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VetMed Pharmacology2
VetMed Pharmacology - MOA
| Question | Answer |
|---|---|
| Agonist | pharmaceutical that exerts a specific (desired) biological or physiological response |
| Partial Agonist | agonists that are incapable of exerting 100% level of "intrinsic" biological activity or physiological response |
| Antagonist | pharmaceutical agents that block or inhibit the biological or physiological effect of a given agonist |
| Surmountable Antagonist or Competitive/Reversible Antagonist | pharmaceutical agents that function as an antagonist but their ability to inhibit can be reversed by increasing agonist concentration |
| Insurmountable Antagonist or Non-Competitive Antagonist | antagonists that inhibit the biological or physiological activity exerted by an agonist and cannot be totally reversed no matter how high the agonist concentration |
| Physiological Antagonist | antagonist that exerts a physiological response that is different than and opposite to the one exerted by a given agonist |
| Receptor (Pharm Term) | any biological entity that represents an intracellular or extracellular molecular "target" that a pharmaceutical agent directly interacts with |
| Receptor (Cell Bio Term) | cell membrane-associated proteins or glycoprotein complexes expressed on the exterior membrane surface of cell or within the cytosol that directly interact in a manner that creates a specific biological or physiological effect |
| Ligand | an endogenous compound or biopharmaceutical agent that physically binds to a biological fraction resulting in the formation of a molecular complex |
| Mechanism of Action | how a pharmaceutical interacts with or modifies at the molecular level to create a biological, biochemical or physiological effect |
| Physiological Effect | ultimate biological or physiological effect created by a pharmaceutical agonist |
| Selectivity | relative difference in the dose (concentration) required to exert a desired therapeutic response compared to the much higher dose necessary to induce a secondary undesirable side effect (e.g. sequelae) |
| Additive | a combination of pharmaceutical agents collectively create a common biological or physiological effect at a level that exceeds the efficacy that can be achieved with just one of the agents |
| Synergism | combinations of pharmaceutical agents collectively create a common biological or physiological effect at an efficacy level that exceeds the anticipated "additive" effect of individual agents |
| Isosteres | molecules of equal size and shape but not necessarily of the same chemical composition |
| Physical Characteristics that Influence Binding of Pharmaceutical to Target | chemical form (ionic charge, lipophilic properties) molecular size molecular shape concentration temperature hydrogen ion concentration (pH) competitive antagonists |
| pH/pKa Influence on Pharmaceutical Binding | increases in hydrogen ion concentration (lower pH) usually causes decrease in pharmaceutical binding affinity for "target" molecule (although there are exceptions) |
| Chemical Bonds & Forces Involved in Pharmaceutical Binding | covalent bond (rare) ionic bond hydrogen ion bond Van der Waals forces (weakest, most important) hydrophobic bond forces |
| Potential Biological Outcomes of Pharm/Target Interactions | stimulation inhibition (blockade) expression irreversible inactivation (rare) |
| Pharmaceutical Targets | extracellular enzyme systems intracellular enzyme systems exterior surface membrane-associated receptor complexes intracellular receptor complexes membrane transport molecules cell membranes sub-cellular organelles nucleic acids |
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