Varenicline

Varenicline
Clinical data
Pronunciation/vəˈrɛnɪkliːn/ və-REN-i-kleen
Trade namesChampix, Chantix, Tyrvaya, others
Other namesOC-01
AHFS/Drugs.comMonograph
MedlinePlusa606024
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth, intranasal
Drug classNicotinic agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding<20%
MetabolismLimited (<10%)
Elimination half-life24 hours
ExcretionKidney (81–92%)
Identifiers
  • 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h] [3]benzazepine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC13H13N3
Molar mass211.268 g·mol−1
3D model (JSmol)
  • n1c2cc3c(cc2ncc1)[C@@H]4CNC[C@H]3C4
  • InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2/t8-,9+ checkY
  • Key:JQSHBVHOMNKWFT-DTORHVGOSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Varenicline, sold under the brand names Chantix and Champix among others, is a medication used for smoking cessation[5][7] and for the treatment of dry eye syndrome.[6][8] It is a nicotinic acetylcholine receptor partial agonist.[5][6] When activated, this receptor releases dopamine in the nucleus accumbens, the brain's reward center, thereby reducing cravings and withdrawal symptoms with smoking cessation, although less pronounced than a full agonist (i.e., nicotine).[9]

Common side effects include nausea, insomnia, abnormal dreams, headache, and nasopharyngitis (inflammation of the nose and throat).[7] Despite these potential adverse effects, varenicline has proven efficacy in helping individuals quit smoking. It is estimated that approximately one in eleven smokers who use varenicline successfully remain abstinent from tobacco at six months.[10]

It is on the World Health Organization's List of Essential Medicines.[11] The medication is available as a generic medication.[12] In the United States, varenicline was prescribed over 1 million times in 2020, ranking as the 275th most commonly prescribed medication.[13][14]

  1. ^ "Champix Product Information". Therapeutic Goods Administration (TGA). 26 September 2021. Archived from the original on 27 September 2021. Retrieved 26 September 2021.
  2. ^ "Champix varenicline (as tartrate) 0.5 mg and 1.0 mg tablet blister pack". Therapeutic Goods Administration (TGA). Archived from the original on 31 March 2022. Retrieved 26 September 2021.
  3. ^ "Product information". Health Canada. 22 October 2009. Retrieved 9 June 2023.
  4. ^ "Champix 0.5 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). Archived from the original on 24 December 2012. Retrieved 26 September 2021.
  5. ^ a b c Cite error: The named reference Chantix FDA label was invoked but never defined (see the help page).
  6. ^ a b c "Tyrvaya- varenicline spray". DailyMed. Archived from the original on 23 October 2021. Retrieved 22 October 2021.
  7. ^ a b c Cite error: The named reference Champix EPAR was invoked but never defined (see the help page).
  8. ^ "Oyster Point Pharma Announces FDA Approval of Tyrvaya (varenicline solution) Nasal Spray for the Treatment of the Signs and Symptoms of Dry Eye Disease" (Press release). Oyster Point Pharma. 18 October 2021. Retrieved 22 October 2021 – via PR Newswire.
  9. ^ Tashkin DP (August 2015). "Smoking Cessation in Chronic Obstructive Pulmonary Disease". Seminars in Respiratory and Critical Care Medicine. 36 (4): 491–507. doi:10.1055/s-0035-1555610. PMID 26238637. S2CID 207870513.
  10. ^ Crawford P, Cieslak D (September 2017). "Varenicline for Smoking Cessation". American Family Physician. 96 (5): Online. PMID 28925657. Archived from the original on 26 May 2019. Retrieved 26 May 2019.
  11. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  12. ^ "Varenicline tablet, film coated". DailyMed. 27 January 2023. Retrieved 9 June 2023.
  13. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 18 March 2020. Retrieved 7 October 2022.
  14. ^ "Varenicline - Drug Usage Statistics". ClinCalc. Archived from the original on 8 October 2022. Retrieved 7 October 2022.