Aids for Smoking Cessation

Bupropion (amfebutamon) shows structural similarity with amphetamine (p.329) and inhibits neuronal reuptake of dopamine and norepinephrine. It is supposed to aid smokers in kicking the habit, possibly because it evokes CNS effects resembling those of nicotine. The high relapse rate after termination of the drug and substantial side effects put its therapeutic value in doubt. 

Nicotine served as an experimental tool for the classification of acetylcholine receptors. 

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Pierce JP, Gilpin LA. Impact of over-the-counter sales on effectiveness of pharmaceutical aids for smoking cessation. JAMA 2002 288 1260-1264. 

Oral mucosal membranes provide a port for systemic therapy as weU. Nitroglycerin sublingual tablets (Nitrostat) abort acute mgina attacks methyl-testosterone [58-18-4] buccal tablets (Android 5) are indicated for testosterone [58-22-0] replacement therapy (39) md nicotine [54-11-5] gum (Nicorette) aids in smoking cessation. 

Despite the limitations imposed by the physiology of the skin, several marketed controUed release transdermal dmg dehvery systems are available in the United States for example, scopolamine [51-34-3] for the treatment of motion sickness, nitroglycerin [55-63-0] for angina, estradiol [50-28-2] for the rehef of postmenopausal symptoms and osteoporosis, clonidine [4205-90-7] for the treatment of hypertension, fentanyl [437-38-7] as an analgesic, and nicotine [54-11-5] as an aid to smoking cessation. These systems are designed to dehver dmg for periods of one to seven days. 

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... 

Depression Bupropion (immediate release) IR, Wellbutrin (sustained release) SR, and bupropion (extended release) XL are indicated for the treatment of depression. Smoking cessation (Zyban only) Indicated as an aid to smoking-cessation treatment. 

As an aid to smoking cessation for the relief of nicotine withdrawal symptoms. Use as part of a comprehensive behavioral smoking-cessation program. 

Lobelia inflata (Indian tobacco) contains lobeline and other pyridine alkaloids. It has been used as an emetic, antidepressant, respiratory stimulant, an aid to smoking cessation, and a treatment for metamfetamine abuse (1). 

Another efficient modality for smoking cessation is bupropion.The antidepressant activity of bupropion is achieved through its effects on the levels of dopamine and norepinephrine in the brain (the effects of bupropion are mediated by blocking the reuptake of both dopamine and norepinephrine ). These effects are thought to underlie its positive results in clinical trials of patients with tobacco dependence (bupropion about doubles long-term abstinence rates compared with placebo). Increased brain levels of dopamine and norepinephrine would be expected to counteract the deficiency of these neurotransmitters during nicotine withdrawal and thereby aid in smoking cessation. 

Wellbutrin and Zyban (an aid in smoking cessation treatment) are trade name products for bupropion. Therefore, the potential exists for an overdose toxicity in a patient receiving multiple brand name and generic prescriptions containing bupropion for the treatment of depression, smoking cessation, and other off-label uses. 

The MIPS were prepared with nicotine as the template to evaluate the feasibility of MIPs as excipients for the controlled transdermal delivery of nicotine [Luis et al, 2014]. The transdermal delivery of nicotine has been suggested as an aid to smoking cessation therapy because a constant plasma level of nicotine reduces the craving for nicotine and therefore, aids in the abstinence from smoking. The MIPs were prepared and included in transdermal systems with vehicles of different polarities. The drug release kinetics revealed that the MIPs can be considered as suitable candidates for the controlled transdermal administration of nicotine. 

A successful pharmacotherapeutic approach is cutaneous nicotine patch combined with Zyban (welbutrin) as an aid to smoking cessation treatment (174). This pharmacological combination should be continued for at least 6 months. 

Nicotinic cholinergic receptors are located on cells that release a wide variety of transmitters (see chapter by Barik and Wonnacott, in this volume), so that nicotine interacts with multiple neurochemical pathways. The roles of cholinergic, dopaminergic, and endogenous opioid systems in physical dependence and withdrawal have been most thoroughly studied and documented. Research on the role of other transmitters and neurochemical mechanisms is rather scattered. Overall, however, research with rodent models of physical dependence has provided a wealth of potential targets for experimental treatments to aid smoking cessation. 

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