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Measuring Drug Action

K A. R + D R:D Response. K D. 1.0. Fraction bound. 0.5. [D] = K D. 0.0. [D]. Measuring Drug Action. Dose – Response Curves. Response  fraction bound (fb) = . D in system ‘R:D’ Response. Measuring Drug Action.

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Measuring Drug Action

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  1. KA R + D R:D Response KD 1.0 Fraction bound 0.5 [D] = KD 0.0 [D] Measuring Drug Action • Dose – Response Curves Response  fraction bound (fb) = MEDC 603 Fall 2007

  2. D in system ‘R:D’ Response Measuring Drug Action • Dose – Response Curves 90% IC50 or EC50 or LD50 50% IC90 or EC90 or LD90 Inhibition Concentration Effective Concentration Lethal Dose Or Log [agonist]O Agonist: An agent that facilitates or enhances the normal action of a receptor. Antagonist: An agent that prevents the normal action of a receptor. MEDC 603 Fall 2007

  3. Drug 1 Drug 2 Measuring Drug Action • Dose – Response Curves MEDC 603 Fall 2007

  4. Measuring Drug Action • Efficacy and Potency …… Potency corresponds to the strength of a drug, while Efficacy corresponds to the effectiveness of a drug. …… e.g., if 1 mg of drug A relieves pain as effectively as 10 mg of drug B, drug A is twice as potent as drug B …… the diuretic furosemide eliminates much more salt and water through urine than does the diuretic chlorothiazide. Thus, furosemide has greater efficacy than chlorothiazide. MEDC 603 Fall 2007

  5. Measuring Drug Action • Efficacy / Potency / Toxicity 100 100 Desired Response (%) Toxicity (%) 50 50 0 0 Log [Drug] Blue lines …. Drug 1 Red lines …. Drug 2 Solid lines …. Desired response Dotted lines …. Toxicity response MEDC 603 Fall 2007

  6. Anticoagulant S S T T S S [A] =0 KI or IC50 Color Development = Activity of Enzyme Inhibition of Enz: [A] = max Time (s) Log [anticoagulant] Measuring Drug Action • How are these drug-response profiles generated? e.g., anticoagulants and inhibition of pro-coagulant enzymes MEDC 603 Fall 2007

  7. Cell Viability Assay Drug Mouse Tail Flick Assay Heat! Drug Heat! Measuring Drug Action • How are these drug-response profiles generated? • Cellular/Pharmacological assays MEDC 603 Fall 2007

  8. 96-well microtiter plate Measuring Drug Action • How are these drug-response profiles generated? • High Throughput Screening Assays • Simultaneous …. 96- or 384-well microtiter plates …. robotic analysis • Chromogenic substrates …. develop color • Yes or No answer ….. fixed concentration of drug • Quantitative …. may also give you KI values!! MEDC 603 Fall 2007

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