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Basic Concepts in
Pharmacokinetics

Dr. Md. Tarique Imam

Department of Clinical Pharmacy
Faculty of Pharmacy
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Definitions

Pharmacokinetics:

Pharmacokinetics is the study of the time course of drug

absorption, distribution, metabolism, and excretion in
relation to the intensity and time course of the
pharmacologic (therapeutic and toxicologic) effects of
drugs.

Pharmacokinetics provides a mathematical basis to

assess the time course of drugs and their effects in the
body.
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Definitions

• Clinical Pharmacokinetics
Application of pharmacokinetics principles in the safe &
effective management of individual patient

• Population Pharmacokinetics
The study of pharmacokinetic differences of drugs in
various population groups

• Toxicokinetics
The application of pharmacokinetic principles to design,
conduct & interpretation of drug safety evaluation studies
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Definitions

• Peak Plasma Concentration (Cmax)

The point of maximum concentration of drug in plasma. It
is expressed in μg/ml

• Time of Peak (Tmax)

The time for drug to reach peak concentration in plasma.
It is expressed in hours (hrs)

• Area Under the Curve (AUC)

It represents the total integrated area under the plasma
level-time profile and expresses the total amount of drug
that comes into the systemic circulation. . It is expressed
in μg x hr/ml
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Definitions
• Half Life (t1/2)
The time required for the concentration of drug in the
body to be reduced to exactly one-half of a given
concentration or amount
• Minimum Effective Concentration (MEC)
The minimum concentration of drug in plasma required to
produce the therapeutic effect
• Maximum Safe Concentration (MSC)
Also called Minimum Toxic Concentration. It is the
concentration of drug in plasma above which adverse or
unwanted effects are precipitated
• Onset of Action
The beginning of pharmacological response
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Definitions

• Onset Time
It is the time required for the drug to start producing
pharmacological response

• Duration of Action
The period for which the plasma concentration of drug
remains above the MEC level

• Intensity of Action
The maximum pharmacological response produced by
the peak plasma concentration of drug
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Definitions
• Therapeutic Range
The drug concentration above MEC and MSC. Also known as
Therapeutic window

• Therapeutic Index
The ratio of MSC to MEC

• Apparent Volume of Distribution (Vd)

The hypothetical volume of body fluid into which a drug is
dissolved or distributed. It is expressed in Litre

• Clearance (Cl)
The hypothetical volume of body fluids containing drug from
which the drug is removed completely in a specific period of
time. It is expressed in L/hr
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Concentration-Time Profile

Cmax (Absorption rate = Elimination

Toxic Rate)
level Maximum Safe Concentration (MSC)

Therapeutic Range or Window

Onset
of AUC Minimum Effective Concentration
Action
(MEC)

Duration of Subtherapeutic Level

Action

Onset Time Tmax

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Bioavailability

• Bioavailability (F)
Rate and extent of absorption of unchanged drug from its
dosage form.

It depends on 3 major factors:

1. Pharmaceutical factors
2. Patient related factors
3. Route of administration

• The order of bioavailability according to route of

administration is:
Parentral > Oral > Rectal > Topical
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Bioavailability

• Absolute Bioavailability
When the systemic availability of a drug administered
orally is determined in comparison to its intravenous
administration.

• Relative or Comparative Bioavailability

When the systemic availability of a drug administered
orally is determined in comparison to an oral standard of
the same drug.
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Bioequivalence

• Bioequivalence
The absence of a significant difference in the rate and
extent to which the active ingredient or active moiety in
pharmaceutical equivalents or pharmaceutical
alternatives becomes available at the site of drug action
when administered at the same dose under similar
conditions
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• AUC = (C1 + C2) (t2 – t1)
2
• Therapeutic Index = MSC
MEC
• t1/2 = 0.693
Ke
• Vd = Amount of drug in the body (X)
Plasma drug concentration (C)
• Clearance = Rate of elimination (dx/dt)
Plasma drug concentration (C)
• Fabsolute = AUCoral
AUCiv
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• Frelative = AUCtest
AUCstd

• Ke = Cl
Vd