Diocor Solo 80 mg tablets # 90

Diocor Solo (DIOCOR Solo) user manual

Composition:

active ingredient: valsartan; 1 film-coated tablet contains valsartan 80 mg or 160 mg;
auxiliary substances: calcium hydrophosphate dihydrate, microcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium, silicon dioxide colloidal anhydrous, talc, magnesium stearate, coating coating Opadry II White (polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide E 171).

Dosage form.

Film-coated tablets.

Pharmacotherapeutic group.

Simple preparations of angiotensin II antagonists. Code ATS C09C A03.

Clinical characteristics.

Indications.

Arterial hypertension in adults and children over 6 years.

Symptomatic heart failure in adult patients when angiotensin-converting enzyme (ACE) inhibitors can not be used, or as an additional therapy with ACE inhibitors when beta-blockers can not be used.

Contraindications.

Hypersensitivity to valsartan or any of the components of the drug.

Severe hepatic insufficiency, biliary cirrhosis and cholestasis.

Simultaneous use of angiotensin receptor antagonists, including valsartan, or angiotensin-converting enzyme inhibitors with aliskiren in patients with diabetes mellitus or renal dysfunction (glomerular filtration rate (GFR) <60 mL / min / 1.73 m2).

Method of administration and dose.

Diocor Solo is taken orally, regardless of food intake, with water.

Arterial hypertension in adults. The recommended initial dose of Diocor Solo for adults is 80 mg once a day.Antihypertensive effect is achieved for 2 weeks, and the maximum effect is evident after 4 weeks. For patients with uncontrolled arterial pressure, the daily dose may be increased to 160 mg and up to a maximum of 320 mg, supplemental diuretics may be prescribed.

Diocor Solo can also be prescribed concomitantly with other antihypertensive agents.

Arterial hypertension in children from 6 years. The recommended initial dose of Diocor Solo is 40 mg once a day for children weighing less than 35 kg and 80 mg once a day for children weighing 35 kg or more. Correct the dose based on the response / change in blood pressure. Possible maximum doses exceeding which are not recommended are given in the table.

Body mass	The maximum dose
From ≥ 18 kg to <35 kg	80 mg
From ≥ 35 kg to <80 kg	160 mg
From ≥ 80 kg to ≤ 160 kg	320 mg

Children with a creatinine clearance <30 ml / min and children on dialysis, valsartan should not be used because of a lack of research. Children with a creatinine clearance> 30 ml / min do not need dose adjustment. A careful monitoring of kidney function and potassium levels in the blood serum is necessary.

Diocor Solo is contraindicated in children with severe hepatic insufficiency, biliary cirrhosis and cholestasis. The clinical experience of using valsartan for children with mild to moderate hepatic impairment is limited. The dose of valsartan for such patients should not exceed 80 mg.

Heart failure in adults. The recommended initial dose of Dicor Solo is 40 mg 2 times a day. Increase in the dose to 80 mg and 160 mg twice a day should be carried out at intervals of not less than 2 weeks, to a higher dose, depending on the patient's tolerance to the drug. The maximum daily dose is 320 mg and is divided into several doses.

Valsartan can be taken in combination with other drugs used in heart failure. However, a triple combination of an ACE inhibitor, a beta-blocker and valsartan is not recommended.

Evaluation of the condition of patients with heart failure should always include an assessment of the state of kidney function.

Note regarding all indications: elderly patients and adults with creatinine clearance> 10 ml / min do not need dose adjustment.

Diocor Solo is contraindicated in patients with severe hepatic insufficiency, biliary cirrhosis and cholestasis. For patients with hepatic insufficiency of mild and moderate severity of non-junior origin and without cholestasis, the dose of the drug should not exceed 80 mg.

Adverse reactions.

Infections and invasions: viral infections, upper respiratory tract infections, pharyngitis, sinusitis, rhinitis.

On the part of the hematopoiesis system: neutropenia, thrombocytopenia.

From the immune system: hypersensitivity reactions, including serum sickness.

Metabolic disorders: hyperkalemia *, hyponatremia.

Disorders of the psyche: insomnia, decreased libido.

From the nervous system: postural dizziness *, dizziness, headache **.

From the side of the organs of vision and labyrinthine disturbances: vertigo.

