butalbital, acetaminophen, caffeine†
byoo-tal-bi-tal, a-seet-a-min-oh-fen, kaf-een
(combination with barbiturate)
† For information on acetaminophen component in formulation, see acetaminophen monograph
Relief of the symptom complex of tension (or muscle contraction) headaches (use should be short-term only as the butalbital component may be habit-forming).
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.
Decreased severity of headache pain with some sedation.
Absorption: Well absorbed.
Distribution: Widely distributed; crosses the placenta and enters breast milk.
Metabolism and 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.
|PO||15–30 min||1–2 hr||30 hr|
- Hypersensitivity to individual components
- 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.
Adverse 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
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- 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.
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).
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 combination drugs.
- Assess type, location, and intensity of pain before and 60 min following administration.
- Prolonged use may lead to physical and psychological dependence and tolerance. This should not prevent patient from receiving adequate analgesia. Most patients who receive butalbital compound for pain do not develop psychological dependence.
- Assess frequency of use. Frequent, chronic use may lead to daily headaches in headache-prone individuals because of physical dependence on caffeine and other components. Chronic headaches from overmedication are difficult to treat and may require hospitalization for treatment and prophylaxis.
Do not confuse Fioricet (butalbital, acetaminophen, caffeine) with Fiorinal (butalbital, aspirin, caffeine).
- Explain therapeutic value of medication before administration to enhance the analgesic effect.
- Limit butalbital use to ≤5 days per month to avoid medication-overuse headache
- Regularly administered doses may be more effective than prn administration. Analgesic is more effective if given before pain becomes severe.
- Medication should be discontinued gradually after long-term use to prevent withdrawal symptoms.
- 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. 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 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.
Decrease in severity of headache without a significant alteration in level of consciousness.