Rx for Change: Clinician-Assisted Tobacco Cessation

Metrix training notes by James Lee

Introduction to Smoking

ventilation holes used to decrease tar yields

Smokers may cover up holes with lips, rendering
them useless

Epidemiology of Tobacco Use

May result in smoking more since cigarettes are

light

Cigarette smoking is the chief, single, avoidable

cause of death in our society and the most im portant
pulic health issue of our time - C. Everett Koop,
MD, former US Surgeon General

15 mg vs 10 mg if used correctly
Smoking in Movies: pervasive

Worldwide tobacco use prevalence

10.9 smoking incidents per hour

3/4 box-office hits
There is causal relationship b/w exposure to smoking
in movies and youth smoking initiation

Men smoke > Women

1 in 3 cigarettes smoked in China
Adult per-capita consumption tobacco

Compounds in smoke: 4,800 compounds, including 11

human carcinogens

Up to 1920s: Chewing, cigars, pipes

Since then: Cigarettes have taken over
All forms are harmful

Gases: CO, hydrogen cyanide, ammonia, benzene,

formaldehyde
Particles: Nicotine, nitrosamines, lead, cadmium,
polonium-210
NB Nicotine is the addictive component, does no
cause ill health effects of tobacco use

Adult smoking has declined 1955 to 2003, but rate of

cessation has been slowing.
20.8 of adults are current smokers
70% want to QUIT
Race: Natives > Black > White > Hispanic > Asian

Premature death attributable to smoking

Education: GED > no diploma > high school grad >

college > undergrad > grad

1 in 5 deaths
437,902 deaths annually
2005: 50,000 persons died due to 2nd hand smokke
exposure

12th-grade 30-day use: whites > hispanic > black; 2007

21.6 of 12th graders had smoked 1 or more cigarettes in
last 30 days
Adolescents experiment; 16.9 yrs is average age of
first time use
Adolescent smoking has declined, but rate of decline
has slowed

Economic impact
Medical expenditures 1995-1999: $ 75.488 billion
Societal impact $ 7.18 per pack

Tobacco industry: $18 per $1

4 major conclusions of 2004 surgeon general report

$13.11 billion spend in US in 2005

Causal relation: More advertising spending $ = increased
tobacco use

Executives have denied addictive nature of tobacco for

many years

Smoking is bad for almost every organ

Quitting smoking is good for long-term
No benefit to light cigs
More diseases known to be caused by cigs

Industry documents (http://legacy.library/ucf.edu) shows

otherwise

There is no safe level of 2nd hand smoke

Mild / Light / Ultralight cigarettes

Smoke-free workplace laws vary by country and state.

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Nicotine Pharmacology and Principles of Addiction

Epidemiology Summary
About 1 in 5 currently smoking
Nearly 500,000 deaths attributed to smoking annually
$ 157.7 billion: smoking costs per year. Lifetime financial
costs of smoking >$ 500,000 for a heavy smoker
At any age, benefits to quitting smoking
Biggest opponent to tobacco control efforts is the tobacco
industry

C* Cigarettes + other forms of tobacco are addicting * Tobacco

dependence = chronic disease; comparable to Heroin and
cocaine addiction * Nicotiana tabacum - nicotine is a natural,
liquid alkaloid

Pharmacokinetics: Abs, Dist, Meta, Excr

Absorption of nic is pH-dependent: crosses membranes
in non-ionized form (basic environment)

Pathophysiology of Tobacco-Related
Disease

7.3-7.5, 31% nic is un-ionized and readily crosses

membranes
Mouth 7.0
Skin: readily absorbed
Lung: 7.4

Adverse effects: harms almost every organ, many diseases

1. Cancer
2. CV disease

Atherogenesis
Thrombosis
Increased O2 demand, decreased delivery

Inhalation is effective means, 10-20c for nic to reach brain

Metabolized primarily in liver, some kidney / lung
10-20% excretion in urine; 70-80% converted to cotinine
Half life: Nicotine: 2 hr, Cotinine: 16 hr
Cotinine used as a marker for 2nd hand smoke

3. Acute and Chronic Respiratory Disease

Pharmacodynamics: Actual effects of drugs

Inflammation, pneuomonia
Reduced lung fct, poor asthma control, COPD, repiratory symptoms (cough, phlegm, wheezing, dyspnea)
COPD pathogenesis: Airway narrowing, fibrosis, inflammatory cells, protease / anti-protease imbalance,
oxidative stress

