Expiration date: 10/2025
Clinico-pharmacological group
(Antagonist of angiotensin II receptor)
Release form, composition and packaging
1 tablet contains medoxomil olmesartan 10, 20 or 40 mg
Pharmacological action
Antagonist of the angiotensin II receptor (type AT1). Angiotensin II is the primary vasoactive hormone of the RAAS and plays an important role in the pathophysiology of hypertension by AT1-receptors. It is assumed that olmesartan blocks all effects of angiotensin II mediated by AT1-receptors regardless of the source or route of synthesis of angiotensin II.
In hypertension, olmesartan causes a dose-dependent long-lasting decrease in blood pressure. No evidence of development of arterial hypotension after the first dose of the drug, tachycardia during long-term treatment (for drugs Cardosa Cardosa 20 and 40) and on the development of the syndrome (sharp increase in blood pressure after discontinuation of the drug).
Welcome olmesartan medoxomil 1 time/day provides an effective and mild reduction of blood pressure within 24 h and the effect after a single dose is similar to the effect of the drug 2 times/day in the same daily dose.
Olmesartan antihypertensive effect usually develops after 2 weeks and the maximum effect develops after approximately 8 weeks after the start of therapy.
Pharmacokinetics
Absorption and distribution
Medoxomil olmesartan is a prodrug. It quickly turns into a pharmacologically active metabolite olmesartan under the action of enzymes in the intestinal mucosa and in portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil unchanged in plasma were not detected. The bioavailability of olmesartan is on average 25.6%. Cmax of olmesartan in plasma is on average reached after 2 h after administration of olmesartan medoxomil inside and increases approximately linearly with increasing single doses up to 80 mg.
Food intake does not have a significant effect on the bioavailability of olmesartan, olmesartan medoxomil so can be taken with or without food.
Clinically significant differences in pharmacokinetic indices of olmesartan in relation to gender is not revealed.
Olmesartan associated with blood plasma proteins (99.7%), but the potential for clinically significant displacement the magnitude of protein binding in the interaction of olmesartan with other wysokomazowiecki and simultaneously used drugs is low (this is corroborated by the absence of clinically significant interaction between warfarin and olmesartan). Communication with olmesartan blood cells is negligible.
Metabolism and excretion
The total plasma clearance is typically 1.3 l/h (coefficient of variation - 19%) is relatively low compared to hepatic blood flow (about 90 l/h). Renal excretion is approximately 40%, with bile - about 60%. Intrahepatic circulation olmesartan minimal. Since a large part of olmesartan is excreted via the liver, its use in patients with obstruction of the biliary tract is contraindicated.
T1/2 of olmesartan is 10-15 h after repeated oral administration. A significant effect of therapy is achieved after taking first few doses and after 14 days repeated application of a further cumulation is not observed. Renal clearance is approximately 0.5-0.7 l/h and not dependent on the dose of the drug.
Pharmacokinetics in special clinical cases
In patients with impaired renal function AUC at steady-state (stable) state was increased by approximately 62%, 82% and 179% in the case of mild, moderate and severe renal dysfunction, respectively, compared to healthy volunteers.
After a single oral AUC values for olmesartan were 6% and 65% higher in patients with mild-to-moderate degree of liver dysfunction, respectively, compared to healthy volunteers. The unbound fraction of olmesartan after 2 h after dose in healthy volunteers, in patients with mild and moderate degrees of liver dysfunction was 0.26%, 0.34% and 0.41%, respectively.
Dosage
It is recommended to take the drug was Cardeal inside every day at the same time regardless of meals 1 times/day.
The recommended starting dose for adults is 10 mg (1 tab. the drug was Catosal 10) 1 times/day. In case of insufficient blood pressure reduction in the drug dose of 10 mg/day, the dose may be increased to 20 mg/day (the drug use was Cardeal 20). If necessary, additional blood pressure lowering, the dose can be increased to a maximum of 40 mg/day (the drug use was Cardeal 40), or it can be assigned to a diuretic (hydrochlorothiazide). Maximum daily dose of 40 mg.
Overdose
Symptoms: expressed lower AD.
Treatment: in severe decrease in blood pressure, it is recommended to lay the patient on the back, lift the legs. Recommended gastric lavage and/or administration of activated charcoal, therapy aimed at correction of dehydration and violations of water-salt metabolism, fill the BCC.
Drug interactions
Not recommended concomitant use of potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium, or other drugs that can increase potassium levels in the blood serum (e.g. heparin) may lead to increased levels of potassium in the blood serum
The antihypertensive effect of therapy olmesartan can be enhanced by combined use with other antihypertensive agents.
NSAIDs, including acetylsalicylic acid in doses over 3 g/day and also COX-2 inhibitors and antagonists of angiotensin II receptors can act synergistically, reducing glomerular filtration. While the use of NSAID and antagonists of the angiotensin II receptor can occur the risk of acute renal failure, so it is recommended to monitor renal function at the beginning of treatment, and regular intake of sufficient amounts of fluid. However, concomitant treatment can reduce antihypertensive effect of receptor antagonists of angiotensin II, resulting in partial loss of therapeutic effectiveness.
While the use of antacids (magnesium and aluminum hydroxide) may moderate reduction in bioavailability of olmesartan.
There are reports of a reversible increase of lithium concentration in serum and the expression of toxicity during simultaneous use of drugs lithium and ACE inhibitors and receptor antagonists of angiotensin II, therefore, the use of olmesartan medoxomil in combination the drug lithium is not recommended. If necessary, the use of an appropriate combination therapy is recommended regular monitoring of lithium level in blood serum.
