Session 6 (Pharmacodynamics) Flashcards
What is critical in determining drug action?
Concentration of drug around receptor
Give an equation relating molarity, concentration and molecular weight
Molarity(M)= MWt x conc(g/L)
What drugs activate receptors?
Agonists
In order to be an agonist what must a drug have in addition to affinity for the receptor?
Intrinsic efficacy (ability to switch receptor on)
What is the drug’s ability to cause a response called?
Its efficacy
What type of drug is said to have efficacy?
Agonists
What is efficacy governed by?
Intrinsic efficacy (receptor activation) + things happening to generate a measurable response
What do agonists have to have in order to work?
Affinity, intrinsic efficacy and efficacy
What do antagonists have to have in order to Work?
Affinity alone
How do we measure drug-receptor interactions by binding?
Bind a radioactively labelled ligand to cells or membranes
Change [ligand] and observe the binding patterns
What is Bmax?
The max binding capacity of a receptor (like Vmax but this is about receptors)
What is Kd?
Indicates ligand affinity (like Km)
[ligand] at which half of the receptors are saturated
What does a low Kd mean?
The ligand has a high affinity
How else can affinity of substrates be measured?
Ka (assay)
What is Emax?
Effect max of drug, (max response of drug)
What is EC50?
Effective concentration of drug giving 50% of max response