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20-September-2008 09:55:56 - Varenicline Varenicline Systematic IUPAC name 7,8,9,10-tetrahydro-6,10-methano- 6H-pyrazino2,3-h3benzazepine Identifiers CAS number 249296-44-4 375815-87-5 ATC code N07BA03 PubChem 170361 Chemical data Formula C13H13N3 Mol. mass 211.267 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability ? Protein binding 20% Metabolism Limited 10% Half life 24 hours Excretion Renal 81-92% Therapeutic considerations Licence data EU, US Pregnancy cat. CUS Legal status ℞ Prescription only Routes Oral Varenicline trade name Chantix in the USA and Champix in Europe and other countries, marketed by Pfizer, usually in the form of varenicline tartrate is a prescription medication used to treat smoking addiction. Varenicline is a nicotinic receptor partial agonist. In this respect, it is similar to cytisine and different from nicotinic antagonist, bupropion, and nicotine replacement therapies NRTs like nicotine patches commonly, the patch and nicotine gum. As a partial agonist, it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products, and through these mechanisms, it can assist some patients in stopping smoking. Contents 1 Indications 2 Mechanism of action 3 Pharmacokinetics 4 Side Effects 5 History 6 Footnotes 7 External links Indications Varenicline is indicated for suggested for use in smoking cessation. It is an alternative to NRTs and agonist medication and has demonstrated greater efficacy than them in comparable studies.1 The FDA has approved its use for twelve weeks. If smoking cessation has been achieved it may be continued for another twelve weeks.2 Varenicline has not been tested in children, those under 18 years old, or pregnant women, and therefore is not recommended for use by these groups. Women currently breastfeeding should also avoid this product, since varenicline may pass into the breast milk, leading to unknown effects on the child. Mechanism of action Varenicline is a partial agonist of the α4β2 subtype of the nicotinic acetylcholine receptor. In addition it acts on α3β4 and weakly on α3β2 and α6-containing receptors. A full agonism was displayed on α7-receptors.3 Pharmacokinetics Most of the active compound is excreted renally 92-93%. A small proportion is glucuronidated, oxidated, N-formylated or conjugated to a hexose.4 The elimination half-life is about 24 hours. Side Effects Nausea occurs commonly in people taking varenicline. Other less common side effects include headache, difficulty sleeping, and abnormal dreams. Rare side effects reported by people taking varenicline compared to placebo include change in taste, vomiting, abdominal pain, flatulence, and constipation.5 In November 2007, the FDA announced it had received post-marketing reports that patients using Chantix for smoking cessation had experienced several serious symptoms, including suicidal ideation and occasional suicidal behavior, erratic behavior, and drowsiness. On February 1, 2008 the FDA issued an Alert to further clarify its findings, noting that it appears increasingly likely that there is an association between Chantix and serious neuropsychiatric symptoms. It is unknown whether the psychiatric symptoms are related to the drug or to nicotine withdrawal symptoms, although not all patients had stopped smoking. The FDA is aware of the highly-publicized case of Carter Albrecht who, in an apparent state of delirium, was shot to death by his neighbour after hitting his girlfriend and then trying to forcibly enter the neighbor's house.6 Although in this case the delirium appeared to be caused by taking varenicline with a high dose of alcohol, the FDA asked Pfizer for additional cases that might be similar. It also recommended that health care professionals and patients watch for behavioral and mood changes.7 On Thursday, May 22, 2008, The New York Times reported that the U.S. Federal Aviation Administration F.A.A. had announced the day before a ban on the use of Chantix varenicline tartrate for both pilots and air traffic controllers, due to concerns with possible adverse neuropsychiatric effects which could be detrimental to public safety.8 On Sunday, May 25, 2008, The Los Angeles Times reported that over 2 dozen traffic accidents had been linked to Chantix and reported to the FDA. Warnings had previously been issued by Pfizer regarding the risks of Chantix while driving, however these warnings have largely been ignored by doctors and patients.9 On Tuesday, June 17, 2008, The Washington Times reported on its Front Page that the United States Department of Veterans Affairs was testing Chantix on war veterans with Post Traumatic Stress Disorder without properly warning them of the side effects, and that in one case a veteran