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Pharmacology > smoking cessation ~ > Flashcards

smoking cessation ~ Flashcards

1
Q

smoking and nicotine

A

Other toxins in tobacco smoke (NOT nicotine) are responsible for majority of adverse health effects
- 4000 different chemicals
-tar, carbon monoxide, irritant and oxidant gases
- > 40 carcinogens

Nicotine:
- MAIN adverse event = addiction causing sustained tobacco use
- bad because smoking = exposure to toxins in tobacco smoke

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2
Q

Smoking relation to CVD, smoking related contributing factors to CVD

A

-Smoking increase risk of CVD
-Smoking cessation significantly decrease risk within 1–3 years

Smoking-related factors contributing to CV risk include:
-increased thrombogenesis
-carbon monoxide
-oxidative damage
-hyperlipidemia

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3
Q

Nicotine properties

A

-Has stimulant and depressant effects
-Rapidly absorbed from mouth and respiratory tract into blood stream
-Can bind to and stimulate nicotinic receptors in autonomic ganglia, CVS, respiratory system and nervous system

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4
Q

nicotine effects: CVS

A

CVS:
-positive inotropic, positive chronotropic
-increase CO
-increase BP: SBP and DBP

Respiratory:
- Low Doses: ↑ Respiration via activation of chemoreceptors
- High Doses: ↑ Respiration via direct activation of respiratory center
- *Toxic Doses: ↓ Respiration via inhibition of respiratory centers in brainstem & neuromuscular junctions

CNS:
-Mild euphoria, increase arousal and concentration, improved memory
- appetite suppression*
-Tremors, convulsions, respiratory stimulation
-Nausea and vomiting (tolerance develops quickly)

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5
Q

nicotine effects: respiratory

A

Respiratory:
- Low Doses: ↑ Respiration via activation of chemoreceptors
- High Doses: ↑ Respiration via direct activation of respiratory center
- *Toxic Doses: ↓ Respiration via inhibition of respiratory centers in brainstem & neuromuscular junctions

CVS:
-positive inotropic, positive chronotropic
-increase CO
-increase BP: SBP and DBP

CNS:
-Mild euphoria, increase arousal and concentration, improved memory
- appetite suppression*
-Tremors, convulsions, respiratory stimulation
-Nausea and vomiting (tolerance develops quickly)

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6
Q

nicotine effects: CNS

A

CNS:
-Mild euphoria, increase arousal and concentration, improved memory
- appetite suppression*
-Tremors, convulsions, respiratory stimulation
-Nausea and vomiting (tolerance develops quickly)

CVS:
-positive inotropic, positive chronotropic
-increase CO
-increase BP: SBP and DBP

Respiratory:
- Low Doses: ↑ Respiration via activation of chemoreceptors
- High Doses: ↑ Respiration via direct activation of respiratory center
- *Toxic Doses: ↓ Respiration via inhibition of respiratory centers in brainstem & neuromuscular junctions

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7
Q

pharmacokinetics of nicotine

A
  • Well absorbed through mucous membranes *** -> good target in treatmet
  • Widely distributed, crosses BBB + placenta (what mom gets baby gets)
    -Inhibits monoamine oxidase – may have dopamine like effects
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8
Q

nicotine metabolism

A

-Nicotine metabolism is induced by the tars in cigarette smoke (via CYP450) –> leads to pharmacokinetic tolerance
-Nicotine also can induce metabolism of BBs, BDZ, opiods and theophylline
-pregnant- mom smokes -> baby smokes (kicking, tachycardia)

Tar in cigarette smoke = Induce metabolism of Nicotine = Long-term tolerance = Need more cigarettes for same feeling
- The more you smoke -> the more DDIs you have with 450

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9
Q

Aversion Therapy vs Substitution Therapy vs abrupt withdrawal

A

Aversion:
-Patient associates smoking with something undesirable
-Not very effective
-Often used w/ hypnosis or acupuncture

