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Fioricet® (Butalbital, Acetaminophen, and Caffeine Tablets USP) is indicated for the relief of the symptom complex of tension (or muscle contraction) headache. Each Fioricet (butalbital, acetaminophen, and caffeine) Tablet contains following active ingredients:
butalbital USP . . . . . . . . . . . . 50 mg
acetaminophen USP . . . . . . 325 mg
caffeine USP . . . . . . . . . . . . . 40 mg
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 this combination product in the treatment of multiple recurrent headaches is unavailable. Caution in this regard is required because butalbital is habit-forming and potentially abusable.
Fioricet and Esgic is made from a combination of butalbital (a barbiturate, 50 mg), acetaminophen (325 mg), and caffeine (40 mg). They are indicated for the treatment of tension headaches and muscle contraction headaches. Although not indicated, they are commonly used to treat migraines and other pain related ailments. Note that Fioricet (and some other pain medications) are implicated as causing repeat headaches with over-use
What is Fioricet and How ca we use it
Fioricet is a barbiturate sedative mixed with a non-aspirin pain medication and caffeine. This non-narcotic pain medication and relaxant is often prescribed for tension headaches caused by contractions of the muscles in the neck and shoulder area, and migraine.
How to Take Fioricet
Fioricet comes as a capsule and tablet to take by mouth. One or 2 tablets every 4 hours as needed. Total daily dosage should not exceed 6 tablets.
Extended and repeated use of this product is not recommended because of the potential for physical dependence.
Fioricet taking Warnings/Precautions
Fioricet may cause you to become drowsy or less alert; therefore, driving or operating dangerous machinery or participating in any hazardous activity that requires full mental alertness is not recommended until you know your response to this drug.
If you are being treated for severe depression or have a history of severe depression or drug abuse, consult with your doctor before taking Fioricet.
Use this drug with caution if you are elderly or in a weakened condition, if you have liver or kidney problems, or if you have severe abdominal trouble.
If you are pregnant or plan to become pregnant, inform your doctor immediately. Fioricet can affect a developing baby. It also appears in breast milk. If this medication is essential to your health, your doctor may advise you to discontinue breastfeeding your baby until your treatment is finished.
Overdose
An overdose of Fioricet, or combining this medication with alcohol or other central nervous system depressant, may lead to unconsciousness or perhaps death. Fioricet overdose is indicated by severe drowsiness, confusion, extreme weakness, hallucination, shortness of breath, too slow or troubled breathing, slurred speech, lack of coordination, vomiting with blood, unusually slow heartbeat.
Do not take more Fioricet than is recommended. An overdose of acetaminophen can cause damage to your liver. Do not use any other cold, allergy, pain, or sleep medication without first asking your doctor or pharmacist. Acetaminophen (sometimes abbreviated as “APAP”) is contained in many combination medicines. If you use certain products together with Fioricet you may accidentally use too much acetaminophen. Read the label of any other medicine you are using to see if it contains acetaminophen or APAP. Avoid drinking alcohol. It can increase the risk of liver damage while you are taking acetaminophen. If you drink more than three alcoholic beverages per day, do not take acetaminophen without your doctor’s advice, and never take more than 2 grams (2000 mg) per day.
Mechanism of action
Butalbital has generalized depressant effect on central nervous system and, in very high doses, has peripheral effects. Acetaminophen has analgesic and antipyretic effects; its analgesic effects may be mediated through inhibition of prostaglandin synthetase enzyme complex. Caffeine is thought to produce constriction of cerebral blood vessels.
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 3 hours.
Fioricet Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using Fioricet and call your doctor at once if you have any of these serious side effects:
- fast, pounding, or uneven heartbeat;
- feeling light-headed or short of breath;
- nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
- easy bruising or bleeding, unusual weakness, fever, chills, body aches, flu symptoms.
Less serious Fioricet side effects may include:
- drowsiness;
- dizziness, confusion or lightheadedness;
- dry mouth;
- nausea, vomiting, stomach pain, loss of appetite;
- feeling anxious or jittery;
- drunk feeling; or
- headache.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
All adverse events tabulated below are classified as infrequent.
Frequently Observed
The most frequently reported adverse reactions are drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, abdominal pain, & intoxicated feeling.
Central Nervous Method: 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, in elderly or debilitated patients, or due to overdosage of butalbital.
Autonomic Nervous Method: dry mouth, hyperhidrosis.
