Olmesartan medoxomil (Olmesartani medoxomilum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Angiotensin II receptor antagonists (AT1 subtype)

Included in the formulation
  • Cardosal® 10
    pills inwards 
    Berlin-Chemie / Menarini Pharma, GmbH     Germany
  • Cardosal® 20
    pills inwards 
    Berlin-Chemie / Menarini Pharma, GmbH     Germany
  • Cardosal® 40
    pills inwards 
    Berlin-Chemie / Menarini Pharma, GmbH     Germany
    • АТХ:

    C.09.C.A.08   Olmesartan medoxomil

    Pharmacodynamics:

    The drug is an angiotensin receptor blocker II, mainly angiotensin receptors II first type. Suppresses mediated through AT1-receptors effects of angiotensin II (including such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, increased reabsorption of sodium in the kidneys).

    Pharmacokinetics:

    Olmesartan medoxomil is a prodrug. During the suction process from GIT It is hydrolyzed and quickly and completely converted into a pharmacologically active form - olmesartan. Absolute bioavailability of olmesartan is approximately 26%, food intake does not significantly affect bioavailability. After oral administration Cmax Olmesartan in the blood plasma is achieved within 1-2 hours.Communication of the drug with plasma proteins is 99.7%, the half-life is 10-15 hours, excreted by the kidneys (40%) and the gastrointestinal tract (60%). Do not cumulate.

    Indications:

    Essential arterial hypertension.

    ICD-10

    IX.I10-I15.I10   Essential [primary] hypertension

    IX.I10-I15.I15   Secondary Hypertension

    Contraindications:

    Pregnancy and lactation, biliary tract obstruction, age under 18, kidney failure (clearance creatinine less than 20 ml / min), condition after kidney transplantation (no clinical experience), bile duct obstruction, lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome.

    Carefully:

    Stenosis of aortic and mitral valves, obstructive hypertrophic cardiomyopathy, chronic heart failure, kidney disease, bilateral stenosis of the renal arteries or stenosis of the single kidney artery, primary hyperaldosteronism, hyperkalemia, hyponatremia (risk of dehydration, arterial hypotension, renal failure), coronary heart disease, cerebrovascular disease, age 65 years, liver dysfunction, volume of circulating blood (including diarrhea, vomiting), as well as a diet with sodium restriction; simultaneous use with diuretics.

    Pregnancy and lactation:

    Category FDA - D. The drug is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Orally, regardless of food intake, the first dose is 10 mg per day, then the dose can be increased to 20 mg per day. The maximum dose is 40 mg per day.

    Side effects:

    From the musculoskeletal system: pain in the back, arthritis, bone pain, myalgia, muscle cramps, increased activity of creatine kinase.

    From the cardiovascular system: angina pectoris, arterial hypotension, thrombocytopenia.

    From the nervous system: dizziness, vertigo, asthenic syndrome, headache.

    From the digestive system: increased activity of hepatic transaminases, dyspepsia, nausea, gastroenteritis, vomiting, nausea.

    From the skin: urticaria, itching, rash, angioedema, allergic dermatitis, edema of the face.

    From the urinary system: urinary tract infection, hematuria.

    From the respiratory system: pharyngitis, cough, rhinitis, bronchitis.

    From the side of metabolism: hyperuricemia, hyperkalemia, hypertriglyceridemia.

    Other: influenza-like symptoms, pain in the chest.

    Overdose:

    Symptoms: marked reduction in blood pressure, tachycardia.

    Treatment: with a pronounced decrease blood pressure it is recommended to put the patient on his back and lift his legs. Recommended gastric lavage and / or reception of activated charcoal, therapy aimed at correcting the dehydration and disturbances of water-salt metabolism, replenishment of the volume of circulating blood.

    Interaction:

    With the simultaneous use of olmesartan medoxomil with lithium preparations, the toxicity of the latter increases (the combination is not recommended).

    The risk of hyperkalemia increases with simultaneous application olmesartan medoxomil with potassium-sparing diuretics, drugs containing potassium, or with other drugs that can cause a rise in serum potassium levels, for example, with heparin (a combination is not recommended).

    When the drug is used with other drugs that have an antihypertensive effect, the hypotensive effect increases.

    Nonsteroidal anti-inflammatory drugs reduce the hypotensive effect of the drug. Olmesartan medoxomil and acetylsalicylic acid in a dose of more than 3 g in day can act synergistically by reducing glomerular filtration. With the simultaneous use of selective inhibitors COX-2 and acetylsalicylic acid in a dose of more than 3 g in day there is a risk of acute renal failure. At the beginning of therapy it is recommended to evaluate the function of the kidneys, and also to correct the disturbances of the water-electrolyte balance. In addition, with simultaneous use with acetylsalicylic acid at a dose of more than 3 g in day it is possible to weaken the hypotensive effect of olmesartan medoxomil.

    Antacids (magnesium and aluminum hydroxide) reduce the bioavailability of the drug.

    Special instructions:

    Impact on the ability to drive vehicles and manage mechanisms

    The drug may cause dizziness, increased fatigue. Do not administer the vehicle during the administration of the drug or perform work that requires concentration of attention.

    Instructions
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