Giposart tab 16mg 28 pc


Giposart tab 16mg 28 pc



Active substance:
1 tablet contains: candesartan cilexetil – 16.00 mg.
Lactose monohydrate – 87.00 mg maize starch – 20.00 mg, giproloza – 2.00 mg, giproloza – 2.00 mg macrogol 6000 – 2.60 mg magnesium stearate – 0.40 mg.
Round, biconvex tablets with Valium on one side, white.
Product form:
16 mg tablets.
To 14 tablets per blister foil Al / PVC / PVDC. 1, 2 or 4 blister together with instructions for use placed in a cardboard box.
Hypersensitivity to candesartan or other components of the formulation.
Lactose intolerance, lactase deficiency, a syndrome of glucose-galactose malabsorption.
Pregnancy and breast-feeding.
Childhood and adolescence to 18 years (effectiveness and safety have been established).
Severe hepatic dysfunction and / or cholestasis.
The simultaneous use of aliskiren and aliskirensoderzhaschimi drugs in patients with diabetes or impaired renal function (glomerular filtration rate of less than 60 ml / min).
Severe renal impairment (creatinine clearance (CC) of less than 30 ml / min), hemodialysis, bilateral renal artery stenosis or artery stenosis single kidney, hemodynamically significant stenosis, aortic and / or mitral valve, hypertrophic obstructive cardiomyopathy (GOKMP) condition after kidney transplantation , cerebrovascular disease and ischemic coronary heart disease (CHD), hyperkalemia in patients with a reduced volume of circulating blood (bcc), general anesthesia and surgical in (risk of hypotension due to blockade of the RAAS), primary aldosteronism.
16 mg
Arterial hypertension.
Chronic heart failure and disturbance of systolic left ventricular function (LVEF
Interaction with other drugs
Application candesartan simultaneously with preparations containing aliskiren, contraindicated in patients with diabetes or moderate or severe renal failure (GFR of less than 60 ml / min / 1.73 m2) (see. The section “Contra ‘).
Studied the simultaneous use of candesartan hydrochlorothiazide, warfarin, digoxin, oral contraceptives (ethinylestradiol / levonorgestrel), glibenclamide, nifedipine and enalapril; clinically significant pharmacokinetic interactions were observed.
Candesartan a small extent metabolized in the liver (via CYP2C9 isozyme).
Revealed no effect on isozymes CYP2C9 and CYP3A4; effect against other isozymes of cytochrome P450 is currently unknown.
Antihypertensives potentiates the antihypertensive effect of candesartan. Experience with other drugs acting on the RAAS reveals that the simultaneous use of the drug and potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations salt substitute containing potassium, or other means capable of increase the content of potassium in the blood serum ( e.g., heparin) can lead to the development of hyperkalemia.
With simultaneous use of drugs lithium and ACE inhibitors have been reports of transient increase of the concentration of lithium in blood serum and the development of toxic effects.
A similar effect is possible by simultaneous use of drugs lithium and angiotensin II receptor antagonists that requires periodic monitoring of the concentration of lithium in the blood serum of the combined use of these drugs.
With simultaneous application ARAII and nonsteroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2) and non-selective NSAIDs, such as acetylsalicylic acid is more than 3 g / d can be reduced antihypertensive effect of candesartan.
Dual blockade of the RAAS
As in the case of ACE inhibitors, and simultaneous use ARAII NSAID increases the risk of loss of kidney function, until 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 plenty of fluids; You need to monitor renal function at initiation of therapy in the future.
Symptoms: marked reduction of blood pressure, dizziness, tachycardia. Described isolated cases of drug overdose (up to 672 mg of candesartan cilexetil) ended convalescence patients without severe consequences.
Treatment: to transfer the patient to “lying” on the back, legs raised at a marked decrease in blood pressure; followed conduct activities aimed at increasing the bcc (addition of 0.9% sodium chloride solution i.v.).
sympathomimetic drugs can be administered in case of need.
Symptomatic therapy under the control of vital body functions.
Hemodialysis is ineffective.
pharmachologic effect
Pharmacological group:
Angiotensin II receptor antagonist.
Angiotensin II – major enzyme renin-angiotensin-aldosterone system (RAAS), taking part in the pathogenesis of hypertension (hypertension), congestive heart failure and other cardiovascular diseases.
