BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE tablet

United States - English - NLM (National Library of Medicine)

Buy It Now

Active ingredient:
Butalbital (UNII: KHS0AZ4JVK) (Butalbital - UNII:KHS0AZ4JVK)
Available from:
Cardinal Health
INN (International Name):
Butalbital
Composition:
Butalbital 50 mg
Prescription type:
PRESCRIPTION DRUG
Authorization status:
Abbreviated New Drug Application

BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE- butalbital, acetaminophen, and

caffeine tablet

Cardinal Health

----------

Butalbital,

Acetaminophen, and

Caffeine Tablets, USP

Rev. 01/09

Rx Only

DESCRIPTION

Each tablet, for oral administration contains:

Butalbital, USP.......................................................................................50 mg

Acetaminophen, USP...........................................................................325 mg

Caffeine, USP.........................................................................................40 mg

In addition, each tablet contains the following inactive ingredients: Colloidal Silicon Dioxide, FD&C

Blue No. 1 Aluminum Lake, Magnesium Stearate, Microcrystalline Cellulose, and Sodium Starch

Glycolate.

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:

CLINICAL PHARMACOLOGY

This combination drug product is intended as a treatment for tension headache.

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 0.5-20 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

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.

INDICATIONS AND USAGE

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.

CONTRAINDICATIONS

This product is contraindicated under the following conditions:

Hypersensitivity or intolerance to any component of this product

Patients with porphyria.

WARNINGS

Butalbital is habit-forming and potentially abusable. Consequently, the extended use of this product is

not recommended.

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.

Information for Patients

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 PRECAUTlONS/Geriatric Use.

Laboratory Tests

In patients with severe hepatic or renal disease, effects of therapy should be monitored with serial liver

and/or renal function tests.

Drug Interactions

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.

Drug/Laboratory Test Interactions

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

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 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.

ADVERSE REACTIONS

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 potentialeffects of the components of

this product. Potential effects of high dosageare listed in the OVERDOSAGE section.

Acetaminophen: allergic reactions, rash, thrombocytopenia, agranulocytosis.

Caffeine: cardiac stimulation, irritability, tremor, dependence, nephrotoxicity, hyperglycemia.

DRUG ABUSE AND DEPENDENCE

Abuse and Dependence

Butalbital: 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.

OVERDOSAGE

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.

Signs and Symptoms

Toxicity from barbiturate poisoning include 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 overdose 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.

Treatment

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 (1g/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.

Toxic Doses (for adults):

Butalbital: toxic dose 1g (20 tablets)

Acetaminophen toxic dose 10 g (30 tablets)

Caffeine toxic dose 1g (25 tablets)

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®*.

DOSAGE AND ADMINISTRATION

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.

HOW SUPPLIED

Butalbital, Acetaminophen and Caffeine Tablets, USP 50 mg/325 mg/40mg are Blue, Round, Unscored,

Compressed Tablets; Debossed “West-ward 787”.

They are available in

Bottles of 30 tablets

Bottles of 50 tablets

Bottles of 100 tablets

Bottles of 500 tablets

Bottles of 1000 tablets

Unit Dose Boxes of 100 tablets

Store at 20-25°C (68-77°F) [See USP Controlled Room Temperature].

Protect from light and moisture.

Dispense in a tight, light-resistant container as defined in the USP using a

child-resistant closure.

*Trademark of Medical Economics Company, Inc.

Manufactured By:

West-ward Pharmaceutical Corp.

Eatontown, NJ 07724

Revised January 2009

Butalbital, Acetaminophen and Caffeine Tablets, USP 50 mg/325 mg/40 mg are available from Cardinal

Health in unit dose packages of 100.

Unit dose package of 100 tablets, NDC 55154-7452-4

Cardinal Health

Zanesville OH 43701

IU37361471209

Principal Display Panel - Carton

NDC 55154-7452-4

Butalbital, Acetaminophen

and Caffeine tablets, USP

50 mg/325 mg/40 mg

100 Tablets

Each tablet contains:

Butalbital, USP 50 mg

Acetaminophen 325 mg

Caffeine, USP 40 mg

See product insert for complete prescribing information, precautions and warnings.

USUAL ADULT DOSAGE: One or two tablets every four hours. Do not exceed six tablets per day.

STORAGE: Store at 20-25°C (68-77°F) [See USP Controlled Room Temperature]. Protect from light

and moisture.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

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 by: West-ward Pharmaceutical Corp.

Eatontown, NJ 07724

Repackaged by: Cardinal Health

Zanesville, OH 43701

LUC37361470708

Principal Display Panel - Pouch

Butalbital, Acetaminophen

and Caffeine Tablet, USP

50 mg/325 mg/40 mg

Principal Display Panel - Bag

Butalbital, Acetaminophen

and Caffeine Tablets, USP

50 mg/325 mg/40 mg

10 Tablets

BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE

butalbital, acetaminophen, and caffeine tablet

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:55154-7452(NDC:0 143-178 7)

Route of Administration

ORAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

Buta lbita l (UNII: KHS0 AZ4JVK) (Butalbital - UNII:KHS0 AZ4JVK)

Buta lbita l

50 mg

Aceta mino phen (UNII: 36 2O9 ITL9 D) (Acetamino phen - UNII:36 2O9 ITL9 D)

Ac e ta mino phe n

325 mg

Ca ffeine (UNII: 3G6 A5W338 E) (Caffeine - UNII:3G6 A5W338 E)

Ca ffe ine

40 mg

Inactive Ingredients

Cardinal Health

Ingredient Name

Stre ng th

FD&C BLUE NO . 1 (UNII: H3R47K3TBD)

Ma g nesium Stea ra te (UNII: 70 0 9 7M6 I30 )

CELLULO SE, MICRO CRYSTALLINE (UNII: OP1R32D6 1U)

SILICO N DIO XIDE (UNII: ETJ7Z6 XBU4)

SO DIUM STARCH GLYCO LATE TYPE A PO TATO (UNII: 58 56 J3G2A2)

Product Characteristics

Color

BLUE (BLUE)

S core

no sco re

S hap e

ROUND (ROUND)

S iz e

11mm

Flavor

Imprint Code

We stwa rd;78 7

Contains

Packag ing

#

Item Code

Package Description

Marketing Start Date

Marketing End Date

1

NDC:55154-7452-4

10 0 in 1 CARTON

1

NDC:55154-7452-6

1 in 1 POUCH

2

NDC:55154-7452-0

10 in 1 BAG

2

1 in 1 POUCH

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA0 8 9 718

0 6 /12/19 9 5

Labeler -

Cardinal Health (188557102)

Establishment

Name

Ad d re s s

ID/FEI

Busine ss Ope rations

Cardinal Health

18 8 55710 2

REPACK(55154-7452)

Revised: 5/2012

Similar products

Search alerts related to this product

Share this information