BUTALBITAL, ACETAMINOPHEN AND CAFFEINE TABLETS, USP 50 mg/325 mg/40 mg | Butalbital, Acetaminophen and Caffeine

10:12 EDT 2nd September 2014 | BioPortfolio
Note: While we endeavour to keep our records up-to-date one should not rely on these details being accurate without first consulting a professional. Click here to read our full medical disclaimer.

Rx only

Butalbital, Acetaminophen and Caffeine Tablets, USP are supplied in tablet form for oral administration.

Each tablet contains the following active ingredients:

Inactive Ingredients:

colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and stearic acid.

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:

IMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-01.jpgIMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-02.jpgIMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-03.jpg

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.

The behavior of the individual components is described below.

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 0.5–20 mcg/mL. This falls within the range of plasma protein binding (20%–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 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.

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.

Butalbital, acetaminophen and caffeine tablets are 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.

This product is contraindicated under the following conditions:

Butalbital is habit-forming and potentially abusable. Consequently, the extended use of this product is not recommended.

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.

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.

For information on use in geriatric patients, see PRECAUTIONS/Geriatric Use .

In patients with severe hepatic or renal disease, effects of therapy should be monitored with serial liver and/or renal function tests.

The CNS effects of butalbital may be enhanced by monoamine oxidase (MAO) inhibitors.

Butalbital, acetaminophen and caffeine may enhance the effects of: other narcotic analgesics, alcohol, general anesthetics, tranquilizers such as chlordiazepoxide, sedative-hypnotics, or other CNS depressants, causing increased CNS depression.

Acetaminophen may produce false-positive test results for urinary 5-hydroxyindoleacetic acid.

No adequate studies have been conducted in animals to determine whether acetaminophen or butalbital have a potential for carcinogenesis, mutagenesis or impairment of fertility.

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.

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.

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.

Safety and effectiveness in pediatric patients below the age of 12 have not been established.

Clinical studies of butalbital, acetaminophen and caffeine tablets 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.

Frequently Observed

The most frequently reported adverse reactions are drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, abdominal pain, and intoxicated feeling.

Infrequently Observed

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.

Cardiovascular:   tachycardia.

Musculoskeletal:   leg pain, muscle fatigue.

Genitourinary:   diuresis.

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.

Barbiturates may be habit-forming:

Tolerance, psychological dependence, and physical dependence may occur especially 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 and fatal dosage becomes smaller. The lethal dose of a barbiturate is far less if alcohol is also ingested. Major withdrawal symptoms (convulsions and delirium) may occur within 16 hours and 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 and gradual withdrawal of the drug. Barbiturate-dependent patients can be withdrawn by using a number of different withdrawal regimens. One method involves initiating treatment at the patient's regular dosage level and gradually decreasing the daily dosage as tolerated by the patient.

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.

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, hypoglycemic coma and thrombocytopenia 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. In adults hepatic toxicity has rarely been reported with acute overdoses of less than 10 grams, or fatalities with less than 15 grams.

Acute caffeine   poisoning may cause insomnia, restlessness, tremor, and delirium, tachycardia and extrasystoles.

A single or multiple 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. Vomiting should be induced mechanically, or with syrup of ipecac, if the patient is alert (adequate pharyngeal and laryngeal reflexes). Oral activated charcoal (1 g/kg) should follow gastric emptying. The first dose should be accompanied by an appropriate cathartic. If repeated doses are used, the cathartic might be included with alternate doses as required. Hypotension is usually hypovolemic and should respond to fluids. Pressors should be avoided. A cuffed endotracheal tube should be inserted before gastric lavage of the unconscious patient and, when necessary, to provide assisted respiration. If renal function is normal, forced diuresis may aid in the elimination of the barbiturate. Alkalinization of the urine increases renal excretion of some barbiturates, especially phenobarbital.

Meticulous attention should be given to maintaining adequate pulmonary ventilation. In severe cases of intoxication, peritoneal dialysis, or preferably hemodialysis may be considered. If hypoprothrombinemia occurs due to acetaminophen overdose, vitamin K should be administered intravenously.

If the dose of acetaminophen may have exceeded 140 mg/kg, acetylcysteine should be administered as early as possible. Serum acetaminophen levels should be obtained, since levels four or more hours following ingestion help predict acetaminophen toxicity. Do not await acetaminophen assay results before initiating treatment. Hepatic enzymes should be obtained initially, and repeated at 24-hour intervals.

Methemoglobinemia over 30% should be treated with methylene blue by slow intravenous administration.

In all cases of suspected overdosage, call your Regional Poison Control Center to obtain the most up-to-date information about the treatment of overdosage. Telephone numbers of certified Regional Poison Control Centers are listed in the Physicians' Desk Reference.

Butalbital: toxic dose 1 g (20 tablets)
Acetaminophen: toxic dose 10 g (30 tablets)
Caffeine: toxic dose 1 g (25 tablets)

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.

Butalbital, Acetaminophen and Caffeine Tablets, USP

Containing 50 mg butalbital, 325 mg acetaminophen and 40 mg caffeine. Available as white, round shaped tablets, debossed "2355" on one side, and debossed "V" on the reverse side. Bottles of 100, 500 and 1000.

Store at 20°-25°C (68°-77°F) with excursions permitted between 15°-30°C (59°-86°F) [see USP Controlled Room Temperature]; dispense in a tight, light-resistant container as defined in the USP.

Trademark of Medical Economics Company, Inc.

