Indications for use:

∙ mental retardation, cerebral palsy, mental retardation and / or psychomotor development,

prevention of cerebral disorders in newborns from high-risk groups;

∙ atherosclerosis of cerebral vessels, discirculatory and hypertensive encephalopathy,

cerebral stroke and its consequences;

∙ mnestic disorders in alcoholism, epilepsy, neuroinfections;

∙ post-traumatic acute and chronic brain damage;

∙ asthenia and depression in the elderly, senile depression;

∙ neurotic conditions, severe stress with overwork, impaired mental and social adaptation;

∙ dizziness;

∙ coma of vascular, toxic or traumatic etiology;

∙ correction of tics in patients with Tourette's syndrome and attenuation of attention deficit hyperactivity disorder (GUANFACIN in small doses);

∙ Parkinson's disease, moderate cognitive impairment, including those associated with age-related cognitive dysfunction and dyscirculatory encephalopathy, age-related sensorineural hearing loss, restless legs syndrome (PIRIBEDIL);

∙ prevention of motion sickness in children (FENIBUT, AMINALON);

∙ stuttering, tics, enuresis in children (FENEBUT);

∙ Parkinson's disease (PIRIBEDIL).

Side effects:

∙ allergic reactions;

∙ headache, dizziness, weakness;

∙ dyspeptic disorders;

∙ irritability, anxiety, anxiety, insomnia, anxiety, (except for GUANFACIN, Phenibut, Cinnarizin, FESAM);

∙ PIRIBEDIL: orthostatic hypotension, flatulence, hallucinations (in predisposed persons);

∙ GUANFACIN: dry mouth, drowsiness, impotence, depression; sudden withdrawal of the drug can cause a hypertensive crisis;

∙ AMINALON: feeling of heat, fluctuations in blood pressure;

∙ PHENIBUT: drowsiness;

∙ GINKGO BILOBA LEAVE EXTRACT: stomatitis;

∙ PIRACETS: exacerbation of angina pectoris in the elderly, weight loss, aggressive behavior, fluctuations in blood pressure;

∙ PYRIDITOL: rarely - alopecia, arthralgia, thrombocytopenia, agranulocytosis, muscle weakness, paresthesia, taste disturbance, anorexia, diarrhea;

∙ ACEFEN: increased delirium, hallucinations, anxiety in mental patients, provocation of arrhythmias (ACEFEN is cleaved to form n-chlorophenoxyacetic acid and dimethylamineethanol, which acts as a choline antagonist in the synthesis of acetylcholine);

∙ CEREBROLYSIN: fever, hot flashes, confusion, hallucinations (in patients with dementia);

∙ CINNARIZIN: drowsiness, dry mouth, increased sweating, arterial hypotension, redness of the face and skin of the upper body, edema of the lower extremities; the appearance (aggravation) of extrapyramidal disorders in certain elderly patients;

∙ NICERGOLIN: discomfort in the heart or abdomen, orthostatic hypotension, impaired ejaculation, sweating;

∙ KAVINTON, VINKAMIN: arterial hypotension, tachycardia, extrasystole, thrombophlebitis at the injection site, heartburn, dry mouth, skin flushing.

∙ PANTOGAM: ∙ a syndrome similar to Reye's syndrome (encephalopathy and fatty degeneration of internal organs), due to impaired metabolism of carnitine;

∙ FESAM: dry mouth, weight gain, drowsiness, extrapyramidal disorders.

Contraindications

∙ persistent and significant disorders of mental activity and intelligence;

∙ PIRACETS: acute renal failure, diabetes mellitus (granules), childhood (up to 1 year);

∙ PHENIBUT and PANTOGAM: pregnancy and breastfeeding;

∙ PANTOGAM and PICAMILON: acute and chronic kidney disease;

∙ PYRIDITOL and ACEPHENE: mental agitation, epilepsy, increased convulsive readiness, neuroinfections, myasthenia gravis.

