Материал: npe

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;

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1. Dependence of the effect on the dose (concentration) of the active substance. The breadth of the therapeutic action. The value of the choice of dosage forms and methods of drug administration.

Depending on the dose of the drug, the rate of development of the effect, its severity, duration, and sometimes character change. Usually, with an increase in the dose (concentration), the latency period decreases and the severity and duration of the effect increases.

Dose -the amount of substance per dose. It is indicated in grams or fractions of a gram. For a more accurate dosage of drugs, their amount is calculated per 1 kg of body weight. Sometimes substances are dosed based on the size of the body surface (per 1 m ^ 2)

Therapeutic doses:

 minimum (threshold) therapeutic dose - the minimum amount of a drug that causes a therapeutic effect;

 average therapeutic dose - the range of doses in which a drug has an optimal prophylactic or therapeutic effect in most patients;

 maximum therapeutic dose - the maximum amount of a drug that does not have a toxic effect.

Lethal doses:

 the minimum lethal dose (LD10) is the dose that causes death in 10% of cases;

 the average lethal dose (LD50) is the dose that causes death in 50% of cases;

 maximum lethal dose (LD100) - the dose that causes the death of all poisoned animals.

Breadth of therapeutic action - the range between average and maximum therapeutic doses.

To achieve a quick therapeutic effect, drugs are sometimes prescribed in shock doses (antibiotics, sulfonamides). Drugs capable of cumulation are used in maintenance doses. In pediatric practice, drugs are dosed based on the weight or surface of the child's body.

The method of administration of the drug is directly related to its dosage form. So liniment is applied externally, rubbing with a thin layer on the affected area. Tablets are used enterally, and solutions in ampoules are used parenterally.

2. Antipsychotics. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. The concept of neuroleptanalgesia

Antipsychotics - ggroup of drugs with antipsychotic properties, i.e. the ability to eliminate or suppress the productive symptoms of psychosis in the form of disorders of thinking (delirium), perception (auditory, visual, olfactory hallucinations) and motor activity.

Classification:

BUT. Typical antipsychotics (often cause extrapyramidal disorders)

1.Phenothiazine derivatives: AMINAZINE, TRIFTHAZINE, FLUOROPHENAZINE, ETHAPERAZINE

2. Derivatives of butyrophenone: GALOPERIDOL, DROPERIDOL

3. Derivatives of thioxanthene : CHLORPROTIXENE

B. "Atypical" antipsychotics (do not cause or very rarely cause extrapyramidal disorders)

1. Derivatives of dibenzodiazepine: KLOZAPIN, QUETIAPIN

2. Benzamide derivatives: SULPIRIDE

3. Derivatives of benzisoxazole: RISPERIDON

The main mechanism of action of neuroleptics is blockade of dopamine receptors of the mesolimbic system, this action determines their ability to eliminate delusions, hallucinations, psychomotor agitation... In addition, antipsychotics can block serotonin, histamine, and alpha-adrenergic receptors in the central nervous system....

AMINAZINE has a pronounced effect on the central nervous system, as well as on peripheral innervation, executive organs and metabolism.

AMINAZIN is characterized by antipsychotic and sedative effects, the ability to cause extrapyramidal disorders with prolonged use. In large doses, it pulls out a hypnotic effect. Aminazine causes a decrease in motor activity, inhibits the center of heat regulation, hypotremia is observed, has an antiemetic effect, potentiates the action of neutrotropic drugs (anesthesia, opioid analgesics). Reduces blood pressure.

TRIFTHAZINEcharacterized by more selective than chlorpromazine, antipsychotic effect and less pronounced sedative. Differs in weak hypotensive and muscle relaxant action.

Neuroleptanalgesia is a combined method of intravenous general anesthesia, in which the patient is conscious, but does not experience emotions (neurolepsy) and pain (analgesia).

3. Cardiac glycosides. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Cardiac glycosides - complex nitrogen-free substances of plant origin with a pronounced cardiotonic effect.

