butalbital, aspirin, and caffeine

Contraindicated in:

Hypersensitivity to individual components (cross-sensitivity may occur with NSAIDs);
Bleeding disorders, thrombocytopenia, or vitamin K deficiency;
Severe hepatic impairment;
Peptic ulcer disease;
Porphyria;
OB: Avoid use of NSAIDs after 30 wk gestation;
Lactation: Lactation.

Use Cautiously in:

History of suicide attempt or drug addiction;
Chronic alcohol use;
Severe renal impairment;
Severe cardiovascular disease;
Concurrent use of other CNS depressants;
Concurrent use of warfarin;
Head injury;
Elevated intracranial pressure;
Hypothyroidism;
Addison's disease;
Benign prostatic hyperplasia;
Asthma;
OB: Use of NSAIDs at or after 20 wk gestation may cause fetal or neonatal renal impairment; if NSAID treatment is necessary between 20 wk and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible;
Pedi: Safety and effectiveness not established in children.
Geri: Butalbital and aspirin appear on Beers list. Older adults may have ↑ risk of physical dependence, tolerance to sleep benefits, and overdose with butalbital and ↑ risk of bleeding with aspirin. Avoid use in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, tachycardia

Derm: dermatitis, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), pruritus, rash, sweating

EENT: ear ache, nasal congestion, tinnitus

GI: bleeding, constipation, dry mouth, dysphagia, epigastric distress, 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 ↑ the 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.
May ↑ the effect of warfarin, oral antidiabetic agents, insulin, 6–mercaptopurine, methotrexate, and NSAIDs.
May ↓ the effect of probenecid.

Drug-Natural Products:

St. John’s wort may ↓ the effectiveness of butalbital.
Concurrent use of kava kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Availability ⬆ ⬇

(Generic available)

Capsules: butalbital 50 mg/aspirin 325 mg/caffeine 40 mg
Tablets: butalbital 50 mg/aspirin 325 mg/caffeine 40 mg
In combination with: codeine. 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).

Action ⬆ ⬇

Contains an analgesic (aspirin) 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; crosses the placenta and enters breast milk.

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

Half-Life: Butalbital = 35 hr; aspirin = 3 hr; caffeine = 3 hr.

Contr. Subst. Schedule ⬆ ⬇

Schedule III (C-III)

Canadian Brand Names ⬆ ⬇

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 weeks, consult health care professional. The dose of aspirin should not exceed the 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, especially St. John's Wort (added).
Caution patient to avoid concurrent use of alcohol or other CNS depressants, including opioids and cannabinoids, may cause overdose.
Advise patient to report any signs of bleeding, bruising, or ringing in ears to a health care professional.
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise women to avoid aspirin in the 3rd trimester of pregnancy (after 29 wk), may cause premature closure of the fetal ductus arteriosus. Use of aspirin after 20 wk may cause fetal renal dysfunction leading to oligohydramnios. May cause reversible infertility in women attempting to conceive; may consider discontinuing aspirin.

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Indications ⬇

Contraind./Precautions ⬆ ⬇