Kardosal 20 coated pills 20mg N28
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Olmesartana Medoxomil
Release form
Pills
Composition
Active ingredient: Olmesartan medoxomil (Olmesartan medoxomil). Concentration of active ingredient (mg): 20
Pharmacological effect
Angiotensin II receptor antagonist (type AT1). Look in more detail on the portal about health. Angiotensin II is the primary vasoactive hormone RAAS and plays a significant role in the pathophysiology of arterial hypertension through AT1 receptors. Look in more detail on the health portal. It is supposed that olmesartan blocks all effects of angiotensin II mediated by AT1 receptors regardless of the source and route of synthesis of angiotensin II. See details on the health portal. In hypertension, olmesartan causes a dose-dependent prolonged decrease in blood pressure. See more on the health portal There is no evidence of the development of arterial hypotension after taking the first dose of the drug, tachycardia during long-term treatment (for drugs Cardosal 20 and Cardosal 40) and the development of withdrawal syndrome (a sharp increase in blood pressure after drug withdrawal). See details on the health portal. Taking olmesartan medoxomil 1 time / day provides an effective and gentle decrease in blood pressure for 24 hours, and the effect after a single dose is similar to the effect of taking the drug 2 times / day in the same daily dose. See more on the portal about health. The hypotensive effect of olmesartan develops, as a rule, already after 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy. See more on the portal about health.
Pharmacokinetics
Absorption and distribution: olmesartan medoxomil is a prodrug. It quickly turns into a pharmacologically active metabolite of olmesartan under the action of enzymes in the intestinal mucosa and in the portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil in unchanged form was not detected in the blood plasma. The bioavailability of olmesartan is on average 25.6%. The maximum concentration (Cmax) of olmesartan in plasma is on average 2 hours after ingestion of olmesartan medoxomil by mouth and increases approximately linearly with an increase in a single dose of up to 80 mg.Eating does not have a significant impact on the bioavailability of olmesartan, so olmesartan medoxomil can be taken regardless of the meal. There were no clinically significant differences in pharmacokinetic parameters of olmesartan depending on gender. Olmesartan binds to plasma proteins (99.7%), but the potential for a clinically significant bias in protein binding when olmesartan interacts with other high-binding and simultaneously used drugs is low (a confirmation of this is the absence of clinically significant interaction between olmesartan and warfarin). Communication olmesartan with blood cells is negligible. Metabolism and excretion: total plasma clearance is usually 1.3 l / h (coefficient of variation - 19%) and is relatively low compared with hepatic blood flow (approximately 90 l / h). Renal excretion is approximately 40%, with bile - about 60%. The intrahepatic circulation of olmesartan is minimal. Since most of olmesartan is excreted through the liver, its use in patients with obstruction of the biliary tract is contraindicated (see section Contraindications). The half-life of olmesartan is 10-15 hours after repeated ingestion. A significant effect of therapy is achieved after taking the first few doses of the drug, and after 14 days of repeated use, no further cumulation is observed. Renal clearance is approximately 0.5-0.7 l / h and does not depend on the dose of the drug. In patients with impaired renal function, the area under the concentration-time curve (AUC) at steady state was increased by approximately 62, 82 and 179% in the case of mild, moderate and severe renal dysfunction, respectively, compared with healthy volunteers. After a single oral administration, the AUC values for olmesartan were 6% and 65% higher in patients with mild and moderate hepatic impairment, respectively, compared with healthy volunteers. The unbound fraction of olmesartan 2 hours after taking the dose of the drug in healthy volunteers, in patients with mild and moderate degrees of liver dysfunction was 0.26, 0.34 and 0.41%, respectively.
Indications
Essential arterial hypertension.
Contraindications
Hypersensitivity to the active substance or to any of the excipients that make up the drug, biliary tract obstruction, renal failure (QA less than 20 mlmin), condition after kidney transplantation (no clinical experience), lactase deficiency, galactosemia or malabsorption syndrome, pregnancy and lactation period. age up to 18 years (efficacy and safety have not been established).
Precautionary measures
The effect of Kardosal 10 on the ability to drive vehicles and control mechanisms has not been studied, therefore, during treatment with Kardosal 10, care should be taken when driving vehicles and practicing potentially hazardous activities that require increased concentration and psychomotor speed (dizziness and weakness are possible).
Use during pregnancy and lactation
Experience with olmesartan medoxomil in pregnant women is absent. However, due to the existing reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, like any drug of this class, olmesartan is contraindicated during pregnancy. In the case of pregnancy during treatment with the drug Cardosal 10, the drug must be withdrawn. It is not known whether olmesartan is excreted with breast milk, so if you need to use the drug Cardosal 10 during lactation, breastfeeding for the period of taking the drug should be stopped.
Dosage and administration
It is recommended to take the drug Cardosal orally every day at the same time, regardless of the meal 1 day. The recommended initial dose for adults is 10 mg (1 tab. Of the drug Cardosal 10) 1 daily. In case of insufficient decrease in blood pressure while taking the drug in a dose of 10 mg a day, the dose of the drug can be increased to 20 mg a day (use of the drug Cardosal 20 is possible). If necessary, an additional reduction in blood pressure can be increased to a maximum dose of 40 mg / day (use of the drug Cardosal 40 is possible) or a diuretic (hydrochlorothiazide) may be added. The maximum daily dose is 40 mg.
