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

Albendazole is a white to off-white powder. It is soluble in dimethylsulfoxide, strong acids, and strong bases. It is slightly soluble in methanol, chloroform, ethyl acetate, and acetonitrile. Albendazole is practically insoluble in water. Each white to off-white, film-coated tablet 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.

The principal mode of action for albendazole is by its inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules.

In the specified treatment indications albendazole appears to be active against the larval forms of the following organisms:

Echinococcus granulosus
Taenia solium

Albenza (Albendazole) is indicated for the treatment of the following infections:

Albenza (Albendazole) is indicated for the treatment of parenchymal neurocysticercosis due to active lesions caused by larval forms of the pork tapeworm, .

Lesions considered responsive to albendazole therapy appear as nonenhancing cysts with no surrounding edema on contrast-enhanced computerized tomography. Clinical studies in patients with lesions of this type demonstrate a 74% to 88% reduction in number of cysts; 40% to 70% of albendazole-treated patients showed resolution of all active cysts.

Albenza (Albendazole) is indicated for the treatment of cystic hydatid disease of the liver, lung, and peritoneum, caused by the larval form of the dog tapeworm, .

This indication is based on combined clinical studies which demonstrated non-infectious cyst contents in approximately 80-90% of patients given Albenza (Albendazole) for 3 cycles of therapy of 28 days each (see DOSAGE AND ADMINISTRATION). Clinical cure (disappearance of cysts) was seen in approximately 30% of these patients, and improvement (reduction in cyst diameter of ≥25%) was seen in an additional 40%.

NOTE: When medically feasible, surgery is considered the treatment of choice for hydatid disease. When administering Albenza (Albendazole) in the pre- or post-surgical setting, optimal killing of cyst contents is achieved when 3 courses of therapy have been given.

NOTE: The efficacy of albendazole in the therapy of alveolar hydatid disease caused by has not been clearly demonstrated in clinical studies.

Albenza (Albendazole) is contraindicated in patients with known hypersensitivity to the benzimidazole class of compounds or any components of Albenza (Albendazole) .

Rare fatalities associated with the use of Albenza (Albendazole) have been reported due to granulocytopenia or pancytopenia (see PRECAUTIONS). Albendazole has been shown to cause bone marrow suppression, aplastic anemia, and agranulocytosis in patients with and without underlying hepatic dysfunction. Blood counts should be monitored at the beginning of each 28-day cycle of therapy, and every 2 weeks while on therapy with albendazole in all patients. Patients with liver disease, including hepatic echinococcosis, appear to be more at risk for bone marrow suppression leading to pancytopenia, aplastic anemia, agranulocytosis, and leukopenia attributable to albendazole and warrant closer monitoring of blood counts. Albendazole should be discontinued in all patients if clinically significant decreases in blood cell counts occur.

Albendazole should not be used in pregnant women except in clinical circumstances where no alternative management is appropriate. Patients should not become pregnant for at least 1 month following cessation of albendazole therapy. If a patient becomes pregnant while taking this drug, albendazole should be discontinued immediately. If pregnancy occurs while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required. Oral or intravenous corticosteroids should be considered to prevent cerebral hypertensive episodes during the first week of anticysticeral therapy.

Pre-existing neurocysticercosis may also be uncovered in patients treated with albendazole for other conditions. Patients may experience 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. Symptoms may occur soon after treatment; appropriate steroid and anticonvulsant therapy should be started immediately.

Cysticercosis may, in rare cases, involve the retina. Before initiating therapy for neurocysticercosis, the patient should be examined for the presence of retinal lesions. If such lesions are visualized, the need for anticysticeral therapy should be weighed against the possibility of retinal damage caused by albendazole-induced changes to the retinal lesion.

Long-term carcinogenicity studies were conducted in mice and rats. In the mouse study, albendazole was administered in the diet at doses of 25, 100, and 400 mg/kg/day (0.1, 0.5, and 2 times the recommended human dose based on body surface area in mg/m, respectively) for 108 weeks. In the rat study, albendazole was administered in the diet at doses of 3.5, 7, and 20 mg/kg/day (0.04, 0.08, and 0.21 times the recommended human dose based on body surface area in mg/m, respectively) for 117 weeks. There was no evidence of increased incidence of tumors in the treated mice and rats when compared to the control group.

In genotoxicity tests, albendazole was found negative in an Ames Salmonella/Microsome Plate mutation assay with and without metabolic activation or with and without pre-incubation, cell-mediated Chinese Hamster Ovary chromosomal aberration test and in vivo mouse micronucleus test. In the in vitro BALB/3T3 cells transformation assay, albendazole produced weak activity in the presence of metabolic activation while no activity was found in the absence of metabolic activation.

Albendazole did not adversely affect male or female fertility in the rat at an oral dose of 30 mg/kg/day (0.32 times the recommended human dose based on body surface area in mg/m).

The adverse event profile of albendazole differs between hydatid disease and neurocysticercosis. Adverse events occurring with a frequency of ≥1% in either disease are described in the table below.

These symptoms were usually mild and resolved without treatment. Treatment discontinuations were predominantly due to leukopenia (0.7%) or hepatic abnormalities (3.8% in hydatid disease). The following incidence reflects events that were reported by investigators to be at least possibly or probably related to albendazole.

The following adverse events were observed at an incidence of

Significant toxicity and mortality were shown in male and female mice at doses exceeding 5,000 mg/kg; in rats, at estimated doses between 1,300 and 2,400 mg/kg; in hamsters, at doses exceeding 10,000 mg/kg; and in rabbits, at estimated doses between 500 and 1,250 mg/kg. In the animals, symptoms were demonstrated in a dose-response relationship and included diarrhea, vomiting, tachycardia, and respiratory distress.

One overdosage has been reported with Albenza (Albendazole) in a patient who took at least 16 grams over 12 hours. No untoward effects were reported. In case of overdosage, symptomatic therapy and general supportive measures are recommended.

Dosing of Albenza (Albendazole) will vary, depending upon which of the following parasitic infections is being treated. In young children, the tablets should be crushed or chewed and swallowed with a drink of water.

Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required. Oral or intravenous corticosteroids should be considered to prevent cerebral hypertensive episodes during the first week of treatment.

Albenza (Albendazole) is supplied as 200 mg, white to off-white, circular, biconvex, bevel-edged, film-coated TILTAB tablets in bottles of 112.

NDC 0007-5500-40 Bottles of 112

Store between 20° and 25°C (68° and 77°F).

Albenza (Albendazole) and TILTAB are registered trademarks of GlaxoSmithKline.

GlaxoSmithKline

Research Triangle Park, NC 27709

©2009, GlaxoSmithKline. All rights reserved.

June 2009                    ALB:8PI

Each Tiltab tablet contains albendazole, 200mg.

GlaxoSmithKline

RTP, NC 27709

Made in Mexico

A070370

Rev. 6/09