Substitution:
- Nicotine replacement therapy - shown to work the best

Abrupt withdrawal:
- Cold turkey: good for strong willed and highly motivated pts
- May be combined w/ agents to reduce craving

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10
Q

3 types of smoking cessation pts

A

-Those willing to quit: 5 As
-Those unwilling to quit: 5 Rs
-Past users who recently quit: help them with issues post quitting and empower their decision ~

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11
Q

pts willing to quit: what do you do

A

5 As: Always encourage pts to quit at each visit (intervening and motivating)

-ASK- systematically identify all users at every visit
-ADVISE- strongly urge all users to quit
-ASSESS- determine if pt is willing to quit or not
-ASSIST- help pt set up a plan to quit
-ARRANGE- schedule f/u contacts to reinforce quitting and identify problem with current plan, best to do during 1st week, 1st month, then PRN

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12
Q

pts NOT willing to quit: what to do

A

5 Rs: intervene and motivate
-RELEVANCE- help pt determine specific areas in life that would benefit from quitting
-RISKS- help pt identify neg consequences of smoking
-REWARDS- help pt identify benefits to quitting
-ROADBLOCKS- help pt identify barriers to quitting
-REPETITION- encourage pt to quit at every visit

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13
Q

pts who recently quit: what do you talk to them about

A

-Reinforce their decision
-Review the benefits of quitting
-Help with problems that may be encountered by quitting

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14
Q

nicotine replacement therapy: benefits

A

Benefit
-NRT delivers nicotine without the TOXINS from tobacco smoke
-NRT helps combat the symptoms of withdrawal
-Nicotine dose from NRT is LOWER and administered more GRADUALLY than with smoking = lower risk of ADDICTION

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15
Q

NRT and cancer

A
  • risk of cancer with NRT is negligible compared to risk from continuing to smoke
  • cancer and smoking is from the tobacco smoke
  • under normal conditions: nicotine is NOT carcinogenic
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16
Q

NRT, smoking, and pregnancy

A

pregnant smoking associated with: poor pregnancy and childhood outcomes
- due to toxins in the smoke

NRT:
- nicotine = potential teratogen
- Benefits of NRT > risks *
- nicotine may contribute to complications like sudden infant death syndrome and obstetrical complications

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17
Q

NRT abuse and liability

A

Abuse prevalence is LOW
- patch: almost 0%
- gum, nasal spray, inhaler: <10%
- higher prevalence in products that deliver nicotine rapidly but way less than cigarettes

Even with abuse: benefits > risks compared to smoking

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18
Q

NRT: indications

A

indication: EVERYONE WHO WANTS TO QUIT
- it is SAFE!! even with CVD pts and even with concomitant smoking
- analysis shows benefits of NRT > risk of NRT ***
- risk of cancer with NRT is negligible compared to risk from continuing to smoke
- pregnancy: benefits still outweigh risks but it is still a potential teratogen and can cause sudden infant death syndrome

19
Q

NRT: drug options

A
  • patch *
  • gum *: chew slowly for slow absorption
  • lozenges *
  • nasal spray: max = 40 doses/day; fastest but irritating
  • inhaler: frequent puffs every 20 min

all of these = FIRST LINE

20
Q

what is the correct way to take nicotine gum?

A

Chew it 3-4 times and leave it inside your cheek -> the nicotine gets released into the buccal cavity, a couple minutes later -> chew some more
- Ppl often take this incorrectly -> EDUCATE PT
- chew slowly to avoid jaw ache and increase buccal absorption

21
Q

Nicotine Gum dosing, duration, ADR

A

For smokers who consume less than 24 cigarettes/day:
- 2 mg gum dose
- max: 24 pieces per day

For smokers who consume more than 24 cigarettes per day:
- 4 mg gum dose
- max: 24 pieces per day

Duration: 12 wks

ADRS: mouth soreness, dyspepsia

(chew slowly to reduce jaw soreness and increase absorption)

22
Q

nicotine inhaler: dose, duration, ADRs

A

Dose: 6-16 cartridges/day
- continuously puff every 20 minutes
Duration: 6 months
ADRs: Local irritation of mouth and throat

