Hydrochlorothiazide + Olmesartan medoxomil (Hydrochlorothiazidum + Olmesartanum medoxomilum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Diuretics

Angiotensin II receptor antagonists (AT1 subtype)

Included in the formulation
  • Cardosal® Plus
    pills inwards 
    BERLIN-PHARMA, CJSC     Russia
    • АТХ:

    C.09.D.A   Angiotensin II antagonists in combination with diuretics

    C.09.D.A.08   Olmesartan medoxomil 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 in both acidosis and alkalosis.

    Olmesartan medoxomil

    Blocking the conversion of angiotensin I in angiotensin II, resulting in a decrease in the release of norepinephrine from the endings of sympathetic fibers, a vasoconstrictor effect,secretion of aldosterone by the adrenal cortex and the content of bradykinin is increased due to a decrease in 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 the blood plasma is reached after 2 hours. The connection with plasma proteins is 40%.

    The therapeutic effect develops 2 hours after admission and lasts for 8-12 hours. Penetrates through the blood-brain and placental barrier, excreted in breast milk. Metabolism in the liver.

    The elimination half-life is 6.4 hours. Elimination by the kidneys, about 75% in unmodified form.

    Olmesartan medoxomil

    Prodrug. After oral administration, fasting to 25.5% is absorbed in the gastrointestinal tract. Here it turns into an active metabolite olmesartan.The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 99.7%.

    Metabolism in the liver.

    The half-life of olmesartan is 10-15 hours. Elimination with feces (60%) and kidneys (40%).

    Indications:

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

    ICD-10

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

    IX.I10-I15.I15   Secondary Hypertension

    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 tablet (hydrochlorothiazide / olmesartan medoxomil: 12.5 / 20 mg or 25/20 mg) 1 time per day.

    The highest daily dose: 1 tablet of 12.5 mg of hydrochlorothiazide and 20 mg of olmesartan medoxomil.

    The highest single dose: 1 tablet of 25 mg hydrochlorothiazide and 20 mg of olmesartan medoxomil.

    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.

    Olmesartan medoxomil

    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,tides 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 requires a correction of doses of oral hypoglycemic agents and insulin preparations.

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

    Anticholinergic 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.

    Olmesartan medoxomil

    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 olmesartan medoxomil.

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

    When used simultaneously with cytostatics, allopurinol, systemic glucocorticosteroids, procainamide, immunosuppressants increase 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.

    Instructions
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