Indications for use:

∙ asthenic-depressive syndrome;

∙ endogenous depression;

∙ menopause;

∙ alcoholic depression;

∙ neuroses and psychopathies;

∙ schizophrenia, accompanied by feelings of fear and anxiety;

∙ affective insanity;

∙ complex therapy of Alzheimer's disease and other involutional mental disorders;

∙ bulimia nervosa;

∙ dependence on benzodiazepines, withdrawal symptoms when they are canceled.

Side effects:

∙ drugs with a stimulating effect - anxiety, anxiety, insomnia, headache, confusion, delirium, disorientation, nightmares, tremors, paresthesia;

∙ drugs with a sedative effect - lethargy, drowsiness;

∙ peripheral M-anticholinergic effects;

∙ cardiotoxicity;

∙ orthostatic hypotension;

∙ violation of leukopoiesis by the type of leukopenia and agranulocytosis;

∙ dyspeptic disorders;

∙ increased appetite and weight gain;

∙ allergic reactions;

∙ in men - erectile dysfunction and ejaculation, gynecomastia,

in women - persistent galactorrhea.

Contraindications:

∙ violation of cerebral circulation;

∙ diseases of the blood system, blood-forming organs, liver, kidneys;

∙ decompensated heart failure, ischemic heart disease, angina pectoris, arterial hypotension, myocarditis;

∙ severe atherosclerosis;

∙ thyrotoxicosis, decompensated diabetes mellitus;

∙ pregnancy, breastfeeding;

∙ glaucoma, prostatic hypertrophy, constipation

∙ danger of sympathoadrenal crisis (convulsions, hyperthermia, coma)!

∙"Serotonin crisis" with the development of dyspeptic disorders, delirium, hyperthermia, arterial hypertension, muscle rigidity, myoclonus. decay of skeletal muscle!

Amitriptyline - antidepressant activity, acts in 10-14 days, there is no psychosedative, stimulating effect.

Imizin acts in 2-3 weeks.

Fluoxetine - high antidepressant activity, acts after 1-4 weeks, no sedative, does not change weight.

Maprotiline - similar to imizine, slowly absorbed.

Moclobemide - action is short, no ↑ blood pressure, sedation.

Nialamide - well tolerated.

87. Antiplatelet agents. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Antiplatelet agents - these are drugs that in various ways inhibit the aggregation of platelets induced by damage to the endothelium or cause the dissolution of the resulting aggregates to the stage of their irreversible adhesion.

Classification:

I Inhibition of the activity of the thromboxane system

1. decreased thromboxane synthesis

1. cyclooxygenase inhibitors (ACETYL SALICYL ACID)

2. thromboxane synthetase inhibitors (DAZOXIBEN)

2. thromboxane receptor block

3. mixed-action substances

II Increase in the activity of the prostacyclin system:

drugs that stimulate prostacyclin receptors (EPOPROSTENOL)

III Drugs that inhibit the binding of fibrinogen to platelet glycoprotein receptors

1. Glycoprotein receptor antagonists (ABCIXIMAB, TYROFIBAN)

2. Means that block the purine receptors of platelets and prevent the stimulating effect of ADP on them (TIKLOPIDIN, KLOPIDOGREL)

IV Means of different types of action (DIPIRIDAMOL, ANTURAN)

Indications: prevention of insufficient cerebral and coronary circulation, strokes; tumbling in case of myocardial infarction, angina pectoris, after coronary angioplasty, in diseases with impaired peripheral circulation, in late pregnancy (DIPIRIDAMOL)

Aspirin - Mechanism: causes an irreversible blockade of cyclooxygenase, due to which it inhibits the synthesis of thromboxane A2 and promotes the synthesis of prostacyclin by endothelium, inhibits the release of platelet factors III and IV.

Apply to prevent the formation of postoperative blood clots, with thrombophlebitis, strokes, ischemic heart disease.

Side effects- dyspepsia, stomach bleeding, allergies. Cannot be used for peptic ulcer disease, portal hypertension, clotting disorders.

Dipyridamole- mechanism: Expands coronary vessels, increases oxygen delivery, improves collateral circulation, previously it was widely used as an antianginap drug in chronic coronary artery disease. inhibits platelet aggregation and thrombus formation, since it increases the content of cAMP in platelets, increases the synthesis of prostacyclin in the endothelium.

Side effects: redness of the face, tachycardia, allergies, sometimes hypotension.

Contraindications: hypotension.

Ticlopidine - works stronger than aspirin, but more slowly, after 7-8 days. It blocks the adenosine diphosphate mechanism of platelet aggregation, stimulates the synthesis of prostaglandins E, D2 and prostacyclin.

It reduces the risk of recurrent strokes and heart attacks

Contraindications: risk of bleeding, hemorrhagic stroke, liver disease, pregnancy.

Side effects: dizziness, stomach pain, diarrhea, allergies, jaundice, thrombocytopenia, leukopenia.

109. Antibiotics of the cephalosporin group. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

a) Generation I (highly active against G + bacteria): cefazolin, cephalothin, cefapirin, cefradine, cephalexin

b) Generation II (highly active against G-bacteria): cefamandol, cefuroxime, cefaclor, cefoxitin, cefmetazole

c) III generation (with high activity against Pseudomonas aeruginosa): cefotaxime, ceftazidime, cefoperazone, cefixime

d) IV generation (active against bacteroids and other anaerobes): cefpirome

Mechanism: inhibit the synthesis of peptidoglycan of the cell wall, inhibit the synthesis of murein. prevent the formation of peptide bonds due to transpeptidase.

Character: bactericidal action.

I - act on gram (+) and some gram (-) and do not act on Pseudomonas aeruginosa, Proteus, bacteroids

II - act on gram (+) and some gram (-), proteus and enterobacteria, do not act on Pseudomonas aeruginosa

III - stronger by gram (-), penetrate the BBB;

IV - act on gram (+), Pseudomonas aeruginosa, gram (-)

Spectrum: wide. Penicillinase resistant, but destroyed by beta-lactamase (I).

IndicationsI:

• urinary, respiratory tract infections

• meningitis

• prevention of septic complications during surgery

• pyelonephritis, cystitis

• streptococcal tonsillopharyngitis

• exacerbation of chronic bronchitis

• community-acquired pneumonia requiring hospitalization

• community-acquired infections of the skin and soft tissues of mild to moderate severity

• infections against the background of neutropenia and immunodeficiency states

• sepsis

Side effects:

• allergies

• kidney damage

• diarrhea

• bleeding

• thrombocytopenia

• dysbiosis

• pseudomembranous colitis

Contraindications:

• hypersensitivity

• pregnancy

• breast-feeding

• gastrointestinal diseases

• bleeding

Cefazolin - penetrates the placental barrier, lasts 6-8 hours.

Cefuroxime - resistant to beta-lactamases, penetrates the BBB, lasts 6-8 hours.

Ceftriaxone - resistant to beta-lactamases, penetrates the BBB, acts for 24 hours.

Cefepim - resistant to beta-lactamases, penetrates the BBB, lasts 12 hours