From the cardiovascular system: orthostatic hypotension, arterial hypotension **, vasculitis.

On the part of the respiratory system: cough.

On the part of the digestive system: diarrhea, abdominal pain; nausea**.

From the skin and subcutaneous tissue: rash, itching, angioedema.

From the musculoskeletal system: back pain, arthralgia, myalgia.

On the part of the genitourinary system: a violation of kidney function **, kidney failure.

General disorders: increased fatigue, asthenia, edema.

Note.

Reports of adverse reactions:

* Symptoms of heart failure;

** with heart failure (dizziness, renal dysfunction, arterial hypotension, headache, nausea). In a few cases, taking the drug may affect the results of laboratory tests, for example, there may be a decrease in hemoglobin and hematocrit.

In individual patients with arterial hypertension, valsartan can cause a significant increase in serum creatinine, potassium and total bilirubin levels. Individual cases of increased liver function were reported.

In individual patients with heart failure with valsartan, serum creatinine levels were elevated, and serum potassium levels were raised and blood urea nitrogen levels increased. Therefore, when treating Diocor Solo, it is necessary to periodically monitor these indices and make adjustments during the course There is no need for special monitoring of laboratory parameters in patients with essential hypertension receiving valsartan therapy.

Children.

Except for certain disorders of the digestive tract (abdominal pain, nausea, vomiting) and dizziness, significant differences with respect to type, frequency and severity of adverse reactions between the safety profile for children aged 6 years and the safety profile for adults have not been revealed. Neurocognitive evaluation and evaluation development of children aged 6 to 16 years did not find a clinically significant overall adverse effect after treatment with valsartan for up to 1 year. Hyperkalemia was more common in children aged 6 about 18 years old with major chronic kidney disease.

Overdose.

Due to an overdose of Diocor Solo, severe arterial hypotension may develop, which can lead to depression, collapse and / or shock. If the drug was taken recently, you should induce vomiting. With arterial hypotension, conventional therapy is intravenous saline. It is unlikely that valsartan can be removed from the body by hemodialysis.

Use during pregnancy or lactation.

The use of angiotensin II antagonists is not recommended during the first trimester of pregnancy and is contraindicated during the II and III trimesters. Epidemiological data regarding the risk of teratogenic effects due to the use of ACE inhibitors during the I trimester of pregnancy are not convincing. Given the mechanism of action of angiotensin II antagonists, the risk of teratogenic effects on the fetus when using Diocor Solo during pregnancy can not be ruled out.Except where continuing therapy is necessary, patients planning a pregnancy should be prescribed an alternative antihypertensive therapy with an established safety profile for use during pregnancy.

If pregnancy is detected during therapy with the drug, Dioxor Solo should be discontinued as soon as possible and, if necessary, an alternative treatment should be started. The use of angiotensin II receptor antagonists during the II and III trimesters of pregnancy induces fetotoxicity (impaired renal function, oligohydramnios, ossification of bones skull) and neonatal toxicity (renal failure, arterial hypotension, hyperkalemia). If angiotensin II receptor antagonists have been used in the second trimester of pregnancy, an ultrasound examination is recommended to check the function of the kidneys and the condition of the bones of the skull. Newborns whose mothers have received angiotensin II receptor antagonists should be examined for the development of arterial hypotension.

It is not known whether valsartan penetrates into breast milk. Therefore, the use of the drug in women during lactation is not recommended.

Children.

Diocor Solo is indicated for the treatment of hypertension in children aged 6 to 18 years. Safety and effectiveness of the use of Diocor Solo for children aged 1 to 6 years are not established. The drug is not recommended for the treatment of heart failure in children due to lack of safety and efficacy data.

Features of application.

Hyperkalemia. The concomitant use of potassium supplements, potassium-sparing diuretics, salt substitutes containing potassium, or other agents that can increase potassium levels (heparin, etc.) is not recommended. If necessary, the level of potassium should be monitored. Patients with a deficiency in the body of sodium and / or volume of circulating blood (BCC). In patients with severe deficit in the body of sodium and / or BCC, for example, those who used high doses of diuretics, in rare cases, symptomatic hypotension may occur at the onset of treatment with Dicor Solo. Therefore, before the beginning of therapy with Diochor Solo, correction of sodium and / or BCC content should be performed, for example, by reducing the dose of diuretic. In case of hypotension, the patient should be moved to a horizontal position and, if necessary, an intravenous infusion with physiological saline. After stabilization of arterial pressure, treatment with Diocor Solo can be continued.

