A reversible competitive antagonist results in inhibition that can be overcome by increasing the concentration of agonist. Local anesthetics cause loss of sensation by blocking nerve conduction only in the particular area where they are applied.
In reality, it is this pharmacokinetic variation that explains most of inter-individual variation in drug response seen in clinical practice.
It considers both drug action, which refers to the initial consequence of a drug-receptor interaction, and drug effect, which refers to the subsequent effects. An irreversible competitive antagonist also involves competition between agonist and antagonist for the same receptors, but stronger binding forces prevent the effect of the antagonist being fully reversed, even at high agonist concentrations.
See Symposium on Drug Antagonism, Pharm.
The receptor concept: pharmacology's big idea. Therapeutic index simulation This is the fourth in a series of 4 simulations related to dose-response relationships.
Arrestins bind to the intracellular portion of the opioid receptor, block G-protein signaling, and induce receptor endocytosis.