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Pharmacotherapy in Smoking Cessation

Pharmacotherapy in Smoking Cessation. Burden of Smoking. Compared with nonsmokers, smoking is estimated to increase the risk of— coronary heart disease by 2 to 4 times stroke by 2 to 4 times men developing lung cancer by 23 times women developing lung cancer by 13 times

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Pharmacotherapy in Smoking Cessation

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  1. Pharmacotherapy in Smoking Cessation

  2. Pharmacotherapy in Smoking Cessation Burden of Smoking • Compared with nonsmokers, smoking is estimated to increase the risk of— • coronary heart disease by 2 to 4 times • stroke by 2 to 4 times • men developing lung cancer by 23 times • women developing lung cancer by 13 times • dying from chronic obstructive lung diseases by 12 to 13 times CDC:Health Effects of Cigarette Smoking

  3. Pharmacotherapy in Smoking Cessation Cost of Smoking.. Prescription drugs, $6.4 billion Other care, $5.4 billion Medical expenditures (1998) Ambulatory care, $27.2 billion Hospital care, $17.1 billion Nursing home, $19.4 billion Societal costs: $7.18 per pack Annual lost productivity costs (1995–1999) Men, $55.4 billion Women, $26.5 billion Billions of dollars Centers for Disease Control and Prevention. (2002). MMWR 51:300–303.

  4. Pharmacotherapy in Smoking Cessation Prevalence of Smoking among Saudi Population • Current smoking among Saudi population ranges form 2.4-52.9% (median 17.5%) • Male 13-38% (median=26%) • Females 1-16% (Median=9%) • Risk of smoking was associated with being male, single and highly educated. • 20-50% of smokers started at or before the age of 15 • Common reasons for smoking: relief from psychological tension, boredom and imitating others. Bassiony M. Smoking In Saudi Arabia. Saudi Med J 2009; 30(7): 876-881

  5. Pharmacotherapy in Smoking Cessation Prevalence of Smoking among Saudi Population

  6. Pharmacotherapy in Smoking Cessation Deadly Habit.. Inhalation tobacco: Cigarettes Cigars Bidis Water pipe (shishah) Smokless tobacco: Spit tobacco Chewing Snuff

  7. Types of Smoking Is Shisha safer than cigarettes with less nicotine content?

  8. Pharmacotherapy in Smoking Cessation Shisha vs. Cigarette • A typical 1 hr session of water-pipe smoking involves inhaling 100-200x volume of smoke inhaled with one cigarette. 20 regular cigarettes Nicotine in 1 head (Mua'sel) = Nicotine in 1 head (unflavored) 70 regular cigarettes =

  9. Pharmacotherapy in Smoking Cessation Pretty Flower… Scientific classification of nicotine: • Kingdom: Plantae • Division: Magnoliophyta • Class: Magnoliopsida • Order: Solanales • Family: Solanaceae • Genus: Nicotine • Species: Nicotiana tabacum

  10. Pharmacotherapy in Smoking Cessation What is in that cigarette…

  11. Pharmacotherapy in Smoking Cessation Pharmacological effects of Nicotine • Ganglionic cholinergic receptor agonist: • Centrally, increases: • Increases cognitive function • Psychomotor activity sensorimotor performance • Attention and memory • Peripherally, increases: • respiratory rate • Heart rate • Blood pressure • Coronary blood flow

  12. Pharmacotherapy in Smoking Cessation Pharmacological effects of Nicotine • low doses • nicotine increases alertness and cognitive functioning by stimulating the cerebral cortex. • High doses • nicotine stimulates the “reward” center in the limbic system of the brain.

  13. Pharmacotherapy in Smoking Cessation Tobacco Dependence.. Tobacco Dependence Physiological Behavioral The addiction to nicotine The habit of using tobacco Treatment Treatment Medications for cessation Behavior change program Treatment should address the physiological and the behavioral aspects of dependence.

  14. Pharmacotherapy in Smoking Cessation Health benefits of Quitting Smoking.. Circulation improves, walking becomes easier Lung function increases up to 30% Lung cilia regain normal function Ability to clear lungs of mucus increases Coughing, fatigue, shortness of breath decrease 2 weeks to 3 months 1 to 9 months Excess risk of CHD decreases to half that of a continuing smoker 1 year Risk of stroke is reduced to that of people who have never smoked 5 years Lung cancer death rate drops to half that of a continuing smoker Risk of cancer of mouth, throat, esophagus, bladder, kidney, pancreas decrease 10 years Risk of CHD is similar to that of people who have never smoked after 15 years

  15. If quitting is so beneficial why do people still smoke!!

  16. Pharmacotherapy in Smoking Cessation Withdrawal Symptoms.. Most symptoms peak 24–48 hr after quitting and subside within 2–4 weeks.

  17. Pharmacotherapy in Smoking Cessation Weight Gain • In a study of 5247 patients age 35 and older people who had quit smoking • former smokers were on average 4.4 kg heavier than men who continued smoking. • Women who were former smokers were on average 5.0 kg heavier than women who continued smoking. N Eng J Med 1995; 333: 1165-1175

  18. Pharmacotherapy in Smoking Cessation • Nearly 41% of smokers try to quit smoking each year, relapse is common, and only about 10% achieve and maintain abstinence MMWR Morb Mortal Wkly Rep. 2004;53:427-431.

