Composition, form of production and packaging
CardosalВ® 10
The tablets covered with a film cover of white color, round, biconcave, with a print "РЎ13" on one side, with hardly perceptible specific smell.
1 tab.
olmesartan medoxomil 10 mg
Excipients: microcrystalline cellulose - 10 mg, low-substituted giprolose - 20 mg, lactose monohydrate - 61.6 mg, giprolose 6-10 mPa? S - 2.5 mg, magnesium stearate - 0.9 mg.
The composition of the film membrane: hypromellose 5 mPa? S - 3.6 mg, talc - 0.7 mg, titanium dioxide (E171) - 0.7 mg.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
14 pcs. - blisters (4) - packs of cardboard.
14 pcs. - blisters (7) - packs of cardboard.
CardosalВ® 20
The tablets covered with a film shell of white color, round, biconcave, with the impression "C14" on one side, with a subtle specific odor.
1 tab.
olmesartan medoxomil 20 mg
Excipients: microcrystalline cellulose - 20 mg, low-substituted giprolose - 40 mg, lactose monohydrate - 123.2 mg, giprolose 6-10 mPa? S - 5 mg, magnesium stearate - 1.8 mg.
Composition of the film coat: hypromellose 5 mPa? S - 5.76 mg, talc - 1.12 mg, titanium dioxide (E171) - 1.12 mg.
14 pcs. - packings of cellular contour (1) - packs cardboard.
14 pcs. - packings cellular planimetric (2) - packs cardboard.
14 pcs. - packings cellular planimetric (4) - packs cardboard.
14 pcs. - packings cellular planimetric (7) - packs cardboard.
Cardosal В® 40
The tablets covered with a film shell of white color, oval, biconcave, with an impression "C15" on one side, with a subtle specific smell.
1 tab.
olmesartan medoxomil 40 mg
Excipients: microcrystalline cellulose - 40 mg, low-substituted giprolose - 80 mg, lactose monohydrate - 246.4 mg, giprolose 6-10 mPa? S - 10 mg, magnesium stearate - 3.6 mg.
The composition of the film shell: hypromellose 5 mPa? S - 8.64 mg, talc - 1.68 mg, titanium dioxide (E171) - 1.68 mg.
14 pcs. - packings of cellular contour (1) - packs cardboard.
14 pcs. - packings cellular planimetric (2) - packs cardboard.
14 pcs. - packings cellular planimetric (4) - packs cardboard.
14 pcs. - packings cellular planimetric (7) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Angiotensin II receptor antagonist (type AT 1) . Angiotensin II is the primary vasoactive hormone of RAAS and plays a significant role in the pathophysiology of hypertension via AT 1 -receptors. It is assumed that olmesartan blocks all the effects of angiotensin II, mediated by AT 1 -receptors, regardless of the source and route of synthesis of angiotensin II.
With arterial hypertension, olmesartan causes a dose-dependent long-term decline in blood pressure. There is no conclusive data on the development of arterial hypotension after taking the first dose of the drug, about tachycardia during long-term treatment (for Cardosal В® 20 and Cardosal В® 40) and about the development of withdrawal syndrome (a sharp increase in BP after drug withdrawal).
Taking olmesartan medoxomil 1 time / day provides an effective and gentle decrease in blood pressure within 24 hours, the effect after a single dose is similar to the effect of taking the drug 2 times / day in the same daily dose.
The hypotensive effect of olmesartan develops, as a rule, after 2 weeks, and the maximum effect develops approximately 8 weeks after the initiation of therapy.
PHARMACOKINETICS
Suction and distribution
Olmesartan medoxomil is a prodrug. It quickly turns into pharmacologically active metabolite olmesartan under the action of enzymes in the intestinal mucosa and in portal blood during absorption from the digestive tract. Olmesartan medoxomil in unchanged form in the blood plasma was not detected. The bioavailability of olmesartan is 25.6% on average. C max of olmesartan in blood plasma is attained on average 2 hours after taking olmesartan medoxomil by mouth and increases approximately linearly with a single dose increase to 80 mg.
Eating does not have a significant effect on the bioavailability of olmesartan, so olmesartan medoxomil can be taken regardless of food intake.
Clinically significant differences in pharmacokinetic parameters of olmesartan, depending on sex, were not revealed.
Olmesartan binds to blood plasma proteins (99.7%), but the potential for a clinically significant shift in the amount of binding to proteins in the interaction of olmesartan with other highly-linked and concomitantly used drugs is low (the absence of a clinically significant interaction between olmesartan and warfarin). The association of olmesartan with blood cells is negligible.
