2. Alpha and alpha, beta adrenomimetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

1. Stimulating alpha and beta-adrenergic receptors: ADRENALINE HYDROCHLORIDE (beta 1,2, alpha 1,2) NORADRENALINE HYDROTARTRAT (alpha 1,2, beta1)

2. Stimulating predominantly alpha-adrenergic receptors: MESATON (alpha1), NAFTHISIN, GALAZOLINE (alpha2)

3. Stimulating predominantly beta-adrenergic receptors: ISADRIN (1,2). SALBUTAMOL, PHENOTHEROL (2). DOBUTAMINE (1)

ADRENALIN - belongs to the group of phenylalkylamines, is a biogenic catecholamine.

Main pharmacological effects:

CNS - increases excitability, improves cerebral circulation, stimulates the secretion of adrenorcorticotropic hormone (ACTH) by the adenohypophysis

EYE- dilates the pupil due to contraction of the radial muscle of the iris, practically does not affect accommodation (since there are no adrenergic receptors in the ciliary muscle). It complicates the outflow of intraocular fluid, but reduces its production (inflow) due to the narrowing of the retinal vessels. The latter effect is predominant; therefore, intraocular pressure as a whole is somewhat reduced. This makes it possible to use the drug in the open-angle form of glaucoma (associated with excessive production of intraocular fluid), but in the closed-angle form (associated with a deterioration in outflow), adrenaline is contraindicated

SPLEEN - reduces the capsule and trabeculae, which leads to the release of deposited erythrocytes and platelets into the blood.

BRONCHI - expands

A HEART - increases the strength of heart contractions, conduction, excitability, automatism, increases stroke and minute blood volumes. It mainly causes tachycardia, which, however, can be replaced by bradycardia. The latter is associated with the emergence of vagal reflexes from vascular baroreceptors (aortic arch, carotid sinus zone) in response to an increase in the stroke volume of blood...

Activates metabolic processes in the myocardium. Improves blood supply to the myocardium (due to the expansion of the coronary vessels)

Epinephrine is effective when administered locally and parenterally (subcutaneous, intravenous, intramuscular). Duration of action - from 5 to 30 minutes

Indications Locally - as a vasoconstrictor for rhinitis, conjunctivitis - open-angle glaucoma - to enhance and prolong the effect of local anesthetics Resorptively: - anaphylactic shock, status asthmaticus, serum sickness, angioedema - hypoglycemic coma - heart failure

Side effects: insomnia, tremors, hypertension, tachycardia, arrhythmias, pain in the heart, nausea, vomiting

Contraindications:hypertension, atherosclerosis, ischemic heart disease, hyperthyroidism, diabetes mellitus, pregnancy, angle-closure glaucoma, fluorothane and cyclopropane anesthesia (these anesthetics increase the sensitivity of the myocardium to catecholamines, as a result of which arrhythmias can develop, up to ventricular fibrillation and death). Adrenaline is contraindicated in all types of shock, with the exception of anaphylactic

MEZATON - It causes a vasoconstrictor effect and increases blood pressure weaker than adrenaline and norepinephrine, but for a longer period (intravenously - up to 20 minutes, subcutaneously - 40-50 minutes). This is due to the fact that mezaton is a synthetic preparation, it is not a catecholamine, therefore it is not destroyed by the COMT enzyme. Effective when taken orally. It can be used in conditions of cyclopropane and fluorothane anesthesia. From the heart causes bradycardia (reflex)

Indications Locally - as a vasoconstrictor for rhinitis, conjunctivitis - open-angle glaucoma - to enhance and prolong the effect of local anesthetics resorptively (intravenous, intramuscular, subcutaneous) - collapse and hypotension of vascular origin, preparation for surgery, intoxication, infectious diseases with a decrease in blood pressure

Side effects insomnia, tremors, hypertension, tachycardia, arrhythmias, pain in the heart, nausea, vomiting

Contraindications - cardiogenic shock - hypovolemic - hypertension - atherosclerosis, - coronary artery disease, - hyperthyroidism, - diabetes, - pregnancy, - angle-closure glaucoma

3. Antihistamines (H1-histamine receptor blockers). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Antihistaminesdrugs- a group of drugs that competitively block histamine receptors in the body, which leads to inhibition of the effects mediated by them.

H1-histamine receptor blockers:

prevent the interaction of histamine with specific receptors and eliminate the main clinical manifestations of an immediate allergic reaction: edema, hyperemia, itching, spasm of gl / m of internal organs, vasodilation, hypersecretion.

Classification:

Derivatives

1. Diphenylmethane - DIMEDROL, TAVEGIL

2. Phenothiazine - DIPRAZINE

3. Piperazine - STUGERON

4. Ethylenediamide - SUPRASTIN

5. Carboline - DIAZOLINE

Different chemical structure: ZIRTEK (cyterizin), ALLERGODIL, KESTIN

Features of 1st generation H1 blockers:

- They penetrate the BBB well, therefore they have a pronounced sedative effect (drowsiness, lethargy, lethargy, decreased performance)

-Low affinity for H1-receptors in therapeutic doses

-Insufficient duration of action (4-6 hours)

H-high selectivity in relation to H1-receptors (they also block M-cholinergic receptors, serotonin 5HT receptors,-adrenergic receptors, dopamine receptors)

-Appetite stimulation and weight gain

-Dysfunction of the gastrointestinal tract

- Often addictive

Indications for use -Allergic rhinitis and conjunctivitis (seasonal and year-round) - Skin allergic diseases: itchy dermatoses (especially CIPROHEPTADINE), atopic dermatitis, eczema, neurodermatitis, acute and chronic urticaria, Quincke's edema, etc. 3) Allergic reactions to insect bites 4) insomnia 5) Vomiting of central genesis 6) Vestibular disorders Premedication Hyperthermia (as part of "lytic mixtures" in combination with non-narcotic analgesics and antipsychotics)

