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60 Cards in this Set
- Front
- Back
What is the mechanism of action for nicotine?
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- binds to nicotinic acetylcholine receptors in the brain and leads to stimulation and depression of the central and peripheral nervous system
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How do low doses of nicotine affect cognitive function and alertness?
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produces heightened alertness and increased cognitive function
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What do high doses of nicotine do to the brain?
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stimulates the “reward” center in the limbic system of the brain mediated via dopamine and leads to
a) Cravings and feeling of positive reward after cigarette smoking b) Enhanced mood and performance |
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What are the three consequences on the brain/body of nicotine use?
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1.Physical dependence - when the body becomes dependent or accustomed to the presence of a substance and abrupt removal of the substance can produce withdrawal. Physical dependence does not equal addiction.
2. Tolerance - the need to increase the amount smoked to achieve the same effects. 3.Withdrawal - abrupt cessation can lead to withdrawal within 24 hours (Sx listed on page 2) |
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What are the behavioral aspects of smoking?
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1.Psychological dependence or addiction - abnormal behaviors that can include compulsive use, little self-control regarding use, cravings, and continued use despite knowledge of harm.
2. Smoking becomes associated with: i.Daily routines (e.g. morning coffee, alcoholic drink, end of a meal) ii.Events and situations iii.Management of stress, anger, and anxiety 3.In order to stop smoking, a smoker must learn new coping skills and break old patterns (self assessment for pt. example on page 2) |
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What are the three current approaches to smoking cessation?
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1. General Approach (5 A's)
2. Behavioral Modification therapy 3. Pharmacological |
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What are the 5 A's of smoking cessation included in the general approach?
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1.Ask about tobacco use: identify and document status for each patient at each visit
2. Advise: urge every tobacco user to quit 3. Assess: willingness to quit 4.Assist in quit attempts: by providing cessation therapies (behavioral + pharmacotherapy) 5. Arrange follow-up within the first week after the quit date to evaluate medications for efficacy and adverse effects |
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For patients unwilling to quit, what interventions can be used to increase future quit attempts?
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- The 5 R’s
• Ask the patient to identify why quitting is relevant • Have the patient identify risks associated with smoking • Have the patient identify rewards of smoking cessation • Ask the patient to identify roadblocks to cessation • Repeat motivation each time the patient visits clinic (this are part of Assist on the 5 A's) |
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What are the five points to Behavioral Modification Theory?
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1. offer to everyone ready to quit
2. efficacy is augmented by pharmacologic therapies 3. necessary to change behaviors/habits 4. Counseling 5. social support inside and outside of treatment |
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What does pharmacological therapy provide to patient?
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only prevents withdrawal and cravings while individuals learn to modify lifestyle behaviors
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What are the four important aspects of pharmacotherapy with smoking cessation?
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a. Should be used with everyone attempting to quit unless contraindicated
b. Should always be used with behavioral modification c. Increases long-term smoking abstinence rates d. Important to set a quit date |
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What are the five drugs classified as Nicotine Replacement therapy?
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1. GUm
2. Lozenges 3. Pathc 4. Nasal Spray 5. Inhaler |
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What are the adverse effects of NRT?
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1. nausea
2. light headedness |
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Is NRT gum OTC/Rx, and what is a specific contraindications for use?
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1.OTC
2. TMJ is contraindication |
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What are side effects of gum use?
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mouth soreness, dyspepsia, hiccups, jaw ache
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What are 3 helpful guidelines to follow for gum use?
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1. Limit to <24/day
2. maximal benefit is received from SCHEDULED use versus waiting for a craving 3.. PROPER CHEWING TECHNIQUE IS ESSENTIAL! Chew and Park! |
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What is the duration of use for gum?
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12 weeks. (short acting MOA)
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Are lozenges OTC/RX?
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OTC
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What are directions and duration of tx for lozenges?
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1.DO NOT CHEW
2. avoid food or drink 15 minutes before/during 3. duration of tx=12 weeks |
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what are adverse effects of lozenges?
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heartburn, hiccups, coughing
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Is nicotine patch OTC/RX and what is it's duration of action?
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1. OTC
2. long acting- releases a constant amount nicotine slowly through the skin |
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What are directions for patch?
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a) Worn for 24 hours, removed and replaced each morning
b) Apply a patch as soon as you wake up c) Remove old patch and apply new patch each morning to a hairless location between the neck and waist (rotate site to prevent irritation) (not specific on objectives, but was bolded) |
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What are Side effects and Tx duration for the patch?
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insomnia, vivid dreams, 50% of subjects develop local skin irritation
a)Local irritation - rotate patch site, may also use 1% hydrocortisone cream b)Insomnia - remove the patch prior to bedtime TX duration- 10 weeks |
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Drug class of Nicotrol NS
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Nicotine Replacement Therapy
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Dosage form of Nicotrol NS
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Rx- Nasal spray
Instill one (0.5mg) spray to each nostril (1mg total). Initially, use 1-2 doses/hour. Increase as needed for symptomatic relief. (Max 40 doses/day, 5 doses/hour) |
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Mechanism of action of Nicotrol NS
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Delivers aqueous nicotine solution to nasal mucosa
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duration of action (long vs short)
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Short?
