PROCESSES OF DRUGS IN THE ORGANISM

Pharmacokinetics is the branch of pharmacology that studies what happens to the drug.
when introduced into the body.

The amount of drug that reaches the site of action, carrying out the therapeutic action,
depends on various factors such as:

Administered dose;
Degree and the speed at which the drug is absorbed and then distributed to the tissues;
Degree of binding to proteins in the blood and tissues;
Localization of the active ingredient in a particular organ;
The degree and the speed at which the drug is metabolized and excreted.

In fact, he encounters a series of phenomena:

Absorption, Distribution, Metabolism, and Progressive Elimination, known as these phenomena

by the acronym ADME, remembering that an active substance is seen as a foreign agent
to the body, which seeks to turn it into something that makes it inactive and more easily
removable.

A medication that is assumed to be a "pharmaceutical form", for example a tablet, that consists of
of one or more active ingredients (component with pharmacological action) and excipients that
they serve to transport the active ingredient without having a healing activity, nor effects
toxics.

The first step that a tablet must undergo after being ingested is its
disintegration into granules, initially larger, then increasingly smaller, with the
release and dissolution of the active ingredient. A medication cannot be absorbed by the
walls of the gastrointestinal tract in solid form, must first melt, and this process
must be carried out quickly in biological fluids; this first phase is called 'phase
pharmaceutical.
Once the pharmaceutical phase has passed, the active ingredient is dissolved in the lumen of the
stomach or intestine must be absorbed by the walls of the stomach or intestine;
this process of 'absorption' depends on both the structure of the cell membranes by the
What has to happen regarding the physical-chemical properties of the drug itself.

Since the membrane factor cannot be varied to optimize the absorption of a

drug therefore we must play with its chemical and physical properties that are
represented by: molecular size, solubility in water and in lipids, and the degree of
ionization.

Once the medication has been absorbed and is in the bloodstream, they bind.
to the specific proteins in the blood and from here it will be distributed to the different organs.

The distribution of the active substance is strongly influenced by the characteristics

chemical and physical properties of the molecule, by local blood flow and by the affinity that the various
organs, fluids, and tissues that are against it.

Drugs that are highly soluble in fats and electrically neutral are those that can be distributed.
easily in all districts, while poorly soluble drugs and equipped with strong
more or less electrostatic charge penetrate into the cells of the tissue through processes
complex and difficult..

The organs with the fastest distribution are the heart, the liver, and the kidneys.
because they are highly spread; on the contrary, it has a slower distribution in the
muscles and in the adipose system.

Many drugs tend to concentrate in certain compartments, making it

these are a kind of deposits from which the active ingredient is gradually released again
in circulation. This phenomenon should always be considered in the body due to the presence
prolonged use of a drug can cause interactions with other medications that are
they manage.

After distribution in the body, the active ingredient reaches the site of action where
it can perform its pharmacological activity by binding to specific tissue receptors
Diana.

The drugs introduced into the body undergo a series of transformation processes,
by changing their molecular characteristics, it can cause them to become inactive, to enhance their
action or produce toxic metabolites.

These metabolic processes are especially important since many principles

active substances, to be excreted by the body in a relatively short time, must be considered
less diffusible through cell membranes and therefore have to be
transformed into molecules with greater electric charge, lower solubility in lipids and little
united with proteins and plasma tissues.

In general, the enzymes responsible for the biotransformation of drugs are

distributed throughout all tissues; the organs that perform this function the most are the kidneys,
the lungs, the muscles, but especially the liver, where the work is carried out to
the metabolism of the liver enzyme systems, among which the most important
they are the cytochromes P-450.

Once the active ingredient has undergone metabolic reactions and has been made
more soluble in water, the metabolite is ready to take the final step of the phase of
pharmacokinetics, which consists of its elimination by the body; it can be from the
excrements, through the kidneys, from the liver (in the bile, then in the feces), the
lungs, saliva, and sweat.

After excretion, the plasma concentrations of active ingredient decrease.

The elimination rate of a drug is quantified by a parameter called half-life, which

what indicates the time needed for the blood to eliminate half of the amount of drug
initially present. Obviously, a drug must have a half-life of sufficient time
for it to carry out its pharmacological activity.

LADME, an acronym for Liberation, Absorption, Distribution, Metabolism, and Excretion is the
model that explains the process a drug undergoes from the moment it is ingested.
continuation, we embark on a journey unknown to many but that happens every time
that we take a medication.

Liberation

When taking a medication orally, the first thing that must happen is that it is released from the
pharmaceutical form of which it is a part (capsule, tablet, solution, or granulate) and it
dissolve in the medium. Therefore, depending on the degree of integration of the active ingredient in the
oral formulation will take more or less time to be released. In this way, the drugs that
we take them in the form of an oral solution, they are already dissolved in water, which will give them an advantage over the

capsules and tablets. The excipients, which are the inactive compounds that are incorporated
to the oral formulation to give body and form (lactose, sucrose, sorbitol, starch...), also
can influence the release of the drug.

Absorption

Once dissolved, they move through the body as if they were food and get absorbed into the
length of the digestive system. Although absorption can occur in any area, the
The small intestine is the part of the gastrointestinal tract specialized in this, due to its
physiological characteristics that provide a greater active absorption surface. Therefore, this
the step will depend on both the state of the patient's intestine and the properties
physicochemical properties of the drug (degree of ionization, solubility, pH, etc.).

