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Isometheptene, Caffeine, and Acetaminophen Tablets

Dosage Form: tablet

Disclaimer: This drug has not been found by FDA to be safe and effective, and this labeling has not been approved by FDA. For further information about unapproved drugs, click here.

Liver Warning

This product contains acetaminophen. Severe liver damage may occur if a person takes:

  • More than 4,000 mg of acetaminophen in 24 hours
  • With other drugs containing acetaminophen
  • With 3 or more alcoholic drinks every day while using this product.

Isometheptene, Caffeine, and Acetaminophen Tablets Description

Each Isometheptene Mucate, Caffeine, and Acetaminophen Caplet contains:

Isometheptene Mucate ......................................... 65 mg
Caffeine ............................................................... 20 mg
Acetaminophen .................................................. 325 mg

Isometheptene Mucate is a white crystalline powder having a characteristic aromatic odor and bitter taste. It is an unsaturated aliphatic amine with sympathomimetic properties. Its molecular weight is 492.65 and it has the following structural formula:

Caffeine is 1H-Purine-2,6-dione, 3,7-dyhydro-1,3,7-trimethyl-. It has the following structural formula:

Acetaminophen, a non-salicylate, occurs as a white, odorless, crystalline powder, possessing a slightly bitter taste. Its molecular weight is 151.16 and it has the following structural formula:

Inactive ingredients include colloidal silicon dioxide, crospovidone polyplasdone, magnesium stearate, microcrystalline cellulose, povidone, pregelatinized starch, and stearic acid.

Isometheptene, Caffeine, and Acetaminophen Tablets - Clinical Pharmacology

Isometheptene mucate, a sympathomimetic amine, acts by constricting dilated cranial and cerebral arterioles, thus reducing the stimuli that lead to vascular headaches. It is particularly desirable in patients predisposed to nausea and vomiting, and where ergotamines are precluded. Its action is similar to ergotamine but possesses a low order of toxicity. 

Caffeine, also a cranial vasoconstrictor, is added to further enhance the vasoconstrictor effect. It is also used as a central stimulant for relief of headache. 

Acetaminophen, an effective non-narcotic analgesic, reduces the perception of pain impulses originating from dilated cerebral vessels; no hyperacidity of stomach and less allergies than aspirin.

INDICATIONS

For relief of tension and vascular headaches.*

*Based on review of this drug (isometheptene mucate), the National Academy of Sciences-National Research Council and/or other information, FDA has classified the other indication as “Possibly” effective in the treatment of migraine headache. Final classification of less than effective indication requires further investigation.

Contraindications

Isometheptene Mucate, Caffeine, and Acetaminophen is contraindicated in Glaucoma and/or severe cases of renal disease, hypertension, organic heart disease, hepatic disease, and in those patients who are on monoamine oxidase inhibitor (MAOI) therapy.

Warnings

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 4,000 milligrams per day, and often involve more than one acetaminophen-containing product. The excessive intake of acetaminophen may be intentional to cause selfharm 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 4,000 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 severe skin reactions, and use of the drug should be discontinued at the first appearance of skin rash or any other sign of hypersensitivity.

Hypersensitivity/Anaphylaxis - There have been post-marketing reports of hypersensitivity and anaphylaxis associated with the 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 Isometheptene Mucate, Caffeine, and Acetaminophen Caplets immediately and seek medical care if they experience these symptoms. Do not prescribe Isometheptene Mucate, Caffeine, and Acetaminophen Caplets for patients with acetaminophen allergy.

Precautions

Caution should be observed in hypertension, peripheral vascular disease and after recent cardiovascular attacks.

INFORMATION FOR PATIENTS

Do not take this product if you are allergic to any of its ingredients. If you develop signs of allergy such as rash or difficulty breathing stop taking this product and contact your healthcare provider immediately.

Do not take more than 4,000 milligrams of acetaminophen per day. Call your doctor if you took more than the recommended dose.

PREGNANCY

Acetaminophen is routinely used for short-term pain relief and fever in all stages of pregnancy.

Acetaminophen crosses the placenta and is believed to be safe in pregnancy when used intermittently for short durations. Isometheptene Mucate, Caffeine and Acetaminophen Caplets should only be given during pregnancy when need has been clearly established.

