Butalbital, Acetaminophen and Caffeine Capsule

Generic name:

Butalbital, Acetaminophen and Caffeine Capsule

Drug class:

Barbiturate combination analgesic

Dosage form:

Oral capsule

Root of administration:

Oral

Dose:

Typical adult dose: 1–2 capsules (butalbital 50 mg/acetaminophen 325 mg/caffeine 40 mg per capsule) every 4 hours as needed; maximum 6 capsules per 24 hours. Variations may exist; consult label.

Mechanism of action:

Butalbital: enhances GABAergic inhibition producing sedation; Acetaminophen: central COX inhibition reducing prostaglandin synthesis; Caffeine: adenosine receptor antagonism leading to vasoconstriction and CNS stimulation.

Drug usage cases:

• Tension-type headache
• Migraine headache (off-label)
• Musculoskeletal pain (off-label)

Drug contra indications:

• Hypersensitivity to butalbital, acetaminophen, caffeine or barbiturates
• Severe hepatic impairment or active liver disease
• History of porphyria
• Use of monoamine oxidase inhibitors within past 14 days
• Severe respiratory depression or sleep apnea
• Symptomatic cardiovascular disease including uncontrolled hypertension

Side effects:

• Drowsiness, sedation, dizziness
• Lightheadedness, hypotension
• Nausea, vomiting, abdominal pain
• Hepatotoxicity (from acetaminophen)
• Respiratory depression
• Dependence, withdrawal symptoms
• Rebound headache (medication overuse headache)
• Allergic reactions: rash, urticaria, anaphylaxis
• Stevens–Johnson syndrome, toxic epidermal necrolysis (rare)
• Tachycardia, arrhythmias

Warnings:

• Potential for physical and psychological dependence; use shortest duration necessary
• Risk of severe hepatotoxicity with overdose or concomitant acetaminophen-containing products
• Avoid alcohol or other CNS depressants
• Caution in patients with renal or pulmonary impairment
• Caution in elderly or debilitated patients
• Risk of medication overuse headache with frequent use
• Monitor for respiratory depression, especially in opioid-sensitized individuals
• Avoid abrupt discontinuation after prolonged use; taper gradually to prevent withdrawal

Use during pregnancy or breastfeeding:

Pregnancy: Animal studies show potential fetal harm with butalbital; classified as Pregnancy Category C. May cause neonatal respiratory depression or withdrawal if used near delivery. Acetaminophen is generally considered safe in recommended doses, caffeine should be limited. Use only if potential benefit justifies risk.

Breastfeeding: Butalbital is excreted in breast milk and may cause sedation or respiratory depression in nursing infants. Acetaminophen passes into milk in small amounts, caffeine may cause irritability or poor sleep in infants. Use with caution; monitor infant for adverse effects.