methohexital 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypnotics, barbituric acid derivatives | 1748 | 151-83-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 100 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 7.62 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 12 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.27 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 27, 1960 | FDA | PAR STERILE PRODUCTS |
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 | N01AF01 | NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Barbiturates, plain |
| ATC | N05CA15 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Barbiturates, plain |
| FDA CS | M0002177 | Barbiturates |
| MeSH PA | D000777 | Anesthetics |
| MeSH PA | D018686 | Anesthetics, Intravenous |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| CHEBI has role | CHEBI:38877 | intravenous anesthetics |
| FDA EPC | N0000175693 | Barbiturate |
| CHEBI has role | CHEBI:88188 | allergenic drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| General anesthesia | indication | 50697003 | |
| Local anesthesia | indication | 386761002 | |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Shock | contraindication | 27942005 | |
| Low blood pressure | contraindication | 45007003 | |
| Chronic heart failure | contraindication | 48447003 | |
| Hepatic failure | contraindication | 59927004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Seizure disorder | contraindication | 128613002 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Morbid obesity | contraindication | 238136002 | DOID:11981 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Porphyria | contraindication | 418470004 | |
| Hypertensive urgency | contraindication | 443482000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.3 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor alpha-1/beta-3/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | WOMBAT-PK | CHEMBL | |||||
| Glycine receptor subunit alpha-1 | Ion channel | WOMBAT-PK | |||||||
| Neuronal acetylcholine receptor; alpha2/beta2 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019827 | VUID |
| N0000147915 | NUI |
| D00712 | KEGG_DRUG |
| 309-36-4 | SECONDARY_CAS_RN |
| 4017455 | VANDF |
| 4019827 | VANDF |
| C0025668 | UMLSCUI |
| CHEBI:102216 | CHEBI |
| CHEMBL7413 | ChEMBL_ID |
| DB00474 | DRUGBANK_ID |
| CHEMBL30219 | ChEMBL_ID |
| D008723 | MESH_DESCRIPTOR_UI |
| 9034 | PUBCHEM_CID |
| 7233 | IUPHAR_LIGAND_ID |
| 807 | INN_ID |
| E5B8ND5IPE | UNII |
| 6847 | RXNORM |
| 184408 | MMSL |
| 3682 | MMSL |
| 5076 | MMSL |
| d00929 | MMSL |
| 001400 | NDDF |
| 004580 | NDDF |
| 373488009 | SNOMEDCT_US |
| 39124003 | SNOMEDCT_US |
| 91594002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Brevital Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-105 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 500 mg | INTRAMUSCULAR | NDA | 26 sections |