Cardosal 20, pills 20mg, 28pcs

Composition

Active ingredients:

olmesartan medoxomil 2.0 mg.

Auxiliary substances:

microcrystalline cellulose-20 mg,

low-substituted hyprolose-40 mg,

lactose monohydrate-123.2 mg,

hyprolose 6-10 MPa*s-5 mg,

magnesium stearate-1.8 mg.

Composition of the film shell:

hypromellose 5 MPa × s – 5.76 mg,

talc-1.12 mg,

titanium dioxide (E 171) – 1.12 mg

Pharmacological action

Angiotensin II receptor antagonist (type AT1). Angiotensin II is the primary vasoactive hormone of RAAS and plays a significant role in the pathophysiology of arterial hypertension via AT1 receptors. It is assumed that olmesartan blocks all the effects of angiotensin II mediated by AT1 receptors, regardless of the source and pathway of angiotensin II synthesis.

In arterial hypertension, olmesartan causes a dose-dependent prolonged decrease in blood pressure. There is no evidence for the development of hypotension after the first dose of the drug, tachycardia during long-term treatment (for the drugs Cardosal ® 20 and Cardosal® 40) and the development of withdrawal syndrome (a sharp increase in blood pressure after discontinuation of the drug).

Taking olmesartan medoxomil 1 time/day provides an effective and gentle reduction 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.

The antihypertensive effect of olmesartan develops, as a rule, after 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.

Pharmacokinetics

Suction and distribution

Olmesartan medoxomil is a prodrug. It is rapidly converted to the pharmacologically active metabolite olmesartan by enzymes in the intestinal mucosa and portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil was not detected unchanged in the blood plasma. The bioavailability of olmesartan is on average 25.6%. Cmax of olmesartan in blood plasma is reached on average 2 hours after oral use of olmesartan medoxomil and increases approximately linearly with an increase in a single dose to 80 mg.

Food intake does not significantly affect the bioavailability of olmesartan, so olmesartan medoxomil can be taken regardless of food intake.

There were no clinically significant differences in the pharmacokinetic parameters of olmesartan depending on gender.

Olmesartan binds to plasma proteins (99.7%), but the potential for a clinically significant shift in the value of protein binding in the interaction of olmesartan with other highly binding and simultaneously used drugs is low (this is confirmed by the absence of a clinically significant interaction between olmesartan and warfarin). The association of olmesartan with blood cells is insignificant.

Metabolism and elimination

Total plasma clearance is usually 1.3 l / h (coefficient of variation-19%) and is relatively low compared to hepatic blood flow (approximately 90 l/h). Renal excretion is approximately 40%, with bile-about 60%. Intrahepatic circulation of olmesartan is minimal. Since most of olmesartan is excreted through the liver, its use in patients with biliary tract obstruction is contraindicated.

T1 / 2 of olmesartan is 10-15 hours after repeated oral use. A significant effect of therapy is achieved after taking the first few doses of the drug, and after 14 days of repeated use, further accumulation is not observed. Renal 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, the steady-state AUC was increased by approximately 62%,82%, and 179% for mild, moderate, and severe renal impairment, respectively, compared with healthy volunteers.

After a single oral dose, 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 was 0.26%,0.34%, and 0.41%, respectively,2 hours after taking the drug dose in healthy volunteers and in patients with mild and moderate hepatic impairment.

Indications

Essential arterial hypertension.

Use during pregnancy and lactation

There is no experience of using olmesartan medoxomil in pregnant women.

However, due to reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, like any drug in this class, olmesartan is contraindicated during pregnancy.

If pregnancy occurs during therapy with Cardosal®, the drug should be discontinued.

There is no data on whether olmesartan is excreted in breast milk, so if it is necessary to use Cardosal® during lactation, breastfeeding should be discontinued while taking the drug.

Contraindications

• Hypersensitivity to the Active ingredient or to any of the excipients included in the product;
• obstruction of the biliary tract;
• renal failure (CC less than 20 ml/min), condition after kidney transplantation (no clinical experience);
• lactase deficiency, galactosemia or malabsorption syndrome;
• pregnancy and lactation;
• age to 18 years (efficacy and safety not established).

With caution, the drug should be used in the following conditions or diseases: aortic or mitral valve stenosis; hypertrophic obstructive cardiomyopathy; primary aldosteronism; hyperkalemia, hyponatremia (risk of dehydration, hypotension, renal failure); renal failure (creatinine clearance greater than 20 ml/min); chronic heart failure; bilateral renal artery stenosis or stenosis of the artery of a single kidney; IHD; cerebrovascular diseases; elderly age (over 65 years); impaired liver function; conditions accompanied by a decrease in BCC (including diarrhea, vomiting), as well as when following a diet with sodium restriction; simultaneous use with diuretics.

Side effects

Possible side effects are listed below by 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 rare (

From the hematopoietic system: very rarely – thrombocytopenia.

