pentobarbital Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypnotics, barbituric acid derivatives | 2095 | 76-74-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 0.10 | g | P |
| 0.10 | g | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 12.61 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.91 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.47 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.39 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 22 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 19, 1973 | FDA | OAK PHARMS |
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 |
|---|---|---|---|---|---|---|
| Status epilepticus | 149.19 | 80.21 | 37 | 793 | 13942 | 46671290 |
| Propofol infusion syndrome | 133.03 | 80.21 | 21 | 809 | 760 | 46684472 |
| Mitochondrial DNULL mutation | 123.35 | 80.21 | 17 | 813 | 234 | 46684998 |
| Gene mutation | 112.29 | 80.21 | 19 | 811 | 1061 | 46684171 |
| Blood gases abnormal | 92.96 | 80.21 | 15 | 815 | 623 | 46684609 |
| Drug ineffective for unapproved indication | 86.93 | 80.21 | 25 | 805 | 16388 | 46668844 |
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 |
|---|
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05CA01 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Barbiturates, plain |
| MeSH PA | D000759 | Adjuvants, Anesthesia |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| MeSH PA | D006993 | Hypnotics and Sedatives |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:91016 | gabaa receptor agonists |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| General anesthesia | indication | 50697003 | |
| Severe anxiety (panic) | indication | 80583007 | |
| Epilepsy | indication | 84757009 | DOID:1826 |
| Seizure disorder | indication | 128613002 | |
| Insomnia | indication | 193462001 | |
| Status epilepticus | indication | 230456007 | DOID:1824 |
| Cerebral ischemia | indication | 287731003 | |
| Local anesthesia | indication | 386761002 | |
| Tetanus Adjunct Treatment | indication | ||
| Benign intracranial hypertension | off-label use | 68267002 | DOID:11459 |
| Apnea | contraindication | 1023001 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Hyperammonemia | contraindication | 9360008 | |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Hepatic encephalopathy | contraindication | 13920009 | DOID:13413 |
| Disorder of lung | contraindication | 19829001 | DOID:850 |
| Depressive disorder | contraindication | 35489007 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hyperactive behavior | contraindication | 44548000 | |
| Low blood pressure | contraindication | 45007003 | |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Hepatic failure | contraindication | 59927004 | |
| Substance abuse | contraindication | 66214007 | |
| Hepatic coma | contraindication | 72836002 | DOID:12550 |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Decreased respiratory function | contraindication | 80954004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Pneumonia | contraindication | 233604007 | DOID:552 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Sleep automatism | contraindication | 247962006 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Respiratory insufficiency | contraindication | 409623005 | |
| Porphyria | contraindication | 418470004 | |
| Acute exacerbation of asthma | contraindication | 708038006 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.81 | acidic |
| pKa2 | 9.51 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit beta-3 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | IC50 | 4.06 | CHEMBL | CHEMBL | |||
| GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 4.30 | WOMBAT-PK | CHEMBL | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 2.55 | WOMBAT-PK | |||||
| GABA A receptor alpha-2/beta-2/gamma-2 | Ion channel | EC50 | 4.30 | CHEMBL | |||||
| GABA-A receptor; anion channel | Ion channel | IC50 | 5.77 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018516 | VUID |
| N0000146838 | NUI |
| D00499 | KEGG_DRUG |
| 24876-35-5 | SECONDARY_CAS_RN |
| 4018036 | VANDF |
| 4018516 | VANDF |
| C0947688 | UMLSCUI |
| CHEBI:7983 | CHEBI |
| RAV | PDB_CHEM_ID |
| CHEMBL448 | ChEMBL_ID |
| CHEMBL971 | ChEMBL_ID |
| D010424 | MESH_DESCRIPTOR_UI |
| DB00312 | DRUGBANK_ID |
| 4737 | PUBCHEM_CID |
| 5480 | IUPHAR_LIGAND_ID |
| 703 | INN_ID |
| I4744080IR | UNII |
| 203085 | RXNORM |
| 2161 | MMSL |
| 3697 | MMSL |
| 5253 | MMSL |
| 5254 | MMSL |
| 71886 | MMSL |
| d00335 | MMSL |
| 001411 | NDDF |
| 001412 | NDDF |
| 33231001 | SNOMEDCT_US |
| 372703009 | SNOMEDCT_US |
| 66843009 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pentobarbital Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-181 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Pentobarbital Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24201-010 | INJECTION, SOLUTION | 50 mg | INTRAMUSCULAR | ANDA | 24 sections |
| pentobarbital sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 25021-676 | INJECTION, SOLUTION | 50 mg | INTRAVENOUS | ANDA | 26 sections |
| Nembutal Sodium | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76478-501 | INJECTION | 50 mg | INTRAVENOUS | ANDA | 25 sections |