Mechanism of Drug Action Flashcards
What is Tachyphylaxis
What are the 3 Mechanisms of Tachyphylaxis
Diminution of receptor response due to continuous stimulation
- intracellular proteins G protein access to activated receptor
- Agonist bound receptor is internalized by endocytosis; can be reinserted
- Substrate depletion of downstream processes
Drug inhibitor of these Neurotransmitter Transporters:
Norepinephrine, Serotonin, Dopamine
Tricyclic Antidepressants - Nor-Ser reuptake inhibitor
Fluoxetine - selective Serotonine reuptake inhibitor
Cocaine - Nor-Ser-Dop reuptake inhibitor
What Alpha Glucosidase Inhibitor does
Inhibits the breakdown of polysaccharide into monosacch –> decrease Carb absorption
Benzodiazepine: What receptor is affected, mechanism, result, DR Interaction, use
GABA-activated receptor, Inc in Cl influx, hyperpolarization, allosteric activator, antiepileptic
Affinity but no efficacy
Competitive Inhibitor
Characteristics of Nuclear Receptor Interaction
Slow acting, Persisting, has Lag Phase
Functions of Phosphorylation
Amplification of signals, Flexible Regulation
3 components of Transmembrane Signaling System
Binding, Activation, Effector
Main Effectors of GPCR
Adenylyl Cyclase, Phospholipase C
Verapamil: receptor type, MOA, result, use
Voltage gated ion channel, inhibit Calcium channels in heart and vascular smooth muscle, anti arrhythmic + lower BP
Barbiturates: receptor type, MOA, result, use
GABA activated receptor, bind to receptor to inc Cl influx, hyperpolarization, induce sleep and anesthetic
Carbamazepine, Phenytoin, Lamotrigrine, Valproate: Receptor type, MOA, result, use
Ligand Gated, closes Na channels, no depolarization, anti seizure
What determines the concentration of drug required?
Receptor affinity
What did Paul Erlich do?
Chemotherapy, receptor word
