Included in the formulation
АТХ:C.09.C.A.03 Valsartan
Pharmacodynamics:Combined antihypertensive.
Sakubitryl
It suppresses the activity of non-uridine, which cleaves natriuretic peptides. As a result, activation of membrane-bound receptors conjugated with guanylate cyclase occurs, which increases the concentration of cyclic guanosine monophosphate (cGMP). Consequently, natriuresis increases, the rate of glomerular filtration and renal blood flow.
Valsartan
Selective antagonist of angiotensin receptors I. Supplements the action of sakubitrila: with an increase in the concentration of angiotensin II in blood plasma after valsartan blockade of AT receptors1 stimulation of unblocked AT receptors occurs2, which regulate the action of AT receptors1. As a result, vasoconstriction and aldosterone secretion are suppressed. Reduces myocardial hypertrophy, does not affect the concentration of triglycerides, glucose, total cholesterol and uric acid.
The combined effects of sakubitrile and valsartan lead to a decrease in sympathetic activity, has antifibrotic and antihypertrophic effects.
Pharmacokinetics:Sakubitryl
After oral administration, fasted to 60% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 3 hours. The connection with plasma proteins is 94%.
Metabolism in the liver to the active metabolite LBQ657.
The half-life of sacubitryl is 1.5 hours, the metabolite LBQ657 - 11.5 hours. Elimination by the kidneys and with feces, mostly in the form of a metabolite LBQ657.
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%.
Metabolism in the liver.
The elimination half-life is 9 hours. Elimination with feces (70%) and kidneys (30%).
Indications:It is used to treat chronic heart failure.
IX.I30-I52.I50.0 Congestive heart failure
IX.I30-I52.I50.1 Left ventricular failure
Contraindications:Severe renal failure, hereditary angioedema, shock, age under 18, pregnancy and lactation, individual intolerance.
Carefully:Hypokalemia, hyponatremia, Renovascular hypertension, renal failure, elderly age.
Pregnancy and lactation:Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside, 80 mg once a day. With insufficient effectiveness, an increase in the dose to 160 mg per day is possible.
The highest daily dose: 320 mg.
The highest single dose: 160 mg.
Side effects:Central and peripheral nervous system: dizziness, headache, general weakness.
Hemopoietic system: reduction of hematocrit and hemoglobin, neutropenia.
Respiratory system: cough.
The cardiovascular system: postural hypotension, hyperkalemia, postural dizziness.
Digestive system: nausea, diarrhea, hyperbilirubinemia.
Dermatological reactions: itching, rash, vasculitis.
Sense organs: vertigo.
urinary system: impaired renal function.
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:During treatment, patients need to use reliable contraceptive methods.
When taking the drug is not recommended driving and working with moving vehicles.