Cardosal (the international name is Olmesartan Medoxomil) is an antagonist of angiotensin II receptors (type AT1), the primary vasoactive hormone of RAAS, which is associated with the development of essential hypertension.
The form of release of the drug, its components
The drug is available in tablets, which are coated. The main substance, which is medoxomil olmesartan, is used in the medicinal product ; tablets contain from 10 to 40 mg (“Cardosal 10”, “Cardosal 20”, “Cardosal 40”).
Additionally, magnesium stearate, microcrystalline cellulose, lactose monohydrate are added to the preparation. Hyprolose and low-substituted hyprolose are also used as auxiliary components. The shell is created from titanium dioxide with the addition of talc and hypromellose.
pharmachologic effect
It is assumed that the drug “Cardosal”, acting on the body, helps block the effects of angiotensin II mediated by AT 1 receptors. With hypertension, the drug reduces blood pressure, this effect persists for a long time. There is no data confirming the occurrence of hypotension after the first use of the initial dose of the drug and tachycardia due to prolonged therapy (Cardosal 20, Cardosal 40), the appearance of withdrawal syndrome, accompanied by a sharp increase in blood pressure.
The use of the drug once a day leads to a mild decrease in blood pressure. The necessary effect develops over 24 hours. Typically, a hypotensive effect is achieved on the fourteenth day of treatment, the maximum result is observed after therapy lasting about two months.
Pharmacokinetics
Absorption of the drug, its distribution
A drunk tablet quickly takes the form of a pharmacologically active metabolite in the intestine (due to the action exerted by enzymes) and in portal blood (during absorption from the digestive tract).
During therapy, the active substance in the unchanged form is not detected in the blood plasma. The average bioavailability is about 26%. The maximum level of the drug is detected on average two hours after its adoption, with an increase in dosage (single dose - 80 mg), it increases.
“Cardosal 40”, like drugs with a different dosage of the active ingredient, can be taken without focusing on the time of eating food. Eating almost no effect on bioavailability.
Communication with plasma proteins is almost complete and corresponds to 99.7%. However, with the simultaneous use of Kardosal with other highly binding medicines, it is significantly reduced.
The metabolism of the drug, its excretion from the body
Basically, the medicine is excreted by the liver (60%), the rest (40%) - by the kidneys. Intrahepatic circulation of the active substance is negligible. Since excretion is carried out mainly by the liver, treatment with the use of Cardosal Plus is prohibited if the patient has bile duct obstruction. After repeated use, the drug is partially excreted in an average of 12 hours. A good effect is observed after taking the drug in a dosage that corresponds to several doses of Cardosal. A significant effect is also present after fourteen days of therapy; further cumulation does not occur. A different dosage of the drug does not affect such an indicator as renal clearance, it ranges from 0.5 to 0.7 l / h (approximately).
Special Clinical Cases
In those patients who have been found to have impaired renal function (mild, moderate, severe), AUC rises by 62, 82, and 179% when the condition is stable.
For liver problems, expressed slightly and moderately, a single dose of the drug helps to increase AUC by 6 and 65%.
Indications
The purpose of the "Cardosal" means of use allows you to produce upon detection of essential arterial hypertension.
It is unacceptable to be treated with Cardosal during pregnancy. If pregnancy has occurred during therapy, drug withdrawal is necessary.
Due to the lack of data confirming the safety of treatment during breastfeeding, breast-feeding is stopped for the duration of treatment.
In order to be able to purchase "Cardosal" and begin to be treated with it, the doctor must write a prescription.
Contraindications
Contraindications include hypersensitivity to those substances that are included in the composition of the drug, children's age (less than 18 years), pregnancy, breastfeeding. In addition, tablets are not prescribed in the following cases:
- bile duct obstruction;
- the presence of malabsorption syndrome, galactosemia;
- lack of lactase;
- the period after the kidney transplant operation;
- renal failure with low QC (less than 20 ml / min).