Neurochemical effects
Dopamine, NE, Ach, Glutamate, Serotonin, endorphin, GABA
Biology of addiction
Chronic condition, not simply a bad habit
Increased Dopamine release activates the dopamine
reward pathway
Withdrawal symptoms after 1 day
Chronic nicotine > increased receptors in CNS, ie
tolerance
Tobacco users tend to titrate tobacco intake to maintain constant level in body

4. Reproductive
Fertility issues, preterm delivery, infant mortality
Gonadotropin release > Impaired implantation
5. Osteoporosis
Osteoblast toxicity, increased resorption due to low
PTH / D + reduced Ca2+ absorption, early meno,
low weight, vascular insufficiency

Fagerstrom test for nicotine dependence

6. Periodontitis
7. Ocular Disease
8. Post-operative complications

Factors contributing to tobacco use

Environment, Physiology, Pharmocology
Conditioned cues become a major factor in relapse

Surgical wound
Respiratory complications

Nicotine Pharmacology and Addiction Summary

Pathophysiology Summary

Tobacco use harms almost every organ, adverse health

outcomes
Mechanisms for disease not established fully; disruption
of many normal cellular processes known
Cessation efforts essential to stop disease progression
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Tobacco effectively delivers nicotine

Nico is highly addictive
Nico activates dopamine reward pathway
Self-regulation / titration prevent withdrawal and maintain pleasurable effects

Forms of Tobacco

8 doses per day age, followed by tapering

Rapid absorption (faster onset than gum / patch /
lozenge)
Contraindications: chronic nasal disorder or airway
disease

Cigarettes are the most popular

Other types increasing in popularity
All tobacco harmful
Attn to all forms needed

Nicotine inhaler
4mg inhaled as vapor + menthol to decrease irritation
Mouthpiece resembles cigarette!
Recommended to start with 6 cartridges/day average,
increase prn, 1 per 1-2 hrs average

Aids for Cessation

Methods for quitting
1. Non-pharma: counseling, behavioral, tapering,
CAMs
Should be used with everyone trying to quit
2. Pharma: FDA-approved medications
NRT, psychotropics (bup), partial nicotinic receptor agonists (Varenicline)

Buproprion SR

Non-nicotine cessation aid

Sustained release oral anti-depressant
May affect NT levels
Contraindicated in seizure disorders
Possible suicide / neuropsychiatric risk
150 mg po q AM x 3 days, then 150 mg po bid for
7-12 wks
If no sig progress, stop treatment

Combination of non-pharma and pharma are more

effective than either alone.
Medications significantly improve success rates

Varenicline

Contraindications: Pregnant, smokeless users, light

smokers, adolescents

Oral partial nicotinic receptor agonist

0.5 and 1.0 mg dose per tablet
Binds to 42 nictoinic ACh receptors with high
affinity
Stims low-level agonist activity
Possible suicide / neuropsychiatric risk

Gum
4 mg more effective than 2 mg, contingent on baseline
smoking rate (25 cig / day)
Fixed schedule is better than PRN
Chewing technique critical to proper release
Too fast may cause hiccip, heartburn, gastric
upset
Avg 9 pieces a day, drink only water,

Second-Line Therapies: Clonidine and Nortriptyline

Clonidine: Reduce Autonomics
Nortriptylene

Lozenge

Herbal drugs

2 and 4 mg doses
25% more delivery than equivalent gum dose
Time to first cig TTFC is used to establish dose
(30 min after waking)
Fixed schedule is better than PRN
Dissolves in 10 min, let it dissolve slowly
Avg at least 9 lozenges a day

Lobeline
Compliance is key for quitting
Costs: Inhaler and Bupropion higher than cost of ciggarettes

Transdermal patch
Nicotine absorbs across skin to reach systemic circulation
7, 14, 21 mg dosages
Dosing varies by avg # cigs / day
No evidence indicates that gradual weaning better
than abrupt quit
Must wait 1 wk before using same patch of skin
Nasal spray
Nicotrol NS (Pfizer)
100 doses / 10-ml bottle, 50 mcL spray / 0.5 mg
nicotine
2 sprays (1/nostril) yields 1 mg per dose
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