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Pharmacokinetics
Shan Nanji
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First Order and Zero Order

n First Order
n Most Medications
n Constant Fraction of Drug is Eliminated/unit Time

n Zero Order
n Constant Amount of drug is metabolized/ Unit Time

Shan Nanji - NanjiMD@gmail.com

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Competitive v. Noncompetitive
n Competitive - K-ompetitive
n Inhibitor is similar to the substrate
n Competing for active site
n Affinity decreased (potency decreases)
n KM Increases
n Vmax does not change (add more substrate)
n Reversible

n Noncompetitive
n Not similar to substrate and does not bind active site
n Binds to regulatory site
n Turns the enzyme off
n KM remains the same
n Vmax decreases (Efficacy decreases)
n Irreversible

Shan Nanji - NanjiMD@gmail.com

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Competitive v. Non-Competitive

Shan Nanji - NanjiMD@gmail.com

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Pharmacokinetics

nCompetitive Antagonist
n Shifts
Curve to the Right
n Decreases Potency
n No Change in Efficacy
n CAN Overcome by Increasing [Agonist Substrate]

Shan Nanji - NanjiMD@gmail.com

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Pharmacokinetics

nNoncompetitive Antagonist
n Shifts Curve Downward

n Decreases Efficacy

n CANNOT be Overcome by Increasing [Agonist Substrate]

Shan Nanji - NanjiMD@gmail.com

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Pharmacokinetics

nPartial Agonist
n Acts at Same Site as Full Agonist

n Reduced Maximal Effect

n Decreases Efficacy

n Increases or Decreases Potency

Shan Nanji - NanjiMD@gmail.com

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Pharmacokinetics

n Therapeutic Index
n LD50/ED50 = Median Lethal Dose/ Median Effective Dose

n Higher TI values = Safer Drugs

n Therapeutic Window
n Measure of the Doses at which a Drug can Be Both Safe and
Effective

Shan Nanji - NanjiMD@gmail.com