Pharmacology - Non-medical drug use Flashcards
Where is most alcohol metabolized?
Liver although some metabolism occurs in stomach
With a big meal more stomach metabolism takes place because absorption is slower
T/F On empty stomach, peak alcohol concentration in blood arrives earlier, peak concentration is higher, and total absorption is greater
True
How can you measure absorption?
area under curve on a plasma concentration vs time graph
What are the two liver enzymes involved in alcohol metabolism?
alcohol dehydrogenase
acetaldehyde dehydrogenase
where are alcohol dehydrogenase and acetaldehyde dehydrogenase found within the cell?
alcohol dehydrogenase (cytoplasm)
acetaldehyde dehydrogenase I (cytoplasm - MINOR)
acetaldehyde dehydrogenase II (mitochondria - MAJOR)
enhanced toxicity from alcohol in certain susceptible individuals is due to
rapid metabolizing alcohol dehydrogenase (producing high levels of acetaldehyde) or defective mitochondrial acetaldehyde dehydrogenase
what is disulfiram?
(anabuse) acetaldehyde dehydrogenase inhibitor ==> acetaldehyde builds up and causes toxicity (nausea, vomiting)
T/F oxidation of ethanol via ADH or ALDH both utilize NAD+ as electron acceptor
true
Under what conditions is the P450 system utilized to metabolize alcohol?
Heavy or chronic drinking
Alcohol metabolism exhibits 1st order or zero order elimination kinetics?
Zero order (saturation) kinetics untill very very low levels (.005%) becomes 1st order kinetics (100 mg/kg/hr - at levels this low rate is not dependent on concentration, dependent on body weight)
NAD+ is limiting (saturatable) factor
Microsomal ethanol oxidizing system (MEOS) utilizes which CYP450 enzyme to metabolize alcohol?
CYP2E1
T/F stomach is greatest site of absorption for alcohol
FALSE - small intestine!
Which allele of ADH is responsible for enhanced sensitivity to alcohol in Asians?
ß2 allele
Which neurotransmitter system do LSD, mescaline, psilocybin, MDMA primarily influence?
serotonin
Metabolic symptoms of excessive alcohol intake
hypoglycemia
lactic acidosis
ketoacidosis
hypertriglyceremia
What else does CYP2E1 metabolize?
acetaminophen, theophylline, halogenated anesthetics
T/F signs of cerebellar dysfunction from alcohol include diplopia, nystagmus, dysarthria, ataxia
True
Alcohol increases or decreases HDL levels?
increases (1-6 drinks/week)
Alcohol increases or decreases risk coronary heart failure?
decreases (1-6 drinks/week)
What is considered safe level of alcohol consumption?
1-2 drinks/day for women
2-3/day for men
T/F Acute alcohol use inhibits drug metabolism while chronic use can increase metabolism
True
T/F alcohol inhibits activity of adrenal cortex
False - adrenal cortex is stimulated
What effect does alcohol have on testosterone synthesis?
Decreased testosterone synthesis: male
alcoholics > hypogonadism & feminization,
gynecomastia
Also suppresses uterine motility & milk ejection
T/F alcohol is the most frequent cause of teratogenically induced mental deficiency in the Western world
True
Effects of alcohol on fetus include?
decreased pre and postnatal body length and below mean weight
Facial/limb deformaties
microcephaly, tremor, seizures, slow development, hyperactivity, learning problems, memory problems
Methyl-alcohol causes acidosis visual disturbances and blindness. What is treatment?
ethanol + bicarbinate
What is major symptom of ethylene glycol toxicity?
Nephrotoxicity
acidosis
CNS excitement —> depression
What is major symptom of methanol toxicity?
retinal damage
acidosis
What is major symptom of methanol toxicity?
Nausea, vomiting, headache, HYPOtension
What is major symptom of isopropyl alcohol toxicity?
gastritis, acidosis, CNS symptoms
T/F Treatment for isopropyl alcohol toxicity is ethanol + bicarb
FALSE (this is for methanol) there is no antedote for isopropyl alcohol toxicity
What are roofies? What type of drug?
flunitrazepam - Rohypnol
Benzo
How is cocaine metabolized?
Mostly by plasma cholinesterase but some P450 metabolism
byproduct detected in urine tests is benzoylecgonine
What is current use of cocaine?
topical anesthetic for upper respiratory tract (vasocontrictor and local anesthesia ==> shrinks mucosa)
T/F hallucinogens are schedule I drugs
true
What is MPTP?
failed attempt at making fentanyl that resulted in death of substantia nigra neurons and drug induced parkinsons
LSD is agonist or antagonist of 5HT2A receptors?
agonist - inhibits firing at Raphe nucleus (which is inhibitory) thus agonism disinhibits post-synaptic neurons
What is anandamide?
natral ligand for canbabanoid receptors
MDMA side effects
Possible hypertensive crisis with spontaneous intracerebral hemorrhage paranoid psychosis, cardiac arrhythmias, death
