Principles of drug action

Principles of drug action - Lecture 2 Principles of Drug...

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Lecture 2 Principles of Drug Action
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Objectives 1. Drug dose and dose-response 1. Pharmacokinetics : factors that contribute to the ADME of a drug. 1. ADME A dministration/ A bsorption D istribution M etabolism E xcretion
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A D A D M M E E A A
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In order for a drug to produce effect it must get to the site of action - Ability of drug to travel in the body and to reach the brain is determined by: - Concentration of drug at its site of action - Rate of accumulation at the site of action These factors are determined by drug dose and pharmacokinetics . = Bioavailability - concentration of a drug present in the blood that is free to bind to specific target sites - usually less than total drug in blood
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Dose: - quantity of drug administered to body * - usually expressed as drug / body weight (mg/kg) - administration of drug / unit of time (mg/kg 4 times a day for 3 days) Question Question : 10mg - higher dose in mouse or human? What about 10mg/kg for each? Caveat: equivalent units of drug / weight are not usually equivalent doses. WHY? Dosage:
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Pharmacokinetics
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Dose-Response Curve 100 75 50 25 Drug Effect Dose, mg 1 10 100 1000 10,000 Increasing doses associated with increasing responses
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Us e of A s p i r i n Head ach e Ar t er y Healt h Main Effect Pain Relief An t i-clot t in g Sid e Effect An t i-clot t in g Pain r elief (b leed in g)
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100 75 50 25 Drug Effect Dose, mg 1 10 100 1000 10,000 Curvilinear or Biphasic Dose-Response Curve
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Effects of Amphetamine Drug Effect High Low Low Dose High Dose locomotion locomotion stereotypy stereotypy
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Dose-Response Curve 100 75 50 25 Drug Effect Dose, mg 1 10 100 1000 10,000 Some doses produce no effect
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Dose-Response Curve 100 75 50 25 Drug Effect Dose, mg 1 10 100 1000 10,000 Threshold dose
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Dose-Response Curve 100 75 50 25 Drug Effect Dose, mg 1 10 100 1000 10,000 Maximal response
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Efficacy 100 75 50 25 Drug Effect Dose, mg 0.01 0.1 1 10 100 1000 10,000 Drug A Drug B
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100 75 50 25 Drug Effect Dose, mg 0.01 0.1 1 10 100 1000 10,000 Drug A Drug B Potency
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Analgesia Efficacy: Rank? Potency: Rank? .
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100 75 50 25 Dose, mg 1 10 100 1000 10,000 % people with drug effect or Percent maximal effect Effective Dose 50 (ED50) ED50 = 100mg
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100 75 50 25 Dose, mg 0.01 0.1 1 10 100 1000 10,000 Therapeutic or Desired effect Unwanted Effects or Side Effects % People with Drug Response ED50 LD50
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Principles of drug action - Lecture 2 Principles of Drug...

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