But not everything is that simple, the drug also encounters obstacles along the way, as not everyone
The transporters in the intestine facilitate the absorption of substances. There is a transport
inverse, secretion or 'efflux' whose function is to protect the bloodstream from intrusion of
toxins and foreign substances. Precisely, drugs are unknown substances to the
organism, and these 'efflux' transporters will be responsible for expelling the drug that may have
managed to access the blood, again towards the intestinal lumen. This leads to failures
therapeutic, as the drug does not reach the site of action. These transporters are the
responsible for the failure of some treatments, such as cancer chemotherapy.
Distribution

Absorption is only the beginning of the drug's journey in the body. After its entry into
bloodstream, it must travel to the site of action, that is to the place where
find the pathology that needs to be cured. Part of the drug makes this journey alone, and another
part accompanied by transport proteins. Those that bind to these proteins, possessing
a large size, they will find it difficult to cross some biological membranes, such as the
blood-brain barrier (brain), which only allows the passage of small molecules
size. It is important to take into account this phenomenon to calculate the ideal dose for the
patient.

Metabolism

From the moment we ingest the medication, our organs responsible for protecting us
in the presence of foreign substances, they come into action. We need to inactivate the toxins when they are no longer
needed. This process occurs mainly in the liver and consists of converting or
chemically transform drugs into more easily eliminable compounds.

Excretion

And finally, the last phase of the LADME cycle is excretion. Drugs are expelled from
our body through the process of excretion. These can be eliminated after the
metabolization or unaltered. The routes of exit are diverse, with the most important being the
urinary and biliary-enteric tracts. It can also be excreted through sweat, saliva, milk, and epithelia.
descaled. These are the last places the drug visits on its journey through our
organism.

Therefore, the journey of the drug through our body consists of a series of processes.
chained, some favor their absorption and others hinder it, but it is precisely this
balance is what makes it possible for drugs to heal us without destroying us.
ADVERSE REACTIONS OF MEDICATIONS

An adverse reaction to a medication is defined as a toxic or unintended reaction.

of a medication used at a standard appropriate dose for prophylactic, diagnostic, or
therapeutic. Adverse drug reactions (ADR) are quite common,
Especially in hospitalized patients, they occur frequently. Affecting about 1%
and 3% of hospitalized patients.

Adverse drug reactions (side effects) are the unwanted effects of a

medication. There are several different types:

Related to the dosage

Allergic
Idiosyncratic

Adverse drug reactions related to the dose present as an excess

of the therapeutic effects of the drug. For example, a person who is being treated with
a drug to control hypertension, feels dizzy or lightheaded if the drug decreases
high blood pressure. A diabetic person shows weakness, sweating, nausea and
palpitations if insulin or an oral antidiabetic drug reduces the level more than expected
blood sugar. This type of adverse drug reaction is usually predictable, but in
On occasions it is inevitable. This circumstance may occur if the dosage of a drug is excessive.
(reaction to overdose), if the person is exceptionally sensitive to it or if another drug
slows the metabolism of the first, thereby increasing its concentration in the blood
(see Drug interactions). Dose-related reactions are usually not
serious, but they are relatively common.

Drug allergic reactions are not related to the dose but require having
previously exposed to the drug in question. Allergic reactions occur when
the immune system of the body develops an inappropriate reaction to a drug (a
situation that is sometimes referred to as sensitization). When a person has already
sensitized, subsequent exposures to the drug produce a specific type of reaction
allergic, among the different types that exist. Sometimes the doctor conducts tests
cutaneous tests to help predict allergic reactions to drugs.

Idiosyncratic adverse reactions are the result of certain mechanisms that have not yet
They know each other well. This type of adverse drug reaction is extremely unpredictable.
Examples of such adverse reactions include the appearance of rashes, jaundice, anemia,
decrease in the number of white blood cells (leukocytes), kidney damage, and nerve damage that
it can lead to visual or auditory disturbances. These reactions tend to be more severe,
but they generally occur in a small number of people. The affected individuals
they can show genetic differences in the way their body metabolizes or responds to
drugs.

Some adverse reactions are not related to the therapeutic effect of the drug, but
They tend to be predictable because the mechanisms involved are very well known. For example, the
gastric irritation and hemorrhage often occur in people who take it regularly.
aspirin (acetylsalicylic acid) or other non-steroidal anti-inflammatory drugs (NSAIDs). The reason is that
These drugs reduce the production of prostaglandins, which help protect the tract.
digestive against gastric acid. If we are concerned about a symptom that you think may
to be an adverse effect, we must follow 2 steps:

Review the medication leaflet. In it, we can find a list of reactions.

known adversities and advises us what to do.

Talk to our doctor or pharmacist, and inform them of our doubts or fears and of the
possible adverse reaction we have experienced.

Lastly, it is important to remember that no medication is completely free of

produce adverse reactions, but the benefit obtained from the medication outweighs its
potential risks. Many adverse reactions are uncommon. In general, most of
people who use a medication do not experience any adverse reaction. Even
The adverse reactions described as common occur in only a small percentage.
of the people who use the medication.

Prevention
To prevent adverse drug reactions, it is necessary to be familiar with the agent.
and the reactions that may occur. A computerized analysis must be used to
control potential drug interactions; the analysis must be repeated whenever it
modify or add medications. In older adults, they must be selected carefully.
the drugs and the initial dosage (see Issues related to drugs in the
elderly: Causes of drug-related problems). They should always be considered
adverse drug reactions before starting symptomatic treatment in the
patients presenting nonspecific symptoms.