Description

Simple

A medication used for smoking cessation in nicotine addictions.

Clinical

A partial agonist at nicotinic acetylcholine receptors used as an aid in smoking cessation.

Overview

Varenicline 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.

On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced.

Pharmacology

Indication

For use as an aid in smoking cessation.

Pharmacodynamic

Varenicline is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain.

Mechanism of action

Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectivity 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 recepto... Read more

Absorption

Information currently not available.

Protein binding

Less than 20%.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

The elimination half-life of varenicline is approximately 24 hours

Route of elimination

Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2.

Toxicity

Information currently not available.

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 16-30%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 27.0%
  • Kind: placebo
    • Percent: 10.0%
  • Post Marketing
    Nausea US
  • Kind: experimental
    • Percent: 25.0%
  • Kind: placebo
    • Percent: 7.0%
  • Post Marketing
    Nausea US
  • Kind: experimental
    • Percent: 25.0%
  • Kind: placebo
    • Percent: 7.0%
  • Post Marketing
    Nausea US
  • Kind: experimental
    • Percent: 24.0%
  • Kind: placebo
    • Percent: 14.0%
  • Post Marketing
    Nausea US
  • Kind: experimental
    • Percent: 24.0%
  • Kind: placebo
    • Percent: 14.0%
  • Post Marketing
    Headache US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 19.0%
  • Post Marketing
    Headache US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 19.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 18-19%
  • Kind: placebo
    • Percent: 13%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 15-19%
  • Kind: placebo
    • Percent: 13%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 17.0%
  • Kind: placebo
    • Percent: 11.0%
  • Post Marketing
    Abnormal dreams US
  • Kind: experimental
    • Percent: 1-13%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 12.0%
  • Kind: placebo
    • Percent: 10.0%
  • Post Marketing
    Headache US
  • Kind: experimental
    • Percent: 12.0%
  • Kind: placebo
    • Percent: 10.0%
  • Post Marketing
    Abnormal dreams US
  • Kind: experimental
    • Percent: 12.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Vomiting US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Vomiting US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Suicidal behaviour, ideation US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Suicidal behaviour, ideation US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Suicidal behaviour, ideation US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Suicidal behaviour, ideation US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Depressed moods and disturbances US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Abnormal dreams US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 8.0%
  • Post Marketing
    Irritability US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 8.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 11.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 10.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 10.0%
  • Kind: placebo
    • Percent: 5.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 10.0%
  • Kind: placebo
    • Percent: 7.0%
  • Post Marketing
    Anxiety US
  • Kind: experimental
    • Percent: 7.0%
  • Kind: placebo
    • Percent: 9.0%
  • Post Marketing
    Insomnia US
  • Kind: experimental
    • Percent: 9.0%
  • Kind: placebo
    • Percent: 7.0%
  • Post Marketing
    Flatulence US
  • Kind: experimental
    • Percent: 6-9%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Suicidal ideation/behavoir US
  • Kind: experimental
    • Percent: 6.0%
  • Kind: placebo
    • Percent: 8.0%
  • Post Marketing
    Abnormal dreams US
  • Kind: experimental
    • Percent: 8.0%
  • Kind: placebo
    • Percent: 4.0%
  • Post Marketing
    Anxiety US
  • Kind: experimental
    • Percent: 8.0%
  • Kind: placebo
    • Percent: 6.0%
  • Post Marketing
    Constipation US
  • Kind: experimental
    • Percent: 5-8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dysgeusia US
  • Kind: experimental
    • Percent: 5-8%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 7.0%
  • Kind: placebo
    • Percent: 4.0%
  • Post Marketing
    Irritability US
  • Kind: experimental
    • Percent: 5.0%
  • Kind: placebo
    • Percent: 7.0%
  • Post Marketing
    Abdominal Pain US
  • Kind: experimental
    • Percent: 5-7%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Upper respiratory tract disorder US
  • Kind: experimental
    • Percent: 5-7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 4-7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Depressed mood disorders and disturbances US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Post Marketing
    Diarrhea US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Post Marketing
    Diarrhea US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Post Marketing
    Depressed mood disorders and disturbances US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 1%
  • Post Marketing
    Suicidal ideation/behaviour US
  • Kind: experimental
    • Percent: 6.0%
  • Kind: placebo
    • Percent: 6.0%
  • Post Marketing
    Anxiety US
  • Kind: experimental
    • Percent: 5.0%
  • Kind: placebo
    • Percent: 6.0%
  • Post Marketing
    Dry Mouth US
  • Kind: experimental
    • Percent: 4-6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial

    Contraindications

    Information currently not available.

    Food Interactions

    Avoid excessive or chronic alcohol consumption. Varenicline may increase the effects of alcohol; therefore, reduce consumption of alcohol when starting varenicline.