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Varenicline | Chantix is a used to treat nicotine addiction. It both reduces craving for and decreases the pleasurable effects of cigarettes and other tobacco products.
Therapeutic Class
Drugs used in substance dependence
Pharmacology
Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors.
The efficacy of Varenicline in smoking cessation is believed to be the result of varenicline’s activity at α4β2 sub-type of the nicotinic receptor where its binding produces agonist activity, while simultaneously preventing nicotine binding to these receptors.
Electrophysiology studies in vitro and neurochemical studies in vivo have shown that varenicline binds to α4β2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, lower level than nicotine. buy chantix (Varenicline) online
Varenicline blocks the ability of nicotine to activate α4β2 receptors and thus to stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
Varenicline is highly selective and binds more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500fold α7, >20,000-fold α1βγδ), or to non-nicotinic (> 2,000-fold). with moderate affinity (Ki = 350 NM) to the 5-HT3 receptor.
Dosage
Smoking cessation therapies are more likely to succeed for patients who are motivated to stop smoking and who are provided additional advice and support. Provide patients with appropriate educational materials and counseling to support the quit attempt.
The patient should set a date to stop smoking. Begin Varenicline dosing one week before this date. Alternatively, the patient can begin Varenicline dosing and then quit smoking between days 8 and 35 of treatment.
The recommended dose of Varenicline is 1 mg twice daily following a 1-week titration as follows:
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Days 1-3: 0.5 mg once daily
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Days 4-7: 0.5 mg twice daily
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Day 8-end of treatment: 1 mg twice daily