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- Nicotine is responsible for the addiction, but other chemicals
contribute to its addictive effects1
- Smoking cigarettes with lower tar and nicotine provides no health
benefit compared to regular cigarettes1
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- Nicotine binding causes an increase in dopamine release1
- Dopamine gives feelings of pleasure and calmness2
- The dopamine decrease between cigarettes leads to withdrawal symptoms of
irritability and stress3,4
- The smoker craves nicotine to release more dopamine to restore pleasure
and calmness2,3
- Chronic exposure to nicotine causes desensitization and compensatory
receptor upregulation2,5
- Withdrawal symptoms occur in the prolonged absence of nicotine (4-6h),
as nicotine levels decrease, and receptors become resensitized1
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- The majority of smokers are motivated to quit2
- Most try to quit without pharmacological assistance3
- 87% of current smokers have tried to quit smoking at least once before4
- 19% of smokers report craving is the most common reason why quitting
smoking is considered difficult4
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- Smoking addiction has two main components that need to be addressed: one
related to the pharmacological action of inhaled nicotine and the other
related to behavioural factors1-3
- Advice and behavioural support increase the chances of quitting
successfully4,5
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- Identify and document tobacco use
- In a clear, strong, personalized manner, urge smoker to quit
- Is the smoker ready to make a quit attempt?
- Use counselling and pharmacotherapy to help him/her quit
- Schedule follow-up contact
- Preferably within 1 week after the quit date
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- Nicotine replacement therapy (NRT)
- Bupropion SR
- Varenicline
- A new smoking cessation aid
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- ACTIVITY 1: Partial agonist
- Varenicline binds to the receptor, partially stimulating dopamine
release
- ACTIVITY 2: Antagonist
- Because varenicline is bound to the receptor, it prevents the binding
of nicotine
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- Indicated for smoking cessation treatment in adults in conjunction with
smoking cessation counselling
- Treatment period is 12 weeks
- An additional course of 12 weeks of treatment may be considered for
patients who have successfully quit at the end of 12 weeks
- Varenicline is supplied for oral administration in 2 strengths: 0.5 and
1.0 mg
- To optimize therapy success, patients should be titrated up to the
maximum recommended dose of 1.0 mg BID, using the following 1-week
titration schedule:
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- Established safety and tolerability profile assessed in approximately
2,300 subjects
- In general, onset of adverse events occurred in the first few weeks of
therapy and severity was generally mild to moderate
- The most commonly observed adverse events associated with varenicline
(>5% and twice the rate seen in placebo-treated patients) were
nausea, abnormal dreams, constipation, flatulence, and vomiting
- Discontinuation rate due to nausea was only 2.7% (vs. 0.6% for placebo)
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- Identify patients who are motivated to quit smoking, since motivated
quitters are more likely to succeed1,2
- Prescribe a 12-week course of CHAMPIX treatment2
- Have patients set a target quit date 1-2 weeks into treatment2-4
- The pivotal studies utilized a day 8 quit date3,4
- Reassess patients after 12 weeks
- For those who were successful, an additional course of 12 weeks may be
considered to help them stay quit2
- Encourage enrollment in a patient support program
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