Albenza

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Take with food.

In a young child (or anyone who is unable to swallow a whole albendazole tablet), the tablet should be crushed or chewed and swallowed with a full glass of water.

You may be given other medicines to prevent certain side effects of albendazole, or certain effects that can result when the parasites die within your body.

Tell your doctor if you have any changes in weight. Albendazole doses are based on weight.

Use this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Albendazole will not treat a viral infection such as the flu or a common cold.

Albendazole can weaken your immune system. Your blood may need to be tested often. You will need frequent blood tests (every 2 weeks) to check your liver function.

Store at room temperature away from moisture and heat.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

>10%

Headache

• Neurocysticercosis (11%)
• Hydatid disease (1.3%)

Abnormal LFT

• Hydatid disease (15.6%)
• Neurocysticercosis (<1%)

1-10%

Abdominal pain

• Hydatid disease (6%)

Nausea/vomiting

• Hydatid disease (3.7%)
• Neurocysticercosis (6.2%)

Dizziness/vertigo

• Hydatid disease (1.2%)
• Neurocysticercosis (<1%)

Increased intracranial pressure

• Neurocysticercosis (1%)

Meningeal signs

• Neurocysticercosis (1%)

Alopecia (reversible)

• Hydatid disease (1.6%)
• Neurocysticercosis (<1%)

Fever

• Hydatid disease (1%)

<1% (selected)

Rash

Urticaria

Agranulocytosis

Aplastic anemia

Bone marrow suppression

Granulocytopenia

Pancytopenia

Thrombocytopenia

Hepatitis

Acute liver failure

Acute renal failure

ALBENZA (albendazole) is an orally administered anthelmintic drug. Chemically, it is methyl 5(propylthio)-2-benzimidazolecarbamate. Its molecular formula is C12H15N3O2S. Its molecular weight is 265.34. It has the following chemical structure:

Albendazole is a white to yellowish powder. It is freely soluble in anhydrous formic acid and very slightly soluble in ether and in methylene chloride. Albendazole is practically insoluble in alcohol and in water.

Tablets

Each white to off-white, circular, biconvex, bevel-edged film coated, TILTAB tablet is debossed with “ap” and “550” and contains 200 mg of albendazole.

Inactive ingredients consist of: carnauba wax, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate, sodium saccharin, sodium starch glycolate, and starch.

Chewable Tablets

Each round, mottled pink, concave chewable tablet is debossed with “ap” above “551” and contains 200 mg of albendazole.

Inactive ingredients consist of: lactose monohydrate, microcrystalline cellulose, D-mannitol, sodium starch glycolate, povidone, N-C Wild Berry Type Flavor, magnesium stearate, crospovidone, polyvinyl acetate, sucralose, colloidal silicone dioxide, sodium lauryl sulfate, D&C Red #30/Helendon Pink Aluminum Lake.

In case of overdosage, symptomatic therapy and general supportive measures are recommended.

Serious side effects have been reported. See "Drug Precautions" section.

Common side effects including:

• stomach pain
• nausea
• vomiting
• headache
• dizziness

This is not a complete list of Albenza side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Albendazole is an anthelmintic (an-thel-MIN-tik) or anti- worm medication. It prevents newly hatched insect larvae (worms) from growing or multiplying in your body.

Albendazole is used to treat certain infections caused by worms such as pork tapeworm and dog tapeworm.

Albendazole may also be used for purposes not listed in this medication guide.

You should not use this medicine if you are allergic to albendazole, or to similar drugs such as mebendazole (Vermox).

To make sure albendazole is safe for you, tell your doctor if you have:

• liver disease; or

• bone marrow suppression.

It is not known whether this medicine will harm an unborn baby. Albendazole should not be used during pregnancy, unless there is no alternate treatment. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine. Use effective birth control to prevent pregnancy while taking this medicine and for at least 1 month after your treatment ends.

You may need to have a negative pregnancy test before starting this treatment.

It is not known whether albendazole passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Contraindications

• Hypersensitivity to benzimidazole derivatives or any component in the formulation.1

Warnings/Precautions

Warnings

Can cause bone marrow suppression, aplastic anemia, and agranulocytosis in patients with or without underlying hepatic dysfunction.1 Reversible leukopenia has occurred in <1% of patients receiving the drug;1 granulocytopenia, pancytopenia, agranulocytosis, or thrombocytopenia reported rarely.1 Rare fatalities reported due to granulocytopenia or pancytopenia.1

Monitor blood counts at the beginning of each 28-day cycle of albendazole treatment and every 2 weeks during treatment.1 Closer monitoring of blood counts is recommended in patients with liver disease, including hepatic echinococcosis, since these individuals may be more susceptible to bone marrow suppression leading to pancytopenia, aplastic anemia, agranulocytosis, and leukopenia.1

Discontinue albendazole if clinically important decreases in blood cell counts occur.1

Teratogenic effects (embryotoxicity, skeletal malformations) reported in rats and rabbits.1

Exclude pregnancy before initiating albendazole.1 Avoid pregnancy during and for at least 1 month after treatment.1 If patient becomes pregnant, immediately discontinue the drug and apprise patient of the potential hazard to the fetus.1 (See Pregnancy under Cautions.)

