An Effective Aide in Quitting Smoking

Quitting smoking is proven to be a task that is not easy to accomplish. The average number of quitting attempts that majority of smokers try in their lifetime varies from 6 to 9 times (Pfizer, Inc. , 2007). The smoking cessation attempts are often not successful because of faulty methodologies used in the endeavor. Majority of smoker’s efforts to quit are without usage of medical drugs. Thus, the meager success rates of only 3 to 5 percent of the total yearly attempts.

The availability of products like bupropion hydrochloride, nortriptyline hydrochloride, and nicotine replacement drugs manifests only modest accomplishments (Nides et al. , 2006). In line with this dilemma, a drug was manufactured to aide smokers in their quitting venture with a step-by-step technique. This drug which is manufactured by Pfizer, Inc. is known for its brand name Chantix® but its generic name is varenicline tartrate. This drug was manufactured to offer an effective support for smokers that want to quit this vice. Drug specifics and mode of action

Varenicline tartrate, the tartrate salt form of varenicline, posses the chemical name – 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine, (2R,3R)-2,3-dihydroxy- butanedioate (1:1). This substance which is the active ingredient of Chantix® remarkably dissolves in water and has a white to slightly yellow color when in powered form. Varenicline has the molecular formula C13H13N3•C4H6O6 (RxList, Inc. , 2009). This drug is a non-nicotinic drug that targets the ? 4? 2 nicotinic receptor in the brain. It acts through blockage of nicotine from attaching to the ?

4? 2 nicotinic receptor. These receptors are the same target of nicotine, a substance present in cigarette. The binding of nicotine with the ? 4? 2 nicotinic receptors after the smoker inhales cigarette smoke conveys a message to a specific part in the brain to discharge dopamine, the substance responsible for creating the pleasure feeling. The addiction to cigarette smoking is due to short duration nature of the pleasurable feeling that is created by dopamine. The body yearns for more nicotine so that a simulation of the pleasurable feeling occurs again and again.

Since varenicline prevents the binding of nicotine with its brain receptors; the intake of this drug will erase the feeling of pleasure that a person experiences every time cigarette is smoked. Therefore, quitting of smoking is easier along with intake of varenicline because the act of smoking does not bring the good feeling anymore (Coe et al. 2005). Another positive attribute of varenicline is its capacity to decrease the smoking withdrawal signs through its interaction with the dopamine receptors. This interaction results in the discharge of the hormones that allows the individual to feel pleasure or “feel-good” hormones (Bullock, 2007).

Thus, during varenicline medication the smoker will not experience the terrible withdrawal symptoms because high amounts of “feel-good” hormones are distributed in his or her blood. Precautions and side effects The adverse reactions associated with the intake of varenicline are: dizziness; nausea; headache; fatigue; behavioral changes like depression and crankiness; boosted appetite; vomiting; decreased bowel motility; flatulence; and, sleeping problems. This drug can not be taken along with cimetidine because the latter will amplify varenicline levels in the plasma.

Insulin; blood thinners like warfarin or coumadin; and theophylline are other therapeutic medicines prohibited during varenicline medication (“MSN health and fitness”). Precautions that need to be observed during varenicline medication are: consultation with a physician about the proper dosage and duration of therapy; monitoring of behavioral changes during the medication period; this drug is not good for individuals whom are below 18 years old, pregnant, and breast feeding mothers; the intake of this drug may also alter the performance of specialized tasks; and, medication should be after food ingestion (MIMS, 2009).

Further precautions indicated in the use of this drug are: non- usage among people with history of mental disease and kidney problems; compliance with proper dosage prescribed by the doctor; and, observance of prescription label (“MSN health and fitness”). Efficacy of varenicline therapy According to its manufacturer, varenicline medication has the smoking quitting success rate of 44 percent while sugar pills only have 18 percent efficacy (Pfizer, Inc. , 2007). In a study conducted by Nides et al.