Stenosis of the renal artery. The safety of valsartan in patients with bilateral stenosis of the renal artery or stenosis of a single kidney is not established. Short-term use of valsartan in patients with vasorenal hypertension, which is secondary due to unilateral stenosis of the renal artery, does not cause any significant changes in hemodynamic parameters of the kidneys, serum creatinine or blood urea nitrogen. Since other drugs that affect the renin-angiotensin-aldosterone system (RAAS) can increase urea levels in the blood and serum creatinine in patients with unilateral or bilateral stenosis of the renal artery, monitoring of renal function is recommended as a safety measure.

Impaired renal function. Adult patients with creatinine clearance> 10 ml / min do not need dose adjustment. At present, there is no data on the safety of the drug for patients with creatinine clearance <10 ml / min and patients on dialysis, so valsartan should be used with caution.

The simultaneous use of angiotensin receptor antagonists, including valsartan, or angiotensin-converting enzyme inhibitors with aliskiren in patients with diabetes mellitus or renal dysfunction (glomerular filtration rate (GFR) <60 mL / min / 1.73 m2) is contraindicated.

Kidney transplantation. There are no data on the safety of valsartan in patients who have recently undergone kidney transplantation.

Violation of the function of the liver. Patients with hepatic insufficiency of mild to moderate severity without cholestasis should be treated with caution.

Primary hyperaldosteronism. Patients with primary hyperaldosteronism should not take Dyokor Solo, because they have not activated the renin-angiotensin system.

Stenosis of aortic and mitral valves, obstructive hypertrophic cardiomyopathy. As with the use of other vasodilators, special care should be taken to prescribe patients with stenosis of the aortic or mitral valves or obstructive hypertrophic cardiomyopathy.

Heart failure. In patients with heart failure who take Dioxor Solo in normal doses, there is a slight decrease in blood pressure, but discontinuation of therapy due to symptomatic hypotension is generally not required, provided that the dosage instructions are followed. Care should be taken in patients with heart failure who begin treatment with the drug.

In patients with severe heart failure, whose kidney function may depend on the activity of the renin-angiotensin-aldosterone system, treatment with ACE inhibitors or angiotensin receptor antagonists may be accompanied by oliguria and / or progressive azotemia, (rarely) acute renal failure and / or death . Evaluation of the condition of patients with heart failure should always include an assessment of the state of kidney function.

In patients with heart failure, the use of a triple combination of ACE inhibitors, beta-blockers and valsartan showed no clinical effect, and this combination may increase the risk of unwanted effects, therefore it is not recommended.

Angioedema in history. With the use of valsartan, the development of patients with angioedema, including edema of the larynx and the glottis, has been reported, leading to airway obstruction and / or edema of the face, lips, pharynx and / or tongue; in some of these patients, the development of angioedema has occurred earlier with the use of other drugs, including ACE inhibitors. The development of angioedema in patients requires immediate discontinuation of the use of Diocor Solo, and re-prescribing should not occur.

Double blockade of the renin-angiotensin-aldosterone system (RAAS). The concomitant use of ARA drugs, including valsartan, with other drugs acting on RAAS, is associated with an increase in the incidence of hypotension, hyperkalemia, and changes in renal function compared to monotherapy. It is recommended to monitor blood pressure, kidney function and electrolytes in patients receiving Diocor Solo and other drugs that affect RAAS.

Children. Features of use in children with impaired renal and hepatic function, see the section "Method of administration and dose".

The ability to influence the reaction rate when driving or working with other machinery.

When using Diocor Solo, as well as other antihypertensive drugs, it is recommended to use caution when driving vehicles and working with precise mechanisms.

Interaction with other drugs and other types of interactions.

Caution should be exercised when using ARA drugs, including Dioxor Solo, with other preparations blocking RAAS, such as preparations of the ACEI group or aliskiren. Concerning the simultaneous use of valsartan with aliskiren in patients with diabetes mellitus or renal dysfunction, see the section Contraindications.

