Mebendazole

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MEBENDAZOLE

Mebendazole 1

1.       TYPE OF DRUG – MEBENDAZOLE
Mebendazole is a member of the benzimidazole class of antiparasitic agents, which also includes thiabendazole, albendazole, and triclabendazole.

 

2.       INDICATIONS (USE) – MEBENDAZOLE
Mebendazole is the drug of choice for the treatment of Trichuris trichuria (whipworm), Enterobius vermicularis (horse pinworm, pinworm), Ascaris lumbricoides (roundworm), as well as hookworm Ancylostoma duodenale and Necator americanus. For all these helminth mebendazole has success rates of at least 90 to 95%.

 

3.       MECHANISM OF ACTION (MOA) – MEBENDAZOLE
Mebendazole 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- MEBENDAZOLE
Tablet – Oral
5.       ONSET OF EFFECT OR ACTION- MEBENDAZOLE
Following administration of 100 mg twice daily for three consecutive days, plasma levels of mebendazole and its primary metabolite, the 2-amine, do not exceed 0.03 µg/mL and 0.09 µg/mL, respectively.
6.      DOSAGE (DOSING INFORMATION) – MEBENDAZOLE
Enterobiasis Adult: 100 mg as a single dose; may repeat if necessary 2-3 wk after initial treatment.

Child: >2 yr: 100 mg as a single dose; may repeat if necessary 2-3 wk after initial treatment. Hepatic impairment: Dose reduction may be required. Oral

Capillariasis  Adult: 200 mg bid for 20 days.

Child: >2 yr: 200 mg bid for 20 days. Hepatic impairment: Dose reduction may be required.

 

7.       HALF LIFE (DURATION OF ACTION) – MEBENDAZOLE
2.5 to 5.5 hours (range 2.5 to 9 hours) in patients with normal hepatic function. Approximately 35 hours in patients with impaired hepatic function (cholestasis).

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – MEBENDAZOLE
stomach/abdominal pain, vomiting, diarrhea, fever, headache, dizziness, or drowsiness.

 

9.       CONTRAINDICATIONS – MEBENDAZOLE
Hypersensitivity. Infants and children <2 yr

 

10.   DRUG INTERACTIONS – MEBENDAZOLE
Reduced plasma levels with enzyme inducers e.g. phenytoin, carbamazepine. Increased plasma levels with cimetidine.

 

11.     EXCRETION- MEBENDAZOLE
approximately 2% of administered mebendazole is excreted in urine and the remainder in the feces as unchanged drug or a primary metabolite.

 

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By Medifit Education

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