Hyposart, pills 16mg 28pcs

Composition

of 1 tab.

candesartan cilexetil 16 mg.

Auxiliary substances:  

lactose monohydrate – 87 mg,

corn starch – 20 mg

of hyprolose (viscosity, water,25°C (5%) 75-150 GPA) of 2 mg

of hyprolose (viscosity, water,25°C (5%) 1500-3000 SDR) – 2 mg,

macrogol 6000 – 2.6 mg,

magnesium stearate – 0.4 mg.

Pharmacological action

Cmax in plasma is reached within 3-4 hours the plasma Concentration increases linearly with increasing doses in the therapeutic range (up to 32 mg). Vd – 0.13 l/kg. Binding to plasma proteins is 99.8%. It is slightly metabolized in the liver (20-30%) with the participation of CYP2C with the formation of an inactive metabolite.

The final T1 / 2 – 9 hours is not cumulative. Total clearance is 0.37 ml / min / kg, while renal clearance is about 0.19 ml/min/kg. Candesartan is excreted by the kidneys (by glomerular filtration and active tubular secretion): 26% – as candesartan and 7% – as an inactive metabolite; with bile – 56% and 10%, respectively. After a single dose within 72 hours, more than 90% of the dose is eliminated.

In elderly patients (over 65 years of age) Cmax and AUC increased by 50% and 80%, respectively, compared with younger patients.

In patients with mild and moderate renal impairment, Cmax and AUC increase by 50% and 70%, respectively, while T1 / 2 of the drug does not change compared to patients with normal renal function.

In patients with severe renal impairment, Cmax and AUC increase by 50% and 110%, respectively, and T1 / 2 increases 2-fold.

Patients with mild to moderate hepatic impairment experienced a 23% increase in AUC.

Indications

-arterial hypertension;- chronic heart failure and impaired left ventricular systolic function (LVEF < 40%) as adjunctive therapy to ACE inhibitors or in case of intolerance to ACE inhibitors.

Contraindications

– severe liver function disorders and / or cholestasis;- concomitant use with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus or impaired renal function (GFR, lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome);- children and adolescents under 18 years of age (efficacy and safety have not been established);- hypersensitivity to candesartan or other components of the drug.

Caution should be exercised when prescribing the drug for severe renal impairment (CC).

Side effects

Classification of the frequency of side effects: very common (≥1/10); common (≥1/100). Side effects of candesartan are mild and transient. The frequency of side effects does not depend on the dose of the drug and the age of the patient.

Nervous system disorders:  often – dizziness, headache, weakness.

From the cardiovascular system:  often-an excessive decrease in blood pressure.

Respiratory system disorders:  often – respiratory infections, pharyngitis, rhinitis, cough.

From the digestive system:  very rarely – nausea, increased activity of hepatic transaminases, impaired liver function or hepatitis.

From the urinary system:  often-impaired renal function, including renal failure in predisposed patients.

Musculoskeletal disorders:  very rarely-back pain, arthralgia, myalgia.

From the hematopoietic system:  very rarely – leukopenia, neutropenia, thrombocytopenia and agranulocytosis.

Laboratory parameters:  very rarely-hyperkalemia, hyponatremia, increased creatinine concentration in the blood, hyperuricemia, a slight decrease in hemoglobin.

Allergic reactions:  very rarely – angioedema, skin rash, pruritus, urticaria.

Other services:  exacerbation of gout, “hot flashes” of blood to the skin of the face.

Interaction

Concomitant use of candesartan with drugs containing aliskiren is contraindicated in patients with diabetes mellitus or moderate to severe renal insufficiency (GFR 2).

Concomitant use of candesartan with hydrochlorothiazide, warfarin, digoxin, oral contraceptives (ethinyl estradiol/levonorgestrel), glibenclamide, nifedipine and enalapril was studied; no clinically significant pharmacokinetic interaction was observed.

Candesartan is only slightly metabolized in the liver (via the CYP2C9 isoenzyme). No effect was found on the CYP2C9 and CYP3A4 isoenzymes; the effect on other cytochrome P 450 isoenzymes is currently unknown.

