methohexital ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
hypnotics, barbituric acid derivatives 1748 151-83-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • methohexital
  • enallynymall
  • methodrexitone
  • methohexitone
  • methohexital sodium
  • metoesital
  • brevital sodium
An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.
  • Molecular weight: 262.31
  • Formula: C14H18N2O3
  • CLOGP: 1.81
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 66.48
  • ALOGS: -3.70
  • ROTB: 5

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.3 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
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
CHEMBL30219 ChEMBL_ID
DB00474 DRUGBANK_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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Brevital Sodium HUMAN PRESCRIPTION DRUG LABEL 1 42023-105 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 500 mg INTRAMUSCULAR NDA 26 sections