Drug/Small Molecule:
pentobarbital

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Pentabarbital
  • Pentabarbitone
  • Pentobarbital Sodium
  • Pentobarbitone
  • Pentobarbiturate
  • Pentobarbituric acid
  • Sodium Pentobarbital
Trade Names
  • Dorsital
  • Ethaminal
  • Mebubarbital
  • Mebumal
  • Nebralin
  • Nembutal
  • Nembutal Sodium
  • Neodorm
  • Rivadorm
Brand Mixture Names
  • Cafergot PB Sup (Belladonna + Caffeine + Ergotamine Tartrate + Pentobarbital)
  • Cafergot PB Tab (Belladonna + Caffeine + Ergotamine Tartrate + Pentobarbital Sodium)

PharmGKB Accession Id:
PA450859

Description

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)

Source: Drug Bank

Indication

For the short-term treatment of insomnia.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

Source: Drug Bank

Pharmacology

Pentobarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

by hepatic microsomal enzyme system

Source: Drug Bank

Absorption

Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.

Source: Drug Bank

Half-Life

5 to 50 hours (dose dependent)

Source: Drug Bank

Toxicity

Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.

Source: Drug Bank

Route of Elimination

Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.

Source: Drug Bank

Chemical Properties

Chemical Formula

C11H18N2O3

Source: Drug Bank

Isomeric SMILES

CCCC(C)C1(C(=O)NC(=O)NC1=O)CC

Source: OpenEye

Canonical SMILES

CCCC(C)C1(CC)C(=O)NC(=O)NC1=O

Source: Drug Bank

Average Molecular Weight

226.2722

Source: Drug Bank

Monoisotopic Molecular Weight

226.131742452

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
CHRNA4 (source: Drug Bank)
CHRNA7 (source: Drug Bank)
GABRA1 (source: Drug Bank)
GABRA2 (source: Drug Bank)
GABRA3 (source: Drug Bank)
GABRA4 (source: Drug Bank)
GABRA5 (source: Drug Bank)
GABRA6 (source: Drug Bank)
GRIA2 (source: Drug Bank)
GRIK2 (source: Drug Bank)

Drug Interactions

Drug Description
pentobarbital The barbiturate, pentobarbital, decreases the effect of aminophylline. (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, betamethasone. (source: Drug Bank)
pentobarbital The enzyme inducer decreases the effect of hormones (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, clomifene. (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
pentobarbital The barbiturate increases the effect of cyclosporine (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, increases the effect of cyclosporine. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, dexamethasone. (source: Drug Bank)
pentobarbital The enzyme inducer decreases the effect of hormones (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, diethylstilbestrol. (source: Drug Bank)
pentobarbital Divalproex sodium increases the effect of the barbiturate, pentobarbital. (source: Drug Bank)
pentobarbital The anticonvulsant decreases the effect of doxycycline (source: Drug Bank)
pentobarbital The anticonvulsant, pentobarbital, decreases the effect of doxycycline. (source: Drug Bank)
pentobarbital The enzyme inducer decreases the effect of hormones (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, estradiol. (source: Drug Bank)
pentobarbital This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
pentobarbital This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of felodipine (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of felodipine. (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, fludrocortisone. (source: Drug Bank)
pentobarbital Folic acid decreases the effect of anticonvulsant (source: Drug Bank)
pentobarbital Folic acid decreases the effect of anticonvulsant, pentobarbital. (source: Drug Bank)
pentobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank)
pentobarbital The CYP3A4 inducer, pentobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of griseofulvin (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of griseofulvin. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, hydrocortisone. (source: Drug Bank)
pentobarbital Phenobarbital decreases the effect of levonorgestrel (source: Drug Bank)
pentobarbital Phenobarbital decreases the effect of levonorgestrel (source: Drug Bank)
pentobarbital The enzyme inducer decreases the effect of hormones (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, medroxyprogesterone. (source: Drug Bank)
pentobarbital The enzyme inducer decreases the effect of hormones (source: Drug Bank)
pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, megestrol. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of methadone (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of methadone. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metronidazole (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of metronidazole. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the calcium channel blocker (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of the calcium channel blocker, nifedipine. (source: Drug Bank)
pentobarbital This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
pentobarbital This product may cause a slight decrease of contraceptive effect (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of oxtriphylline. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisolone. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisone. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of metabolized beta-blocker (source: Drug Bank)
pentobarbital The anticonvulsant decreases the effect of quinidine (source: Drug Bank)
pentobarbital The anticonvulsant, pentobarbital, decreases the effect of quinidine. (source: Drug Bank)
pentobarbital Pentobarbital may decrease the plasma concentration of Telithromycin. Consider alternate therapy. (source: Drug Bank)
pentobarbital Pentobarbital may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of theophylline (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, decreases the effect of theophylline. (source: Drug Bank)
pentobarbital Pentobarbital may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance. (source: Drug Bank)
pentobarbital The CYP3A4 inducer, Pentobarbital, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Pentobarbital is initiated, discontinued or dose changed. (source: Drug Bank)
pentobarbital The CYP3A4 inducer, Pentobarbital, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Pentobarbital is initiated, discontinued or dose changed. (source: Drug Bank)
pentobarbital The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, triamcinolone. (source: Drug Bank)
pentobarbital The barbiturate, Pentobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Pentobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required. (source: Drug Bank)
pentobarbital The CNS depressants, Triprolidine and Pentobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
pentobarbital The CNS depressants, Triprolidine and Pentobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
pentobarbital Pentobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Pentobarbital is initiated, discontinued or dose changed. (source: Drug Bank)
pentobarbital Pentobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if pentobarbital is initiated, discontinued or dose changed. (source: Drug Bank)

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to pentobarbital: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
67386-501-55
DrugBank:
DB00312
ChEBI:
7983
KEGG Compound:
C07422
KEGG Drug:
D00499
PubChem Compound:
4737
PubChem Substance:
46508399
9626
Drugs Product Database (DPD):
141690
ChemSpider:
4575
Therapeutic Targets Database:
DAP000671
FDA Drug Label at DailyMed:
f302ddf5-0213-43b3-b6c1-b3edf2bafbcd

Clinical Trials

These are trials that mention pentobarbital and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.