Manufactured for: QUALITEST PHARMACEUTICALS Huntsville, AL 35811

8181466R3/08-R2

Butalbital, Acetaminophen and Caffeine Tablets, USP, containing 50 mg of butalbital,

325 mg acetaminophen and 40 mg caffeine are available from Cardinal Health in unit

dose packages of 100.

Unit dose package of 100 tablets, NDC 55154-0832-4

Cardinal Health

Zanesville OH 43701

IU42964890410

NDC: 55154-0832-4

Butalbital, Acetaminophen and Caffeine Tablets, USP

50 mg/ 325 mg/ 40 mg

100 Tablets

EACH TABLET CONTAINS:

Butalbital, USP 50 mg

Acetaminophen, USP 325 mg

Caffeine, USP 40 mg

See product insert for prescribing information, precautions and warnings.

USUAL ADULT DOSAGE: 1 or 2 tablets every four hours as needed. Total daily dose should not exceed 6 tablets.

STORAGE: Store at 20° - 25°C (68° - 77°F) with excursions permitted between 15° - 30°C (59° - 86°F) [see USP Controlled Room Temperature].

DISPENSE in a tight, light-resistant container as defined in the USP.

RX ONLY

WARNING: This package is intended for institutional use only. This package is not child resistant. Keep this and all drugs out of the reach of children.

See window for lot number and expiration date.

Manufactured for: QUALITEST PHARMACEUTICALS

HUNTERSVILLE, AL 35811

Repackaged by: Cardinal Health

Zanesville, OH 43701

LUC42964890610

IMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-04.jpg

Butalbital, Acetaminophen and Caffeine Tablet, USP

50 mg/ 325 mg/ 40 mg

IMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-05.jpg

Butalbital, Acetaminophen and Caffeine Tablets, USP

50 mg/ 325 mg/ 40 mg

10 Tablets

IMAGE ab17d24a-57af-4d8d-ae01-7e6846107373-06.jpg

Manufacturer

Cardinal Health, Inc.

Active Ingredients

Source

Clinical Trials [206 Associated Clinical Trials listed on BioPortfolio]

T3AI-Pain After Breast Surgery

Current standard of care for post-operative analgesia after breast surgery in CDHA is Tylenol #3® (300 mg acetaminophen, 30 mg codeine, 15 mg caffeine per tablet). We are proposing to tes...

Treximet® Versus Butalbital-Containing Combination Medications for the Acute Treatment of Migraine in Adults (Study 2 of 2)

Study TRX109013, A Randomized, Double-Blind, Double-Dummy, Placebo-Controlled, Crossover Study to Evaluate the Efficacy of TREXIMET® (Sumatriptan + Naproxen Sodium) versus Butalbital-Con...

Effects of Low Doses of Caffeine on Mood, Physiology and Mental Function

It is often assumed that levels of caffeine found in ‘decaffeinated’ beverages are below any psychopharmacological threshold. However, recent findings indicate that caffeine doses as l...

The Effect of Caffeine in Elderly Citizen Following Eight Hour Abstinence From Caffeine Containing Drinks & Foods

The study investigated the effect of caffeine on physical performance in healthy citizens aged over 70 years following eight hours of abstinence from caffeine containing drinks and foods. ...

A Study on Health - Related Quality of Life in Patients With Rheumatic Diseases Taking Tramadol 37.5mg/Acetaminophen 325mg Tablets

The objective of this observational study is to assess improvement of quality of life in the patients who are administered Tramadol 37.5mg/Acetaminophen 325mg tablets for 10~14 weeks accor...

PubMed Articles [268 Associated PubMed Articles listed on BioPortfolio]

Caffeine Content Labeling: A Missed Opportunity for Promoting Personal and Public Health.

Current regulation of caffeine-containing products is incoherent, fails to protect consumers' interests, and should be modified in multiple ways. We make the case for one of the regulatory reforms tha...

Characterization of heroin samples by (1)H NMR and 2D DOSY (1)H NMR.

Twenty-four samples of heroin from different illicit drug seizures were analyzed using proton Nuclear Magnetic Resonance ((1)H NMR) and two-dimensional diffusion-ordered spectroscopy (2D DOSY) (1)H NM...

Results of a multicenter, double-blind, randomized, parallel-group, placebo-controlled, single-dose study comparing the fixed combination of acetaminophen, acetylsalicylic acid, and caffeine with ibuprofen for acute treatment of patients with severe migraine.

In a multicenter, double-blind, randomized, parallel-group, placebo-controlled, single-dose study ( N  = 1555), a fixed combination of acetaminophen 500 mg, acetylsalicylic acid 500 mg, and ca...

Caffeine and Cognitive Performance: Persistent Methodological Challenges in Caffeine Research.

Human cognitive performance is widely perceived to be enhanced by caffeine at usual dietary doses. However, the evidence for and against this belief continues to be vigorously contested. Controversy h...

Drug Utilization, Dosing, and Costs After Implementation of Intravenous Acetaminophen Guidelines for Pediatric Patients.

The objectives of this evaluation of medication use were to characterize the use of intravenous acetaminophen at our institution and to determine if acetaminophen was prescribed at age-appropriate dos...

Search BioPortfolio:
Advertisement

Relevant Topic

Pain
Latest News Clinical Trials Research Drugs Reports Corporate
Pain is defined by the International Association for the Study of Pain as “an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage”. Some illnesses can be excruci...

Advertisement

Drugs and Medication Quicklinks


Searches Linking to this Drug Record