What Is Butalbital APAP Caffeine ?
Fioricet is a Combination Medication for chronic tension headaches. A tension headache causes moderate pain in the front, sides, or back of the head. Tension headaches are common, and most people experience them occasionally. However, when people suffer from more than ten or fifteen headaches every month, a health care provider may write a prescription for Fioricet. Doctors sometimes also prescribe Fioricet for migraines, which are headaches that cause severe pain in one side of the head along with hyper-sensitivity to light and sound.
What Are The Ingredients In Butalbital APAP Caffeine ?
A Combination Medication is a drug which includes two or more pharmaceutical ingredients in a fixed dose. There are three ingredients in standard Fioricet: Acetaminophen, Butalbital, and Caffeine. All three ingredients have different effects which combine to soothe headaches.
- Acetaminophen is a medication which alleviates pain and reduces fever. It’s more widely known by the brand name Tylenol. Acetaminophen works by impairing the production of the prostaglandin chemical in the brain. This chemical activates pain signals in the nervous system.
- Butalbital is a Sedative Barbiturate which stimulates the brain’s production of GABA. This neurotransmitter calms the nervous system by blocking signals among neurons. It also relaxes muscle tension in the head, thereby alleviating headaches. Butalbital is a Schedule III controlled substance in the United States.
- Caffeine is a Stimulant which raises a person’s blood pressure. While high blood pressure is not necessarily healthy, low blood pressure worsens headaches by causing blood vessels to expand and push against the brain. By raising blood pressure, Caffeine causes blood vessels to constrict and increases blood flow. This effect helps relieve headaches.
With these three ingredients at work, Fioricet can be an effective source of headache relief. However, the medication also poses risks for side effects, overdose, and addiction. For this reason, doctors usually refrain from prescribing Fioricet until safer over-the-counter medications fail to help their patients.
Is Butalbital APAP Caffeine Addictive?
Although it’s only a prescription headache medication, Fioricet has the potential to cause addiction. If a person follows their prescription guidelines and uses the medication correctly, the risks of addiction are low. However, if someone takes too much Fioricet, they may develop tolerance to its effects. A person with tolerance to a certain dose of Fioricet will require higher doses of the medication to alleviate their headaches.
When a person with tolerance starts to take more Fioricet, possibly by obtaining more prescriptions, they may eventually become dependent on it. In other words, they may feel unable to get through the day without taking Fioricet; if they stop, they will experience symptoms of withdrawal. These symptoms arise because their body has grown accustomed to Fioricet in high doses.
If a Fioricet-dependent person attempts to weather withdrawal alone, it’s likely they will take Fioricet again just to relieve the symptoms of withdrawal. This is a hallmark characteristic of addiction. Anyone who compulsively abuses Fioricet to avoid withdrawal likely has an addiction to Fioricet. Additionally, people with an addiction to Fioricet will experience cravings for the medication which further compel them to keeping using it.
Moreover, the ingredient Butalbital is an addictive substance in its own right. Butalbital can cause someone to get “high” because it’s a Central Nervous System (CNS) Depressant. Since Butalbital is part of Fioricet, it is possible for someone to abuse Fioricet as a recreational drug. At high doses, Fioricet can intoxicate a person in a manner similar to alcohol. People who abuse Fioricet for this purpose have as much of a risk of developing an addiction as they would have if they repeatedly used an illegal drug.
Butalbital APA Caffeine Overdose and Treatment
Following an acute overdosage of butalbital, acetaminophen and caffeine, toxicity may result from the barbiturate or the acetaminophen. Toxicity due to caffeine is less likely, due to the relatively small amounts in this formulation.
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of Fioricet can be fatal.
The first signs of an acetaminophen overdose include loss of appetite, nausea, vomiting, stomach pain, sweating, and confusion or weakness. Later symptoms may include pain in your upper stomach, dark urine, and yellowing of your skin or the whites of your eyes.
Overdose symptoms may also include insomnia, restlessness, tremor, diarrhea, increased shallow breathing, uneven heartbeats, seizure (convulsions), or fainting.
Signs And Symptoms
Toxicity from barbiturate poisoning includes drowsiness, confusion, and coma; respiratory depression; hypotension; and hypovolemic shock.
In acetaminophen overdosage: dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necroses, hypoglycemiccoma and coagulation defects may also occur. Early symptoms following a potentially hepatotoxic overdose may include: nausea, vomiting, diaphoresis and general malaise. Clinical and laboratory evidence of hepatic toxicity may not be apparent until 48 to 72 hours post-ingestion.
