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tropisetron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin receptor antagonists (5-HT3) | 2775 | 89565-68-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
| 5 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 11 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 8 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.25 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 66 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 9.70 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 26 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.60 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 42 | |||
| kinase-selectivity-class | AXL,CAMK2D,DYRK1B,EIF2AK3,STK33,TTK | 6 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1992 | 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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 110.81 | 51.21 | 38 | 1287 | 53553 | 90573569 |
| Neutrophil count decreased | 107.39 | 51.21 | 40 | 1285 | 71492 | 90555630 |
| White blood cell count decreased | 104.25 | 51.21 | 50 | 1275 | 167059 | 90460063 |
| Bone marrow failure | 99.61 | 51.21 | 31 | 1294 | 32190 | 90594932 |
| Platelet count decreased | 76.34 | 51.21 | 38 | 1287 | 136931 | 90490191 |
| Vomiting | 74.74 | 51.21 | 73 | 1252 | 788220 | 89838902 |
| Nausea | 70.41 | 51.21 | 83 | 1242 | 1110233 | 89516889 |
| Initial insomnia | 55.76 | 51.21 | 15 | 1310 | 9295 | 90617827 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 103.85 | 46.31 | 38 | 962 | 40423 | 42579912 |
| White blood cell count decreased | 86.98 | 46.31 | 45 | 955 | 110351 | 42509984 |
| Platelet count decreased | 74.72 | 46.31 | 44 | 956 | 138537 | 42481798 |
| Neutrophil count decreased | 62.01 | 46.31 | 30 | 970 | 63385 | 42556950 |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 199.73 | 40.12 | 77 | 2513 | 94263 | 110492446 |
| White blood cell count decreased | 190.68 | 40.12 | 97 | 2493 | 229293 | 110357416 |
| Neutrophil count decreased | 161.47 | 40.12 | 71 | 2519 | 120870 | 110465839 |
| Platelet count decreased | 147.66 | 40.12 | 82 | 2508 | 230361 | 110356348 |
| Bone marrow failure | 125.02 | 40.12 | 48 | 2542 | 57800 | 110528909 |
| Lymphocyte count decreased | 77.48 | 40.12 | 34 | 2556 | 57209 | 110529500 |
| Hypokalaemia | 63.18 | 40.12 | 44 | 2546 | 182404 | 110404305 |
| Hypocalcaemia | 55.05 | 40.12 | 28 | 2562 | 65338 | 110521371 |
| Hepatic function abnormal | 54.84 | 40.12 | 31 | 2559 | 89264 | 110497445 |
| Vomiting | 53.25 | 40.12 | 84 | 2506 | 910591 | 109676118 |
| Initial insomnia | 47.11 | 40.12 | 15 | 2575 | 10374 | 110576335 |
| Nausea | 45.31 | 40.12 | 93 | 2497 | 1235597 | 109351112 |
| Hypoalbuminaemia | 45.06 | 40.12 | 19 | 2571 | 28955 | 110557754 |
| Anaemia | 44.33 | 40.12 | 59 | 2531 | 547027 | 110039682 |
| Hypoproteinaemia | 41.65 | 40.12 | 12 | 2578 | 5933 | 110580776 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A04AA03 | ALIMENTARY TRACT AND METABOLISM ANTIEMETICS AND ANTINAUSEANTS ANTIEMETICS AND ANTINAUSEANTS Serotonin (5HT3) antagonists |
| MeSH PA | D000932 | Antiemetics |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D058831 | Serotonin 5-HT3 Receptor Antagonists |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:36335 | trypanocidal drug |
| CHEBI has role | CHEBI:47958 | nicotinic acetylcholine receptor agonist |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:50846 | immunomodulator |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:63726 | neuroprotective agent |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:68494 | apoptosis inhibitor |
Related Drugs by ATC class:
A04AA Serotonin (5HT3) antagonists 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chemotherapy-induced nausea and vomiting | indication | 236084000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.91 | acidic |
| pKa2 | 9.49 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 3A | Ion channel | ANTAGONIST | Ki | 8.80 | IUPHAR | IUPHAR | |||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.59 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.28 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 5.61 | DRUG MATRIX | |||||
| Glycine receptor subunit alpha-1 | Ion channel | ANTAGONIST | Ki | 4.10 | IUPHAR | ||||
| Glycine receptor subunit alpha-2 | Ion channel | ANTAGONIST | Ki | 4.90 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 4 | GPCR | Ki | 6.85 | WOMBAT-PK | |||||
| Neuronal acetylcholine receptor subunit alpha-7 | Ion channel | Ki | 8.16 | CHEMBL | |||||
| Glycine receptor subunit beta | Ion channel | ANTAGONIST | Ki | 5.30 | IUPHAR | ||||
| Neuronal acetylcholine receptor; alpha4/beta2 | Ion channel | Ki | 4.26 | CHEMBL | |||||
| Acetylcholine receptor; alpha1/beta1/delta/gamma | Ion channel | Ki | 4.57 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 3B | Ion channel | Ki | 8.80 | CHEMBL | |||||
| Neuronal acetylcholine receptor subunit alpha-3 | Ion channel | Ki | 4.80 | CHEMBL | |||||
| Neuronal acetylcholine receptor subunit alpha-7 | Ion channel | EC50 | 8 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | Ki | 7.20 | CHEMBL | |||||
| Neuronal acetylcholine receptor subunit alpha-7 | Ion channel | Ki | 8.16 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 3A | Ion channel | Kd | 7.52 | CHEMBL | |||||
| Serotonin 3 (5-HT3) receptor | Ion channel | Ki | 8.89 | CHEMBL | |||||
| Serotonin 3 receptor (5HT3) | Ion channel | Ki | 8.42 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | Ki | 6.90 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | ANTAGONIST | Ki | 7.10 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D02041 | KEGG_DRUG |
| C0063322 | UMLSCUI |
| CHEBI:32269 | CHEBI |
| TKT | PDB_CHEM_ID |
| CHEMBL56564 | ChEMBL_ID |
| DB11699 | DRUGBANK_ID |
| D000077526 | MESH_DESCRIPTOR_UI |
| 656665 | PUBCHEM_CID |
| 260 | IUPHAR_LIGAND_ID |
| 6535 | INN_ID |
| 105826-92-4 | SECONDARY_CAS_RN |
| 6I819NIK1W | UNII |
| 235997 | RXNORM |
| 004472 | NDDF |
| 004473 | NDDF |
| 322201005 | SNOMEDCT_US |
| 395917006 | SNOMEDCT_US |
| 426339000 | SNOMEDCT_US |
| 6I819NIK1W | INXIGHT DRUGS |
Pharmaceutical products:
None