Most rapid nicotine delivery system - peaks within 10 minutes |
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place in therapy for Nicotrol NS (contraindications)
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Contraindications: reactive airway disease (asthma)
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Special considerations Nicotrol NS
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Produces higher peak nicotine levels than other forms of NRT leading to the highest dependence potential. 20% of patients use longer than recommended due to dependence.
Due to higher peak levels, this form may be most effective for those who are most addicted Cost= $200.00 per bottle |
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Adverse effects of Nicotrol NS
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Moderate to severe nasal irritation
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Drug class for Nicotrol
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Nicotine replacement therapy
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Dosage form for Nicotrol
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Inhaler
-1 inhalation= 1 dose -Used as needed to control cravings during the day |
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Is Nicotrol OTC or Rx?
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Rx
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Mech of action for Nicotrol
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Delivers nicotine vapor (not smoke) into mouth and throat
Nicotine absorbed in oral mucosa with minimal delivery to lung |
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Special considerations for Nicotrol
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a) High administration burden (puffs/hour)
b) Requires deep and vigorous inhalations c) Potential benefit in those needing the fix of hand to mouth movement d) expense- $200.00 for 1 box of 168 cartridges (recommended 6-16 cartridges/day) |
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Adverse effects of Nicotrol
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local mouth irritation, coughing, rhinitis
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Drug class for Bupropion sustained-release (SR) (Zyban®, Wellbutrin SR®)
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Antidepressant, Dopamine-reuptake inhibitor
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dosage form for Bupropion sustained-release (SR) (Zyban®, Wellbutrin SR®)
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0.5 mg and 1 mg tablets
i. Begin therapy 1-2 weeks before quit date and stop smoking during 2nd week of treatment ii. Can consider a maintenance therapy of 150 mg BID x 6 months iii. Those who are not making improvements towards cessation by week 7 of therapy should have treatment discontinued as cessation is not likely iv. Can be used in combination with NRT v. Do not crush sustained release products |
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Is Bupropion OTC or Rx?
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Rx
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Mech of action for Bupropion
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Inhibits the neuronal reuptake and potentiates the effects of norepinephrine and dopamine (decreases withdrawal symptoms)
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Special considerations for Bupropion (contraindications)
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i. Patients with a history of seizures/epilepsy or eating disorders
ii. Use of monoamine-oxidase inhibitors (MOAi) within 14 days (i.e. phenelzine, rasagiline, selegiline, tranylcypromine, isocarboxazid, procarbazine, linezolid) |
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Adverse effects of Bupropion
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insomnia, dry mouth, tremor, rash, headache
i.Insomnia - take evening dose earlier in the afternoon (but at least 8 hours after first dose) |
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Duration of action (long or short) for Buproprion
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long
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Drug class for Varenicline (Chantix®)
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Partial Nicotine Agonist
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Dosage form for Varenicline (Chantix®)
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Tablet
i. Start 1 week before quit date ii. Take with food or water iii. If patient successfully quits in 12 weeks, an additional 12 weeks may be offered to maintain success. If patient has not quit in 12 weeks, stop therapy and re-evaluate. |
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Is Varenicline (Chantix®) OTC or Rx?
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Rx
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Mechanism of action for Varenicline (Chantix®)
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selective nicotinic agonist that binds specifically at the α4β2 nicotinic receptor which mediates the rewarding properties of nicotine by causing a release of dopamine. Causes 30-60% of the dopamine release associated with nicotine which will attenuate craving and withdrawal. It has a higher affinity than nicotine for the receptor therefore is a competitive antagonist for nicotine.
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Duration of action (long or short) for Varenicline (Chantix®)
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Long
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Special considerations for Varenicline (Chantix®)
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-psychiatric illness (bipolar, schizophrenia, depression)
-Do NOT use in combination with NRT or bupropion -Cost: $130.00 for 30 day supply |
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Adverse effects of Varenicline (Chantix®)
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FDA Warning: depressed mood, agitation, behavioral changes, suicidal ideations and suicide have been reported. Psychiatric illness or history of should be disclosed prior to initiation. Mood and behavior should be monitored closely.
nausea, insomnia, abnormal dreams i. Take with food if nausea occurs ii. Move dose further from bedtime if sleep disturbances occur iii. SE may warrant a temporary dose reduction |
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When might combination NRT tx be beneficial?
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in highly nicotine dependent patients or those with a history of severe withdrawal symptoms
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The patch is associated with good compliance, but what are some draw backs?
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slow onset of action
no dose flexibility for cravings |
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When creating a combination NRT therapy, what should you consider regarding duration of action?
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combination of long and short acting NRT agents
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Bupropion SR + nicotine patch facts
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i. Proven effective in clinical trials
ii. Combination is FDA-approved |
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Smoking is an inducer of what enzymes?
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Cytochrome P450 enzymes
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What effect does tobacco smoke have on some drugs
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induces metabolism
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During smoking, these drugs are metabolized more quickly, so what do you need to do to tx while smoking?
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increase dose while smoking
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Upon cessation, what should you be aware of related to other medications the pt may be on?
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Inducer is removed, so concentrations of other meds may be increased and can lead to toxicity
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What meds should you be concerned about toxicity with after smoking cessation?
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Olanzapine
haloperidol clozapine alprazolam (xanax) caffeine theophylline Etc. |
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Does NRT have the same effects on P450s as smoking?
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NO
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