SMOKING CESSATION
Dr/Radwa Maher,PhD
Lecture of Clinical Pharmacy
Ain Shams University
Outline
• Tobacco dependence: chronic disease that often requires repeated
intervention and multiple attempts to quit, is characterized by psychological
dependence (addiction to nicotine) and behavioral habit of using tobacco.
• Nicotine, a chemical that meets the criteria for an addictive substance:
(a) Induces psychoactive effects.
(b) it is used in a highly controlled or compulsive manner.
(c) behavioral patterns of tobacco use are reinforced by the pharmacologic
effects of nicotine.
❑Nicotine is absorbed and passes through the blood-brain barrier(within
seconds) contributes to its addictive nature.
Nicotine Pharmacology
• Nicotine stimulates the release of several neurotransmitters:
Nicotine binds to
• pleasure specific acetylcholine
Dopamine
receptors (mainly
Acetylcholine • cognitive enhancement alpha4beta2 nicotinic
acetylcholine
Ach, NE • Arousal receptor) in the
nucleus accumbens
DA, NE, 5-HT • Appetite suppression
area of the forebrain
Glutamate • Learning, memory enhancement which stimulate the
release of
5-HT • Mood Modulation neurotransmitters.
β-endorphin and GABA • reduction of anxiety and tension
Consequences
• Nicotine addiction is the second-leading cause of death
worldwide.
• The important causes of smoking-related mortality are
atherosclerotic vascular disease, cancer, and chronic
obstructive pulmonary disease (COPD).
Benefits of Quitting
• Improvements in pulmonary function, circulation, and
2W-3M ambulation.
• The excess risk of coronary heart disease is reduced to
1 Year half that of continuing smokers.
• The risk of stroke is reduced to a rate similar to that of
5-15 Y people who are lifetime nonsmokers
• Chance of dying of lung cancer is half that of continuing
smokers, risk of developing mouth, throat, esophagus,
10-15Y bladder, kidney, or pancreatic cancer is decreased.
Nicotine withdrawal symptoms
• Caused by suddenly stopping nicotine supply. Nicotine
withdrawal can manifest itself in the first four to twelve hours
after stopping smoking.
• The symptoms vary depending on the individual:
✓Some smokers feel withdrawal more intensely than others.
• All these manifestations are temporary, reaching maximum
intensity in the first 24 to 72 hours and decreasing over 3-4
weeks.
Nicotine withdrawal symptoms
• Symptoms include:
✓ Acute/uncontrollable need to smoke (craving)
✓ Irritability / aggression / anger;
✓ Anxiety;
✓ Restlessness;
✓ Tiredness;
✓ Increased appetite;
✓ Difficulty concentrating;
✓ Depression;
✓ Headaches;
✓ Night time awakenings;
✓ Light headedness/dizziness.
Assisting Patients With Quitting
BEHAVIORAL PHARMACOTHERAPY
COUNSELING OPTIONS
STRATEGIES “5 A’s”
Assisting Patients With Quitting Counseling
1. BEHAVIORAL COUNSELING STRATEGIES “5 A’s” for tobacco
cessation
Asking Advising Assessing Assisting Arranging
Increase
motivation
to quit
Strategies for working with patients who are not ready to
quit involve enhancing motivation to quit, and this can be
accomplished by applying the “5 R’s”
Enhancing Motivation to Quit: The “5 R’s” for Tobacco Cessation
Counseling
Relevance—Encourage patients to think about the reasons why quitting is important.
Risks—Ask patients to identify potential negative health consequences of smoking.
Rewards—Ask patients to identify potential benefits that they anticipate from quitting.
Roadblocks—Help patients identify barriers to quitting and assist in developing coping strategies .
Repetition—Continue to work with patients who are successful in their quit attempt. Discuss
circumstances in which smoking occurred to identify the trigger(s) for relapse. Repeat interventions
when possible.
5 Rs
Stages of change for smoking cessation
Pharmacological Therapy
• According to the seminal tobacco use clinical practice
guideline, there are seven first-line medications available to
treat nicotine use disorders:
✓Decrease withdrawal symptoms
✓Decrease Craving
5 formulations of Bupropion
NRT Varenicline
Nicotine Replacement Therapy
❑ Reduce the physical withdrawal symptoms associated with
tobacco cessation while the patient focuses on modifying his
or her behavior and coping with the psychological aspects of
quitting.
❑Onset of action for NRT is not as rapid as that of nicotine
obtained through smoking, patients become less accustomed
to the nearly immediate, reinforcing effects of inhaled nicotine.
