Olimestra

Olimestra is an angiotensin II receptor blocker.

Indications Olimestra

It is used for elevated blood pressure of the essential type.

Release form

The drug is produced in tablets of 10 or 20 mg. There are 14 such tablets inside a blister cell. There are 2 or 4 blister plates in a pack. It can also be produced with 15 tablets inside a blister, 2 or 4 blister packs in a pack.

It is also produced in tablets of 40 mg, in the amount of 7 pieces inside a blister plate. The package contains 4 or 8 such blisters. They also produce 10 tablets inside a blister cell, 3 or 6 such blisters inside a pack.

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Pharmacodynamics

Olmesartan medoxomil is a potent and active orally selective angiotensin 2 (AT1 form) antagonist. It is possible that this component inhibits all AT1 receptor-mediated angiotensin 2 actions, regardless of the source or the angiotensin 2 binding pathway. Selective antagonism of the AT1 angiotensin 2 pathway results in increases in plasma renin and angiotensin 1 and 2 levels, and a small decrease in plasma aldosterone levels.

Angiotensin 2 is the main vasoactive hormone of the renin-angiotensin system. It is an important participant in the pathophysiological processes that occur at elevated blood pressure levels, caused by the action of AT1 receptors.

With increased blood pressure, the drug promotes a long-term reduction of these values (the effectiveness depends on the size of the drug dose). There is no information on a pathological decrease in blood pressure after taking the first dose of the drug. There is also no data on the development of tachyphylaxis after prolonged therapy or withdrawal syndrome as a result of drug withdrawal.

A single dose of the drug per day provides a gentle and effective reduction in blood pressure readings that lasts for 24 hours. A single dose demonstrates a reduction in blood pressure similar to that which occurs when taking the total daily dose in 2 doses.

After prolonged therapy, the blood pressure level decreased maximally after 8 weeks from the start of treatment, but the main part of the hypotensive effect is noted after 2 weeks of the course. When used in combination with hydrochlorothiazide, an additional decrease in blood pressure values is noted, and the combined use is tolerated without complications.

Pharmacokinetics

Absorption and distribution.

Olimestra is a prodrug that is rapidly converted into the medicinally active breakdown product olmesartan. This occurs with the participation of esterases located in the portal blood and intestinal mucosa during the absorption of the drug from the gastrointestinal tract.

No intact active substance or unchanged medoxomil-category side chain was detected in plasma or excretory products. The mean absolute bioavailability of the olmesartan metabolite from the tablet was 25.6%.

Average peak values of the active ingredient in plasma are observed after 2 hours of drug administration. Plasma values increase almost linearly with an increase in a single oral dose up to 80 mg.

Food has almost no effect on the bioavailability of the metabolite, which allows the drug to be taken regardless of food intake.

Protein synthesis of the active component inside the plasma is 99.7%, but the potential for a significant shift in the protein binding level for therapy during the interaction of the drug with other drugs that have a high synthesis rate with proteins remains low (this can be confirmed by the absence of a noticeable drug interaction of Olimestra with warfarin, as well as medoxomil). Synthesis of olmesartan with blood cells is quite weak. The average value of the distribution volume with intravenous injection is also quite low - within 16-29 liters.

Metabolic processes and excretion.

The total plasma clearance rate is 1.3 l/h (19%). This is quite slow compared to the hepatic blood flow values (approximately 90 l/h).

When a single dose of 14C-labeled active substance is administered, 10-16% of the administered radioactive component is excreted in the urine (most of it within 24 hours after administration), and the remaining part of the restored radioactive element is excreted in the feces.

Considering the systemic availability of the fraction of 25.6%, it can be concluded that after absorption, olmesartan is excreted both via the kidneys (approximately 40%) and via the liver via the bile duct (approximately 60%). All recovered radioactive fraction is the element olmesartan. No significant decay products are found within the body. Recirculation of the substance within the intestine and liver is minimal.

The terminal half-life of olmesartan is within 10-15 hours with repeated use. Stable values are reached after the first few doses, accumulation after 2 weeks of use is not observed. Renal clearance is approximately 0.5-0.7 l/hour and does not depend on the dose size.

Dosing and administration

The initial dose is 10 mg, taken once a day. People who do not experience an adequate reduction in blood pressure after taking this dose are allowed to increase it to the optimal dose - a single dose of 20 mg per day. If there is a need for an additional reduction in blood pressure, the dose can be increased to 40 mg per day (this is the maximum permissible dose per day) or supplement the treatment with hydrochlorothiazide.

The drug demonstrates its maximum hypotensive effect 8 weeks after the start of treatment, but a noticeable decrease in blood pressure values is noted after 2 weeks of therapy. This fact must be taken into account when adjusting the dosage regimen for any patient.

To comply with the therapeutic regimen, the medicine should be taken at approximately the same time every day. The intake does not depend on food intake, so the tablet can be taken, for example, with breakfast.

