General

**BEERS Drug**

Pronunciation:
byoo-tal-bi-tal a-seet-a-min-oh-fen kaf-een

Trade Name(s)

• Esgic
• Fioricet

Ther. Class.

nonopioid analgesics

(combination with barbiturate)

Pharm. Class.

barbiturates

† For information on acetaminophen component in formulation, see acetaminophen monograph.

Indications

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).

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 Effect(s):

Decreased severity of headache pain with some sedation.

Pharmacokinetics

Absorption: Well absorbed.

Distribution: Widely distributed to tissues.

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.

TIME/ACTION PROFILE

Contraindication/Precautions

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.

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, hepatotoxicity (with higher doses of acetaminophen)

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.

Interactions

Drug-Drug

• Additive CNS depression with other  CNS depressants, including  alcohol,  antihistamines,  antidepressants,  opioid analgesics, and  sedative/hypnotics.
• May ↓ levels and effectiveness of  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 ↑ levels and risk of toxicity of butalbital.

Drug-Natural Products:

•  St. John's wort  may ↓ levels and effectiveness of butalbital.
•  Kava-kava,  valerian,  skullcap,  chamomile, or  hops  can ↑ risk of CNS depression.

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).

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.

Assessment

• 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.
• Assess amount, frequency, and type of drugs taken in patients self-medicating, especially with OTC drugs. Prolonged use of acetaminophen ↑ risk of adverse hepatic and renal effects. Do not exceed maximum daily dose of acetaminophen when considering all routes of administration and all combination products containing acetaminophen.

Implementation

• 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 as needed administration. Analgesic is more effective if given before pain becomes severe.
• Medication should be discontinued gradually after long-term use to prevent withdrawal symptoms.

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 provider. 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 or 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 provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants; may cause overdose.
• Rep:  Advise women of reproductive potential to notify health care provider 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.

Evaluation/Desired Outcomes

Decrease in severity of headache without a significant alteration in level of consciousness.