Acute caffeine poisoning may cause insomnia, restlessness, tremor, and delirium, tachycardia and extrasystoles.
Treatment
A single or multiple drug overdose with this combination product is a potentially lethal polydrug overdose, and consultation with a regional poison control center is recommended. Immediate treatment includes support of cardiorespiratory function and measures to reduce drug absorption.
Oxygen, intravenous fluids, vasopressors, and other supportive measures should be employed as indicated. Assisted or controlled ventilation should also be considered.
Gastric decontamination with activated charcoal should be administered just prior to N-acetylcysteine (NAC) to decrease systemic absorption if acetaminophen ingestion is known or suspected to have occurred within a few hours of presentation. Serum acetaminophen levels should be obtained immediately if the patient presents 4 hours or more after ingestion to assess potential risk of hepatotoxicity; acetaminophen levels drawn less than 4 hours post-ingestion may be misleading. To obtain the best possible outcome, NAC should be administered as soon as possible where impending or evolving liver injury is suspected. Intravenous NAC may be administered when circumstances preclude oral administration.
Vigorous supportive therapy is required in severe intoxication. Procedures to limit the continuing absorption of the drug must be readily performed since the hepatic injury is dose dependent and occurs early in the course of intoxication.
CONTRAINDICATIONS
This product is contraindicated under the following conditions:
- Hypersensitivity or intolerance to any component of this product.
- Patients with porphyria.
CLINICAL PHARMACOLOGY
This combination drug product is intended as a treatment for tension headache.
It consists of a fixed combination of butalbital, acetaminophen and caffeine. The role each component plays in the relief of the complex of symptoms known as tension headache is incompletely understood.
Pharmacokinetics
The behavior of the individual components is described below.
Butalbital
Butalbital is well absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body. Barbiturates in general may appear in breast milk and readily cross the placental barrier. They are bound to plasma and tissue proteins to a varying degree and binding increases directly as a function of lipid solubility.
Elimination of butalbital is primarily via the kidney (59% to 88% of the dose) as unchanged drug or metabolites. The plasma half-life is about 35 hours. Urinary excretion products include parent drug (about 3.6% of the dose), 5-isobutyl-5-(2,3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5 (3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8% of the dose), products with the barbituric acid ring hydrolyzed with excretion of urea (about 14% of the dose), as well as unidentified materials. Of the material excreted in the urine, 32% is conjugated.
The in vitro plasma protein binding of butalbital is 45% over the concentration range of 0.5 to 20 mcg/mL. This falls within the range of plasma protein binding (20% to 45%) reported with other barbiturates such as phenobarbital, pentobarbital, and secobarbital sodium. The plasma-to-blood concentration ratio was almost unity, indicating that there is no preferential distribution of butalbital into either plasma or blood cells (See OVERDOSAGE for toxicity information).
Acetaminophen
Acetaminophen is rapidly absorbed from the gastrointestinal tract and is distributed throughout most body tissues. The plasma half-life is 1.25 to 3 hours, but may be increased by liver damage and following overdosage. Elimination of acetaminophen is principally by liver metabolism (conjugation) and subsequent renal excretion of metabolites. Approximately 85% of an oral dose appears in the urine within 24 hours of administration, most as the glucuronide conjugate, with small amounts of other conjugates and unchanged drug. (See OVERDOSAGE for toxicity information).
Caffeine
Like most xanthines, caffeine is rapidly absorbed and distributed in all body tissues and fluids, including the CNS, fetal tissues, and breast milk.
Caffeine is cleared through metabolism and excretion in the urine. The plasma half-life is about 3 hours. Hepatic biotransformation prior to excretion, results in about equal amounts of 1-methylxanthine and 1-methyluric acid. Of the 70% of the dose that is recovered in the urine, only 3% is unchanged drug. (See OVERDOSAGE for toxicity information).
PATIENT INFORMATION
Information For Patients /Caregivers
- Do not take Esgic® Capsules if you are allergic to any of its ingredients.
- If you develop signs of allergy such as a rash or difficulty breathing, stop taking Esgic® Capsules and contact your healthcare provider immediately.
- Do not take more than 4000 milligrams of acetaminophen per day. Call your doctor if you took more than the recommended dose.
This product may impair mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a car or operating machinery. Such tasks should be avoided while taking this product.
Alcohol and other CNS depressants may produce an additive CNS depression, when taken with this combination product, and should be avoided.
Butalbital may be habit-forming. Patients should take the drug only for as long as it is prescribed, in the amounts prescribed, and no more frequently than prescribed.