Jim Thigpen, PharmD, BCPS ETSU Bill Gatton College of Pharmacy.
-
Upload
salma-heslop -
Category
Documents
-
view
218 -
download
1
Transcript of Jim Thigpen, PharmD, BCPS ETSU Bill Gatton College of Pharmacy.
Assisting a Quitter – The Medications Used in Smoking Cessation
Jim Thigpen, PharmD, BCPSETSU Bill Gatton College of Pharmacy
Learning Outcomes
Describe the pharmacotherapy used in smoking cessation
Determine the appropriate therapy to recommend for a specific patient
Describe patient expectations when using smoking cessation products
A Pediatric Disease1….
Extent of harms to children caused by tobacco use and secondhand smoke exposure
Relationship of pediatric tobacco use and exposure to adult tobacco use
Existence of effective interventions to reduce the use
Documented underuse of those interventions
Policy Statement – Tobacco Use: A Pediatric Disease, Pediatrics 124(5), Nov 2009
The role of Pediatricians…. Provide counseling to expectant parents to quit
using tobacco products and avoid SHS exposure during and after pregnancy
Assist new parents in their efforts to continue their tobacco use-abstinence or –cessation efforts after delivery
Counsel parents to reduce or eliminate children’s exposure to SHS
Counsel preadolescents and adolescents to prevent initiation
Counsel adolescents and parents to quit using tobacco
The role of Pediatricians….
85% of parents who smoke consider it acceptable for their child’s pediatrician to prescribe a smoking-cessation medication for them1
In 2005, the American Medical Association adopted a policy statement supporting the practice of pediatricians addressing parental smoking2
American Medical Association H-490.917 Physician Responsibilities for Tobacco Cessation. Adopted June 2005, Chicago IL
What should you expect?
18.4% will quit if you do nothing
23.1% will quit if you intervene Families with children ages 4-17 more
likely Interventions whose primary goal was
cessation Interventions that offered medications Interventions with high follow-up rates
Rosen LJ, Noach MB et al. Parental smoking cessation to protect young children: a systematic review and meta-analysis. Pediatrics 129(1) Jan 2012
Strategies and Evidence
Cessation rates are ↑ when smokers attended two or more sessions of ≥ 20 minutes
Motivating the unwilling patient The five Rs
Relevant reasons to quit Risks associated with continued smoking Rewards for quitting Roadblocks to successful quitting Repetition of the counseling of subsequent
visits
Counseling
There is a consistent relationship between more intensive counseling and abstinence from smoking No counseling (11%) 1 – 3 minutes (14%) 4 – 30 minutes (19%) 31 – 90 minutes (27%)
Counseling should be sympathetic and supportive, not confrontational
1-800-QUIT-NOW (1-800-784-8669
Nonpharmacologic
Cold turkey 5% success
Unassisted tapering 5% success
Assisted tapering QuitKey® Computer-assisted behavior modification▪ 19-24% abstinence rate 1 year after quitting
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
Some basic pharmacology3…. Nicotine is carried by tar particles to the lung alveoli
and then to the brain Nicotine binds with to nicotinic cholinergic receptors
in the brain, leading to neurotransmitter release Tolerance develops with chronic smoking, resulting
in the proliferation of nicotine receptors and permitting higher levels of self-administration of nicotine
A lack of binding to these receptors due to decreased smoking results in withdrawal symptoms
About half of phenotypic variance in tobacco dependence is attributable to genetic influence
Fiore MC, Baker TB. Treating smokers in the health care setting NEJM 2011;365:1222-31
Pharmacologic Methods
Three general classes of FDA-approved drugs for smoking cessation: Nicotine Replacement Therapy (NRT)▪ Gum, patch, lozenge, nasal spray, inhaler
Psychotropics▪ Sustained-release bupropion (Zyban®)
Partial nicotinic receptor agonist▪ Varenicline (Chantix®)
Pharmacotherapy - Pregnancy
The clinical practice guideline states that pregnant smokers should be encouraged to quit without medication based on insufficient evidence of effectiveness and hypothetical concerns NRT products are category D Bupropion is category C Varenicline is category C
PharmacotherapyNot recommended for…..
