Материал: npe

Ticket 50

1. Side and toxic effects of medicinal substances. Allergic and non-allergic side effects. Toxicity. Teratogenicity. Embryotoxicity. Carcinogenicity. Idiosyncrasy.

Side effects - the rest (except for the main one, that is, beyond the scope of the purpose for which the medicine is prescribed), the effects of the drug when it is used in a therapeutic dose.

• Toxicity - the ability of a substance to cause disturbances in the physiological functions of the body. Toxic effect - medicinal substances develop, as a rule, with the growth of toxic doses of the substance into the body (in case of an overdose).

In case of an absolute overdose (with an absolute excess of single, daily and course doses), excessively high concentrations are created in the blood and tissues. Toxic effect also occurs with a relative overdose of the drug, with the appointment of medium therapeutic doses to patients who have a reduced detoxification function of the liver or excretory function kidney, with long-term treatment with medicinal substances capable of cumulation.

• Allergic reactions (allos-other, ergon-action) - These reactions, which occur when drugs are re-administered, are based on immune mechanisms. Drugs in this case act as allergens. Allergic reactions do not depend on the dose of the administered substance and are varied in their own way nature and severity: from mild skin manifestations to anaphylactic shock. • Teratogenic action (teras-freak) - develops during 4-8 weeks of pregnancy. At this time, the formation of the skeleton and the laying of internal organs occurs. At this stage of pregnancy, organs and tissues are most sensitive to the action of damaging factors. Therefore, the use of medicinal substances can lead to anomalies in the development of the skeleton and internal organs. • Embryotoxic effect (embryon - embryo) - drugs develops in the first 12 weeks of pregnancy. In the early stages of pregnancy (1-3 weeks), this is a consequence of the action of medicinal substances on the zygote and blastocysts located in the lumen of the fallopian tubes and uterus (before implantation), as well as on the process of implantation of the embryo into the uterus. • Carcinogenic decree (canser-cancer) - the ability of drugs to cause the development of malignant neoplasms.

• Idiosyncrasy is a genetically determined hypersensitivity that occurs in some people in response to certain nonspecific (as opposed to allergies) stimuli.

2. Ganglion blocking agents. Classification. Mechanism of action. Indications for use. Side effects. Contraindications. Comparative evaluation of the drug.

Ganglion blockers - These are drugs that selectively block the H-cholinergic receptors in the autonomic ganglia (sympathetic and parasympathetic). In addition, ganglion blockers block the H-cholinergic receptors of the chromaffin cells of the adrenal medulla (reducing the release of catecholamines), as well as the H-cholinergic receptors reflex arousal of respiratory and vasomotor)

Classification:

1. Short-acting: Gigronium (12-20 min.), Arfonad (15-20 min.), Imekhin (4-10 min.)

2.Medium duration: Pentamin (1-2 hours), benzohexonium (2-4 hours), Pachikarpin (4-6 hours)

3. Long-term action: Camphonium (6-8 hours), Pyrylene (8-12 hours) - an unfavorable effect on the central nervous system.

Mechanism of action: Ganglion blockers block sympathetic and parasympathetic ganglia, as well as n-cholinergic receptors of the cells of the adrenal medulla and the carotid glomerulus, they are referred to as antidepolarizing substances.

Pharmacological effects: sedative effect on the central nervous system, dilated pupil, decreased IOP, tachycardia, dilates blood vessels, lowers blood pressure, dilated bronchi, decreased tone of smooth muscles and peristalsis in the gastrointestinal tract, decreased tone of the bladder.

Pyrylene is well absorbed from the gastrointestinal tract, well penetrates the blood-brain barrier, has a stimulating effect on the myometrium.

Pentamine - high activity, pronounced selectivity, poorly absorbed in the gastrointestinal tract, so it is advisable to administer it intravenously.

3. Preparations of pituitary hormones. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Corticotropin - a diagnostic tool for assessing the reserves of the adrenal cortex in primary adrenal insufficiency or in case of its hypofunction against the background of prolonged use of glucocorticoids.

Tetracosactide (synacthen depot, cozintropin)

• has less immunogenicity

• less likely to cause allergic reactions

lasts longer and can be applied once a day.

Indications for use

- prevention of complications of long-term use of GC;

- in the complex therapy of connective tissue diseases, allergic diseases, dermatoses, ulcerative colitis.

