Monograph
N07BA03 - Varenicline |
Propably not porphyrinogenic |
PNP |
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.
Similar drugs
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 |
Tradenames
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Byteqi 0,5 mg + 1 mg filmomhulde tabletten · Byteqi 0,5 mg filmomhulde tabletten · Byteqi 1 mg filmomhulde tabletten · Champix 0,5 mg + 1 mg, filmomhulde tabletten · Champix 0,5 mg, filmomhulde tabletten · Champix 1 mg, filmomhulde tabletten · Cuitvar 0,5 mg + 1 mg, filmomhulde tabletten · Cuitvar 0,5 mg, filmomhulde tabletten · Cuitvar 1 mg, filmomhulde tabletten · Varenicline axunio 0,5 mg + 1 mg filmomhulde tabletten · Varenicline axunio 0,5 mg filmomhulde tabletten · Varenicline axunio 1 mg filmomhulde tabletten · Varenicline CF 0,5 mg + 1 mg, filmomhulde tabletten · Varenicline CF 0,5 mg, filmomhulde tabletten · Varenicline CF 1 mg, filmomhulde tabletten · Varenicline Faye 0,5 mg + 1 mg tabletten · Varenicline Faye 0,5 mg tabletten · Varenicline Faye 1 mg tabletten · Varenicline Glenmark 0,5 mg filmomhulde tabletten · Varenicline Glenmark 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 
Champix 0.5 mg - 1 mg compr. pellic. · Champix 0.5 mg compr. pellic. · Champix 1 mg compr. pellic. · Varenicline Teva 0.5 mg - 1 mg compr. pellic. · Varenicline Teva 0.5 mg compr. pellic. · Varenicline Teva 1 mg compr. pellic. 
Byteqi · Byteqi 0,5 mg Comprimidos Recubiertos con Pelicula efg · CHAMPIX 0,5 mg 1mg comprimidos recubiertos con pelicula · CHAMPIX 0,5 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · CHAMPIX 0,5 mg y 1 mg comprimidos recubiertos con pelicula · CHAMPIX 0,5, 1 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · CHAMPIX 0,5mg 1mg comprimidos recubiertos con pelicula · CHAMPIX 1 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · CHAMPIX 1mg comprimidos recubiertos con pelicula · Cuitvar 0,5 mg + 1 mg Comprimidos Recubiertos con Pelicula efg · Cuitvar 0,5 mg Comprimidos Recubiertos con Pelicula efg · Cuitvar 1 mg Comprimidos Recubiertos con Pelicula efg · Vareniclina · Vareniclina Kern Pharma 0,5 mg + 1 mg Comprimidos Recubiertos con Pelicula efg · Vareniclina Kern Pharma 1 mg Comprimidos Recubiertos con Pelicula efg · Vareniclina Normon 0,5 mg Comprimidos Recubiertos con pel?Cula efg · Vareniclina Normon 1 mg Comprimidos Recubiertos con pel?Cula efg · Vareniclina Teva 0,5 mg +1 mg Comprimidos Recubiertos con Pelicula efg · Vareniclina Teva 0,5 mg Comprimidos Recubiertos con Pelicula efg · Vareniclina Teva 1 mg Comprimidos Recubiertos con Pelicula efg 
Champix 
CHAMPIX 0,5mg+1mg · CHAMPIX 1mg 
Champix · Varenicline 
Champix · Champix Startpakke · Civarenix · Civarenix Startpakke · Vareniclin Axunio · Vareniclin Axunio Startpakke · Vareniclin Stada · Vareniclin Stada Startpakke · Varenicline Zentiva · Varenicline Zentiva Startpakke 
Apo-varenicline · Champix · Varenicline apotex · Varenicline Zentiva · Vareniklin axunio 
Champix 
Champix · Vareniclin · Vareniclin-ratiopharm 
Champix · Vareniclin Normon · Varenicline Newbury · Varenicline Teva 
Champix · Varenicline Glenmark · Varenicline ratiopharm 
Champix
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