was almost killed when he had a psychotic episode and threatened police officers.10 History Varenicline was discovered at Pfizer through the research aimed at modifying the structure of cytisine,11 a European smoking cessation aid and also a partial α4β2-nicotinic antagonist.1213 Varenicline received a priority review by the U.S. Food and Drug Administration in February 2006, shortening the usual 10-month review period to 6 months because of its demonstrated effectiveness in clinical trials and perceived lack of safety issues.14 The agency's approval of the drug came on May 11, 2006.2. Beginning August 1, 2006, varenicline has been available for sale in the United States, and on September 29, 2006, it was approved for sale in the European Union. Footnotes ^ Jorenby D E, Hays J T, Rigotti N A, Azoulay S, Watsky E J, Williams K E, Billing C B, Gong J, Reeves K R 2006. Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA 296 1: 56-63. doi:10.1001/jama.296.1.56. PMID 16820547. ^ a b U.S. Food and Drug Administration. FDA Approves Novel Medication for Smoking Cessation. Press release, 11 May 2006. ^ Mihalak KB, Carroll FI, Luetje CW 2006. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol. Pharmacol. 70 3: 801-5. doi:10.1124/mol.106.025130. PMID 16766716. ^ 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;34:121-30. PMID 16221753. ^ American Cancer Society. Cancer Drug Guide: Varenicline. Retrieved on 2008-01-19. ^ ABC News: Did Quit-Smoking Pill Lead to Man's Death?. Retrieved on 2007-12-15. ^ Early Communication About an Ongoing Safety Review: Varenicline marketed as Chantix. United States Food and Drug Administration November 20 2007. Retrieved on 2007-11-21. ^ Saul, Stephanie 2008-05-22. F.A.A. Bans Antismoking Drug, Citing Side Effects, New York Times. Retrieved on 2008-05-22. ^ Alonso-Zaldivar, Ricardo 2008-05-25. Drug taken to stop smoking is linked to traffic mishaps, Los Angeles Times. Retrieved on 2008-05-25. ^ Hudson, Audrey 2008-06-17. VA Testing Drugs on War Veterans, The Washington Times, p. A1. ^ Coe JW, Brooks PR, Vetelino MG, et al 2005. Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J. Med. Chem. 48 10: 3474-7. doi:10.1021/jm050069n. PMID 15887955. ^ Schwartz JL 1979. Review and evaluation of methods of smoking cessation, 1969-77. Summary of a monograph. Public Health Rep 94 6: 558-63. PMID 515342. Full text at PMC: 1431736 ^ Etter JF 2006. Cytisine for smoking cessation: a literature review and a meta-analysis. Arch. Intern. Med. 166 15: 1553-9. doi:10.1001/archinte.166.15.1553. PMID 16908787. ^ Kuehn BM 2006. FDA speeds smoking cessation drug review. JAMA 295 6: 614. doi:10.1001/jama.295.6.614. PMID 16467225. External links Wikinews has related news: New drug for smoking cessation is under investigation Official website FDA Alert v d e Parasympathomimetics / cholinergic agonists / acetylcholinesterase inhibitors N06DA, N07AA Direct at receptor muscarinic: Muscarine - Oxotremorine - M1 Xanomeline - M3 Bethanechol, Pilocarpine, Arecoline, Cevimeline, Aceclidine nicotinic: Nicotine - Lobeline - Varenicline - Epibatidine M N: Acetylcholine/Choline alfoscerate - Methacholine - Carbachol Indirect/AIs in synapse Reversible carbamates: Ambenonium - Stigmine Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine, Distigmine Edrophonium anti-dementia Galantamine, Donepezil, Tacrine Irreversible/ organophosphate ophthalmological Echothiophate, Isoflurophate antiparasitic Malathion, Metrifonate chemical warfare see Nerve agent v d e Drugs used in addictive disorders N07B Nicotine dependence/ Nicotinic agonist Nicotine - Bupropion - Dianicline - Varenicline - Lobeline - Mecamylamine - Clonidine - Scopolamine - Surinabant Alcohol dependence Disulfiram - Calcium carbimide - Acamprosate - Naltrexone - Nalmefene - Topiramate - Clonidine - Buprenorphine - Morphine Opioid dependence Buprenorphine - Methadone - Levacetylmethadol - Fentanyl - Dihydrocodeine - Dihydroetorphine - Clonidine - Lofexidine - Naltrexone - Ibogaine - 18-Methoxycoronaridine - Extended Release Morphine - Extended Release Hydromorphone Stimulant dependence Dexamphetamine - Bupropion - Vanoxerine - Nocaine - Vigabatrin Benzodiazepine dependence Clonidine - Diazepam - Phenytoin - Phenobarbital Cocaine dependence Bupropion - Vanoxerine - Nocaine - Baclofen - Vigabatrin Sedative-Hypnotic dependence Phenobarbital - Diazepam - Lorazepam - Clonidine - Chloral Hydrate Retrieved from http://en..org/wiki/Varenicline Categories: Tobacco cessation | Pyrazines | Nicotinic agonists Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Česky Deutsch Español Français Italiano Nederlands 日本語 Polski Português Suomi This page was last modified on 10 August 2008, at 08:04
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