Ticket 10

1. Definition of pharmacology as a science, its tasks, place among other medical and biological sciences. Scientific substantiation of the need for animal experiments.

Pharmacology is the science of the interaction of chemical compounds with living organisms. Pharmacon (Greek) - medicine (poison). Logos (Greek) - word, doctrine.

PURPOSE pharmacology is the search for means for the treatment, prevention and diagnosis of diseases. TASKSis the creation of new highly effective and safe drugs based on chemical synthesis products and raw materials of natural origin. Pharmacology studies the effect of drugs on biological systems (from the whole organism to individual cells, receptors and enzymes). As a biomedical science, pharmacology is also associated with experimental and practical medicine. Pharmacology influences the development of physiology and biochemistry (for example, many complex functions of the central nervous system have become available for study thanks to neutrotropic agents). Pharmacology is also important for practical medicine (as a result of the creation of highly effective drugs, pharmacotherapy has become a universal method of treating many diseases). Pharmacology plays an important role in the development of clinical disciplines (the emergence of drugs for anesthesia,

The experiment on animals was introduced in 19 and is an integral part of preclinical studies of drugs, since this allows you to determine the therapeutic efficacy of the drug, its effect on the main anatomical and physiological systems of the body. In the process of studying the pharmacodynamics of a substance, not only its specific activity is established, but also possible side reactions associated with pharmacological activity. In addition, the specific toxicity of the drug is established - oncogenicity, mutagenicity, embryotoxicity, including teratogenic effects.

2. Ethyl alcohol. Antimicrobial effect of alcohol, effect on the central nervous system, skin and mucous membranes, on digestion. Acute and chronic alcohol poisoning. Poisoning treatment.

Ethyl alcohol is a typical substance of a narcotic type of action. It has a depressing effect on the central nervous system, when applied topically, it is an antiseptic (70% alcohol - denaturation of microbial cell proteins). Also, 70% ethyl alcohol solution is used to treat the operating table and the surgeon's hands, 95% - for the treatment of suture material and instruments. It irritates tissues (40%) and therefore can be used as compresses. When taken orally, alcohol has an irritating agent on the CO of the oral cavity, stomach, and enhances the secretion of their glands. In high concentrations (90%) - drying and tanning effect.

Manifestation of central action:

- with a resorptive action, alcohol inhibits the central nervous system (like anesthetics) and in this case, 4 stages are distinguished in the action of alcohol: analgesia, agitation, anesthesia, paralysis)

- increases heat transfer, affecting thermoregulation (vasodilatation by suppressing the vasomotor center)

- a diuretic effect (the production of ADH by the posterior lobe of the pituitary gland decreases)

- enhances the secretory activity of the salivary glands

- 10% or less% alcohol is used to increase appetite and stimulate juice production

- 20% alcohol inhibits the secretion of hydrochloric acid and the digestive activity of gastric juice, resulting in a lot of mucus

- spasm of the pylorus and decreased gastric motility at high alcohol levels (70%)

Acute alcohol poisoning... A person poisoned with alcohol is unconscious, the skin is pale, breathing is rare, the pulse is frequent, the body temperature is low. The severity of poisoning depends on the dose of alcohol and its concentration.

Chronic poisoning. A symptom of aclogolism is a painful need to get drunk. A person develops the phenomena of unstable mood, irritability, sleep and digestive disorders. Decreases memory, mental and physical performance. Later - psychosis, neuritis, chronic gastritis, cirrhosis of the liver.

Poisoning treatment. Teturam is used - it delays the oxidation of alcohol at the acetaldehyde stage, this causes intoxication, a feeling of fear, nausea. As a result, a person develops negative reflexes to alcohol.

3. Means that reduce the tone and contractile activity of the myometrium. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

The contractile activity and tone of the myometrium are regulated by neurohumoral mechanisms. In the myometrium there are m-cholinergic receptors, alpha and beta2-adrenergic receptors. Stimulation of m-cholino and alpha-adreno is a stimulating effect, and beta 2-adreno is a depressing one.

Drugs that weaken the contractile activity of the myometrium (tocolytic drugs)

1. Substances stimulating beta2-adrenergic receptors: PHENOTHEROL, SALBUTAMOL

2. Medication for anesthesia: SODIUM OXIBUTIRATE

3. Miscellaneous: MAGNESIUM SULFATE

PHENOTHEROL are prescribed to delay premature labor, with the threat of termination of pregnancy due to increased tone of the uterus and with violent labor. Fenoterol does not have a selective effect, therefore, when beta2-adrenergic receptors are stimulated, it not only relaxes the myometrium, but can also stimulate other organs. When administered enterally, fenoterol acts faster, but for a short time than salbutamol. Side effects include maternal and fetal tachycardia, fetal hyperglycemia

SODIUM OXIBUTIRATEused to weaken excessively strong labor pains. A side effect is hypokalemia and seizures.

MAGNESIUM SULPHATE violates the penetration of calcium ions into the cells of the myometrium, which are necessary for contractions.

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:

1. Erythromycin, oleandomycin

2. Spiramycin, dirithromycin

3. 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

Indications for use: - infections of the upper and lower respiratory tract - whooping cough and its prevention - diphtheria - infections of the skin and soft tissues - other functions of the oral cavity - trachoma - sexually transmitted infections

Side-by-side: - nausea, vomiting - cramping abdominal pain - fever - jaundice - with i / v - thrombophlebitis, Hearing impairment

Contraindications: - hypersensitivity - pregnancy - breast-feeding

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;