Smoking Cessation Flashcards

1
Q

Pk interactions with smokings

Drugs that decreased effect due to induction of CYP1A2

A
  • Caffeine
  • Clozapine
  • Fluvoxamine
  • Olanzapine
  • Tacrine
  • Theophylline
  • Bendamustine
  • Warfarin
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2
Q

Drugs that may have an increased effect due to induction of CYP1A2

A

Clopidogrel(prodrug)

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3
Q

PK interactions with Cessation

Drugs that may have an increased effect due to induction of CYP1A2

A
  • Caffeine
  • Clozapine
  • Fluvoxamine
  • Olanzapine
  • Tacrine
  • Theophylline
  • Bendamustine
  • Warfarin
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4
Q

Smoking Cessation

Drugs that may have a decreased effect due to induction of CYP1A2

A

Clopidogrel

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5
Q

Smokers who use combined hormonal contraceptives have an increased risk of serious cardivascular ADR which include:

A
  • Stroke
  • Myocardial infarction
  • Thromboembolism

Women 35 years and older AND smoke are at a significantly elevated risk

Smoking does not decrease the efficacy of hormonal contraceptives

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6
Q

Pharmacotherapy for Smoking cessation

A
  • Nicotine replacement therapy (Rx and OTC)
  • Bupropion SR
  • Varenicline
  • Second line agents
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7
Q

Nicotine replacement therapies (NRTs)

A
  • Gum
  • Lozenge
  • Patch
  • Nasal spray
  • Inhaler
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8
Q

Nicotine Gum

Availability

A

2mg and 4mg

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9
Q

Nicotine Gum

Dosing

A
  • Smoke first cigarette >30mins after waking
    —> 2mg every 1-2hrs for 6 wks
  • Smoke** first cigarette <30mins after waking**
    —>4mg every 1-2 hours for 6 weeks
    Decrease to every 2-4 hrs in wks 7-9, and every 4-8 hours in weeks 10-12

Max dose: 24 pieces

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10
Q

Nicotine Gum

Precribing instructions

A

Chew and park technique
This should be continued until all taste dissipitates from the gum
Acidic beverages interfere w/ nicotine absorption

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11
Q

Nicotine Gum

Precautions/contraindications

A

Not recommended in pregnant women
Use with caution in patients with a recent MI, serious arrhyhtmias, and unstable angina pectoris

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12
Q

Nicotine Gum

Side effects

A

Mouth soreness/irritation,hiccups,dyspepsia

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13
Q

Nicotine Gum

Advantages

A
  • May satisify oral cravings
  • May delay weight gain
  • Patients can titrate therapy to manage withdrawal symptoms
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14
Q

Nicotine Lozenges

Dosing

A
  • Smoke 1st cigarette >30 minsafter waking—>2mg every 1-2hours for 6 weeks
  • Smoke **1st cigarette <30mins after waking ** —> 4mg every 1-2 hrs for 6 weeks
    Decrease to every 2-4 hours in weeks 7-9, and every 4-8 hours in weeks 10-12
    Max dose: 20pieces
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15
Q

Nicotine Lozenges

Prescribing instructions

A
  • Allow lozenge to completely dissolve
  • Do not chew or swallow
  • Acidic beverages interfere with nicotine absorption
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16
Q

Nicotine Lozenges

Contraindications

A

Same as Nicotine Gum

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17
Q

Nicotine Lozenge

Advantages

A
  • May satisfy oral cravings
  • Easy to use and conceal
  • Patients can titrate therapy to manage withdrawal symptoms
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17
Q

Nicotine Lozenges

Side effects

A

Nausea,dyspepsia,headache

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18
Q

Nicotine Lozenge

Disadvantages

A

GI side effects (nauses and dyspepsia) may be bothersome

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19
Q

Nicotine Patches

Availability

A

21,14, or 7mg delivered transdermally over 24 hours

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20
Q

Nicotine Patches

Dosing

A
  • Smoke >10 cigarettes per day —->21mg patch daily for 6 weeks, 14mg patch for 2 weeks,then 7mg patch for 2 weeks
  • Smoke </ _ 10 cigarettes per day —->14mg patch daily for 6 weeks, then 7mg patch for 2 weeks
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21
Q

Nicotine Patches

Prescirbing Instructions

A
  • Should be applied at beginning ging of the day to a hairless location between the neck and neck
  • There are no restrictions to activites while wearing the patch
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22
Q

Nicotine Patch

Contraindications

A

Same as the lozenges

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23
Q

Nicotine Patches

Side effects

A
  • Local skin reactions (itching,burning,tingling)
  • Insomnia and/or vivid dreams
  • Remove before MRI
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24
Q

Nicotine Patches

Advantages and Disadvantages

A
  • Advantages
    1. The patch provides consistent nicotine levels
    2. Easy to use and conceal
    3. Fewer compliance issues are associated with patch use
  • Disadvantages
    1. Patients cannot titrate the dose
    2. Allergic reactions to the adhesive may occur
    3. Patients with dermatologic conditions (e.g eczema) should not use the patch
25
Q