Simultaneous application is not recommended.

Lithium. With simultaneous use of lithium preparations with angiotensin-converting enzyme (ACE) inhibitors, a reversible increase in serum lithium concentration and toxicity was noted. The experience of simultaneous application of valsartan and lithium preparations is not available, therefore this combination is not recommended. If the use of drugs is still necessary, it is recommended to monitor the concentration of lithium in the blood serum during their simultaneous application.

Potassium-sparing diuretics, potassium supplements, substitutes for edible salt containing potassium, or other medications that can raise the level of potassium in the blood serum. Simultaneous use with potassium-sparing diuretics (eg spironolactone, triamterene, amiloride), potassium supplements or salt substitutes containing potassium, can lead to increased potassium levels in serum and an increase in serum creatinine in patients with heart failure. It should be careful to control the serum potassium level if necessary use in combination with valsartan means influencing the level of potassium.

Caution is needed while the application.

Nonsteroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors, acetylsalicylic acid> 3 g / day, and non-selective NSAIDs. Possible reduced antihypertensive effect while the use of nonsteroidal anti-inflammatory drugs (such as salicylic acid derivatives, indomethacin). The concomitant use of these drugs may lead to a deterioration of renal function and an increase in serum potassium. It is therefore recommended monitoring of renal function during treatment, as well as adequate control of patient hydration.

Transporters. According to studies in vitro, valsartan is a substrate for hepatic transporter capture OATR1V1 / OATR1V3 and hepatic excretion transporter MRP2. The clinical implications of these findings is unknown. The simultaneous use of inhibitors gripping conveyor (e.g. rifampicin, cyclosporine) or removal conveyor (e.g. ritonavir) can increase the systemic exposure of valsartan. Observe appropriate measures at the beginning or at the end of the joint use of these drugs.

Other.

No clinically significant drug interactions valsartan was observed with the following substances: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, glibenclamide.

Children.

Caution is advised with concomitant use of children with hypertension valsartan and other means of oppressing the renin-angiotensin-aldosterone system, which can increase the level of potassium in the blood serum. It is necessary to carefully monitor renal function and potassium levels in the blood serum.

Pharmacological properties.

Pharmacodynamics.Valsartan is an active specific angiotensin II receptor antagonist. It acts selectively on the AT1 receptor subtype responsible for the well-known effects of angiotensin II. Increased Angiotensin II levels in plasma after blockade with valsartan AT1-receptor can stimulate the unblocked AT2 receptor, which balances the effect of the AT1 receptor. Valsartan does not exhibit any partial agonist activity relative AT1- receptor, but has a much higher (about 20,000 times) AT1- receptor affinity than the AT2 receptor.

Valsartan does not inhibit ACE (angiotensin converting enzyme), also known under the name kininaza II, which converts angiotensin I in angiotensin II and destroys bradykinin. Use of the drug to patients with hypertension leads to reduced blood pressure without affecting the frequency pulsa.Nachalo hypotensive effect observed within 2 hours, maximum - within 4-6 hours after ingestion. After ingestion antihypertensive effect lasts for 24 hours. Maximum therapeutic effect develops within 2-4 weeks of starting treatment and persists during prolonged terapii.V case of a combination with hydrochlorothiazide drug achieved significant additional reduction in blood davleniya.Vnezapnoe discontinuation of the drug is not accompanied by the development of withdrawal syndrome.With prolonged use of the drug to patients with hypertension found that the drug had no significant effect on total cholesterol, uric acid, as well as in the study of fasting, the concentration of glucose and triglycerides in the serum.

Use of the preparation causes a decrease in hospitalization for heart failure, slowing the progression of heart failure, improving functional class NYHA classification, increase in ejection fraction and also reducing the symptoms of heart failure and improvement in quality of life compared with placebo.

