Monograph
P02CA01 - Mebendazole |
Propably not porphyrinogenic |
PNP |
Rationale
Mebendazole is a substrate of CYP 3A4. It is not suspected to induce or inhibit any CYP enzymes in vivo.
Chemical description
Benzimidazole.
Therapeutic characteristics
Mebendazole is used for the treatment of whipworm, pinworm, roundworm and hookworm in gastrointestinal infestations. It is administered orally. Abdominal pain is a common adverse reaction of mebendazole that may be confused with an acute porphyric attack.
Metabolism and pharmacokinetics
Mebendazole has a poor bioavailability due to low absorption of (between 5-22 per cent), and extensive first pass metabolism (Dayan 2003).
It is listed as a substrate of CYP 3A4 and as an inducer of CYP 1A1 (drugbank).
In an in vitro study mebendazole provoked a significant increase in CYP 1A1/2 protein expression and P4501A activity (Baliharova 2003).
The concurrent administration of mebendazole in 12 healty volunteers did not alter the disposition of theophylline, indicating that mebendazole does not induce CYP 1A significantly in vivo (Adebayo 1988).
Mebendazole is not listed as an inducer of other CYP enzymes besides CYP 1A (VelÃk 2004).
IPNet drug reports
Uneventful use reported in one patient with acute porphyria.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Baliharová V1, Skálová L et al. The effects of mebendazole on P4501A activity in rat hepatocytes and HepG2 cells. Comparison with tiabendazole and omeprazole.
J Pharm Pharmacol. 2003 Jun;55(6):773-81. |
|
| 2. | Theophylline disposition--effects of cimetidine, mebendazole and albendazole.
Adebayo GI, Mabadeje AF. Aliment Pharmacol Ther. 1988 Aug;2(4):341-6. |
2979257 |
| 3. | Albendazole, mebendazole and praziquantel. Review of non-clinical toxicity and pharmacokinetics.
Dayan AD. Acta Trop. 2003 May;86(2-3):141-59. |
12745134 |
| 4. | Benzimidazole drugs and modulation of biotransformation enzymes.
Velík J, Baliharová V, et al. Res Vet Sci. 2004 Apr;76(2):95-108. |
|
| * | Drug reference publications | |
| 5. | DrugBank. Mebendazole.
|
|
| * | Summary of Product Characteristics | |
| 6. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Vermox.
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