSCUI |
| 957 | INN_ID |
| 5577 | PUBCHEM_CID |
| W2X096QY97 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tigan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9964 | INJECTION | 100 mg | INTRAMUSCULAR | NDA | 12 sections |
| Tigan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9964 | INJECTION | 100 mg | INTRAMUSCULAR | NDA | 12 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-448 | CAPSULE | 300 mg | ORAL | ANDA | 16 sections |
| Tigan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-853 | INJECTION | 100 mg | INTRAMUSCULAR | NDA | 17 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23155-180 | CAPSULE | 300 mg | ORAL | ANDA | 14 sections |
| Tigan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-119 | INJECTION | 100 mg | INTRAMUSCULAR | NDA | 17 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43386-660 | CAPSULE | 300 mg | ORAL | ANDA | 18 sections |
| TIGAN(R) (TRIMETHOBENZAMIDE HYDROCHLORIDE) | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1430 | INJECTION | 100 mg | INTRAMUSCULAR | NDA | 12 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54288-158 | INJECTION | 100 mg | INTRAMUSCULAR | ANDA | 17 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5741 | CAPSULE | 300 mg | ORAL | ANDA | 10 sections |
| Trimethobenzamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-884 | CAPSULE | 300 mg | ORAL | ANDA | 9 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-773 | CAPSULE | 300 mg | ORAL | ANDA | 22 sections |
| Trimethobenzamide Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-0800 | CAPSULE | 300 mg | ORAL | ANDA | 18 sections |