Hyposart pills 8 mg 28 pcs
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Active ingredients
Candesartan
Release form
Pills
Composition
Candesartan Cilexetil 8 mg; Excipients: lactose monohydrate - 197.9 mg, corn starch - 40 mg, hyprolose (viscosity, water, 25 ° C (5%) 75-150 spz) - 4 mg, hyprolosis (viscosity, water, 25 ° C (5%) 1500-3000 spz) - 4 mg, macrogol 6000 - 5.2 mg, magnesium stearate - 0.8 mg, iron dye red oxide (E172) - 0.1 mg.
Pharmacological effect
Angiotensin II receptor antagonist. Angiotensin II is the main enzyme of the RAAS that is involved in the pathogenesis of arterial hypertension, heart failure and other cardiovascular diseases. Candesartan is a selective antagonist of angiotensin II receptors, subtype 1 (AT1 receptors). Does not show agonist properties (does not affect ACE and does not result in the accumulation of bradykinin or substance P, does not bind to receptors of other hormones, does not affect the state of the ion channels involved in the regulation of the cardiovascular system). As a result of blocking angiotensin II receptor AT1, a compensatory dose-dependent increase in renin activity, angiotensin I concentration, angiotensin II concentration and aldosterone concentration in the blood plasma decreases; hypertension; . There is no data on the development of severe arterial hypotension after taking the first dose or the development of withdrawal syndrome after stopping therapy. The onset of antihypertensive effect after taking the first dose of the drug usually develops within 2 hours, the duration of the effect is 24 hours. Against the background of continuing therapy with candesartan in a fixed dose The maximum reduction in blood pressure is usually achieved within 4 weeks and lasts throughout the treatment. The addition of thiazide diuretic hydrochlorothiazide to candesartan enhances its antihypertensive effect. The patient’s age and sex do not affect the effectiveness of the drug. Candesartan increases renal blood flow and does not alter or increase the glomerular filtration rate, while renal vascular resistance and filtration fraction decrease.; Candesartan has a less pronounced antihypertensive effect in patients of the negroid race (a population with a predominantly low renin activity in the blood plasma) .; There are no data on Candesartan effects on the progression of diabetic nephropathy.In patients with arterial hypertension and type 2 diabetes mellitus, candesartan does not adversely affect blood glucose concentration and lipid profile.; Heart failure; Candesartan therapy reduces mortality and hospitalization rates in patients with chronic heart failure (CHF) regardless of age, sex and concomitant therapy, leads to a decrease in the functional class of CHF according to the NYHA classification.; Candesartan is effective in patients taking beta-adrenergic blocking ry in combination with ACE inhibitors; however, its effectiveness does not depend on the dose of the ACE inhibitor. In patients with CHF and reduced systolic function of the left ventricle (left ventricular ejection fraction (LVEF) is less than 40%), candesartan reduces the round focal disease and the wedging pressure in the pulmonary capillaries.
