Pharmacology of Ethanol

Question 1

Where is EtOH absorbed?

Answer 1

in the whole GI tract but esp the small intestine

Question 2

Name 3 important ezymes for EtOH metabolism. Which one(s) can be targeted with drugs?

Answer 2

Alcohol dehydrogenase
CYP2E1
aldehyde dehydrogenase *** inhibited by disulfram (Antabuse)

Question 3

What is Disulfram (Antabuse)?

Answer 3

an alcohol sensitizing drug that blocks aldehyde dehydrogenase –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions

Question 4

This is an alcohol sensitizing drug that blocks aldehyde dehydrogenase –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions.

Answer 4

Disulfram (Antabuse)

Question 5

How is BAC calculated?

Answer 5

r factor male = 0.68, female = 0.55 (women have more body fat)
Grams EtOH/ grams body weight = EtOH in the body- divide by r factor –> BAC

Question 6

_____ increases acetyladehyde levels by 5-10x.

Answer 6

Disulfram (Antabuse)

Question 7

Disulfram (Antabuse) increases ______ levels by 5-10x.

Answer 7

acetyladehyde

Question 8

______ –> decreased Krebs, decreased gluconeogenesis –> hypoglycemia

Answer 8

Increased NADH

Question 9

Increased NADH –> _______ –> hypoglycemia

Answer 9

decreased Krebs, decreased gluconeogenesis

Question 10

Increased NADH –> decreased Krebs, decreased gluconeogenesis –> ______

Answer 10

hypoglycemia

Question 11

How does EtOH causes emesis?

Answer 11

Stimulates chemoreceptor trigger zone + GI irritation

Question 12

What are the effects of EtOH on the liver?

Answer 12

reversible fatty liver –> cell death and replacement by collagen –> cirrhosis; esophageal varices; decreased synthesis of clotting proteins –> increased bleeding time

Question 13

What are the effects of EtOH on the kidney?

Answer 13

when BAC is rising, inhibits ADH –> diuresis

Question 14

What are the effects of EtOH on the GI tract?

Answer 14

irritant –> ulceration (esp. when taken with aspirin); pancreatitis; decreased nutritional absorption

Question 15

What are the effects of EtOH on the fetus?

Answer 15

prenatal or postnatal growth retardation AND altered morphogenesis AND CNS involvement

Question 16

What is EtOH dependence?

Answer 16

continued administration is needed to prevent the appearance of withdrawal symptoms; involves resetting of homeostatic mechanisms

Question 17

What is EtOH tolerance?

Answer 17

decreased response to same dose

Question 18

What is EtOH withdrawal?

Answer 18

rebound effects on the physiological systems that have been modified by chronic drug use, and such effects are the opposite of the acute effects of the drug

Question 19

This is a decreased response to same dose.

Answer 19

tolerance

Question 20

This is when continued administration is needed to prevent the appearance of withdrawal symptoms; involves resetting of homeostatic mechanisms.

Answer 20

dependence

Question 21

What is withdrawal?

Answer 21

rebound effects on the physiological systems that have been modified by chronic drug use, and such effects are the opposite of the acute effects of the drug

Question 22

List the major drug-drug interactions associated with alcohol use.

Answer 22

a. Additive to CNS depressants but cross tolerance can develop chronically (ex. anesthetics and benzos)
b. Aspirin –> GI bleeding
c. Disulfram-like symptoms if taken with metronidazole or oral hypoglycemics

Question 23

How do you treat acute EtOH intox.?

Answer 23

resp. support, IV fluids, glucose, thiamine, electrolytes (K+ and Mg++)

Question 24

How do you treat EtOH withdrawal?

Answer 24

Benzos (chlordiazepoxide, lorazepam) to prevent hyperexcitability of CNS via cross-tolerance
α2 adrenergic agonists (clonidine) for ANS hyperactivity