Pregnancy and lactation
Experience with the use of olmesartan medoxomil in pregnant women is missing. However, because of the reports of severe teratogenicity of drugs, acting directly on the renin-angiotensin system, like any drug of this class, olmesartan contraindicated during pregnancy. In the case of pregnancy during therapy with the drug was Catosal the drug should be stopped.
No data is allocated if olmesartan breast milk, so if you need the use of the drug was Cardeal lactation breastfeeding at the period of the drug should be discontinued.
Side effects
Possible side effects listed below in descending frequency of occurrence: very often (>, 1/10), often (>, 1/100 of < 1/10), sometimes (>, 1/1000, <, 1/100), rarely (>, 1/10 000, <, 1/1000), very rare (<, 1/10 000), including individual messages.
With the hematopoietic system: rarely - thrombocytopenia.
CNS: rarely - dizziness, rarely - headache.
The respiratory system: often - pharyngitis, rhinitis very rare cough, bronchitis.
From the digestive system: often - diarrhea, dyspepsia, gastroenteritis, very rare - abdominal pain, nausea, vomiting.
With the skin: rarely - itching, rash, angioedema, allergic dermatitis, urticaria.
From the side of musculoskeletal system: often - back pain, bone pain, arthralgia, arthritis, rarely - muscle cramps, myalgia.
From the urinary system: often - hematuria, urinary tract infection, very rarely - acute renal failure.
From the laboratory parameters: very rarely - increased creatinine and urea in blood serum, increased activity of liver enzymes.
Of the cardiovascular system: sometimes- angina, tachycardia, rarely - expressed lower AD.
From the metabolic: often - the increase in CPK level, hypertriglyceridemia, hyperuricemia, rarely - hyperkalemia.
From the body as a whole: often - pain in the chest, flu-like symptoms, peripheral edema, rarely - asthenia, fatigue, malaise, somnolence.
Terms and conditions storage
The drug should be stored out of reach of children at temperature not exceeding 30°C. shelf Life - 3 years. Do not use after the expiry date printed on the package.
Testimony
— essential hypertension.
Contraindications
— obstruction of biliary tract,
— renal failure (KK less 20 ml/min), condition after kidney transplantation (no experience of clinical application),
— lactase deficiency, galactosemia or malabsorption syndrome,
— pregnancy,
— lactation,
— the age 18 years (effectiveness and safety have not been established),
— hypersensitivity to the active substance or to any of the excipients included in the drug.
With caution the drug should be used under the following conditions or diseases:
— stenosis of the aortic or mitral valves
— hypertrophic obstructive cardiomyopathy,
— primary aldosteronism,
— hyperkalemia, hyponatremia (the risk of dehydration, arterial hypotension, renal failure),
— renal impairment (CC 20 ml/min),
— chronic heart failure,
— bilateral renal artery stenosis or stenosis of artery only kidneys,
— Coronary heart disease,
— cerebrovascular disease,
— elderly age (over 65 years),
— abnormal liver function,
— state, accompanied by a decrease in BCC (W. diarrhea, vomiting), as well as in the diet with restriction of sodium,
— concomitant use of diuretics.
Special instructions
Symptomatic hypotension, especially after the first dose of the drug can occur in patients with reduced BCC and/or a reduced level of sodium due to intensive diuretic therapy, limit salt intake from food in the diet, as well as due to diarrhea or vomiting. Relevant factors should be eliminated before the application of drug was Cardeal.
In patients whose vascular tone and renal function depend to a large extent on the activity of the RAAS (e.g., patients with severe chronic heart failure or impaired renal function, including renal artery stenosis), treatment with other drugs acting on this system due to the possibility of development of acute hypotension, azotemia, oliguria or, in rare cases, acute renal failure. The possibility of similar action cannot be ruled out with the use of antagonists of angiotensin II receptors.
There is an increased risk of severe arterial hypotension and renal failure if the patient with bilateral renal artery stenosis or stenosis of the artery only functioning kidney is receiving therapy with drugs affecting the RAAS.
In applying the drug was Cardonal in patients with impaired renal function it is recommended to conduct a periodic monitoring of potassium and creatinine in serum. The experience of the drug was Cardonal in patients with a recent kidney transplant or in patients with end-stage of renal dysfunction (for example, the spacecraft is less than 12 ml/min).
As in the case of other receptor antagonists of angiotensin II and ACE inhibitors, in the treatment of drug has Catosal can develop hyperkalemia if the patient suffers from impaired renal function and/or congestive heart failure. In patients of this risk group is recommended to control the level of potassium in the blood serum.
As in the case of other antagonists of the angiotensin II receptor, is not recommended combination of drugs lithium and drug was Cardeal.
As in the case of other antagonists of the angiotensin II receptor, in patients of black race, hypertension, efficiency of drug therapy was Cardeal slightly lower than in patients of other races.
As with any antihypertensive agents, excessive blood pressure decrease in patients with coronary artery disease or cerebrovascular insufficiency can lead to myocardial infarction or stroke.
Effects on ability to drive vehicles and management mechanisms
The effect of the drug was Cardeal on the ability to drive vehicles and management mechanisms have not been studied, so the period of drug treatment was Cardeal be careful when driving vehicles and activities potentially hazardous activities, require high concentration and psychomotor speed reactions (dizziness and weakness).
Use in impaired renal function
With caution in impaired renal function, with QC < 20 ml/min - contraindicated.
Use in hepatic impairment
Caution: impaired liver function.
