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.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.