Lecture 12 - Substance abuse 2 Flashcards
addictive drugs are addictive because they cause release of ____ at the _____
dopamine, nucleus accumbens
what receptor does this drug act on,..
LSD/mushrooms = ____:
marijauna/K2 = _____;
caffeine =
5HT;
cannabinoid receptors;
adenosine receptors
all act on GPCRs
cocaine and amphetamine prevents reuptake of ____ and ____
dopamine, NE;
also increase release of these things
alcohol:
mainly activates ____ receptors via ____ binding;
also is a ____ receptor inhibitor
GABA-A, allosteric;
NMDA
nicotine - acts as a (Agonist or antagonist) for _____ receptors;
PCP and ketamine are both _____ _____;
of note, these act on ion channels or GPCRs?
agonist, inotropic Ach receptors (ie nicotinic);
NMDA antagonists;
ion channels!
cannabinoids/opioids are thought to act on ____ receptors on _____ interneurons. they bind to ____ proteins and inhibit or stimulate release?
GABA;
VTA;
Gi. inhibit
== increased dopamine release
cannabinoid receptors are notably not expressed where in the brain? this is the reason ____ does not occur with very high dose
respiratory centers;
respiratory depression/coma
what NT is thought to be involved in causing hallucinations?
serotonin
LSD:
causes increased ____ cortex cerebral blood flow;
notably, causes decreased connectivity between parahippocampus and retrosplenial cortex –> cause of “____”
visual;
ego-dissolution
LSD/psilocin bind to ____ coupled ____ receptors = hallucinations
Gq, 5HT
ketamine and PCP:
binding of NDMA receptors inhibits release of ____, disinhibiting ____ ____ neurons = increased firing
glutamate;
cortical pyramidal
LSD and psilocin both contain the ____ Structure, found in endogenous _____
tryptamine;
serotonin
psychedelics:
______ are usually GABA + NMDA related and ____ perception of self and enviornment ie PCP
dissociatives, distort
psychedelics:
deliriants are usually _____ related and cause a ____ State ie salvia, diphenhydramine
anti-Ach;
confused
psychedelics:
hallucinogens give the ____ of perception of sensory cues in the external space and are due to _____ related actions
illusion;
5HT
PCP:
a NMDA antagonist and a ____ receptor _____
causes _____ notably. cause of injury is typically _____
D2, agnoist;
dissociation;
trauma (i.e. self mutilation)
_____ are mainly metabolized by CYP2D6 and CYP3A4–> drug drug interactions
opioids
______ is a benzo that is preferred for alcohol withdrawal because of its additional anti-convulsant capabilities
chlordiazepoxide
name 2 drugs that can cause a disulfiram like reaction. these drugs both inhibit …..
metronidazole, 1st gen sulfonylureas (tolbutaminde;
aldehyde dehydrogenase
alcohol upregulates ____ which can cause liver toxicity with acetaminophen due to increased ______ (toxic metabolite)
CYP2E1;
NAPQI
THC is metabolized in the ____ and excreted via ___
liver, bile
few drug interactions
_____ is used to provide relief from opioid withdrawal because of its extremely long half life
methadone
_____ is a partial mu agonst. what happens when it is given along with presence of a full agonist?
buprenorhpine;
acts as antagonist–>withdrawal symptoms
suboxone is a mixture of what?
if taken sublingually, ____ is active;
if taken via IV, ____ is active
buprenorphine, naloxone;
buprenorphine;
naloxone
reduces abuse potential
nalaxone is not orally bioavailable, but it has effects if injected
_____ is a long acting opioid antagonist used to prevent relapse.
naltrexone
vs naloxone (V short acting for overdose)
diphenoxylate is given with _____ to prevent abuse. what is it used for?
atropine;
anti-diarrheal
alcohol:
CYPE21/microsomal ethanol oxidizing system has a ____ km and is active at _____ alcohol conjcentrations.
alcohol has ____ kinetics
high, high (ie low affinity);
0-order
disulfiram (antabuse) inhibits _____ –> causes hangover like symptoms.
what group often has SNPs in this enzyme?
acetaldehyde dehydrogenase;
asians
asians with ALDH2 SNP:
heterozygotes experience _____ with alcohol consumption;
homozygotes experience _____ with alcohol consumption
flushing (can still drink);
disulfiram like reaction (don’t usually drink)
alcoholism treatment:
_____ is a NDMA receptor antagonist/GABA agonist;
_____ is a opioid recptor antagonist;
acamprosate;
naltrexone
which type of drug screen is more sensitive, urine or blood screen? example of a drug that has a very long half life in blood? what about very short?
blood;
methadone;
LSD