[2] Mechanism Of Drug Action Flashcards
Two mechanisms of drug action
Receptor mediated
Non receptor mediated
What are responsible for selectivity of drug action?
Receptors
Most receptors are made up of?
Protein macromolecules
What are the exceptions to the common chemical structure of receptors?
DNA
2 Major Domains in the Receptor
Ligand Binding Domain
Effector Domain
Main Targets of Drugs (4)
Regulatory Proteins
Enzymes
Transport Proteins
Structural Proteins
(Targets are not always necessarily receptors!)
Function: Alpha Glucosidase Inhibitor
What is the effect of inhibition of this?
Enzymatic digestion of polysaccharides into monosaccharides
Delayed absorption of carbohydrates
4 Receptor Superfamilies
Ligand Gated Ion Channels (Ionophores)
Enzyme-Linked
G-Protein Coupled Receptor
Nuclear Receptor
Examples of Ligand Gated Channels (4)
Acetylcholine
Serotonin
GABA
Glutamate
Acetylcholine binding to the receptor allows the entry of what?
Sodium
Mechanism of Action: Barbiturates and BZD
Increases intracellular chloride in the cells, causing a net hyper polarization resulting in decreased stimulation
Time Course of Action: Ligand-Gated Ion Channels
Milliseconds
Function: Verapamil
Inhibit voltage gated calcium channels
Anti Arrythmic, reduces BP
How many transmembrane domains are present in GPCRs?
7
What is the largest superfamily of receptors?
G Protein Coupled Receptors
