Olimestra

Olimeters is a means of blocking the receptors of the substance angiotensin II.

Indications of the olimestra

It is used at an increased level of blood pressure of the essential type.

Release form

The release occurs in tablets with a volume of 10 or 20 mg. Inside the blister cell there are 14 such tablets. In a pack - 2 or 4 blister plates. Also, 15 tablets can be produced inside the blister, 2 or 4 blister packs per pack.

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

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Pharmacodynamics

Medoxomil Olmesartan is a potent and active selective antagonist of the conductors of angiotensin 2 (form of AT1), which is taken orally. Perhaps this component slows down any exposure to angiotensin 2 mediated by the AT1 receptor, regardless of the source, as well as the way of binding angiotensin 2. Selective antagonism of AT1 angiotensin 2 conductors causes an increase in plasma values of renin, as well as angiotensin 1 and 2, and in addition to this slightly reduces the plasma level of aldosterone.

Angiotensin 2 is the main vasoactive hormone of renin-angiotensin. He is an important participant in the pathophysiological processes occurring at an elevated level of blood pressure, caused by the action of AT1 receptors.

With increased blood pressure, the drug contributes to a long-term decrease in these values (the effectiveness depends on the size of the portion of the drug). Information on the pathological decrease in the level of blood pressure after the use of the first dose of the drug there. There is also no information about the development of tachyphylaxis after prolonged therapy or withdrawal syndrome due to withdrawal of drugs.

A single dose of the drug for a day provides a gentle and effective reduction in blood pressure, which continues for 24 hours. A single dose demonstrates a decrease in the level of blood pressure, similar to the one that occurs when you use a total daily dose of 2 doses.

After prolonged therapy, the level of blood pressure decreased as much as possible after 8 weeks from the start of treatment, but the main part of the hypotensive effect was observed after 2 weeks of the course. When used in conjunction with hydrochlorothiazide, there is an additional decrease in the values of blood pressure, and the joint method is tolerated without complications.

Pharmacokinetics

Absorption and distribution.

Olimestra is a prodrug that quickly converts to a drug-active degradation product of olmesartan. This happens with the participation of intra-portal blood and intestinal mucous esterases in the process of absorption of drugs from the gastrointestinal tract.

Inside the plasma or excretion products, there was no undissolved active substance or unchanged side compound of the medoxomil category. The mean absolute bioavailability index of the metabolite olmesartan from the drug pill is 25.6%.

The average peak values of the active component inside the plasma are observed after 2 hours after the drug is consumed. Plasma values increase almost linearly with an increase in a single oral dose to 80 mg.

Food almost does not affect the level of bioavailability of the metabolite, which allows you to take the medicine regardless of eating.

Protein synthesis of the active component within the plasma is equal to 99.7%, but the potential for a significant level of protein binding during the interaction of drugs with other drugs with a high protein synthesis index remains low (this can be confirmed by the absence of a drug-marked interaction Olimeters with warfarin, as well as medoxomil). Synthesis of olmesartan with blood cells is rather weak. The average value of the distribution volume for IV injection is also quite low - in the range of 16-29 liters.

Metabolic processes and excretion.

The total level of plasma clearance is 1.3 l / h (19%). It is rather slow in comparison with the values of hepatic blood flow (about 90 l / h).

With a single use of a portion of a 14C-labeled active substance, 10-16% of the administered radioactive component is excreted in the urine (most of it within 24 hours after ingestion), and the rest of the reconstituted radioactive element is excreted with feces.

Given the systemic availability of a part of 25.6%, it is possible to deduce that after absorption, olmesartan is excreted both through the kidneys (about 40%) and by the liver with the ZHVP (approximately 60%). The entire recovered radioactive part is an element of olmesartan. No significant degradation products are found inside the body. Recirculation of the substance inside the intestine and liver is minimal.

The final half-life of olmesartan is within 10-15 hours with multiple use. Stable values reach after using the first few servings, cumulation after a 2-week admission is not noted. Kidney clearance is approximately 0.5-0.7 l / hour and does not depend on the size of the portion.

Dosing and administration

The size of the initial portion is 10 mg, which must be taken once per day. People who do not have an adequate reduction in blood pressure after this dose is allowed to increase it to the optimal size - a one-time intake of 20 mg per day. If there is a need for an additional reduction in blood pressure, the size of the drug can be increased to 40 mg per day (this is the maximum allowable dose per day) or supplemented with hydrochlorothiazide.

The maximum antihypertensive effect of the drug is demonstrated after 8 weeks after the start of treatment, but a marked decrease in blood pressure values is observed after 2 weeks of therapy. It is necessary to take this fact into account when adjusting the dosing schedule for any patient.