  19. Pharmacotherapy in Smoking Cessation Pharmacologic MethodsFirst-Line Therapies.. Three general classes of FDA-approved drugs for smoking cessation: • Nicotine replacement therapy (NRT) • Nicotine gum, patch, lozenge, nasal spray, inhaler • Psychotropics • Sustained-release bupropion • Partial nicotinic receptor agonist • Varenicline

  20. Pharmacotherapy in Smoking Cessation Pharmacologic Methods Second-Line Therapies.. • Clonidine • Nortriptyline

  21. Pharmacotherapy in Smoking Cessation NRT: PRODUCTS.. Nasal spray • Nicotrol NS (Rx) Inhaler • Nicotrol (Rx) Polacrilex gum • Nicorette (OTC) • Generic nicotine gum (OTC) Lozenge • Commit (OTC) • Generic nicotine lozenge (OTC) Transdermal patch • Nicoderm CQ(OTC) • Generic nicotine patches (OTC, Rx)

  22. Pharmacotherapy in Smoking Cessation 25 Cigarette Moist snuff 20 Nasal spray 15 Inhaler Plasma nicotine (mcg/l) 10 Lozenge (2mg) Gum (2mg) 5 Patch 0 1/0/1900 1/10/1900 1/20/1900 1/30/1900 2/9/1900 2/19/1900 2/29/1900 PLASMA NICOTINE CONCENTRATIONS for NICOTINE-CONTAINING PRODUCTS..

  23. Pharmacotherapy in Smoking Cessation Considerations with NRT.. • Patients with underlying cardiovascular disease: • Recent myocardial infarction (within past 2 weeks) • Serious arrhythmias • Serious or worsening angina • Patients with other underlying conditions • Active temporomandibular joint disease (gum only) • Pregnancy • Lactation NRT products may be appropriate for these patients if they are under medical supervision.

  24. Pharmacotherapy in Smoking Cessation Considerations with NRT.. • NRT is not FDA-approved for use in children or adolescents • Nonprescription sales (patch, gum, lozenge) are restricted to adults ≥18 years of age • NRT use in minors requires a prescription • Patients should stop using all forms of tobacco upon initiation of the NRT regimen

  25. Pharmacotherapy in Smoking Cessation Nicotine Gum .. • Resin complex • Nicotine • Polacrilin • Sugar-free chewing gum base • Contains buffering agents to enhance buccal absorption of nicotine • Available: 2 mg, 4 mg; regular, FreshMint, Fruit Chill, mint, & orange flavor

  26. Pharmacotherapy in Smoking Cessation Nicotine Gum .. DISADVANTAGES • Gum chewing may not be socially acceptable. • Gum is difficult to use with dentures. • Patients must use proper chewing technique to minimize adverse effects. ADVANTAGES • Gum use may satisfy oral cravings. • Gum use may delay weight gain. • Patients can titrate therapy to manage withdrawal symptoms.

  27. Pharmacotherapy in Smoking Cessation "Nicotine gum is not gum“.. Dosing is based on current smoking pattern: # of cigarettes/drecommended strength <25 cigarettes/day 2 mg > 25 cigarettes/day 4 mg week 1-6week 7-9week 10-12 1 q 1-2 h 1 q 2-4 h 1 q 4-8 h Recommended usage schedule: (not to exceed 24 pieces/d)

  28. Pharmacotherapy in Smoking Cessation "Nicotine gum is not gum“..

  29. Pharmacotherapy in Smoking Cessation Nicotine Lozenges.. • Nicotine polacrilex formulation • Delivers ~25% more nicotine than equivalent gum dose • Sugar-free, mint or cherry flavor (boxed or POP-PAC) • Contains buffering agents to enhance buccal absorption of nicotine • Available: 2 mg, 4 mg

  30. Pharmacotherapy in Smoking Cessation Nicotine Lozenges.. • Dosage is based on the “time to first cigarette” (TTFC) as an indicator of nicotine addiction

  31. Pharmacotherapy in Smoking Cessation Nicotine Lozenges.. week 1-6week 7-9week 10-12 1 lozenges 1 lozenges 1 lozenges q 1-2 h 1 q 2-4 h 1 q 4-8 h • at least 9 Lozenges/day during the first 6 weeks • no more than 5 lozenges in 6 hrs, 20 lozenges/day • Stop using at the end of 12 weeks

  32. Pharmacotherapy in Smoking Cessation Nicotine Lozenges.. DISADVANTAGES • Gastrointestinal side effects (nausea, hiccups, and heartburn) may be bothersome. ADVANTAGES • Lozenge use may satisfy oral cravings. • The lozenge is easy to use and conceal. • Patients can titrate therapy to manage withdrawal symptoms.