Genetically engineered somatotropin analogs - sayen, humatrop, biosome, genotropin, zomactone, norditropin

Indications for use:

• pituitary dwarfism;

• growth disorders in children with chronic renal failure;

• gonadal dysgenesis (Shereshevsky-Turner syndrome)

Menotropins (menopausal gonadotropin, pergonal, menogon, humegon) - FSH and LH in a 1: 1 ratio (75 IU each).

Urofolitropin - FSH and a small amount of LH.

Follitropin alpha (gonal-F) and follitropin beta (puregon) - recombinant FSH.

Indications for use

Among women - anovulatory infertility due to hypothalamic-pituitary disorders during reproductive procedures.

in men - violation of spermatogenesis, hypothalamic-pituitary hypogonadism.

Oxytocin

Desaminooxytocin (Sandopart, Demoxytocin)

(tablet form, buccal, does not increase blood pressure)

Hyphotocin (pituitrin M)

Indications for use:

• stimulation of labor in post-term pregnancy, premature discharge of amniotic fluid, weakness of labor in the second stage of labor (expulsion of the fetus);

• treatment and prevention of atonic uterine bleeding after abortion, in the early postpartum period;

• to accelerate the involution of the uterus;

• hypolactation in the postpartum period.

4. Antibiotics from the group of macrolides and aminoglycosides. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Macrolides are low-toxic agents for oral administration for infections caused by G + bacteria and intracellular microorganisms. There are 3 generations of macrolides:

4. Erythromycin, oleandomycin

5. Spiramycin, dirithromycin

6. Azithromycin (sumamed)

Mechanism of action of AB - inhibit microbial cell protein synthesis

Origin classification:

Natural - erythromycin, oleandomycin, spiromycin

Prodrugs - oleandomycin-troleandromycin esters

Semi-synthetic - azithromycin

Macrolides, depending on the type of microorganism and dose, can have a bracteriostatic or bactericidal effect. Spectrum of action: staphylococcus, streptococcus, pneumococcus, meningococcus, gonococcus, corynebacterium diphtheria, clostridium gas gangrene

Macrolides are prescribed orally and some intravenously (erythromycin).

Macrolides:

- have a mucoregulatory effect

- weaken the inflammatory reaction as a result of inhibition of the synthesis of PG, LTE and IL

- about immunomodulatory properties

There are 3 generations of aminoglycoside antibiotics (classification):

- I generation - streptomycin, kanamycin, neomycin (used only for local action);

- II generation - gentamicin, tobramycin, amikacin;

- III generation - netilmicin (has less oto- and vestibulotoxicity).

Streptomycin and kanamycin suppress mycobacterium tuberculosis, streptomycin is active against brucella, the causative agents of plague and tularemia. The most sensitive to neomycin are Escherichia coli, Klebsiella, Enterococcus, Proteus and Enterobacter species. Antibiotics of the II - III generation are toxic for E. coli, Klebsiella, Serration, Pseudomonas aeruginosa, Proteus species, Enterobacter and Acinetobacter. All aminoglycosides inhibit 90% of Staphylococcus aureus strains. Resistance to aminoglycosides is characteristic of anaerobic bacteria, hemolytic streptococci, and pneumococci.

The bactericidal effect of aminoglycosides is due to the formation of abnormal proteins and the detergent effect on the lipoprotein cytoplasmic membrane of microorganisms.

Antibiotics of the β-lactam group, inhibiting the synthesis of the cell wall, potentiate the antimicrobial effect of aminoglycosides. Levomycetin, blocking transport systems in the cytoplasmic membrane, weakens their action.

When these antibiotics are taken by mouth, dyspeptic disorders are common. Anaphylactic shock is mainly caused by streptomycin sulfate, which in this respect is in second place after penicillin preparations.

Aminoglycosides can disturb hearing, balance (in 10 - 25% of patients), kidney function, and cause neuromuscular blockade. At the beginning of aminoglycoside therapy, tinnitus appears.

Aminoglycosides are contraindicated in hypersensitivity, botulism, myasthenia gravis, Parkinson's disease, drug parkinsonism, hearing and balance disorders, severe kidney disease. Their use during pregnancy is allowed only for health reasons. During treatment, breastfeeding is stopped.

Indications:Tuberculosis-streptomycin, kanamycin; plague streptomycin; tularemia-streptomycin, gentamicin, brucellosis-streptomycin

purulent-septic diseases - sepsis, peritonitis, meningitis, abscess;

postoperative infectious complications;

kidney infections - pyelonephritis, respiratory tract - pneumonia, lung abscess;

infective endocarditis;