Clinical and pharmacological group: & nbsp

Renin inhibitors

Angiotensin II receptor antagonists (AT1 subtype)

Included in the formulation
АТХ:

C.09.D.X.02   Aliskiren and valsartan

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.

Valsartan

Selective antagonist of angiotensin receptors II. Supplements the action of aliskiren: with an increase in the concentration of angiotensin II in the blood plasma after valsartan blockade of AT receptors1 stimulation of unblocked AT receptors occurs2, which regulate the action of AT receptors1.

The simultaneous simultaneous action on the renin-angiotensin system leads to a maximum and persistent decrease in blood pressure.

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.

Valsartan

After ingestion, up to 23% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 94-97%.

Therapeutic effect develops after the reception. Metabolism in the liver.

The elimination half-life is 9 hours. Elimination with feces (70%) and kidneys (30%).

Indications:

It is used to treat arterial hypertension, chronic heart failure.

IX.I10-I15.I15   Secondary Hypertension

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

IX.I10-I15.I11.0   Hypertensive (hypertensive) disease with predominant heart involvement with (congestive) heart failure

IX.I30-I52.I50.0   Congestive heart failure

Contraindications:

Severe renal failure, hereditary angioedema, shock, individual intolerance, children under 18 years of age.

Carefully:

Hypokalemia, hyponatremia, Renovascular hypertension, elderly age.

Pregnancy and lactation:

Recommendations for FDA - Category C.Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside, regardless of the time of ingestion, 1 tablet once a day daily (1 tablet 150/160 mg). In the absence of a therapeutic effect, it is possible to increase the dose to the maximum: 1 tablet (300/320 mg) 2-4 weeks after the start of treatment.

The highest daily dose: 300/320 mg.

The highest single dose: 300/320 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.

Valsartan

Central and peripheral nervous system: headache, dizziness, general weakness.

Hemopoietic system: reduction of hematocrit and hemoglobin, neutropenia.

The cardiovascular system: postural hypotension, hyperkalemia, postural dizziness.

Digestive system: nausea, diarrhea, hyperbilirubinemia.

Dermatological reactions: itching, rash, vasculitis.

Allergic reactions.

Overdose:

Arterial hypotension.

Treatment is symptomatic.

Interaction:

When used simultaneously with potassium-sparing diuretics (spironolactone, amiloride, triamterene), salt substitutes containing potassium and potassium preparations may increase the potassium content in the blood serum.

Special instructions:

Care should be taken when treating vehicles while driving vehicles.

Instructions
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