Mebendazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Mebendazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ Mebendazole is a (synthetic) broad-spectrum anthelmintic. The principal mode of action for albendazole is by its inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules.
Mebendazole¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 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).
Absorption
Mebendazole¿¡ ´ëÇÑ Absorption Á¤º¸ Poorly absorbed (approximately 5 to 10%) from gastrointestinal tract. Fatty food increases absorption.
Pharmacokinetics
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Èí¼ö : 2-10%
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Biotransformation
Mebendazole¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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.
Toxicity
Mebendazole¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
Drug Interactions
Mebendazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Ethotoin The hydantoin decreases the efficiency of mebendazoleFosphenytoin The hydantoin decreases the efficiency of mebendazoleMephenytoin The hydantoin decreases the efficiency of mebendazolePhenytoin The hydantoin decreases the efficiency of mebendazole
Mebendazole¿¡ ´ëÇÑ Description Á¤º¸ A benzimidazole that acts by interfering with carbohydrate metabolism and inhibiting polymerization of microtubules. [PubChem]
The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. MEBENDAZOLE [GGT Increase] [Composite Activity] (Score) NA (Marginal) 0 (Active) 0
[Alkaline Phosphatase Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
[SGOT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
[SGPT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
[LDH Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA
[GGT Increase] (Activity Score) NA (Number of Rpts) NA (Index value) NA