butalbital, acetaminophen, caffeine

Contraindicated in:

Hypersensitivity to individual components;
Porphyria;
Lactation: Lactation.

Use Cautiously in:

History of suicide attempt or drug addiction;
Chronic alcohol use;
Severe renal impairment;
Severe hepatic impairment;
Severe cardiovascular disease;
Concurrent use of other CNS depressants;
OB: Safety not established in pregnancy;
Pedi: Children <12 yr (safety and effectiveness not established);
Geri: Butalbital appears on Beers list. Older adults may have ↑ risk of physical dependence, tolerance to sleep benefits, and overdose. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, tachycardia

Derm: dermatitis, pruritus, rash, sweating

EENT: ear ache, nasal congestion, tinnitus

GI: constipation, dry mouth, dysphagia, flatulence, heartburn

MS: leg pain, muscle weakness

Neuro: drowsiness, confusion, delirium, depression, dizziness, excitation, headache (with chronic use), insomnia, irritability, lethargy, nervousness, numbness, tingling

Resp: respiratory depression

Misc: fever, physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Additive CNS depression with other CNS depressants, including alcohol, antihistamines, antidepressants, opioid analgesics, and sedative/hypnotics.
May increase the liver metabolism and ↓ the effectiveness of other drugs including amiodarone, benzodiazepines, bupropion, calcium channel blockers, carbamazepine, citalopram, clarithromycin, cyclosporine, erythromycin, fluoxetine, fluvoxamine, glipizide, hormonal contraceptives, losartan, methadone, mirtazapine, nateglinide, nefazodone, nevirapine, phenytoin, pioglitazone, promethazine, propranolol, protease inhibitors, proton pump inhibitors, rifampin, ropinirole, selegiline, sertraline, tacrolimus, theophylline, venlafaxine, voriconazole, warfarin, and zafirlukast.
MAO inhibitors, felbamate, primidone, and valproic acid may prevent metabolism and ↑ the effectiveness of butalbital.

Drug-Natural Products:

St. John’s wort may ↓ barbiturate effect.
Concurrent use of kava kava, valerian, skullcap, chamomile, or hops can increase CNS depression.

Availability ⬆ ⬇

(Generic available)

Capsules: butalbital 50 mg/acetaminophen 300 mg/caffeine 40 mg; butalbital 50 mg/acetaminophen 325 mg/caffeine 40 mg
Tablets: butalbital 50 mg/acetaminophen 325 mg/caffeine 40 mg
In combination with: codeine Rx. See Appendix [not included in this PDA edition].

Route/Dosage ⬆ ⬇

PO (Adults ): 1–2 capsules or tablets (50–100 mg butalbital) every 4 hr as needed for pain (should not exceed 6 tablets or capsules/24 hr).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Contains an analgesic (acetaminophen) for relief of pain, a barbiturate (butalbital) for its sedative effect, and caffeine, which may be of benefit in tension headaches.

Therapeutic effects:

Decreased severity of headache pain with some sedation.

Classifications ⬆ ⬇

Therapeutic Classification: nonopioid analgesics (combination with barbiturate)

Pharmacologic Classification: barbiturates

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Butalbital primarily eliminated by kidneys as unchanged drug or metabolites (59–88% of dose); acetaminophen and caffeine primarily metabolized by liver.

Half-Life: Butalbital: 35 hr; acetaminophen: 1–3 hr; caffeine: 3 hr.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	15–30 min	1–2 hr	30 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication exactly as directed. Do not increase dose because of the habit-forming potential of butalbital. If medication appears less effective after a few wk, consult health care professional. Dose of acetaminophen should not exceed maximum recommended daily dose of 4 g/day. Chronic excessive use of >4 g/day (2 g in chronic alcoholism) may lead to hepatotoxicity, renal or cardiac damage. Discontinue gradually to prevent withdrawal symptoms (anxiety, diaphoresis, disturbed sleep, nausea/vomiting, restlessness, seizures, worsened headache).
Advise patients with tension headaches to take medication at first sign of headache. Lying down in a quiet, dark room may also be helpful. Medications taken for prophylaxis should be continued.
May cause drowsiness or dizziness. Advise patient to avoid driving and other activities requiring alertness until response to medication is known.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Caution patient to avoid concurrent use of alcohol or other CNS depressants, may cause overdose.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Advise patient to use an additional nonhormonal method of contraception while taking butalbital compound.

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Indications ⬇

Contraind./Precautions ⬆ ⬇