Food intake has no significant effect on the bioavailability of olmesartan, olmesartan medoxomil therefore can be taken regardless of meals. No clinically significant differences in pharmacokinetic parameters of olmesartan according to sex is not revealed.
Olmesartan is bound to plasma proteins (99.7%), but the potential for clinically significant displacement values ??of protein binding in the interaction with other vysokosvyazyvayuschimisya olmesartan and simultaneously applied drugs is low (proof of this is the lack of a clinically significant interaction between olmesartanom and warfarin). Contact omnadren olmesartan blood cells is negligible.
Metabolism and excretion: total plasma clearance typically 1,3 l / h (coefficient of variation – 19%) and is relatively low in comparison with the hepatic blood flow (about 90 l / h). Renal excretion is approximately 40%, with bile – about 60%. Intrahepatic circulation of olmesartan is minimal. Since most of olmesartan is output from the liver, its use in patients with biliary tract obstruction is contraindicated (see. Section Contraindications).
The half-life of olmesartan is 10-15 h. After repeated ingestion. The significant effect of treatment is achieved after administration of the first few doses, and after 14 days of repeated application further accumulation is observed. Renal clearance is approximately 0.5-0.7 l / h and is independent of dose.
In patients with impaired renal function, the area under the curve “concentration-time» (AUC) at steady state (steady) state has been increased by approximately 62, 82 and 179% for mild, moderate and severe renal impairment, respectively, compared with healthy volunteers.
After a single oral administration of olmesartan AUC values ??were 6 and 65% higher in patients with mild to moderate hepatic dysfunction, respectively, compared to healthy volunteers. Unbound fraction of olmesartan at 2 hours. After taking a dose of the drug in healthy volunteers, in patients with mild to moderate degrees of hepatic dysfunction was 0.26, 0.34 and 0.41%, respectively.
- Hypersensitivity to the active substance or to any of the excipients included in the formulation (see. section
obstruction of the biliary tract;
- renal impairment (creatinine clearance (CC) of less than 20 ml / min.), condition after kidney transplantation (no clinical experience);
- pregnancy, lactation;
- age of 18 years (effectiveness and safety have been established);
- lactase deficiency, galactosemia or malabsorption syndrome.
- stenosis of the aortic or mitral valves;
- hypertrophic obstructive cardiomyopathy; primary aldosteronism;
- hyperkalemia, hyponatremia (risk of dehydration, hypotension, renal failure);
- renal failure (creatinine clearance of more than 20 ml / min.); chronic heart failure;
- sided renal artery stenosis or stenosis of the artery to a solitary kidney;
- cardiac ischemia;
- cerebrovascular omnadren diseases;
- advanced age (over 65 years);
- abnormal liver function;
- state, accompanied by a decrease in circulating blood volume (including diarrhea, vomiting), as well as in patients on a diet with restriction of sodium;
- while the use of diuretics.
Pregnancy and breast-feeding
The experience of olmesartan medoxomil in pregnant women available. However, due to the available reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, as well as any drug in this class, olmesartan is contraindicated during pregnancy. In case of pregnancy during therapy with the drug Kardosal 10 to cancel.
No information is released whether olmesartan with breast milk, so if you need to use the drug Kardosal 10 during lactation breastfeeding while taking the drug should be discontinued.
Dosage and administration:
It is recommended to take into Kardosal 10 every day at the same time, regardless o. If necessary, an additional blood pressure lowering the dose can be increased to the maximum – 40 mg / day ) or can additionally be assigned to a diuretic (hydrochlorothiazide). The maximum daily dose – 40 mg.
Possible side effects are listed below in descending frequency of occurrence: very common (> 1/10); often (> 1/100 <1/10); sometimes (> 1/1000, <1/100); rare (> 1/10000, <1/1000); very rare (<1/10000), including isolated reports.
From the circulatory and lymphatic system Very rare: thrombocytopenia.
On the part of the central nervous system sometimes: . Dizziness Very rare: headache.
The respiratory system Common: pharyngitis, rhinitis. Very rare: cough, bronchitis.
On the part of the digestive tract Common: diarrhea, indigestion, gastroenteritis. Very rare: abdominal omnadren pain, nausea, vomiting.
For the skin Very rare: pruritus, rash, angioedema, allergic dermatitis, urticaria.
On the part of the musculoskeletal system often: . Back pain, bone pain, arthralgia, arthritis Very rare: muscle cramps, myalgia.
On the part of the system mochevydelitepnoy Often: haematuria, urinary tract infection. Very rare: acute renal failure.
From the laboratory parameters Very rare: increase in serum creatinine and urea in serum, elevated liver enzymes.
Cardio-vascular system Rare: excessive blood pressure reduction. Sometimes: angina pectoris, tachycardia.
On the part of metabolism Common: increase in creatine phosphokinase, hypertriglyceridaemia, hyperuricaemia. Rare: hyperkalemia.
Other disorders Common: chest pain, flu-like symptoms, peripheral edema. Very rare: asthenia, fatigue, malaise, drowsiness.
Symptoms: marked reduction of blood pressure. Treatment: In marked decrease in blood pressure is recommended to put the patient on his back, raised his legs. It is recommended gastric lavage and / or administration of activated charcoal, therapy aimed at correcting dehydration and violations of water-salt metabolism, replenishment of circulating blood volume.
Interaction with other drugs
Not recommended combined use of potassium-sparing diuretics, drugs potassium salt substitute containing potassium, or other agents capable of enhancing the level of potassium in the serum (e.g., heparin), it may increase the level of potassium in the serum (section Special sm. instructions).
The antihypertensive effect of the therapy olmesartanom can be enhanced by the combined use with other antihypertensives.
Nonsteroidal anti-inflammatory drugs (NG1VP), including aspirin doses of more than 3 g / day, and the cyclooxygenase-2 (COX-2), and angiotensin II receptor antagonists may act synergistically to decrease glomerular filtration. With simultaneous use of NSAIDs and angiotensin II receptor antagonists may be a risk of developing acute renal failure, therefore monitoring of renal function is recommended at the start of treatment, and regular intake of adequate amounts of fluid. However, simultaneous treatment can reduce the antihypertensive effect of angiotensin II receptor antagonists, resulting in a partial loss of therapeutic effectiveness.
In an application with antacids (magnesium and aluminum hydroxide) may moderate decrease in the bioavailability of olmesartan.
There are reports of reversible increases in lithium serum concentration and toxicity during the simultaneous application of lithium products with angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor antagonists, therefore, the use of olmesartan medoxomil in combination with lithium therapy is not recommended (see. Section Special instructions). If necessary, the application of the appropriate combination therapy recommended regular monitoring of lithium levels in blood serum. Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.