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Ticket 17.

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 violations of the physiological functions of the body.

The toxic effect of medicinal substances develops, 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 drugs 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 non-specific (as opposed to allergy) stimuli.

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

Analeptics are a group of drugs that primarily excite the centers of the medulla oblongata - vasomotor and respiratory.

Classification:

1. Analeptics of direct action: caffeine, cordiamine, bemegrid, camphor, etymizole.

2.Analeptics of reflex action: cititon, lobelin.

Mechanism of action: Analeptics increase the excitability of the respiratory center. Its sensitivity to humoral stimuli and nerve stimuli increases. In some analeptics, the central action is complemented by a reflex one (from the chemoreceptors of the carotid sinus zone). Analeptics excite not only the respiratory, but also the vasomotor center. They lead to an increase in the total peripheral vascular resistance and an increase in blood pressure.

Camphor, in addition to its analeptic properties, can also have a number of effects. Locally: irritating effect on the skin and mucous membranes, improving blood circulation, if it enters the gastrointestinal tract, it has a weak deodorizing, choleretic, antimicrobial effect. After absorption: improves tissue respiration, metabolic processes; displaces toxic substances from the surface of cells; constricts peripheral vessels, dilating the vessels of the lungs and heart; inhibits platelet aggregation.

Indications: 1. Respiratory depression, asphyxia of newborns.

2. Poisoning with drugs, sleeping pills.

3. Acute and chronic circulatory disorder.

4. Shock state

5. To speed up the urge after anesthesia.

Side effects: Bemegrid: nausea, vomiting, convulsions.

Etimizole: nausea, dyspepsia

Contraindications: Tendency to seizures.

Comparative characteristics: 1. A solution of camphor in oil reflexively acts from the injection site

2.Cityton reflex action from chemoreceptors of the carotid sinus zone,

3. Caffeine-sodium benzoate dilates blood vessels, bicyclic ketone (terpene) constricts blood vessels.

4.Cordiamin has a greater effect on the vasomotor center

5. Bemegrid has a greater effect on the respiratory center.

4. Anti-spirochete drugs. Classification. Mechanism of action. Indications for use. Side effects. Comparative characteristics.

Anti-spirochetes are a group of drugs used to treat diseases caused by spirochetes.

Classification: short-acting (benzylpenicillin sodium or potassium salt)

Long-acting: (novocaine benzylpenicillin salt, bicillins)

Mechanism: block thiol enzymes containing sulfhydryl groups.

Indications: Used for spirochetosis and syphilis.

Side effects: headache, vomiting, fainting, collapse, dermatitis, erythema, fever, euphoria, convulsions, liver damage.

Organic bismuth preparations: biloquinol, bismoverol, pentabismol. Only for syphilis. Cumulate in parenchymal organs, in the central nervous system. Mechanism: block sulfhydryl groups of thiol enzymes. The nature of the action: treponemostatic. Side effects - gingivitis, stomatitis, nephropathy. Contraindications: liver, kidney, oral cavity diseases.

Ticket 18.

1. Pharmacological work of domestic physiologists and clinicians (im Sechenov, ip Pavlov, sp Botkin, ni Pirogov)

Sechenov - pharmacology of neurotropic drugs. In 1866, "Reflexes of the head of the brain."

Pavlov - the founder of psychopharmacology, began his activity in the field of pharmacology in the clinic of S.P. Botkin, where he headed the experimental laboratory for 11 years. There, under the leadership of Pavlov, cardiac glycosides, antipyretics, and a number of ions were studied. For the first time in the history of science, Pavlov and his colleagues studied the effect of substances (bromides, caffeine) on higher nervous activity in healthy animals and in experimentally induced neuroses. Pavlov also studied the effects of various substances - acids, alkalis, ethyl alcohol, bitterness - on digestion.

Botkin - studied cardiotropic drugs. In 1860 he founded a clinical experimental laboratory, where the first Russian studies on clinical pharmacology and a therapy experiment were carried out.

Pirogov - research of drugs for anesthesia. The first operation under anesthesia in 1847 on the battlefield.

2. Beta-adrenergic agonists. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Beta-adrenergic agonists are biological or synthetic substances that stimulate beta-adrenergic receptors and have a significant effect on the basic functions of the body.

