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VetMed Pharmacology2

VetMed Pharmacology - MOA

QuestionAnswer
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
Created by: 26509889