M.

C GILBERTO QUIONEZ PALACIO

In medicine pharmacology generally makes emphasis in pharmacologic

aspects like ways of administering drugs ,dose, time intervals: and in a few
cases side effects and adverse reactions
Todays pharmacology must be oriented to the principles of
pharmacokinetics and the use of parameters created by this science for
the administration of drugs, parameters like: absorption velocity, excretion
velocity, elimination, t1/2 , volume of distribution, etc.
All these concepts, factors and parameters should be taken in
consideration to be able to obtain a clinical therapeutic response.

CLINICAL
PHARMACOKINETICS
Application of principles of pharmacokinetics for the
therapeutic management of a patient
Science that studies the time course of the pharmacologic
response, creating models for interpreting results

PHARMACOKINETIC
PRINCIPLE
Union of concepts of the mechanism of absorption,
distribution, metabolism and elimination of a drug

PHARMACOKINETC PHASE:
Is where the dose, presentation, frequency and way of
administering are related with the concentration level and
time it takes to reach the blood stream.
.
PHARMACODYMAMIC PHASE:
Where the concentration and the site of action of the
drug are related to the magnitude of the final effect .

bsorption

istribution

etabolism

xcretion

Absorption : Transport process of the

administration to the systemic circulation

drug from the site of

Distribution : Once in blood the drug distributes in tissue, in one or

more it will exercise his action. The distribution determines the amount
of the drug that will reach the site of action
Elimination : Is the sum of all the process that conduce to the removal
of the drug from the organism. These procedure is done by
biotransformation and excretion.
The great majority of the active principles of drugs and their
metabolites are eliminated by the kidney, feces, there is a degree of
elimination by respiration, milk, sweat, saliva and tears.

Biotransformation : Process of chemical transformation of the active

principles
of
drugs
in
the
body.
The organism tries to eliminate all strange substances using diverse
biochemical mechanisms. Drugs are transformed into more polar
metabolites (Active or inactive), this by hydrolysis, redox, synthesis; all of
these by enzymatic process
Most of these reactions occur in the Liver , but they may also happen in
plasma, kidney and other tissues
There
are
two
types
of
biotransformation
:
Phase 1. Degradation reactions : oxidation, reduction and hydrolysis
Phase 2. Synthesis reactions : conjugation with Glucoronic Acid, Glicyne
Excretion : Process done by the organism that eliminates an active
principle of a drug or its metabolite without modification. The main organ
of
excretion
is
the
kidney

Before Administration

After Administration

Two Compartment Model

Before
Administration

Immediately after
Administration

After distribution
equilibrium

Pharmacokinetics
studies
the
variation
of
blood
concentrations of drugs in a time period and also the velocity
of changes in all the processes involved.
It relates an independent variable (Time) with a dependent
variable (Concentration) in blood, urine or tissue.
With that we define the kinetics of the parameters that we use

Maximum Plasmatic concentration (Cmax). Is the quantity of the drug

that we find in plasma in a determine time (Tmax) after the
administration. That is why absorption and way of administration are
key factors
Area under the curve (ABC). It is the most important parameter and is
obtained from the curve of concentration of the drug vs. The time. It is
the best estimation of the absorbed drug and is availability in the
organism to carry out its pharmacologic action.
Maximum Time (Tmax). The time required to obtain a maximum
concentration
Half life (t ). The time that takes the plasmatic concentration of a
drug to reach exactly half of it.

Pharmacokinetic equations
ko = Kd Vd Cp Max ( 1 - e KdT )
__________
( 1 e Kdt )
Kd = ln Cp2 ln Cp1
____________
t2 t1
T1/2 = .693
_____
Kd

Graphic levels of a
pharmacologic active
principle

Thank you