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Basic Clinical Pharmacology Bertram, Katzung 15th Edition Summary - Chapter 3 and Chapter 4

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  • Clinical Pharmacology
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  • Basic and Clinical Pharmacology 15e

Basic Clinical Pharmacology Bertram, Katzung 15th Edition Summary - Chapter 3 and Chapter 4 Chapter 3: Pharmacokinetics Chapter 4: Drug Metabolism

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  • Chapter 3 to chapter 4
  • October 22, 2021
  • 10
  • 2021/2022
  • Summary

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  • pharmacokinetics
  • drug metabolism
  • biotransformation
  • bertram
  • katzung
  • basic and clinical pharmacology

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  • University of Oxford
  • Clinical Pharmacology
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CHAPTER 3:
PHARMACOKINETICS
22nd October 2021
INTRODUCTION:
 Pharmacokinetics denotes the effects of biologic systems on drugs
 The major processes involved in pharmacokinetics are
o

o absorption o metabolism
o distribution o elimination

 Pharmacokinetic data are essential to calculate the “loading” and “maintenance” doses

HIGH-YIELD TERMS TO LEARN:
 Volume of Distribution (V d ):
amount of drug in body
V d=
drug concentration in plasma or blood
 Clearance (CL):
rate of elimination of drug
CL=
plasma drug concentration
 Half-Life: period of time in which the drug concentration in body / blood drops by 50%
 Bioavailability: the fraction / percentage of administered drug that reaches the
systemic circulation (i.e., bioavailability in case of IV administration = 100%)
 Area Under the Curve (AUC): the area under the drug concentration – time curve
 Peak and Trough Concentration: maximum and minimum drug concentration
achieved during repeated dosing cycle
 Minimum Effective Concentration: plasma drug concentration bellow which a
patient’s response is too small for clinical benefit
 First-pass effect, presystemic elimination: elimination of drug that occurs after
administration but before it enters the systemic circulation (e.g., during passage
through gut wall, portal circulation or liver when drug is taken orally)
 Steady State: the condition in which the average total amount of drug in the body does
not change over multiple dosing cycle (i.e., rate of elimination = rate of administration)
 Biodisposition: synonym for pharmacokinetics (absorption, distribution, metabolism,
elimination)

, EFFECTIVE DRUG CONCENTRATION:
 The concentration of the drug (DC) at the receptor site is called EDC
 The plasma concentration is a function of:
o Rate of drug input
o Rate of elimination
o Rate of distribution
 If the rate of input is known, the remaining processes are described by:
o Apparent Volume of Distribution (V d )
o Clearance (CL)

VOLUME OF DISTRIBUTION:
amount of drug in body
V d=
drug concentration in plasma or blood
 Denoted as apparent V d
 V d is sometimes expressed as V d /kg
 Liver disease can alter the V d for drugs that bind to plasma proteins (e.g., albumin)
 The V d may:
o greatly exceed the total body volume
 e.g., Quinacrine: 50,000 L/V d in a person whose body volume is 70 L
o greatly fall to a small portion of the body volume
 e.g., if a drug is completely retained in the plasma

CLEARANCE:
rate of elimination of drug
CL=
plasma drug concentration
 First-Order Kinetics: is a concentration-dependent process (i.e., the higher the
concentration, the faster the clearance)
 For a drug eliminated with first order kinetics, clearance is a constant.
 clearance is sometimes expressed as CL/Kg
 Clearance depends on
o the drug
o the blood flow
o the condition of the organs of elimination in the patient


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