Lecture 65: Nicotine

Question 1

How many adults are current smokers?

Answer 1

21%

Question 2

What is epidemiology of nicotine use/smoking

Answer 2

Nicotine dependence is present in 59% of smokers

• tobacco’s main ingredient is nicotine
• leading PREVENTABLE cause of disease

Question 3

What is nicotine?

Answer 3

A psychoactive drug
An alkalid that binds at nicotinic CHOLINERGIC receptors
Can induce tolerance and withdrawal
Increases dopamine release because they are Na and Ca channels

Question 4

What are the properties of nicotinE?

Answer 4

-bind to cholinergic receptors
10-20 seconds required for nicotine to reach brain
Half-life of nicotine is 1.5 hours so that’s why people smoke so frequently
Metabolism through CYP2A6

Question 5

What is the risk of nicotine addiction?

Answer 5

33%
When you smoke, nicotine reinforces behavior
Activates Reward system through mesocorticolimbic system

Question 6

What is the purpose of Nicotinic acetylcholine receptors (NAchRs)?

Answer 6

NAchRs modulate dopamine activity
Nicotine binds to NAchRs and increase dopamine release
-also activates glutamate and GABA

Question 7

What is MOA of nicotine addiction?

Answer 7

Nicotine increases the PHASIC dopamine release from accumbal slices and inhibits the TONIC firing dopamine release

• creates a larger DIFFERENCE between basal synaptic dopamine levels and phasic firing
• magnitude of difference is electrophysiologic measure of rewarding valence of drug

Question 8

What is the Fagerstrom Test for Nicotine Dependence?

Answer 8

1. smokes first cigarette within 30 minutes of awakening
2. difficulty refraining from smoking in forbidden places
3. Smokes a pack a day or more
4. cigarette that they would hate most to give up is first one in morning

Question 9

What are current treatments for nicotine addiction?

Answer 9

1. Abrupt cessation (“Cold Turkey”) or self-help efforts
2. Cessation counseling
3. Medications
   i. nicotine replacement therapy
   ii. Buproprion SR
   iii. Varenicline
4. Combination of counseling and medication

Question 10

How effective is abrupt cessation?

Answer 10

5% long-term abstinence…not effective
70% of smokers see physician annually and just recommending stopping increases quit rates..
-brief intervention

Question 11

How do you stage a brief intervention for quitting?

Answer 11

1. set a quit date
2. review past quit attempts
3. emphasize that abstinence is the goal
4. prescribe pharmacotherapy to maintain abstinence
   Brief advice is important!

Question 12

How do you stage an intensive counseling?

Answer 12

1. Cognitive behavioral strategies
2. Motivational interviewing techniques
3. Reaches fewer patients
4. more appropriate for addicted smokers

Question 13

Who should receive pharmacotherapy for smoking therapy?

Answer 13

Everyone except

1. smoking fewer than 10 cigs a day
2. pregnant/breastfeeding women
3. adolescent smokers

Question 14

What are types of first-line nicotine therapies?

Answer 14

. Nicotine Replacement Therapy (NRT)
	-gum
	-patch
	-inhaler
	-nasal spray
	-Lozenge
All of them improve abstinence
2. Buproprion SR
3. Varenicline

Question 15

What nicotine replacement therapy is over the counter? Prescription only?

Answer 15

Gum and Patch are OTC

Inhaler and nasal spray

Question 16

What is significant about nicotine gum?

Answer 16

1. abstinent rates are 30-80% higher than placebo
2. should be used with caution in patients with TMJ or dental problems
   -you don’t chew like regular gum
   Chew and Park

Question 17

What is significant in the nicotine patch?

Answer 17

1. only thing that doesn’t need a prescription lol
2. 8-12 week treatment, 50% replacement
   Effective
   Contraindicated in persons with severe skin disorders

Question 18

What is significant about Buproprion?

Answer 18

Bup + transdermal nicotine = more effective in abstinence

An antidepressant that has antiadrenergic properties?

Question 19

What is significant about combination therapies?

Answer 19

Combining nicotine patch with a self-administered from of nicotine replacement therapy is more efficacious than either individually
Combined therapy = second line treatment

Question 20

What is Varenicline?

Answer 20

A drug used to treat nicotine addiction
Decreases dopamine release while decreasing craving
Most effective at treating nicotine addiction
Aka Chantix

Question 21

What is the MOA of Varenicline?

Answer 21

Partial agonist at alpha4beta2 nicotinic acetylcholine receptor
Agonist: relieves craving and withdrawal
Antagonist: blocks satisfaction and rewarding effects!
Wow, perfect drug if not for the side effects

Question 22

What are the side effects of Varenicline?

Answer 22

1. suicide
2. CV disease!
3. nausea

Question 23

How does health risks of smoking compare to risk associated with smoking cessation treatments?

Answer 23

Health risks associated with smoking cessation treatments are dwarfed by risk of risks of continued smoking