The maximum
Gum number of pieces of
gum is 24
pieces in 24 hours.
• Dose and Duration
• Patients who smoke 25 cigarettes/day or more should use the 4-
mg dose.
• Those who smoke < than 25 cigarettes should use the 2-mg dose.
• One piece of gum should be used every 1–2 hours for the first 6
weeks of therapy,
• Followed by 1 piece every 2–4 hours for weeks 7–9,
• Then 1 piece every 4–6 hours for weeks 10–12.
• Total Duration 12 weeks
Gum
• Patient counselling
• Chew each piece slowly, Park between cheek and gum when
peppery or tingling sensation appears (∼15–30 chews) then
resume chewing when tingle fades. Repeat chew and park
steps until most of nicotine is gone (tingle does not return;
generally 30 minutes)
• Park in different areas of mouth
• No food or beverages 15 minutes before or during use
Gum
• Side effects:
• Sore mouth, hiccups, stomachache, dyspepsia, insomnia
• Warnings and Precautions:
• Pregnancy category D
• CV risks: Recent (< 2 weeks) MI, arrhythmias, unstable angina
Lozenge
• Dose and Duration
• First cigarette≤30 minutes after waking: 4mg
• First cigarette>30 minutes after waking: 2mg
• Weeks 1–6: 1 lozenge every 1–2 hours
• Weeks 7–9: 1 lozenge every 2–4 hours
• Weeks 10–12: 1 lozenge every 4–8 hours
• Maximum, 20 lozenges/day
• Duration: up to 12 weeks
Lozenge
• Patient counselling
• Allow to dissolve slowly (20–30 minutes )
• Nicotine release may cause a warm, tingling sensation
• Do not chew or swallow
• Occasionally rotate to different areas of the mouth
• No food or beverages 15 minutes before or during use
Lozenge
• Side effects:
• Hiccups, cough, heartburn, nausea, headache, insomnia
• Warnings and Precautions:
• Pregnancy category (not evaluated)
• CV risks: Recent (< 2 weeks) MI, arrhythmias, unstable angina
Transdermal Patch (NicoDerm)
Dosing Patient Counseling
• >10 cigarettes/day: • May wear patch for 16 hours if
21 mg/day ×4 weeks patient experiences sleep
14 mg/day×2-4 weeks disturbances (remove at bedtime)
7 mg/day×2-4 weeks
• ≤10 cigarettes/day:
14 mg/day ×6 weeks
7 mg/day×2 weeks
• Duration: 8–10 weeks
Transdermal Patch (NicoDerm)
Precautions, Warnings, and
Adverse Effects Contraindications
• Local skin reactions (erythema, • Recent (≤2 weeks) myocardial
pruritus, burning) infarction
• Headache • Serious underlying arrhythmias
• Sleep disturbances (insomnia, • Serious or worsening angina
abnormal or vivid dreams); pectoris
associated with nocturnal
nicotine absorption • Pregnancy and breast-feeding
• Adolescents (<18 years)
Nasal Spray (Nicotrol NS)
Dosing Patient Counseling
• 1–2 doses/hour (8–40 • Do not sniff, swallow, or inhale
doses/day) through the nose as the spray is
being administered
• One dose=2 sprays (one in each
nostril); each spray delivers 0.5 • The pump must be primed until a
mg . fine spray is visible (about six to
eight times).
• Maximum 5 doses/hour or 40 • Upon administration, the patient
doses/day should tilt the head back slightly
• For best results, initially use at and insert the tip of the bottle into
least 8 doses/day the nostril as far as is comfortable.
• After 6 to 8 weeks, the dose • The spray increases the likelihood
should be gradually decreased of tearing, coughing, and sneezing,
so patients should wait 5 minutes
during an additional 4 to 6 weeks. before driving or operating heavy
• Duration: 3–6 months. machinery.
Nasal Spray (Nicotrol NS)
Precautions, Warnings, and
Adverse Effects Contraindications
• Nasal or throat irritation (hot, • Recent (≤2 weeks) myocardial
peppery, or burning sensation) infarction
• Rhinitis • Serious underlying arrhythmias
• Tearing • Serious or worsening angina
• Sneezing pectoris
• Cough • Underlying chronic nasal
• Headache disorders (rhinitis, nasal polyps,
sinusitis)
• Severe reactive airway disease
• Pregnancy and breast-feeding
• Adolescents (<18 years)
Oral Inhaler (Nicotrol Inhaler)
Dosing Patient Counseling
• 6–16 cartridges/day • Nicotine in cartridge is
Individualize dosing; initially depleted after 20 minutes of
use1 cartridge every 1–2 hours active puffing
• Best effects with continuous • Inhale into back of throat or
puffing for 20 minutes puff in short breaths
• Initially use at least 6 • Do NOT inhale into the lungs
cartridges/day (like a cigarette) but “puff” as if
• Duration: 3–6 months lighting a pipe
• Open cartridge retains potency
Each puff delivers 4 mg. for 24 hours
Each cartridge delivers • No food or beverages 15
80 inhalations.