Comparative evaluation:they do not have a pronounced psychostimulating or sedative effect. At the same time, they stimulate the transfer of information between the cerebral hemispheres, improve energy and plastic processes in the brain tissue. All nootropic drugs are characterized by low toxicity and good tolerance by patients of different age groups.

3. Antihypertensive drugs of peripheral neurotropic action. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

ganglion blockers (benzohexonium, pentamine, arfonade, hygronium);

sympatholytics (octadine, reserpine);

α-blockers (phentolamine, tropafen, prazosin);

β-blockers (anaprilin, talinolol, metoprolol, atenolol);

α-β-blockers (labetalol).

Ganglion blockers- effects: ↓ VD, return of blood to the heart. For the treatment of hypertension, they are rarely used, because have many side effects (block both sympathetic and parasympathetic ganglia) - orthostatic collapse, constipation, intestinal obstruction, ↓ bladder tone, impaired accommodation, dry mouth, addiction. It is used for controlled hypotension during operations, with pulmonary and cerebral edema.

Sympatholytics (octadine)- mechanism: ↓ transport to oxoplasm and granule, ↓ release of norepinephrine from the depot (the depot is depleted). When administered intravenously, the action is in 2 phases: ↑ BP, then ↓ BP due to depot depletion (2-3 days). Effects: ↑ vein tone, ↓ strength and heart rate, does not pass through the blood-brain barrier. Side effects: orthostatic collapse, drowsiness, weakness, varicose veins in the extremities, diarrhea. Aid measures: atropine, bandaging of limbs, inject lying down. Octadine is more effective than reserpine.

Adrenoblockers:phentolamine - vasodilation, ↓ blood pressure, especially diastolic. (orthostatic collapse). With hypertensive crises. Quickly addictive. Side effects: tachycardia, nausea, diarrhea.

Anaprilin - mechanism ↓ blood pressure, ↓ release of renin by juxtaglomerular kidney cells, ↑ activity of the paraventricular depressor nucleus of the hypothalamus, excite α-receptors of the medulla oblongata. Gradual ↓ BP, maximum for 2-3 weeks. ↓ strength and heart rate. Side effects: narrowing of the bronchi. Used for hypertension.

Labetalol - ↓ TPR and BP, does not affect cardiac output, ↓ HR and renin production.

Prescribed for hypertension. Side effects: dizziness, orthostatic collapse. Prazosin - acts postsynaptically, there is no tachycardia, ↓ BP and OPSS, does not affect renin. The action develops after 4 hours and lasts 10 hours. With hypertension. Side effects: headache, palpitations, drowsiness, edema, orthostatic collapse.

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).

Contraindications: Kanamycin is contraindicated in inflammation of the auditory nerve, impaired liver and kidney function (with the exception of tuberculous lesions).

Individual intolerance to the drug.

Epilepsy.

Severe psychosis.

Tendency to seizures.

History of poliomyelitis.

History of toxic hepatitis due to taking GINK drugs.

Acute hepatic and renal failure.

An absolute contraindication to the appointment of streptomycin is the lack of sensitivity of Koch's bacilli to it.

Side effect:Dizziness, discomfort in the region of the heart, tinnitus, headache (often due to a decrease in blood pressure, mainly systolic). Anaphylactic shock, vestibular disorders, hearing loss, deafness, drug fever, skin rash, contact dermatitis, muscle weakness and joint pain, dizziness, tinnitus, palpitations and pain in the region of the heart. In severe cases, paresthesias, insomnia, memory loss, muscle twitching, polyneuritis, ataxia, convulsions occur (due to the developing deficiency of pyridoxine and thiamine chloride). Changes in blood are possible: agranulocytosis, eosinophilia. Convulsive states, lesions of the optic nerve and polyneuritis are also possible. Endocrine system disorders: gynecomastia in men, dysmenorrhea in women, "cushingoid", hyperglycemia.

Ticket 16

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.

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 effect, 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.