Drug Targets Flashcards
Corticosteroids
Nomenclature: “-son” or “-one”
MOA: bind glucocorticoid receptors and ultimately modulate transcription
Imatinib (Gleevec)
MOA: Y kinase inhibitor binds ATP binding site on bcr-abl
Use: CML
Strychnine
MOA: competitive inhibitor of glycine at glycine receptors
Effect: excessive spasticity
Methylxantines
Ex: caffeine, theophylline
MOA: competitive inhibitors of adenosine receptors
Tetrodotoxin
MOA: blocks voltage gated Na+ channels in nerve and muscle
Midazolam metabolism
MOA: benzodiazipine - increases frequency of GABAa receptor Cl- channel openings
Metabolism: CYP3A4 + glucuronide conjugation
Benzodiazepines
Nomenclature: “-azepam” or “-azolam” drugs
MOA: allosteric activator of GABAa receptors, increasing frequency of GABAa-gated Cl- channel opening and increasing synaptic inhibition.
Tetanus toxin
MOA: presynaptic inhibitor of glycine release
Effect: excessive spasticity
Memantine
MOA: open channel blocker (uncompetitive inhibitor) of glutamate-NMDA Ca2+ channel
Use: Alzheimer’s
Cimetidine metabolism
MOA: H2 histamine receptor blocker
Notes: also inhibits many CYPs
Diazepam (Valium)
MOA: Allosteric activator of GABAa gated Cl- channel
Notes: Good TI (~100)
Zolpidem (Ambien)
MOA: allosteric activator of GABAa-gated Cl- channel
Use: sleep aid
Local anaesthetics
MOA: block voltage gated Na+ channel associated with the action potential; preferentially binds inactivated state of channel
Warfarin
MOA: inhibits synthesis of clotting factors via inhibition of VKORC1
Use: Prevent clots after surgery, Afib
Notes: Low TI (~1)
Penicillin
MOA: open channel blocker of GABAa receptor
Effect: inhibition of inhibitory signalling => excessive excitation and seizures