Candesartan is a selective antagonist of angiotensin II receptor subtype 1 (AT1- receptor). Shows no agonist properties (does not affect the angiotensin-converting enzyme (ACE) and does not lead to accumulation of bradykinin or substance P, does not bind to receptors of other hormones, it does not affect the state of the ion channels involved in the regulation of the cardiovascular system). As a result of blocking angiotensin II AT1-receptor occurs compensatory dose-dependent increase in renin concentration angiotensin I, angiotensin II and aldosterone decline in plasma concentration.
Arterial hypertension
Receiving candesartan provides dose-dependent inward, gradual decrease in blood pressure (BP) by decreasing total peripheral vascular resistance (SVR) with no reflex increases in heart rate (HR). No data on the development of severe arterial hypotension after the first dose, or about the development of the syndrome of “cancellation” after the cessation of therapy.
Starting antihypertensive action after the first dose of drug usually develops within 2 h, duration of effect – 24 hours. With the continued therapy candesartan a fixed dose maximal blood pressure reduction is usually achieved within 4 weeks and persists throughout the treatment. Adding a thiazide diuretic hydrochlorothiazide to candesartan increases its antihypertensive effect.
The age and sex of the patient does not affect the efficacy of the drug. Candesartan increases renal blood flow, and does not change or increases glomerular filtration rate, while renal vascular resistance and filtration fraction are reduced.
Candesartan has a less pronounced antihypertensive effect in patients blacks (population with predominantly low renin activity in blood plasma).
There are no data on the effect of candesartan on the progression of diabetic nephropathy.
Patients with hypertension and Type 2 diabetes candesartan no negative influence on the concentration of blood glucose and lipid profile.
Heart failure
Treatment with candesartan reduces mortality and hospitalization rate in patients with chronic heart failure (CHF), regardless of age, gender and concomitant therapy, reduces the functional class of heart failure of NYHA classification.
Candesartan is effective in patients taking beta-blockers simultaneously in combination with ACE inhibitors; thus its effectiveness does not depend on the dose of ACE inhibitor.
Patients with CHF and reduced left ventricular systolic function (left ventricular ejection fraction (LVEF) of less than 40%) and candesartan reduces round wedge pressure in the pulmonary capillaries.
Candesartan cilexetil is a prodrug. Candesartan cilexetil after ingestion is rapidly converted to the active ingredient – candesartan, by ester hydrolysis.
When the suction from the digestive tract is closely associated with the AT1-receptor and dissociates slowly, it has no agonist properties.
Absorption and distribution
The absolute bioavailability of candesartan is about 40% after oral administration.
The relative bioavailability is approximately 34%.
The maximum concentration (Cmax) in the blood serum is reached after 3-4 hours after ingestion. concentration in plasma increased linearly with increasing doses in the therapeutic range (up to 32 mg). Communication to plasma proteins is high (over 99%). The volume of distribution of candesartan is 0.13 l / kg. Pharmacokinetic parameters of candesartan is not affected by age, sex of the patient and of meal times.
Metabolism and excretion
Candesartan is mainly excreted via the kidneys and intestine unchanged.
Slightly metabolized in the liver (20-30%) with the participation of CYP2C9 isozyme to form inactive derivative.
The half-life (T1 / 2) of candesartan is about 9 hours. Not accumulates. Total clearance – about 0.37 ml / min / kg, the renal clearance of the drug – 0.19 ml / min / kg. After oral administration of 14C-labeled Candesartan cilexetil 26% of the dose excreted by the kidneys in the form of candesartan and 7%, – in the form of an inactive metabolite while 56% of the dose excreted in bile via the intestine in the form of candesartan and 10% – in the form of an inactive metabolite. After a single oral administration for 72 hours to return more than 90% of the dose.
Special patient groups
In elderly patients (over 65 years) Cmax and area under the curve “concentration-time» (AUC) of candesartan are increased compared to those of young age by about 50% and 80%, respectively. But the reaction on the part of BP and the possible side effects when using candesartan did not depend on the age of the patient.
Patients with mild or moderate renal dysfunction Cmax and AUC of candesartan increased by approximately 50% and 70%, respectively, wherein T1 / 2 is not changed as compared to patients with preserved renal function.
The pharmacokinetics in patients undergoing hemodialysis, is similar to that in patients with severely impaired renal function.
In patients with severely impaired renal function, Cmax and AUC increased by 50% and 110%, respectively, and T1 / 2 of the drug is increased by 2 times.
Patients with mild to moderate hepatic impairment average value candesartan AUC increases by about 20% in one study and 80% – in another study.
No experience of use in patients with severe hepatic impairment.
