Exam I Flashcards
(188 cards)
Nicotine: 2nd line drugs for smoking cessation include:
- Combination (nicotine + buproprione)
- Clonidine
- Nortriptyline
What are 1st line therapy drugs?
- Nicotine replacement (patch, gum, vaping)
- Buproprione (anti-depressant)
- Varenicline (nicotinic receptor agonist)
Nicotine: After smoking, nicotine can reach the brain in about 10 seconds. It acts by acting on ______ inc. dopamine release and eliciting positive reinforcement (reward, relaxation).
nACh receptors
- nACh-R’s become desensitize (inactivated)
- upregulation of receptors
- inc. need
NOTE: withdrawal occurs when there is no nicotine
Nicotine: True/False - In the absence of nicotine, patient’s can undergo withdrawal symptoms including irritability, restlessness and increased craving (inc. desire to smoke)
True
Nicotine: 1 cigarette is equivalent to about ~10 puffs, meaning a person can receive ~10 positive reinforcements. Thus, > 5 ciggies/day can lead to dependence.
Dopamine is released in the ____, which is regulated by presynaptic nAChRs.
nucleus accumbens
*Nicotine activates nAChRs in the Ventral tegmental area
Nicotine: True/False - Treatment of tobacco dependence shoud address the physiological and the behavioral aspects of dependence
True
Physiologic:
- -addiction to nicotine
- -meds for cessation
Behavioral:
- -habit
- -behavior change program
Nicotine: Nicotine is an alkaloid obtained from the leaves of Nicotiana species.
It is a prototype agonist that stimulates different nAChRs (non-specific).
Nicotrine replacement therapy is approved (FDA) for smoking cessation. What are its actions?
- dec. withdrawal symptoms
- -irritability, anxiety, concentration, inc. appetite - decreases craving
- -long term benefit
*nasal sprays = most efficacious
Nicotine: Nicotine is metabolized by the liver into a long-acting metabolite (cotinine).
What is the risk for individuals who are poor metabolizers?
Inc. risk of addiction
NIcotine: Adverse effects of nicotine (esp. high dose) include Nausea, Insomnia and Headache.
What are adverse effects of vaping?
coughing, pulmonary disease
Nicotine: What are drug interactions and contraindications of nicotine use?
- Interactions
a. avoid smoking – N/V, tachycardia, nicotine overdose - Contraindications
- -pregnancy, lactating
- -pulmonary diseases
Nicotine: _____ is FDA approved as a monotherapy for smoking cessation.
It releives symptoms of nicotine withdrawal and craving, and also improves long term abstinence
Buproprion
- dec. weight gain after cessation
- also used in MDD
Nicotine: Buproprione acts by inhibiting both ____ and _____, thereby increasing dopamine and NE. This leads to relief of symptoms.
It also acts by inhibiting _____, whih aids its function as an anti-depressant and in efficacy as a smoking cessation agent.
- Inhibits DAT and NET
2. Inhibits different nAChRs
Nicotine: Buproprione acts by inhibiting both ____ and _____, thereby increasing dopamine and NE. This leads to relief of symptoms.
It also acts by inhibiting _____, whih aids its function as an anti-depressant and its efficacy as a smoking cessation agent.
- Inhibits DAT and NET
- Inhibits different nAChRs
DAT: dopamine transporter
Nicotine: Contraindications to use of Buproprione include:
- Epilepsy
- Bipolar disorder
What are Interactions?
- Drugs that modify CYP enzyme
(e. g. MAO inhibitors) = increase the risk of hypertension.
Nicotine: ______ is FDA approved as monotherapy for smoking cessation. It acts by decreasing nicotine reward.
It relieves symptoms of nicotine withdrawal and craving, with higher efficacy thatn bupropion or NRT.
Veranicline (Chantix)
Nicotine:
- Nicotine binds __1___ nicotinic receptors promoting DA release.
- During smoking cessation, there is NO dopamine release
- Varenicline (partial agonist) binds ___1___ nAChRs with higher affinity than nicotine. This permits inhibition of nicotine binding, while activating nAChRs.
alpha 4 Beta 2 receptors
less DA release than nicotine
Nicotine: Varenicline has minimal liver metabolism and is excreted in the urine.
Side effects include:
- N/V
- Insomnia
- Potential psychiatric effects (black box)
What are contraindications?
- Kidney disease (renal metabolism)
- Psychiatric conditions
- Pregnant/Lactating women
- -potential risk
Nicotine: 2nd line therapies for nicotine addiction include:
- Bupropioe + Nicotine patch
OR buproprione + varenicline - Nortriptyline
- Clonidine
_____ has a higher clinical efficacy than monotherapy as it provides sustained release. This therapy is most often used when monotherapy fails (heavy smokers)
Combination therapy (patch + buproprion)
Nicotine: 2nd line therapies for nicotine addiction include:
- Bupropion combined with nicotine patch or varenicline
- Nortriptyline
- Clonidine
Combination of bupropion and Varenicline has been shown to have a higher clinical efficacy than monotherapy.
*See slide 29
Nicotine: 2nd line therapies for nicotine addiction include:
- Bupropion combined with nicotine patch or varenicline
- Nortriptyline
- Clonidine
_____ is an NE transporter inhibitor (NET inhibitor) that is used when 1st line treatments fail or are contraindicated. It minimizes withdrawal symptoms, but is not FDA approved. It is effective in smokers w/out depression.
Nortriptyline
MOA: NE transporter; NET inhibitor
- effective in smokers w/out depression
- can be combined with nicotine patch
Nicotine: 2nd line therapies for nicotine addiction include:
- Bupropion combined with nicotine patch or varenicline
- Nortriptyline
- Clonidine
____ is very effective during the first stage of withdrawal. It minimizes withdrawal symptoms (from several addictive drugs, including nicotine). It however, does not improve craving
Clonidine
MOA: a2-agonist
*does not treat addiction (does not improve craving)
Nicotine: Which of the following is an adverse effect of Clonidine (anti-HTN)?
a. Dry mouth
b. Sedation
c. Weight gain
d. Dizziness
A and B
*hypotension
Cx: CV disease, pregnancy
Nicotine: Which of the following is an adverse effect of Nortriptyline (anti-depressant)?
a. dry mouth
b. sedation
c. hypertension
d. dizziness
Weight gain, dizziness, HTN
Cx: CV disease
Addiction Medicine: Addiction is a genetic, biological disease, NOT a moral failure.
Addiction may occur via many different substances including:
- Stimulants
- Depressants
- Hallucinogens
List examples of stimulants
- Cocaine
- Nicotine (deadliest in the world)
- Caffeine (most abused substance)
- AMphetamine and Methamphetamine
Addiction Medicine: Addiction is a genetic, biological disease, NOT a moral failure.
Addiction may occur via many different substances including:
- Stimulants
- Depressants
- Hallucinogens
Depressants include _____, opoids, benzos, and marijuana
a. alcohol
b. topiramate
c. caffeine
d. biotin
alcohol
*MJ - depressant/hallucinogen