Pharmacology of Alcohol and Drugs of Abuse - Linger Flashcards
most commonly abused drug in world
ethanol
75% adults in US
use alcohol
only 8% become disorder
ethanol PK
amphipathic - hydrophilic and hydrophobic
first pass metabolism
zero order kinetics
BAC sedation, high, slower rxn time
50-100
BAC impaired motor fxn, slurred speech, ataxia
100-200
BAC emesis, stupor
200-300
BAC coma
300-450
BAC resp depression and death
> 500
0.08% BAC
= 80mg/dL blood alcohol concentration
tolerance
decrease in responsiveness to drug following repeated exposure
can happen in acute alcohol consumption
sensitization
reverse tolerance
increase in responsiveness to drug following repeated exposure
with cocaine
drugs sedative hypnotics
class B - benzos and newer drugs - plateau
class A - barbs, alclhol, older sedative hypnotic - linear - to coma
enzyme of alcohol metabolism
alcohol dehydrogenase (ADH)
aldehyde DH (ALDH)
microsomal ethanol oxidizing system (MEOS)
-CYP450s
enzyme mutations
hyperactive AHD
low active ALDH
accumulate of acetaldehyde
adverse effects
disulfram
inhibit ALDH
aka anabuse
fomepizole
inhibit ADH
tx - methanol OD - so don’t metabolize it
ethanol vs. methanol
ethanol higher affinity for ADH
tx of methanol poisoning
acetaldehyde
toxic - from alcohol metabolism
metabolize 1 mol of ethanol
need 2 mol NAD+
saturate enzymes quickly - zero-order kinetics
tx of alcohol intox
resp support gastric lavage - naloxone (short acting) fluid replacement short acting benzo thiamine (prevent wernicke) glucose
mostly supportive
receptors for ethanol
NMDA - glutamate - excitation (memory impairment)
-ethanol decrease NMDA
GABA-A - inhibition
-ethanol increase NMDA
liver and alcohol
fatty liver > hepatitis > cirrhosis > liver failure
CV and alcohol
cardiomyopathy HF arrhythmia HTN stroke coronary heart disease