week 1 Flashcards
Receptors have three common
properties
Sensitivity, Selectivity, Specificity
Sensitivity
Drug response occurs from a low
concentration
Selectivity
Produced by structurally similar chemicals
Specificity
The response from a given set of receptors is
always the same because the cells themselves
determine the response
Bonds that form between drugs and
receptors
– van der Waals
– Hydrophobic
– Hydrogen
– Ionic
– Covalent
Affinity
Degree of attraction between
a drug and its receptor on the cell’s
surface
Efficacy
a drug’s capacity to produce
an effect
Pure Antagonists
– Are similar in molecular structure to
their corresponding agonist drugs
– They have receptor affinity, but lack
intrinsic activity or efficacy
Agonist-Antagonists
Second major type of antagonist drugs
– Have receptor protein affinity and
intrinsic activity, but often only a
fraction of the potency of the pure
agonist
* Nalbuphine (mixed agonist-antagonist)
Physiologic Antagonism
– Involves two agonist drugs that bind to
different receptors
– Both drugs bind to specific unrelated
receptor proteins and initiate a protein
conformational shift with elicited
individual tissue response
– These responses however generate
opposing forces
* Isuprel and Levophed
Chemical Antagonism
– Occurs when a drugs action is blocked
and no receptor activity is involved
– Example
* Protamine
* Sugammadex