Varenicline: A Medication to Help Quit Smoking
Varenicline is a nicotine receptor partial agonist used to help people stop smoking. It works by stimulating nicotine receptors in the brain while also blocking nicotine from activating these receptors, reducing withdrawal symptoms and the pleasure of smoking.
Mechanism of Action
Varenicline binds to the α4β2 nicotinic acetylcholine receptors in the brain, stimulating a partial release of dopamine, which helps alleviate withdrawal symptoms while also preventing nicotine from exerting its pleasurable effects.
Indications
● Smoking Cessation: Generally used in chronic smokers who are to quit smoking by reducing cravings and withdrawal symptoms.
Dosage and Administration
● Adults: It is generally started with 0.5 mg once daily for the first 3 days, then increased to 0.5 mg twice daily for 4 days. Finally, 1 mg twice daily for the remainder of the 12-week treatment period.
● Pediatric dose: Safety and efficacy has not been established in infants and children.
Side Effects
● Common: Nausea, headache, sleep disturbances, and vivid dreams.
● Serious: Suicidal thoughts, depression, and cardiovascular events.
Pregnancy Category: Category C – Use during pregnancy only if the benefits outweigh the risks.
Common Brands
● Champix