Albendazole

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ALBENDAZOLE

Albendazole 1

1.       TYPE OF DRUG – ALBENDAZOLE
Albendazole is an anthelmintic. It works by killing sensitive parasites.

 

2.       INDICATIONS (USE) – ALBENDAZOLE
This medication is an anthelmintic, prescribed for tapeworm infections, hydatid cyst disease, cysticercosis or neurocysticercosis, capillariasis, cutaneous larva migrans, giardiasis, microsporidiosis including Septata intestinalis infection, intestinal parasites in immigrants, strongyloidiasis, trichinosis, trichostrongyliasis. It works by killing sensitive parasites.

 

3.       MECHANISM OF ACTION (MOA) – ALBENDAZOLE
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.

 

4.       ROUTES OF ADMINISTRATION- ALBENDAZOLE
Tablet: 200 mg

Chewable Tablet: 200 mg

 

5.       ONSET OF EFFECT OR ACTION- ALBENDAZOLE
Within 2-4 hrs.

 

6.      DOSAGE (DOSING INFORMATION) – ALBENDAZOLE
Adults < 60 kg: 15 mg/kg/day (not to exceed 800 mg/day) given in two divided doses for 28 days followed by a 14-day drug-free period. Repeat as above.

Children >= 6 years: 15 mg/kg/day given in two divided doses for 28 days, followed by a 14-day drug-free period. Repeat as above.

 

7.       HALF LIFE (DURATION OF ACTION) – ALBENDAZOLE
Terminal elimination half-life ranges from 8 to 12 hours (single dose, 400mg).

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – ALBENDAZOLE
CNS Headache (11%); raised intracranial pressure (2%); dizziness/vertigo, meningeal signs (1%). Dermatologic Reversible alopecia (2%); erythema multiforme, hypersensitivity including rash and urticaria (less than 1%); Stevens-Johnson syndrome (postmarketing). GI Abdominal pain, nausea/vomiting (6%). Genitourinary Acute renal failure (postmarketing). Hepatic Abnormal LFTs (16%); hepatitis (postmarketing). Hematologic-Lymphatic Leukopenia (less than 1%); agranulocytosis, granulocytopenia, pancytopenia, thrombocytopenia (rare); aplastic anemia (postmarketing). Miscellaneous Fever (1%).

 

9.       CONTRAINDICATIONS – ALBENDAZOLE
Contraindicated in pregnant and breastfeeding women, neonates, patients with known hypersensitivity, and liver impairment.

 

10.   DRUG INTERACTIONS – ALBENDAZOLE
Cimetidine In hydatid cyst patients, albendazole sulfoxide concentrations in bile and cystic fluid may be increased about 2-fold; however, plasma levels are unchanged 4 h after dosing. Dexamethasone Albendazole C trough at steady state was about 56% higher when coadministered with dexamethasone 8 mg. Praziquantel Albendazole sulfoxide C max may be elevated about 50%, increasing the risk of adverse reactions. Theophylline Although theophylline pharmacokinetics are unchanged by albendazole, monitor plasma concentrations during and after albendazole treatment.

 

11.     EXCRETION- ALBENDAZOLE
Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine.

 

Albendazole 2

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