Champix - General Information
Champix is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.
Pharmacology of Champix
Champix is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain.
Champix for patients
- Patients should be instructed to set a date to quit smoking and to initiate CHANTIX treatment one week before the quit date.
- Patients should be advised that CHANTIX should be taken after eating, and with a full glass of water.
- Patients should be instructed how to titrate CHANTIX, beginning at a dose of 0.5 mg/day. Prescribers should explain that one 0.5 mg tablet should be taken daily for the first three days, and that for the next four days, one 0.5 mg tablet should be taken in the morning and one 0.5 mg tablet should be taken in the evening.
- Patients should be advised that, after the first seven days, the dose should be increased to one 1 mg tablet in the morning and one 1 mg tablet in the evening.
- Patients should be encouraged to continue to attempt to quit if they have early lapses after quit day.
- Patients should be informed that nausea and insomnia are side effects of CHANTIX and are usually transient; however, patients should be advised that if they are persistently troubled by these symptoms, they should notify the prescribing physician so that a dose reduction can be considered.
- Patients should also be provided with educational materials and necessary counseling to support an attempt at quitting smoking.
- Patients should be informed that some medications may require dose adjustment after quitting smoking,
- Patients intending to become pregnant or planning to breast-feed an infant should be advised of the risks of smoking and risks and benefits of smoking cessation with CHANTIX.
No clinically meaningful pharmacokinetic drug-drug interactions have been identified.
Additional information about Champix
Champix Indication: For use as an aid in smoking cessation.
Mechanism Of Action: Champix is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor agonist. The drug shows high selectiviyty for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Varenicline
Synonyms: Not Available
Drug Category: Nicotinic Agonists
Drug Type: Small Molecule; Approved
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Less than 20%.
Biotransformation: Metabolism is limited (<10%). Most of the active compound is excreted renally (81%). A small proportion is glucuronidated, oxidated, N-formylated or conjugated to a hexose.
Half Life: The elimination half-life of varenicline is approximately 24 hours
Dosage Forms of Champix: Tablet, film coated Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C13H13N3
Varenicline on Wikipedia: https://en.wikipedia.org/wiki/Varenicline
Organisms Affected: Humans and other mammals