Pharmacokinetics. After oral administration of valsartan drug is rapidly absorbed, but the extent of absorption varies greatly. The average value of the absolute bioavailability of the drug is 23%. When assigning valsartan with food area under the curve "concentration-time" (AUC) is reduced by 48%, although starting at about the 8th hours after dosing, Valsartan plasma concentrations as in the case of reception of his fasting, and in case of reception with food the same. Reducing the area under the curve "concentration-time", however, it is not accompanied by a clinically significant decrease in therapeutic effect. Therefore, the drug can be taken on an empty stomach, and during edy.Farmakokineticheskaya valsartan curve has a downward multiexponential character (t1 / 2α≤ 1 hour, and t1 / 2β about 9 hours). The range of doses studied the kinetics of valsartan is linear.Repeated use of the drug changes the kinetic parameters were noted. While taking the drug 1 time per day accumulation is insignificant. The drug concentration in blood plasma in women and men were odinakovy.Valsartan largely (at 94-97%) binds to serum proteins, predominantly to albumin. Volume of distribution during the equilibrium state is low (about 17 L). Compared with the hepatic blood flow (about 30 liters / hour), valsartan plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of valsartan, is excreted in the feces, it is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.While taking the drug 1 time per day accumulation is insignificant. The drug concentration in blood plasma in women and men were odinakovy.Valsartan largely (at 94-97%) binds to serum proteins, predominantly to albumin. Volume of distribution during the equilibrium state is low (about 17 L). Compared with the hepatic blood flow (about 30 liters / hour), valsartan plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of valsartan, is excreted in the feces, it is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.While taking the drug 1 time per day accumulation is insignificant. The drug concentration in blood plasma in women and men were odinakovy.Valsartan largely (at 94-97%) binds to serum proteins, predominantly to albumin. Volume of distribution during the equilibrium state is low (about 17 L). Compared with the hepatic blood flow (about 30 liters / hour), valsartan plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of valsartan, is excreted in the feces, it is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.Valsartan largely (by 94-97%) binds to serum proteins, mainly albumin. Volume of distribution during the equilibrium state is low (about 17 L). Compared with the hepatic blood flow (about 30 liters / hour), valsartan plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of valsartan, is excreted in the feces, it is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.Valsartan largely (by 94-97%) binds to serum proteins, mainly albumin. Volume of distribution during the equilibrium state is low (about 17 L). Compared with the hepatic blood flow (about 30 liters / hour), valsartan plasma clearance occurs relatively slowly (about 2 liters / hour). The amount of valsartan, is excreted in the feces, it is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.It is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.It is 83% (of the value of an oral dose). The urine output of about 13%, preferably in an unmodified form. The half-life of valsartan is 6 hours.

The average time to reach the highest concentration and elimination half-life of valsartan in patients with heart failure and healthy volunteers alike. Indicators area under the curve "concentration-time" (AUC) and maximum concentration of valsartan and increased almost linearly proportional to dose increase above clinical range (40-160 mg 2 times a day). cumulation factor is an average of 1.7. Clearance of valsartan after oral administration is about 4.5 l / hr. Age does not affect the clearance of the drug in patients with heart failure.

Pharmacokinetics in specific patient groups.

Patients of advanced age.Some elderly patients systemic exposure to valsartan was more pronounced than in younger patients, but did not show any clinical significance etogo.Patsienty with impaired renal function. There was no correlation between renal function and systemic exposure to valsartan. Therefore, patients with impaired renal function (creatinine clearance of> 10 ml / min), the dose correction is not required. While there is no data on the safety of the drug in patients with creatinine clearance <10 ml / min and those who are on dialysis, therefore valsartan should be used with caution. Valsartan has a high degree of binding to plasma proteins, therefore its excretion in hemodialysis unlikely.

Patients with impaired liver function.About 70% of the sucked dose excreted in bile, preferably in an unmodified form. Valsartan is not subjected to significant biotransformation and as can be expected, the systemic exposure of valsartan is not correlated with the degree of disturbances pecheni.Bylo functions shown that patients with biliary cirrhosis or biliary tract obstruction valsartan AUC increased approximately 2-fold.

Pharmaceutical characteristics.

Basic physical and chemical properties:

DioCore Solo 80 - tablets with a round biconvex shaped surface, film-coated white color, with Valium.
DioCore Solo 160 - tablets of round biconvex shape with a surface, film-coated white.

Shelf life.

3 years.

Storage conditions.

Keep out of the reach of children, in their original packaging at a temperature not higher than 25? C.

Packaging.

10 tablets in a blister; 1, 3 or 4 in the blister cardboard pack.

Category vacation.

On prescription.