Fioricet is a brand name consisting of a combination of butalbital (a barbiturate), acetaminophen and caffeine which is indicated for the treatment of tension headaches, muscle contraction headaches and post-dural puncture headaches. Although not indicated, they are commonly used to treat migraines and other pain related ailments. Butalbital is a barbiturate class drug that acts as a muscle relaxant and is often prescribed for the treatment of headaches and other moderate level pain that may not respond to over-the-counter preparations.
Fioricet (Butalbital, Acetaminophen, and Caffeine Tablets, USP) is supplied in tablet form for oral administration.
Each tablet contains the following active ingredients:
butalbital USP . . . . . . . . . .50 mg
acetaminophen USP . . . . 325 mg
caffeine USP . . . . . . . . . . .40 mg
Butalbital (5-allyl-5-isobutylbarbituric acid), is a short to intermediate-acting barbiturate. It has the following structural formula:
Acetaminophen (4´-hydroxyacetanilide), is a non-opiate, non-salicylate analgesic and antipyretic. It has the following structural formula:
Caffeine (1,3,7-trimethylxanthine), is a central nervous system stimulant. It has the following structural formula:
Inactive Ingredients: crospovidone, FD&C Blue #1 (aluminum lake), magnesium stearate, microcrystalline cellulose, povidone, pregelatinized starch, and stearic acid.
Fioricet (butalbital/acetaminophen/caffeine) has been around forever and is used by many for the treatment of chronic migraine or tension headaches. It is a mixture of a barbiturate, Tylenol (acetaminophen) and caffeine.
Fioricet® (Watson Laboratories, Inc) is a combination tablet consisting of 40 mg of caffeine (1,3,7–trimethylxanthine), 325 mg of acetaminophen, and 50 mg of butalbital (5-allyl-5-isopropylbarbituric acid). Fioricet® is primarily intended as treatment for tension headaches
Caffeine is a methylxanthine similar to theophylline and theobromine. While caffeine is used for stimulant and mood-elevating effects in drinks such as coffee, it also has been used to treat neonatal apnea and headaches in combination with other analgesics. Theophylline has classically been used to treat bronchospastic airway diseases such as asthma and COPD, although it has generally fallen out of favor to pure ?-adrenergic agonists due to their better safety profiles. As a group, methylxanthines cause the release of catecholamines, which subsequently stimulate ?1 and ?2 receptors, accounting for their stimulant effects. Methylxanthines’ role in treating bronchospastic disease is due to both bronchodilatory and anti-inflammatory mechanisms. Toxic concentrations of caffeine (such as those achieved with oral doses >1 g) inhibit phosphodiesterase and thus increase levels of cAMP, promoting central nervous system (CNS) excitation, peripheral vasodilation, myocardial stimulation, and smooth muscle relaxation. In addition, methylxanthines antagonize the benzodiazepine receptor, which likely contributes to the refractoriness of seizures from toxicity from these agents.
Acetaminophen, the second ingredient in Fioricet®, inhibits the synthesis of prostaglandins and hypothalamic heat regulation in the CNS and blocks peripheral pain impulses. Finally, butalbital is a short-to-intermediate acting barbiturate. The effects of butalbital in isolation are not well understood, as it is only available in combination products. Barbiturates have muscle-relaxing and anti-anxiety properties. A reason for butalbital’s use in conjunction with caffeine may be to antagonize the unwanted central stimulating effect of caffeine.
Fiorinal is a Schedule III controlled drug but Fioricet is not! Fioricet contains: 325 mg of acetaminophen (APAP), 50 mg of butalbital, and 40 mg of caffeine. … The potential for abuse is decreased if a sufficient amount of a non-controlled substance(e.g., aspirin or acetaminophen) is added.
Fioricet is a prescription medication used to relieve tension headaches. It works by relaxing muscle contractions that can result in mild to moderate head pain. Fioricetis a combination of three ingredients: the pain reliever acetaminophen; butalbital, a barbiturate; and caffeine, a stimulant.
Codeine is an opioid pain medication. An opioid is sometimes called a narcotic. Acetaminophen is a less potent pain reliever that increases the effects of codeine. Butalbital is in a group of drugs called barbiturates.
Fioricet contains a combination of acetaminophen, butalbital, and caffeine Acetaminophen is a pain reliever and fever reducer. Butalbital is in a group of drugs called barbiturates. It relaxes muscle contractions involved in a tension headache. Caffeine is a central nervous system stimulant.
