Smoking cessation bupropion

Nicotine replacement medications have been used for over two decades to help smokers quit. However, nicotine delivery from medications could potentially be improved by formulations that better mimic the effects of tobacco-delivered nicotine. Antidepressants such as bupropion have also been shown to aid smoking cessation. Bupropion was initially studied for smoking cessation based upon anecdotal reports... 

Bupropion Increased norepinephrine and dopamine activity Presynaptic release of catecholamines Major depression smoking cessation (bupropion) sedation Extensive metabolism in liver Toxicity Lowers seizure threshold (amoxapine,... 

Of the more recently introduced methods for smoking cessation, bupropion (an antidepressant with dopaminomimetic properties) has recently been introduced. Clinical trial data, in which the nicotine patch, bupropion at 300 mg, and a combination of the two drugs were compared with placebo treatment, have shown cessation of smoking rates of 36% for the patch, 49% for bupropion and 58% for the combined treatments following 7 weeks of treatment. The placebo response rate was 23%. All subjects received relapse prevention therapy. Thus bupropion appears to be a reasonably safe and effective treatment for nicotine dependence. It is however contraindicated in those subject to epilepsy its main side effects are dry mouth and insomnia. 

Jorenby DE, Leischow SJ, Nides MA, et al A controlled trial of sustained-release bupropion, a nicotine patch, or both for smoking cessation. N Eng J Med 340 685— 691, 1999... 

Nortriptyline. Nortriptyhne, a tricychc antidepressant, has been shown in double-blind, placebo-controlled randomized trials to be superior to placebo for smoking cessation (Prochazka et al. 1998). Nortriptyline appears to have efficacy comparable to that of bupropion for smoking cessation (Hall et al. 2002). The efficacy of this agent may be improved with more intensive behavioral therapies (Hall et al. 1998). Nortriptyline s mechanism of action is thought to relate to its noradrenergic and serotonergic reuptake blockade, because these two neurotransmitters have been implicated in the neurobiology of nicotine dependence. Side effects of nortiptyline are typical of tricyclic antidepressants and include dry mouth, blurred vision, constipation, and orthostatic hypotension. Nortriptyline appears to have some utility for smokers with a past history of major depression, and it can be recommended as a second-... 

Briggs G, Freeman R, Yaffe S Drugs in Pregnancy and Lactation A Reference Guide to Maternal and Fetal Risk. Philadelphia, Lippincott, Williams Wilkins, 2002 Chengappa KN, Kambhampati R, Perkins K, et al Bupropion sustained release as a smoking cessation treatment in remitted depressed patients maintained on neatment with selective serotonin reuptake inhibitor antidepressants. J Clin Psychiatry 62 503—508, 2001... 

Evins AE, Mays VK, Rigotti NA, et al A pilot trial of bupropion added to cognitive behavioral therapy for smoking cessation in schizophrenia. Nicotine Tob Res 3 397-M03, 2001... 

Hall SM, Reus VI, Munoz RF, et al Nortriptyline and cognitive-behavioral therapy in the treatment of cigarette smoking. Arch Gen Psychiatry 55 683-690, 1998 Hall SM, Humfleet GL, Reus VI, et al Psychological intervention and antidepressant treatment in smoking cessation. Arch Gen Psychiatry 59 930-936, 2002 Hayford KE, Patten CA, Rummans TA, et al Efficacy of bupropion for smoking cessation in smokers with a former history of major depression or alcoholism. Br J Psychiatry 174 173-178, 1999... 

Hays JT, Hurt RD, Rigotti NA, et al Sustained-release bupropion for pharmacologic relapse prevention after smoking cessation. Ann Intern Med 135 423 33, 2001 Henningfleld JE Nicotine medications for smoking cessation. N Engl J Med 333 1196-1203, 1995... 

West R. (2003). Bupropion SR for smoking cessation. Expert Opin. Pharmacother. 4, 533-40. 

