Ticket 9

one. Basic principles of action of medicinal substances. Their interactions with recipes.

Local - d-e at the site of application (enveloping, surface anesthetics). Resorptive - e after absorption, entering the blood and tissues, depends on the routes of administration, the way to penetrate the barriers. Direct e - at the place of direct contact of the in-va with the tissue. Reflex d-e - influence on extero- and interoreceptors, the effect was manifested by changing the state of the nerve / centers or executing organs (mustard plasters, lobelin - a breathing stimulator).

Receptors, ion channels, enzymes, transport systems (proteins), and genes serve as targets for drugs. Receptors are active groups of substrate macromolecules, with which the substance interacts. Specific receptors provide the manifestation of e-I in-islands (adenosine, adreno-, angiotensin, bradykinin, histamine, dopamine, choline). The affinity of the substance to the receptor, leading to the image of a complex with it, is affinity. The way to stimulate the receptor and cause the effect is internal activity. Agonists are active internally (full agonist - maximal effect). Antagonists - when interacting with receptors, they do not stimulate them (there is no internal activity). There are receptors that bind to cats and do not cause any effects - nonspecific receptors.

Depending on the strength of the "in-in - receptor" bond, reversible and irreversible d-e are distinguished. Selects d-e - in-in interacts only with definite receptors and does not affect others. Intermediates that bind the receptor to the effector are G-proteins, enzymes (cyclases, phospholipases), secondary transmitters (cAMP, Ca ++).

2. M - and M, H - Cholinomimetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Muscarine poisoning, measures of assistance.

I. M-cholinomimetics:

1) Pilocarpine (ocular forms only)

2) Acyclidine (ophthalmic forms, tablets, injections.)

Mechanism of action: stimulates m-cholinergic receptors. They stimulate the central nervous system, narrow the pupil, reduce IOP, accommodation spasm, narrow the bronchi, bradycardia, increase the tone of smooth muscles in the bladder and uterus, increase the secretion of sweat glands, increase the tone of smooth muscles of the gastrointestinal tract, peristalsis.

Indications: glaucoma, intestinal atony, paralytic intestinal obstruction, xerostomia.

Contraindications: bronchial asthma, conduction disturbances in the myocardium, epilepsy, hyperkinesis, pregnancy.

Side effects: hyperexcitability, tremor, bradycardia, bronchospasm, spasm in the gastrointestinal tract and urinary tract, diarrhea, increased uterine tone.

II.M, H-cholinomimetics:

- Acetylcholine (only in experiments, quickly degrades)

- Carbocholine (eye forms only)

Mechanism of action: They act on both M- and H-cholinergic receptors, but the effect on H-cholinergic receptors is weak. The effects are the same as those of M-cholinomimetics.

Indications:

Glaucoma only.

Side effects and contraindications:

Like M-cholinomimetics.

Muscarine poisoning, measures of assistance: Use M-anticholinergics, most often atropine.