Aliskiren + Hydrochlorothiazide (Aliskirenum + Hydrochlorothiazidum)

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

Renin inhibitors

Diuretics

Included in the formulation
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    Novartis Pharma AG     Switzerland
    • АТХ:

    C.09.X.A.52   Aliskiren and hydrochlorothiazide

    Pharmacodynamics:

    Combined antihypertensive drug.

    Aliskiren

    Selective inhibitor of renin of non-peptide structure, blocks the conversion of angiotensin into angiotensin I, reducing the plasma renin level, angiotensin I and angiotensin II.

    Renin is excreted by the kidneys with a decrease in renal perfusion and the volume of circulating blood. Once in the bloodstream, renin cleaves angiotensin to an inactive decapeptide of angiotensin I, which, in turn, with the help of an angiotensin-converting enzyme is converted into active octapeptide angiotensin II, which causes vasoconstriction and stimulates the release of adrenal catecholamines from the adrenal medulla, also enhances the reabsorption of sodium and aldosterone ions, which increases blood pressure. By increasing the level of angiotensin II there is an expression of markers and mediators of inflammation and fibrosis of the organ. In addition, angiotensin II inhibits the release of renin, adversely affecting the system. As a result, increased activity of renin leads to an increased risk of cardiovascular complications.

    The action of inhibitors of renin leads to a compensatory increase in the concentration of renin in the blood plasma. The action of aliskiren neutralizes the feedback effect, which leads to a persistent decrease in plasma renin activity.

    Hydrochlorothiazide

    Has hypotensive and diuretic effect. Displays sodium and stores potassium in the blood plasma. Diuretic effect begins 2 hours after taking the drug. The maximum effect is noted after 4 hours and lasts for 6-12 hours. At the initial normal arterial pressure, there is no decrease.

    Pharmacokinetics:

    Aliskiren

    After oral ingestion, up to 2.5% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-3 hours. The equilibrium concentration in blood plasma is reached within 5-7 days after the start of the administration once a day, the equilibrium level is approximately 2 times higher than at the initial dose. The connection with plasma proteins is up to 50%.

    Metabolism in the liver.

    The half-life is 40 hours. Elimination with feces, mostly unchanged.

    Hydrochlorothiazide

    The highest concentration of the drug in the blood plasma is observed 3-4 hours after oral administration.

    Bioavailability of 60-80%, communication with blood plasma proteins - up to 70-75%. Metabolism in the liver.

    The half-life is 6-9 hours.

    Elimination by the kidneys (99%), decreased in chronic renal failure and in the elderly.

    Indications:

    It is used for the treatment of arterial hypertension.

    ICD-10

    IX.I10-I15.I15   Secondary Hypertension

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

    Contraindications:

    Aliskiren

    Anuria, severe renal and hepatic insufficiency, hereditary angioedema, shock, individual intolerance, children under 18 years of age.

    Hydrochlorothiazide

    Hyperkalemia (with a content of potassium ions in the blood plasma of 5.5 kV / L and more), decompensated diabetes mellitus, Addison's disease, gout, individual intolerance.

    Carefully:

    Chronic renal failure, hypokalemia, hyponatremia, Renovascular hypertension, advanced age.

    Pregnancy and lactation:

    Recommendations for FDA - category C in the I trimester, category D in the 2nd and 3rd trimesters. It enters the breast milk, reduces lactation: it is recommended to stop breastfeeding during treatment.

    Dosing and Administration:

    Inside, 1 tablet (aliskiren / hydrochlorothiazide at a dose of 150 / 12.5 mg, 150/25 mg, 300 / 12.5 mg or maximum 300/25 mg) once a day.

    The highest daily dose: 300/25 mg.

    The highest single dose: 300/25 mg.

    Side effects:

    Aliskiren

    Central and peripheral nervous system: dizziness.

    The cardiovascular system: hypotension, peripheral edema.

    Digestive system: diarrhea.

    Dermatological reactions: hyperemia, toxic epidermal necrolysis, Stevens-Johnson syndrome, skin itching.

    urinary system: impaired renal function.

    Allergic reactions.

    Hydrochlorothiazide

    Central and peripheral nervous system: a change in mood and psyche, headache, dizziness, paresthesia.

    Respiratory system: respiratory distress syndrome, pneumonitis.

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

    The cardiovascular system: arrhythmia, vasculitis.

    Digestive system: pancreatitis, cholecystitis, constipation, anorexia,

    Musculoskeletal system: myalgia, convulsions.

    Dermatological reactions: photosensitization.

    Sense organs: transient visual impairment.

    urinary system: interstitial nephrosis.

    Reproductive system: decreased potency.

    Allergic reactions.

    Overdose:

    Aliskiren

    Arterial hypotension.

    Treatment is symptomatic.

    Hydrochlorothiazide

    Dehydration, pronounced electrolyte disorders, lowering blood pressure, tachycardia, confusion, lethargy, dry mouth, muscle weakness, drowsiness, hypotension, oliguria, shock.

    Treatment is symptomatic.

    Interaction:

    Aliskiren

    Clinically significant interactions are not described.

    Hydrochlorothiazide

    Potentiates the effect of antihypertensive drugs.

    Nonsteroidal anti-inflammatory drugs weaken the hypotensive and diuretic effect.

    Increases the toxicity of cardiac glycosides.

    Reduces the clearance of amantadine, increasing its toxicity.

    Reduces the level of iodine in the plasma.

    Increases the level of bilirubin.

    With the simultaneous use of barbiturates, narcotic analgesics, ethanol, the risk of orthostatic hypotension increases.

    Special instructions:

    At the beginning of treatment, it is not recommended to drive vehicles and work with moving mechanisms.

    Instructions
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