Pharmacodynamics 1 Flashcards
Drug
Can be naturally occurring or synthetic organic molecule that acts with a receptor to produce physiologic effect
Also antibodies or vaccines
Receptor
Any macromolecule to which an NT or drug binds to initiate effects…function is in neurotransmission of physiologic regulation
Examples of Ion channel drugs
Calcium channel blockers, anti-arrythmic drugs, local anesthetics
GPCRs
On cell surface….where norep and epi act…activates 2ndary messenger
Tyrosine kinase
Dimerize and autophosphorylate…lots of cancer drugs
Steroid hormones
Agonist receptor complex moves to the nucleus and changes protein synthesis
Some receptors
Don’t need anything to bind
Affinity
Determines the binding to the receptor
Electrostatic forces
Measure of strength that a durg binds to receptor
Structural differences will
Result in differences in receptor affinity
Affinity equation
K1/K-1
(DR)/(D*R)
K1 = rate of association K-1 = rate of dissociation
Higher number = higher affinity
Kd equation
Kd = K-1/K1
= (D*R)/(DR)
= 1/affinity
Equilibrium dissociation constant
Kd units and that it means
Concentration
Concentration of a drug that will occupy 50% of the total receptor population
SMaller Kds will
Bind tighter to the receptor
Means that you would need a smaller concentration of the drug to bind to half of the receptors