23
Q

Nicotine Nasal Spray: dose, duration, ADRs

A

Dose:
- 1 dose = 2 sprays = 1 mg of nicotine
- max dose: 5 doses/10 sprays per hour AND 40 doses/day

Duration: 3-6 months

ADRs: nasal irritation

24
Q

Nicotine Patch: dosing, duration, ADRs

A

Dosing: recommendations not hard in stone (these are the MC regimens)
- -21mg/24 hr x 4 weeks
-14mg/24 hr x 2 weeks
-7mg/24 hr x 2 weeks
- nicotrol: comes in 15mg,10mg & 5mg/24 hr

ADRs: local skin rxn, insomnia

25
Q

Nicotine lozenge: dosing, duration, ADRs

A

Dose based on timing of the first cigarette of the day:
- if its within 30 minutes of waking up: 4 mg dose
- if its smoked after 30 minutes of waking up: 2 mg dose

Duration: 12 wks
- first 6 wks: one lozenge every 1-2 hrs
- next 3 wks: one lonzenge every 2-4 hrs
- final 3 wks: one lozenge every 4-8 hrs

26
Q

NRT: duration of each type

A

Patch: ~ few weeks (4 wks, chatGPT says 8-12 wks)
Gum: 12 wks
Lozenge: 12 wks
Nasal Spray: 3-6 months
Inhaler: 6 months

27
Q

pharmacological tx: first line vs second line vs third line tx drug names and classes

A

First line:
- Bupropion: antidepressant (NDRI)
- Varenicline: partial nicotinic acetylcholine receptor agonist (less ADRs and precautions than bup)

Second line:
- Nortriptyline: TCA

Third line:
- Clonidine: alpha 2 agonist

Try bupropion or varenicline first and if they don’t work switch to the opposite med -> then try second line

28
Q

Bupropion: MOA, indication and precaution

A

MOA:
- Antidepressant: NE- dopamine reuptake inhibitor
- weakly inhibits serotonin, dopamine, NE reuptake
- does NOT inhibit MAO

Indication: first line tx

precaution:
- seizure risk: higher risk with dose >450 mg/day or individual dose >150 mg

29
Q

Bupropion: ADRs and dosing, duration

A

ADRs:
- insomnia
- dry mouth
- HTN ( risk w/ nicotine patch)

Dosing:
- start 2 wks before the quit date
- first 3 days: 150 mg PO QD
- afterwards (7-12 wks): 150 mg PO BID

duration: up to 6 months

30
Q

Smoking and MAO

A
  • MAO: enzyme in the brain that breaks down dopamine, serotonin and NE
  • smoking = INHIBITION OF MAO -> increase in serotonin in the brain -> addiction

smoking cessation: MAO activity returns to normal and neurotransmitter levels decrease

31
Q

varenicline (Chantix): MOA, indication and precaution

A

MOA:
- Partial nicotinic ACH receptor agonist
- Reduces craving and withdrawal symptoms

indication: first line tx

Precaution: Nausea -> take with full glass of water

32
Q

varenicline (Chantix): ADRs

A

Common ADRs:
- GI effects, (nausea, vomiting, dysgeusia)
- sleep disturbances: abnormal dreams*
- headaches
- anxiety
- irritability

Behavioral & Psychiatric side effects:
- anxiety
- irritability
- restlessness
- emotional disturbances
- vivid dreams*
- angry outbursts*
- irrational behavior*
- depression*
- suicidal ideation*

33
Q

Reports from Institute for Safe Medication Practices (ISMP) on a certain drug

A

varenicline (chantix)

additional reports of:
-Accidents/injuries
-Visual disturbances
-Dysrhythmias
-Seizures
-Dermatological reactions
-Diabetes

monitor individuals who are taking Chantix for pyschiatric and behavioral sx!!!!!

