PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
phenobarbital

2D structure

Overview

Generic Names: Fenobarbital; Phenobarbitol; Phenobarbituric Acid; Phenylethylbarbiturate; Phenylethylbarbituric Acid; Phenylethylmalonylurea
Trade Names: Adonal; Aephenal; Agrypnal; Amylofene; Aphenylbarbit; Aphenyletten; Barbenyl; Barbinal; Barbiphen; Barbiphenyl; Barbipil; Barbita; Barbivis; Barbonal; Barbophen; Bardorm; Bartol; Bialminal; Blu-Phen; Cabronal; Calmetten; Calminal; Cardenal; Chinoin; Codibarbita; Coronaletta; Cratecil; Damoral; Dezibarbitur; Dormina; Dormiral; Dormital; Doscalun; Duneryl; Ensobarb; Ensodorm; Epanal; Epidorm; Epilol; Episedal; Epsylone; Eskabarb; Etilfen; Euneryl; Fenbital; Fenemal; Fenosed; Fenylettae; Gardenal; Gardepanyl; Glysoletten; Haplopan; Haplos; Helional; Hennoletten; Henotal; Hypnaletten; Hypnette; Hypno-Tablinetten; Hypnogen; Hypnolone; Hypnoltol; Hysteps; Lefebar; Leonal; Lephebar; Lepinal; Lepinaletten; Linasen; Liquital; Lixophen; Lubergal; Lubrokal; Lumen; Lumesettes; Lumesyn; Luminal; Lumofridetten; Luphenil; Luramin; Molinal; Neurobarb; Nirvonal; Noptil; Nova-Pheno; Nunol; Parkotal; Pharmetten; Phen-Bar; Phenaemal; Phenemal; Phenemalum; Phenobal; Phenobarbyl; Phenoluric; Phenolurio; Phenomet; Phenonyl; Phenoturic; Phenyletten; Phenyral; Phob; Polcominal; Promptonal; Seda-Tablinen; Sedabar; Sedicat; Sedizorin; Sedlyn; Sedofen; Sedonal; Sedonettes; Sevenal; Sinoratox; Solfoton; Solfoton Talpheno; Solu-Barb; Sombutol; Somnolens; Somnoletten; Somnosan; Somonal; Spasepilin; Starifen; Starilettae; Stental; Stental Extentabs; Talpheno; Teolaxin; Teoloxin; Thenobarbital; Theoloxin; Triabarb; Tridezibarbitur; Triphenatol; Versomnal; Zadoletten; Zadonal
PharmGKB Accession Id: PA450911

Description

A barbituric acid derivative that acts as a nonselective central nervous system depressant. It promotes binding to inhibitory gamma-aminobutyric acid subtype receptors, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. PubChem (source: Drug Bank)

Indication

For the treatment of all types of seizures except absence seizures. (source: Drug Bank)

ATC Therapeutic Category

  • N03AA:Barbiturates and derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Phenobarbital acts on GABAA receptors, increasing synaptic inhibition. This has the effect of elevating seizure threshold and reducing the spread of seizure activity from a seizure focus. Phenobarbital may also inhibit calcium channels, resulting in a decrease in excitatory transmitter release. The sedative-hypnotic effects of phenobarbital are likely the result of its effect on the polysynaptic midbrain reticular formation, which controls CNS arousal. (source: Drug Bank)

Pharmacology

Phenobarbital, the longest-acting barbiturate, is used for its anticonvulsant and sedative-hypnotic properties in the management of all seizure disorders except absence (petit mal). (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
Take on an empty stomach for quicker absorption (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (mostly via CYP2C19). (source: Drug Bank)

Protein Binding

20 to 45% (source: Drug Bank)

Absorption

Absorbed in varying degrees following oral, rectal or parenteral administration. The salts are more rapidly absorbed than are the acids. The rate of absorption is increased if the sodium salt is ingested as a dilute solution or taken on an empty stomach. (source: Drug Bank)

Toxicity

CNS and respiratory depression which may progress to Cheyne-Stokes respiration, areflexia, constriction of the pupils to a slight degree (though in severe poisoning they may wshow paralytic dilation), oliguria, tachycardia, hypotension, lowered body temperature, and coma. Typical shock syndrome (apnea, circulatory collapse, respiratory arrest, and death) may occur. (source: Drug Bank)

Isomeric SMILES Code:

