Acetaminophen/butalbital

Acetaminophen/butalbital, sold under the brand name Fioricet among others, is a combination medication used to treat tension headaches and migraine headaches.[1][2] It contains butalbital, a barbiturate and paracetamol (acetaminophen), an analgesic.[1] Some versions also contain caffeine.[3] It is taken by mouth.[1]

Acetaminophen/butalbital
A bottle of acetaminophen/butalbital
Combination of
ButalbitalBarbiturate
AcetaminophenMiscellaneous analgesic
CaffeineXanthine
Clinical data
Trade namesFioricet, others
AHFS/Drugs.comFDA Professional Drug Information
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		By mouth
    Legal status
    Legal status
    • In general: ℞ (Prescription only)
    Identifiers
    ChemSpider
    • none
    KEGG

    The most common side effects include sleepiness, dizziness, trouble breathing, and abdominal pain.[1] Other severe side effects may include liver problems, confusion, addiction, and allergic reactions.[1] Frequent use may result in medication overuse headache.[4] Barbiturate withdrawal may occur if rapidly stopped following long term use.[5] Use is not generally recommended during pregnancy or breastfeeding.[6]

    The combination was approved for medical use in the United States in 1984.[1] It is available as a generic medication.[3] In the United States the wholesale cost is about 1.20 USD per dose as of 2019.[7] In 2016 it was the 202nd most prescribed medication in the United States with more than 2 million prescriptions.[8][9] In the United States it is a schedule III controlled substance in some states but not federally.[2][10] It is banned in a number of European countries.[5]

    Medical uses

    Acetaminophen/butalbital is indicated for the treatment of tension headaches. It is also commonly prescribed for migraines, although it is not approved by the FDA for this. The usual adult dose is one to two tablets every four hours as needed, not to exceed six tablets in a twenty-four-hour period.[11][12]

    Side effects

    Commonly reported side effects include euphoria, dizziness or lightheadedness, drowsiness or sedation, intoxication, nausea, vomiting, dependence, shortness of breath, and abdominal pain.

    Prolonged use can cause rebound headaches.[13]

    Rarely, use of barbiturates can lead to Stevens–Johnson syndrome.

    Overdose

    Butalbital exerts its toxicity through excessive sedation, resulting in respiratory depression and ultimately death via hypoxia. Nonlethal overdoses may also result in coma and death. There is no specific antidote to barbiturate overdose; treatment is supportive, generally including the administration of intravenous saline, naloxone, thiamine, glucose, sodium bicarbonate to alkalize the urine and increase rate of excretion, and activated charcoal via nasogastric tube.

    Acetaminophen exerts its toxicity through the production of a toxic metabolite that can cause liver damage at doses as low as four grams. Larger doses can precipitate acute liver failure, acute kidney injury, or gastrointestinal bleeding; death has been known to occur with ingestion of ten to fifteen grams. The specific antidote to acetaminophen overdose is N-acetylcysteine.

    Mechanism of action

    Butalbital exerts a generalized depressant effect on the central nervous system and, in very high doses, has peripheral effects. Acetaminophen has analgesic and antipyretic effects mediated by a metabolite that acts at cannabinoid receptors. Caffeine is thought to produce constriction of cerebral blood vessels and serves to counteract the sedative effect of butalbital.

    Butalbital has a half-life of about 35 hours. Acetaminophen has a half-life of about 1.25 to 3 hours, but may be increased by liver damage and after an overdose. Caffeine has a half-life of about 2.5 to 4.5 hours.[14]

    Formulation

    Fiorcet historically contained 50 mg of butalbital, 40 mg of caffeine, and 325 mg of acetaminophen per dose. However, in accordance with FDA guidelines advising manufacturers to limit doses of acetaminophen in prescription drugs,[15] the acetaminophen content was lowered to 300 mg as of 2014.[16][17]

    Fioricet is also available in a formulation containing 30 mg of codeine per dose.[18]

    References
    1. "Butalbital and Acetaminophen - FDA prescribing information, side effects and uses". Drugs.com. Retrieved 19 April 2019.
    2. "Fioricet Capsules (acetaminophen/butalbital/caffeine)". Prescribers' Digital Reference. Retrieved 19 April 2019.
    3. PUBLISHING, TARASCON (2009). Pharmacopoeia. Jones & Bartlett Learning. p. 3. ISBN 9780763774196.
    4. Woo, Teri Moser; Robinson, Marylou V. (2015). Pharmacotherapeutics For Advanced Practice Nurse Prescribers. F.A. Davis. p. 1057. ISBN 9780803645813.
    5. Young, WB; Siow, HC (April 2002). "Should butalbital-containing analgesics be banned? Yes". Current Pain and Headache Reports. 6 (2): 151–5. doi:10.1007/s11916-002-0012-y. PMID 11872187.
    6. "Acetaminophen / butalbital Use During Pregnancy". Drugs.com. Retrieved 19 April 2019.
    7. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
    8. "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
    9. "Fioricet- butalbital, acetaminophen, and caffeine capsule". dailymed.nlm.nih.gov. Retrieved 8 June 2019.
    10. "West Virginia Board of Pharmacy" (PDF). Retrieved 8 June 2019.
    11. Fioricet at RxList
    12. http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=4417
    13. A Hidden Cause of Headache Pain - New York Times
    14. https://examine.com/supplements/caffeine/#summary2-7
    15. Food and Drug Administration. FDA drug safety communication: prescription acetaminophen products to be limited to 325 mg per dosage unit; boxed warning will highlight potential for severe liver failure.
    16. (Old formulation) Fioricet package insert, Cardinal Health, Inc.
    17. (New formulation) Fioricet package insert, Watson Pharma, Inc.
    18. Fioricet with codeine capsule package insert, Watson Pharma, Inc
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