Sweatman Anti-Smoking therapy

Question 1

what attributes to the physiologic changes associated with addiction regarding nicotine

Answer 1

rapid increase in nicotine in the

brain

Question 2

what attributes to the time of onset and severity of nicotine withdraw and dependence

Answer 2

speed of decline

Question 3

Nicotine is a

Answer 3

• -> parasympatheticomimetic

- -> nACHR agonist

Question 4

reward system of the brain

Answer 4

mesolimbic pathway

Question 5

dependencies associated with nicotine

Answer 5

psychological and physical

*tolerance

Question 6

what brings about physical dependance

Answer 6

attempt to avoid withdrawal symptoms–> habituation
*insomnia irritability, anxiety, lack of focus
restlessness
increased appetite or weight gain

Question 7

VTA contains which types of nACHR’s

Answer 7

alpha-7

alpha-4 beta-2

Question 8

drugs that are addicitive increase what

Answer 8

dopamine

Question 9

dopamine is increased by what 3 mechanisms

Answer 9

1. binding to ion channels–> nicotine
2. binding to GCPR’s–> opiods
3. binding to transporters of biogenic amines–> ecstacy

Question 10

addictiveness of nicotine

Answer 10

amphetamines and cocaine > nicotine and opiates> alcohol and benzo’s

Question 11

best single drug anti-smoking therapy

Answer 11

varenicline

Question 12

partial agonist of alpha4beta2 nACHR

Answer 12

varenicline

Question 13

major side effect of varenicline

Answer 13

suicidal ideation

Question 14

most common adverse effect with varenicline

Answer 14

mild-self limiting nausea

Question 15

varenicline MOA

Answer 15

blocks the effects of additional nicotine challenge while causing release of mesolimbic dopamine
*Acting as a partial agonist varenicline binds to, and partially stimulates, the α4β2 receptor without producing a full effect like nicotine. Thus varenicline does not greatly increase the downstream release of dopamine.

Question 16

Classification of Buproprion

Answer 16

NorEpi and Dopamine re-uptake inhibitor

* decreases cravings and withdrawal symptoms while interacting with pathways underlying addiciton

Question 17

rate the effectiveness of the smoking cessatioin drugs

Answer 17

varenicline> wellbutrin> NRT’s

Question 18

side effects of wellbutrin

Answer 18

dry mouth, insomnia, nausea

Question 19

Blocks cravings, axiety restlessness tension and hunger

Answer 19

clonidine

Question 20

sideeffects of clinidine

Answer 20

dry mouth, dizziness

Question 21

best drug for restless ex smokers

Answer 21

clonidine

Question 22

antihypertensive drug with sedative action

Answer 22

clonidine

Question 23

nicotine agonist

Answer 23

mecamylamine (inversine)

Question 24

ganglionic blocker

Answer 24

mecylamine

Question 25

moderates smoking-cure induced emotional responses in smokers

Answer 25

mecylamine

*best to give with NRT’s coincidingly

Question 26

contraindication for mecylamine

Answer 26

cornary, renal insuficiency, glaucoma, uremia

Question 27

has a side effect of orthostatic hypertension

Answer 27

mecylamine

Question 28

opiate receptor antagonist

Answer 28

Naltrexone (ReVia)

Question 29

Alternative delivery of NRT does what

Answer 29

prevents withdrawal symptoms

Question 30

most constant nicotine blood level

Answer 30

patches

Question 31

goal of NRT–>

Answer 31

• ->produce a sustained plasma nicotine level that can be tapered off gradually–> avoiding symptoms of withdrawal
• ->lower accumulation to peak levels avoiding DOPAMINE release in response to rapidly increasing nicotine levels–>avoid dependence
• slower onset and slower decline will combat addiction and habituation (avoidance of withdrawal)

Question 32

stopping smoking can have wahat effect other than withdrawal, depression

Answer 32

altered PK’s of any concurrent psychiatric drugs

Question 33

COULD NRT be justified in pregnancy

Answer 33

yes, gum is best–> but psychological (counseling) interventions goes first