Pharmacokinetics
Absorption and distribution; Candesartan cilexetil is a prodrug. After oral administration, candesartan cilexetil is rapidly transformed into the active substance - candesartan, by means of ether hydrolysis. When absorbed from the digestive tract, it binds strongly to AT1 receptors and slowly dissociates, has no agonist properties.; The absolute bioavailability of candesartan after oral administration is approximately 40%. Relative bioavailability is approximately 34%. Cmax in serum is reached within 3-4 hours after ingestion. Plasma concentration increases linearly with increasing dose in the therapeutic range (up to 32 mg). The degree of binding to plasma proteins is high (more than 99%). Vd candesartan is 0.13 L / kg. Does not accumulate. The pharmacokinetic parameters of candesartan do not depend on the age, sex of the patient and the time of eating.; Metabolism and excretion; Candesartan is mainly excreted by the kidneys and through the intestines unchanged. Slightly metabolized in the liver (20-30%) with the participation of CYP2C9 with the formation of an inactive derivative.; T1 / 2 candesartan is about 9 hours. Total clearance is about 0.37 ml / min / kg, while the renal clearance of the drug is 0.19 ml / min / kg After ingestion of 14C-labeled candesartan cilexetil, 26% of the dose was eliminated by the kidneys in the form of candesartan and 7% in the form of an inactive metabolite, while 56% of the dose is eliminated through the intestine with bile in the form of candesartan and 10% in the form of an inactive metabolite.After a single oral administration over 72 hours, more than 90% of the dose is eliminated. Pharmacokinetics in special groups of patients; In elderly patients (over 65 years), Cmax and AUC of candesartan are increased by about 50% and 80% compared with young patients, respectively . However, the response from AD and possible side effects when using candesartan do not depend on the age of patients. In patients with mild or moderate renal impairment, Cmax and AUC of candesartan increase by about 50% and 70%, respectively, while T1 / 2 does not change compared with patients with intact renal function. Pharmacokinetics in patients on hemodialysis is similar to that in patients with severe impaired renal function. In patients with severe impaired renal function, Cmax and AUC are increased by 50% and 110%, respectively, and T1 / 2 of the drug is increased by 2 times. In patients with mild or moderate hepatic insufficiency, the average AUC value of candesartan increases by about 20% in one study and 80% in another study. There is no experience of use in patients with severely impaired liver function.
Indications
- arterial hypertension; - chronic heart failure and violation of the systolic function of the left ventricle (LVEF ≤40%) as an additional therapy to ACE inhibitors or in case of intolerance to ACE inhibitors.
Contraindications
- abnormal liver function and / or cholestasis; - simultaneous use with aliskiren and aliskiren-containing drugs in patients with diabetes or impaired renal function (GFR less than 60 ml / min); - lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; - pregnancy; - lactation period (breastfeeding); - children's and teenage age up to 18 years (efficiency and safety are not established); - hypersensitivity to candesartan or other components of the drug.; The drug should be prescribed with caution for severe renal dysfunction (CC less than 30 ml / min) for patients undergoing hemodialysis, with bilateral renal artery stenosis or arterial stenosis of the only kidney that is hemodynamically significant stenosis of the aortic and / or mitral valve,hypertrophic obstructive cardiomyopathy (GOKMP), condition after kidney transplantation, cerebrovascular disorders of ischemic genesis and coronary artery disease, hyperkalemia in patients with reduced BCC, general anesthesia and surgical interventions (risk of arterial hypotension due to blockade of RAAS), primary hyperemia, and surgical interventions (the risk of arterial hypotension due to blockade of RAAS), primary hyperemia, and surgical intervention
Use during pregnancy and lactation
Hyposart preparation is contraindicated for use during pregnancy, because it has a direct effect on the RAAS and can cause impaired fetal development (especially in the second and third trimesters of pregnancy) or have a negative effect on the newborn, even death, if the drug was used during pregnancy.; It is known that angiotensin II receptor antagonists therapy ( ARA II) may cause impaired fetal development (impaired renal function, oligohydramnios, delayed ossification of the skull bones) and the development of complications in the newborn (renal failure, arterial hypotension, erkalemia). When establishing the fact of pregnancy, Hyposart needs to be canceled as soon as possible. When planning pregnancy it is necessary to transfer the patient to adequate alternative therapy. It is not known whether candesartan is excreted in breast milk, but it is known that it penetrates the milk of lactating rats. During drug treatment Hyposarth breastfeeding should be stopped. Newborns whose mothers took Giposart during pregnancy should be under close medical supervision due to the likelihood of developing hypotension.