From the central nervous system: sometimes-dizziness; very rarely-headache.

From the respiratory system: often-pharyngitis, rhinitis; very rarely-cough, bronchitis.

From the digestive system: often – diarrhea, dyspepsia, gastroenteritis; very rarely-abdominal pain, nausea, vomiting.

From the skin: very rarely-pruritus, rash, angioedema, allergic dermatitis, urticaria.

From 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.

From the side of laboratory parameters: very rarely-increased serum creatinine and urea, increased activity of liver enzymes.

From the cardiovascular system: sometimes-angina pectoris, tachycardia; rarely-a pronounced decrease in blood pressure.

From the side of metabolism: often-increased CPK levels, hypertriglyceridemia, hyperuricemia; rarely-hyperkalemia.

From the body as a whole: often – chest pain, flu – like symptoms, peripheral edema; very rarely-asthenia, fatigue, malaise, drowsiness.

Interaction

It is not recommended to use concomitantly with potassium-sparing diuretics, potassium preparations, salt substitutes containing potassium, or other drugs that can increase the level of potassium in the blood serum (for example, heparin), this may lead to an increase in the level of potassium in the blood serum.

The antihypertensive effect of olmesartan therapy may be enhanced when combined with other antihypertensive agents.

NSAIDs, including acetylsalicylic acid at doses greater than 3 g / day, as well as COX-2 inhibitors, and angiotensin II receptor antagonists can act synergistically, reducing glomerular filtration.

Concomitant use of NSAIDs and angiotensin II receptor antagonists may increase the risk of acute renal failure, so monitoring of renal function at the beginning of treatment is recommended, as well as regular intake of sufficient fluids. However, concomitant treatment may reduce the antihypertensive effect of angiotensin II receptor antagonists, leading to a partial loss of their therapeutic effectiveness.

When used concomitantly with antacids (magnesium and aluminum hydroxide), a moderate decrease in the bioavailability of olmesartan is possible.

There are reports of reversible increases in serum lithium concentrations and toxicity during concomitant use of lithium preparations with ACE inhibitors and angiotensin II receptor antagonists, so the use of olmesartan medoxomil in combination with lithium preparations is not recommended. If appropriate combination therapy is required, regular monitoring of serum lithium levels is recommended.

How to take it, course of use and dosage

It is recommended to take Cardosal® orally every day at the same time, regardless of food intake 1 time / day.

The recommended starting dose for adults is 10 mg (1 tablet of Cardosal® 10) 1 time / day. If there is insufficient reduction in 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® 20 may be used).

If an additional reduction in blood pressure is necessary, the dose of the drug can be increased to a maximum of 40 mg / day (Cardosal ® 40 may be used) or an additional diuretic (hydrochlorothiazide) can be prescribed. The maximum daily dose is 40 mg.

Overdose

Symptoms: marked decrease in blood pressure.

Treatment: with a marked decrease in blood pressure, it is recommended to lay the patient on his back, lifting his legs. Gastric lavage and/or use of activated charcoal, therapy aimed at correcting dehydration and disorders of water-salt metabolism, and BCC replenishment are recommended.

Special instructions

Symptomatic hypotension, especially after the first dose of the drug, may occur in patients with reduced BCC and / or reduced sodium levels due to intensive diuretic therapy, restriction of salt intake with dietary nutrition, as well as due to diarrhea or vomiting. These factors should be addressed before starting Cardosal®.

In patients whose vascular tone and renal function depend to a large extent on the activity of the RAAS (for example, in patients with severe chronic heart failure or impaired renal function, 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 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 stenosis of the artery to a single functioning kidney receives therapy with drugs that affect the RAAS.

When using Cardosal® in patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood serum. There is no experience of using Cardosal® in patients with a recent kidney transplant or in patients with late-stage renal impairment (for example, creatinine clearance less than 12 ml/min).

As with other angiotensin II receptor antagonists and ACE inhibitors, hyperkalemia may occur when treated with Cardosal if the patient suffers from impaired renal function and / or chronic heart failure. In patients of this risk group, monitoring of serum potassium levels is recommended.

As with other angiotensin II receptor antagonists, the combination of lithium and Cardosal is not recommended.

As with other angiotensin II receptor antagonists, the effectiveness of Cardosal therapy is slightly lower in black patients with arterial hypertension than in patients of other races.

As with any antihypertensive agent, excessive lowering of blood pressure in patients with CHD or cerebrovascular insufficiency can lead to myocardial infarction or stroke.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

The effect of Cardosal® on the ability to drive vehicles and operate mechanisms has not been studied, so during treatment with Cardosal®, caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (dizziness and weakness are possible).

Form of production

Tablets covered with a white film-coated color, round, biconvex, with the imprint “C 14” on one side, with a barely perceptible specific smell.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Olmesartan medoxomil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets