Alcohol Treatment

Question 1

Acute (infrequent) ethanol use produces its sedative-hypnotic effects by acting at which 3 target receptors and do they mediate excitatory or inhibitory neurotransmission?

Answer 1

GABA(a) inhibitory
glycine inhibitory
NMDAR excitatory

Question 2

Does acute (infrequent) ethanol use shift the balance toward inhibitory or excitatory neurotransmission?

Answer 2

inhibitory

Question 3

Acute (infrequent) ethanol use produces euphoric and rewarding effects by acting on what pathway, and does it increase or decrease neurotransmission along this pathway?

Answer 3

Mesolimbic DA pathway (VTA –> NAc; Increases neurotransmission signaling reward)

Question 4

CNS responds to chronic (frequent) ethanol intake with what 4 compensatory changes?

Answer 4

Decreased GABA and glycine R sensitivity
Decreased DA release along the reward pathway
Increased NMDAR density and sensitivity

Question 5

4 drugs/classes of drugs used in treatment of alcohol withdrawal

Answer 5

thiamine, benzos, anticonvulsants, antipsychotics

Question 6

Why each of these 4 drugs/classes useful for this indication?

Answer 6

thiamine: treat/prevent Wernicke’s encephalopathy
benzos: taper off of alcohol by substituting another GABA(a) receptor agonist that is safer and easier to titrate
anticonvulsants: treat seizures
antipsychotics: treat hallucination and agitation

Question 7

3 drugs used in preventing relapse of alcohol use disorders

Answer 7

disulfiram
naltrexone
acamprosate

Question 8

Which receptor does disulfiram target?

Answer 8

inhibits aldehyde dehydrogenase (ALDH) irreversibly

Question 9

Which receptor does naltrexone target?

Answer 9

long-acting opioid receptor antagonist that blocks reward pathways

Question 10

Which receptor does acamprosate target?

Answer 10

acts as a weak NMDAR antagonist (and possible GABA(a) agonist)

Question 11

Mechanism of disulfiram

Answer 11

inhibits ALDH enzyme thus reducing metabolism of acetaldehyde, causing it to accumulate and make you feel bad when you drink

Question 12

Useful effect of acamprosate

Answer 12

reduces alcohol cravings

Question 13

Major precautions for naltrexone

Answer 13

screen for opioid use/abuse

Question 14

Major precaution for acamprosate

Answer 14

dangerous to use in patients with renal impairment

Question 15

What does the term “tolerance development” mean and how is it related to the compensatory changes after chronic exposure?

Answer 15

need for higher dose to produce same effect; caused neuronal adaptations; they counter the effects of ethanol

Question 16

Alcohol withdrawal syndrome and its symptoms

Answer 16

-removal of alcohol which induces a rebound stimulatory effect (hyperexcitability)
-insomnia, hallucinations, seizures, delirium tremens