Nicotine Nasal Spray

Availability

A

0.5mg deleivered per actuation per nostril

26
Q

Nicotine Nasal Spray

Dosing

A
  • Initial dosing should be 1-2 doses per hour, increasing as needed for symptoms relief (Do not exceed 40 mg {80 sprays }per day or 5mg {10sprays}
    per hour)
  • Best results: at least 8 doses per day
  • Can be used up to 3 months
27
Q

Nicotine Nasal Spray

Prescribing Instructions

A
  • Do NOT inhale or sniff through the nose when spraying
    Directions for use
    1. Wait 2-3mins before blowing nose
    2. Wait 5 mins before driving or operating heavy machinery (can cause tearing,coughing, or sneezing)
28
Q

Nicotine Nasal Spray

Contraindications

A

Same as Nicotine
+
* Nasal spray produces higher peak concentrations of nicotine and has highest dependency potential
* Severe reactive airway diseaseor chronic nasal disorders(rhinitis,nasal polyps,sinusitis)

29
Q

Nicotine Nasal Spray

Side effects

A
  • Moderate to severe nasal irritation (hot peppery feeling in nose/throat, sneezing,coughing,water eyes,runny nose) in first 2 days reported by 94% of users
  • Nasal congestion and transient changes
30
Q

Nicotine Nasal Spray

Advantages/Disadvantages

A
  • Advantages
    1. Patients can easily titrate therapy to rapidly manage withdrawal symptoms
  • Disadvantages
    1. Nasal/throat irritation may be bothersome
    2. Nasal spray has higher dependence potential
    3. Patients with chronic nasal disorders or severe reactive airway disease should not use the spray
31
Q

Nicotine Inhaler

Availabilty

A

4mg delivers over 80 inhalations per cartridge

32
Q

Nicotine Inhaler

Dosing

A

Recommended daily dosage to ranges from** 6-16 cartridges (24 to 64 mg) per day **for months
Followed by gradual reduction in dosage in dosage over 6-12 weeks
Can be used up to 6 months

33
Q

Nicotine Inhaler

Prescribing Instructions

A
  • Delivery of nicotine from the inhaler declines in cold weather(<40F)
  • Frequent puffing leads to best results
  • Acidic beverages interfere with nicotine absorption
34
Q

Nicotine Inhaler

Contraindications

A

Same as Nicotine Lozenges
+
Use with caution in patients with bronchospastic disease

35
Q

Nicotine Inhaler

Side effects

A
  • Local irritation in the mouth and throat
  • coughing
  • rhinitis
36
Q

Nicotine Inhaler

Advantages/Disadvantages

A
  • Advantages
    1. Patients can easily titrate therapy to managewithdrawal symptoms
    2. The inhaler mimics the hand-to-mouth ritual of smoking
  • Disadvantages
    1. The initial throat or mouth irritation can be bothersome
    2. Cartridges should not be stored in very warm conditions or used in very cold conditions
    3. Patients with underlying bronchospastic disease must use the inhaler with caution
37
Q

NRT

PK/PD

A

Metabolism—-> primary metabolites are cotinine and trans-3-hydroxycotinine

38
Q

Combination therapies

A
  • Buproprion SR+Nicotine Patch
  • Nicotine Patch (>14weeks) + other NRT PRN
  • Nicotine Patch + Nicotine Inhaler
39
Q

Prescription Smoking Cessations

A
  • Buproprion
  • Varenicline
  • Second line(Clonidine,Nortriptyline)
40
Q

Buproprion for smoking cessation

A
  • MOA–> Antagonism of nAchR, dopaminergic effects on reward mechanisms
  • PD–>Decreases craving for cigarettes,decreases symptoms of nicotine withdrawal
41
Q

Buprion SR:PK

A
  • Absorption–>Bioavailabity 5-20%
  • Metabolism–>Extensive hepatic metabolism(CYP2D6),Strong inhibitor of CYP2D6(antidepressants,tramadol,codeine)
  • Elimination–>Urine(87%)and feces(10%)
  • Half-life–>Burprion: 21 hours, Metabolites 20-37 hours
42
Q

Buprion SR

Dosing

A
  • Start 150mg PO daily x 3days
  • Then increase to 150mg PO BID
    Duration of therapy
  • 7-12 weeks recommended
  • Can be taken for 12 months
    NB: Patient should begin therapy 1 to 2 weeks PRIOR to their quit date to ensure that therapeutic plasma levels of the drug are achieved
43
Q

Buproprion SR

Patient Response

A
  • Can be used w/ or w/out NRT
  • No difference in bupropion concentrations
  • If no significant progress toward abstinence is seen by week 7 therapy unlikely to be effective (Discontinue treatment, Reevaluate and restart at a later date)
  • Dose tapering is not required when stopping
44
Q

