Buy Uperio pills 50mg (25.7mg + 24.3mg) 28 pcs

Valsartan, Sakubitril

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Available since: 2019-09-19

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Clinical Pharmacology

The action of the drug Uperio 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 is a form of an antivitevative of an antivirus, which is an antifacting receptor blockade. 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 associated with guanylyl cyclase, which leads to an increase in the concentration of cyclic guanosine monophosphate (cGMP), which causes symptoms of vasodilatation, an increase in natririesis and diuresis, an increase in glomerular filtration rate and renal blood flow, inhibition of renin and aldosterone, and a decrease, and a decrease in heart rate, and a decrease in the development of the renal and aldosterone, and a decrease in the development 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 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 restructuring of the cardiovascular system, aggravating disturbances in its functioning.

Indications

Chronic heart failure (NYHA Class II-IV class) in patients with systolic dysfunction to reduce the risk of cardiovascular mortality and hospitalization for heart failure.

Composition

1 tablet, film coated, 50 mg (25.7 mg + 24.3 mg) contains:

Active ingredient: sacubitrile and valsartan hydrate complex of sodium salts -56.551 mg (in terms of anhydrous acid form 50 mg, equivalent to 24.3 mg of sacubitrile and 25.7 mg of valsartan);

excipients: microcrystalline cellulose - 91,449 mg, hyprolosis - 25,000 mg, crospovidone - 18,000 mg, magnesium stearate - 6,000 mg, talc - 2,000 mg, colloidal silicon dioxide - 1,000 mg;

shell: white premix premix - 7.957 mg (hypromellose - 5.681 mg, titanium dioxide - 1.138 mg, macrogol 4000 - 0.569 mg, talc - 0.569 mg), red premix shell - 0.019 mg (hypromellose - 0.014 mg, red iron oxide - 0.003 mg, macrogol 4000 -0.001 mg, talc - 0.001 mg), shell premix black - 0.024 mg (hypromellose - 0.017 mg, iron dye black oxide - 0.003 mg, macrogol 4000 - 0.002 mg, talc - 0.002 mg).

Valsartan, Sacubitril is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Uperio	Novartis)	Package Size - 50mg (25.7mg + 24.3mg	pills
Uperio	Novartis)	Package Size - 200mg (102.8mg + 97.2mg	pills
Uperio	Novartis)	Package Size - 100 mg (51.4 mg + 48.6 mg	pills

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Dosage and Administration

The time of taking the drug Jupério does not depend on the time of eating.

The target (maximum daily) dose of Uperio is 200 mg (102.8 mg + 97.2 mg) 2 times a day. The recommended initial dose of Uperio is 100 mg (51.4 mg + 48.6 mg) 2 times a day.

In patients who have not previously received therapy with ACE or APA II inhibitors, or who have received these drugs in low doses, therapy with Uperio should be started at a dose of 50 mg (25.7 mg + 24.3 mg) 2 times a day with a slow dose increase ( doubling the daily dose 1 time in 3-4 weeks). Depending on the tolerance, the dose of the drug Intresto should be doubled every 2-4 weeks until the target (maximum daily) dose of 200 mg (102.8 mg + 97.2 mg) is reached 2 times a day.

Use of the drug Uperio is possible no earlier than 36 hours after discontinuation of the ACE inhibitor, since in the case of simultaneous use, angioedema may develop. Since ARPA II valsartan is part of the drug, it should not be used simultaneously with another drug that includes ARA II.

With the development of signs of impaired portability of the drug Uperio (clinically pronounced decrease in blood pressure, hyperkalemia, impaired renal function), it is necessary to consider the question of a temporary dose reduction or dose adjustment of simultaneously used drugs.

Special Category Patients

Patients with impaired renal function

In patients with impaired renal mild (eGFR 60–90 ml / min / 1.73 m2) or moderate severity (eGFR 30–60 ml / min / 1.73 m2), dose adjustment is not required. In patients with severe impaired renal function (RSKF2), the recommended initial dose of the drug is 50 mg twice a day. When using the drug Uperiou patients in this category it is recommended to be careful due to the limited data.

Patients with impaired liver function

Patients with impaired mild liver function (Child-Pugh class A) do not require dose adjustment of the drug Juperio. In patients with impaired moderate liver function (Child-Pugh class B), the recommended initial dose of the drug is 50 mg twice a day. The drug Uperio is not recommended for use in patients with severely impaired liver function (class C according to the Child-Pugh classification).

Use in children and adolescents under the age of 18

There are no data on the safety and efficacy of the use of the drug Uperio in children and teenagers.

