Orissz® (Ordiss®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceCandesartanCandesartan
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    • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: candesartan cilexetil 8.0 mg / 16.0 mg / 32.0 mg;

    Excipients: pregelatinized starch 3.75 mg / 7.5 mg / 15.0 mg; poloxamer 188 0.5 mg / 1.0 mg / 2.0 mg; povidone-KZO 4.0 mg / 8.0 mg / 16.0 mg; dye iron oxide red (E172) 0.075 mg / 0.15 mg / 0.3 mg; carmellose calcium 1.65 mg / 3.3 mg / 6.6 mg; cellulose microcrystalline 17.5 mg / 35.0 mg / 70.0 mg; lactose monohydrate 43.725 mg / 87.45 mg / 174.9 mg; magnesium stearate 0.8 mg / 1.6 mg / 3.2 mg.

    Description:

    Tablets 8 mg. Pink capsule tablets with a risk on both sides and engraved "8 | C" on one side and "C | 8" on the other side of the tablet.

    Tablets 16 mg. Pink capsule-shaped tablets with a risk on one side and engraved "C | C" on opposite sides of the risk, on the other side of the tablet - engraving "16".

    Tablets 32 mg. Pink capsule tablets with a risk on one side and engraved "C | C" on both sides of the risk, on the other side of the tablet the engraving "32".

    Pharmacotherapeutic group:angiotensin II receptor antagonist
    ATX: & nbsp

    C.09.C.A.06   Candesartan

    Pharmacodynamics:Angiotensin II is the main hormone of the renin-aigiotensin-aldosterone system (RAAS), which plays an important role in the pathogenesis of arterial hypertension, cardiac insufficiency and other cardiovascular diseases. The main physiological effects of angiotensin II are vasoconstriction, stimulation of aldosterone production, regulation of the water-electrolyte state and stimulation of cell growth. Effects are mediated by the interaction of angiotensin II with angiotensin receptors of type 1 (AT1-receptors).

    Candesartan is a selective antagonist AT1receptors of angiotensin II, does not inhibit the angiotensin-converting enzyme (ACE), which converts angiotensin I into angiotensin II, which destroys bradykinin, does not lead to accumulation of bradykinin or substance P. As a result of blocking AT1receptors of angiotensin II, a dose-related increase in the content of renin, angiotensin I, angiotensin II, and a decrease in aldosterone in the blood plasma.

    When comparing candesartan with ACE inhibitors, the development of cough was less common in patients who received candesartan.

    Candesartan does not bind to the receptors of other hormones and does not block the ion channels involved in the regulation of cardiovascular functions.

    Pharmacokinetics:

    Suction and distribution. When absorbed from the gastrointestinal tract (GIT) candesartan cileksetil through ether hydrolysis quickly turns into an active substance - candesartan, firmly communicates with AT1receptors and dissociates slowly, does not have the properties of an agonist.

    Absolute bioavailability of candesartan after oral administration is about 40%. The relative bioavailability of the tablet form compared to the oral solution is approximately 34%. Thus, the calculated absolute bioavailability of the tablet form of the drug is 14%. Eating does not have a significant effect on the area under the concentration-time curve (AUC), i.e. food does not significantly affect the bioavailability of the drug.

    The maximum concentration in the blood plasma (Cmax) is achieved 3-4 hours after taking the tablet form of the drug.With an increase in the dose of the drug within the recommended limits, the concentration of candesartan rises linearly. The binding of candesartan to plasma proteins is more than 99%. Plasma volume distribution (Vd) candesartan is 0.1 l / kg.

    The pharmacokinetic parameters of candesartan do not depend on the sex of the patient.

    Metabolism and excretion. Candesartan, is mainly excreted from the body by the kidneys and through the intestine in an unchanged form and is only slightly metabolized in the liver.

    Half-life (T1/2) candesartan is approximately 9 hours. Cumulation of the drug in the body is not observed.

    The total clearance of candesartan is about 0.37 ml / min / kg, with a kidney clearance of about 0.19 ml / min / kg. Renal excretion of candesartan is carried out by glomerular filtration and active tubular secretion.

    When administered radically-labeled candesartan, about 26% of the administered amount is excreted by the kidneys in the form of candesartan and 7% in the form of an inactive metabolite, whereas in the stool 56% of the administered amount in the form of candesartan and 10% in the form of an inactive metabolite is detected.

