Monograph

N07BA03 - Varenicline

Propably not porphyrinogenic

Rationale

Probably insignificant hepatocyte load. Only limited metabolism, no induction or inhibition of CYP 3A4 or 2C9. No clinical reports available on use in acute porphyria.

Chemical description

7,8,9,10-tetrahydro-6,10-methano-6 H -pyrazino[2,3-h][3]benzazepine. Highly soluble in water.

Therapeutic characteristics

Partial agonist selective for alpha 4 beta 2 nicotinic acetylcholine receptor subtypes. Varenicline binds with high affinity and selectivity at alpha 4 beta 2 neuronal nicotinic acetylcholine receptors. Common adverse reactions that can be confused with acute porphyria are insomnia, gastrointestinal disturbances (for example nausea, obstipation, diarrhoea etc), tiredness.

Hepatic exposure

Probably insignificant hepatic exposure (Obach RS 2006).

Metabolism and pharmacokinetics

Less than 10 % is metabolized, by glucuronidation and oxidation. Details on pathway for metabolism is not known. Elimination half life is approximately 24 hours. CYP 2C9 and 3A4 is not inhibited by varenicline. CYP 3A4 is not induced by varenicline. CYP 2C9 is probably not induced as the pharmacokinetics of the substrate warfarin is not affected by concomitant varenicline treatment (Burstein AH 2007).

Published experience

No reports of clinical experience are located.

References

#	Citation details	PMID
*	Scientific articles
1.	Lack of pharmacokinetic and pharmacodynamic interactions between a smoking cessation therapy, varenicline, and warfarin: an in vivo and in vitro study. J Clin Pharmacol 2007;47(11):1421-9. Burstein AH, Clark DJ et al.
2.	Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos 2006;34(1):121-30. Obach RS, Reed-Hagen AE et al.	16221753

Citation details

PMID

Scientific articles

Lack of pharmacokinetic and pharmacodynamic interactions between a smoking cessation therapy, varenicline, and warfarin: an in vivo and in vitro study. J Clin Pharmacol 2007;47(11):1421-9.

Burstein AH, Clark DJ et al.

Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos 2006;34(1):121-30.

Obach RS, Reed-Hagen AE et al.

16221753

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Tradenames and packages

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Netherlands

Byteqi · Byteqi 0,5 mg + 1 mg filmomhulde tabletten · Byteqi 0,5 mg filmomhulde tabletten · Byteqi 1 mg filmomhulde tabletten · Champix · Champix 0,5 mg + 1 mg, filmomhulde tabletten · Champix 0,5 mg, filmomhulde tabletten · Champix 1 mg, filmomhulde tabletten · Cuitvar · Cuitvar 0,5 mg + 1 mg, filmomhulde tabletten · Cuitvar 0,5 mg, filmomhulde tabletten · Cuitvar 1 mg, filmomhulde tabletten · Varenicline · Varenicline axunio 0,5 mg + 1 mg filmomhulde tabletten · Varenicline axunio 0,5 mg filmomhulde tabletten · Varenicline axunio 1 mg filmomhulde tabletten · Varenicline Teva 0,5 mg + 1 mg, filmomhulde tabletten · Varenicline Teva 0,5 mg, filmomhulde tabletten · Varenicline Teva 1 mg, filmomhulde tabletten

Belgium

Champix · Champix 0.5 mg - 1 mg compr. pellic. · Champix 0.5 mg compr. pellic. · Champix 1 mg compr. pellic. · Varenicline · Varenicline Teva 0.5 mg - 1 mg compr. pellic. · Varenicline Teva 0.5 mg compr. pellic. · Varenicline Teva 1 mg compr. pellic.

United Kingdom

Champix · Champix 0.5mg tablets · Champix 0.5mg/1mg 2 week treatment initiation pack · Champix 0.5mg/1mg 4 week treatment initiation pack · Champix 1mg tablets · Varenicline · Varenicline 1mg tablets · Varenicline 1mg tablets and Varenicline 500microgram tablets · Varenicline 500microgram tablets

Denmark