Gastrointestinal: difficulty swallowing, heartburn, flatulence, constipation.
Cardiovascular: tachycardia.
Genitourinary: diuresis.
Musculoskeletal: leg pain, muscle fatigue.
Miscellaneous: pruritus, fever, earache, nasal congestion, tinnitus, euphoria, allergic reactions.
Several cases of dermatological reactions, including toxic epidermal necrolysis & 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.
Butalbital may be habit-forming and should be used only by the person it was prescribed for. Fioricet should never be shared with another person, especially someone who has a history of drug abuse or addiction. Keep the medication in a secure place where others cannot get to it.
Do not take Fioricet without first talking to your doctor if you drink more than three alcoholic beverages per day or if you have had alcoholic liver disease (cirrhosis). You may not be able to take medication that contains acetaminophen.
You should not take Fioricet if you are allergic to acetaminophen, butalbital, or caffeine, or if you have porphyria.
Before using Fioricet, tell your doctor if you are allergic to any drugs, or if you have:
- kidney disease,
- liver disease; or
- a history of mental illness or suicidal thoughts.
If you have any of these conditions, you may need a dose adjustment or special tests to safely take Fioricet.
Side Effects by Body System
Nervous system
Nervous system side effects including drowsiness, lightheadedness, dizziness, sedation, and an intoxicated feeling have been reported frequently from the use of butalbital. Headache and seizures have been reported infrequently. Mental confusion, excitement, or depression have also been reported due to either intolerance (primarily in elderly or debilitated patients) or due to an overdose of butalbital.
General
General side effects including caffeinism have been reported. Consumption of higher doses of caffeine (>600 mg/day) has been reported to have lead to caffeinism. Caffeinism is a syndrome characterized by anxiety, restlessness, and sleep disorders (similar to anxiety states). It has also been reported that chronic, heavy caffeine ingestion may be associated with depression. Caffeine may cause anxiety and panic in panic disorder patients and may aggravate PMS.
Hepatic
Hepatic side effects including severe and sometimes fatal dose dependent hepatitis has been reported with the use of acetaminophen in alcoholic patients. Hepatotoxicity has been increased during fasting.
Alcoholic patients may develop hepatotoxicity after even modest doses of acetaminophen. In healthy patients, approximately 15 grams of acetaminophen is necessary to deplete liver glutathione stores by 70% in a 70 kg person. However, hepatotoxicity has been reported following smaller doses. Glutathione concentrations may be repleted by the antidote N-acetylcysteine. One case report has suggested that hypothermia may also be beneficial in decreasing liver damage during overdose.
In a recent retrospective study of 306 patients admitted for acetaminophen overdose, 6.9% had severe liver injury but all recovered. None of the 306 patients died.
One study has suggested that acetaminophen may precipitate acute biliary pain and cholestasis. The mechanism of this effect may be related to inhibition of prostaglandin and alterations in the regulation of the sphincter of Oddi.
Cases of acute pancreatitis have been reported rarely with the use of acetaminophen.
A 19-year-old female developed hepatotoxicity, reactive plasmacytosis and agranulocytosis followed by a leukemoid reaction after acute acetaminophen toxicity.
Gastrointestinal
Gastrointestinal side effects are rare with acetaminophen use, except in alcoholics and after overdose. Nausea, vomiting, and abdominal pain have been reported frequently with the use of butalbital. In clinical trials of caffeine citrate, five cases of necrotizing enterocolitis were reported among the 46 infants exposed to the caffeine citrate injection.
Renal
Acute tubular necrosis usually occurs in conjunction with liver failure, but has been observed as an isolated finding in rare cases. A possible increase in the risk of renal cell carcinoma has been associated with chronic acetaminophen use as well.
A recent case-control study of patients with end-stage renal disease suggested that long term consumption of acetaminophen may significantly increase the risk of end-stage renal disease particularly in patients taking more than two pills per day.
Renal side effects are rare with acetaminophen and include acute tubular necrosis and interstitial nephritis. Adverse renal effects are most often observed after overdose, after chronic abuse (often with multiple analgesics), or in association with acetaminophen-related hepatotoxicity.
Hypersensitivity
Hypersensitivity side effects including anaphylaxis and fixed drug eruptions have been reported rarely in association with acetaminophen use.
Hematologic
Hematologic side effects including rare cases of thrombocytopenia associated with acetaminophen have been reported. Methemoglobinemia with resulting cyanosis has also been observed in the setting of acute overdose.
