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Pharmacokinetics Principles

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Pharmacokinetics

Principles and Application


• Pharmacokinetic principles relate specifically to the variations in drug concentration as a
result of pharmacokinetic processes i.e. absorption, distribution and elimination with
time.
• Accordingly, pharmacokinetics may also be defined as the mathematical description of
concentration changes of drug as a function of time.
• Pharmacokinetic principles are useful in determination of following factors:
• The extent and rate to which a pharmacokinetic parameter (ADME) occurs in body.
• The dose and dosing schedule of a drug and its modification according to individual
needs.
• The drug concentrations which produce therapeutic and toxic effects.
• The drug concentrations in various body fluids and tissues, and its accumulation .
• The half-life and duration of action of a drug.
• The effect of disease state on various Pharmacokinetic parameters.
• The withdrawal time for meats, eggs and dairy products.
• The nature and extent of drug interactions.
PLASMA DRUG CONCENTRATION-TIME
PROFILE
• The speed of onset, intensity and duration of a pharmacological effect depend
on the concentration of drug at its site(s) of action.

• As it is difficult to collect tissue samples, the time course of drug


concentration at its site of action is approximated by measuring drug
concentrations in plasma, which can be measured with accuracy.

• The plasma drug concentration-time curve is obtained by measuring the


concentrations of drug in plasma taken at different time intervals after
administration of the drug and then plotting the concentrations of drug in
plasma (Y-axis) versus the corresponding time at which the plasma samples
were collected (X-axis).
• If a drug is administered by oral or extravascular (lM, SC, IP, etc.) route, it
slowly enters the systemic circulation and plasma drug concentration
gradually rises to a maximum (peak) level.
• As the drug is being absorbed into blood, it is distributed to body tissues
and may also simultaneously being eliminated.
• The ascending portion of the curve to left of peak represents the absorption
phase.
• Generally the distribution phase of a non-intravenous dose is masked by
the absorption phase.
• The descending section of the curve to right of peak generally represents
the elimination phase.
• The rate or velocity with which absorption and elimination processes occur
is given by the respective slopes of curve and are expressed by absorption
rate constant (Ka) and elimination rate constant (β), respectively.
• Minimum effective concentration (MEC)
• Maximum safe concentration (MSC) or Minimum toxic concentration
(MTC)
• Maximum plasma concentration/Peak plasma concentration (Cmax or
Cpmax)
• Area under curve (AUC)
• Peak effect
• Time of maximum concentration/Time of peak concentration (tmax)
• Onset of action
• Onset time
• Duration of action
• Before going to start absorption, distribution, metabolism and elimi
nation, watch the video first by clicking on following link

• https://www.youtube.com/watch?v=NKV5iaUVBUI
• https://www.youtube.com/watch?v=8-Qtd6RhfVA
• https://www.youtube.com/watch?v=pWW-aq7iSa0 (Absorption)
• https://www.youtube.com/watch?v=6erefsWCVxg (Distribution)
• https://www.youtube.com/watch?v=ztsBn8gsfHw (Metabolism)
• https://www.youtube.com/watch?v=VZRVt9r4oSM (Elimination)

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