    Pharmacokinetics in special clinical cases

    The pharmacokinetic parameters of candesartan do not depend on the sex of the patient.

    In patients older than 65 years of age, Cmax and AUC candesartan increased by 50% and 80%, respectively, compared with young patients. However, the hypotensive effect and incidence of side effects with candesartan do not depend on the age of the patients.

    In patients with mild to moderate renal impairment, CmOh and AUC candesartan increased by 50% and 70%, respectively, whereas T1/2 the drug does not change in comparison with patients with a normal function of the nights.

    In patients with severe renal dysfunction and / or on hemodialysis Cmax and AUC candesartan increased by 50% and 110% respectively, and T1/2 of the drug increased 2-fold.

    In patients with mild and moderate impairment of liver function, there was an increase AUC candesartan by 23%.

    Indications:

    Arterial hypertension.

    Chronic heart failure and systolic function of the left ventricle (left ventricular ejection fraction (LVEF) not more than 40%) as adjunctive therapy with ACE inhibitors or with intolerance to ACE inhibitors.

    Contraindications:Hypersensitivity to candesartan and other components of the drug; lactose intolerance; deficiency of lactase; glucose-galactosyl malabsorption syndrome; severe liver dysfunction and / or cholestasis; pregnancy; the period of breastfeeding; children's age till 18 years; simultaneous application with aliskirenom in patients with diabetes mellitus and impaired renal function (CC less than 60 ml / min).

    Carefully:

    Hemodiaamically significant stenosis of the aortic and mitral valves, cerebrovascular diseases, coronary heart disease (CHD), hypertrophic obstructive cardiomyopathy (GOCMP), condition after kidney transplantation, bilateral stenosis of the renal arteries or stenosis of the single kidney artery, primary hyperaldosteronism, severe renal failure (creatinine clearance (CC) less than 30 ml / min), hemodialysis, hyperkalemia; in patients with reduced circulating blood volume (BCC), general anesthesia and surgical interventions (risk of arterial hypotension, due to RAAS blockade).

    Pregnancy and lactation:

    The drug Orissis® is contraindicated for use in pregnancy due to the fact that candesartan has a direct effect on RAAS, can cause fetal developmental disorders or have a negative impact on the newborn, up to a lethal outcome. If pregnancy is detected during treatment with Ordiss®, it is necessary to immediately discontinue the drug. When planning pregnancy, it is necessary to transfer the patient to adequate therapy, permitted for use in pregnancy.

    Newborns, whose mothers took during the pregnancy drug Ordiss®, should be under medical supervision because of the likelihood of developing arterial hypotension.

    It is not known whether the candesartan in breast milk. Hc should use Orissis ® during breastfeeding. You should stop breastfeeding if you need to use the drug from your mother.

    Dosing and Administration:

    Inside, regardless of food intake, 1 time per day.

    Arterial hypertension
    The recommended initial dose of Ordiss® is 8 mg once a day. Patients who require further reduction in blood pressure (BP), it is recommended to increase the dose to 16 mg once a day.The maximum antihypertensive effect is achieved within 4 weeks from the start of treatment. The maximum daily dose of 32 mg / day. In case, against the background of treatment drug Ordiss ® is not adequately controlled by BP, it is recommended to add a thiazide diuretic to therapy.

    Have patients of the aged there is no need to correct the initial dose of the drug.

    Have patients with reduced BCC there is a risk of developing arterial hypotension, so you should start treatment with the drug at a dose of 4 mg / day (1/2 tablet 8 mg).

    Have patients with renal insufficiency. When used in patients with mild or moderate renal failure (CC not less than 30 ml / min / 1.73 m2 body surface area) the initial dose of 4 mg / day (1/2 tablet 8 mg).

    Clinical experience of the drug in patients with severe renal failure (CC less than 30 ml / min / 1.73 m2 surface area of ​​the body) ogis vulnerable. In these cases, you should consider starting treatment with a dose of 4 mg / day (1/2 tablet 8 mg).

    Have patients with impaired liver function. When using the drug in patients with a malfunction of the liver of mild and moderate severity, an initial dose of 2 mg / day (1/4 tablet of 8 mg) is recommended. If necessary, it is possible to increase the dose.Clinical experience of the drug in patients with severe impairment of liver function and / or cholestasis is limited (see the section "Contraindications").

    Ordriss® can be used in conjunction with thiazide diuretics (for example, hydrochlorothiazide), which leads to increased hypotensive effect.