Use for patients older than 65 years

Patients over 65 years of age do not require dose adjustment.

Adverse reactions

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 - a pronounced decrease in blood pressure; often - a syncope, orthostatic hypotension.
Disturbances from 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.
Disturbances from 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 - 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.

Carefully

Care should be taken when using the drug Yupiro in patients with severely impaired renal function (eGFR

Caution must 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.

Drug interactions

Contraindicated drug interactions ACE inhibitors The drug Uperio 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.

Use of the drug Uperio 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, Jupério.

Aliskiren

In patients with diabetes and in patients with impaired renal function (eGFR

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 shows that sacubitrile inhibits the activity of the OATR1B1 and OATR1BZ carriers. Uperio can increase the systemic exposure of OATP1B1 and OATP1BZ substrates, such as statins. In patients receiving the drug Uperio simultaneously with atorvastatin, the maximum plasma concentration (Cmax) of atorvastatin and its metabolites increased to 2 times, and AUC - up to 1.3 times. For this reason, the drug Uperio simultaneously with the statins should be used with caution.

Sildenafil

In patients with a pronounced increase in blood pressure, receiving the drug Uperio (before reaching the equilibrium concentration), a single use of sildenafil increased the antihypertensive effect compared with the use of the drug Uperio in monotherapy. For this reason, use of sildenafil or another type 5 phosphodiesterase inhibitor should be used in patients receiving Uperio.

Estimated drug interactions that need to be considered

Potassium

The simultaneous use of potassium-sparing diuretics (for example, triamterene and amiloride), antagonists of mineralocorticoids (for example, spironolactone and eplerenone), potassium preparations or potassium-containing salt substitutes can cause an increase in potassium and serum creatinine concentration. In patients receiving the drug Uperio 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)

The use of drug Uperio simultaneously with NSAIDs in patients over the age of 65 years, in patients with hypovolemia (including patients receiving diuretics) and in patients with impaired renal function may increase the risk of impaired renal function. In patients receiving Uperio at the same time as NSAIDs, when prescribing such a treatment regimen and in case of its change, it is recommended to monitor renal function.

Lithium preparations

The possibility of drug interactions between the drug and drugs Yupiro lithium is not 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 regard, toxic manifestations. In patients receiving the drug Jupério along with lithium preparations, it is recommended to carefully monitor the lithium content in the blood serum. In the case of additional use of a diuretic drug, the risk of the toxic effect of lithium may increase.

Protein carriers

The active metabolite of sacubitrile (LBQ657) and valsartan are substrates of carrier proteins 0ATP1B1, 0ATP1BZ and OATZ; valsartan is also a substrate of the protein carrier MRP2. In patients receiving Uperio simultaneously with inhibitors OATP1B1, OATPR1VZ, OATZ (for example, rifampicin and cyclosporine) or MRP2 (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 Jupério and this group of drugs requires caution.

No significant drug interactions

In the case of the use of the drug Uperio in combination with furosemide, digoxin, warfarin, hydrochlorothiazide, amlodipine, metformin, omeprazole, carvedilol, nitroglycerin intravenously (iv) or the combined preparation of levonorgestrel and ethinyl estradiol, we found no significant interactions.

No interactions with atenolol, indomethacin, glibenclamide (glyburide) or cimetidine when combined with the drug Uperio is not expected.

Interactions with isoenzymes of cytochrome P450 system

Available studies demonstrate that the likelihood of drug interactions mediated by cytochrome CYP450 isoenzymes is small, since the complex of active substances to a small extent is metabolized with the participation of CYP450 isoenzymes. The complex of active ingredients of the drug Uperio is not an inhibitor or inducer of CYP450 isoenzymes.

Pregnancy and Lactation

Patients with preserved reproductive potential should be informed about the possible consequences of the use of the drug during pregnancy, as well as the need to use reliable methods of contraception during drug treatment and within a week after its last dose.

Like other drugs directly acting on the RAAS, drug Uperio should not be used during pregnancy. The action of the drug Yuprio is mediated by blockade of angiotensin II receptors, so the risk to the fetus cannot be excluded. In pregnant women who took valsartan, there have been cases of spontaneous abortion, low flow and impaired renal function in the newborn.

If pregnancy occurs during drug treatment, the patient should stop taking the drug and inform your doctor. Since preclinical studies have noted the release of sacubitrile and valsartan with the milk of lactating animals, it is not recommended to use the drug Uperio during breastfeeding. The decision to refuse breastfeeding or to discontinue the drug Uperio and the continuation of breastfeeding should be made taking into account the importance of its use for the mother. There is no data on the effect of Juperio on the fertility of men and women.In studies of the drug Uperio in animals, no decrease in fertility was noted.

