PharmacologyBasics-UCSDCognitiveScience.pptVIP

* * * * * * * * Response Hi Lo Time A B Additive Effects A + B The effect of two chemicals is equal to the sum of the effect of the two chemicals taken separately, eg., aspirin and motrin. Response Hi Lo Time A B A + B Synergistic Effects The effect of two chemicals taken together is greater than the sum of their separate effect at the same doses, e.g., alcohol and other drugs Response Hi Lo Time A B A + B Antagonistic Effects The effect of two chemicals taken together is less than the sum of their separate effect at the same doses Pharmacodynamics Receptor target/site of drug action (e.g. genetically-coded proteins embedded in neural membrane) Lock and key or induced-fit models drug acts as key, receptor as lock, combination yields response dynamic and flexible interaction Pharmacodynamics (cont.) Affinity propensity of a drug to bind with a receptor Selectivity specific affinity for certain receptors (vs. others) Agonism and Antagonism Agonists facilitate receptor response Antagonists inhibit receptor response (direct ant/agonists) Modes of Action Agonism A compound that does the job of a natural substance. Does not effect the rate of an enzyme catalyzed reaction. Up/down regulation Tolerance/sensitivity at the cellular level may be due to a change in # of receptors (without the appropriate subunit) due to changes in stimulation Antagonism A compound inhibits an enzyme from doing its job. Slows down an enzymatically catalyzed reaction. Agonists/Antagonists Full Partial Direct/Competitive Indirect/Noncompetitive Inverse A single drug can bind to a single receptor and cause a mix of effects (agonist, partial agonist, inverse agonist, antagonist) Functional Selectivity Hypothesis: Conformational change induced by a ligand-receptor interaction may cause differential functional activation depending on the G-protein and other proteins associated with the target receptor Important implications ofdrug-receptor interaction drugs can potentially alter