PCL201H1 Lecture Notes - Lecture 5: Intrinsic Activity, Terbutaline, Asthma

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14 Sep 2016
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PCL201
Winter 2014
Lecture 5 Dose Response
1. Examine the physiological response of drug receptor interactions (drug induced response)
2. Understand the Dose-Response curve
Information can be determined by this measurement (potency, efficacy)
3. Types of interaction, effectiveness of interaction
Agonist
Antagonist
Allosteric Modulators
4. Application of Dose-Response curve
Lethal doses
Evaluating Safety
Therapeutic Index
1. Examine the physiological response of drug receptor interactions (drug induced response)
Drug response = α[DR]
o α = intrinsic activity (a measure of how effective the drug is)
o D = concentration of drug
o R = concentration of receptors
Affinity measures the strength of the DR interaction
2. Understand the Dose-Response curve
The curve associated with a specific drug interaction is logarithmic and reaches saturation
The curve associated with a non-specific drug interaction is linear and does not reach
saturation
Response is defined by the researcher (i.e. what he wants to measure)
Information can be determined by this measurement (potency, efficacy)
Emax = (efficacy) maximal response achieved by an agonist
EC50 = (potency or affinity) drug concentration at 50% of Emax
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