Dermatologic
Dermatologic side effects including acetaminophen associated bullous erythema and purpura fulminans have been reported. Erythematous skin rashes associated with acetaminophen have been reported rarely.
Respiratory
Respiratory side effects including dyspnea have been reported frequently with the use of butalbital. A case of acetaminophen-induced eosinophilic pneumonia has also been reported.
Cardiovascular
Two cases hypotension have been reported following the administration of acetaminophen. Both patients experienced significant decreases in blood pressure. One of the two patients required pressor agents to maintain adequate mean arterial pressures. Neither episode was associated with symptoms of anaphylaxis. Neither patient was rechallenged after resolution of the initial episode.
Cardiovascular side effects including several cases of hypotension have been reported following the administration of acetaminophen.
DRUG ABUSE AND DEPENDENCE
Abuse & Dependence
Butalbital
Barbiturates may be habit-forming: Tolerance, psychological dependence, & physical dependence may occur following prolonged use of high doses of barbiturates. The average daily dose for the barbiturate addict is usually about 1500 mg. As tolerance to barbiturates develops, the amount needed to maintain the same level of intoxication increases; tolerance to a fatal dosage, however, does not increase more than two-fold. As this occurs, the margin between an intoxication dosage & fatal dosage becomes smaller. The lethal dose of a barbiturate is far less if alcohol is also ingested. Major withdrawal symptoms (convulsions & delirium) may occur within 16 hours & last up to 5 days after abrupt cessation of these drugs. Intensity of withdrawal symptoms gradually declines over a period of approximately 15 days. Treatment of barbiturate dependence consists of cautious & gradual withdrawal of the drug. Barbiturate-dependent patients can be withdrawn by using a quantity of different withdrawal regimens. One scheme involves initiating treatment at the patient’s regular dosage level & gradually decreasing the daily dosage as tolerated by the patient.
PRECAUTIONS
General
Butalbital, acetaminophen, and caffeine tablets should be prescribed with caution in certain special-risk patients, such as the elderly or debilitated, and those with severe impairment of renal or hepatic function, or acute abdominal conditions.
Laboratory Tests
In patients with severe hepatic or renal disease, effects of therapy should be monitored with serial liver and/or renal function tests.
Carcinogenesis, Mutagenesis, Impairment of Fertility
No adequate studies have been conducted in animals to determine whether acetaminophen or butalbital have a potential for carcinogenesis, mutagenesis or impairment of fertility.
Pregnancy
Teratogenic Effects
Pregnancy Category C: Animal reproduction studies have not been conducted with this combination product. It is also not known whether butalbital, acetaminophen, and caffeine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. This product should be given to a pregnant woman only when clearly needed.
Nonteratogenic Effects
Withdrawal seizures were reported in a two-day-old male infant whose mother had taken a butalbital-containing drug during the last two months of pregnancy. Butalbital was found in the infant’s serum. The infant was given phenobarbital 5 mg/kg, which was tapered without further seizure or other withdrawal symptoms.
Nursing Mothers
Caffeine, barbiturates, and acetaminophen are excreted in breast milk in small amounts, but the significance of their effects on nursing infants is not known. Because of potential for serious adverse reactions in nursing infants from butalbital, acetaminophen, and caffeine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
Safety and effectiveness in pediatric patients below the age of 12 have not been established.
Geriatric Use
Clinical studies of Fioricet® (Butalbital, Acetaminophen, and Caffeine Tablets USP) did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Butalbital is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.
Always discuss with your doctor your medical history, allergies and health problems. Fioricet can be habit-forming, and can be physically and psychologically addictive.
Close supervision by your doctor is needed. Caution is advised if you have diabetes, heart, kidney and/or liver problems. Avoid mixing Fioricet with alcohol. It may increase intoxication. Alcohol taken during therapy with Fioricet can be very damaging to your liver. It is advised to take extra care when driving or using machinery due to possible effects such as drowsiness and dizziness. Avoid sleeping pills, antihistamines, sedatives, and tranquilizers to keep you from getting drowsy unless otherwise prescribed by your doctor.
Symptoms of Fioricet overdose include nausea, vomiting, diarrhea, abdominal pain, sweating, seizures, drowsiness, decreased breathing,dizziness or fainting, confusion, an irregular heartbeat, and coma.
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