Monograph

R06AE05 - Meclozine

Possibly porphyrinogenic

Rationale

Only scanty information is obtainable concerning the metabolism and pharmacokinetics of meclozine, and induction of CYP3A4 cannot be ruled out.

Chemical description

Meclozine is also known as meclizine.

Therapeutic characteristics

Meclozine is used in the prevention of motion sickness and for the treatment of post-operative vomiting and nausea after radiation therapy.

Metabolism and pharmacokinetics

Meclozine is metabolized via N-oxidation, oxidative N-dealkylation, methyl oxidation, aromatic hydroxylation, O-methylation and glucuron- and taurin conjugation (SPC). In vitro data indicates that meclozine is metabolized primarily by CYP2D6 (Wang 2012) and that it is an agonist of human pregnane X receptor (Lau 2011). Elimination half-life is 6 hours. Interaction studies with meclozine have not been executed (SPC).

Published experience

Meclozine is listed as a safe drug for patients with acute porphyria (Eales 1979, Moore 1980, Disler 1982, Moore 1997).

IPNet drug reports

Uneventful use reported in 4 patients with acute porphyria.

References

#	Citation details	PMID
*	Scientific articles
1.	Disler, P. B., G. H. Blekkenhorst, et al. (1982). Guidelines for drug prescription in patients with the acute porphyrias. S Afr Med J 61(18): 656-660.
2.	Eales, L. (1979). Porphyria and the dangerous life-threatening drugs. S Afr Med J 56(22): 914-917.
3.	Lau, A. J., G. Yang, et al. (2011). Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor. J Pharmacol Exp Ther 336(3): 816-826.
4.	Moore, M. R. (1980). International review of drugs in acute porphyria--1980. Int J Biochem 12(5-6): 1089-1097.	7004930
5.	Moore, M. R. and R. J. Hift (1997). Drugs in the acute porphyrias--toxicogenetic diseases. Cell Mol Biol (Noisy-le-grand) 43(1): 89-94.
6.	Wang, Z., B. Lee, et al. (2012). Meclizine metabolism and pharmacokinetics: formulation on its absorption. J Clin Pharmacol 52(9): 1343-1349.
*	Summary of Product Characteristics
7.	Norwegian medicines agency. Summary of Product Characteristics (SPC). Meklozin.

Citation details

PMID

Scientific articles

Disler, P. B., G. H. Blekkenhorst, et al. (1982). Guidelines for drug prescription in patients with the acute porphyrias. S Afr Med J 61(18): 656-660.

Eales, L. (1979). Porphyria and the dangerous life-threatening drugs. S Afr Med J 56(22): 914-917.

Lau, A. J., G. Yang, et al. (2011). Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor. J Pharmacol Exp Ther 336(3): 816-826.

Moore, M. R. (1980). International review of drugs in acute porphyria--1980. Int J Biochem 12(5-6): 1089-1097.

7004930

Moore, M. R. and R. J. Hift (1997). Drugs in the acute porphyrias--toxicogenetic diseases. Cell Mol Biol (Noisy-le-grand) 43(1): 89-94.

Wang, Z., B. Lee, et al. (2012). Meclizine metabolism and pharmacokinetics: formulation on its absorption. J Clin Pharmacol 52(9): 1343-1349.

Summary of Product Characteristics

Norwegian medicines agency. Summary of Product Characteristics (SPC). Meklozin.

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