Buprprion SR

Side effects

A

Common
1. Insomnia
2. Dry mouth
3. Dizziness
4. Anxiety
Less Common
1. CNS effects(tremors)
2. skin rash

45
Q

Bupropion SR

Side Precautions/Contraindications

A
  • Precautions
    1. Seizure Risk(Cranial trauma,CNS tumors)
    2. Concurrent medications that lower seizure threshold(Antipsychotics,Antidepressants,Theophylline,Systemic steroids)
    3. Uncontrolled HTN
    4. Psychosis or other neuropsychiatric rxns
    5. Angle-closure glaucoma
    6. Svere hepatic cirrhosis(Child-Pugh>7 requires dose adjustment)
  • Contraindications
    1. Seizure disorders
    2. Current or prior anorexia or bulimia nervosa
    3. Patients undergoing abrupt discontinuation of alcohol or sedatives
    4. Patients taking: Wellbutrin,Wellbutrin SR, Wellbutrin XL, MAOI w/in the last 14 days,Linezolid,methylene blue
46
Q

Buproprion SR

Boxed Warning

A
  • Suicidal thoughts and behaviors(children,adoescetns and young adults)
  • Pregnancy (crosses the placenta and enters breast milk)
47
Q

Bupropion SR

Advantages/Disadvantages

A
  • Advantages
    1. Oral formulation
    2. Aids w/ withdrawal symptoms and cravings
    3. Added benefit if history of depression
    4. No risk of nicotine poisoning; can be used w/NRT
  • Disadvantages
    1. Seizure risk
    2. Contraindications and precautions
48
Q

Varenicline MOA

A
  • Partial agonist selective for alpha-4,beta 2 nicotinic Ach receptors
  • Prevents the binding of nictotine to receptor
49
Q

Varenicline Clinical effects

A
  • Decrease symptoms of nicotine withdrawal
  • Blocks effects of nicotine if patient resumes smoking
  • Breaks dopamine reward cycle from smoking
50
Q

Varenicline

Dosing

A

Patient should begin **therapy 1 week PRIOR **to their quit date to minimize treatment -related nauses and insomnia
* Treatment
1. Day 1 to 3—> 0.5mg qd
2.Day 4 to day 7–>0.5mg bid
3.Day 8 to end of treatment—>1mg bid
–>Doses should be taken AFTER eating with a full glass of water
–>Do NOT use with NRT

51
Q

Varenicline

Patient Response

A
  1. Evaluate response after 12 weeks of therapy (an additional 12 weeks is recommended to increase likelihood of long-term abstinence)
  2. If patient fails therapy, may consider second attempt
  3. Dose tapering is not neccessary when stopping
52
Q

Varenicline Side effects

A
  1. Nausea
  2. Sleeping disturbances
  3. Headaches
  4. Vomiting
  5. Flatulence
  6. Constipation
53
Q

Varenicline

Precautions

A
  • Alcohol consumption
  • Cardivascular events
  • Psychiatric illness
  • Renal impairment(CrCl<30ml/min): maiantenance dose 0.5mg BID; (ESRD): maintenance dose 0.5mg QD
  • Seuzures
  • Pregnancy —> limited information related to pregnancy
54
Q

Varenicline

Advantages/Disadvantages

A
  • Advantages
    1. Oral formulation
    2. Decreases w/drawal symptoms
    3. Novel MOA
  • Disadvantages
    1. High incidence of nausea , can not take with NRT
    2. Possible cardivascular and psychiatric concerns
55
Q

Seond line therapies of smoking cessations

A
  • Clonidine
  • Nortriptyline
56
Q

Clonidine

Dosing

A
  • Oral–> 0.15 to 0.75/day
    Start: 0.1mg BID
  • Transdermal –> 0.1to 0.3mg/day
    Start: 0.1 mg patch
    Titrate by 0.1mg/day per week as tolerated
    Duration —> 3-10weeks
    MUST taper when discontinuing
57
Q

Clonidine

Side effects/Precuations

A
  • Side effects
    1. Dry mouth
    2. Drowsiness
    3. Dizziness
    4. Sedation
    5. Constipation
    6. Decreased blood pressure
  • Precautions
    1. Rebound hypertension(taper dose)
    2. Use with caution if –>reduced vnetricular functiom
    —> slow hear rate —>AV node conduction issues
    3.Pregnancy category C
58
Q

Notriptyline

MOA

A

Tricyclic antidepressant

59
Q

Nortiptyline

Dosing

A
  • Range: 75-100mg/day
  • start 25mg QHS
    –>Duration of therapy
  • 6-14 weeks
  • Most trials gradually tapered the dose over an additional 1-2 weeks
  • start prior to quit date to achieve steady-state
60
Q

Nortryptyline

Side effects/Precautions

A
  • Side effects
    1. Sedation
    2. Dry mouth
    3. Blurred vision
    4. Urinary retention
    5. Lightheadedness
    6. Tremor
  • Precautions
    1. Risk of arrhythmias and postural hypotension
    2. Pregnancy category D