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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
THANK YOU.

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Overview Of Pharmacodynamics 04.15.09

  • 1. OVERVIEW OF PHARMACODYNAMICS Pia C. Campo, RPh
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  • 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
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  • 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
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  • 43. TIME - RESPONSE RELATIONSHIPS Latency Duration of Response Maximal (Peak) Effect Effect/ Response Time
  • 44. TIME - RESPONSE RELATIONSHIPS Effect/ Response Time IV SC IM
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  • 46. POTENCY Effect Dose A B Which drug is more potent? A! Why? Therapeutic Effect
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  • 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
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  • 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
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