"Cardosal" is a medicine that is prescribed with extreme caution to patients with the following conditions:
- Ischemic heart disease;
- aldosteronism (primary);
- disturbances in the liver;
- renal failure, in which QC exceeds 20 ml / min;
- stenosis, accompanied by damage to the mitral valve or aortic;
- heart failure chronic course;
- cerebrovascular disease;
- a diet accompanied by a limited intake of sodium;
- hyponatremia, hyperkalemia (there is a risk of renal failure, the development of hypotension or dehydration);
- conditions when bcc decreases, vomiting, diarrhea appear;
- stenosis affecting the arteries of a single kidney, bilateral stenosis, in which the renal arteries are affected;
- hypertrophic obstructive cardiomyopathy;
- age over 65 years;
- the need for diuretics.
Using Cardosal
"Cardosal" instructions for use recommend the use of 10 mg, which corresponds to the initial dose. With insufficient normalization of blood pressure per day, you need to use 20 mg of the drug. Exceeding a dose of 40 mg of the drug in one day is unacceptable. Every day, the medicine should be drunk once, at the same time. For patients who have kidney problems of mild or moderate severity, when the clearance is in the range from 20 to 60 ml / min, the maximum dose of “Cardosal” cannot be more than 20 mg. In cases where there is a need to enhance the effect obtained, a comprehensive treatment is performed (in addition to Cardosal, Hydrochlorothiazide is used).
Side effects
In the treatment with the drug "Cardosal" the instructions for use allow such side effects:
- negative reactions from the respiratory and digestive systems, the appearance of disorders in the musculoskeletal system, urinary tract and kidneys, a change in some laboratory parameters, the development of general disorders (such side effects often occur);
- the development of angina pectoris, the appearance of disorders affecting the nervous system (sometimes appear);
- changes in the work of the cardiovascular system, the development of hyperkalemia (rarely observed).
Side effects that occur very rarely after taking the cardosal medication, the instructions for use include:
- disorders in the hematopoietic system;
- cough;
- acute renal failure;
- skin problems
- asthenic syndrome;
- headache, dizziness;
- myalgia;
- convulsive conditions;
- nausea, accompanied by vomiting, pain in the abdomen;
- increase in the content of urea, creatinine in the blood;
- changes in the liver - increased activity of its enzymes.
Overdose
An overdose is possible, it is manifested by a pronounced decrease in blood pressure. In the case of such a result of treatment, regular monitoring of the patient is required. To eliminate the symptoms that accompany an overdose of Cardosal, doctors recommend that symptomatic treatment be performed as well as maintenance therapy to normalize blood pressure. In case of an overdose, the patient is placed on his back and his legs are raised. In addition, when using a large dose of the drug, it is recommended to perform gastric lavage, give a person activated charcoal. There is a need to replenish bcc, eliminate dehydration and restore the water-salt balance. There is no evidence of the possibility of excreting olmesartan medoxomil from the body through dialysis.
special instructions
In patients who, before starting therapy, were intensively treated with diuretics and adhered to a diet excluding salt intake, hypotension may occur due to the use of the first dose of the drug. The same result can be observed in patients who have experienced vomiting or diarrhea. The reason for this reaction of the body is a decrease in bcc. A side effect of this nature must be prevented. The risk of its occurrence should be considered before starting therapy.
If a person has impaired kidney function, it is important to periodically check such indicators as creatinine and potassium in the blood serum. The use of ACE inhibitors in patients who have been diagnosed with hyperaldosteronism (primary) is meaningless, therefore they are not prescribed the “Cardosal” agent (reviews show no reaction to ACE inhibitors).
It should be borne in mind that a strong decrease in blood pressure in patients with atherosclerosis, in which the cerebral vessels are affected, or with coronary heart disease can cause the development of dangerous conditions such as ischemic stroke or myocardial infarction.
If a person has to perform maintenance of technically complex mechanisms or drive a vehicle, it is important to know that taking “Cardosal” can cause a loss of well-being (fatigue, weakness, dizziness), although this rarely happens.
Due to the content of lactose in the medication, its administration is prohibited for patients with hereditary galactose intolerance. The same applies to patients with malabsorption syndrome of galactose and glucose, a deficiency in the body of lactase.
