Albendazole IP 400 mg Tablet

Monitor blood counts and liver function. Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required..

It is important to take iron every day while you are being treated for hookworm infection because it causes anemia.

Perform liver function tests and blood counts before and every 2 wk during high dose therapy of hydatid disease. It may cause bone marrow depression. It may cause dizziness.In young children, the tablets should be crushed or chewed and swallowed with glass of water.

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

Albendazole may cause side effects.Tell your doctor if any of these symptoms are severe or do not go away:

Stomach Pain

Nausea

Vomiting

Headache

Dizziness

Reversible hair loss

This is Preferred Dosage:
Dosing of Albendazole will vary, depending upon which of the following parasitic infections is being treated.

Disclaimer:To be taken only after consulting with the doctor.

Mechanism of Action

Vermicidal; albendazole causes degenerative alterations in the tegument and intestinal cells of the worm by binding to the colchicine-sensitive site of tubulin, thus inhibiting its polymerization or assembly into microtubules. The loss of the cytoplasmic microtubules leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores. Degenerative changes in the endoplasmic reticulum, the mitochondria of the germinal layer, and the subsequent release of lysosomes result in decreased production of adenosine triphosphate (ATP), which is the energy required for the survival of the helminth. Due to diminished energy production, the parasite is immobilized and eventually dies.

Absorption and Metabolism: Albendazole is poorly absorbed from the gastrointestinal tract due to its low aqueous solubility. Albendazole concentrations are negligible or undetectable in plasma as it is rapidly converted to the sulfoxide metabolite prior to reaching the systemic circulation. The systemic anthelmintic activity has been attributed to the primary metabolite, albendazole sulfoxide. Oral bioavailability appears to be enhanced when albendazole is coadministered with a fatty meal (estimated fat content 40 g) as evidenced by higher (up to 5-fold on average) plasma concentrations of albendazole sulfoxide as compared to the fasted state.
Maximal plasma concentrations of albendazole sulfoxide are typically achieved 2 to 5 hours after dosing and are on average 1.31 mcg/mL (range 0.46 to 1.58 mcg/mL) following oral doses of albendazole (400 mg) in 6 hydatid disease patients, when administered with a fatty meal. Plasma concentrations of albendazole sulfoxide increase in a dose-proportional manner over the therapeutic dose range following ingestion of a fatty meal (fat content 43.1 g). The mean apparent terminal elimination half-life of albendazole sulfoxide typically ranges from 8 to 12 hours in 25 normal subjects, as well as in 14 hydatid and 8 neurocysticercosis patients. Following 4 weeks of treatment with albendazole (200 mg three times daily), 12 patients‚ plasma concentrations of albendazole sulfoxide were approximately 20% lower than those observed during the first half of the treatment period, suggesting that albendazole may induce its own metabolism.

Distribution: Albendazole sulfoxide is 70% bound to plasma protein and is widely distributed throughout the body; it has been detected in urine, bile, liver, cyst wall, cyst fluid, and cerebral spinal fluid (CSF). Concentrations in plasma were 3- to 10-fold and 2- to 4-fold higher than those simultaneously determined in cyst fluid and CSF, respectively.

Metabolism and Excretion: Albendazole is rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine. Following oral administration, albendazole has not been detected in human urine. Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine. Biliary elimination presumably accounts for a portion of the elimination as evidenced by biliary concentrations of albendazole sulfoxide similar to those achieved in plasma.

The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance:
• Cimetidine (albendazole sulfoxide concentrations are increased in patients treated with cimetidine; increased concentrations are observed in bile and cystic fluid.
• Corticosteroids (concurrent use with albendazole increases steady-state trough concentrations of albendazole sulfoxide
• Praziquantel (concurrent use with albendazole increases mean plasma concentration and area under the plasma concentration–time curve of albendazole sulfoxide.
• Theophylline(albendazole induces cytochrome P450 1A in human hepatic cells; plasma concentrations of theophylline should be monitored during and after concurrent treatment with albendazole.

Patients should be advised that:
• Some people, particularly young children, may experience difficulties swallowing the tablets whole. In young children, the tablets should be crushed or chewed and swallowed with a drink of water.
• Albendazole may cause fetal harm, therefore, women of childbearing age should begin treatment after a negative pregnancy test.
• Women of childbearing age should be cautioned against becomingpregnant while on albendazole or within 1 month of completing treatment.
• During albendazole therapy, because of the possibility of harm to theliver or bone marrow, routine (every 2 weeks) monitoring of blood counts and liver function tests should take place.
• Albendazole should be taken with food.

Albendazole) is an orally administered broad-spectrum anthelmintic. 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 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.