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Pharmacokinetics
Shan Nanji

First Order and Zero Order

n

First Order
n
n

Most Medications
Constant Fraction of Drug is Eliminated/unit Time

Zero Order
n

Constant Amount of drug is metabolized/ Unit Time

Shan Nanji - NanjiMD@gmail.com

Competitive v. Noncompetitive
n

Competitive - K-ompetitive
n
n
n
n
n
n

Inhibitor is similar to the substrate

Competing for active site
Affinity decreased (potency decreases)
KM Increases
Vmax does not change (add more substrate)
Reversible

Noncompetitive
n
n
n
n
n
n

Not similar to substrate and does not bind active site

Binds to regulatory site
Turns the enzyme off
KM remains the same
Vmax decreases (Efficacy decreases)
Irreversible

Shan Nanji - NanjiMD@gmail.com

Competitive v. Non-Competitive

Shan Nanji - NanjiMD@gmail.com

Pharmacokinetics
nCompetitive
n Shifts

Antagonist

Curve to the Right

n Decreases Potency
n No Change in Efficacy
n CAN Overcome by Increasing [Agonist Substrate]

Shan Nanji - NanjiMD@gmail.com

Pharmacokinetics
nNoncompetitive Antagonist
n Shifts Curve Downward
n Decreases Efficacy
n CANNOT be Overcome by Increasing [Agonist Substrate]

Shan Nanji - NanjiMD@gmail.com

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

Pharmacokinetics
n Therapeutic

Index

LD50/ED50 = Median Lethal Dose/ Median Effective Dose

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