In case of renal dysfunction.

People with mild to moderate renal impairment (with CC values within 20-60 ml/minute) can take no more than 20 mg once a day, because information on the use of higher doses in this category of patients is limited.

People with severe forms of the disorder (creatinine clearance level is <20 ml/minute) should not be prescribed Olimestra, because there is too little information about the use of this drug for this category of patients.

In case of liver dysfunction.

People with a mild degree of disorder do not need to change the dosage. In case of a moderate form of disorder, it is necessary to initially take a single dose of 10 mg of the drug per day, and the maximum daily dose is 20 mg. In addition, it is necessary to carefully monitor the blood pressure values and kidney function in people with liver dysfunction who are also taking diuretics or other antihypertensive drugs.

There is no experience of using the drug in people with severe stages of liver functional disorders, which is why it is not recommended to prescribe it to people in this category.

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Use Olimestra during pregnancy

Olimestra should not be prescribed to pregnant women or women planning pregnancy. If pregnancy is diagnosed during the period of using this drug, it should be stopped immediately and then replaced with another drug that is allowed to be taken by pregnant women.

Children whose mothers used drugs from this drug category should be carefully examined for decreased blood pressure. It is recommended to perform an ultrasound of the fetus's skull, as well as its renal function.

Since there is no information on the use of the drug in nursing women, it should not be prescribed during lactation. It is recommended to use alternative drugs whose safety for use in nursing mothers has been established.

Contraindications

Main contraindications:

• the presence of hypersensitivity to the active component of the drug or other elements of the drug;
• obstruction in the area of the gallbladder;
• assignment to children.

Side effects Olimestra

The use of the drug may occasionally cause the appearance of certain side effects:

• damage to the systemic blood flow and lymph: development of thrombocytopenia;
• digestive and metabolic disorders: development of hyperkalemia;
• manifestations of the nervous system: occurrence of headaches or dizziness;
• respiratory dysfunction: appearance of cough;
• symptoms from the gastrointestinal tract: the appearance of nausea, abdominal pain or vomiting;
• damage to the subcutaneous layer and surface of the skin: rash or itching, as well as signs of allergy - urticaria, swelling of the face, allergic dermatitis and Quincke's edema;
• disorders of bone and muscle function: development of myalgia or the appearance of muscle cramps;
• dysfunction of the urinary system and kidneys: renal dysfunction and renal failure in the acute stage;
• systemic disorders: the appearance of a feeling of fatigue, lethargy, discomfort, the development of a lethargic state or asthenia;
• Laboratory test results: increased blood urea and creatinine levels, as well as liver enzyme levels.

Overdose

There is limited information on drug poisoning. Most often, overdose results in a strong decrease in blood pressure. In this case, the patient's condition will need to be closely monitored, with supportive and symptomatic treatment procedures.

There is no information on the elimination of the drug by dialysis.

Interactions with other drugs

Effect of other drugs on the drug.

Potassium-sparing diuretics and potassium supplements.

Taking into account the experience of using other drugs that have an effect on the RAS, when combined with potassium supplements, potassium-sparing diuretics, salt substitutes that contain potassium, as well as other drugs that can increase serum potassium values (including heparin), an increase in potassium levels in the blood serum is possible. For this reason, combining these drugs is prohibited.

Other antihypertensive drugs.

The antihypertensive effect of Olimestra may be potentiated in case of combined use with other antihypertensive drugs.

NSAID drugs.

NSAIDs (including aspirin at a dosage of >3 g/day, and also COX-2 inhibitors) together with angiotensin 2 antagonists can have a synergistic effect (due to weakening of glomerular filtration). When taking drugs from the category of angiotensin 2 antagonists in combination with NSAIDs, there is a risk of developing acute renal failure. It is necessary to constantly monitor renal function at the initial stage of therapy, and in addition to this, constantly monitor that the patient's body receives the required amount of fluid.

In addition, combined use with NSAIDs may reduce the hypotensive effect of angiotensin 2 antagonists, leading to partial loss of effectiveness.

Other means.

When used together with antacids (aluminum/magnesium hydroxide), there is a moderate decrease in the bioavailability of the substance olmesartan.

The effect of the drug on other medications.

Lithium substances.

Reversible increases in serum lithium levels and increased toxicity have been observed with the combined use of the drug with ACE inhibitors. For this reason, combining Olimestra with lithium is prohibited. If such a combination is necessary, plasma lithium levels should be monitored very closely during therapy.

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Storage conditions

Olimestra is stored under standard conditions for medicinal substances, out of the reach of small children.

Special instructions

Reviews

Olimestra is considered a drug with an excellent hypotensive effect - most reviews note the high effectiveness of the drug.

But at the same time, many patients often complain about the development of side effects - chest pain or a constant feeling of weakness. Therefore, if such symptoms develop, you must immediately consult your doctor.

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Shelf life

Olimestra can be used for 3 years from the date of release of the drug.