    Chronic heart failure (CHF)

    The recommended initial dose of Ordiss® is 4 mg once a day (1/2 tablet 8 mg). An increase in the dose to 32 mg once a day or up to the maximum tolerated dose is carried out by doubling it at intervals of not less than 2 weeks.

    Ordriss® can be used in conjunction with other drugs used for CHF, for example, with ACE inhibitors, beta-blockers, diuretics and cardiac glycosides.

    Special patient groups

    Older patients, patients with renal insufficiency or liver dysfunction, do not need to change the initial dose of the drug.

    Side effects:The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including single messages.

    On the part of the blood and lymphatic system: very rarely - leukopenia, neutropenia, thrombocytopenia, agranulocytosis.

    From the immune system: very rarely - skin rash, itching, hives, angioedema.

    From the nervous system: often - dizziness, headache, weakness.

    From the respiratory system: often - respiratory infections, pharyngitis, rhinitis.

    From the gastrointestinal tract: very rarely - nausea.

    From the cardiovascular system: often a marked decrease in blood pressure.

    From the liver and biliary tract: very rarely - increased activity of "liver" transaminases, a violation of liver function, hepatitis.

    From the musculoskeletal system and connective tissue: very rarely - back pain, arthralgia, myalgia.

    From the side of the kidneys and urinary tract: often - a violation of kidney function (see section "Special instructions").

    Laboratory indicators: very rarely - hyperkalemia, hyponatremia, increased creatinine concentration, hyperuricemia, decreased hemoglobin.

    Other: very rarely - exacerbation of the gout, the "tides" of blood to the face.
    Overdose:

    Symptoms: analysis of the pharmacological properties of the drug suggests that the main manifestation of an overdose may be a clinically pronounced decrease in blood pressure, dizziness. Individual cases of drug overdose (up to 672 mg candesartan), which resulted in the recovery of patients without severe consequences, were described.

    Treatment: When developing a clinically pronounced BP reduction, symptomatic treatment and monitoring of the patient's condition should be performed. Lay the patient on his back and raise his legs. If necessary, increase BCC, for example, by iv introduction of 0.9% sodium chloride solution. If necessary, you can apply sympathomimetic drugs. Withdrawal of candesartan by hemodialysis is ineffective.

    Interaction:With the simultaneous use of candesartan with hydrochlorothiazide, warfarin, digoxin, oral contraceptives (ethinyl estradiol / levonorgesgrel), glibenclamide, nifedipine, and enalapril, no clinically relevant drug interactions have been identified.

    With the simultaneous use of candesartan with ACE inhibitors, other angiotensin II receptor antagonists, aliskiren, the risk of hyperkalemia, a sharp decrease in blood pressure, renal dysfunction, including acute renal failure, requires careful monitoring of blood pressure, as well as renal function and water- electrolyte balance.

    The simultaneous use of candesartan with aliskiren in patients with diabetes mellitus and renal dysfunction (YS less than 60 ml / min) is not recommended. Candesartan metabolized in the liver to a small extent with the participation of isoenzyme CYP2C9. The conducted studies on the interaction did not reveal the influence of candesartan on isoenzymes CYP2C9 and CYP3A4, the effect on other isoenzymes of the cytochrome P450 system has not been studied.

    The simultaneous use of candesartan with other antihypertensive drugs increases the antihypertensive effect.

    The experience of using other drugs acting on RAAS shows that concomitant therapy with potassium-sparing diuretics, potassium preparations, salt substitutes containing potassium, and other agents,increasing potassium content in the blood serum (eg, heparin), may lead to the development of hyperkalemia.

    With the simultaneous use of lithium and ACE inhibitors, a reversible increase in the concentration of lithium in the blood serum and the development of toxic reactions occur. Similar reactions can occur with the use of angiotensin II receptor antagonists, and therefore it is recommended to monitor the lithium content in serum.

    Simultaneous use with nonsteroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2), acetylsalicylic acid (more than 3 g / day) and nonselective NSAIDs, may reduce the antihypertensive effect of candesartan, and may lead to an increased risk of dysfunction kidney, including the development of acute renal failure and an increase in potassium in the blood serum. Caution is necessary to use a combination of these drugs, especially in elderly patients.

    Special instructions:

    Impaired renal function. Against the backdrop of the use of Ordiss®, as in the case of other drugs that oppress RAAS, renal dysfunction may develop in some cases.

