Kandekor

Candecor is part of the group of drugs that affect the activity of the PA system. It is an antagonist of angiotensin 2.

Indications of the candecora

It is used to eliminate such disorders:

• increased values of blood pressure;
• CHF and left ventricular systolic activity (the fraction of left ventricular ejection is ≤40%) - in combination with ACE inhibitors or instead of them in case of increased sensitivity of the patient to them.

Release form

Release of the drug is carried out in tablets, 14 pieces inside the blister plate. The box contains 2, 4 or 7 such blisters.

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Pharmacodynamics

Angiotensin 2 is the main hormone of the RAAS complex, which has a vasoactive effect. He is an important participant in the pathogenesis of increasing blood pressure and other pathologies affecting the function of SSS. In addition, it is important in the pathogenesis of damage to various limbs and hypertrophy. Among its main physiological properties: vasoconstrictor action, aldosterone stimulation, stabilization of water-salt homeostasis, and stimulation of cell growth activity (cells that transmit through the end of type 1 AT1).

Candecor is a prodrug that, after absorption from the digestive tract, is quickly converted to the active element candesartan (in the process of ether hydrolysis). The drug is a selective antagonist of the end of angiotensin 2 and AT1, has a strong synthesis and slow dissociation from the end. Has no affinity for the ending. The drug does not slow the activity of ACP, which converts angiotensin 1 to angiotensin 2, and also destroys the integrity of bradykinin.

The drug is not synthesized and does not block other hormonal endings or ion channels, which are important participants in stabilizing the function of CCC. Because of the antagonism of the endings of angiotensin 2 (AT1), the increase in the plasma values of renin and angiotensin 1 and 2, as well as the decrease in the plasma level of aldosterone, develop depending on the size of the portion.

With a decrease in the elevated values of AD, the drug (taking into account the size of the dose) has a prolonged antihypertensive effect. The hypotensive properties of the drug depend on the total peripheral resistance, but not on the reflex increase in heart rate. Symptoms of a significant reduction in blood pressure when introducing the initial dose or the development of the reverse effect after the end of therapy, did not arise.

After consuming a single dose of drugs, the hypotensive effect develops over a period of 120 minutes. With permanent therapy, a decrease in blood pressure generally occurs with the use of any dosage; this effect is often achieved during 4 weeks, remaining with prolonged treatment. The average additive effect associated with an increase in the dose from 16 to 32 mg, used once a day - is immaterial. Given individual variability, individual patients may exhibit more than an average effect.

A single use of Kandekor per day results in a smooth and effective decrease in blood pressure during 24 hours. In this case, only a minor difference is observed between the peak and residual exposure of the drug at the dosing interval.

Cilexetil candesartan enhances blood circulation inside the kidneys without affecting them, or increases the glomerular filtration rate during the lowering of the filtration fraction, as well as the vascular resistance in the kidneys.

In people with high blood pressure in combination with diabetes mellitus type 2, and in addition with microalbuminuria, hypotensive treatment with drugs reduces the excretion of urine albumin. At the moment, there is no information on the effect of the drug on the progression of diabetic nephropathy. Individuals with the above disorders did not develop complications (negative effect on the lipid profile and blood sugar values) after 12 weeks of therapy using portions of 8-16 mg.

Insufficiency of the heart.

In people with CHF and weakened systolic activity of the left cardiac ventricle (the fraction of left ventricular ejection fraction is ≤40%), the medication reduces the overall resistance of the vessels and the wedging pressure inside the capillaries of the pulmonary arteries. In addition, Candecor increases the functional activity of renin within the blood plasma and angiotensin 2 indices, and together with this reduces the values of aldosterone.

Pharmacokinetics

After oral administration, the active ingredient is converted to a component of candesartan. The indicator of its absolute bioavailability after oral administration is 14%. In this case, the average peak values within the serum medication reaches after 3-4 hours. The level of candesartan within the blood serum increases linearly - along with the increase in the portion in the therapeutic dosage interval. The AUC values inside the blood serum do not change under the influence of food.

Candesartan has a high binding rate with plasma protein (more than 99%). At the same time, the apparent distribution volume of the drug is 0.1 l / kg.

Excretion of unchanged substance is mainly carried out through urine and bile. Only a very small part of the drug is excreted by metabolism inside the liver (CYP2C9). The half-life of drugs is approximately 9 hours. There is no accumulation of a drug within the body.

The total clearance of the drug within the blood is approximately 0.37 ml / minute / kg, and the clearance in the kidneys is approximately 0.19 ml / minute / kg. The drug is excreted through the kidneys, by filtering the glomeruli and active secretion of the tubules.

The unchanged part of the drug and inactive metabolic products of drugs are excreted in the urine (26% and 7%, respectively), as well as with feces (56% and 10%, respectively).

In elderly people (65 years of age), peak values and AUC levels increase by approximately 50% and 80% when compared with younger patients. But at the same time, blood pressure and the incidence of side effects after drug use remain the same in both groups of patients.

In people with kidney failure in mild or moderate degree, the peak level and the AUC value after a repeated portion are increased by approximately 50% and 70%, although the half-life remains at the same time.

In people with the above pathology in a difficult stage, these rates changed by approximately 50% and 110%. The terminal half-life of the drug in these patients is doubled.

The pharmacokinetic properties of individuals who undergo hemodialysis procedures correspond to the characteristics noted in patients with kidney failure in severe form. In people with this disorder in mild to moderate degree, the average level of AUC of the substance is increased by approximately 23%.

Dosing and administration

Candecor is consumed once a day, without tying the use of drugs to eating.

Reduction of elevated blood pressure values.