Special instructions

A pronounced decrease in blood pressure

In patients who received the drug Uperio, there were cases of clinically severe hypotension. When a pronounced decrease in blood pressure occurs, the question of dose adjustment of diuretics, concomitant antihypertensive drugs should be considered, as well as the elimination of the causes of the pronounced decrease in blood pressure (for example, hypovolemia). If, despite these measures, a pronounced decrease in blood pressure persists, the dose of the drug Jupiro should be reduced or the drug should be discontinued for a while. Final drug withdrawal is usually not required. The probability of a pronounced decrease in blood pressure is usually higher in patients with hypovolemia, which can be caused by diuretic therapy, a low-salt diet, diarrhea, or vomiting.

Before starting the use of the drug Uperio, a correction should be made to the sodium content in the body and / or replenish the BCC.

Renal dysfunction

Like any other drug that acts on the RAAS, Juperio can cause kidney function deterioration. In a comparative study of the safety and efficacy of 14/17 (compared with enalapril), clinically significant impairment of renal function was rarely observed, and Uperio was less frequently canceled due to similar disorders (0.65%) than enalapril (1.28%). In the case of clinically significant impairment of renal function, consideration should be given to reducing the dose of the drug Juperio. When using the drug Uperio in patients with severely impaired renal function, caution should be exercised.

Hyperkalemia

Like any other drug that is acting on the RAAS, drug Uperio may increase the risk of developing hyperkalemia. In a comparative study of safety and efficacy (compared with enalapril), clinically significant hyperkalemia was rarely observed; Due to hyperkalemia, the drug Uperio was canceled in 0.26% of patients, and enalapril in 0.35% of patients. Drugs that can increase the content of potassium in the blood serum (for example, potassium-saving diuretics, potassium preparations) should be used with caution at the same time as the drug Uperio. In the event of a clinically significant hyperkalemia, measures such as reducing food intake of potassium or adjusting the dose of related drugs should be considered. It is recommended to regularly monitor the content of potassium in the blood serum, especially in patients with such risk factors as severe renal dysfunction, diabetes mellitus, hypoaldosteronism, or a diet high in potassium.

Angioedema

Against the background of the use of the drug Uperio, there were cases of angioedema. In the event of angioedema, drug Uperio should be immediately canceled and appropriate treatment and monitoring of the patient should be prescribed until all symptoms have been resolved. Reappoint the drug Jupério should not be. In cases of confirmed angioedema, in which the edema spreads only to the face and lips, this condition was usually resolved without intervention, although the use of antihistamines helped alleviate the symptoms.

Angioedema, accompanied by swelling of the larynx, can be fatal. In cases where edema spreads to the tongue, vocal folds or larynx, which can lead to obstruction of the respiratory tract, proper treatment should immediately begin, for example, subcutaneous administration of epinephrine (adrenaline) solution 1: 1000 (0.3-0.5 ml) and / or take appropriate measures to ensure airway obstruction.

Patients with a history of angioedema due to the use of an ACE inhibitor or ARA II should not be used.Patients of the Negroid race may be more at risk for angionsvrotic edema.

Patients with renal artery stenosis

Like other drugs acting on the RAAS, Uperio may cause an increase in serum urea and creatinine concentrations in patients with unilateral or bilateral stenosis of the renal arteries. In patients with renal artery stenosis, the drug should be used with caution, regularly monitoring kidney function.

Impact on ability to drive vehicles and / or mechanisms

There are no data on the effect of the drug on the ability to drive vehicles and / or mechanisms. In connection with the possible occurrence of dizziness or increased fatigue, caution should be exercised when driving vehicles or working with mechanisms.

Overdosage

There is not enough data on overdose with Juperio in humans. A single use of the drug at a dose of 1200 mg and multiple doses of 900 mg in healthy volunteers was accompanied by good tolerability.

The most likely symptom of an overdose is a pronounced decrease in blood pressure due to the antihypertensive effect of active substances. In this case, symptomatic treatment is recommended.

In case of accidental overdose, it is necessary to induce vomiting (if the drug has been taken recently) or to perform a gastric lavage. If a pronounced decrease in blood pressure occurs as a therapy, intravenous administration of 0.9% sodium chloride solution is necessary, the patient should be laid, raising his legs for a period of time necessary for therapy, to take active measures to support the cardiovascular system, including regular monitoring of the heart and respiratory system, circulating blood volume (BCC) and the amount of urine released. Removal of active substances during hemodialysis is unlikely, since a significant part of them binds to plasma proteins.