Phenols: for vegetative forms of bacteria and fungi. (Disinfection of tools, household items) side: headache, collapse, shortness of breath.

Resorcinol - less antiseptic, keratoplastic and keratolytic action; with skin diseases.

Tar - antimicrobial, keratoplastic, keratolytic, irritating effect; for skin diseases, scabies.

Furacilin - antibacterial action; for treating wounds, washing cavities.

Dyes - antiseptic effect, antidote for cyanide poisoning; outwardly for the treatment of wounds.

Formalin, lysoform - disinfectant and deodorizing for sweating, for washing hands.

Hexamethylenetetramine (urotropine) is an antiseptic for diseases of the urinary tract.

Alcohols - for disinfection of instruments, treatment of the hands of the surgeon and the operating field.

Ticket 45.

1. Types of action of medicinal substances.

There are the following types of action: local and resorptive, reflex, direct and indirect, main and side, and some others.

The drug has a local effect on contact with tissues at the site of its application (usually skin or mucous membranes). For example, with surface anesthesia, the local anesthetic acts on the endings of the sensory nerves only at the site of application to the mucous membrane. To provide local action, medicinal substances are prescribed in the form of ointments, lotions, rinses, patches. When prescribing certain medicinal substances in the form of eye or ear drops, they also count on their local action. However, a certain amount of the drug is usually absorbed from the site of application into the bloodstream and has a general (resorptive) effect. With local application of medicinal substances, a reflex action is also possible.

Resorptive action (from Lat. Resorbeo - I absorb) - the effects caused by medicinal substances after absorption into the bloodstream or direct injection into a blood vessel and distribution in the body. With a resorptive action, as with a local one, the substance can excite sensitive receptors and cause reflex reactions.

Direct (primary) action - a change in the functions of organs by drugs as a result of action on the cells of these organs (cardiac glycosides increase heart contractions, blocking Na + -, K + -ATPase of myocardial muscle cells; diuretics increase diuresis, disrupting the reabsorption of ions and water in the kidneys tubules).

Indirect (secondary) effect - a change in the functions of organs and cells by drugs as a result of action on other organs and cells that are functionally related to the former (cardiac glycosides have a diuretic effect, as they increase heart contractions → improve blood flow in the kidneys → increase filtration and urine formation) ...

A special case of indirect action is reflex - a change in the functions of organs due to direct stimulation of sensitive nerve endings. Depolarization of nerve endings causes an impulse, which is transmitted to the executive organs along reflex arcs with the participation of nerve centers. Skin irritants have reflex effects as a result of excitation of exteroreceptors; interoreceptors - expectorant, emetic, choleretic, laxatives; vascular chemoreceptors - analeptics; skeletal muscle proprioceptors - muscle relaxants.

The reversible action is due to the establishment of fragile physicochemical bonds with cytoreceptors, which is typical for most drugs.

An irreversible effect occurs as a result of the formation of covalent bonds with cytoreceptors, which is characteristic of few drugs, usually highly toxic and used topically.

The main action is the therapeutic effects of drugs.

Side effect - additional, undesirable effects.

The pharmacological effects of the same drug can be major or side effects in various diseases. So, in the treatment of bronchial asthma, the main effect of adrenaline is the expansion of the bronchi, with hypoglycemic coma - an increase in glycogenesis and an increase in blood glucose.

Adverse reactions are observed when taking many medicines. Their frequency in outpatient treatment reaches 10 - 20%, and 0.5 - 5% of patients require hospitalization due to complications of pharmacotherapy.

Selective action - the effect of drugs on the functions of only certain organs and systems. It is due to a greater extent to selective binding to cytoreceptors, to a lesser extent to selective accumulation in organs and tissues, although there are examples of drugs creating high concentrations in cells on which they act. Magnesium sulfate, not being absorbed from the intestines, enhances peristalsis and causes a choleretic effect. When administered parenterally, magnesium ions inhibit the central nervous system. Inhalation anesthetic drugs create a concentration in the brain that is 1.5 - 2 times higher than in the blood. Iodine intensively enters only the thyroid gland.

2. Antidepressants. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Antidepressants Is a group of drugs used to treat depression, capable of improving pathologically altered mood and general mental state, restoring interest in life, activity and optimism in patients with depression.

Classification:

4. 3-cycle

BUT... Antidepressants - inhibitors of the action of monoamines (potentiation of the action of monoamines due to the violation of their reuptake):

a) indiscriminate monoamine reuptake blockers - imizine, amitriptyline, azafen, coaxil;

b) selective serotonin reuptake blockers - fluoxetine, sertraline, trazodone, paroxetine, fluvoxamine

c) selective blockers of the reuptake of serotonin and norepinephrine - venlafaxine, duloxetine, mianserin

5. Gink derivatives

B. Antidepressants - MAO inhibitors => an increase in the level of neurotransmitters in the brain tissue:

a) MAO inhibitors of irreversible indiscriminate action - nialamide;

b) reversible MAO inhibitors — moclobemide, befol;

6. 4-cycle - mixed mechanism (A + B): pyrazidol, incazan, maprotiline

Mechanism of action: inhibition of monoamine oxidase (MAO), localized in the mitochondria of adrenergic and serotonergic nerve endings in the central nervous system, as well as in the cells of the liver, myocardium and other tissues. As a result of enzyme inhibition, intracellular inactivation of monoamines - serotonin, norepinephrine, dopamine - is delayed and the release of mediators into the synaptic cleft increases when impulses arrive. Facilitation of synaptic transmission is accompanied not only by the restoration of mood, but also by the elimination of psychomotor retardation, which is often associated with depression.