Fioricet is indicated for the treatment of muscle tension or muscle contraction headaches. It is also commonly prescribed for migraines although it is not FDA indicated for this use in the United States. The usual adult dose is 1-2 tablets every four hours as needed, not exceeding six tablets in a 24-hour period.
Fioricet (Butalbital, Acetaminophen, and Caffeine Tablets, USP) is indicated for the relief of the symptom complex of tension (or muscle contraction) headache.
Evidence supporting the efficacy and safety of Fioricet in the treatment of multiple recurrent headaches is unavailable. Caution in this regard is required because butalbital is habit-forming and potentially abusable.
Now, many formularies are no longer covering Fioricet capsules. For those of you who have relied on it for years, this (understandably) may make you nervous.
Well, it turns out it doesn’t really work that well—and there are much better options out there.
- Fioricet and Fioricet with Codeine are not as effective for acute migraine as newer medications. There isn’t any evidence that shows that barbiturate-containing meds (the butalbital in Fioricet) help for migraine treatment. In fact, the use of Fioricet with Codeine often results in chronic migraine and a “medication overuse headache.”
- NSAIDS. Start with these instead. There is good evidence that nonsteroidal anti-inflammatory drugs—ibuprofen, naproxen, and others—work well for the treatment of acute migraine.
- Triptans. Imitrex (sumatriptan), Maxalt (rizatriptan), Relpax(eletriptan), and Frova (frovatriptan) are examples. Used alone or in combination with an NSAID, triptans work well for moderate to severe headaches that aren’t relieved by NSAIDs alone. Wondering which to choose? They generally work the same but you may notice fewer side effects with one over the other. Cost can also be an issue so you’ll want to pick a triptan that is covered by your insurance plan. It’s also a good idea to check GoodRx to see if the cash or discount price beats your co-pay.
- Adding a nausea medication. For folks with moderate to severe migraine accompanied by nausea or vomiting, adding Reglan(metoclopramide) , Zofran (ondansetron) or Compazine(prochlorperazine) also helps.
Fioricet Side Effects
Frequently Observed Fioricet Side Effects
The most frequently reported adverse reactions are drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, abdominal pain, and intoxicated feeling.
Commonly reported side effects for Fioricet include:
- Intoxicated feeling
- Substance dependence
- Shortness of breath
- Abdominal pain
Infrequently Observed Fioricet Side Effects
All adverse events tabulated below are classified as infrequent.
Central Nervous System: headache, shaky feeling, tingling, agitation, fainting, fatigue, heavy eyelids, high energy, hot spells, numbness, sluggishness, seizure. Mental confusion, excitement, or depression can also occur due to intolerance, particularly in elderly or debilitated patients, or due to overdosage of butalbital.
Autonomic Nervous System: dry mouth, hyperhidrosis.
Gastrointestinal: difficulty swallowing, heartburn, flatulence, constipation.
Musculoskeletal: leg pain, muscle fatigue.
Miscellaneous: pruritus, fever, earache, nasal congestion, tinnitus, euphoria, allergic reactions.
Several cases of dermatological reactions, including toxic epidermal necrolysis and erythema multiforme, have been reported.
The following adverse drug events may be borne in mind as potential effects of the components of this product. Potential effects of high dosage are listed in the OVERDOSAGE section.
Acetaminophen: allergic reactions, rash, thrombocytopenia, agranulocytosis.
Caffeine: cardiac stimulation, irritability, tremor, dependence, nephrotoxicity, hyperglycemia.
How to take Fioricet ?
One or 2 tablets every 4 hours as needed. Total daily dosage should not exceed 6 tablets.
Extended and repeated use of Fioricet is not recommended because of the potential for physical dependence.
How does Fioricet work?
The acetaminophen in Fioricet is a pain reliever, the caffeine works as a stimulant to increase the acetaminophen’s effectiveness, and the butalbital is a sedative that decreases anxiety while causing relaxation and sleepiness. These actions are believed to ease migraine symptoms, but there is limited evidence that barbituates ease migraine symptoms.
Butalbital has generalized depressant effect on central nervous system and, in very high doses, has peripheral effects.
Acetaminophen has analgesic and antipyreticeffects mediated by a metabolite which acts at cannabinoid receptors, contrary to popular belief it is not an antiinflammatory at safe levels (it becomes toxic at doses above 1,000mg per dose and/or 3,000mg per day).
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.