Lerman, C.R.D., Kaufmann, V., Audrain, J., Hawk, L., Liu, A., Niaura, R., Epstein, L. Mediating mechanisms for the impact of bupropion in smoking cessation treatment. Drug Alcohol Depend. 67 219, 2002. 

Durcan, M.J.D.G., White, J., Johnston, J.A., Gonzales, D., Niaura, R., Rigotti, N., Sachs, D.P. The effect of bupropion sustained-release on cigarette craving after smoking cessation. Clin. Ther. 24 540, 2002. 

Many neurotransmitters are inactivated by a combination of enzymic and non-enzymic methods. The monoamines - dopamine, noradrenaline and serotonin (5-HT) - are actively transported back from the synaptic cleft into the cytoplasm of the presynaptic neuron. This process utilises specialised proteins called transporters, or carriers. The monoamine binds to the transporter and is then carried across the plasma membrane it is thus transported back into the cellular cytoplasm. A number of psychotropic drugs selectively or non-selectively inhibit this reuptake process. They compete with the monoamines for the available binding sites on the transporter, so slowing the removal of the neurotransmitter from the synaptic cleft. The overall result is prolonged stimulation of the receptor. The tricyclic antidepressant imipramine inhibits the transport of both noradrenaline and 5-HT. While the selective noradrenaline reuptake inhibitor reboxetine and the selective serotonin reuptake inhibitor fluoxetine block the noradrenaline transporter (NAT) and serotonin transporter (SERT), respectively. Cocaine non-selectively blocks both the NAT and dopamine transporter (DAT) whereas the smoking cessation facilitator and antidepressant bupropion is a more selective DAT inhibitor. 

Bupropion A drug that inhibits the presynaptic neuronal reuptake of both dopamine and noradrenaline which is used as an antidepressant and to prevent relapse following smoking cessation. 

First-line pharmacotherapies for smoking cessation are bupropion sustained release, nicotine gum, nicotine inhaler, nicotine nasal spray, and... 

Bupropion sustained release (SR) is an effective smoking-cessation treatment. It is contraindicated in patients with a seizure disorder, a current or prior diagnosis of bulimia or anorexia nervosa, and use of a monoamine oxidase inhibitor within the previous 14 days. It can be used in combination with NRT. 

Nicotine replacement therapies can be combined with each other and/or bupropion to increase long-term abstinence rates. bOo not abruptly discontinue. Taper up initially, and taper off once therapy is complete. cClonidine and nortriptyline are not FDA approved for smoking cessation. 

After more than a decade of use, bupropion (24) is considered a safe and effective antidepressant, suitable for use as first-line treatment. In addition, it is approved for smoking cessation and seasonal affective disorder. It is also prescribed off-label to treat the sexual dysfunction induced by SSRIs. Bupropion is often referred to as an atypical antidepressant and has much lower affinity for the monoamine transporters compared with other monoamine reuptake inhibitors. The mechanism of action of bupropion is still uncertain but may be related to inhibition of dopamine and norepinephrine reuptake transporters as a result of active metabolites [71,72]. In a recently reported clinical trial, bupropion extended release (XL) had a sexual tolerability profile significantly better than that of escitalopram with similar re-... 

Patterson F, Schnoll R, Wileyto E, Pinto A, Epstein L, Shields P, Hawk L, Tyndale R, Benowitz N, Lerman C (2008) Toward Personalized Therapy for Smoking Cessation A Randomized Placebo-controlled Trial of Bupropion. Chn Pharmacol Ther 84(3) 320-325 Perez-Stable EJ, Herrera B, Jacob P 3rd, Benowitz NL (1998) Nicotine metabohsm and intake in black and white smokers. JAMA 280(2) 152-156 Perry RJ, Griffiths W, Dextraze P, Solomon RJ, Trebbin WM (1984) Elevated nicotine levels in patients undergoing hemodialysis. A role in cardiovascular mortality and morbidity Am J Med 76(2) 241-246... 

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