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

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

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Active ingredient:
BUTALBITAL (UNII: KHS0AZ4JVK) (BUTALBITAL - UNII:KHS0AZ4JVK), ACETAMINOPHEN (UNII: 362O9ITL9D) (ACETAMINOPHEN - UNII:362O9ITL9D), CAFFEINE (UNII: 3G6A5W338E) (CAFFEINE - UNII:3G6A5W338E)
Available from:
West-Ward Pharmaceutical Corp
INN (International Name):
BUTALBITAL
Composition:
BUTALBITAL 50 mg
Administration route:
ORAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
Butalbital, Acetaminophen, and Caffeine Capsules, USP 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: * Hypersensitivity or intolerance to any component of this product. * Patients with porphyria. 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 ma
Product summary:
Butalbital 50 mg, Acetaminophen 500 mg and Caffeine 40 mg Capsules, USP are supplied as salmon/red capsules printed “170” in white ink and are available in:       Bottles of 100 capsules Store at 20° to 25°C (68° to 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. Manufactured By: West-Ward Pharmaceutical Corp. Eatontown, NJ 07724 Revised November 2013
Authorization status:
Abbreviated New Drug Application
Authorization number:
0143-0170-01

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

caffeine capsule

West-Ward Pharmaceutical Corp

----------

Butalbital, Acetaminophen, and Caffeine Capsules

BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE CAPSULES, USP

Rx Only

Hepatotoxicity

Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver

transplant and death. Most of the cases of liver injury are associated with the use of

acetaminophen at doses that exceed 4000 milligrams per day, and often involve more than one

acetaminophen containing product.

DESCRIPTION:

Butalbital, Acetaminophen, and Caffeine is supplied in capsule form for oral administration. Each

capsule contains:

Butalbital, USP……………………..50 mg

Acetaminophen, USP………………500 mg

Caffeine, USP…………………… …40 mg

In addition, each capsule contains the following inactive ingredients: colloidal silicon dioxide,

magnesium stearate, sodium lauryl sulfate, and sodium starch glycolate.

Capsule shell contains: D&C Red #33, D&C Yellow #10, FD&C Red #40, Gelatin and Titanium

Dioxide. The imprinting ink contains Titanium Dioxide.

Butalbital (5-allyl-5-isobutylbarbituric acid), a white, odorless, crystalline powder having a slightly

bitter taste, is a short to intermediate-acting barbiturate. It has the following structural formula:

Acetaminophen (4´-hydroxyacetanilide), a slightly bitter, white, odorless, crystalline powder, is a non-

opiate, non-salicylate analgesic and antipyretic. It has the following structural formula:

Caffeine (1,3,7,-trimethylxanthine), a bitter, white crystalline powder or white-glistening needles, 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.

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.)

INDICATIONS AND USAGE:

Butalbital, Acetaminophen, and Caffeine Capsules, USP 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.

Hepatotoxicity

Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver

transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at

doses that exceed 4000 milligrams per day, and often involve more than one acetaminophen containing

product. The excessive intake of acetaminophen may be intentional to cause self-harm or unintentional

as patients attempt to obtain more pain relief or unknowingly take other acetaminophen-containing

products.

The risk of acute liver failure is higher in individuals with underlying liver disease and in individuals

who ingest alcohol while taking acetaminophen.

Instruct patients to look for acetaminophen or APAP on package labels and not to use more than one

product that contains acetaminophen. Instruct patients to seek medical attention immediately upon

ingestion of more than 4000 milligrams of acetaminophen per day, even if they feel well.

Serious skin reactions

Rarely, acetaminophen may cause serious skin reactions such as acute generalized

exanthematous pustulosis (AGEP), Stevens-Johnson Syndrome (SJS), and toxic epidermal necrolysis

(TEN), which can be fatal. Patients should be informed about the signs of serious skin reactions. And

use of the drug should be discontinued at the first appearance of skin rash or any other sign of

hypersensitivity.