CCC1(C(=O)NC(=O)NC1=O)c2ccccc2 (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs2032582 at chr7:86998554 in ABCB1
    This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).
    Variant Name:
    ABCB1: 2677T/A>G
    Related Drugs:
    carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
    Related Diseases:
    Epilepsy
    Evidence:
    PMID:19450124
  2. rs3789243 at chr7:87058822 in ABCB1
    This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).
    Related Drugs:
    carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
    Related Diseases:
    Epilepsy
    Evidence:
    PMID:19450124
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2B6
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
  •   
  •   
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP2C8
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  •   
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP2E1
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Has annotations
DRD2
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
NR1I3
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
PRKAA1
  •   
  • PD
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
UGT1A1
  • CO
  • PD
  • PK
  • FA
  • GN
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
GABRA1 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
clonazepam
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
donepezil
  •   
  •   
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
acenocoumarol Uncurated Annotation The barbiturate decreases the anticoagulant effect (source: Drug Bank)
clomifene Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
cortisone acetate Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
cyclosporine Uncurated Annotation The barbiturate decreases the effect of cyclosporine (source: Drug Bank)
dasatinib Uncurated Annotation Decreased levels/efficacy of ddasatinib (source: Drug Bank)
delavirdine Uncurated Annotation The anticonvulsant decreases the effect of delavirdine (source: Drug Bank)
dexamethasone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
dicumarol Uncurated Annotation The barbiturate decreases the anticoagulant effect (source: Drug Bank)
diethylstilbestrol Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
disopyramide Uncurated Annotation Phenobarbital decreases levels of disopyramide (source: Drug Bank)
doxycycline Uncurated Annotation The anticonvulsant decreases the effect of doxycycline (source: Drug Bank)
estradiol Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
estrone Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
ethinyl estradiol Uncurated Annotation This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
felbamate Uncurated Annotation Felbamate increases the effect and toxicity of phenobarbital/primidone (source: Drug Bank)
felodipine Uncurated Annotation The barbiturate decreases the effect of felodipine (source: Drug Bank)
folic acid Uncurated Annotation Folic acid decreases the effect of anticonvulsant (source: Drug Bank)
gefitinib Uncurated Annotation This CYP3A4 inducer may reduce gefitinib plasma concentrations and pharmacological effects (source: Drug Bank)
griseofulvin Uncurated Annotation The barbiturate decreases the effect of griseofulvin (source: Drug Bank)
hydrocortisone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
imatinib Uncurated Annotation Phenobarbital decreases levels of imatinib (source: Drug Bank)
itraconazole Uncurated Annotation The barbiturate decreases the effect of itraconazole (source: Drug Bank)
levonorgestrel Uncurated Annotation Phenobarbital decreases the effect of levonorgestrel (source: Drug Bank)
medroxyprogesterone Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
megestrol Uncurated Annotation The enzyme inducer decreases the effect of hormones (source: Drug Bank)
mestranol Uncurated Annotation This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
methadone Uncurated Annotation The barbiturate decreases the effect of methadone (source: Drug Bank)
methoxyflurane Uncurated Annotation The barbiturate increases the renal toxicity of methoxyflurane (source: Drug Bank)
methylprednisolone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
metoprolol Uncurated Annotation The barbiturate decreases the effect of the metabolized beta-blocker (source: Drug Bank)
metronidazole Uncurated Annotation The barbiturate decreases the effect of metronidazole (source: Drug Bank)
nifedipine Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
norethindrone Uncurated Annotation This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
prednisolone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
prednisone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
propranolol Uncurated Annotation The barbiturate decreases the effect of the metabolized beta-blocker (source: Drug Bank)
quinidine Uncurated Annotation The anticonvulsant decreases the effect of quinidine (source: Drug Bank)
sunitinib Uncurated Annotation Possible decrease in sunitinib levels (source: Drug Bank)
theophylline Uncurated Annotation The barbiturate decreases the effect of theophylline (source: Drug Bank)
triamcinolone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
verapamil Uncurated Annotation The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
voriconazole Uncurated Annotation The barbiturate decreases the effect of voriconazole (source: Drug Bank)
warfarin Uncurated Annotation The barbiturate decreases the anticoagulant effect (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Drug Hypersensitivity
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Drug Toxicity
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Epidermal Necrolysis, Toxic
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Epilepsy
  •   
  • PD
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
HIV
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Leukemia
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Stevens-Johnson Syndrome
  •   
  • PD
  •   
  •   
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

  1. Genetic determinants of UGT1A1 inducibility by phenobarbital in hepatocytes
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • PD
    • FA
    Submitted by Mark J. Ratain, MD involving UGT1A1, and phenobarbital
  2. mRNA expression levels of PXR splice variants in livers
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • FA
    Submitted by Erin G. Schuetz, PhD involving CYP3A4, NR1I2, , amiodarone, cimetidine, dopamine, erythromycin, ethanol, glucocorticoids, hmg coa reductase inhibitors, midazolam, nicotine, phenobarbital, phenytoin, propofol, thyroid preparations and vasopressin

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01174
ChEBI ID:
8069
KEGG Compound ID:
C07434
KEGG Drug ID:
D00506
PubChem Compound ID:
4763
PubChem Substance ID:
7847572

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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