Clinical and pharmacological group: & nbsp

Diuretics

Angiotensin II receptor antagonists (AT1 subtype)

Included in the formulation
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  • АТХ:

    C.09.D.A.02   Eprosartan in combination with diuretics

    Pharmacodynamics:

    Combined antihypertensive.

    Hydrochlorothiazide

    The benzothiadiazepine derivative selectively blocks the transport system of sodium, potassium and chlorine ions, stopping their transport through the apical membrane into the cells of the epithelium of the thick segment of the ascending section of the Henle loop. The suppression of reabsorption of ions leads to their removal from the body. Simultaneously with ions of sodium, potassium and chlorine ions of calcium and magnesium are deduced. Hypocalcemia does not develop due to active reabsorption in the distal convoluted tubule of the loop of Henle.

    Effective with any fluctuations in acid-base balance, retains a diuretic effect, both with acidosis and with alkalosis.

    Eprosartan

    Blocking the conversion of angiotensin I in angiotensin II, resulting in the release of norepinephrine from the endings of sympathetic fibers, the vasoconstrictor effect, the secretion of aldosterone by the adrenal cortex, and the contentBradykinin by reducing its inactivation by the angiotensin-converting enzyme.

    Bradykinin stimulates B2-cinin receptors of the vascular endothelium, which leads to the rapid release of prostacyclin and other vasodilating substances that cause relaxation of smooth muscles.

    Reduces the overall peripheral resistance of blood vessels, without affecting the heart rate.

    Pharmacokinetics:

    Hydrochlorothiazide

    After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 2 hours. The connection with plasma proteins is 40%.

    The therapeutic effect develops 2 hours after ingestion and lasts for 8-12 hours. It penetrates the blood-brain and placental barrier, it is excreted in breast milk. Metabolism in the liver.

    T ½ is 6.4 h. Elimination by the kidneys, about 75% in unmodified form.

    Eprosartan

    After oral administration, up to 13% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1-2 hours. The connection with plasma proteins is 99%.

    Metabolism in the liver.

    T ½ eprosartan is 5-9 h. Elimination with feces and kidneys.

    Indications:

    It is used for the treatment of arterial hypertension. Used in the therapy of chronic heart failure.

    IX.I10-I15.I10   Essential [primary] hypertension

    IX.I10-I15.I15   Secondary Hypertension

    IX.I30-I52.I50.1   Left ventricular failure

    Contraindications:

    Severe renal and hepatic insufficiency, congenital angioedema or a history, patients on hemodialysis, pregnancy and lactation, age under 18, individual intolerance.

    Carefully:

    Bronchial asthma, ischemic heart disease, gout, psoriasis, systemic connective tissue diseases, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside, 1 (hydrochlorothiazide / eprosartan: 12.5 / 735.8 mg) tablet 1 time / day.

    The highest daily dose: 1 tablet of 12.5 mg of hydrochlorothiazide and 735.8 mg of eprosartan.

    The highest single dose: 1 tablet of 12.5 mg of hydrochlorothiazide and 735.8 mg of eprosartan.

    Side effects:

    Hydrochlorothiazide

    Central and peripheral nervous system: headache, dizziness, depression, sleep disorders, paresthesia.

    Respiratory system: pneumonitis, pulmonary edema.

    Hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia, hemolytic anemia.

    The cardiovascular system: orthostatic hypotension, rarely - arrhythmia.

    Musculoskeletal system: spasms of the calf muscles.

    Dermatological reactions: photosensitization, rash, rarely - toxic epidermal necrolysis.

    Sense organs: visual impairment.

    Urinary system: glycosuria, hyperuricemia.

    Reproductive system: impotence.

    Eprosartan

    Central and peripheral nervous system: headache, dizziness, sleep disorders, paresthesia, confusion.

    Respiratory system: dry cough, shortness of breath, sinusitis, bronchospasm.

    Hemopoietic system: anemia, thrombocytopenia, agranulocytosis, pancytopenia.

    The cardiovascular system: arterial hypotension, tachycardia, rarely - pain in the chest, flushes of blood.

    Digestive system: glossitis, vomiting, diarrhea, constipation, rarely - hepatitis, cholestatic jaundice, pancreatitis.

    Musculoskeletal system: myalgia, cramps of the calf muscles.

    Dermatological reactions: a rash.

    Sense organs: a noise in the ears, a violation of taste perception, blurred vision.

    Urinary system: dysuria, rarely - acute renal failure.

    Reproductive system: erectile disfunction.

    Allergic reactions.

    Overdose:

    Pronounced decrease in blood pressure, electrolyte imbalance, bradycardia, cardiovascular shock, renal failure.

    Treatment: intravenous epinephrine, blood substitution solutions, hydrocortisone.

    Interaction:

    Hydrochlorothiazide

    Strengthens the effects of nondepolarizing muscle relaxants.

    Patients with diabetes mellitus when using hydrochlorothiazide require correction of doses of oral hypoglycemic agents and insulin preparations.

    Enhance the hypokalemic effect of glucocorticosteroids, adrenocorticotropic hormone, carbenoxolone, amphotericin, cardiac glycosides.

    Antichollerergic drugs increase the bioavailability of hydrochlorothiazide.

    With simultaneous use with lithium preparations, a paradoxical antidiuretic effect is possible.

    With simultaneous application with vitamin D and calcium preparations may develop hypercalcemia.

    With simultaneous use with cyclosporine, the risk of developing gout and hyperuricemia increases.

    Eprosartan

    Strengthens the hypoglycemic action of insulin and oral hypoglycemic drugs.

    Enhances the toxic effects of lithium preparations.

    Sodium chloride, non-steroidal anti-inflammatory drugs reduce the hypotensive effect of eprosartan.

    With simultaneous use with potassium-sparing diuretics (amiloride, triamterene, spironolactone), products with a high content of potassium, hyperkalemia develops.

    When used simultaneously with cytostatics, allopurinol, systemic glucocorticosteroids, procainamide, immunosuppressants, - increases the risk of developing leukopenia.

    With simultaneous use with drugs for general anesthesia and for local anesthesia, it is possible to develop arterial hypotension.

    Special instructions:

    Monitoring of blood pressure, composition of peripheral blood.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

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