The size of the recommended initial, as well as the standard maintenance dosage is 8 mg, which are taken once per day. The portion can be doubled - up to 16 mg / day. If there is no result after the 1st month of therapy with taking 16 mg / day, it is allowed to increase the dose to the maximum permissible 32 mg / day. If, after using this dosage fails to achieve the desired effect, it is recommended to consider alternative methods of treatment.

Scheme of treatment is selected taking into account the patient's reaction - changes in blood pressure indicators. Often the hypotensive effect develops during the first month after the start of therapy.

If there is no result after the treatment (the BP values do not decrease to the optimal level), it is necessary to change the therapy scheme - to try the combined system (candesartan with hydrochlorothiazide).

Elderly people do not need to change the size of portions of drugs.

For persons with depleted intravascular volume values, an initial dose of 4 mg should be given.

People with problems in the work of the kidneys (this includes patients undergoing hemodialysis procedures) should use an initial dose of drugs, which is 4 mg. The size of the portion should be selected taking into account the response of the patient's body. In people with extremely severe or terminal form of kidney failure (CC values are <15 ml / minute), the drug was almost not used.

People with liver failure in the mild or moderate stage need to use drugs in the initial dosage of 2 mg (with a single dose per day). Portion is selected taking into account the patient's response. There is no data on the use of Candecor in people with liver failure in the severe stage.

Scheme of CHF treatment.

The standard size of the recommended initial dose is 4 mg with a one-time intake per day. Increase the dose to the planned daily dose of 32 mg or to the maximum dosage by doubling it is allowed with an interval of at least 2 weeks.

It is allowed to use the medication for combined treatment of heart failure (along with diuretics, and ACF, beta-blockers and digitalis medicines) or using a complex of these drugs.

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Use of the candecora during pregnancy

It is forbidden to appoint Candecor to pregnant women.

Contraindications

The main contraindications:

• the presence of hypersensitivity to the active component and auxiliary elements of drugs;
• women breastfeeding;
• cholestasis or liver failure in severe degree.

Side effects of the candecora

The use of drugs to reduce high blood pressure often causes such side effects:

• infection in the respiratory duct;
• vertigo or headaches;
• increase in C-ALT (C-GPT), urea, creatinine or potassium levels, as well as lower sodium values;
• when combined with other agents that slow down the activity of RAAS, there was a slight decrease in hemoglobin.

During the elimination of heart failure, such disorders often developed:

• an increase in urea or creatinine, as well as the development of hyperkalemia;
• a strong decrease in blood pressure;
• kidney failure.

At the stage of postmarketing research, we were noted individually:

• neutrophilic or leukopenia, as well as agranulocytosis;
• hyponatremia or hyperkalemia;
• headaches with dizziness, and nausea;
• increased activity of the action of liver enzymes and a disorder in the work of the liver or hepatitis;
• rashes, angioedema, itching and urticaria;
• arthralgia, pain in the back and myalgia;
• kidney deficiency (this also includes functional kidney disorders in persons who are predisposed to them).

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Overdose

Signs of poisoning: dizziness and marked decrease in blood pressure.

To remove the disorder, it is necessary to conduct symptomatic measures, as well as monitor the work of important organs for life. It is necessary to lay the victim on his back and lift his legs up. If this action is not enough, you need to increase the plasma volume by introducing a special infusion system (such as isotonic saline solution). If there is no result after using the above procedures, you should apply sympathomimetics. The drug is not excreted by the hemodialysis procedure.

Interactions with other drugs

There was no medically significant drug interaction with warfarin, hydrochlorothiazide and digoxin, and in addition nifedipine, glibenclamide, enalapril and oral contraception (eg, ethinyl estradiol and levonorgestrel).

Candesartan is only slightly excreted by metabolism inside the liver (CYP2C9). Hypotensive effects of drugs can be increased with other medications that lower blood pressure, regardless of the appointment of antihypertensive drugs or other indications for use.

The experience of using other drugs that affect the activity of RAAS, in combination with potassium-containing salt substitutes, potassium-sparing diuretics, potassium supplements and other drugs that can increase potassium levels (such as heparin), suggests that the potassium values inside the blood serum at such the combination may increase.

Combination of lithium with ACEI leads to a curable increase in the values of lithium within the blood serum, as well as its toxic effect. This effect can be noted with the use of angiotensin 2 terminations, and therefore, when combined, it is necessary to carefully monitor the values of lithium inside the blood serum.

The combination of angiotensin 2 endothelial antagonists with NSAIDs (eg, selective agents that slow down the activity of COX-2), aspirin (application> 3 g / day), and with indiscriminate NSAIDs may lead to a decrease in hypotensive properties of the drug. When combining the endings of angiotensin 2 with NSAIDs, it is possible to increase the probability of weakening the renal function (for example, suspicion of kidney failure in the acute stage), and in addition increase potassium levels inside the blood serum (especially in persons with chronic kidney failure). Therefore, to combine these drugs should be cautious, especially for elderly patients. Patients should drink a sufficient amount of fluid and monitor the work of the kidneys after the start of complementary treatment, and periodically do this in the future.

Storage conditions

Candecore is required to be kept in a place closed from the access of small children. The temperature level is not higher than 30 ° C.

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Shelf life

Candecor can be used for 2 years after the release of the drug.

Application for children

Since information on the safety and effectiveness of the drug in persons under the age of 18 is absent, it is forbidden to assign it to this group.

Analogues

Analogues of the medication are the medications of Angiocard, Angiakand, Ordiss, Atakand, and in addition Hyposart with Candesartan, Candesartan-SZ, Xarten and Candesartan cilexetil.

Reviews

Candecore usually receives positive feedback from patients who have used this drug. People note that the drug helps to normalize blood pressure values, reducing them to the optimal level.

But at the same time there are individual reviews, which indicate the presence of certain side-effects - for example, the severity and severe pain in the sternum.