(2006) comparing varenicline with bupropion a significantly higher success rate among varenicline medicated subjects was observed. The efficacy of this drug in the said study was 21. 9 percent, whereas, bupropion only had 16. 1 percent. Another study which proves the capacity of this drug to increase the success rate of smoking cessation is that one done by Cahill et al. (2007). It is noted in the said study that varenicline triples the achievement of smoking termination as compared to those who are medicated with antidepressants or had no medications at all.

Issues on varenicline medication Among the issues that are coupled with the medication of varenicline are the harsh side effects like hallucinations and the alterations in the perception of joy. A varenicline medicated individual reported that during his therapy with varenicline he experienced intense hallucinations as well as alterations in his fulfillment after activities that can supposedly make an individual happy. Given examples of the activities he can’t find pleasure anymore were: writing, exercising, self-stimulation tricks, and socialization (Cloud, 2009).

Another issue with varenicline medication is the suicidal inclination of individuals taking this drug. There are reports of individuals having suicide thoughts and committing suicides that are attributed to the intake of varenicline as a therapeutic aide for smoking cessation. This drug is also accounted to amplify psychiatric conditions like schizophrenia and bipolar disorder. These reports were already reported to FDA thus the advice of this agency to take tremendous caution when prescribing and taking varenicline (FDA, 2007).

Biochemical Pathway The maximum plasma concentration of varenicline is attained 3 – 4 hours post oral intake of the drug. This drug’s bioavailability is high after oral intake and is not altered by the dosing time and the presence or absence of food. Varenicline though has a plasma protein binding that is below or equal to 20 percent. It takes an estimate of 24 hours for the half-life elimination of this drug to take place and negligible metabolism was observed (RxList, Inc. , 2009). Conclusion

Despite the side effects that are said to be attributed to the administration of varenicline, this drug’s efficacy as a smoking cessation aide remains to be unaffected. Almost all of the available drugs have side effects thus it is not alarming for varenicline to also have some side effects. That is why precautions are available to eliminate the occurrence of most of a drug’s side effects. The proper observance of all the precautions indicated for this drug ensures that the person undergoing varenicline therapy and smoking cessation endeavor will have no health problems attributable to the medication.

The weight of support that this drug can lend to the smokers who are trying to leave their deadly vice (smoking) is significantly higher as compared to the risks of side effects manifestation during the therapeutic period. Thus, cessation of smoking can be made easier through the aide of varenicline tartrate (Chantix® ).

Reference List

Bullock, Carole. (2007). Smokers get a kick from varenicline; new research finds drug triples quit rate. Heartwire. Retrieved March 25, 2009 from http://www.theheart. org/article/768455. do Cloud, John. (2009). Can One Drug Cure Addiction to Another? Time, Inc. Retrieved March 26, 2009 from http://www. time. com/time/health/article/0,8599,1883588,00. html? xid=rss-fullhealthsci-yahoo 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. (2005). Varenicline: An ?

4? 2 Nicotinic Receptor Partial Agonist for Smoking Cessation. Journal of Medicinal Chemistry, 48(10), 3474-3477. U. S. Food and Drug Administration, (FDA). (2007). Early Communication About an Ongoing Safety Review Varenicline (marketed as Chantix). Retrieved March 26, 2009 from http://www. fda. gov/Cder/Drug/early_comm/varenicline. htm MIMS. (2009) Varenicline. Retrieved March 25, 2009 from http://www. mims. com/Page. aspx? menuid=mng&name=varenicline&genmono=true

“MSN health and fitness” (2008). Varenicline. Center Multum, Inc. Retrieved March 25, 2009 from http://health. msn. com/medications/articlepage. aspx? cp-documentid=100160707 Nides, M. , Oncken, C. , Gonzales, D. , Rennard, S. , Watsky, E. J. , Anziano, R. , and Reeves, K. R. (2006). Smoking Cessation with Varenicline, a Selective an ? 4? 2 Nicotinic Receptor Partial Agonist. Archives of Internal Medicine, 166. Retrieved March 25, 2009 from http://archinte. ama-assn. org/cgi/reprint/166/15/1561

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