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
2
Q
Drugs that may have an increased effect due to induction of CYP1A2
A
Clopidogrel(prodrug)
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
4
Q
Smoking Cessation
Drugs that may have a decreased effect due to induction of CYP1A2
A
Clopidogrel
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
6
Q
Pharmacotherapy for Smoking cessation
A
- Nicotine replacement therapy (Rx and OTC)
- Bupropion SR
- Varenicline
- Second line agents
7
Q
Nicotine replacement therapies (NRTs)
A
- Gum
- Lozenge
- Patch
- Nasal spray
- Inhaler
8
Q
Nicotine Gum
Availability
A
2mg and 4mg
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
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
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
12
Q
Nicotine Gum
Side effects
A
Mouth soreness/irritation,hiccups,dyspepsia
13
Q
Nicotine Gum
Advantages
A
- May satisify oral cravings
- May delay weight gain
- Patients can titrate therapy to manage withdrawal symptoms
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
15
Q
Nicotine Lozenges
Prescribing instructions
A
- Allow lozenge to completely dissolve
- Do not chew or swallow
- Acidic beverages interfere with nicotine absorption
16
Q
Nicotine Lozenges
Contraindications
A
Same as Nicotine Gum
17
Q
Nicotine Lozenge
Advantages
A
- May satisfy oral cravings
- Easy to use and conceal
- Patients can titrate therapy to manage withdrawal symptoms
17
Q
Nicotine Lozenges
Side effects
A
Nausea,dyspepsia,headache
18
Q
Nicotine Lozenge
Disadvantages
A
GI side effects (nauses and dyspepsia) may be bothersome
19
Q
Nicotine Patches
Availability
A
21,14, or 7mg delivered transdermally over 24 hours
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
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
22
Q
Nicotine Patch
Contraindications
A
Same as the lozenges
23
Q
Nicotine Patches
Side effects
A
- Local skin reactions (itching,burning,tingling)
- Insomnia and/or vivid dreams
- Remove before MRI
24
Nicotine Patches
| Advantages and Disadvantages
* 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
Nicotine Nasal Spray
| Availability
0.5mg deleivered per actuation per nostril
26
Nicotine Nasal Spray
| Dosing
* 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
Nicotine Nasal Spray
| Prescribing Instructions
* 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
Nicotine Nasal Spray
| Contraindications
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
Nicotine Nasal Spray
| Side effects
* 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
Nicotine Nasal Spray
| Advantages/Disadvantages
* 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
Nicotine Inhaler
| Availabilty
4mg delivers over 80 inhalations per cartridge
32
Nicotine Inhaler
| Dosing
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
Nicotine Inhaler
| Prescribing Instructions
* Delivery of nicotine from the inhaler declines in **cold weather**(<40F)
* Frequent puffing leads to best results
* Acidic beverages interfere with nicotine absorption
34
Nicotine Inhaler
| Contraindications
Same as Nicotine Lozenges
+
**Use with caution in patients with bronchospastic disease**
35
Nicotine Inhaler
| Side effects
* Local irritation in the mouth and throat
* coughing
* rhinitis
36
Nicotine Inhaler
| Advantages/Disadvantages
* 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
NRT
| PK/PD
Metabolism----> primary metabolites are cotinine and trans-3-hydroxycotinine
38
Combination therapies
* Buproprion SR+Nicotine Patch
* Nicotine Patch (>14weeks) + other NRT PRN
* Nicotine Patch + Nicotine Inhaler
39
Prescription Smoking Cessations
* Buproprion
* Varenicline
* Second line(Clonidine,Nortriptyline)
40
Buproprion for smoking cessation
* MOA--> Antagonism of nAchR, dopaminergic effects on reward mechanisms
* PD-->Decreases craving for cigarettes,decreases symptoms of nicotine withdrawal
41
Buprion SR:PK
* 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
Buprion SR
| Dosing
* 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
Buproprion SR
| Patient Response
* 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
Buprprion SR
| Side effects
Common
1. Insomnia
2. Dry mouth
3. Dizziness
4. Anxiety
Less Common
1. CNS effects(tremors)
2. skin rash
45
Bupropion SR
| Side Precautions/Contraindications
* 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
Buproprion SR
| Boxed Warning
* Suicidal thoughts and behaviors(children,adoescetns and young adults)
* Pregnancy (crosses the placenta and enters breast milk)
47
Bupropion SR
| Advantages/Disadvantages
* 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
Varenicline MOA
* Partial agonist selective for alpha-4,beta 2 nicotinic Ach receptors
* Prevents the binding of nictotine to receptor
49
Varenicline Clinical effects
* Decrease symptoms of nicotine withdrawal
* Blocks effects of nicotine if patient resumes smoking
* Breaks dopamine reward cycle from smoking
50
Varenicline
| Dosing
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
Varenicline
| Patient Response
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
Varenicline Side effects
1. Nausea
2. Sleeping disturbances
3. Headaches
4. Vomiting
5. Flatulence
6. Constipation
53
Varenicline
| Precautions
* 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
Varenicline
| Advantages/Disadvantages
* 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
Seond line therapies of smoking cessations
* Clonidine
* Nortriptyline
56
Clonidine
| Dosing
* 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
Clonidine
| Side effects/Precuations
* 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
Notriptyline
| MOA
Tricyclic antidepressant
59
Nortiptyline
| Dosing
* 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
Nortryptyline
| Side effects/Precautions
* 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