  33. Pharmacotherapy in Smoking Cessation Transdermal Nicotine Patch.. • Nicotine is well absorbed across the skin • Delivery to systemic circulation avoids hepatic first-pass metabolism • Plasma nicotine levels are lower and fluctuate less than with smoking

  34. Pharmacotherapy in Smoking Cessation Transdermal Nicotine Patch..

  35. Pharmacotherapy in Smoking Cessation Transdermal Nicotine Patch..

  36. Pharmacotherapy in Smoking Cessation Transdermal Nicotine Patch.. ADVANTAGES • The patch provides consistent nicotine levels. • The patch is easy to use and conceal. • Fewer compliance issues are associated with patch use. DISADVANTAGES • Patients cannot titrate the dose. • Allergic reactions to the adhesive may occur. • Should not used in patients with dermatologic conditions

  37. Pharmacotherapy in Smoking Cessation Nicotine Nasal Spray.. • Aqueous solution of nicotine in a 10-ml spray bottle • Rapid absorption across nasal mucosa • faster onset of action: (tmax 11–13 minutes) compared to other NRT

  38. Pharmacotherapy in Smoking Cessation Nicotine Nasal Spray.. • One dose = 1 mg nicotine • (2 sprays, one 0.5 mg spray in each nostril) • Start with 1–2 doses per hour • Increase prn to max 5 doses/hr or 40 mg (80 sprays; ~½ bottle) daily • For best results, use at least 8 doses daily for the first 6–8 weeks • Termination: gradual tapering over an additional 4–6 weeks

  39. Pharmacotherapy in Smoking Cessation Nicotine Nasal Spray.. ADVANTAGES • Easy to titrate therapy to rapidly manage withdrawal symptoms. DISADVANTAGES • Nasal/throat irritation may be bothersome. • Nasal spray has higher dependence potential. • Should not use in patients with chronic nasal disorders or severe reactive airway disease.

  40. Pharmacotherapy in Smoking Cessation Nicotine Inhaler.. • Nicotine inhalation system consists of: • Mouthpiece • Cartridge with porous plug containing 10 mg nicotine • Delivers 4 mg nicotine vapor, absorbed across buccal mucosa • May satisfy hand-to-mouth ritual of smoking

  41. Pharmacotherapy in Smoking Cessation Nicotine Inhaler.. • Start with 6 cartridges/day • Increase prn to max of 16 Cartridges/day • Use for min of 3 weeks, max of 12 weeks • Gradual dosage reduction: if needed over additional 6–12 weeks

  42. Pharmacotherapy in Smoking Cessation Nicotine Inhaler.. ADVANTAGES • Easy to titrate therapy to manage withdrawal symptoms. • Inhaler mimics the hand-to-mouth ritual of smoking. DISADVANTAGES • Bothersome throat or mouth irritation. • Cartridges should not be stored in very warm conditions or used in very cold conditions. • Use with caution in patients with underlying bronchospastic disease.

  43. Pharmacotherapy in Smoking Cessation NRT Summary … • Compliance highest with the patch. • Smoking cessation is similar with continuous abstinence rates at 12 weeks : • odds ratio for abstinence with NRT vs. control was 1.77 (95% CI 1.66-1.88) with odds ratio: • 1.66 for gum (at least 48 trials) • 1.81 for patches (at least 30 trials) • 2.35 for nasal spray (at least 4 trials) • 2.14 for inhaled nicotine (at least 4 trials) • 2.05 for nicotine sublingual tablet/lozenge (at least 2 trials)

  44. Pharmacotherapy in Smoking Cessation BUPROPION SRZyban (GlaxoSmithKline); generic • Non nicotine cessation aid • Sustained-release • Antidepressant • Oral formulation • Pregnancy Category C

  45. Pharmacotherapy in Smoking Cessation BUPROPION SR • Clinical effects •  craving for cigarettes •  symptoms of nicotine withdrawal

  46. Pharmacotherapy in Smoking Cessation Bupropion Contraindications: • Seizure disorder • Patients taking • Wellbutrin, Wellbutrin SR, Wellbutrin XL • MAO inhibitors in preceding 14 days • Current or prior diagnosis of anorexia or bulimia nervosa • Patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines)

  47. Pharmacotherapy in Smoking Cessation Bupropion Dosing.. Patients should begin therapy 1 to 2 weeks PRIOR to their quit date to ensure that therapeutic plasma levels of the drug are achieved. Initial treatment • 150 mg po q AM x 3 days Then… • 150 mg po bid • Duration, 7–12 weeks If no significant progress toward abstinence by 7th week, D/C treatment Reevaluate and restart at later date

  48. Pharmacotherapy in Smoking Cessation Bupropion Side Effects Common: • Insomnia (avoid bedtime dosing) • Dry mouth Less common: • Tremor • Skin rash

  49. Pharmacotherapy in Smoking Cessation Bupropion.. ADVANTAGES • Convenient, an oral formulation with twice-a-day dosing. • Beneficial for patients with depression. DISADVANTAGES • Increased seizure risk • Several contraindications and precautions preclude use.

  50. Pharmacotherapy in Smoking Cessation VARENICLINE Chantix (Pfizer) • Nonnicotine cessation aid • Partial nicotinic receptor agonist • Oral formulation • Pregnancy Category C

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