Medication Summary

Two types of pharmacologic therapy are available as part of a smoking cessation program nicotine and antidepressants. The goals of pharmacotherapy are to induce smoking cessation, reduce morbidity, and prevent complications.

Class Summary

Nicotine replacement therapy (NRT) is available in the form of cutaneous patches, inhaled or nasal delivery, or chewing gum. Nicotine patches are sold under various trade names (see below). For each proprietary system, the dosing schedule involves a graduated decrease of the drug dose over 9-12 weeks.

Nicotine acetylcholine receptor partial agonists are also used as smoking cessation aids. They bind to nicotine receptors and elicit mild central effects to ease nicotine withdrawal symptoms. They also decrease the stimulatory effect of nicotine consumption by blocking nicotine receptors.

Nicotine transdermal system (NicoDerm CQ, Nicorette, Thrive, Nicotrol Inhaler, Nicotrol NS, Nicorelief)

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Nicotine stimulates all autonomic ganglia and catecholamine discharge in the adrenal medulla at small doses. At larger doses transmission through autonomic ganglia is blocked and catecholamine discharge from the medulla is inhibited.

Nicotine replacement therapy works best when used in conjunction with a support program, such as counseling, group therapy, or behavioral therapy.

Nicotine chewing gum, if chewed correctly, increases quit rates up to 2-fold. At 1 year, the abstinence rate with the patch is 20%. At 4 years, the abstinence rate is 12.4%, as opposed to 4.5% with placebo. Nicotine patches are sold under various trade names (see below). For each proprietary system, the dosing schedule involves a graduated decrease of the drug dose over 9-12 weeks.

Nicotine gum is marketed in 2 strengths, 2 mg and 4 mg. Individuals who smoke 1 pack per day should use the 4-mg pieces; those who smoke less than 1 pack per day should use the 2-mg pieces. Instruct the patient to chew hourly and for their initial cravings for 2 weeks, then gradually reduce the amount chewed over the next 3 months.

The nicotine nasal spray and the inhaler dosage forms provide nicotine delivery through the nasal and oral mucosa, respectively.

The nicotine in nicotine polacrilex is absorbed through the oral mucosa. Absorption is quick and closely approximates the time course of plasma nicotine levels observed after cigarette smoking.

Intranasal nicotine and nicotine from an oral inhaler may closely approximate the time course of plasma nicotine levels observed after cigarette smoking.

Varenicline (Chantix)

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Varenicline is a partial agonist that is selective for alpha-4, beta-2 nicotinic acetylcholine receptors. Its action is thought to result from activity at a nicotinic receptor subtype, where its binding produces agonist activity while simultaneously preventing nicotine binding. Its agonistic activity is significantly lower than that of nicotine. It also elicits moderate affinity for serotonin receptors. Maximum plasma concentrations occur within 3-4 hours after oral administration. With regular dosing, a steady state is reached within 4 days.

Class Summary

These medications ameliorate withdrawal symptoms while the smoker deals with behavioral aspects of smoking cessation.

Bupropion is used as a non–nicotine-containing aid to smoking cessation. It acts by enhancing central nervous nonadrenergic function. A 23% sustained cessation rate is achieved with bupropion tablets at 1 year, compared with a 12% sustained cessation rate with placebo. Bupropion also is effective for patients in whom nicotine replacement therapy fails.

Bupropion hydrochloride (Zyban, Aplenzin, Fortivo XL, Wellbutrin XL)

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Bupropion is used in conjunction with a support group, behavioral counseling, or both. It may also be used in combination with nicotine replacement therapy. It inhibits neuronal dopamine reuptake, in addition to being a weak blocker of serotonin and norepinephrine reuptake. For any given dosage form use the same total daily dose but adjust frequency as indicated for immediate (3-4 times daily), sustained release (twice daily), or extended release (once daily).

Questions

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Smoking cessation strategies for clinicians.

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Author

R Gregory Lande, DO, COL (Ret), FACN, FAOAAM Editor-in-Chief, Journal of Addictive Diseases; Former Director, Psychiatry Continuity Service, Former Clinical Consultant, Addiction Treatment Program, Walter Reed National Military Medical Center

R Gregory Lande, DO, COL (Ret), FACN, FAOAAM is a member of the following medical societies: American Osteopathic Academy of Addiction Medicine, American Osteopathic Association

Disclosure: Nothing to disclose.

Specialty Editor Board

Francisco Talavera, PharmD, PhD Adjunct Assistant Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference

Disclosure: Received salary from Medscape for employment. for: Medscape.

Chief Editor

Glen L Xiong, MD Associate Clinical Professor, Department of Psychiatry and Behavioral Sciences, Department of Internal Medicine, University of California, Davis, School of Medicine; Medical Director, Sacramento County Mental Health Treatment Center

Glen L Xiong, MD is a member of the following medical societies: AMDA - The Society for Post-Acute and Long-Term Care Medicine, American College of Physicians, American Psychiatric Association, Central California Psychiatric Society

Disclosure: Serve(d) as a director, officer, partner, employee, advisor, consultant or trustee for: SafelyYou, Blue Cross Blue Shield<br/>book co-editor for: Wolter Kluwer, American Psychiatric Publishing Inc.

Acknowledgements

Morley Lertzman, MD, FRCP(C) Professor, Department of Medicine, Section of Pulmonary Medicine, St Boniface Hospital, University of Manitoba, Canada

Disclosure: Nothing to disclose.

Sat Sharma, MD, FRCPC Professor and Head, Division of Pulmonary Medicine, Department of Internal Medicine, University of Manitoba; Site Director, Respiratory Medicine, St Boniface General Hospital

Sat Sharma, MD, FRCPC is a member of the following medical societies: American Academy of Sleep Medicine, American College of Chest Physicians, American College of Physicians-American Society of Internal Medicine, American Thoracic Society, Canadian Medical Association, Royal College of Physicians and Surgeons of Canada, Royal Society of Medicine, Society of Critical Care Medicine, and World Medical Association

Disclosure: Nothing to disclose.