Hypers ens itivity/anaphylaxis

There have been post-marketing reports of hypersensitivity and anaphylaxis associated with use of

acetaminophen. Clinical signs included swelling of the face, mouth, and throat, respiratory distress,

urticaria, rash, pruritus, and vomiting. There were infrequent reports of life-threatening anaphylaxis

requiring emergency medical attention. Instruct patients to discontinue Butalbital, Acetaminophen and

Caffeine Capsules immediately and seek medical care if they experience these symptoms. Do not

prescribe Butalbital, Acetaminophen and Caffeine Capsules for patients with acetaminophen allergy.

PRECAUTIONS:

General:

Butalbital, Acetaminophen, and Caffeine Capsules 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/Caregivers:

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.

Do not take Butalbital, Acetaminophen and Caffeine 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 Butalbital,

Acetaminophen and Caffeine 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.

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 Capsules 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-hydroxyindoleacetic 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:

Barbiturates, acetaminophen and caffeine 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 capsules 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: 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: 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.

To report SUSPECTED ADVERSE REACTIONS, contact West-Ward Pharmaceutical Corp. at 1-877-

233-2001, or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

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 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.

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 (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.

Toxic Doses (for adults):

Butalbital: toxic dose 1 g (20 capsules)

Acetaminophen: toxic dose 10 g (20 capsules)

Caffeine: toxic dose 1 g (25 capsules)

DOSAGE AND ADMINISTRATION:

Oral: one capsule every four hours. Total daily dosage should not exceed 6 capsules.

Extended and repeated use of this product is not recommended because of the potential for

physical dependence.

HOW SUPPLIED:

Butalbital 50 mg, Acetaminophen 500 mg and Caffeine 40 mg Capsules, USP are supplied as salmon/red

capsules printed “170” in white ink and are available in:

Bottles of 100 capsules

Store at 20° to 25°C (68° to 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.

Manufactured By:

West-Ward Pharmaceutical Corp.

Eatontown, NJ 07724

Revised November 2013

PRINCIPAL DISPLAY PANEL

NDC 0143-1115-01

Butalbital, Acetaminophen, and

Caffeine Tablets, USP

50 mg/500 mg/40 mg

Rx Only

100 Tablets

BUTALBITAL, ACETAMINOPHEN, AND CAFFEINE

butalbital, acetaminophen, and caffeine capsule

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:0 143-0 170

Route of Administration

ORAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

BUTALBITAL (UNII: KHS0 AZ4JVK) (BUTALBITAL - UNII:KHS0 AZ4JVK)

BUTALBITAL

50 mg

ACETAMINO PHEN (UNII: 36 2O9 ITL9 D) (ACETAMINOPHEN - UNII:36 2O9 ITL9 D)

ACETAMINOPHEN

50 0 mg

CAFFEINE (UNII: 3G6 A5W338 E) (CAFFEINE - UNII:3G6 A5W338 E)

CAFFEINE

40 mg

Inactive Ingredients

Ingredient Name

Stre ng th

SILICO N DIO XIDE (UNII: ETJ7Z6 XBU4)

MAGNESIUM STEARATE (UNII: 70 0 9 7M6 I30 )

SO DIUM LAURYL SULFATE (UNII: 36 8 GB5141J)

D&C RED NO . 3 3 (UNII: 9 DBA0 SBB0 L)

D&C YELLO W NO . 10 (UNII: 35SW5USQ3G)

FD&C RED NO . 4 0 (UNII: WZB9 127XOA)

GELATIN (UNII: 2G8 6 QN327L)

TITANIUM DIO XIDE (UNII: 15FIX9 V2JP)

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

Product Characteristics

Color

RED (salmo n/red)

S core

no sco re

S hap e

CAPSULE

S iz e

18 mm

West-Ward Pharmaceutical Corp

Flavor

Imprint Code

Contains

Packag ing

#

Item Code

Package Description

Marketing Start Date

Marketing End Date

1

NDC:0 143-0 170 -0 1

10 0 in 1 BOTTLE

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA0 40 26 1

10 /28 /19 9 8

Labeler -

West-Ward Pharmaceutical Corp (001230762)

Revised: 11/2013

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