Interaction with other means
The doctor should write a prescription and find out if the patient is being treated with other means to prevent unwanted reactions of the body. It is not recommended to use Cardosalum and the following types of drugs at the same time:
- products containing potassium;
- salt substitutes in which potassium is present;
- potassium-sparing diuretics;
- medications that affect the level of potassium in the blood serum (increase this indicator).
An example of such a remedy is Heparin. It is able to influence the potassium content in the blood. If treatment with the Cardosal drug is not possible, the analogs make it possible to replace it.
An increase in the antihypertensive effect is observed when other antihypertensive drugs and NSAIDs are included in the composition of therapy, that is, with the implementation of complex treatment. Therapy with an integrated approach includes the use of COX-2 inhibitors, acetylsalicylic acid (daily dose - more than 3 g). The action of angiotensin II receptor antagonists can occur synergistically, affecting glomerular filtration by reducing it.
With the simultaneous use of drugs such as angiotensin II receptor antagonists and NSAIDs, there is a possibility of acute renal failure in a patient. For this reason, monitoring the condition of the kidneys at the initial stage of therapy should be performed regularly. With this treatment, you should definitely drink enough fluids. However, it is possible to reduce the severity of the antihypertensive effect, as a result of which there is a frequent deterioration in the effectiveness of therapy.
If Kardosal is used during treatment with antacids, namely aluminum and magnesium hydroxide, there is a risk of reducing the bioavailability of the active substance (moderate).
A reversible increase in serum lithium levels and the display of toxic properties have been reported as a result of the combined use of ACE inhibitors, angiotensin II receptor antagonists and agents containing lithium. In connection with such reports, the combined treatment with Cardosalom and drugs, one of the components of which is lithium, is not recommended. However, if such a need exists, monitoring of blood composition should be regular.
The cost of the medicine, analogues, reviews
When prescribing Kardosal tablets, the price does not suit all patients, so they are interested in the possibility of treatment using another, more profitable means. Cardosal containing 10 mg of the active ingredient can be purchased for 610 rubles, a drug containing 20 mg of the active ingredient for 756 rubles. "Cardosal", the price of which is approximately 860 rubles., Contains 40 mg of the main component.
As an analogue, when you need to choose another remedy for the implementation of therapy, instead of “Cardosal” you can use the medicine “Olimetra” or make a combination treatment based on the use of “Hydrochlorothiazide”, “Medoxomil olmesartan”. You can use such analogues as "Lozarel" or "Cozaar". In addition, Nortian and Valsartan Zentiva medicines are suitable for replacement.
It is known about such drugs as Olmesar, Plaunak. Usually, substitutes differ from the original means, one of the differences is the affordable price and reduced bioavailability, so they are considered less effective, although they may well cope with their task.
Analogs are always used under the constant supervision of a specialist, it is necessary to regularly check blood pressure. If you need to choose an analogue to the Cardosal product, how to replace this drug, the doctor decides, taking into account various points. If side effects are detected during the treatment period with an analog, it is necessary to timely take the necessary actions aimed at eliminating them. During therapy, it is necessary to check the effect on the body.
When you can’t do without replacing the original product, you should give preference to medicines made by proven European companies. When planning to replace the Cardosal tablets, analogues should be selected only with the highest quality.
The reviews left on the forums by doctors and patients show that the drug “Cardosal” during the treatment period often causes negative reactions of the body, the most common of which are chest pain and constant weakness. But despite these unpleasant moments, the antihypertensive effect is always excellent. The appearance of side effects requires contacting a specialist for advice and, possibly, changing the treatment regimen.
In the treatment of patients with arterial hypertension, it is important to provide the patient with constant monitoring. The implementation of therapy, thus, will allow you to get the desired effect and monitor the condition of the body, and in case of violations, in time to eliminate them. An integrated approach is important, only medical treatment is not enough, you still need to choose a special diet. Among the necessary conditions of therapy are compliance with a sparing work regime, getting rid of bad habits, limiting physical activity and observing other tips that were suggested by the doctor for the best treatment result.