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Pharmacokinetics/dynamics
types of receptors etc
16
Medical
Professional
04/24/2013

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Term
Pharmacokinetic
Definition
absorbtion, distribution, elimniation
Term
Pharmacodynamic
Definition
microenvironment of receptor
Term
Receptor types and speeds
Definition
1. Ion channel - fastest
2. Enzyme dimers - 2nd slowest
3. G-protein
4. Steroid Hormone - slowest and in cytoplasm
Term
Kd
Definition
=1/affinity = (d)(r)/(dr)

= concentration @ 50% receptors occupied
Term
Intrinsic activity
Definition
ability agonist to impart stimulus from binding receptor
either FULL or PARTIAL AGONIST
Term
Receptor reserve
Definition
Non-linear response to receptor occupancy

*not 100% receptors need to be bound in order to elicit a maximum response*
Term
ED50
Definition
Dose at which 50% of maximal effect is elicited
Term
Potency
Definition
concentration required to produce required effect (IE affinity)
Term
Efficacy
Definition
Maximum stimulus a drug can impart
Term
Reversible Antagonist
Definition
Can be replaced/compensated for with higher doses of agonist... shift dose response curve right

also called competitive
Term
Partial agonist on fll
Definition
can actually antagonize full agonists!!
Term
Irreversible antagonist
Definition
bind functional groups
cannot be overcome by agonist

think warfarin, aspirin, clopidogrel
Term
constituatively active receptor
Definition
does not need a ligand to assume active conformation

bound by inverse agonist!!
Term
drug that occupies only one receptor type
Definition
specific
Term
drug that occupies multiple receptor types but only produces one type of effect at one concentration
Definition
selecitve
Term
Theraputic Index
Definition
LD50/ED50 (always greater than one)
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