Antihypertensive agents potentiate the antihypertensive effect of candesartan. Experience with other drugs that affect the RAAS shows that the simultaneous use of the drug and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, or other agents that can increase the concentration of potassium in the blood serum (for example, heparin), can lead to the development of hyperkalemia.

When lithium preparations and ACE inhibitors were used simultaneously, cases of transient increase in the concentration of lithium in the blood serum and the development of toxic effects were noted. A similar effect is possible with the simultaneous use of lithium preparations and angiotensin II receptor antagonists, which requires periodic monitoring of the concentration of lithium in the blood serum with the combined use of these drugs.

Concomitant use of ARA II and NSAIDs, including selective COX-2 inhibitors and non-selective NSAIDs (for example, acetylsalicylic acid at a dose of more than 3 g/day), may reduce the antihypertensive effect of candesartan.

Double blockade of the RAAS

As with ACE inhibitors, concomitant use of ARA II and NSAIDs increases the risk of decreased renal function, up to the development of renal failure, which leads to hyperkalemia in patients with impaired renal function. This combination should be used with caution, especially in elderly patients. All patients should receive sufficient fluids and renal function should be monitored at the beginning of therapy and thereafter.

How to take, course of use and dosage

The drug is taken orally,1 time/day, regardless of food intake.

Arterial hypertension

The recommended initial and maintenance dose of Hyposart is 8 mg 1 time / day. If necessary, the dose can be increased to 16 mg 1 time/day. The maximum antihypertensive effect is achieved within 4 weeks of therapy. The maximum daily dose is 32 mg 1 time/day.

If adequate blood pressure control is not achieved against the background of the maximum daily dose, it is recommended to add a thiazide diuretic (for example, hydrochlorothiazide) to therapy. This may increase the antihypertensive effect of Hyposart.

In patients at risk of developing arterial hypotension (including patients with reduced BCC), therapy is recommended to start with a dose of 4 mg.

In patients with mild to moderate renal impairment (creatinine clearance 30-80 ml/min/1.73 m2), including patients on hemodialysis, the initial dose of the drug is 4 mg. The dose should be titrated depending on the therapeutic effect. Clinical experience of using the drug in patients with severe renal impairment or end-stage renal failure (creatinine clearance less than 15 ml / min) restricted.

The initial daily dose of the drug in patients with mild to moderate liver disease is 4 mg. It is possible to increase the dose if necessary. There is no clinical experience of using the drug in patients with severe hepatic impairment and / or cholestasis.

Chronic heart failure

The recommended initial dose of Hyposart is 4 mg 1 time / day. An increase to the maximum daily dose of 32 mg 1 time/day or to the maximum tolerated dose is carried out by doubling the dose at intervals of at least 2 weeks.

Elderly patients and patients with impaired renal or hepatic function do not need to adjust the initial dose of the drug.

The safety and efficacy of Hyposart in children and adolescents under 18 years of age have not been established.

Concomitant therapy

Hyposart can be used concomitantly with other medications for the treatment of CHF, including ACE inhibitors, beta-blockers, diuretics, cardiac glycosides, or combinations of these medications.

Overdose

Symptoms: excessive lowering of blood pressure, dizziness, tachycardia. Individual cases of overdose of the drug (up to 672 mg of candesartan cilexetil), which resulted in recovery of patients without serious consequences, are described.

Treatment: if there is an excessive decrease in blood pressure, the patient should be moved to a horizontal position with a low headboard; then, measures should be taken to increase the BCC (use of 0.9% sodium chloride solution IV). If necessary, sympathomimetic drugs may be prescribed. It is recommended to conduct symptomatic therapy under the control of vital body functions. Hemodialysis is ineffective.

Special instructions

Use in patients with liver function disorders

In the treatment of arterial hypertension, the initial daily dose of the drug in patients with mild to moderate liver disease is 4 mg. It is possible to increase the dose if necessary. There is no clinical experience of using the drug in patients with severe hepatic impairment and / or cholestasis.

In the treatment of chronic heart failure, patients with impaired liver function do not need to adjust the initial dose of the drug. The drug is contraindicated in patients with severe hepatic impairment and / or cholestasis.