Metabolism and excretion
The total plasma clearance is usually 1.3 l / h (the coefficient of variation is 19%) and is relatively low in comparison with the hepatic blood flow (approximately 90 l / h). Kidney excretion is approximately 40%, with bile - about 60%. The intrahepatic circulation of olmesartan is minimal. Since most of the olmesartan is excreted through the liver, its use in patients with bile duct obstruction is contraindicated.
T 1/2 Olmesartan is 10-15 hours after repeated oral administration. A significant effect of therapy is achieved after the first few doses of the drug, and after 14 days of repeated use, further cumulation is not observed. Kidney clearance is approximately 0.5-0.7 l / h and does not depend on the dose of the drug.
Pharmacokinetics in special clinical cases
In patients with impaired renal function, AUC in a steady state was increased by approximately 62%, 82% and 179% in the case of mild, moderate and severe renal impairment, respectively, compared to healthy volunteers.
After a single oral dose, the AUC values ​​for olmesartan were 6% and 65% higher in patients with mild to moderate liver failure, respectively, compared to 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 impaired liver function were 0.26%, 0.34%, and 0.41%, respectively.
INDICATIONS
- essential hypertension.
DOSING MODE
It is recommended to take the drug Cardosal В® inside every day at the same time, regardless of food intake 1 time / day.
The recommended initial dose for adults is 10 mg (1 tablet of Cardosal В® 10) 1 time / day. In case of insufficient reduction of blood pressure when taking the drug at a dose of 10 mg / day, the dose of the drug can be increased to 20 mg / day (Cardosal В® 20 can be used). If it is necessary to further reduce blood pressure, the dose of the drug can be increased to a maximum of 40 mg / day (Cardosal В® 40 may be used) or an additional diuretic (hydrochlorothiazide) may be prescribed. The maximum daily dose is 40 mg.
SIDE EFFECT
Possible side effects are given below on the descending frequency of occurrence: very often (> 1/10); often (> 1/100 <1/10); sometimes (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), including individual messages.
From the hemopoietic system: very rarely - thrombocytopenia.
From the side of the central nervous system: sometimes - dizziness; very rarely - a headache.
From the respiratory system: often - pharyngitis, rhinitis; very rarely - cough, bronchitis.
From the digestive system: often - diarrhea, indigestion, gastroenteritis; very rarely - pain in the abdomen, nausea, vomiting.
From the skin: very rarely - skin itching, rash, angioedema, allergic dermatitis, urticaria.
On the part of the musculoskeletal system: often - back pain, bone pain, arthralgia, arthritis; very rarely - muscle cramps, myalgia.
From the urinary system: often - hematuria, urinary tract infection; very rarely acute renal failure.
On the part of laboratory indicators: very rarely - increasing the level of creatinine and urea in the blood serum, increasing the activity of liver enzymes.
From the cardiovascular system: sometimes - angina, tachycardia; rarely a marked decrease in blood pressure.
From the side of metabolism: often - increased levels of CK, hypertriglyceridemia, hyperuricemia; rarely - hyperkalemia.
On the part of the body as a whole: often - pain in the chest, influenza-like symptoms, peripheral edema; very rarely - asthenia, fatigue, malaise, drowsiness.
CONTRAINDICATIONS
- Obstruction of the biliary tract;
- renal failure (CC less than 20 ml / min), condition after kidney transplantation (no experience of clinical use);
- deficiency of lactase, galactosemia or malabsorption syndrome;
- Pregnancy;
- lactation period;
- age under 18 years (efficiency and safety not established);
- Hypersensitivity to the active substance or to any of the excipients that make up the preparation.
Caution should be applied to the drug in the following conditions or diseases:
- stenosis of the aortic or mitral valves;
- hypertrophic obstructive cardiomyopathy;
- primary aldosteronism;
- Hyperkalemia, hyponatremia (risk of dehydration, arterial hypotension, renal failure);
- renal failure (CC more than 20 ml / min);
- Chronic heart failure;
- bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney;
- IHD;
- cerebrovascular diseases;
- Older age (over 65 years);
- impaired liver function;
- Conditions accompanied by a decrease in BCC (including diarrhea, vomiting), as well as with a diet with sodium restriction;
- simultaneous use with diuretics.
PREGNANCY AND LACTATION
The experience of using olmesartan medoxomil in pregnant women is absent. However, in view of the available reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, like any medicinal product of this class, olmesartan is contraindicated during pregnancy. In the case of pregnancy during treatment with Cardosal В®, the drug should be discarded.
