R06AE05 - Meclozine |
Possibly porphyrinogenic |
PSP |
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.
Similar drugs
References
| # | Citation details | PubMed ID |
|---|---|---|
| 1. | Guidelines for drug prescription in patients with the acute porphyrias.
Disler PB, Blekkenhorst GH, et al. S Afr Med J. 1982 May; 61(18):656-60.
|
6123155 |
| 2. | Porphyria and the dangerous life-threatening drugs.
Eales L. S Afr Med J. 1979 Nov; 56(22):914-7.
|
515871 |
| 3. | Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor.
Lau AJ, Yang G, et al. J Pharmacol Exp Ther. 2011 Mar; 336(3):816-26.
|
21131266 |
| 4. | Drugs in the acute porphyrias--toxicogenetic diseases.
Moore MR, Hift RJ. Cell Mol Biol (Noisy-le-grand). 1997 Feb; 43(1):89-94.
|
9074793 |
| 5. | International review of drugs in acute porphyria--1980.
Moore MR. Int J Biochem. 1980; 12(5-6):1089-97.
|
7004930 |
| 6. | Meclizine metabolism and pharmacokinetics: formulation on its absorption.
Wang Z, Lee B, et al. J Clin Pharmacol. 2012 Sep; 52(9):1343-9.
|
21903894 |
| Summary of Product Characteristics | ||
| 7. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Meklozin.
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Tradenames
Suprimal 
Agyrax · Postafene 
Agyrax 
Chiclida · Navicalm 
Sea-Legs · Traveleeze Soft & Chewy 
Postafen 
Postafen 
Postafen 
Vermec · Vertinon 
Meclozine · Sea-legs · Travel · Travel Ease · Travel Legs · Travel Well 
Agyrax · Postafene 
Postafen 
Postafen 
Meclizine