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QuickView for Pentobarbital (compound)


PubChem
Name: Pentobarbital
PubChem Compound ID: 11514319
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)
Molecular formula: C11H18N2NaO3+
Molecular weight: 249.262 g/mol
DrugBank
Identification
Name: Pentobarbital
Name (isomeric): DB00312
Drug Type: small molecule
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)
Synonyms:
Sodium Pentobarbital; Pentabarbitone; Pentobarbitone; Pentabarbital; Pentobarbital Sodium; Pentobarbiturate; Pentobarbituric acid
Brand: Nembutal, Neodorm, Dorsital, Nembutal Sodium, Rivadorm, Nebralin, Mebumal, Mebubarbital, Ethaminal
Brand name mixture: Cafergot PB Sup(Belladonna + Caffeine + Ergotamine Tartrate + Pentobarbital), Cafergot PB Tab(Belladonna + Caffeine + Ergotamine Tartrate + Pentobarbital Sodium)
Category: Adjuvants, Anesthesia, GABA Modulators, Hypnotics and Sedatives, Barbiturates
CAS number: 76-74-4
Pharmacology
Indication: For the short-term treatment of insomnia.
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.
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 co...
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Absorption: Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
Biotransformation: by hepatic microsomal enzyme system
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.
Half Life: 5 to 50 hours (dose dependent)
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.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
VerapamilPentobarbital, 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.
PrednisoneThe barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisone.
TriprolidineThe CNS depressants, Triprolidine and Pentobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
FludrocortisoneThe barbiturate, pentobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
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