pharmacodynamics

pharmacodynamics

1. pharmacologic effect

   • clinical response
     • toxicity
     • efficacy

2. Target Sites

   • Non-specific interactions/non receptor mediated mechanism
     • chemical rxn (non receptor-mediated mechanism
       • antacid
     • surfactant (non recept. med. rxn
       • docusate sodium
     • protein denaturation (shrink, tighten mucus membranes, anti-inflammatory effects,
       • astringents
     • osmotic effects
       • alter the flow of h2o b/t compartments
         • diuretics
           • mannitol
     • selective toxicity
       • chemotherapy compounds
         • targets a select grp of cells
           • Lipids: amphotericin B
           • Nucleic Acids
             • DNA
               • daunorubicin, doxorubicin
             • RNA
               • macrolides, aminoglycosides, fomivirsen, amantidine

3. 4 levels for mechanism of drug action

   • Molecular
     • targets regulatory receptors
   • cellular
     • drug binds to receptor to signaling pathway to start or be inhibited
   • tissue
     • affects fxn of organ
   • system
     • organ system fxn is altered

4. Ligand

   • moecule or compd that interacts with a receptor
     • Albuterol
       • acts on Beta 2 receptor which is activated, inducing intracellular changes, PKA phosphorylates enzymes to inhibit muscle contraction, cAMP keeps calcium in ER 
   • selective sub typing
     • Based on what the drug binds to

5. Receptors

   • Regions
     • Extracellular
     • intracellular
       • to reach this type of active site, a drug needs to be lipophilic or small to go thru the pores of the cell membrane; can diffuse through a transporter
     • transmembrane
   • Classification
     • 2 overlapping systems
       • Neurotransmitter Receptors
         • Gprotein coupled receptors
           • acetylcholine, serotonin
         • ligand gated ion channels
           • Acetylcholine, serotinin
       • G-Protein Coupled Receptors
         • Neurotransmitter: norepinephrine
         • Peptides: Glucagon