Side effects - Sedative and hypnotic effects (least pronounced in Diazolin, Fenkarol, Tavegil): lethargy, drowsiness, fatigue, impaired coordination, ataxia, decreased concentration, increased time of motor reactions (effects are potentiated by alcohol) -Headaches, dizziness, decreased blood pressure (especially Diprazine, Diphenhydramine, Tavegil) - M-anticholinergic effects: dry mouth, dry skin, impaired accommodation, increased IOP, tachycardia, intestinal atony (constipation), urinary tract atony (urination disorder) - Irritation of the gastrointestinal mucosa (Diazolin, Fenkarol) - Agranulocytosis (Diazolin, Diprazin) - Cholestasis (Diprazine) - Skin rashes

four. Antihelminthic drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Anthelminthic agents disrupt the function of the neuromuscular system of helminths, exhibiting anticholinesterase (emetine), cholinomimetic (ditrazine, combantrine) or anticholinergic (piperazine) action. Many drugs (levamisole and others) disrupt various types of metabolism in helminths

Mechanisms of action	Drugs
Cell poisons	Ethylene tetrachloride
Drugs that disrupt the function of the neuromuscular system in roundworms	Piperazine, ditrazine
Drugs that paralyze the neuromuscular system in flatworms and destroy integumentary tissues	Fenasal, Bithionol
Means acting on the energy processes of helminths	Aminoacriquine, Levamisole, Pirvinia pamoat, Oxygen

The effectiveness of antihelminthic agents for various helminthiasis is not the same and is primarily determined by the biological species of parasitic worms and their localization in the body. On the basis of ideas about the direction of action of drugs on various classes of helminths, a classification of antihelminthic agents is constructed. In accordance with this, funds are allocated that are used mainly for the treatment of nematodes, cestedoses and trematodes.

Anthelminthic agents used mainly for nematodes

A drug	Helminthiasis
Citric Seed (Santonin)	Ascariasis
Levamisole (decaris)	Ascariasis
Piperazine adipate (vermitox)	Ascariasis, enterobiasis
Naphtamon (befenium)	Ankyostomosis, trichocephalosis
Diphezil	Trichocephalosis
Pirantel (Combatrin)	Enterobiasis, ascariasis, non-cardiosis
Thiabenzadol (mintezol)	Strongyloidiasis, noncatorosis, trichinosis
Ditrazine (notezin)	Filariasis

Anthelminthic drugs used mainly for cestodosis

A drug	Helminthiasis
Male fern extract	Teniosis, teniarinchiasis, hymenolepiasis, diphyllobothriasis
Fenasal (niclosamide)	Teriarynchiasis, diphyllobothriasis, hymenolepiasis

Broad-spectrum anti-herbal remedies

A drug	Helminthiasis
Ambilgar (niridazole)	Nematodes, trematodes
Praxivantel (Pickwiton)	Cestodoses, trematodes
Mebendazole (vermox, mebenvent)	Nematodes, trematodes, cestodoses
Albendazole (Zentel)	Nematodoses, cestodoses
Bithionol (actamer)	Nematodoses, cestodoses

One of the most effective remedies for ascariasis is levamisole (decaris). A single injection of the drug leads to deworming in 90 - 100% of patients, regardless of the degree of their infection. Unlike santonin, the drug acts on ascaris of all age groups. Levamisole is less effective in ankylostomiasis and strongyloidiasis.

The mechanism of the anthelmintic action of levamisole is based on the specific inhibition of the enzyme succinate dehydrogenase, as a result of which the fumarate reduction reaction, which is most important for nematodes, is blocked. It should be borne in mind that levamisole does not affect succinate dehydrogenase in mammals and only inhibits the helminth enzyme.

The main indication for the use of the drug is ascariasis. Treatment with levamisole (unlike treatment with many anthelmintic drugs) does not require preliminary preparation of the patient - a special diet, the use of laxatives, etc. It is used once before bedtime (for adults at a dose of 150 mg). The drug is well tolerated.

In the treatment of cestodoses, the most common remedy is male fern extract, which is highly toxic and requires careful special preparation of the patient. The main active principles of the male fern extract - philicic acid, aspidin and desaspidin - cause paralysis of the neuromuscular apparatus of flatworms.

Treatment is carried out according to a specific scheme, including diet and laxatives. The dose of the extract for adults is up to 8 g. Often there are numerous side effects in the form of nausea, vomiting, abdominal pain, palpitations. Convulsions, collapse, heart failure are possible. These side and toxic effects, as well as certain contraindications, limit the use of male fern preparations.

In modern medical practice, for the treatment of cestodosis, fenasal is mainly used, which is highly effective in theriarynchiasis, diphyllobothriasis and hymenolepiasis. Fenasal paralyzes tapeworms. In addition, it causes the destruction of the integumentary tissues of helminths and reduces their resistance to the action of proteolytic enzymes of the gastrointestinal tract, contributing to the digestion of cestodes (in this regard, phenasal is not recommended for use in teniasis due to the risk of developing cystcercosis).

Treatment with fenasal does not require special preparation of patients. It is usually taken at night after a light dinner at a dose of 3 g (for adults); with hymenolepiasis, a course treatment is carried out.

The drug is well tolerated. The high efficiency of phenasal in cestodosis, the absence of contraindications and pronounced side effects ensures its widespread use in medical practice, not only in adults, but also in children.