PHARMACOLOGY

Basic terminologies

Pharmacology: It is the study of how drugs exert their effects on living systems.

Drug: It is a chemical substance capable of interacting with molecules and producing a

response in a biological being.

Drug: Refers to the drug used in a biological being for therapeutic purposes.

Medication: Refers to any drug used on a human being.

Pharmacy: It is the science that deals with the preparation and dispensing of medications.

GENERAL PHARMACOLOGY: Deals with the general principles of drug action

pharmacokinetics_pharmacodynamics.

SPECIAL PHARMACOLOGY: Deals directly with drugs.

PHARMACOKINETICS: It can be summarized as everything that the body does with the drug,
from the moment it comes into contact with our body until it reaches its biophase (its site of
pharmacological action in our body).

PHARMACODYNAMICS: It can be summarized as all the effects that the drug triggers in our
body, whether desired or not.

CLINICAL PHARMACOLOGY: Studies the actions of drugs in humans at the molecular,

subcellular, organ and entire body levels. The goal of this discipline is to treat patients and
prevent diseases.

CONCEPT OF PHARMACOKINETICS: Pharmacokinetics is the set of processes that determine

how much of the administered drug will reach its site of action, which is called BIOPHASE.
These processes are absorption, distribution, metabolization, and excretion.
For a drug to produce its effects, it must reach a certain concentration range in that biophase.
Below that range, no effects will be observed because they are subtherapeutic. Higher
concentrations can produce excessive effects or unwanted effects, the concentration obtained
in the BIOPHASE, although it depends on the dose of the product administered, is also a
consequence of the pharmacokinetic processes...

ABSORPTION : It is the entry of the drug into the body, it includes the release of its
pharmacoceutical form, the dissolution and the absorption itself, the latter can be, for
example, from the lumen of the digestive tract into the blood in the case of oral administration
or from the interstitial fluid of a muscle also into the blood (directly or through lymphatic
drainage) in the case of intramuscular administration.

A drug molecule is said to have been absorbed when it passes from a compartment in
communication with the outside (for example, the digestive tract or a hypodermic needle) to
the persistentemic circulation, that is, to the circulation located before the pulmonary veins, it
is said to have been absorbed. reaches the systemic circulation. By this definition, a drug
administered intravenously is not absorbed.

DISTRIBUTION: It is the path of the drug, first from its place of absorption to the systemic
circulation and from there to the tissues including its site of action. To do this, it must cross
several biological membranes.

The passage of the drug to the tissues depends largely on the binding of the drug to plasma
proteins, since only the unbound fraction will be able to freely dilute the tissues.

METABOLIZATION AND EXCRETION: Together they determine the elimination of the drug.

Metabolization occurs mainly in the liver, usually resulting in an inactive metabolite,

sometimes the metabolite is active, excretion of the drug without alteration through urine,
bile, etc. may also occur.

LOCAL ADMINISTRATION: It is the administration of the drug directly at the target site of the
therapeutic effect. As common examples in practice we can mention the administration of
SALBUTAMOL OR CORTICOIDS by inhalation. What is sought is to achieve high concentrations
at the site of action (in our example, the brochial tree and lower concentrations at a systemic
level to reduce the possibilities of unwanted effects occurring in the rest of the organism, and
in this way LOCATE the effect of the drug.

When a drug is administered locally, the area under the local curve is intended to be greater
than the area under the systemic curve, that is, the total amount of the drug that passes
through the site of action is greater than that which reaches the systemic circulation. . If this
cannot be achieved, a second objective is sought, which is that the local peak is greater than
the systemic one assuming that the drug is greater with a higher peak and, or that the adverse
effects are lower with lower systemic peaks.

DISTRIBUTION AND BINDING OF DRUGS TO PROTEINS: Drugs reach the anatomical

compartments carried in the water of the plasma. In turn, a drug can be dissolved in this water
(free drug) or bound to plasma proteins (bound drug). Less frequently, the drug may be bound
to blood cells.

As we already mentioned, it is the free fraction that diffuses to the tissues and that is
considered, since only the free fraction will be the one that can fulfill its effects in the
BIOPHASE.