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.

3. Class I antiarrhythmic drugs (sodium channel blockers, or membrane stabilizers). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Class I antiarrhythmics -substances that block fast sodium channels of the cell membrane, that is, inhibiting the rate of initial depolarization of cells with a fast electrical response.

Classification:

1) Subclass IA-quinidine, novocainamide.

2) Subclass IB-lidocaine, diphenine

3) Subclass IC-propafenone, etmosine.

Mechanism of action:

Quinidine inhibits the transmission of excitation from the vagus nerve to the heart (due to m-anticholinergic properties), and also somewhat reduces cardiotropic sympathetic (adrenergic) effects. The blocking effect on a-adrenergic receptors is also manifested in relation to peripheral vessels (the total peripheral resistance decreases slightly).

Indications: Supraventricular and ventricular premature beats, atrial tachycardia, AV tachycardia.

Side effects: ringing in the ears, headache, visual impairment. Diarrhea, nausea, and vomiting are often observed. Idiosyncrasy is sometimes noted. Thrombocytopenic purpura is a severe complication1. Atrioventricular and interventricular blocks are possible, as well as toxic tachyarrhythmia. Quinidine lowers blood pressure (total peripheral vascular resistance falls). In the presence of blood clots in the ears of the heart, embolism is sometimes observed (during the transition from atrial fibrillation to sinus rhythm).

Lidocaine - has a depressing effect on automatism (the rate of phase 4 - diastolic depolarization decreases). It does not affect the rate of rapid depolarization (phase 0) or slightly reduces it. In contrast to quinidine, the duration of the action potential (i.e., the repolarization phase) and, to a small extent, the effective refractory period, lidocaine decreases. On the ECG, a shortening of the Q-T interval is noted. The contractility of the myocardium lidocaine does not change or somewhat decreases. It has no vagolytic properties. It has an insignificant effect on hemodynamics. The drug is characterized by a rapidly developing and short-term effect (after a single injection it lasts for 10-20 minutes).

Indications: ventricular arrhythmias (extrasystoles and tachycardia arising from myocardial infarction, open heart surgery, in the postoperative period).

Subclass IC - pronounced arrhythmogenic activity, reduce automatism, more reduce conductivity, do not affect repolarization.

Side effects: ringing in the ears, headache, blurred vision, diarrhea, dyspepsia, decreased blood pressure.

Contraindications: idiosyncrasy, atrioventricular block, liver disease.

Novocainamide - decreases myocardial contractility less than quinidine, vagolytic activity is less pronounced. It is administered enterally and parenterally.

Diphenin - like lidocaine, absorbed slowly, cumulates. Applied for overdose with cardiac glycosides.

4. Anti-tuberculosis drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Anti-tuberculosis drugs - Chemotherapeutic substances that suppress the vital activity and growth of acid-resistant mycobacteria - the causative agents of tuberculosis.

Classification

Group 1 (A) - the most effective drugs (isoniazid and rifampicin);

Group II (B) - drugs of average efficiency [streptomycin sulfate, prothionamide, ethionamide, ethambutol, pyrazinamide, kanamycin sulfate, cycloserine, florimycin sulfate (viomycin)];

Group III (C) - drugs of the lowest efficiency [PASK-sodium, thioacetazone (tibon)].

Mechanism of action: Synthetic anti-tuberculosis drugs (most effective): the mechanism of their anti-tuberculosis action is not completely clear, but there are several points of view:

1. Derivatives of GINK bind important biochemical substances containing a carbonyl group (pyruvic acid, acetaldehyde, pyridoxal, etc.).

2. They inhibit the activity of microbial cell enzymes (catalase, transaminase, amino oxidase, etc.). The inhibition of enzyme activity comes from bacteriostatic concentrations. This is the leading point of view.

3. They are able to form complexes with substances containing metals, and metals are most often constituents of enzymes.

Synthetic anti-tuberculosis drugs of different chemical structure: It has a bacteriostatic effect, equally affecting the intra- and extracellular Mycobacterium tuberculosis. Acts mainly on multiplying mycobacteria. Drug resistance can develop very quickly during treatment.

Indications: Prevention and treatment of active tuberculosis of any localization - isoniazid;

Streptomycin is most effective in the treatment of newly diagnosed and especially fresh cases of tuberculosis;

Kanamycin sulfate is used to treat tuberculosis of the lungs and other organs with resistance to anti-tuberculosis drugs of the 1st and 2nd row (except for florimycin).