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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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Pharmacology for Anesthesia I

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Pharmacology for anesthesia i

Pharmacology for Anesthesia I


What is a drug

What is a Drug?

Pharmacokinetics pk

Pharmacokinetics (PK)

What the body does to the drug

  • Absorption

  • Distribution

  • Metabolism

  • Excretion

Pharmacology for anesthesia i


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 =



Diffusion coefficient =

Pharmacology for anesthesia i

Ionization State

Henderson – Hasselbalch Equation

concentration (protonated)

concentration (unprotonated)


= pKa - pH

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The process of diffusion of a drug throughout the body

Generally governed by the same characteristics as absorption

Vd = volume of distribution

Protein Binding



  • The enzymatic modification of the drug molecule by the body

    • Often occurs in liver

    • May occur elsewhere

Hepatic metabolism

Hepatic Metabolism

Example of phase ii prior to phase i

Example of Phase II prior to Phase I

Cyp enzymes

CYP Enzymes

Pharmacogenetics of drug metabolism

Pharmacogenetics of Drug Metabolism

Examples of drug drug interactions

Examples of Drug-Drug Interactions



  • The removal of the drug from the body

    • Renal

    • Hepatic

    • Respiratory

    • Cutaneous



  • Used to describe our ability to eliminate the active ingredient

    • Combination of metabolism and excretion

      Example of Zero order kinetics

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Distribution and Clearance

  • First Order Kinetics

    • Single compartment model

    • Double compartment model

    • Three compartment model

    • Etc.

Absorption and clearance

Absorption and Clearance

Effect not always governed by plasma concentration

Effect Not Always Governed by Plasma Concentration

Dosing regimens

Dosing Regimens

Pharmacology for anesthesia i

Can speed accumulation time by administering a loading dose

Routes of administration

Routes of Administration



  • What the drug does to the body

    • Typically receptor mediated

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  • What factors affect the ability of a drug to interact with a receptor?

  • Drug size

    • Large enough to be specific

    • Not so large as to be unable to interact with the receptor

  • Drug Shape

Pharmacology for anesthesia i

  • Some drugs do not appear to fit into these categories

    • Osmotic agents

    • Transport regulators

Pharmacology for anesthesia i





Allosteric Activators


Pharmacology for anesthesia i

Partial agonists

Inverse agonists



Noncompetitive antagonist and spare receptors

Noncompetitive Antagonist and Spare Receptors

Full and partial agonists

Full and Partial Agonists

Cellular receptors

Cellular Receptors

Different drugs similar effects

Different Drugs Similar Effects

Potency vs. Efficacy

Population variation and therapeutic window

Population Variation and Therapeutic Window

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