General Precautions

Adverse CNS effects (e.g., seizures and/or hydrocephalus) resulting from inflammatory reactions to damaged intracerebral cysts may occur when albendazole is used for treatment of neurocysticercosis.5 7 Use appropriate corticosteroid and anticonvulsant treatment as required.1 5 7 8 Consider oral or IV corticosteroid therapy during the first week of treatment to prevent cerebral hypertension.1

Destruction of cysticercal lesions by albendazole may cause retinal damage.1 5 8 Prior to treatment of neurocysticercosis, examine patient for retinal lesions.1 In those with such lesions, weigh the need for treatment against the possibility of irreparable retinal damage.1 5 8

Mild to moderate increases of hepatic enzymes occurred in about 16% of patients in clinical trials.1 Hepatic enzymes generally return to normal when the drug is discontinued, but acute liver failure of uncertain casualty and hepatitis have been reported.1

Perform liver function tests (hepatic transaminase concentrations) prior to each cycle of albendazole treatment and at least every 2 weeks during treatment.1 If hepatic enzymes exceed twice the ULN, consider discontinuing the drug based on the individual patient circumstance.1 Decisions to reinstitute albendazole when hepatic enzymes return to pretreatment levels should be individualized taking into account the risks and benefits of further albendazole treatment.1 If the drug is reinstituted, perform laboratory tests frequently.1

Specific Populations

Category C.1 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Use during pregnancy only if benefits justify risks to the fetus and only when no alternative management is appropriate.1

Use in women of childbearing age only after a negative pregnancy test; caution women against becoming pregnant while receiving albendazole and for at least 1 month after completing treatment.1

Discontinue immediately if patient becomes pregnant.1

Distributed into animal milk; not known whether distributed into human milk.1 Use with caution in nursing women.1

Only limited experience in children <6 years of age.1

Has been used for treatment of neurocysticercosis in pediatric patients as young as 1 year of age; efficacy appeared to be similar to that in adults and no unusual problems were reported.1

Has been used without unusual problems for treatment of hydatid disease in infants and young children.1

Experience in patients ≥65 years of age is limited.1 Has been used without unusual problems for treatment of neurocysticercosis or hydatid disease in geriatric adults.1

Individuals with hepatic impairment are at increased risk for hepatotoxicity and bone marrow suppression during albendazole treatment.1

Discontinue albendazole if hepatic enzymes exceed twice the ULN or if clinically important decreases in blood cell counts occur.1

Not studied, but clearance of albendazole unlikely to be affected.1

Common Adverse Effects

Treatment of hydatid disease: Abnormal liver function test results, abdominal pain, nausea, vomiting, reversible alopecia, headache, dizziness.1

Treatment of neurocysticercosis: Headache, nausea, vomiting, raised intracranial pressure, meningeal signs.1

Absorption

Bioavailability

Poorly absorbed from GI tract because of low aqueous solubility.1

Rapidly converted to active metabolite (albendazole sulfoxide) before reaching systemic circulation.1 Peak plasma concentrations of albendazole sulfoxide attained 2–5 hours after a dose.1

Food

Oral bioavailability enhanced by coadministration with fatty meal (estimated fat content 40 g); plasma concentrations up to fivefold higher compared with administration in fasted state.1

Distribution

Extent

Widely distributed throughout body.1 Detected in urine, bile, liver, cyst wall, cyst fluid, and CSF.1

Plasma Protein Binding

70% bound to plasma protein.1

Elimination

Metabolism

Rapidly converted in liver to active metabolite (albendazole sulfoxide) which is responsible for anthelmintic activity.1 Further metabolized to albendazole sulfone and other primary oxidative metabolites.1

Elimination Route

Albendazole is undetectable in urine; <1% of albendazole sulfoxide detectable in urine.1 Albendazole sulfoxide partially eliminated in bile.1

Half-life

Albendazole sulfoxide: 8–12 hours.1

Special Populations

Patients with extrahepatic obstruction: Increased albendazole sulfoxide serum concentration and prolonged half-life.1 Elimination half-life may be 31.7 hours.1

Patients with renal impairment: Pharmacokinetics not studied to date.1

Geriatric patients: Pharmacokinetics not fully evaluated; data from patients up to 79 years of age with hydatid cysts suggest pharmacokinetics similar to young, healthy adults.1

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of albendazole to treat neurocysticercosis in children. However, hydatid disease is uncommon in children.

Geriatric

Although appropriate studies on the relationship of age to the effects of albendazole have not been performed in the geriatric population, no geriatric-specific problems have been documented to date.

Pregnancy

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Bone marrow problems (eg, agranulocytosis, aplastic anemia, granulocytopenia, pancytopenia)—Use with caution. May make these conditions worse.

• Cysticercosis involving the eye—Patients who are being treated with albendazole for neurocysticercosis should be examined for lesions in the eye. Using this medicine may increase your risk of side effects involving the eye.