To comply with the therapeutic regimen, you should use the medication at approximately the same time every day. Reception is not dependent on eating, so you can take the pill, for example, with breakfast.

In the disorder of renal activity.

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

Persons with severe form of disorder (CC level is <20 ml / minute) are prohibited from appointing OliMestr, because for this category of patients there is too little information on the use of this remedy.

In the disorder of hepatic activity.

People with a mild degree of impairment do not need to change their dosage. With a moderate form of the disorder, one must first take 10 mg of the drug per day, and the maximum daily dose is 20 mg. In addition, the values of blood pressure and kidney function should be carefully monitored in individuals with hepatic function disorders who also take diuretics or other antihypertensive drugs.

There is no experience of using the drug in people with severe stages of hepatic functional disorders, because of which it is not recommended to assign it to people from this category.

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Use of the olimestra during pregnancy

Olimestra can not be administered to pregnant women and women planning pregnancy. When diagnosing pregnancy during the use of this drug, you must immediately stop taking it, then replace it 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 reduced blood pressure values. It is recommended to perform ultrasound of the fetal skull, as well as its renal activity.

Due to the fact that there is no information on the use of medicines in lactating women, it should not be prescribed during lactation. It is recommended to use alternative drugs, the safety of which, when used by nursing mothers, was established.

Contraindications

The main contraindications:

• the presence of hypersensitivity to the active component of drugs or other elements of the drug;
• Obstruction in the area of GWP;
• appointment to children.

Side effects of the olimestra

Use of the medication occasionally can cause the appearance of certain side effects:

• defeat of systemic blood flow and lymph: development of thrombocytopenia;
• disorders of digestive processes and metabolism: development of hyperkalemia;
• manifestations of the organs of the National Assembly: occurrence of headaches or dizziness;
• violation of respiratory function: the appearance of cough;
• symptoms on the part of the digestive tract: the appearance of nausea, abdominal pain or vomiting;
• damage to the subcutaneous layer and skin surface: a rash or itching, as well as signs of allergy - urticaria, swelling on the face, dermatitis of an allergic nature and edema Quincke;
• disorders of the function of bones and muscles: the development of myalgia or the appearance of muscle cramps;
• violation in the work of the urethra and kidneys: a disorder of kidney function and kidney failure in the acute stage;
• systemic disorders: the appearance of a feeling of fatigue, inhibition, discomfort, the development of a lethargic state or asthenia;
• the results of laboratory tests: an increase in urea and creatinine in the blood, as well as indicators of liver enzymes.

Overdose

There is only limited information about the poisoning of the medicine. Most often, as a result of an overdose, there is a strong decrease in blood pressure. In this case, you need to carefully monitor the patient's condition, performing the procedures of supportive and symptomatic treatment.

There is no information on the withdrawal of the drug using the dialysis procedure.

Interactions with other drugs

The effect of other drugs on the drug.

Potassium-sparing diuretics and potassium supplements.

Given the experience of using other drugs that have an effect on the RAS, combined with potassium supplements, potassium-sparing diuretics, salt substitutes, which contain potassium, and other drugs that can increase the serum potassium values (among such heparin), potassium may be increased inside the blood serum. Because of this, combining these drugs is prohibited.

Other antihypertensive medication.

Antihypertensive effects Oliesters can be potentiated in the case of combined use with other antihypertensive drugs.

Medicines NSAIDs.

NSAIDs (among them aspirin at a dosage> 3 g / day, and in addition, inhibitors of the element COX-2) together with antagonists of the conductors of angiotensin 2 are able to exert a synergistic effect (due to weakened glomerular filtration). When taking drugs from the category of antagonists of the angiotensin 2 element in combination with NSAIDs, there is a risk of developing kidney failure to an acute degree. It is required to constantly monitor the kidney activity at the initial stage of therapy, and in addition, to monitor all the time, so that the patient's body receives the required amount of fluid.

In addition, combined use with NSAIDs may reduce the hypotensive effect of angiotensin II conductor antagonists, leading to a partial loss of efficacy.

Other means.

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

The effect of the drug on other medications.

Lithium substances.

A reverse increase in serum lithium values, as well as an increase in toxicity, was noted with the combined use of a drug with ACE inhibitors. Because of this, it is forbidden to combine Olimestra with lithium. If such a connection is required, it is necessary to closely monitor the plasma values of lithium during the period of therapy.

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Storage conditions

Olimestra is stored in standard for medicinal substances conditions, in a place inaccessible to small children.

Special instructions

Reviews

Olimestra is considered a medicine with an excellent hypotensive effect - most reviews point out the high effectiveness of drugs.

But at the same time, many patients often complain about the development of side effects - pain in the sternum or a constant sense of weakness. Therefore, with the development of such manifestations, you should immediately consult your doctor.

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Shelf life

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