Pharmacy 303: Pharmacokinetics Essentials

Drug Development Process

• Medicinal chemists develop potential new drugs for testing.
• A pharmacologist evaluates the drugs' efficacy and effects.

HDL Cholesterol Drugs

• New drugs were designed to increase HDL cholesterol by inhibiting cholesterol production enzymes.

Enzyme Inhibition Testing

• In vitro experiments measure the potency and effect of drugs through the following indices:
  • IC50: Indicates concentration required for 50% inhibition.
    • Drug 1: 0.01 nM
    • Drug 2: 0.05 nM
    • Drug 3: 1 nM
• Emax: Maximum effect achievable by drugs, all achieving 100%.

Drug Potency

• Potency expectation in humans based on IC50 values:
  • Drug 1 is anticipated to be most potent due to the lowest IC50 value.

Efficacy vs. Potency

• Efficacy: The drug's capability to produce a desired effect.
• Potency: The amount needed to elicit an effect, defined by IC50 values.

In Vivo vs. In Vitro Discrepancies

• Drug effects in vivo may differ from in vitro studies; this variance is fundamental to pharmacological evaluation.

Pharmacology Fundamentals

• Pharmacology: The science of drugs (Pharmac- = drugs; -ology = study).
• Divided into:
  • Pharmacodynamics: Effects of drugs on the body.
  • Pharmacokinetics: Movement and disposition of drugs within the body.

Interaction Dynamics

• Drug administration leads to:
  • Drug entering the bloodstream.
  • Drug reaching the site of action.
  • Drug binding to receptors and triggering physiological changes.

Concentration and Effect Relationship

• Relationships between drug concentration and physiological responses can be graphically represented (e.g., serum levels vs. physiological response over time).

Example Drugs

• Amiodarone: Demonstrates pharmacodynamic responses when binding to receptors.
• Mexiletine: Used to illustrate serum concentration effects on physiological changes over time.

This quiz covers the fundamental concepts of pharmacokinetics as discussed in Pharmacy 303. It explores the processes involved in drug testing, including enzyme inhibition and in vitro experiments. Dive into the pharmacological aspects of HDL cholesterol-raising drugs and their mechanisms.