There is no data whether olmesartan is excreted in breast milk, so if you need Cardosal В® during lactation, breastfeeding for the period of taking the drug should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution in the violation of kidney function, with CC <20 ml / min - is contraindicated.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: a violation of the liver.
APPLICATION IN ELDERLY PATIENTS
Contraindicated in old age (over 65 years).
SPECIAL INSTRUCTIONS
Symptomatic arterial hypotension, especially after taking the first dose of the drug, can occur in patients with reduced BCC and / or reduced sodium levels due to intensive diuretic therapy, restricting salt intake from food in dietary nutrition, and also due to diarrhea or vomiting. Corresponding factors should be eliminated before using Cardosal В® .
In patients whose vascular tone and renal function depend to a large extent on the activity of RAAS (for example, in patients with severe chronic heart failure or renal dysfunction, including renal artery stenosis), treatment with other drugs acting on this system is associated with the possibility of developing acute arterial hypotension, azotemia, oliguria, or, in rare cases, acute renal failure. The possibility of a similar effect can not be ruled out with the use of angiotensin II receptor antagonists.
There is an increased risk of severe arterial hypotension and renal failure if a patient with bilateral stenosis of the renal arteries or stenosis of the artery of a single functioning kidney receives therapy with drugs that affect RAAS.
When using Cardosal В® in patients with impaired renal function, it is recommended that periodic monitoring of serum levels of potassium and serum creatinine is recommended. The experience of using Cardosal В® in patients with recent kidney transplantation or in patients with the last stage of renal dysfunction (eg, KC less than 12 ml / min) is absent.
As with other antagonists of angiotensin II receptors and ACE inhibitors, hyperkalemia may develop in the treatment with Cardosal В® if the patient suffers from impaired renal function and / or chronic heart failure. Patients at this risk group should be monitored for serum potassium levels.
As with other angiotensin II receptor antagonists, a combination of lithium preparations and Cardosal В® is not recommended .
As in the case of other angiotensin II receptor antagonists, in Negroid patients suffering from hypertension, the effectiveness of Cardosal В® therapy is slightly lower than in patients of other races.
As with any antihypertensive drug, excessive BP reduction in patients with IHD or with cerebrovascular insufficiency can lead to myocardial infarction or stroke.
Impact on the ability to drive vehicles and manage mechanisms
The influence of Cardosal В® on the ability to drive vehicles and control mechanisms has not been studied, therefore, during the treatment with Cardosal В® , caution should be exercised when driving vehicles and engaging in potentially dangerous activities requiring increased concentration and speed of psychomotor reactions (dizziness and weakness are possible).
OVERDOSE
Symptoms: marked decrease in blood pressure.
Treatment: with a marked decrease in blood pressure, it is recommended to put the patient on his back, lifting his legs. Recommended gastric lavage and / or reception of activated charcoal, therapy aimed at correcting dehydration and disturbances of water-salt metabolism, replenishment of BCC.
DRUG INTERACTION
It is not recommended to use together with potassium-sparing diuretics, potassium preparations, substitutes for salts containing potassium, or other drugs that can raise the level of potassium in the blood serum (for example, heparin), this can lead to an increase in serum potassium levels.
The antihypertensive effect of olmesartan therapy can be enhanced when combined with other antihypertensive agents.
NSAIDs, including acetylsalicylic acid in doses greater than 3 g / day, as well as COX-2 inhibitors, and angiotensin II receptor antagonists can act synergistically, reducing glomerular filtration. With the simultaneous use of NSAIDs and angiotensin II receptor antagonists, there may be a risk of developing acute renal failure, so it is recommended that kidney function be monitored at the beginning of treatment and that a sufficient amount of fluid is taken regularly. However, simultaneous treatment can reduce the antihypertensive effect of angiotensin II receptor antagonists, leading to a partial loss of their therapeutic effectiveness.
When used simultaneously with antacids (magnesium and aluminum hydroxide), a moderate decrease in the bioavailability of olmesartan is possible.
There have been reports of a reversible increase in serum lithium concentration and toxicity during simultaneous use of lithium drugs with ACE inhibitors and with angiotensin II receptor antagonists, so the use of olmesartan medoxomil in combination with lithium preparations is not recommended . If appropriate combination therapy is necessary, regular monitoring of serum lithium levels is recommended.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years. Do not use after the expiry date printed on the package.
