Mark Fholine C.

Serrano

BSN 2-3

PHARMACOKINETICS
Pharmacokinetics, sometimes abbreviated as PK, (from Ancient
Greek pharmakon "drug" and kinetikos "to do with motion"; see
chemical kinetics) is a branch of pharmacology dedicated to the
determination of the fate of substances administered externally
to a living organism. In practice this discipline is applied mainly to
drug substances, though in principle it concerns itself with all
manner of compounds ingested or otherwise delivered externally
to an organism, such as nutrients, metabolites, hormones, toxins,
etc.

Pharmacokinetics is often studied in conjunction with

pharmacodynamics. Pharmacodynamics explores what a drug
does to the body, whereas pharmacokinetics explores what the
body does to the drug. Pharmacokinetics includes the study of the
mechanisms of absorption and distribution of an administered
drug, the rate at which a drug action begins and the duration of
the effect, the chemical changes of the substance in the body
(e.g. by enzymes) and the effects and routes of excretion of the
metabolites of the drug.

PHARMACODYNAMICS
Pharmacodynamics is the study of the physiological effects of
drugs on the body or on microorganisms or parasites within or on
the body and the mechanisms of drug action and the relationship
between drug concentration and effect.[1] One dominant example
is drug-receptor interactions as modeled by

where L=ligand (drug), R=receptor (attachment site), reaction

dynamics that can be studied mathematically through tools such
as free energy maps. Pharmacodynamics is often summarized as
the study of what a drug does to the body, whereas
pharmacokinetics is the study of what the body does to a drug.
Pharmacodynamics is sometimes abbreviated as "PD", and when
referred to in conjunction with pharmacokinetics can be referred
to as "PK".

MEDIAN LETHAL DOSE

In toxicology, the median lethal dose, LD50 (abbreviation for

“Lethal Dose, 50%”), LC50 (Lethal Concentration, 50%) or LCt50
(Lethal Concentration & Time) of a toxic substance or radiation is
the dose required to kill half the members of a tested population
after a specified test duration. LD50 figures are frequently used as
a general indicator of a substance's acute toxicity. The test was
created by J.W. Trevan in 1927.[1] It is being phased out in some
jurisdictions in favor of tests such as the Fixed Dose Procedure;[2]
however the concept, and calculation of the median lethal dose
for comparison purposes, is still widely used.

As a measure of toxicity, LD50 is somewhat unreliable and results

may vary greatly between testing facilities due to factors such as
the genetic characteristics of the sample population, animal
species tested, environmental factors and mode of
administration.[3] Another weakness is that it measures acute
toxicity only (as opposed to chronic toxicity at lower doses), and
does not take into account toxic effects that do not result in death
but are nonetheless serious (e.g. brain damage). There can be
wide variability between species as well; what is relatively safe for
rats may very well be extremely toxic for humans, and vice versa.
In other words, a relatively high LD50 does not necessarily mean a
substance is harmless, but a very low one is always a cause for
concern.

The term semilethal dose is occasionally used with the same

meaning, particularly in translations from non-English-language
texts, but can also refer to a sublethal dose; because of this
ambiguity, it is usually avoided

THERAPEUTIC DOSE
The therapeutic index (also known as therapeutic ratio), is a
comparison of the amount of a therapeutic agent that causes the
therapeutic effect to the amount that causes death.
Quantitatively, it is the ratio given by the lethal dose divided by
the therapeutic dose. A therapeutic index is the lethal dose of a
drug for 50% of the population (LD50) divided by the minimum
effective dose for 50% of the population (ED50). A high therapeutic
index is preferable to a low one: this corresponds to a situation in
which one would have to take a much higher dose of a drug to
reach the lethal threshold than the dose taken to elicit the
therapeutic effect.

Generally, a drug or other therapeutic agent with a narrow

therapeutic range (i.e. with little difference between lethal and
therapeutic doses) may have its dosage adjusted according to
measurements of the actual blood levels achieved in the person
taking it. This may be achieved through therapeutic drug
monitoring (TDM) protocols. The therapeutic index for diazepam is
somewhat forgiving, about = 100. Other drugs, however are
much less so, such as Digoxin, which has an index of 2 or 3. [1]
Other examples of drugs with a narrow therapeutic range, that
may require drug monitoring both to achieve therapeutic levels
and minimize toxicity, include: dimercaprol, theophylline, warfarin
and lithium carbonate. Some antibiotics require monitoring to
balance efficacy with minimizing adverse effects, including:
gentamicin, vancomycin, amphotericin B, and polymyxin B.

The effective therapeutic index can be affected by targeting, in

which the therapeutic agent is concentrated in its area of effect.
For example, in radiation therapy for cancerous tumors, shaping
the radiation beam precisely to the profile of a tumor in the
"beam's eye view" can increase the delivered dose without
increasing toxic effects, though such shaping might not change
the therapeutic index. Similarly, chemotherapy or radiotherapy
with infused or injected agents can be made more efficacious by
attaching the agent to an oncophilic substance, as is done in
peptide receptor radionuclide therapy for neuroendocrine tumors
and in chemoembolization or radioactive microspheres therapy
for liver tumors and metastases. This concentrates the agent in
the targeted tissues and lowers its concentration in others,
increasing efficacy and lowering toxicity.

EFFICACY OF THE DRUG

Efficacy is the capacity to produce an effect. It is used to mean
different specific things in different fields.

POTENCY OF THE DRUG

In the field of pharmacology, potency is a measure of drug
activity expressed in terms of the amount required to produce an
effect of given intensity. A highly potent drug (e.g., morphine,
alprazolam, chlorpromazine) evokes a larger response at low
concentrations, while a drug of lower potency (ibuprofen,
acetylsalicylic acid) evokes a small response at low
concentrations. It is proportional to affinity and efficacy.