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

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1,10-Phenanthroline
The risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Varenicline.
Abacavir
Abacavir may decrease the excretion rate of Varenicline which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Varenicline which could result in a higher serum level.
Acebutolol
The risk or severity of adverse effects can be increased when Acebutolol is combined with Varenicline.
Aceclofenac
Aceclofenac may decrease the excretion rate of Varenicline which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Varenicline which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Varenicline which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Varenicline which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Varenicline which could result in a higher serum level.
Aclidinium
Varenicline may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acotiamide
The risk or severity of adverse effects can be increased when Acotiamide is combined with Varenicline.
Acrivastine
Varenicline may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Varenicline which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Varenicline which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Varenicline which could result in a higher serum level.
Agmatine
The serum concentration of Agmatine can be increased when it is combined with Varenicline.
Albutrepenonacog alfa
Varenicline may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Varenicline which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Varenicline which could result in a higher serum level.
Allopurinol
Allopurinol may decrease the excretion rate of Varenicline which could result in a higher serum level.
5 References
  1. 1 . Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR: Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006 Jul 5;296(1):56-63.PubMed: 16820547
  2. 2 . Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9.PubMed: 16766716
  3. 3 . Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW: Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos. 2006 Jan;34(1):121-30. Epub 2005 Oct 12.PubMed: 16221753
  4. 4 . Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT: Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005 May 19;48(10):3474-7.PubMed: 15887955
  5. 5 . Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614.PubMed: 16467225