    When using Ordiss® in patients with arterial hypertension and severe renal insufficiency (QC less than 30 ml / min), it is recommended to regularly monitor the potassium content and serum creatinine concentration. The clinical experience of using the drug in patients with terminal stage of renal failure (QC less than 15 ml / min) is limited. When using Orissit ® in such patients, it is necessary to select the dose of Orissit ® under the control of blood pressure.

    Patients with CAS need to periodically monitor kidney function, especially in patients over the age of 75 and patients with impaired renal function. When increasing the dose, it is also recommended to monitor the potassium content and serum creatinine concentration.

    There are no data on the use of Ordiss® in patients with CHF with a creatinine concentration greater than 265 μmol / L (more than 3 mg / ml).

    Hemodialysis. During hemodialysis, blood pressure may be particularly sensitive to blockade AT1-receptors as a result of a decrease in bcc and activation of the RAAS. Therefore, patients on hemodialysis need to monitor blood pressure and individually adjust the dose of Ordiss® in accordance with the indices of blood pressure.

    Simultaneous use with ACE inhibitors in CHF. With the simultaneous use of ACE inhibitors, the risk of side effects increases, especially renal dysfunction and hyperkalemia. It is necessary to monitor the clinical status of patients and the corresponding laboratory parameters.

    Stenosis of the renal artery. Drugs that affect RAAS (eg, ACE inhibitors) can lead to increased serum urea and creatinine levels in patients with bilateral renal artery stenosis or stenosis of the single kidney artery. A similar effect can be expected with angiotensin II receptor antagonists.

    Transplantation kidneys. The experience of using Ordiss® in patients who have recently undergone kidney transplantation is absent.

    Arterial hypotension. In patients with CHF with the drug Orissz® may develop hypotension. It is also possible to develop arterial hypotension in patients with BCC deficiency, for example, when using large doses of diuretics. In this case, before applying the Ordiss®, it is necessary to correct the BCC.

    General anesthesia and / or surgery. Patients receiving angiotensin II antagonists may develop arterial hypotension as a result of RAAS blockade during general anesthesia and during surgical interventions. In rare cases, arterial hypotension can be pronounced, requiring intravenous fluid and / or vasopressors.

    Stenosis of aortic and / or mitral valves, GOKMP. Care should be taken when using Ordiss® in patients with GOKMP or hemodynamically significant stenosis of the aortic or mitral valves.

    Primary hyperaldosteronism. Patients with primary hyperaldosteronism are usually resistant to therapy with antihypertensive drugs that affect RAAS, so it is not recommended to use Ordiss® in this group of patients. Hyperkalemia. The simultaneous use of Ordiss® with potassium-sparing diuretics, potassium preparations or salt substitutes containing potassium, or other drugs that can increase serum potassium levels (eg, heparin) can lead to hyperkalemia in patients with hypertension.

    Hyperkalemia can also develop in patients with CHF who are taking Ordiss®.On the background of therapy with the Ordiss® drug in patients with CHF it is recommended to periodically check the potassium content in the blood serum, especially with the simultaneous use of ACE inhibitors and potassium-sparing diuretics (spironolactone, triamterene, amiloride).

    Are common. Patients who have vascular tone and renal function preferentially depend on RAAS activity (for example, patients with severe chronic heart failure, kidney disease, including renal artery stenosis) are particularly sensitive to drugs acting on RAAS. The use of such drugs is accompanied in these patients by severe arterial hypotension, azotemia, oliguria and, more rarely, acute renal failure. The possibility of developing these effects is not excluded even when angiotensin II receptor antagonists are used. A sharp decrease in blood pressure in patients with ischemic cardiopathy, cerebrovascular disease of ischemic genesis with the use of any antihypertensive drugs, can lead to the development of myocardial infarction or stroke.

    Use in Pediatrics. The safety and efficacy of Ordisse ® before the age of 18 years are not established.

    Effect on the ability to drive transp. cf. and fur:

    When there are undesirable effects from the central nervous system during drug therapy Ordiss® should be careful when performing actions that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets 8 mg, 16 mg, 32 mg.

    Packaging:

    For 10 tablets in blisters from PVC / A1 / OPA-PVC / PVAH / A1. 3 blisters with instructions for use in a cardboard bundle.

    For 5 tablets in PVC / Al / OPA-PVC / PVAH / A1 blisters. 6 blisters with instructions for use in a cardboard pack.

    Storage conditions:

    Store in a dry place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002127
    Date of registration:05.07.2013
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp03.04.2014
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