Dosage and administration
The drug is taken orally, 1 time / day, regardless of the time of a meal.; Hypertension; The recommended initial and maintenance dose of the drug 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, against the background of the maximum daily dose, adequate blood pressure control is not achieved, it is recommended to add a thiazide diuretic (for example, hydrochlorothiazide) to therapy. This may enhance the antihypertensive effect of the drug Hyposart. In patients at risk of developing hypotension (includingpatients with reduced BCC) therapy is recommended to start with a dose of 4 mg.; In patients with impaired mild or moderate kidney function (CC 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 with the drug in patients with impaired severe kidney function or end-stage renal failure (CC less than 15 ml / min) is limited. The initial daily dose of the drug in patients with mild and moderate liver disease is 4 mg. May increase the dose if necessary. Clinical experience with the drug in patients with severely impaired liver function and / or cholestasis is absent.; Chronic heart failure; The recommended initial dose of the drug Hyposart is 4 mg 1 time / day. Increasing up to a 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 liver function do not need to adjust the initial dose of the drug. use of the drug Hyposart in children and adolescents under the age of 18 years have not been established.; Concomitant therapy; The drug Hyposart can be used simultaneously with other drugs for the treatment of CHF, including ACE inhibitors, beta-adrenal blockers, diuretics, cardiac glycosides, or combinations of these drugs.
Side effects
Classification of the incidence of side effects: very often (≥1 / 10); often (≥1 / 100, less than 1/10); infrequently (≥1 / 1000, less than 1/100); rarely (≥1 / 10,000, less than 1/1000); very rarely (less than 1/10 000), including individual messages.; Side effects of candesartan are mild and transient. The frequency of side effects does not depend on the dose of the drug and the patient's age. From the nervous system: often - dizziness, headache, weakness. From the cardiovascular system: often - pronounced decrease in blood pressure. From the respiratory system: often - respiratory infections, pharyngitis, rhinitis, cough.; From the digestive system: very rarely - nausea, increased activity of hepatic transaminases,abnormal liver function or hepatitis. From the urinary system: often - impaired renal function, including renal failure in predisposed patients; From the musculoskeletal system: very rarely - back pain, arthralgia, myalgia.; From the hematopoietic system: very rarely - leukopenia, neutropenia, thrombocytopenia and agranulocytosis; Laboratory indicators: very rarely - hyperkalemia, hyponatremia, increased creatinine concentration in the blood, hyperuricemia, a slight decrease in hemoglobin.; Allergic p reactions: very rarely - angioedema, skin rash, itching, urticaria;; Other: exacerbation of the flow of gout, "flushes" of blood to the skin of the face.
Overdose
Symptoms: excessive decrease in blood pressure, dizziness, tachycardia. The individual cases of drug overdose are described (up to 672 mg of candesartan cilexetil), which ended in the recovery of patients without serious consequences.; Treatment: if the blood pressure is pronounced, the patient should be placed in a supine position, the legs should be raised; then - to carry out activities aimed at increasing the BCC (introduction of a 0.9% solution of sodium chloride in / in). If necessary, sympathomimetic drugs may be prescribed. Symptomatic therapy is recommended under the control of vital body functions. Hemodialysis is ineffective.
Interaction with other drugs
The use of candesartan simultaneously with drugs containing aliskiren is contraindicated in patients with diabetes mellitus or moderate and severe renal insufficiency (GFR less than 60 ml / min / 1.73 m2); the simultaneous use of candesartan with hydrochlorothiazide, warfarin, digoxin, oral contraceptives (ethinyl estrate is studied). levonorgestrel), glibenclamide, nifedipine and enalapril; clinically significant pharmacokinetic interaction was not observed.; Candesartan is slightly metabolized in the liver (using the isoenzyme CYP2C9). No effect on CYP2C9 and CYP3A4 isoenzymes; the effect on other cytochrome P450 isoenzymes is currently unknown.; Antihypertensives potentiate the antihypertensive effect of candesartan. The experience of using other drugs acting on the RAAS showsthat the simultaneous use of the drug and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, or other means capable of increasing the concentration of potassium in the blood serum (eg, heparin) can lead to the development of hyperkalemia .; With the simultaneous use of lithium preparations and ACE inhibitors, there have been cases of a transient increase in the concentration of lithium in the blood serum and the development of toxic effects. A similar effect is possible with simultaneous use of lithium preparations and angiotensin II receptor antagonists, which requires periodic monitoring of serum lithium concentrations in the combined use of these drugs. With simultaneous use of APA II and NSAIDs, including selective COX-2 inhibitors and non-selective NSAIDs (for example, acetylsalicylic acid in a dose of more than 3 g / day), can decrease the antihypertensive effect of candesartan.; Double blockade of the RAAS; As with ACE inhibitors, the simultaneous use RA II and NSAIDs increases the risk of reduced kidney function, until the development of renal failure, leading to hyperkalemia in patients with impaired renal function. This combination should be used with caution, especially in elderly patients. All patients should receive an adequate amount of fluid; it is necessary to monitor renal function at the beginning of therapy and in the future.
