Isometheptene, Caffeine, and Acetaminophen Tablets

Dosage Form: tablet

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Isometheptene, Caffeine, and Acetaminophen Tablets

BOXED WARNING
WARNINGHepatotoxicityIsometheptene, Caffeine, and Acetaminophen Tablets contain acetaminophen, isometheptene mucate and caffeine. 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 in combination with other acetaminophen-containing products.

Isometheptene, Caffeine, and Acetaminophen Tablets Description

Each Isometheptene, Caffeine, and Acetaminophen Tablet contains:

Isometheptene Mucate ...................................... 130 mg

Caffeine ............................................................... 20 mg

Acetaminophen .................................................. 500 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. Isometheptene mucate has the following structural formula:

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Figure 1: Isometheptene mucate

(C9H19N)2•C6H10O8 M.W. 492.65

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

Figure 2: Caffeine

C8H10N4O2 M.W. 194.19

Acetaminophen, a non-salicylate, occurs as a white, odorless, crystalline powder, possessing a slightly bitter taste. Acetaminophen is Acetamide, N-(4-hydroxyphenyl)-. It has the following structural formula:

Figure 3: Acetaminophen

C8H9NO2 M.W. 151.16

INACTIVE INGREDIENTS

Inactive ingredients include calcium phosphate, colloidal silicone dioxide, crospovidone polyplasdone, magnesium stearate, microcrystalline cellulose, Povidone, Prosolv, 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 and Usage for Isometheptene, Caffeine, and Acetaminophen Tablets

For relief of tension and vascular headaches.*

Based on a 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

This Product 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 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 4,000 milligrams of acetaminophen per day, even if they feel well.

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, Caffeine, and Acetaminophen Tablets immediately and seek medical care if they experience these symptoms. Do not prescribe Isometheptene, Caffeine, and Acetaminophen Tablets for patients with acetaminophen allergy.

Adverse Reactions

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

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.

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

FOR RELIEF OF MIGRAINE HEADACHE: The usual adult dosage is two tablets at once, followed by one tablet every hour until relieved, up to 5 tablets within a twelve hour period.

FOR RELIEF OF TENSION HEADACHE: The usual adult dosage is one or two tablets every four hours up to 8 tablets a day.

How is Isometheptene, Caffeine, and Acetaminophen Tablets Supplied

Isometheptene, Caffeine, and Acetaminophen Tablets are supplied as white tablets debossed “130” on one side, and scored on the opposite side. Available in bottles of 50 tablets, NDC 50967-620-50.

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.

Storage and Handling

Store at 20°-25°C (68°-77°F). See USP Controlled Room Temperature. Avoid exposure to heat.

Dispense in a tight, light-resistant container as defined in USP/NF with a child-resistant closure.

Manufactured for:

Women’s Choice Pharmaceuticals

Gilbert, AZ 85233

(877) 774-4949

500421 Rev. 09/2011

PRINCIPAL DISPLAY PANEL

Figure 4: Bottle Label

ISOMETHEPTENE MUCATE, CAFFEINE, AND ACETAMINOPHEN 
isometheptene mucate, caffeine, and acetaminophen tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:50967-620
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
ACETAMINOPHEN (ACETAMINOPHEN) ACETAMINOPHEN 500 mg
CAFFEINE (CAFFEINE) CAFFEINE 20 mg
ISOMETHEPTENE MUCATE (ISOMETHEPTENE) ISOMETHEPTENE MUCATE 130 mg
Inactive Ingredients
Ingredient Name Strength
ANHYDROUS DIBASIC CALCIUM PHOSPHATE  
SILICON DIOXIDE  
CROSPOVIDONE  
MAGNESIUM STEARATE  
CELLULOSE, MICROCRYSTALLINE  
POVIDONE K30  
STEARIC ACID  
Product Characteristics
Color WHITE Score 2 pieces
Shape CAPSULE Size 19mm
Flavor Imprint Code 130
Contains         
Packaging
# Item Code Package Description
1 NDC:50967-620-50 50 TABLET (TABLET) in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
Unapproved drug other 10/12/2011
Labeler - Womens Choice Pharmaceuticals, LLC (833067841)
Registrant - Womens Choice Pharmaceuticals, LLC (833067841)
Establishment
Name Address ID/FEI Operations
Sovereign Pharmaceuticals, LLC 623168267 MANUFACTURE
Revised: 08/2011
 
Womens Choice Pharmaceuticals, LLC
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