Smokeless tobacco users No FDA indication
Individuals smoking < 10 cigarettes per day
Adolescents OTC sales are restricted to ≥ 18 NRT use in minors requires a prescription
NRT: Rationale for Use
Reduces physical withdrawal from nicotine
Eliminates the immediate, reinforcing effects of nicotine that is rapidly absorbed via tobacco smoke
Allows patient to focus on behavioral and psychological aspects of tobacco cessation
Use of NRT approximately doubles long-term quit rates relative to placebo
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
NRT Products
Polacrilex gum Nicorette®, generics
Lozenge Nicorette® Lozenge Nicorette ® Mini
Lozenge Generics
Transdermal Patch
Nicoderm CQ ®
Generics
Nasal Spray Nicotrol ® NS
Inhaler Nicotrol ®
Patients should stop using all forms of tobacco upon initiation of NRT
NRT Precautions
Patients with underlying cardiovascular disease Recent myocardial infarction Serious arrhythmias Serious or worsening angina
NRT products may be appropriate for these patients if they are under medical supervision
Nicotine GumNicorette® (GSK); generics
Resin complex Nicotine Polacrilin
Sugar-free chewing gum base Contains buffering agents to
enhance buccal absorption of nicotine
Available in 2mg, 4mg; original, cinnamon, fruit, mint (various), and orange flavors
Nicotine Gum
Dosage based on current smoking patterns:If patient smokes Recommended
strength
≥ 25 cigarettes (1 pack)/day
4 mg
< 25 cigarettes/day 2 mg
Recommended Usage Schedule for Nicotine Gum
Weeks 1 - 6 Weeks 7-9 Weeks 10 - 12
1 piece q 1 – 2 h
1 piece q 2 – 4 h
1 piece q 4 – 8 h
Do not use more than 24 pieces per day
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
Nicotine Gum – Directions
Chew each piece slowly several times
Stop chewing at first sign of peppery taste
“park” gum between cheek and gum
Resume chewing when taste or tingle fades
Return to “park” when taste or tingle resumes
Repeat chew/park until most of the nicotine is gone (≈ 30 minutes)
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
Nicotine Gum
Use at least nine pieces per day Do not eat or drink anything for 15 minutes
before or while using nicotine gum Nicotine polacrilex is buffered to pH 8.5 Acidic beverages may reduce the pH of the
saliva, reducing the buccal absorption of nicotine▪ Coffee, wine, juices, soft drinks
Chewing gum too rapidly can cause excessive nicotine release Lightheadedness, N/V, irritation, hiccups, reflux
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
Nicotine Gum
Advantages Satisfy oral
cravings Might delay
weight gain (4 mg)
Therapy can be titrated to manage withdrawal symptoms
Flavors
Disadvantages Need for frequent
dosing Dental work Must use proper
technique Gum might not be
socially acceptable
Nicotine Lozenge
Dosage is based on “time to first cigarette” as an indicator of nicotine dependence Use the 2 mg strength if you smoke the
first cigarette more than 30 minutes after waking
Use the 4 mg strength if you smoke the first cigarette less than 30 minutes after waking
Use is essentially identical to gum Dosing intervals, titration, use, etc
Transdermal nicotine patchNicoderm® CQ, generics
Nicotine is well absorbed across the skin
Delivery to systemic circulation avoids hepatic first pass effect
Plasma nicotine levels are lower and fluctuate less than with smoking
Treatment Estimated abstinence rate
Placebo 13.8%
Nicotine patch (6-14 weeks)
23.4%
Nicotine patch (> 14 weeks)
23.7%
Transdermal nicotine patch
Product Light Smoker Heavy Smoker
Nicoderm® CQ ≤ 10 cigarettes/dayStep 2 (14 mg X 6 weeks)Step 3 (7 mg X 2 weeks)
10 cigarettes/dayStep 1 (21 mg X 6 weeks)Step 2 (14 mg X 2 weeks)Step 3 (7 mg X 2 weeks)
Generic ≤ 10 cigarettes/dayStep 2 (14 mg X 6 weeks)Step 3 (7 mg X 2 weeks)
10 cigarettes/dayStep 1 (21 mg X 4 weeks)Step 2 (14 mg X 2 weeks)Step 3 (7 mg X 2 weeks)
Transdermal nicotine patch
Choose an area of skin on the upper body or upper outer part of the arm
Make sure the skin is clean, dry, hairless, and not irritated
Apply patch to different area each day
Do not use same area again for at least 1 week