Pregnancy and breast-feeding
Giposart drug is contraindicated for use during pregnancy because it has a direct impact on the RAAS and may cause abnormalities of fetal development (particularly in the second and third trimesters of pregnancy) or have a negative effect on the newborn, including death, if the drug is used during pregnancy.
It is known that antagonists of angiotensin II (ARAII) therapy can induce fetal disorders (renal failure, oligohydramnios, slowing ossification of bones of the skull) and the development of complications in the newborn (renal failure, hypotension, hyperkalaemia).
In determining whether the pregnancy drug Giposart to cancel as soon as possible.
When planning a pregnancy is necessary to transfer the patient to adequate alternative therapy.
It is not known whether candesartan passes into breast milk, but it is known that it penetrates into the milk of lactating rats.
During treatment Giposart breastfeeding should be discontinued.
Newborns whose mothers took during pregnancy Giposart should be under close medical supervision because of the likelihood of arterial hypotension.
Conditions of supply of pharmacies
On prescription.
side effects
Classification of the incidence of side effects of the World Health Organization (WHO): very common (> 1/10); common (> 1/100, 1/1000, 1/10 000,
Side effects of candesartan are mild and transient in nature. The frequency of side effects depends on the dose and age of the patient.
From the nervous system: often – dizziness, headache, and weakness.
The respiratory system: often – respiratory infections, pharyngitis, rhinitis, cough.
With the cardiovascular system: often – marked reduction of blood pressure.
With the genitourinary system: often – impaired renal function, including renal failure in susceptible patients.
From the hematopoietic system and lymphatic system: very rarely – leukopenia, neutropenia, thrombocytopenia, and agranulocytosis.
From the digestive system: very rarely – nausea.
On the part of the hepatobiliary system: very rarely – increased activity of “liver” transaminases, liver dysfunction or hepatitis.
On the part of the musculoskeletal system: very rarely – back pain, arthralgia, myalgia.
Laboratory findings: very rarely – hyperkalemia, hyponatremia, elevated serum creatinine concentration in the blood, hyperuricemia, a slight decrease in hemoglobin.
Allergic reactions: seldom – angioedema, rash, pruritus, urticaria.
Other: current worsening of gout, “tides” of blood to the skin.
special instructions
ethnic features
The antihypertensive effect of candesartan in patients blacks is less pronounced compared to patients other races, in this connection, often require an increase in dose
Giposart, as well as combination with other antihypertensive agents.
Renal function
The experience of the drug in patients with severe renal failure, or are in end-stage renal failure (creatinine clearance less than 15 mL / min) is limited. In such patients, dose selection requires strict Giposart drug under careful control of blood pressure.
In patients with heart failure, especially those older than 75 years, and in patients with impaired renal function should be periodically monitor renal function. During the selection of a dose of the drug is recommended to control Giposart concentration of creatinine and potassium in serum.
Combination therapy with ACE inhibitors in CHF
In applying the drug Giposart in combination with the ACE inhibitor may increase the risk of side effects: renal function and hyperkalaemia. In these cases, careful observation and monitoring of the relevant laboratory parameters.
During hemodialysis blood pressure may be particularly sensitive to AT1-receptor blockade as a result of reducing the BCC and the activation of the RAAS. Therefore, patients on hemodialysis, and blood pressure control is required individual selection Giposart dose preparation.
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 to a solitary kidney. A similar effect may occur when using ARAII.
kidney transplantation
The experience of the drug in patients who have recently undergone kidney transplantation, no.
In patients with heart failure who receive the drug Giposart may develop hypotension.
It is also possible the development of arterial hypotension in patients with reduced BCC, for example, receiving high doses of diuretics. At the beginning of therapy, care should be taken when necessary to compensate for the BCC.
General anesthesia / surgery
During surgery under general anesthesia in patients taking ARAII may develop hypotension due to blockade of the RAAS. Very rarely, hypotension may be severe and require intravenous fluids and / or vasopressor.
Stenosis of the aortic and / or mitral valves GOKMP
Giposart drug must be used with caution in patients with hemodynamically significant stenosis of the aortic and / or mitral valves or GOKMP.
primary aldosteronism
Patients with primary hyperaldosteronism resistant to antihypertensive drugs affecting RAAS therefore such patients are not recommended application Giposart preparation.
Simultaneous use of the drug Giposart and potassium-sparing diuretics, potassium preparations salt substitute containing potassium, or other means capable of increase the content of potassium in the serum (e.g., heparin) can lead to the development of hyperkalemia in hypertensive patients.
