medicalmeds.eu Medicines Antagonists of receptors of angiotensin II. Diokor Solo

Diokor Solo

Препарат Диокор Соло. ООО «Фарма Старт» Украина

Producer: LLC Pharm Start Ukraine

Code of automatic telephone exchange: C09CA03

Release form: Firm dosage forms. Tablets.

Indications to use: Arterial hypertension. Heart failure.

General characteristics. Structure:

Active agent: валсартан 80 mg

Other ingredients: calcium hydrophosphate dihydrate, cellulose microcrystallic, gidroksipropilmetiltsellyuloza, sodium of a kroskarmelloz, silicon dioxide colloid anhydrous, talc, magnesium stearate, opadry II White.

Active agent: валсартан 160 mg

Covering for drawing a cover of Opadry II White: polyethyleneglycol, polyvinyl alcohol, talc, titanium E171 dioxide.

Pharmacological properties:

Pharmacodynamics. Active ingredient of drug Diokor Solo — валсартан — is an active specific antagonist of receptors of angiotensin II. It affects selectively the AT1 subtype receptors responsible for the known effects of angiotensin II. The increased angiotensin II levels after blockade of AT1-receptors valsartany can stimulate not blocked AT2-receptor which counterbalances effect of the AT1-receptor in a blood plasma. Valsartan does not show any partial activity of an agonist concerning the AT1-receptor, but has much more bigger (approximately by 20 000 times) affinity to AT1 to a receptor, than to the AT2-receptor.
Valsartan does not oppress APF known also under the name of a kininaza II which turns angiotensin I into angiotensin II and bradikinin destroys. Use of drug for patients with AG leads to decrease in the ABP without influence on pulse rate.
The beginning of hypotensive action is noted within 2 h, at most — in 4–6 h after intake. After administration of drug anti-hypertensive action remains during 24 h. The maximum therapeutic effect develops in 2–4 weeks from an initiation of treatment and remains at long therapy.
In case of a drug combination with a hydrochlorothiazide reliable additional decrease in the ABP is reached.
The sudden termination of administration of drug is not followed by development of a withdrawal. At prolonged use of drug by sick AG it is established that drug had no significant effect on the level of the general XC, uric acids, and also at a research on an empty stomach on concentration of TG and glucose in a blood plasma.
Drug use Diokor Solo causes reduction of cases of hospitalization because of heart failure, delay of progressing of heart failure, improvement of a functional class on NYHA classifications, increase in fraction of emission, and also reduction of expressiveness of symptoms of heart failure and improvement of quality of life in comparison with placebo.

Pharmacokinetics. After oral administration of drug валсартан it is soaked up quickly, however extent of absorption considerably varies. The average size of absolute bioavailability of drug makes 23%. The pharmacokinetic curve valsartana has the descending multiexponential character (T½α <1 h and T½β about 9 h). In the range of the studied doses the kinetics of a valsartan has linear character. At repeated use of drug of changes of kinetic indicators did not note. At administration of drug of 1 times a day cumulation insignificant. In a blood plasma women and men had an identical concentration of drug.
Valsartan substantially (for 94–97%) contacts proteins of a blood plasma, is preferential with albumine. Distribution volume in the period of an equilibrium state low (about 17 l). In comparison with a hepatic blood-groove (about 30 l/h), the plasma clearance of a valsartan occurs rather slowly (about 2 l/h). The quantity of the valsartan which is excreted with a stake makes 70% of the dose accepted inside. With urine about 30% are removed, it is preferential in not changed look. At purpose of a valsartan with AUC food decreases by 48% though since about the 8th hour after administration of drug of concentration of a valsartan in a blood plasma both in case of its reception on an empty stomach, and at reception with food, identical. AUC reduction nevertheless is not followed by clinically significant decrease in therapeutic effect therefore drug can be accepted and on an empty stomach, and during food.
The average time of achievement of Cmax and T½ of a valsartan at patients with heart failure and healthy volunteers identical. Indicators of AUC and Cmax of a valsartan raise linearly and are almost proportional to increase in a dose above clinical range (40–160 mg 2 times a day). The coefficient of cumulation averages 1,7. The clearance of a valsartan after oral administration makes about 4,5 l/h. The age does not influence clearance of drug at patients with heart failure.
Patients of advanced age. Some patients of advanced age had more expressed system influence of a valsartan, than at patients of young age, however was not established to any clinical importance of it.
Patients with a renal failure. Correlation between function of kidneys and system influence of a valsartan is not revealed. Therefore with a renal failure of dose adjustment of drug it is not required to patients. Drug pharmacokinetics researches at the patients who are on a hemodialysis are not conducted yet. However валсартан has high extent of linkng with proteins of a blood plasma therefore its removal at a hemodialysis is improbable.
Patients with an abnormal liver function. About 70% of size of the soaked-up dose of drug are excreted with bile, is preferential in not changed look. Valsartan is not exposed to considerable biotransformation and as it is possible to expect, system influence of a valsartan does not correlate with degree of abnormal liver functions. Therefore patients with a liver failure of not biliary origin and in the absence of a cholestasia do not need dose adjustment of a valsartan. It was shown what at patients with biliary cirrhosis or obstruction of biliary tract of AUC of a valsartan increases approximately twice.