Classification:

I. Stimulating predominantly Beta1-adrenergic receptors:

Dobutamine

Beta2-adrenergic receptors:

-Salbutamol

-Terbutaline (bricanil)

-Phenoterol (Berotec, Partusisten)

-Salmeterol (Servent)

-Formoterol

Beta1 Beta2-adrenergic receptors:

-Izadrin

Beta2 Beta1-adrenergic receptors:

-Orciprenaline (Alupent, Asthmopent)

Izadrin - Stimulation of Beta1 receptors: increased strength and heart rate, improved atrioventricular conduction, systolic blood pressure increases, diastolic blood pressure decreases, mean blood pressure decreases.

At the same time, the need for oxygen in the heart sharply increases; it cannot be used parenterally in order to avoid the development of microinfarctions.

Stimulation of β2-receptors leads to a decrease in the tone of the bronchi, blood vessels, uterus.

Indications for use:

- atriventricular block (sublingual tablets);

- bronchial asthma, pulmonary emphysema.

- to facilitate bronchoscopy and bronchography.

Side effects: tachycardia, arrhythmias, nausea, hand tremors.

Contraindications: ischemic heart disease, hypertension, severe atherosclerosis, hyperthyroidism, diabetes mellitus.

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

Choleretic drugs are drugs that activate liver function, increasing the secretion of bile.

1. Drugs that enhance the secretion or production of bile (choleretics, cholesecretics)

• Bile preparationsof animal origin, cholenzyme, allochol, decholin, hologon, liobil

• Herbal preparations cholosas, Liv-52, cholagol, olimetin, sandy immortelle flowers, flamin, corn silk extract

• Synthetic drugs oxafenamide (osalmide), cyclovalon (tsikvalone), hydroxymethylnicotinamide (nicodine)

2. Means that stimulate the excretion of bile

1.Cholekinetics: cholecystokinin, xylitol, sorbitol, magnesium sulfate, barberry preparations, tansy flowers, Karlovy Vary salt.

2. Cholespasmolytics: atropine, platifillin, belladonna tincture and extract, no-spa, mebeverin, olimetin, gimecromone.

Mechanism of action: Means increase the production of bile by hepatic cells. The mechanism of action of choleretics consists of several points:

• direct stimulation of the secretory function of the hepatic parenchyma;

• increased osmotic filtration of water and electrolytes into the bile capillaries;

• stimulation of receptors in the mucous membrane of the small intestine, which enhances bile formation.

HYDROCHOLERETICS

They increase the amount of bile due to the water component:

• the secretion of bile increases;

• the reabsorption of water and electrolytes in the gallbladder is limited. This leads to an increase in the colloidal stability of bile.

CHOLEKINETICS

Mechanism of action. They irritate the mucous membrane of the duodenum - cholecystokinin is released, which calls for contraction of the muscular wall of the gallbladder and relaxation of the sphincter of Oddi.

HOLESPASMOLYTICS.

They are used not only as cholespasmolytics, but ultimately they relieve spasm of the biliary tract, increasing the passage of bile. ...

Indications: Cholesecretics: chronic cholecystitis and cholangitis, chronic hepatitis, pancreatitis, flatulence, functional disorders of the gastrointestinal tract.

Cholekinetics: gallbladder atony with bile congestion and dyskinesia, chronic cholecystitis and chronic hepatitis.

Side effects: Allergic reaction, diarrhea.

Contraindications: Cholesecretics: acute hepatitis, cholangitis, cholecystitis, pancreatitis, peptic ulcer, jaundice.

Cholekinetics: in the acute phase of liver disease, in the presence of stones in the gallbladder, with exacerbations of hyperacid gastritis and peptic ulcer disease.

Comparative characteristics: Dehydrocholic acid (hologon) - causes a significant increase in the secretion of bile, at the same time has little effect on the secretion of cholesterol and phospholipids into bile.

The sodium salt of dehydrocholic acid (decholin) - the sodium salt of dehydrocholic acid - also stimulates the bile-forming function of the liver cells.

Allochol is an officinal film-coated tablet containing dry animal bile, dry garlic extract, dry nettle extract and activated charcoal.

Cholenzym is a preparation containing dry bile, powder of dried pancreas and mucous membrane of the small intestines of slaughter animals. Has a weak choleretic activity, but increases the content of cholates in bile. Cholenzyme improves the digestion of food in the intestine due to the content of trypsin and amylase in it.

Salbutamol - dilates the bronchi, there is no tachycardia, blood pressure does not change, the effect on the heart is insignificant. The main therapeutic effects are bronchodilatory and tocolytic (relax the uterus).

Terbutaline is a drug of medium duration of action (up to 4 - 6 hours). Available in aerosol, tablet and ampoule form. They are used for broncho-obstructive diseases, with the threat of termination of pregnancy due to increased uterine tone.