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OVERVIEW OF PHARMACODYNAMICS Pia C. Campo, RPh
PHARMACODYNAMICS ,[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],MECHANISMS OF DRUG ACTION
 
RECEPTORS ,[object Object],[object Object]
RECEPTOR INTERACTIONS Agonist Receptor Agonist-Receptor Interaction Lock and key mechanism
RECEPTOR INTERACTIONS Receptor Perfect Fit! Induced Fit
RECEPTOR INTERACTIONS Antagonist Receptor Antagonist-Receptor Complex DENIED! Competitive Inhibition
RECEPTOR INTERACTIONS Agonist Receptor Antagonist ‘ Inhibited’-Receptor DENIED! Non-competitive  Inhibition
AGONISTS, ANTAGONISTS AND PARTIAL AGONISTS ,[object Object],[object Object]
AGONISTS, ANTAGONISTS AND PARTIAL AGONISTS ,[object Object]
[object Object],[object Object],LOW EFFICACY PARTIAL AGONISTS
[object Object],MODERATE EFFICACY PARTIAL AGONISTS
HIGH EFFICACY PARTIAL AGONISTS ,[object Object]
[object Object],AGONIST
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],AFFINITY VERSUS EFFICACY
[object Object],[object Object],[object Object],[object Object],[object Object],ANTAGONISM
[object Object],[object Object],[object Object],[object Object],ANTAGONISM
DRUG RECEPTORS Nuclear receptors Steroid hormones Thyroid hormone 4 Enzyme-linked receptors Insulin Growth factors 3 G-Protein coupled receptors Slow transmission e.g. norephinephrine 2 Ligand gated ion chanels Fast neurotransmittors e.g. acetylcholine 1 STRUCTURE ENDOGENOUS LIGAND SUPERFAMILY
DRUG RECEPTORS ,[object Object],[object Object],[object Object]
 
 
 
DRUG RECEPTORS ,[object Object],[object Object]
[object Object],[object Object],DRUG RECEPTORS
 
[object Object],[object Object],[object Object],G PROTEINS
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],SIGNIFICANCE OF G PROTEINS
 
DRUG RECEPTORS ,[object Object],[object Object],[object Object],[object Object],[object Object]
 
 
 
DRUG RECEPTORS ,[object Object],[object Object]
 
D 2 DPA 5HT 2A 5HT 1A ,[object Object],[object Object],[object Object],h
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],NON-RECEPTOR INTERACTIONS
[object Object],[object Object],[object Object],[object Object],NON-RECEPTOR INTERACTIONS
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],NON-RECEPTOR INTERACTIONS
[object Object],[object Object],[object Object],[object Object],NON-RECEPTOR INTERACTIONS
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],NON-RECEPTOR INTERACTIONS
[object Object],[object Object],DRUG - RESPONSE RELATIONSHIPS
TIME - RESPONSE RELATIONSHIPS Latency Duration of Response Maximal (Peak) Effect Effect/ Response Time
TIME - RESPONSE RELATIONSHIPS Effect/ Response Time IV SC IM
[object Object],[object Object],[object Object],DOSE - RESPONSE RELATIONSHIPS
POTENCY Effect Dose A B Which drug is more potent? A! Why? Therapeutic Effect
[object Object],[object Object],[object Object],[object Object],DOSE - RESPONSE RELATIONSHIPS
DOSE - RESPONSE RELATIONSHIPS Which drug has the lower threshold dose? Effect Dose A B Which has the greater maximum effect? A B Therapeutic Effect
[object Object],[object Object],[object Object],[object Object],DOSE - RESPONSE RELATIONSHIPS
[object Object],[object Object],[object Object],[object Object],THERAPEUTIC INDEX
THERAPEUTIC INDEX Why don’t we use a drug with a TI <1? ED50 < LD50  = Very Bad!
PHASES AFFECTING DRUG ACTIVITY Absorption  Distribution Metabolism  Excretion I – Pharmaceutical Phase II – Pharmacokinetic Phase III – Pharmacodynamic Phase Administration Drug available for absorption Drug available for action EFFECT Disintegration of dosage form Dissolution of drug Drug-receptor Interaction Dose of formulated drug
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],SOURCES
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Overview Of Pharmacodynamics 04.15.09

  • 1. OVERVIEW OF PHARMACODYNAMICS Pia C. Campo, RPh
  • 2.
  • 3.
  • 5.
  • 6. RECEPTOR INTERACTIONS Agonist Receptor Agonist-Receptor Interaction Lock and key mechanism
  • 7. RECEPTOR INTERACTIONS Receptor Perfect Fit! Induced Fit
  • 8. RECEPTOR INTERACTIONS Antagonist Receptor Antagonist-Receptor Complex DENIED! Competitive Inhibition
  • 9. RECEPTOR INTERACTIONS Agonist Receptor Antagonist ‘ Inhibited’-Receptor DENIED! Non-competitive Inhibition
  • 10.
  • 11.
  • 12.
  • 13.
  • 14.
  • 15.
  • 16.
  • 17.
  • 18.
  • 19. DRUG RECEPTORS Nuclear receptors Steroid hormones Thyroid hormone 4 Enzyme-linked receptors Insulin Growth factors 3 G-Protein coupled receptors Slow transmission e.g. norephinephrine 2 Ligand gated ion chanels Fast neurotransmittors e.g. acetylcholine 1 STRUCTURE ENDOGENOUS LIGAND SUPERFAMILY
  • 20.
  • 21.  
  • 22.  
  • 23.  
  • 24.
  • 25.
  • 26.  
  • 27.
  • 28.
  • 29.  
  • 30.
  • 31.  
  • 32.  
  • 33.  
  • 34.
  • 35.  
  • 36.
  • 37.
  • 38.
  • 39.
  • 40.
  • 41.
  • 42.
  • 43. TIME - RESPONSE RELATIONSHIPS Latency Duration of Response Maximal (Peak) Effect Effect/ Response Time
  • 44. TIME - RESPONSE RELATIONSHIPS Effect/ Response Time IV SC IM
  • 45.
  • 46. POTENCY Effect Dose A B Which drug is more potent? A! Why? Therapeutic Effect
  • 47.
  • 48. DOSE - RESPONSE RELATIONSHIPS Which drug has the lower threshold dose? Effect Dose A B Which has the greater maximum effect? A B Therapeutic Effect
  • 49.
  • 50.
  • 51. THERAPEUTIC INDEX Why don’t we use a drug with a TI <1? ED50 < LD50 = Very Bad!
  • 52. PHASES AFFECTING DRUG ACTIVITY Absorption Distribution Metabolism Excretion I – Pharmaceutical Phase II – Pharmacokinetic Phase III – Pharmacodynamic Phase Administration Drug available for absorption Drug available for action EFFECT Disintegration of dosage form Dissolution of drug Drug-receptor Interaction Dose of formulated drug
  • 53.