Tobacco cessation fall 2011 Instructor (1)_ For use in lecture (3)

If no significant progress toward abstinence by

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If no significant progress toward abstinence by  seventh week, therapy is unlikely to be effective Discontinue treatment Reevaluate and restart at later date
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BUPROPION SR: SUMMARY DISADVANTAGES The seizure risk is  increased. Several contraindications  and precautions preclude  use in some patients. ADVANTAGES Easy to use oral  formulation. Twice daily dosing  might reduce  compliance problems. Bupropion might be  beneficial for patients  with depression.
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VARENICLINE  Chantix (Pfizer) Nonnicotine  cessation aid Partial nicotinic  receptor agonist Oral formulation  
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VARENICLINE: MECHANISM of ACTION Binds with high affinity and selectivity at  α 4 β 2   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
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VARENICLINE: PHARMACOKINETICS Absorption Virtually complete after oral administration; not affected by  food Metabolism Undergoes minimal metabolism Elimination Primarily renal through glomerular filtration and active  tubular secretion; 92% excreted unchanged in urine Half-life 24 hours
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VARENICLINE: WARNING In 2008, Pfizer added a warning label advising  patients and caregivers:  Patients should stop taking varenicline and contact  their healthcare provider immediately if agitation,  depressed mood, or changes in behavior that are  not typical for them are observed, or if the patient  develops suicidal ideation or suicidal thoughts. 
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VARENICLINE: DOSING Patients should begin therapy 1 week PRIOR to their quit date. The dose is gradually increased to minimize  treatment-related nausea and insomnia. Treatment Day Dose Day 1 to day 3 0.5 mg qd Day 4 to day 7 0.5 mg bid Day 8 to end of treatment* 1 mg bid Initial dose titration * Up to 12 weeks
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VARENICLINE: ADVERSE EFFECTS Common ( 5% and 2-fold higher than placebo) Nausea Sleep disturbances (insomnia, abnormal dreams) Constipation Flatulence Vomiting
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VARENICLINE:  ADDITIONAL PATIENT  EDUCATION Doses should be taken after eating, with a full glass of water  Nausea and insomnia are side effects that are usually  temporary If symptoms persist, notify your health care provider Dose tapering not necessary when discontinuing treatment Stop taking varenicline and contact a health-care provider  immediately if agitation, depressed mood, suicidal thoughts  or changes in behavior are noted
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VARENICLINE: SUMMARY DISADVANTAGES May induce nausea in up to  one third of patients.
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