CLASSIFICATION

1. Short-acting drugs with a short latency period and low cumulative potential: Korglikon (Landysh), Strofantin (Strofant) - in / in

2. Medium duration drugs with an average latency period and an average cumulative capacity: DIGOXIN, CELLANIDE (intravenous, inside). ADONISIDE, HORIZONTAL HERBAL NATURAL, CARDIOVALENE - inside

All drugs in this group are characterized by: The beginning of the development of the effect - 30 min - 2 h

1. Maximum effect - 6-8 hours

2. Complete cessation of action - 2-7 days

By chemical structure - medium polarity

3. Long-acting drugs with a pronounced latency period and the ability to cumulate: DIGITOXIN, CORDIGIT

1. Preparations for oral administration only

2. Well absorbed from the gastrointestinal tract (low polarity, lipophilic)

3. The beginning of the development of the effect - 2-4 hours

4. Maximum effect - 12 hours

5. Complete cessation of action - 2-3 weeks

EFFECTS OF GLYCOSIDES:

- chronotron negative (AV-conductivity decreases)

- negative dromotropic (slows down the repolarization phase and increases the refractory period)

- put batmotropic - increase the efficiency of the myocardium

- increases automatism

- reduction of edema, shortness of breath

- decrease in venous pressure and BCC

- increased urine output

Cardiac glycosides differ in the duration of the latent period of action and the rate of increase in the effect. When administered intravenously, STROFANTIN begins to act in 5-10 minutes, and CELANID in 5-30. With the introduction of DIGOXIN, the effect develops after 30 minutes, and with the administration of DIGITOXIN after 2 hours

With intravenous administration, the maximum effect occurs especially quickly with STROFANTIN (30 min), then DIGOXIN AND CELLANIDE (1-5H), then DIGITOXIN (4-12H),

4. Antifungal drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Antifungal agents (antimycotics) - medicines used for the prevention and treatment of fungal infections (mycoses).

Mycoses are diseases caused by pathogenic or opportunistic fungi. Fungal infections can be systemic (deep) and superficial.

Antifungal agents differ from each other in origin (natural or synthetic), spectrum and mechanism of action, effect (fungicidal or fungistatic), indications for use (local or systemic infections), methods of administration (oral, parenteral, external).

Classification:

I. Means used in the treatment of diseases caused by pathogenic fungi:

1. With systemic or deep mycoses (coccidioidomycosis, paracoccidioidomycosis, histoplasmosis, cryptococcosis, blastomycosis):

- antibiotics (amphotericin B, mycoheptin);

- derivatives of imidazole (miconazole, ketoconazole);

- derivatives of triazole (itraconazole, fluconazole).

2. With superficial (dermatomycosis):

- antibiotics (griseofulvin);

- derivatives of N-methylnaphthalene (terbinafine);

- derivatives of nitrophenol (chloronitrophenol);

- iodine preparations (alcohol solution of iodine, potassium iodide).

II. Drugs used in the treatment of diseases caused by opportunistic fungi (for example, with candidiasis):

- antibiotics (nystatin, levorin, amphotericin B);

- derivatives of imidazole (miconazole, clotrimazole);

- bis-quaternary ammonium salts (dequalinium chloride).

Polyene antibiotics- antimycotics of natural origin produced by molds: Streptomyces nodosum (amphotericin B), Actinomyces levoris Krass (levorin), actinomycetes Streptoverticillium mycoheptinicum (mycoheptin), actinomycetes Streptomyces noursei (nystomyces noursei). These are substances with a complex chemical structure containing a polyunsaturated macrocyclic lactone ring.

Mechanism of action.

The drugs firmly bind to ergosterol (the main component of the fungal membrane), as a result of which hydrophilic pores are formed in the membrane, through which ions and low molecular weight substances escape from the cell, which leads to cell death

Spectrum of action. Polyenes differ in their spectrum of action. Topical preparations (nystatin, natamycin, levorin) act mainly on fungi of the genus Candida spp. Preparations for systemic use have a wide spectrum of action. Also, some drugs are characterized by activity against some protozoa - Trichomonas (natamycin), leishmania and amoebas (amphotericin B). Insensitive to amphotericin B causative agents of zygomycosis. Dermatomycetes (genus Trichophyton, Microsporum and Epidermophyton), Pseudoallescheria boydi, etc. are resistant to polyenes.

Common systemic side effects of polyenes taken by mouth are: nausea, vomiting, diarrhea, abdominal pain, and allergic reactions; with local use - irritation and burning sensation of the skin. Amphotericin B - chills, nausea, vomiting, headache, hypotension, phlebitis, as well as nephro-, hepato-, neurotoxicity, hematological reactions, electrolyte metabolism disorders.

Contraindications: diseases of the gastrointestinal tract (gastric ulcer and duodenal ulcer, acute gastroenterocolitis), impaired renal and liver function, individual drug intolerance.

Azoles - the most numerous group of synthetic antifungal agents.

Mechanism of action.

The antifungal effect of azoles, like polyene antibiotics, is due to a violation of the integrity of the fungal cell membrane, but the mechanism of action is different: azoles disrupt the synthesis of ergosterol - the main structural component of the fungal cell membrane