Migraine and headache:

Indications for: Butalbital/Aspirin/Caffeine

Tension (or muscle contraction) headache.

Adult Dosage:

Use lowest effective dose for shortest duration. Not recommended for extended or repeated use. 1–2 caps every 4hrs, as needed; max 6 caps/day. 

Children Dosage:

Not established.

Butalbital/Aspirin/Caffeine Contraindications:

Hemorrhagic diathesis (eg, hemophilia, hypoprothrombinemia, von Willebrand's disease, the thrombocytopenias, thrombasthenia and other ill-defined hereditary platelet dysfunctions, severe vitamin K deficiency, severe liver damage). Syndrome of nasal polyps, angioedema and bronchospastic reactivity to aspirin or other nonsteroidal anti-inflammatory drugs. Peptic ulcer or other serious GI lesions. Porphyria.

Butalbital/Aspirin/Caffeine Warnings/Precautions:

Abuse potential. Bleeding disorders. Coagulation disorders. Head injuries. Elevated intracranial pressure. Acute abdominal conditions. Hypothyroidism. Urethral stricture. Addison's disease. Prostatic hypertrophy. Underlying hemostatic defects. Reye's syndrome. Children/teenagers with chicken pox or flu. Asthma. Aspirin allergy. Severe renal or hepatic impairment. Elderly. Debilitated. Embryo-fetal toxicity. Pregnancy (avoid during ≥30 weeks gestation): increased risk of premature closure of the fetal ductus arteriosus; (20–30 weeks gestation): may cause fetal renal dysfunction/oligohydramnios; if treatment needed, limit dose and duration of use. Risk of neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.

See Also:

Butalbital/Aspirin/Caffeine Classification:

Barbiturate + salicylate + methylxanthine.

Butalbital/Aspirin/Caffeine Interactions:

Additive effects of CNS depression with alcohol and other CNS depressants (eg, narcotic analgesics, general anesthetics, tranquilizers, chlordiazepoxide, sedative-hypnotics); avoid. Concomitant MAOIs may enhance CNS effects. Increased risk of bleeding with concomitant NSAIDs (avoid), oral anticoagulants. Increased hypoglycemia with oral antidiabetic agents, insulin. Withdrawal of corticosteroids may result in salicylism in those receiving concomitant corticosteroids and chronic use of aspirin. May potentiate 6-mercaptopurine, methotrexate. Antagonizes uricosuric agents (eg, probenecid, sulfinpyrazone). May interfere with lab tests in blood or urine (eg, serum amylase, fasting blood glucose, cholesterol, protein, SGOT, uric acid, prothrombin time, bleeding time, glucose, 5- hydroxyindoleacetic acid, Gerhardt ketone, VMA, uric acid, diacetic acid, and spectrophotometric detection of barbiturates).

Adverse Reactions:

Drowsiness, dizziness, lightheadedness, nausea, vomiting, flatulence; hypersensitivity reactions, DRESS (discontinue if occurs), erythema multiforme, TEN.

Note:

Formerly known under the brand name Fiorinal.

Metabolism:

Aspirin: The biotransformation of aspirin occurs primarily in the hepatocytes. The major metabolites are salicyluric acid (75%), the phenolic and acyl glucuronides of salicylate (15%), and gentisic and gentisuric acid (1%). 

Caffeine:  Hepatic biotransformation prior to excretion results in about equal amounts of 1-methylxanthine and 1-methyluric acid.

 

Drug Elimination:

Aspirin: The clearance of total salicylates is subject to saturable kinetics; however, first-order elimination kinetics are still a good approximation for doses up to 650 mg. The plasma half-life for aspirin is about 12 minutes and for salicylic acid and/or total salicylates is about 3 hours. The elimination of therapeutic doses is through the kidneys either as salicylic acid or other biotransformation products. The renal clearance is greatly augmented by an alkaline urine as is produced by concurrent administration of sodium bicarbonate or potassium citrate.

Butalbital: Elimination of butalbital is primarily via the kidney (59% to 88% of the dose) as unchanged drug or metabolites. The plasma half-life is about 35 hours. 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-methyl1-propyl) barbituric acid (about 4.8% of the dose), products with the barbituric acid ring hydrolyzed with excretion of urea (about 14% of the dose), as well as unidentified materials. Of the material excreted in the urine, 32% was conjugated. 

Caffeine: Caffeine is cleared rapidly through metabolism and excretion in the urine. The plasma half-life is about 3 hours. Of the 70% of the dose that has been recovered in the urine, only 3% was unchanged drug.

How Supplied:

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