trimetaphan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2752 | 7187-66-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A nicotinic antagonist that has been used as a ganglionic blocker in hypertension, as an adjunct to anesthesia, and to induce hypotension during surgery.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.25 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.11 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | ROCHE |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C02BA01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, GANGLION-BLOCKING Sulfonium derivatives |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| CHEBI has role | CHEBI:35620 | vasodilator agents |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| CHEBI has role | CHEBI:48878 | nicotinic antagonists |
| CHEBI has role | CHEBI:60807 | anaesthestic adjuvant |
| MeSH PA | D000759 | Adjuvants, Anesthesia |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D005730 | Ganglionic Blockers |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018733 | Nicotinic Antagonists |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pulmonary edema | indication | 19242006 | DOID:11396 |
| Hypertensive Emergencies | indication | ||
| Controlled Hypotension | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Neuronal acetylcholine receptor; alpha3/beta4 | Ion channel | ANTAGONIST | WOMBAT-PK | CHEMBL | |||||
| Neuronal acetylcholine receptor subunit alpha-10 | Ion channel | WOMBAT-PK | |||||||
| Neuronal acetylcholine receptor subunit alpha-7 | Ion channel | WOMBAT-PK | |||||||
| Acetylcholine receptor subunit alpha | Ion channel | IC50 | 5.15 | CHEMBL | |||||
| Nicotinic acetylcholine receptor alpha 5 subunit | Ion channel | Ki | 5.56 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000007602 | NUI |
| D00612 | KEGG_DRUG |
| 4017807 | VANDF |
| CHEBI:9728 | CHEBI |
| CHEMBL1201329 | ChEMBL_ID |
| C017774 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68-91-7 | SECONDARY_CAS_RN |
| DB01116 | DRUGBANK_ID |
| 10828 | RXNORM |
| 5631 | MMSL |
| d00738 | MMSL |
| 000654 | NDDF |
| 004498 | NDDF |
| 20217007 | SNOMEDCT_US |
| 350607006 | SNOMEDCT_US |
| 373771001 | SNOMEDCT_US |
| C0041040 | UMLSCUI |
| D014294 | MESH_DESCRIPTOR_UI |
| CHEMBL1245 | ChEMBL_ID |
| 23576 | PUBCHEM_CID |
| 296 | INN_ID |
| 6G8X656T45 | UNII |
Pharmaceutical products:
None