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

RESERPIN penetrates well through the BBB, causing depression of the central nervous system. Therefore, it can cause lethargy, drowsiness, depression, decreased potency, with prolonged use - drug parkinsonism

OCTADINE does not affect the central nervous system. Its hypotensive effect is more pronounced, orthostatic collapse is possible (after taking the drug, it is necessary to be in a horizontal position for 1.5 - 2 hours)

Indications: Both drugs are used for the systematic treatment of arterial hypertension.

Side effects:

Common to OCTADINE and RESERPINE:

• dizziness

• general weakness

• bradycardia

• swelling of the nasal mucosa

• increased secretion of the digestive glands (possible ulcerogenic effect)

• increased gastrointestinal motility (diarrhea is possible)

• sodium and water retention (it is recommended to combine with diuretics)

Additionally: RESERPIN - depression of the central nervous system

OCTADINE - orthostatic hypotension

• Contraindications: Severe organic cardiovascular diseases with symptoms of decompensation, severe bradycardia, pronounced atherosclerosis, gastric ulcer and duodenal ulcer, renal failure, lactation period

• Do not prescribe drugs (hypertensive crisis is possible):

1. With pheochromocytoma

2. Together with MAO inhibitors

3. Together with tricyclic antidepressants

Comparative characteristics: ORNID (bretilium tosylate)

• The mechanism of action is associated with the stabilization of the presynaptic membrane and blocking the release of the mediator into the synaptic cleft. The hypotensive effect of the drug is not sufficiently pronounced for clinical use, but the antiarrhythmic effect is clearly manifested, mainly in ventricular arrhythmias (especially those resistant to other drugs)

• Side effects: nephrotoxicity, orthostatic hypotension, fever, weakness, swelling of the nasal mucosa

• Contraindications: hypotension, acute cerebrovascular accident, severe renal failure

METHYLDOPA (aldomet, dopegit)

The drug penetrates well into the central nervous system and, integrating into the synthesis chain of the mediator, promotes the formation of methylnorepinephrine, which stimulates (and is stronger than the true mediator) 2-adrenergic receptors of inhibitory neurons in the central nervous system

This leads to an increase in inhibitory effects on sympathetic impulses to the heart and blood vessels (the action is similar to CLOFELINE, see), as a result of which the vessels expand, the total peripheral vascular resistance decreases and bradycardia develops

Causes sedation Orthostatic hypotension is rare

• It is used for arterial hypertension

• Side effects: general weakness, dyspeptic disorders, redness of the upper half of the trunk (due to vasodilation), reversible leukopenia and thrombocytopenia, hemolytic anemia, liver dysfunction with cholestasis and jaundice (control blood and liver function!). Retention of sodium and water (must be combined with diuretics!)

• Contraindications: diseases of the blood system (leukopenia, agranulocytosis, thrombocytopenia, hypo- and aplastic anemias), liver (hepatitis, cirrhosis), pheochromocytoma

3. Preparations of adrenal cortex hormones (glucocorticoids, mineralocorticoids). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Classification:

Mineralocorticoids: Aldosterone, 11-Deoxycorticosterone, 11-Desaxi-17-hydroxycorticosterone

Glucocorticoids: I. Preparations of natural hormones and their esters: CORTISONE, HYDROCORTISONE

II. Synthetic drugs: 1) Inhalation:

TRIAMCINOLONE (azmacort)

FLUNISOLID (ingacort)

BECLOMETAZONE (beclomet, becotide)

BUDESONID (pulmicort, benacort)

FLUTICAZONE (flixotide)

2) System:

Prednisolone (decortin, medopred)

METHYLPEDNIZOLONE (metipred)

BETAMETAZONE (celeston)

DEXAMETHAZONE (dexona, dexazone)

TRIAMCINOLON (berlikort, kenalog)

3) Local action:

FLUMETAZONE PIVALATE ("lokakorten" "lorinden")

FLUOCINOLONE ACETONIDE ("sinaflan", "sinalar")

BUDESONID (apulein)

HALOMETAZONE (sicorten)

BETAMETAZONE ("diprolene", "celestoderm")

Mechanism of action: Mineralocorticoids: Increase the reabsorption of sodium and water, at the same time increase the secretion of potassium and magnesium ions, calcium in the renal tubules.

GLUCOCORTICOIDS:

1. Anti-inflammatory

2. Antiallergic and immunosuppressive

3. Anti-shock

Anti-inflammatory:

1. Suppression of the production of prostaglandins, leukotrienes and platelet activating factor due to inhibition of phospholipase A2.

2. Inhibition of hyaluronidase activity.

3. Decreased permeability and increased resistance of capillary walls, cell membranes and subcellular structures.

4. Delayed development of connective tissue.

5. Decrease in the number of leukocytes in the area of ​​inflammation.

6. Suppression of the activity of macrophages and fibroblasts.

7. Inhibition of cyclooxygenase-2 activity

Antiallergic:

1. Decrease in the activity of T- and B-lymphocytes.

2. Inhibition of antibody synthesis.

3. Suppression of the release of histamine, serotonin, acetylcholine.

4. Increased activity of histaminase and cholinesterase.

5. Slowdown in the development of lymphoid tissue.

6. Suppression of production of interleukins and other cytokines.

Anti-shock:

1. Potentiation of the action of vasopressor substances (angiotensin, adrenaline, norepinephrine) and an increase in blood pressure.

2. Improving the work of the heart.

Indications: Mineralocorticoids:

1. Addison's disease (chronic adrenal insufficiency).

2. Hypotension with orthostatic disorders.

3. Myasthenia gravis.

4. Adynamia.

5. Hypochloremia.

Glucocorticoids: Inflammatory diseases of an infectious and allergic nature (rheumatism, systemic lupus erythematosus, collagenoses, rheumatoid arthritis, generalized dermatitis, eczema, neurodermatitis, psoriasis, etc.).

2. Severe infectious diseases occurring with high fever and intoxication (diffuse peritonitis, meningitis, typhoid fever).

3. Severe allergic and toxic-allergic conditions (anaphylactic shock, reaction to a blood transfusion of another group, acute hemolytic anemia, bronchial asthma, etc.).

4. Shock states.

5. Malignant diseases of the hematopoietic organs (leukemia, lymphogranuloma, etc.).

Side effects: Mineralocorticods: 1. Edema.

2. Arterial hypertension.

3. Hypokalemia (impaired heart function, arrhythmias).

4. Allergic reactions.

5. Development or worsening of heart failure.

Glucocorticoids: Withdrawal syndrome and acute adrenal insufficiency (with abrupt withdrawal of drugs).

2. Itsenko-Cushing's symptom complex (edema, arterial hypertension, obesity, "moon face", "bovine hump").

3. Hyperglycemia (steroidal diabetes).

4. Osteoporosis, multiple caries.

5. Slowing down the regeneration processes (slowing down the healing of wounds, fractures).

6. Decrease in resistance to infections, exacerbation of a dormant infection.

7. Violation of the menstrual cycle, impotence.

8. Ulceration of the gastric mucosa, exacerbation of peptic ulcer disease.

Contraindications: Mineralocorticoids: 1. Acute and chronic heart failure.

2. Arterial hypertension.

3. Atherosclerosis.

4. Cirrhosis of the liver.

5. Jade.

Glucocorticoids: 1. Severe hypertension.

2. Itsenko-Cushing's disease.

3. Pregnancy.

4. Insufficiency of blood circulation of the III degree.

5. Acute endocarditis.

6. Psychoses.

7. Osteoporosis.

8. Peptic ulcer of the stomach and duodenum.

9. Active forms of tuberculosis