minutes before or during use
Oral Inhaler
Precautions, Warnings, and
Adverse Effects Contraindications
• Mouth or throat irritation • Recent (≤2 weeks) myocardial
• Cough infarction
• Headache • Serious underlying arrhythmias
• Rhinitis • Bronchospastic disease
• Dyspepsia • Pregnancy and breast-feeding
• Hiccups • Adolescents (<18 years)
SUSTAINED-RELEASE BUPROPION
• Atypical antidepressant that acts as a nicotine receptor antagonist that
block the reuptake of DA and NE in the CNS.
• It reduces cravings for nicotine and withdrawal symptoms.
• SR Bupropion doubles the long-term abstinence rate when compared
with placebo.
Bupropion SR (Zyban)
Dosing Patient Counseling
• 150 mg PO every morning ×3 • Avoid bedtime dosing to
days, then increase to 150 mg minimize insomnia
PO BID • Dose tapering is not necessary
• Do not exceed 300 mg/day • Can be used safely with NRT
• Begin therapy 1–2 weeks before (FDA approved)
quit date
• Allow at least 8 hours between
doses
• Duration: 7–12 weeks, with
maintenance up to 6 months in
selected patients
Bupropion SR
Precautions, Warnings, and
Adverse Effects Contraindications
• Insomnia • Concomitant therapy with
medications or medical conditions
• Dry mouth known to lower seizure threshold
• Severe hepatic cirrhosis
• Nervousness or difficulty • Pregnancy and breast-feeding
concentrating • Adolescents (<18 years)
• Rash • Warning: Black-boxed warning for
neuropsychiatric symptoms
• Constipation
• Seizures (risk is∼0.1%) • Contraindications: Seizure disorder,
Concomitant bupropion (e.g.,
• Neuropsychiatric symptoms Wellbutrin) therapy, Current or prior
diagnosis of bulimia or anorexia
nervosa, Simultaneous abrupt
discontinuation of alcohol or
sedatives (including benzodiazepines),
Monoamine oxidase inhibitor therapy
in previous 14 days.
VARENICLINE
• Partial agonist that binds with high affinity and selectivity at
α4β2 neuronal nicotinic acetylcholine receptors + competitive
inhibitor of nicotine binding.
• The partial agonist activity induces modest receptor stimulation,
leading to increased dopamine levels, which attenuates the
symptoms of nicotine withdrawal.
• In addition, by blocking the ability of nicotine to activate α4β2
nicotinic acetylcholine receptors, varenicline inhibits the surges
of dopamine release that are believed to be responsible for the
reinforcement and reward associated with smoking.
• Use of varenicline more than doubles the long-term
abstinence rate when compared in clinical trials with placebo.
Varenicline (Chantix)
Dosing Patient Counseling
• Days 1–3: 0.5 mg PO every • Take dose after eating with a
morning
full glass of water
• Days 4–7: 0.5 mg PO BID
• Weeks 2–12: 1mgPO BID • Dose tapering is not necessary
• Begin therapy 1 week before quit • Nausea and insomnia are side
date.
effects that are usually
• Alternatively, the patient can begin
therapy and then quit smoking temporary.
between days 8 and 35 of • Patients should be advised to
treatment. discontinue varenicline and
• Dosing adjustment is
recommended for patients with contact their health care
severe renal impairment provider immediately if they
• Duration: 12 weeks; an additional experience agitation, hostility,
12-week course may be used in depressed mood, or changes in
selected patients
behavior.
Varenicline (Chantix)
Adverse Effects Precautions, Warnings, and
Contraindications
• Nausea • Severe renal impairment
• Sleep disturbances (insomnia, (dosage adjustment is
necessary)
abnormal or vivid dreams)
• Pregnancy (category C) and
• Constipation breast-feeding
• Flatulence • Adolescents (<18 years)
• Vomiting • Warnings: Black-boxed warning
• Neuropsychiatric symptoms for neuropsychiatric symptoms
• Safety and efficacy have not
been established in patients
with serious psychiatric illness
• Cardiovascular adverse events
in patients with existing
cardiovascular disease
