Informational only — Not medical advice. Always consult a licensed healthcare provider.

Community data Updated 23 hours ago

Indications

Varenicline Tartrate is a nicotinic receptor partial agonist. Doctors prescribe it as an aid to smoking cessation treatment.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Varenicline binds with high affinity and selectivity to α4β2 neuronal nicotinic acetylcholine receptors. Its effect in helping people stop smoking is believed to come from its action at the α4β2 sub-type of the nicotinic receptor. There it produces agonist activity, and at the same time it stops nicotine from binding to these receptors.

In vitro electrophysiology studies and in vivo neurochemical studies have shown that varenicline binds to α4β2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, but at a much lower level than nicotine does. Varenicline also blocks nicotine from activating the α4β2 receptors, so it blocks the stimulation of the central nervous mesolimbic dopamine system. This system is believed to be the neuronal mechanism behind the reinforcement and reward a person feels when smoking.

Varenicline is highly selective. It binds more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold for α3β4, >3,500-fold for α7, >20,000-fold for α1βγδ) or to non-nicotinic receptors and transporters (>2,000-fold). It also binds with moderate affinity (Ki = 350 nM) to the 5-HT3 receptor.

Pregnancy & Breastfeeding

The data we have so far don't show a higher risk of major birth defects when women take varenicline during pregnancy, compared with women who smoke. Smoking in pregnancy carries its own risks for the mother, the baby before birth and the newborn.

For breastfeeding, nobody knows yet whether varenicline passes into human milk, what it might do to a breastfed infant, or whether it affects milk production. In animal studies, varenicline was found in the milk of lactating rats.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: Start Varenicline one week before the date the patient has set for stopping smoking. The other way is to start Varenicline first and let the patient quit smoking between days 8 and 35 of treatment. In the starting week, the dose is 0.5 mg once daily on days 1 to 3, then 0.5 mg twice daily on days 4 to 7. In the continuing weeks, the dose is 1 mg twice daily, for a total of 12 weeks. For people who manage to quit, another 12 weeks of treatment is recommended to increase the likelihood of long-term abstinence. Some patients are sure they can't or won't quit all at once. For them, consider a gradual approach with Varenicline. The patient starts the medicine and cuts smoking by 50% from baseline within the first four weeks, then by another 50% over the next four weeks. After that they keep reducing, with the goal of complete abstinence by 12 weeks. Treatment then continues for another 12 weeks, making 24 weeks in all. Severe renal impairment (estimated creatinine clearance less than 30 mL/min): begin with 0.5 mg once daily and titrate to 0.5 mg twice daily. For patients with end-stage renal disease on hemodialysis, a maximum of 0.5 mg daily may be given if tolerated. Consider a lower dose for patients who can't tolerate the adverse effects. If a patient fails to stop smoking or relapses, another attempt at treatment is recommended once the factors behind the failed attempt have been addressed. Provide patients with suitable educational materials and counseling to support the quit attempt. Pediatric use: Varenicline is not recommended for patients 16 years of age or younger, because its efficacy in this group was not demonstrated.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.