Pharmacology of Ethanol Flashcards
Where is EtOH absorbed?
in the whole GI tract but esp the small intestine
Name 3 important ezymes for EtOH metabolism. Which one(s) can be targeted with drugs?
Alcohol dehydrogenase
CYP2E1
aldehyde dehydrogenase *** inhibited by disulfram (Antabuse)
What is Disulfram (Antabuse)?
an alcohol sensitizing drug that blocks aldehyde dehydrogenase –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions
This is an alcohol sensitizing drug that blocks aldehyde dehydrogenase –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions.
Disulfram (Antabuse)
How is BAC calculated?
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
_____ increases acetyladehyde levels by 5-10x.
Disulfram (Antabuse)
Disulfram (Antabuse) increases ______ levels by 5-10x.
acetyladehyde
______ –> decreased Krebs, decreased gluconeogenesis –> hypoglycemia
Increased NADH
Increased NADH –> _______ –> hypoglycemia
decreased Krebs, decreased gluconeogenesis
Increased NADH –> decreased Krebs, decreased gluconeogenesis –> ______
hypoglycemia
How does EtOH causes emesis?
Stimulates chemoreceptor trigger zone + GI irritation
What are the effects of EtOH on the liver?
reversible fatty liver –> cell death and replacement by collagen –> cirrhosis; esophageal varices; decreased synthesis of clotting proteins –> increased bleeding time
What are the effects of EtOH on the kidney?
when BAC is rising, inhibits ADH –> diuresis
What are the effects of EtOH on the GI tract?
irritant –> ulceration (esp. when taken with aspirin); pancreatitis; decreased nutritional absorption
What are the effects of EtOH on the fetus?
prenatal or postnatal growth retardation AND altered morphogenesis AND CNS involvement
What is EtOH dependence?
continued administration is needed to prevent the appearance of withdrawal symptoms; involves resetting of homeostatic mechanisms
What is EtOH tolerance?
decreased response to same dose
What is EtOH withdrawal?
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
This is a decreased response to same dose.
tolerance
This is when continued administration is needed to prevent the appearance of withdrawal symptoms; involves resetting of homeostatic mechanisms.
dependence
What is withdrawal?
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
List the major drug-drug interactions associated with alcohol use.
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
How do you treat acute EtOH intox.?
resp. support, IV fluids, glucose, thiamine, electrolytes (K+ and Mg++)
How do you treat EtOH withdrawal?
Benzos (chlordiazepoxide, lorazepam) to prevent hyperexcitability of CNS via cross-tolerance
α2 adrenergic agonists (clonidine) for ANS hyperactivity
