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Pharmacology for Anesthesia I. Introduction. What is a Drug?. Pharmacokinetics (PK). What the body does to the drug Absorption Distribution Metabolism Excretion. Absorption. The process of diffusion or transport of a drug from the site of administration to the plasma.

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Pharmacokinetics pk
Pharmacokinetics (PK)

What the body does to the drug

  • Absorption

  • Distribution

  • Metabolism

  • Excretion


Absorption

The process of diffusion or transport of a drug from the site of administration to the plasma

Skipped by administering drugs parenterally

Inhaled agents require special considerations


Fick s law
Fick’s Law

concentration gradient x surface area x diffusion coefficient

membrane thickness

Rate of Diffusion =

Permeability

Size

Diffusion coefficient =


Ionization State

Henderson – Hasselbalch Equation

concentration (protonated)

concentration (unprotonated)

log

= pKa - pH



Distribution
Distribution

The process of diffusion of a drug throughout the body

Generally governed by the same characteristics as absorption

Vd = volume of distribution

Protein Binding


Metabolism
Metabolism

  • The enzymatic modification of the drug molecule by the body

    • Often occurs in liver

    • May occur elsewhere





Pharmacogenetics of drug metabolism
Pharmacogenetics of Drug Metabolism



Elimination
Elimination

  • The removal of the drug from the body

    • Renal

    • Hepatic

    • Respiratory

    • Cutaneous


Clearance
Clearance

  • Used to describe our ability to eliminate the active ingredient

    • Combination of metabolism and excretion

      Example of Zero order kinetics


Distribution and Clearance

  • First Order Kinetics

    • Single compartment model

    • Double compartment model

    • Three compartment model

    • Etc.







Pharmacodynamics
Pharmacodynamics

  • What the drug does to the body

    • Typically receptor mediated




Agonists receptor?

Antagonists

Competitive

Noncompetitive

Allosteric Activators

Potentiators


Partial agonists receptor?

Inverse agonists


Antagonists
Antagonists receptor?





Different drugs similar effects
Different Drugs Similar Effects receptor?

Potency vs. Efficacy



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