• Liver disease or
• Liver enzymes, elevated—Use with caution. May increase risk for more serious side effects.

Bone Marrow Suppression

Fatalities associated with the use of Albenza have been reported due to granulocytopenia or pancytopenia Albenza may cause bone marrow suppression, aplastic anemia, and agranulocytosis. Monitor blood counts at the beginning of each 28-day cycle of therapy, and every 2 weeks while on therapy with Albenza in all patients. Patients with liver disease and patients with hepatic echinococcosis are at increased risk for bone marrow suppression and warrant more frequent monitoring of blood counts. Discontinue Albenza if clinically significant decreases in blood cell counts occur.

Teratogenic Effects

Albenza may cause fetal harm and should not be used in pregnant women except in clinical circumstances where no alternative management is appropriate. Obtain pregnancy test prior to prescribing Albenza to women of reproductive potential. Advise women of reproductive potential to use effective birth control for the duration of Albenza therapy and for one month after end of therapy. Immediately discontinue Albenza if a patient becomes pregnant and apprise the patient of the potential hazard to the fetus [see Use in Specific Populations (8.1)].

Risk of Neurologic Symptoms in Neurocysticercosis

Patients being treated for neurocysticercosis should receive steroid and anticonvulsant therapy to prevent neurological symptoms (e.g. seizures, increased intracranial pressure and focal signs) as a result of an inflammatory reaction caused by death of the parasite within the brain.

Risk of Retinal Damage in Patients with Retinal Neurocysticercosis

Cysticercosis may involve the retina. Before initiating therapy for neurocysticercosis, examine the patient for the presence of retinal lesions. If such lesions are visualized, weigh the need for anticysticeral therapy against the possibility of retinal damage resulting from inflammatory damage caused by Albenza-induced death of the parasite.

Hepatic Effects

In clinical trials, treatment with Albenza has been associated with mild to moderate elevations of hepatic enzymes in approximately 16% of patients. These elevations have generally returned to normal upon discontinuation of therapy. There have also been case reports of acute liver failure of uncertain causality and hepatitis [see Adverse Reactions (6)].

Monitor liver enzymes (transaminases) before the start of each treatment cycle and at least every 2 weeks during treatment. If hepatic enzymes exceed twice the upper limit of normal, consideration should be given to discontinuing Albenza therapy based on individual patient circumstances. Restarting Albenza treatment in patients whose hepatic enzymes have normalized off treatment is an individual decision that should take into account the risk/benefit of further Albenza usage. Perform laboratory tests frequently if Albenza treatment is restarted.

Patients with elevated liver enzyme test results are at increased risk for hepatotoxicity and bone marrow suppression [see Warnings and Precautions (5.1)]. Discontinue therapy if liver enzymes are significantly increased or if clinically significant decreases in blood cell counts occur.

Unmasking of Neurocysticercosis in Hydatid Patients

Undiagnosed neurocysticercosis may be uncovered in patients treated with Albenza for other conditions. Patients with epidemiologic factors who are at risk for neurocysticercosis should be evaluated prior to initiation of therapy.

Albenza (albendazole) is an orally administered anthelmintic drug. Chemically, it is methyl 5-(propylthio)-2-benzimidazolecarbamate. Its molecular formula is C12H15N3O2S. Its molecular weight is 265.34. It has the following chemical structure:

Albendazole is a white to yellowish powder. It is freely soluble in anhydrous formic acid and very slightly soluble in ether and in methylene chloride. Albendazole is practically insoluble in alcohol and in water.

Tablets

Each white to off-white, circular, biconvex, bevel-edged film coated, TILTAB tablet is debossed with “ap” and “550” and contains 200 mg of albendazole.

Inactive ingredients consist of: carnauba wax, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate, sodium saccharin, sodium starch glycolate, and starch.

Chewable Tablets

Each round, mottled pink, concave chewable tablet is debossed with “ap” above “551” and contains 200 mg of albendazole.

Inactive ingredients consist of: lactose monohydrate, microcrystalline cellulose, D-mannitol, sodium starch glycolate, povidone, N-C Wild Berry Type Flavor, magnesium stearate, crospovidone, polyvinyl acetate, sucralose, colloidal silicone dioxide, sodium lauryl sulfate, D&C Red #30/Helendon Pink Aluminum Lake.

Patients should be advised that:

• Some people, particularly children, may experience difficulties swallowing the Albenza tablets whole. Albenza chewable tablet is available for children and patients who may be unable to swallow a tablet.
• Take Albenza with food.
• Albenza may cause fetal harm, therefore, obtain a pregnancy test in women of reproductive potential prior to initiating therapy.
• Advise women of reproductive potential to use effective birth control while on Albenza and for one month after completing treatment.
• During Albenza therapy, monitor blood counts and liver enzymes every 2 weeks because of the possibility of harm to the liver or bone marrow.

Albenza and TILTAB are registered trademarks of GlaxoSmithKline, used with permission.

Distributed by:

Amedra Pharmaceuticals LLC
Horsham, PA 19044

LB# 799-04