Side effects
From the hematopoietic system: very rarely - thrombocytopenia.From the side of the central nervous system: sometimes - dizziness. very rarely - headache. On the part of the respiratory system: often - pharyngitis, rhinitis. very rarely - cough, bronchitis. On the part of the digestive system: often - diarrhea, dyspepsia, gastroenteritis. very rarely - abdominal pain, nausea, vomiting. For the skin: very rarely - pruritus, rash, angioedema, allergic dermatitis, urticaria. On the part of the musculoskeletal system: often - back pain, bone pain, arthralgia, arthritis. very rarely - muscle cramps, myalgia. On the part of the urinary system: often - hematuria, urinary tract infection. very rarely, acute renal failure. From the laboratory indicators: very rarely - an increase in serum creatinine and urea levels, an increase in the activity of liver enzymes. Since the cardiovascular system: sometimes - angina, tachycardia. rarely - a pronounced decrease in blood pressure. On the part of the metabolism: often - increased levels of CPK, hypertriglyceridemia, hyperuricemia. rarely - hyperkalemia. On the part of the organism as a whole: often - pain in the chest, flu-like symptoms, peripheral edema. very rarely - asthenia, fatigue, malaise, drowsiness.
Overdose
Symptoms: marked reduction in blood pressure. Treatment: with a pronounced decrease in blood pressure, it is recommended to lay the patient on his back, raising his legs. Recommended gastric lavage and / or reception of activated carbon, therapy aimed at correcting dehydration and disorders of water-salt metabolism, replenishment of circulating blood volume.
Interaction with other drugs
Combined use with potassium-sparing diuretics, potassium preparations, salt substitutes containing potassium, or other drugs that can increase the level of potassium in the blood serum (eg, heparin) is not recommended; this may lead to an increase in the level of potassium in the blood serum (see the section instructions). The antihypertensive effect of olmesartan therapy can be enhanced when combined with other antihypertensive drugs. Non-steroidal anti-inflammatory drugs (NG1VP), including acetylsalicylic acid in doses of more than 3 g / day, as well as cyclooxygenase-2 inhibitors (COX-2), and angiotensin II receptor antagonists can act synergistically, reducing glomerular filtration.With simultaneous use of NSAIDs and angiotensin II receptor antagonists, there may be a risk of developing acute renal failure, therefore, monitoring renal function at the beginning of treatment is recommended, as well as regular intake of a sufficient amount of fluid. However, simultaneous treatment can reduce the antihypertensive effect of angiotensin II receptor antagonists, leading to a partial loss of their therapeutic efficacy. With simultaneous use with antacids (magnesium and aluminum hydroxide), a moderate decrease in the bioavailability of olmesartan is possible. There are reports of a reversible increase in serum lithium concentration and toxicity during simultaneous use of lithium preparations with angiotensin-converting enzyme inhibitors (ACE) and angiotensin II receptor antagonists, therefore, the use of olmesartan medoxomil in combination with lithium preparations is not recommended (see section Special instructions). If necessary, the use of appropriate combination therapy is recommended to regularly monitor the level of lithium in the serum.
special instructions
Symptomatic arterial hypotension, especially after taking the first dose of the drug, can occur in patients with reduced blood volume and / or low sodium levels due to intensive diuretic therapy, restriction of salt intake with food in the diet, and also due to diarrhea or vomiting. Relevant factors should be eliminated before starting Cardosal 10. In patients whose vascular tone and kidney function depend to a large extent on the activity of the renin-angiotensin-aldosterone system (for example, in patients with severe chronic heart failure or impaired renal function, including stenosis renal arteries), treatment with other drugs acting on this system is associated with the possibility of developing acute arterial hypotension, azotemia, oliguria, or, in rare cases, swarm of renal failure. The possibility of a similar effect cannot be excluded when using angiotensin II receptor antagonists. There is an increased risk of developing severe arterial hypotension and renal failure if a patient with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney receives therapy with drugs that affect the renin-angiotensin-aldosterone system.When using the drug Cardosal 10 in patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood serum. Experience with the use of the drug Cardosal 10 is absent in patients with recently performed kidney transplantation or in patients with the last stage of impaired renal function (for example, CC less than 12 ml / min). As in the case of other angiotensin II receptor antagonists and ACE inhibitors, hyperkalemia may develop when treated with Cardosal 10 if the patient has impaired renal function and / or chronic heart failure (see Interaction with other drugs). In patients of this risk group, it is recommended to monitor the level of potassium in the serum. As in the case of other angiotensin II receptor antagonists, a combination of lithium preparations and the drug Cardosal 10 is not recommended (see the section on Interaction with Other Drugs). As in the case of other angiotensin II receptor antagonists, in patients of the Negroid race suffering from arterial hypertension, the effectiveness of treatment with Cardosal 10 is somewhat lower than in patients of other races. As in the case of any antihypertensive agent, an excessive decrease in blood pressure in patients with ischemic heart disease or cerebrovascular insufficiency can lead to myocardial infarction or stroke. Influence on ability to drive motor transport and control mechanisms. The effect of Kardosal 10 on the ability to drive vehicles and control mechanisms has not been studied, therefore, during treatment with Kardosal 10, care should be taken when driving vehicles and practicing potentially hazardous activities that require increased concentration and psychomotor speed (dizziness and weakness are possible).