Final - Vanrign Pt 2 Flashcards
2 main pathways of action for cocaine
Increase in catecholamines - by being an antagonist of DAT
and
decrease Na+ transport
what drugs can be used for narcolepsy
amphetamine
methylphenidate
armodafinil/modafinil
Sodium Oxybate
which stimulant inhibits BOTH DAT and NET
methylphenidate
which stimulant is a prodrug of amphetamine and modulates dopamine transport
lisdexamphetamine
how do drugs like phentermine for weight loss work?
stimulate release of NE and DA in lateral hippocampus aka feeding center of brain
Nicotine:
full agonist, or partial agonist, or antagonist at nicotinic ach receptors?
full agonist
Nicotinic ach receptors are what kind of structure?
pentameric
T or F: Nicotine is degraded by Acetylcholinesterase just like Ach
False - nicotine is not and thus has a long half life than Ach
what meds can be used for treating nicotine addiction — specifically agonist meds
nicotine patch/gum/e-cig
what meds can be used for treating nicotine addiction — specifically partial agonist meds
varenicline
what meds can be used for treating nicotine addiction — specifically antagonist meds
bupropion
methylxanthines (like caffeine) are ______ to adenosine receptors
antagonists
how does cocaine affect the dopamine transporter
it is an antagonist to it in the nucleus accumbens
same as methylphenidate
how does meth/ecstasy/bath salts affect DA
it pushes DA out from vesicles, changes gradient, whihc forces transporter to work in the reverse
is cocaine or meth a bigger structure?
cocaine - why only an antagonist and doesn’t go inside the cell like meth does to affect vesicle release of DA
Nicotine is inhibitory or excitatory
excitatory
amphetamines are contraindicated with antidepressants???
to vanrijn yes because amphetamines are MAOIs too and that is not ok with antidepressants (but who knows if actually applicable)
crack or cocaine gets smoked and why?
crack does because you add ammonia to make a free base = lower melting temp when free base
bath salt is known as a synthetic ______
cathinone
ADEs of Cathinone use (aka bath salts)
hyperthermia
paranoid delusion
cardiac arrest
anxiety/violence
PK of alcohol:
peaks in ______ minutes
30 - 90
PK of alcohol:
alcohol increase or decrease acid release
increase acid release
PK of alcohol:
absorption is promoted or slowed by food
slowed
PK of alcohol:
has zero, 1st, or 2nd order kinetics
mainly 0 ( but at end it goes to 1st order)
PK of alcohol:
what is the rate limiting step of alcohol
ADH (aka 1st step)
PK of alcohol:
most metabolism is done by what organ
liver
PK of alcohol:
what two things can be done to get alcohol to acetylaldehyde
ADH (alcohol dehydrogenase)
or
MEOS (microsomal ethanol oxidizing system) — only done at high alcohol concentrations
PK of alcohol:
acetylaldehyde gets metabolized by ______
ALDH (aldehyde dehydrogenase)
T or F: acetylaldehyde is an antioxidant
false… well guessing so since the molecule is TOXIC!
what drug is known as an ADH inhibitor and why would you want to use it
Fomepizole
use when methanol ingestion/poisoning – drug given because it prevents acetylaldehyde (a toxic metabolite) from being made
what SNP in ALDH2 reduces activity
ALDH2 *2
what drug is an irreversible inhibitor of ALDH2
disulfiram
what happens if you are heterozygous ALDH2*2
flushing and increase skin temp
reduced metabolized activity
what happens if you are homozygous ALDH2*2
strong!!! hangover
alcoholic neuropathy bc neurotoxic acetylaldehyde
cant really metabolize acetylaldehyde at all
what pharmacological things happen with alcohol at each level:
30 - 60 mg/dL: 60 - 90: 80 - 120: 100 - 200: 300 - 500:
30: euphoria, disinhibition, talkative
60: analgesia
80: CNS stimulation (mood swings, aggression)
100: CNS depression (slurred speech, ataxia)
300: coma/death
alcohol causes hypo or hyper thermia
hypo
alcohol upregulates what CYP enzyme (affects APAP)
CYP2E1
what are the 3 accepted drugs for treating alcoholism
disulfiram
acaprosate
naltrexone
FDA approved drugs for txing alcoholism: MOA of Disulfiram?
ALDH inhibitor
FDA approved drugs for txing alcoholism: MOA of Acamprosate?
NMDA receptor antagonist/GABA agonist
FDA approved drugs for txing alcoholism: MOA of Naltrexone?
opioid receptor antagonist
what SNP in mu receptor gene causes pts (mainly asians) respond better to naltrexone
118G
what are 3 other drugs (NOT FDA approved tho) for txing alcoholism
topiramate (also NMDA receptor antagonist)
Baclofen (GABA(B) receptor agonist)
Varenicline (partial nicotinic receptor agonist)
heroin is also known as ______
diacetylmorphine
aka acetyl groups on pos 3 and pos 6
heroin is lipophillic or hydrophillic
lipophillic bc acetyl groups soooo cross BBB v well!
heroin or morphine is a prodrug?
heroin is! heroin gets metabolized into morphine!
what plant (other than opium poppy) contains opioids
kratom
which is more potent? fentanyl or morphine or heroin
fentanyl by hella much
what drugs are typically being added to heroin recently to make the batches more strong
remifentanil
acetylfentanyl
________ drugs can cause low birth wt and premature birth when mom took them when pregnant
amphetamines/marijauna/nicotine
________ can cause lower IQ/decrease developmental learning when mom took them when pregnant
cocaine
________ can cause heart defects, head/face deformities, and mental problems when mom took them when pregnant
alcohol
how does methadone work for opioid dependence?
is a full agonist for mu opioid receptor but acts slowly/leaves slowly soooo no big peaks