special instructions
Ethnic features; The antihypertensive effect of candesartan in patients of the Negroid race is less pronounced compared to patients of other races, and therefore more often requires an increase in the dose of Hyposart, as well as combination with other antihypertensive drugs; severe renal failure or end-stage renal disease (CC less than 15 ml / min) is limited. In such patients, careful selection of the dose of the Hyposart preparation under strict control of blood pressure is required. 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 control the concentration of creatinine and potassium in the serum.In these cases, careful monitoring and control of relevant laboratory parameters is necessary. Hemodialysis; During hemodialysis, blood pressure may be particularly sensitive to blockade of AT1 receptors as a result of a decrease in the BCC and activation of the RAAS. Therefore, patients on hemodialysis need monitoring of blood pressure and individual selection of the dose of the drug Hyposart; Renal artery stenosis; Preparations affecting the RAAS, such as ACE inhibitors, can cause hyperuricemia and hypercreatininemia in patients with bilateral renal artery stenosis or a single artery stenosis the kidneys. A similar effect may develop with the use of APA II.; Kidney transplantation; Experience with the use of the drug in patients who have recently undergone kidney transplantation is absent. Arterial hypotension; Patients with CHF receiving Hyposart may develop hypotension. It is also possible to develop arterial hypotension in patients with reduced BCC, for example, receiving diuretics in high doses. At the beginning of therapy, care must be taken and if necessary, to compensate for the BCC. General anesthesia / surgical interventions; If surgical interventions are performed under general anesthesia, patients taking ARA II may develop arterial hypotension due to blockade of the RAAS. Very rarely, arterial hypotension can be severe and may require intravenous fluids and / or vasopressors.; Aortic and / or mitral valve stenosis, GOKMP; Hyposart preparation should be used with caution in patients with hemodynamically significant aortic and / or mitral stenosis or GOKMP.; Primary hyperaldosteronism; Patients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS, so use of the drug Hyposart is not recommended for such patients.; Hype rkalemia; Simultaneous use of the drug Hyposart and potassium-sparing diuretics, potassium preparations, potassium-containing salt substitutes, or other drugs that can increase serum potassium concentration (for example, heparin) can lead to the development of hyperkalemia in patients with arterial hypertension. Hyperkalemia can also develop in patients with CHF who take Hyposart.During therapy with Hyposarth, patients with CHF should be periodically monitored for serum potassium concentrations, especially with simultaneous use of ACE inhibitors and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride) mainly depend on the activity of the RAAS (for example, patients with severe decompensated CHF or concomitant kidney disease, including unilateral stenosis of the renal artery), therapy with other drugs and, affecting the RAAS, may be accompanied by the development of arterial hypotension, azotemia, oliguria and, less commonly, acute renal failure. It cannot be excluded for angiotensin II receptor antagonists. An excessive decrease in blood pressure in patients with ischemic heart disease or cerebrovascular disease of ischemic genesis can lead to the development of myocardial infarction or stroke. Double RAAS blockade when using drugs containing aliskiren; , hyperkalemia and renal dysfunction.; Influence on ability to drive motor vehicles and control mechanisms; Influence of the drug Hyposart on ability The control of vehicles and work with complex mechanisms has not been studied, but the pharmacodynamic properties of the drug indicate that there is no such effect. Care must be taken when driving vehicles and occupations of potentially hazardous activities that require increased concentration and psychomotor speed due to the risk of dizziness.