The most common thing is that this drug-protein binding is reversible, that is, competition
between drugs that bind to the same proteins is possible. Thus, if a patient is receiving an oral
hypoglycemic agent, which has high protein binding, and decides to self-medicate with aspirin,
which also has high binding, competition will occur between the drugs for the binding sites,
increasing the free (ACTIVE) fractions of both medications and the patient will be more likely to
suffer the adverse effects of these drugs. It is not uncommon for diabetics to suffer
hypoglycemia due to this mechanism. Protein binding is considered high with respect to the
possibility of clinically important hospitalizations when it is greater than 80%.

Acidic and neutral drugs bind mainly to albumin. Basic drugs bind with greater affinity to acid
glycoprotein, and with lower affinity to albumin and other proteins. Although the binding to
albumin is of lower affinity, because it is found in much higher concentrations than the A1 acid
glycoprotein, it has greater capacity.

DIRECT ACTING CHOLINERGIC AGONISTS:

ACETYLCHOLINE, BETANECOL, CARBACOL, METHACHOLINE, PILOCARPINE……………….

They produce effects similar to those of Achasa (acetylcholine) by binding to cholinergic

receptors, it ends when these agents are destroyed by ACETYLCHOLINESTERASE.

Its topical ophthalmic application produces pupillary constriction, stimulates ciliary muscles
and increases the flow of aqueous humor.

CARBACOL/PILOCARPINE

CARBACOL: Carbamil ofteno, 0.75 and 1.5% (1)

Pilocarpine: pil ofteno, ophthalmic solution 0.5 1, 2, 4 and 6%

Pilo grin ophthalmic solution 1, 2, 4% (2).

1 open angle glaucoma. 1 drop, 1 to 3 times a day

2 chronic and closed-angle glaucoma: individualize dose according to needs

3 miosis to counteract the ophthalmic action of sympathomimetics: 1 drop 1 to 3 times a day

INDIRECT ACTION CHOLINERGIC AGONISTS:

They inhibit achase (acetylcholine) and act indirectly, allowing achase to accumulate in the
synapse and produce reversible inhibition of the effects of cholinesterase, which enhances the
action of achase.

Its topical ocular application produces intense miosis and muscle contraction and reduces
intraocular pressure by reducing the resistance to the flow of aqueous humor.

They are used in the treatment of Glaucoma. In their systemic administration they are used as
antidotes in: INTOXICATION, OR OVERDOSE OF ANTICHOLINERGICS. Antidepressants: tricyclics,
diazepam and morphine, in pesticide poisoning PRALIDOXINE is also used in pathologies
related to the urinary tract.

ECOTIOPHATE IODIDE: 0.25% dropper bottle with diluent.

Administration: ophthalmic

Miotic, ocular hypotensive, open angle and aphakic glaucoma, acodomative isotropy

Adults and children: 1 to 2 drops every 12 to 24 hours.

TRANSMITTERS OF THE AUTONOMOUS NERVOUS SYSTEM:

The main transmitters are acetylcholine (Ach) and norepinephrine, where:

….All preganglionic neurons are cholinergic

...post-ganglion parasympathetic neurons are cholinergic and act on muscarinic receptors in

target organs.

…post-ganglion sympathetic neurons are mainly non-adrenergic, although there are some that
are cholinergic (sweat glands).

There are other transmitters in addition to Ach (Acetylcholine) and noradrenaline that act in
many situations (particularly in the enteric nervous system and also in other parts of the
sympathetic and parasympathetic nervous system.

In addition, there is another subdivision of the ANS, which depends on the neurotransmission
released by its terminals. It has been called non-cholinergic, since apparently its
neurotransmission is nitric oxide (NO) and the main site now known for its action is in the
lungs at the level of the bronchial muscle and local nervous circuits.

SITE OF ACTION OF DRUGS THAT ACT ON THE ANS:

D ue to the number of steps in the transmission of autonomic commands from the CNS to the
effector, there are many points where autonomic drugs can act. These sites include CNS
centers, ganglia, postganglionic nerve endings, effector cell receptors, and mechanisms
responsible for termination of transmitter action. The most selective blockade is achieved with
drugs that act on receptors that mediate very specific activities where two groups can be
considered: 1) cholinergic (parasympathomimetic) agonists and antagonists and 2) adrenergic
agonists and antagonists.