Drug/Small Molecule:
butalbital

2D structure

Overview

Generic Names: Allylbarbital; Butalbital M (OH)
Brand Mixtures: Fiorinal C1/2 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate); Fiorinal C1/4 Cap (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate); Fiorinal Tab (Acetylsalicylic Acid + Butalbital + Caffeine); Ratio-Tecnal (Acetylsalicylic Acid + Butalbital + Caffeine); Ratio-Tecnal C 1/2 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate); Ratio-Tecnal C1/4 (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate); Trianal Capsules (Acetylsalicylic Acid + Butalbital + Caffeine); Trianal Tablet (Acetylsalicylic Acid + Butalbital + Caffeine); Trianal-C 1/2 Capsule (Acetylsalicylic Acid + Butalbital + Caffeine + Codeine Phosphate)
PharmGKB Accession Id: PA448695

Description

Butalbital, 5-allyl-5-isobutylbarbituric acid, is a barbiturate with an intermediate duration of action. It has the same chemical formula as talbutal but a different structure. Butalbital is often combined with other medications, such as acetaminophen or aspirin, and is commonly prescribed for the treatment of pain and headache. Wikipedia (source: Drug Bank)

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. (source: Drug Bank)

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Butalbital binds at a distinct binding site associated with a Cl<sup>-</sup> ionopore at the GABA<sub>A</sub> receptor, increasing the duration of time for which the Cl<sup>-</sup> ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. (source: Drug Bank)

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. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

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%). (source: Drug Bank)

Protein Binding

45% (source: Drug Bank)

Absorption

Well absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body. (source: Drug Bank)

Toxicity

Symptoms of acute barbiturate poisoning include drowsiness, confusion, coma, respiratory depression, hypotension, and shock. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)CC1(C(=O)NC(=O)NC1=O)CC=C (source: Drug Bank)

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)

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

Non-Curated Information

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

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00241
PubChem Compound ID:
2481
PubChem Substance ID:
149431

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Non-Curated Publications

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

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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