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Description
Tablets Jupiro in a film cover. The action of the drug Yuperio is mediated by a new mechanism, namely, the simultaneous suppression of the activity of neprilysin (neutral endopeptidase (neutral endopeptidase, NEP)) with LBQ657 (the active metabolite of sacubitrile) and blockade of receptors for angiotensin II type 1 (AT1) valsartan and that is a virus that is an antiviral receptor that is an antiviral receptor blockade of type 1 angiotensin II (AT1), which is an antiviral receptor that is an anubitine inhibitor. II (APA II). The mutually complementary beneficial effects of sacubitrile and valsartan on the cardiovascular system and kidneys in patients with heart failure are due to an increase in the number of peptides cleaved by neprilisin (such as natriuretic peptides (NP)), which is mediated by LBQ657, while the negative effects of angiotensin are suppressed by valsartan Ii. NPs activate membrane-bound receptors coupled with guanylyl cyclase, which leads to an increase in the concentration of cyclic guanosine monophosphate (cGMP), which causes symptoms of vasodilation, an increase in natriuresis and diuresis, an increase in glomerular filtration rate and renal blood flow, suppression of renin and aldosterone, and suppression of the renal and aldosterone, and a reduction of the symptomatology of the renal and aldosterone; and antifibrotic action. Valsartan, selectively blocking the AT1 receptor, suppresses the negative effects of angiotensin II on the cardiovascular system and kidneys, and also blocks angiotensin II-dependent release of aldosterone. This prevents the persistent activation of the renin-angiotensin-aldosterone system (RAAS), which causes vasoconstriction, sodium and water retention by the kidneys, growth activation and cell proliferation, as well as the subsequent rearrangement of the cardiovascular system, which aggravates impairments in its functioning.
Active ingredients
Valsartan + Sakubitril
Release form
Pills
Composition
Active ingredient: sacubitrile and valsartan hydrate complex of sodium salts - 113.103 mg (in terms of anhydrous acid form 100 mg, equivalent to 48.6 mg of sacubitrile and 51.4 mg of valsartan),
Indications
Chronic heart failure (NYHA Class II-IV) in patients with systolic dysfunction to reduce the risk of cardiovascular mortality and hospitalization for heart failure.
Precautionary measures
Caution must be exercised when using Yuperio in patients with severely impaired renal function (eGFR <30 ml / min / 1.73 m2 of body surface area), incl. in patients on hemodialysis or undergoing hemodialysis (eGFR <15 ml / min / 1.73 m2 of body surface area) due to the lack of safety data in patients of this category, patients with bilateral renal artery stenosis, which may cause be caused by diuretic therapy, low salt diet, diarrhea or vomiting, as well as in patients taking drugs that can increase the content of potassium in the blood serum (for example, potassium-saving diuretics, potassium drugs). Caution should be exercised with the simultaneous use of the drug with statins, inhibitors of phosphodiesterase type 5. Care should be taken when using the drug in patients with angioedema in the history of the drug due to the lack of data on the use of the drug in patients in this category. Patients of the Negroid race may be more at risk for angioedema. If you have one of these diseases, be sure to consult with your doctor before taking the drug.
Use during pregnancy and lactation
Contraindicated in pregnancy, pregnancy planning and during breastfeeding.
Dosage and administration
The time of taking the drug Juperio does not depend on the time of eating. The target (maximum daily) dose of the drug Juperio is 200 mg (102.8 mg + 97.2 mg) 2 times a day. The recommended initial dose of Yuperio is 100 mg (51.4 mg + 48.6 mg) 2 times a day. In patients who have not previously received ACE or APA II inhibitors, or who received these drugs in low doses, they should begin therapy with Uperio. at a dose of 50 mg (25.7 mg + 24.3 mg) 2 times a day with a slow increase in dose (doubling the daily dose 1 time in 3-4 weeks). Depending on tolerability, the dose of Yuperio should be doubled every 2 - 4 weeks until reaching the target (maximum daily) dose of 200 mg (102.8 mg + 97.2 mg) 2 times a day The use of the drug Yuperio is possible not earlier than 36 hours after discontinuation of the ACE inhibitor, as in the case of simultaneous use, angioedema can occur. Since APA II contains valsartan, it should not be used simultaneously with another drug. which includes ARA II. If patients have problems with tolerability of the drug Juperio (clinically pronounced decrease in blood pressure,hyperkalemia, impaired renal function), should consider the question of a temporary dose reduction or dose adjustment of concomitant medications.