Hyperkalemia may occur in patients with chronic heart failure receiving Giposart. The therapy Giposart drug in patients with CHF is recommended periodic monitoring the potassium content in blood serum, especially while the use of ACE inhibitors and potassium sparing diuretics (spironolactone, eplerenone, triamterene, amiloride).
Are common
Patients with vascular tone and renal function is predominantly dependent on the activity of the RAAS (e.g., patients with decompensated CHF severe concomitant disease or kidney, including unilateral renal artery stenosis), therapy other drugs affecting through RAAS, may be accompanied by the development of arterial hypotension, azotemia, oliguria, and rarely – acute renal failure. It can not be excluded and angiotensin II receptor antagonists.
Чрезмерное снижение АД у пациентов с ишемической болезнью сердца или цереброваскулярными заболеваниями ишемического генеза может привести к развитию инфаркта миокарда или инсульта.
Двойная блокада РААС при применении препаратов, содержащих алискирен
Не рекомендуется двойная блокада РААС путем одновременного применения кандесартана и алискирена, ввиду увеличения риска развития артериальной гипотензии, гиперкалиемии и нарушения функции почек.
Применение препарата одновременно с алискиреном и алискиренсодержащими препаратами у пациентов с сахарным диабетом или нарушением функции почек (СКФ менее 60 мл/мин/1,73 м2 ) (см. раздел «Противопоказания»).
Влияние на способность управления автотранспортом и работу со сложными механизмами
Влияние препарата Гипосарт на управление автотранспортом и работу со сложными механизмами не изучалось, но фармакодинамические свойства препарата указывают на то, что подобное влияние отсутствует.
Необходимо соблюдать осторожность при управлении автотранспортом и занятиями потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций в связи с риском развития головокружения.
Storage conditions
Store at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Внутрь, 1 раз в сутки, вне зависимости от времени приема пищи.
Arterial hypertension
Рекомендуемая начальная и поддерживающая доза препарата Гипосарт составляет 8 мг 1 раз/сут.
При необходимости дозу можно увеличить до 16 мг 1 раз/сут.
Максимальный антигипертензивный эффект достигается в течение 4 недель терапии.
Максимальная суточная доза – 32 мг 1 раз/сут.
Если на фоне максимальной суточной дозы не достигается адекватный контроль АД, рекомендуется добавить к терапии тиазидный диуретик.
Пациенты со сниженным ОЦК
У пациентов с риском развития артериальной гипотензии терапию рекомендуется начинать с начальной дозы 4 мг.
Patients with impaired renal function
У пациентов с легким или умеренным нарушением функции почек (КК 30-80 мл/мин/1,73 м2 площади поверхности тела), включая пациентов, находящихся на гемодиализе, начальная доза препарата составляет 4 мг. Дозу титровать в зависимости от терапевтического эффекта. Клинический опыт применения препарата у пациентов с тяжелыми нарушениями функции почек или терминальной стадией почечной недостаточности (КК менее 15 мл/мин) ограничен (см. раздел «Особые указания».)
Patients with impaired liver function
Начальная суточная доза препарата у пациентов с заболеваниями печени легкой и средней степени тяжести составляет 4 мг. Возможно увеличение дозы при необходимости.
Клинический опыт применения препарата у пациентов с тяжелыми нарушениями функции печени и/или холестазом отсутствует (см. раздел Противопоказания).
Сопутствующая терапия
Применение препарата Гипосарт одновременно с тиазидными диуретиками (например, гидрохлоротиазид) может усилить антигипертензивный эффект препарата.
Chronic heart failure
Рекомендуемая начальная доза препарата Гипосарт составляет 4 мг 1 раз/сут. Увеличение до максимальной суточной дозы – 32 мг 1 раз/сут или до максимально переносимой дозы проводится путем удвоения дозы с интервалом не менее 2 недель.
Special patient groups
Пациентам пожилого возраста и пациентам с нарушениями функции почек или печени не требуется коррекции начальной дозы препарата.
Use in children and adolescents
Безопасность и эффективность применения препарата Гипосарт у детей и подростков в возрасте до 18 лет не установлены.
Сопутствующая терапия
Препарат Гипосарт можно одновременно применять с другими препаратами для лечения ХСН, включая ингибиторы АПФ, бета-адреноблокаторы, диуретики, сердечные гликозиды или комбинации этих лекарственных средств.
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg


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