Uperio (sacubitril, valsartan) coated tablets 50 mg. №28

Description

Uperio (sacubitril, valsartan) coated tablets 50 mg. №28

Composition

active substances: sacubitril and valsartan;

1 tablet of 50 mg contains: 24.3 mg of sacubitril and 25.7 mg of valsartan (as a complex of sodium salt of sacubitril and valsartan);

Excipients: microcrystalline cellulose, low-substituted hydroxypropylcellulose, crospovidone, magnesium stearate, talc, colloidal silicon dioxide, hypromellose, titanium dioxide (E 171), macrogol 4000, iron oxide, red (E 172), oxide (E 172), oxide.

1 tablet of 100 mg contains: 48.6 mg of sacubitril and 51.4 mg of valsartan (as a complex of sodium salt of sacubitril and valsartan);

Excipients: microcrystalline cellulose, low-substituted hydroxypropylcellulose, crospovidone, magnesium stearate, talc, colloidal silicon dioxide, hypromellose, titanium dioxide (E 171), macrogol 4000, iron oxide, red (E 172), yellow (E 172), yellow (E 172), oxide.

1 tablet of 200 mg contains: 97.2 mg of sacubitril and 102.8 mg of valsartan (as a complex of sodium salt of sacubitril and valsartan);

Excipients: microcrystalline cellulose, low-substituted hydroxypropylcellulose, crospovidone, magnesium stearate, talc, colloidal silicon dioxide, hypromellose, titanium dioxide (E 171), macrogol 4000, iron oxide, red (E 172), oxide (E 172), oxide.

Dosage form

Film-coated tablets.

Basic physical and chemical properties:

Uperio 50 mg: Oval, biconvex, film-coated, violet-white film, bevelled, scored, embossed with NVR on one side and LZ on the other.

Uperio 100 mg: Oval, biconvex, light yellow film-coated tablets, bevelled, scored, embossed with NVR on one side and L1 on the other.

Uperio 200 mg: Oval, biconvex, light pink film-coated tablets, bevelled, scored, embossed with NVR on one side and L11 on the other.

Pharmacotherapeutic group

Drugs that affect the renin-angiotensin system. Angiotensin II antagonists, other combinations.

ATX code C09D X04.

Pharmacological properties

The pharmacodynamic effects of sacubitrile and valsartan were evaluated after single and multiple administration of the drug in healthy volunteers and in patients with chronic heart failure. The observed effects corresponded to the mechanism of action of the complex of active substances, which consists in the simultaneous inhibition of neprilysin and blockade of the renin-angiotensin-aldosterone system (RAAS).

Indication

Treatment of chronic heart failure in adult patients with reduced left ventricular ejection fraction.

Contraindication:

• hypersensitivity to the active substance or to any of the excipients;
• concomitant use with ACE inhibitors. Yuperio can be taken if at least 36 hours have passed since the ACE inhibitor was discontinued;
• presence of a history of angioneurotic edema with ACE inhibitors or ARBs;
• hereditary or idiopathic angioneurotic edema;
• concomitant use with aliskiren-containing medicinal products in patients with diabetes mellitus or in patients with renal impairment (GFR <60 ml / min / 1.73 m2);
• severe hepatic impairment, biliary cirrhosis and cholestasis;
• the second and third trimester of pregnancy.

Method of application and dosage

The drug is intended for oral use. The timing of Uperio coated tablets does not depend on the timing of the meal. The tablets should be swallowed whole and washed down with a glass of water.

The recommended starting dose of Uperio is 1 tablet of 100 mg twice a day, except as described below. The dose should be doubled after 2–4 weeks of administration so that the dose is one 200 mg tablet twice daily, provided that the patient is well tolerated.

If patients develop intolerance (systolic blood pressure (SBP) ≤ 95 mm Hg, symptomatic hypotension, hyperkalaemia, renal impairment) it is recommended to adjust combination therapy, temporarily reduce the dose or discontinue therapy with Uperio coated tablets.

There is limited information on the treatment of patients who do not take ACE inhibitors or ARBs or take them in low doses. Therefore, for this category of patients, the recommended starting dose is 50 mg twice daily with a slow dose increase (doubling the daily dose once every 3-4 weeks).

It is not recommended to start treatment in patients with serum potassium> 5.4 mmol / l or with SAT <100 mm Hg. Art. An initial dose of 50 mg twice daily is recommended for patients with CAT ≥ 100–110 mm Hg. Art. Superio should not be used with an ACE inhibitor or ARB. Due to the potential risk of angioneurotic edema when co-administered with an ACE inhibitor, the drug should not be used if at least 36 hours have elapsed since the withdrawal of the ACE inhibitor.

Valsartan, in the form of a complex salt contained in Uperio , has a higher bioavailability compared to valsartan contained in other tablets.

If a patient misses a dose, he should take the next dose at the appointed time.

Children

The safety and efficacy of Uperio in children (under 18 years of age) have not been established. No data available.

Overdose

There are insufficient data on human overdose of Uperio coated tablets.

Single administration of 1200 mg and multiple administration of 900 mg was well tolerated by healthy volunteers.

The most likely symptom of overdose is a marked decrease in blood pressure due to the antihypertensive effect of the active substances. In this case, symptomatic treatment is recommended. The likelihood of drug withdrawal during hemodialysis is extremely low due to the high binding to plasma proteins.

Side effects:

• from the blood and lymphatic system – anemia;
• on the part of metabolism and nutrition – hyperkalemia, hypokalemia, hypoglycemia;
• from the nervous system – dizziness, headache, fainting (syncope);
• from the organs of hearing and balance – vertigo;
• from vessels – hypotension, orthostatic hypotension;
• from the respiratory system, chest and mediastinum – cough;
• from the gastrointestinal tract – diarrhea, nausea, gastritis;
• from the kidneys and urinary tract – renal dysfunction, renal failure (including acute renal failure);
• general disorders – fatigue, asthenia.