Use in patients with impaired renal function

In the treatment of arterial hypertension in patients with mild to moderate renal impairment (creatinine clearance 30-80 ml/min/1.73 m2), including patients on hemodialysis, the initial dose of the drug is 4 mg. The dose should be titrated depending on the therapeutic effect. Clinical experience of using the drug in patients with severe renal impairment or end-stage renal failure (creatinine clearance less than 15 ml / min) restricted.

In the treatment of chronic heart failure, patients with impaired renal function do not need to adjust the initial dose of the drug.

Caution should be exercised when prescribing the drug for severe renal impairment (CC).

Use in children

The drug is contraindicated in children and adolescents under 18 years of age (efficacy and safety have not been established).

Use in elderly patients

Elderly patients do not need to adjust the initial dose of the drug.

 Ethnic features

The antihypertensive effect of candesartan in patients of the black race is less pronounced compared to patients of other races, and therefore, an increase in the dose of Hyposart is more often required, as well as a combination with other antihypertensive agents.

Impaired renal function

Experience of using the drug in patients with severe renal insufficiency or who are in the end stage of renal insufficiency (CC

In patients with CHF, especially over the age of 75 years, and in patients with impaired renal function, it is necessary to periodically monitor renal function. During the selection of the dose of Hyposart, it is recommended to monitor the concentration of creatinine and potassium in the blood serum.

Combination therapy with an ACE inhibitor for CHF

When using the drug Hyposart in combination with an ACE inhibitor, the risk of side effects may increase: impaired renal function and hyperkalemia. In these cases, careful monitoring and monitoring of appropriate laboratory parameters is necessary.

Hemodialysis

During hemodialysis, blood pressure may be particularly sensitive to AT1-receptor blockade as a result of BCC reduction and RAAS activation. Therefore, patients undergoing hemodialysis need to monitor blood pressure and individually select the dose of Hyposart.

Renal artery stenosis

Drugs that affect the RAAS, such as ACE inhibitors, can cause hyperuricemia and hypercreatininemia in patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney. A similar effect can develop with the use of ARA II.

Kidney transplantation

There is no experience of using the drug in patients who have recently undergone kidney transplantation.

Arterial hypotension

Patients with CHF receiving Hyposart may develop hypotension. Hypotension may also occur in patients with reduced BCC, such as those receiving high-dose diuretics. At the beginning of therapy, care should be taken and, if necessary, compensate for BCC.

General anesthesia/surgical procedures

When performing surgery under general anesthesia, patients taking ARA II may develop hypotension due to RAAS blockade. Very rarely, hypotension may be severe and require intravenous fluids and/or vasopressors.

Aortic and/or mitral valve stenosis, HOCMP

Hyposart should be used with caution in patients with hemodynamically significant aortic and/or mitral valve stenosis or with HOCMP.

Primary hyperaldosteronism

Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS, so the use of Hyposart is not recommended for such patients.

Hyperkalemia

Concomitant use of Hyposart with potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium, or other agents capable of increasing serum potassium concentrations (for example, heparin) may lead to the development of hyperkalemia in patients with arterial hypertension. Hyperkalemia may also occur in patients with CHF who are taking Hyposart. During therapy with Hyposart in patients with CHF, it is recommended to periodically monitor the concentration of potassium in the blood serum, especially with the simultaneous use of ACE inhibitors and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride).

General information

Patients whose vascular tone and renal function are predominantly dependent on RAAS activity (for example, patients with severe decompensated CHF or concomitant renal disease, including unilateral renal artery stenosis), therapy with other drugs that affect RAAS may be accompanied by the development of arterial hypotension, azotemia, oliguria and, less often, acute renal failure. This cannot be excluded for angiotensin II receptor antagonists. Excessive lowering of blood pressure in patients with CHD or cerebrovascular diseases of ischemic origin can lead to the development of myocardial infarction or stroke.

Double blockade of the RAAS when using drugs containing aliskiren

Double blockade of the RAAS by concomitant use of candesartan and aliskiren is not recommended, due to the increased risk of hypotension, hyperkalemia and impaired renal function.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect of Hyposart on the ability to drive vehicles and work with complex mechanisms has not been studied, but the pharmacodynamic properties of the drug indicate that there is no such effect. Caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions due to the risk of dizziness.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Candesartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Hypertension