MEBENDAZOLE TABLET 100mg

Mebendazole

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

(5-benzoyl-1H-benzimidazol-2-yl)-carbamic acid methyl ester | MBDZ | Mebendazol | Mébendazole | Mebendazolum | Mebendazole |

Description

A benzimidazole that acts by interfering with carbohydrate metabolism and inhibiting polymerization of microtubules. [PubChem]

Indication

For the treatment of Enterobius vermicularis (pinworm), Trichuris trichiura (whipworm), Ascaris lumbricoides (common roundworm), Ancylostoma duodenale (common hookworm), Necator americanus (American hookworm) in single or mixed infections.

Mechanism of Action

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.

Pharmacodynamics

Mebendazole is a (synthetic) broad-spectrum anthelmintic. The principal mode of action for Mebendazole is by its inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules.

Pharmacokinetics

Absorption:

Poorly absorbed (approximately 5 to 10%) from gastrointestinal tract. Fatty food increases absorption.

Distribution:

Not Available

Metabolism:

Primarily hepatic. Primary metabolite is 2-amino-5-benzoylbenzimidazole, but also metabolized to inactive hydroxy and hydroxyamino metabolites. All metabolites are devoid of anthelmintic activity.

Elimination:

In man, approximately 2% of administered mebendazole is excreted in urine and the remainder in the feces as unchanged drug or a primary metabolite.

Half-life

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).

Clearance

Not Available

Toxicity

Acute oral toxicity (LD50): 620 mg/kg [Mouse]. Symptoms of overdose include elevated liver enzymes, headaches, hair loss, low levels of white blood cells (neutropenia), fever, and itching.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

MEBENDAZOLE TABLET 100mg was registered with Health Science Authority of Singapore by BEACONS PHARMACEUTICALS PTE LTD. It is marketed with the registration number of SIN00229P with effective from 1988-05-04.

This product contains 100mg of Mebendazole in the form of TABLET.

The medicine was manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE

It is a Pharmacy Only Medicine which can be obtained from a pharmacist at a retail pharmacy.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: P02CA01

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