Transdermal nicotine patch
Side effects to expect in first hour: Mild itching Burning Tingling
Additional possible side effects: Vivid dreams or sleep disturbances Headache
Up to 50% will have local skin reactions
Nicotine nasal sprayNicotrol® NS (Pfizer)
Aqueous solution of nicotine (10 ml) Each metered dose delivers
50 mcl spray 0.5 mg nicotine
≈ 100 doses/bottle Rapid absorption across nasal mucosa More rapid onset compared to gum, patch, or
inhaler 26.7% 6-month abstinence rate
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 maximum dosage of
5 doses per hour or 40 mg (80 sprays; ½ bottle) daily
For best results, patients should use at least 8 doses daily for the first 6-8 weeks
Gradual tapering over an additional 4-6 weeks
Nicotine inhaler
Start with at least 6 cartridges/day during the first 3-6 weeks of treatment Increase to a maximum of 16 cartridges
per day In general, use 1 cartridge every 1-2
hours Recommended duration of therapy is
3 months Gradually reduce daily dosage over
the following 6-12 weeks
Nicotine inhaler
During inhalation, nicotine is vaporized and absorbed across oropharyngeal mucosa
Inhale into back of throat or puff in short breaths
Nicotine in cartridges is depleted after about 20 minutes of active puffing Cartridge does not have to be used all at
once Open cartridge retains potency for 24
hours Mouthpiece is reusable; clean
regularly
Nicotine inhaler
Side effects associated with the nicotine inhaler include: Mild irritation of mouth or throat Cough Headache Rhinitis Dyspepsia
Severity generally rated as mild, and frequency of symptoms declined with use
Bupropion SRZyban®, generics
Non-nicotine Sustained release antidepressant Oral only
Estimated abstinence rate is 24.2%
Bupropion
Atypical antidepressant thought to affect levels of dopamine and norepinephrine
Clinical effects ↓ craving for cigarettes ↓ symptoms of nicotine withdrawal
Fiore MC, Jaen CR, Baker TB, et al. (2008) Treating tobacco use and dependence, 2008 Update. Clinical Practice Guideline. Rockville, MD: US DHHS
Bupropion
Contraindications/Precautions History of epilepsy Other sources of bupropion
(Wellbutrin®) MAO inhibitors in preceding 14 days Prior diagnosis of anorexia, bulemia,
other psychiatric disorders (suicide risk) Abrupt discontinuation of
benzodiazepines, sedatives, or alcohol (↑ seizure risk)
Hepatic disease
Bupropion
Patients should begin therapy 1 – 2 weeks prior to their quit date to ensure target plasma levels
150 mg once daily for 3 days, then BID Duration is 7-12 weeks
Common side effects include: Insomnia, dry mouth
Less common Tremor, skin rash
Varenicline (Chantix®)
Binds with high affinity and selectivity to α4β2 neuronal nicotinic acetylcholine receptors Stimulates low-level agonist activity Competitively inhibits binding of nicotine
Clinical effects ↓ symptoms of nicotine withdrawal Blocks dopaminergic stimulation responsible for
reinforcement & reward associated with smoking
Varenicline
Neurophychiatric symptoms and suicidality Changes in mood Psychosis/hallucinations/paranoia/
delusions Homicial ideation/hostility Agitation/anxiety/panic Suicidal ideation or attempts Completed suicide
Varenicline
Patients should begin therapy 1 week prior to their quit date
Treatment Day Dose
Day 1 to day 3 0.5 mg daily
Day 4 to day 7 0.5 mg BID
Day 8 to end of treatment
1 mg BID
Verenicline
Adverse Effects (> 5% and x2 higher than placebo) Nausea Sleep disturbances Constipation Flatulance Vomiting Vivid dreams (< 5%)
Second-line therapies
Clonidine α2-adrenergic agonist that reduces
sympathetic outflow that reduces the autonomic symptoms of withdrawal
May be beneficial Nortriptyline
TCA May be beneficial
Long-term (> 6 month) quit rates
1815.8 16.1
23.9
17.119 20.2
0
5
10
15
20
25
Gum Lozenge Inhaler Verenicline
Patch
Nasal Spray
Bupropion
Combination Pharmacotherapy
Combination NRT Patch + gum/inhaler/nasal spray
Bupropion + Nicotine patch
Comparative Daily Costs
Gum Lozenge Patch Inhaler Nasal Spray
Bupropion
Verencline
$4.68 $4.95 $3.89 $7.02 $3.92 $7.78 $4.70
$2.16 $3.24 $1.90 $3.62