Varenicline

Information about Varenicline

Varenicline is a partial agonist of the nicotinic acetylcholine receptor and is used to help in smoking cessation.

Liver safety of Varenicline

Varenicline has been associated with a low rate of serum enzyme elevations during therapy, and since approval and its wide scale use, with rare instances of clinically apparent mild liver injury.

Mechanism of action of Varenicline

Varenicline (var en' i kleen) is a partial agonist of the α4 β2 nicotinic acetylcholine receptor and appears to act by blocking the binding of nicotine to this receptor while providing partial agonist effect thus relieving nicotine craving. Use of varenicline in a program to stop smoking has been shown to increase the rate of smoking cessation and to decrease relapse.

FDA approval information for Varenicline

Varenicline was approved for use in the United States in 2006 and is widely used in smoking cessation programs.

Dosage and administration for Varenicline

Varenicline is available in tablets of 0.5 and 1 mg under the brand name Chantix. The usually recommended regimen is to start with 0.5 mg once daily and increase to a maintenance dose of 1 mg twice daily, continuing therapy for at least 12 weeks after smoking cessation.

Side effects of Varenicline

Common side effects include nausea, vivid dreams, insomnia, anxiety, depression, dizziness, drowsiness, headache, dry mouth, and change in appetite, some of the symptoms being those of nicotine withdrawal. Varenicline has been reported to cause hypersensitivity reactions including Stevens Johnson syndrome.

Substance abuse treatment agents

• Acamprosate, Buprenorphine, Disulfiram, Methadone, Nalmefene, Naloxegol, Naloxone, Naltrexone, Nicotine, Varenicline.

• Dailymed label info on Varenicline
• FDA Varenicline