Varenicline
- Atc Codes:N07BA03
- CAS Codes:375815-87-5#249296-44-4
- PHARMGKB ID:375815-87-5#249296-44-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Champix; Belgium: Champix; Bulgaria: Champix; Czech Republic: Champix; Denmark: Champix; Estonia: Champix; Finland: Champix; France: Champix; Germany: Champix; Greece: Champix; Ireland: Champix; Italy: Champix; Latvia: Champix; Lithuania: Champix; Netherlands: Champix; Poland: Champix; Portugal: Champix; Romania: Champix; Slovakia: Champix; Spain: Champix; Sweden: Champix; UK: Champix.
North America
Canada: Chanpix; USA: Chantix.
Latin America
Argentina: Champix; Mexico: Champix.
Asia
Japan: Champix.
Drug combinations
Chemistry
Varenicline Tartrate: C~13~H~13~N~3~ C~4~H~6~O~6~. Mw: 361.35. (1) 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-, (2R,3R)-2,3-dihydroxybutanedioate (1:1); (2) 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine (2R,3R)-2,3-dihydroxybutanedioate. CAS-375815-87-5; CAS-249296-44-4 (varenicline)(2003).
Pharmacologic Category
Autonomic Drugs, Miscellaneous. Partial Nicotine Agonist. Smoking Cessation Aid. (ATC-Code: N07BA03).
Mechanism of action
Partial neuronal α~4~β~2~ nicotinic receptor agonist. Prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction. Also binds to 5-HT~3~ receptor with moderate affinity. Varenicline stimulates dopamine activity, resulting in decreased craving and withdrawal symptoms.
Therapeutic use
Treatment to aid in smoking cessation.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. There are no adequate, well-controlled studies in pregnant women. Use only if benefit outweighs potential risk to fetus. Not recommended in nursing women.
Unlabeled use
Contraindications
No significant contraindications known to date.
Warnings and precautions
Nausea may occur (dose-dependent). Neuropsychiatric symptoms, including suicidal thoughts and erratic/aggressive behavior, reported with use and following withdrawal. May cause sedation. Worsening of psychiatric illness reported (use with caution in pre-existing psychiatric illness (e.g. bipolar disorder, major severe depression, schizophrenia)). Use with caution in renal impairment. Increased adverse events when used concurrently with nicotine replacement therapy. Use in patients <18 years of age not recommended.