Side effects
Identified adverse events (AEs) corresponded to the pharmacological characteristics of the drug Juperio and associated diseases that are present in patients. The most common AEs were a pronounced decrease in blood pressure, hyperkalemia, and impaired renal function, caused by dose adjustment of the drug Uperio or discontinuation of therapy. The frequency of AE was not dependent on the gender, age, or race of the patients. AEs are listed in accordance with the system-organ class of the medical dictionary for the regulatory activities of MedDRA. Within each system-organ class, NAs are distributed by frequency of occurrence in order of decreasing importance. The following criteria were used to estimate the frequency: very often (? 1/10), often (from? 1/100 to <1/10), infrequently (from? 1 / 1,000 to <1/100), rarely (from? 1 / 10,000 to <1/1000), very rarely (<1/10000), including individual messages. Metabolic and nutritional disorders: very often - hyperkalemia, often - hypokalemia. Nervous system disorders: often - dizziness, headache, infrequently - orthostatic dizziness. Disturbances from an organ of hearing and labyrinth disturbances: often - vertigo. Violations of the vessels: very often - marked reduction in blood pressure, often - fainting, orthostatic hypotension. Disturbances of the respiratory system, chest and mediastinal organs: often - cough. Disorders of the gastrointestinal tract: often - diarrhea, nausea. Violations of the skin and subcutaneous tissues: infrequently - angioedema. Disorders of the kidneys and urinary tract: very often - impaired renal function, often - renal failure (including acute renal failure). General disorders and disorders at the injection site: often - increased fatigue, asthenia. If any of the side effects indicated in the instruction are aggravated, or you have noticed any other side effects that are not indicated in the instruction, inform your doctor.
Interaction with other drugs
Contraindicated drug interactions ACE inhibitors The drug Yuperio is contraindicated for use simultaneously with ACE inhibitors, since the suppression of neprilysin simultaneously with the use of an ACE inhibitor may increase the risk of developing angioedema.The use of the drug Yuperio can be possible not earlier than 36 hours after discontinuation of the ACE inhibitor. The use of an ACE inhibitor is possible no earlier than 36 hours after the last dose of the drug, Juperio. Aliskiren In patients with diabetes mellitus and in patients with impaired renal function (eGFR <60 ml / min / 1.73 m2 of body surface area), Uperio should not be used simultaneously with aliskiren. Not recommended drug interactions Angiotensin receptor antagonists Since one of the active ingredients of the drug is an antagonist of angiotensin II receptors, simultaneous use with another drug containing ARA II is not recommended. Drug interactions that need to be considered HMG-CoA reductase inhibitors (statins) Research data show that sacubitrile inhibits the activity of OATP1B1 and OATP1B3 transporters. Uperio may increase the systemic exposure of OATP1B1 and OATP1B3 substrates, such as statins. In patients who received the drug Yuperio simultaneously with atorvastatin, the maximum plasma concentration (Cmax) of atorvastatin and its metabolites increased up to 2 times, and AUC - up to 1.3 times. For this reason, Yuperio should be used with caution at the same time as statins. Sildenafil In patients with a pronounced increase in blood pressure, receiving the drug Yuperio (before reaching the equilibrium concentration), a single use of sildenafil increased the antihypertensive effect compared with the use of the drug Yuperio in monotherapy. For this reason, use of sildenafil or another type 5 phosphodiesterase inhibitor should be used in patients receiving Yuperio. Estimated drug interactions that need to be taken into account In patients receiving the drug Yuperio simultaneously with these drugs, it is recommended to regularly monitor the content of potassium in the blood serum.Nonsteroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 inhibitors (COX-2 inhibitors) Use of Uperio at the same time as NSAIDs in patients over 65 years of age, in patients with hypovolemia (including patients receiving diuretics) and in patients with impaired function kidney problems may increase the risk of kidney function. In patients receiving the drug Yuperio simultaneously with NSAIDs, when prescribing such a treatment regimen and in case of its change, it is recommended to monitor renal function. Lithium Drugs The possibility of drug interaction between the drug Uperio and lithium drugs have not been studied. With the simultaneous use of lithium preparations with ACE and APA II inhibitors, there was a reversible increase in the concentration of lithium in the blood serum and an increase, in this connection, toxic manifestations. In patients receiving the drug Yuperio with lithium preparations, it is recommended to carefully monitor the lithium content in the serum. In the case of additional use of a diuretic drug, the risk of the toxic effect of lithium may increase. Carrier proteins The active metabolite of sacubitrile (LBQ657) and valsartan are substrates of carrier proteins OATP1B1, OATP1B3 and OAT3, valsartan is also a substrate of carrier protein MRP2. In patients receiving Yuperio simultaneously with inhibitors of OATP1B1, OATP1B3, OAT3 (for example, rifampicin and cyclosporin) or MPR2 (for example, ritonavir), systemic exposure to LBQ657 or valsartan, respectively, may increase. At the beginning and at the time of completion of the joint use of the drug Juperio and this group of drugs requires caution. Lack of significant drug interactions In the case of the use of the drug Yuperio in combination with furosemide, digoxin, warfarin, hydrochlorothiazide, amlodipine, metformin, omeprazole, carvedilol, nitroglycerin intravenously (iv) or the combined preparation of levonorgestrel and ethinylestradiol, you should not have a wary of a wedite or ethynestradiol. No interactions with atenolol, indomethacin, glibenclamide (glyburide) or cimetidine when combined with the drug Uperio is not expected. Interactions with isoenzymes of the cytochrome P450 system. Existing studies demonstrate that the probability of drug interactions mediated by cytochrome CYP450 isoenzymes is small, since the complex of active substances is metabolized to a small extent with the participation of CYP450 isoenzymes.The complex of active ingredients of the drug Yuperio is not an inhibitor or inducer of CYP450 isoenzymes.