34
Q

varenicline (Chantix): dosing

A

Dosing: Start one week before quit date and continue for 12 weeks
- If patient successfully quits: you can continue treatment for additional 12 weeks to maintain success

Schedule
-Day 1-3: 0.5 mg PO QD
-Day 4-8: 0.5 mg PO BID
-Day 8 – end of treatment: 1 mg PO BID

35
Q

chantix efficacy

A

-FDA-approval based on combined data from 5 clinical trials (3659 patients total)
-Smoked at least 10 cigarettes per day (Average 21 cigarettes per day for an average of 25 years)
-Compared to placebo: More effective in reducing urge to smoke, less withdrawal and more likely to maintain abstinence during follow-up
-Compared to bupropion: Similar efficacy rates with less adverse effects and precautions*

36
Q

Nortriptyline: MOA, indication, ADRs

A

2nd line tx

MOA: unknown but drug is TCA
- reduces craving
- not FDA approved

ADRs:
- dry mouth
- arrhythmias *
- sedation

Try bupropion or varenicline first and if they don’t work switch to the opposite med -> then try second line

37
Q

Clonidine

A

3rd line tx

MOA: alpha 2 agonist
- limited efficacy

Dose:
- 0.15-0.75 mg/day for 3-10 weeks
- Can use PO or patch

ADRs
- rebound HTN
- dry mouth
- CNS effects

38
Q

Investigational Treatment for nicotine withdraw

A

Nicotine Vaccine!!

MOA: Induce antibodies which bind to nicotine → Nicotine cant cross blood brain barrier → Reduces addictive effect
- Currently in Phase 2 Trial
- further research needed with immuno therapy

39
Q

counseling and behavioral therapy

A

Should be utilized in combination w/ pharmacological therapy***
- increases success rate for quitting when pharmacological + counseling

Includes:
-practical counseling (problem solving and skills training)
-social support
-person to person contact

40
Q

other pharm tx for nicotine withdrawal

A

-appetite suppressants
-benzodiazepines
-beta-blockers
-buspirone
-caffeine/ephedrine
-cimetidine
-dextrose tablets (food supplement)
-lobeline
–moclobemide (monoamine oxidase inhibitor)
-SSRIs

41
Q

US public health service guidelines

A
  • clinic screening systems: should expand vital signs to include tobacco use status -> reminder systems with chart stickers or computer prompts would be great for consistent assessment
  • routine screening: always screen for tobacco use and assess interest in quitting
  • strongly advise every pt who smokes to quit **
  • repeatedly and consistently provide smoking cessation interventions: NRT or bupropion/varenicline
  • max efficiency: interventions should include individual counseling, group sessions, or telephone contact
42
Q

areas of further research in smoking cessation

A

-The elements of behavioural interventions that enhance effectiveness
-Effectiveness of combining: different NRT formulations; NRT + non-nicotine pharmacotherapies
-Long-term use of NRT or other pharmacotherapies to prevent relapse or reduce harm
-Interventions for adolescent smokers
-Improving access to effective interventions
-Organization of healthcare systems for delivery of appropriate interventions
-Optimal sequence of treatment combinations for repeated attempts to quit
-Treatment of smokers with co-morbidities

43
Q

summary slide

A

-Toxins in tobacco smoke cause most adverse health effects
-Nicotine is addicting therefore it sustains tobacco use
-Smoking Cessation Therapy may include aversion therapy, substitution therapy or abrupt withdrawal
-Tobacco Cessation Guidelines have identified 3 types of patients for smoking cessation
-Nicotine Replacement Therapy is first-line per guidelines. It is available in various dosage forms and essentially helps reduce the withdrawal symptoms associated with quitting
-NRT can be combined with bupropion (also first-line) to reduce craving
-Varenicline (Chantix) is a partial nicotinic receptor agonist used to reduce craving and withdrawal. It is considered first-line but not yet part of official guidelines. Chantix is associated with potential behavioral and psychiatric side effects
-The success rate for quitting is increased when pharmacological agents are combined with counseling and behavioral therapies

Pharmacology (15 decks)

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