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27 Cards in this Set

  • Front
  • Back
What type of drug is nicotine?
Highly addictive psychoactive drug
What three methods have the strongest evidence of effect for smoking cessation?
1. Advise to quit/avoid second-hand smoke
2. OFFER NICOTINE REPLACEMENT THERAPY and/or NON-NICOTINE MEDICATIONS
3. Recommending a smoking cessation program
What is the leading cause of preventable death in the US today?
Smoking
Do cigarettes or non-cigarette products show more sustained levels of nicotine?
Non-cigarette
What is responsible for triggering the physiological changes in the brain associated with addiction?
The rapid increase in nicotine in the brain
What does the speed of decline in nicotine dictate?
Time of onset and severity of nicotine withdrawal symptoms
Where are the nicotine acetylcholine receptor subtypes that we focused on located? What were the names?
Ventral tegmental area
alpha-7, alpha-4, beta-2
Describe the acute stage of nicotine exposure.
Activation of GABA
Rewarding effects though GABA-dependent system that projects into the TPP (alpha-7 subunit)
Also, direct action on nAChRs with beta-2 subunit on GABA or DOPAMINE neurons.
Describe the chronic stage of nicotine exposure.
GABA becomes desensitized.
Leads to net shift in action of nicotine to DA neurons.
Mediated by increase in glutamatergic input to the DA system.
Responsible to aversive nicotine craving/withdrawal and sensitized incentive salience signal to nucleus accumbens.
What three processes do addictive drugs work through to modulate drug levels?
Ion channel modulation
G-protein coupled receptors
Amine transporter process
What do all addictive drugs significantly increase?
Dopamine concentration in target structures of the mesolimbic projection.
What is nicotine more addictive than?
Less addictive than?
On par with?
Alcohol or benzodiazepines
Amphetamine or cocaine
Opiates
What is the most effect single drug for smoking cessation?
VARENICLINE (Chantix)
What is its mechanism?
Partial agonist of a-4,b-2 nicotinic receptor
Blocks effect of additional nicotine challenge while causing release of mesolimbic dopamine
What is a serious side effect of non-nicotine replacement therapy?
Psychiatric (from nicotine withdrawal and from drug induced action)
SUICIDE
Common adverse effect is nausea
What drug is better than nicotine replacement but less effective than varenicline?
BUPROPION (Wellbutrin SR)
What is its mechanism?
Nori and dopa re-uptake inhibitor
Decreases cravings and withdrawal symptoms
May reduce depressive symptoms of withdrawal
What is an oral antihypertensive drug used for smoking cessation?
What does it do?
What patients should take it?
CLONIDINE (catapres) --oral or patch
Blocks cravings, anxiety, restlessness, tension, and hunger
Agitated ex-smokers (has a sedative effect)
Some side effects = sedation, dry mouth, dizziness
Which drug is a nicotine antagonist (ganglionic blocker)?
What patients should not take it?
What are some common AEs?
What is it best used in combination with?
MECAMYLAMINE (Inversine)
Coronary or renal problems, glaucoma, uremia patients
Orthostatic hypotension, sedation, N/V, dry mouth
In combination with nicotine replacement therapy
Which drug is an opiate antagonist?
What else is it used to treat for?
What does recent research say?
NALTREXONE (ReVia)
Alcoholism
Not effective for smoking cessation
What is the goal of nicotine therapy?
To produced a sustained plasma nicotine level that can be tapered off gradually (avoid symptoms of withdrawal)
Slower accumulation to peak levels to avoid dopamine release.
What produces the most constant nicotine blood level?
The patch
Who should not take patches?
*Stimulates both branches of autonomic nervous system
CV disease, diabetics, hepatic problems, peptic ulcers, pheochromocytoma, and uncontrolled hyperthyroidism
DO NOT SMOKE WHILE ON PATCH!
What is a problem with nicotine gum?
Patients may transfer addiction from cigarettes to gum.
Which NRTs are the best?
Spray > inhaler (less data), then patch > gum (much more data)
What are the potential harms of quitting smoking?
Withdrawal symptoms, depression, changes in metabolism can affect PKs of certain psychiatric drugs.
If patient refuses to quit smoking (give up nicotine), what is an option?
Oral nicotine replacement therapy (not the best choice, but better than smoking cigarettes).