all drugs midterm #2 Flashcards
for all drugs, name the receptor target, treatment/use, and type of mechanism
propanol
type of drug?
effect?
pharmacological use?
beta blocker
decrease blood pressure
prophylactic migraines
gabapentin
type of drug?
effect?
pharmacological use?
anticonvulsant
block pain transmission
migraine prophylactic
amitriptyline
type of drug?
effect?
pharmacological use?
antidepressant
blocks SERT (SSRI)
prophylactic migraine
caffeine
target and action?
effect on vessels?
adenosine receptor antagonist
vasoconstriction
migraines
ergotamines site of action and mode of action? possible side effect? use? excretion?
5BT-1b/d agonist
coronary vasoconstriction
migraines
bile
triptans site of action and mechanism? what does it do to improve migraines? what enzyme in the liver metabolizes excretion?
5-HT1b/d selective agonist vasoconstriction and inhibition of trigeminal nerve monoamine oxidase urine migraines
BIBN4096 Olcegepant
issues?
abandonment phase?
mechanism
poor bioavailability
abandoned at Phase II
CGRP antagonist
migraines
MK-0974 Telcagepant
issues?
abandoned at what phase?
mechanism?
elevation of aminotransferase
abandoned at Phase III
CGRP antagonist
migraines
Rimegepant (Nurtek)
mechanism?
CGRP antagonist
migraines
Lysergamides where do they come from? type of hallucinogen? target? activates what in G pathway?
ergot alkaloids
classical hallucinogen
5HT-2a partial agonist
phospholipase A2
Psilocybin
site of action, mechanism and affinity
type of drug
metabolized to ___
5HT-2b/c high affinity, and 5HT-2a low-affinity partial agonist
prodrug
psilocin
classical hallucinogen
Phencyclidine
type of hallucinogen
mechanisms and sites of action
dissociative hallucinogen
NMDA receptor antagonist & dopamine transporter inhibitor
nitrous oxide
type of hallucinogen
mechanisms (3)
dissociative
non-competitive NMDA antagonist
stimulate the endogenous opioid release
positive allosteric modulator of GABA
datura stanmonium
tropane alkaloids within this plant?
mechanism
type of hallucinogens
scopolamine, atropine
antagonist at muscarinic cholinergic
deliriant
pencillin
type of antibiotic
target and action
cell wall inhibitor beta lactam
inhibits cell wall by inhibiting DD-transpeptidase
cephalosporins type of antibiotic function and mechanism
cell wall inhibitor betta lactam
inhibits cell wall by inhibiting DD-transpeptidase
vancomycin
type of antibiotic
mechanism
cell wall inhibitor
inhibits peptidoglycan cross linking
sulfonamides and trimethoprim
mode of action?
type of antibiotic?
resemble PABA and dihydrofolic acid
folic acid inhibitor
chloramphenicol and macrolides
type of antibiotic
mechanism
protein synthesis inhbitors
bind to 50S subunit and block transpeptidation
tetracyclines
where do they bind
what kind of antibiotic
mechanism
30s subunit
protein synthesis inhibitor
prevent binding of tRNA
aminoglycosides
type of antibiotic?
binding site?
actions
protein synthesis inhibtion
30s ribosomal subunit
block initiation of complex, cause misreading, inhibit translocation
TRV250
site of action mechanism
function
delta-opioid receptor biased agonist
benefits without seizure liability
opioid
CR845 function and site
kappa agonist
analgesic
opioid
methodone site of action function and use
mu opioid agonist
opioid use disorder
buprenorphine
site of action and mechanism
use
partial agonist at mu opioid
antagonist at kappa and delta
agonist replacement therapy
naloxone
mechanism and sitr?
non-selective competitive opioid antagonist
codeine
type of drug
metabolized by ____ into _____
prodrug
CYP2D6, morphine
morphine
metabolized by___
UGT2B7
beta-endorphins, enkephalins, dynorphins
type of opioid
endogenous opioid receptors
THC
site and mechanism
metabolized by ____
partial agonist at CB1
cytochrome P450 2C9
CBD
site of action and mechanism
negative allosteric modulator at CB1
Nabilone and Dronabilone
type of drug
mechanism
synthetic cannabinoids
partial agonist at CB1
nabiximols (sativex)
mixture
1:1 TBH anf cannabinol
rimonabant
site of action
use
inverse agonist at CB1
obesity
AEA and 2-AG site of action and mechanism where does it come from type of neurotransmitter broken down by \_\_\_\_
CB1
endocannabinoid (made in vivo)
retrograde
FAAH and MAGL
benzodiazepine
mechanism and site of action
what does it do to this receptor
increases potency or efficacy
positive allosteric modulator at GABA receptors
increases the frequency at which the GABA receptor opens
increases potency
seizure
barbiturates
mechanism and site of action
what does it do to this receptor
increases potency or efficacy
positive allosteric modulator at GABA
increase duration that GABA is open
increases efficacy
seizure
vigabatrin
what does it treat
site and mechanism
seizures
inhibits GABA aminotransaminase
tiagabine
mechanism and site of action
treatment for ___
inhibits GABA transporter
seizures
gabapentin
mechanism and site
inhibits voltage-gated Ca channels, reducing neurotransmitter release
seizures
perampel
mechanism of action
non-competitive antagonist at AMPA
seizures
reserpine
what was it used for
what did it cause and how
antihypertensive drug
caused depression because it depletes neurons of dopamine and norepinephrine
ipronoazid
mechanism
inhibits monoamine oxidase which breaks down amines
depression
selective reuptake inhibitors ex) fluoxetine function mechanism of action
inhibit serotonin or noradrenaline transporters to increase extracellular concentration of these neurotransmitters
depression
ketamine
site and mechanism of action
noncompetitive NMDA receptor antagonist
opioid and depression
haloperidol
mechanism
type of antipsychotic
type of kinetics
D2 receptor antagonisr
first generation
fast on slow off
depression
chlopromazine
mechanism
type of antipsychotic
Kinetic type
D2 receptor antagonist
frist generation
fastt on fast off