NURSING MOTHERS

Acetaminophen is excreted into human milk in small concentrations. There are no data on the excretion of isometheptene into human milk.

PEDIATRIC USE

Studies with this medicine have been done only in adult patients, and there is no specific information about its use in children.

GERIATRIC

There is no specific published information comparing use of this combination medicine in the elderly with use in other age groups. Geriatric patients are more likely to have peripheral vascular disease, and are therefore more likely to be adversely affected by peripheral vasoconstriction, than are younger adults. However, isometheptene may be safer for elderly patients than the ergot derivatives used to abort acute vascular headaches. Also, elderly patients are more likely to have age related renal function impairment, which may require caution in patients receiving acetaminophen and isometheptene.

Adverse Reactions

Hypersensitive patients have shown rash and transient dizziness. This can be eliminated by reducing dosage.

Call your doctor or physician for medical advice about side effects. To report SUSPECTED ADVERSE REACTIONS, contact Burel Pharmaceuticals, Inc. at (601)706-9819 or FDA at 800-FDA-1088, www.fda.gov/medwatch.

Overdosage

Following an acute overdosage, toxicity may result.

Acetaminophen – In acetaminophen overdosage: dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necrosis, hypoglycemic coma 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.

Isometheptene, Caffeine, and Acetaminophen Tablets Dosage and Administration

Do not exceed the recommended dosage because severe liver damage may occur.

Tell your doctor about all usage of pain relievers.

   For relief of migraine headache:
   The usual adult dosage is one or two caplets at once, followed by one caplet every hour until relieved, up to 5 caplets within a twelve-hour period.

   For relief of tension headache:
   The usual adult dosage is one or two caplets every four hours up to 8 caplets a day.

How is Isometheptene, Caffeine, and Acetaminophen Tablets Supplied

Isometheptene Mucate, Caffeine, and Acetaminophen caplets are supplied as white caplets debossed “BL 50” on one side and scored on the other side. Available in bottles of 50 caplets, NDC 35573-310-50.

KEEP THIS AND ALL MEDICATION OUT OF THE REACH OF CHILDREN. IN CASE OF ACCIDENTAL OVERDOSE, CALL A DOCTOR OR CONTACT A POISON CONTROL CENTER IMMEDIATELY.

Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F). Avoid exposure to heat. Dispense in a tight, light-resistant container (USP/NF) with a child-resistant closure.

All prescription substitutions using this product shall be pursuant to state statutes as applicable. This is not an Orange Book product.

􀀀Rx Only

Manufactured for:
Burel Pharmaceuticals, Inc.
Richland, MS 39218

Rev. 12/2015

NDC 35573-310-50

Isometheptene Mucate,

Caffeine, and

Acetaminophen

CAPLETS

EACH CAPLET CONTAINS

Isometheptene Mucate ......................................... 65 mg
Caffeine ............................................................... 20 mg
Acetaminophen .................................................. 325 mg

Rx Only

burelpharma

Net Contents: 50 Caplets

ISOMETHEPTENE MUCATE, CAFFEINE, AND ACETAMINOPHEN 
isometheptene mucate, caffeine, and acetaminophen tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:35573-310
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
ISOMETHEPTENE MUCATE (ISOMETHEPTENE) ISOMETHEPTENE MUCATE 65 mg
CAFFEINE (CAFFEINE) CAFFEINE 20 mg
ACETAMINOPHEN (ACETAMINOPHEN) ACETAMINOPHEN 325 mg
Inactive Ingredients
Ingredient Name Strength
SILICON DIOXIDE  
CROSPOVIDONE  
MAGNESIUM STEARATE  
CELLULOSE, MICROCRYSTALLINE  
POVIDONE  
STARCH, PREGELATINIZED CORN  
stearic acid  
Product Characteristics
Color white Score 2 pieces
Shape capsule (Caplet) Size 19mm
Flavor Imprint Code BL;50
Contains         
Packaging
# Item Code Package Description
1 NDC:35573-310-50 50 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
unapproved drug other 04/17/2016
Labeler - Burel Pharmaceuticals, Inc (002152814)
Revised: 02/2016
 
Burel Pharmaceuticals, Inc
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