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QuickView for Butalbital (compound)

Name: butalbital
PubChem Compound ID: 2481
Molecular formula: C11H16N2O3
Molecular weight: 224.256 g/mol
Allylisobutylbarbital; D03182; DEA No. 2100; Tetrallobarbital; NINDS_000970; Sandoptal (TN); 23554-70-3; Butalbarbital; Allylbarbital; Profundal.
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Name: butalbital
Name (isomeric): DB00241
Drug Type: small molecule
Butalbital M (OH); Allylbarbital
Brand name mixture:
Trianal Tablet(Acetylsalicylic Acid + Butalbital + Caffeine), Trianal-C 1/2 Capsule(Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate), Ratio-Tecnal(Acetylsalicylic Acid + Butalbital + Caffeine), Fiorinal C1/2 Cap(Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate), Ratio-Tecnal C1/4(Acetylsalicylic Acid + Butalbital...
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Category: Analgesics
CAS number: 77-26-9
Indication: Used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain.
Pharmacology: Butalbital is a short to intermediate-acting barbiturate. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia.
Mechanism of Action: Butalbital 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.
Absorption: Well absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body.
Protein binding: 45%
Biotransformation: Hepatic, although most of the dose is eliminated via the kidney (59 to 88%). Urinary excretion products included parent drug (about 3.6% of the dose), 5-isobutyl-5-(2,3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8%).
Half Life: 35 hours
Toxicity: Symptoms of acute barbiturate poisoning include drowsiness, confusion, coma, respiratory depression, hypotension, and shock.
Affected organisms: Humans and other mammals
Drug interaction:
EstradiolThe enzyme inducer, butalbital, decreases the effect of the hormone agent, estradiol.
VoriconazoleButalbital may reduce serum concentrations and efficacy of voriconazole. Concomitant voriconazole and long-acting barbiturates therapy is contraindicated.
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
TeniposideBarbiturates such as butalbital may decrease the serum concentration of teniposide. Consider alternatives to combined treatment with barbiturates and teniposide due to the potential for decreased teniposide concentrations. If the combination cannot be avoided, monitor teniposide response closely.
FelodipineThe barbiturate, butalbital, decreases the effect of felodipine.
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