Indications to use:

Arterial hypertension. Heart failure (the II-IV class on classification of the New York association of cardiologists (NYHA)).

Route of administration and doses:

AG. The recommended Diokor Solo's dose for adults makes 80 or 160 mg of 1 times a day. The anti-hypertensive effect is reached during 2 weeks, and the maximum effect is obvious in 4 weeks. At patients with the uncontrollable ABP the dose can be raised to maximum — 320 mg, perhaps additional purpose of diuretics. Diokor Solo it is possible to apply also along with other anti-hypertensive means.
Heart failure. The recommended initial dose of Diokor Solo makes 40 mg 2 times a day. Increase in a dose from 80 and 160 mg 2 times a day to the highest dose has to be carried out according to portability of drug by the patient. The maximum daily dose makes 320 mg.
Assessment of a condition of patients with heart failure always has to include assessment of a condition of function of kidneys.
The note concerning all indications: with renal failures or with a liver failure of not bilious origin and without cholestasia of dose adjustment of drug it is not required to patients.

Features of use:

Patients with deficit in an organism of sodium and/or OTsK. At patients with the expressed deficit in an organism of sodium and/or OTsK as, for example, at use of diuretics in high doses, occasionally in an initiation of treatment valsartany there can be arterial hypotension with clinical manifestations. Therefore before an initiation of treatment Diokor Solo it is necessary to carry out correction of contents in an organism of sodium and/or OTsK, for example by a diuretic dose decline.
In case of development of hypotension the patient should give horizontal position and if necessary to carry out to infusion of physiological solution. After stabilization by the ABP treatment by Diokor Solo can be continued.
Renal artery stenosis. Short-term use of drug for patients with the renovascular hypertensia which is secondary owing to a unilateral renal artery stenosis does not cause any essential changes of a hemodynamics of kidneys, creatinine or an urea nitrogen of blood. As other medicines influencing renin-angiotensin-aldosteronovuyu system can increase urea level in blood and creatinine in a blood plasma at patients with a unilateral or bilateral renal artery stenosis, as a security measure monitoring of these indicators is recommended.
Renal failure. With a renal failure of dose adjustment it is not required to patients. However in hard cases (clearance of creatinine <10 ml/min.) it is necessary to be careful as there is no experience of use of drug in these cases.
Abnormal liver function. With a liver failure of dose adjustment it is not required to patients. Valsartan is brought mainly with bile in not changed look. At patients with obstructive disturbances of biliary tract noted lower clearance of a valsartan. Therefore patients should observe extra care at purpose of a valsartan with obstructive disturbances of biliary tract.
Heart failure. At the patients with heart failure accepting drug in usual doses reveal insignificant decrease in the ABP, but the termination of therapy because of long symptomatic hypotension, as a rule, is not required if to follow instructions on a drug dosing. At the beginning of therapy by drug patients have to be careful with heart failure.
Owing to oppression at persons with hypersensitivity renal failures can note system renin-angiotensin-aldosteronovoy. At patients with heavy heart failure at whom function of kidneys can depend on activity system renin-angiotensin-aldosteronovoy treatment by APF inhibitors or antagonists of receptors of angiotensin can be followed by an oliguria and/or the progressing azotemia, (rarely) OPN and/or death. Assessment of a condition of patients with heart failure always has to include assessment of a condition of function of kidneys.
The combination of a valsartan with captopril was not more effective in comparison with use only of captopril. No distinctions in the general mortality depending on age, sex, race, basic treatment or a basic disease are revealed. Besides, the advantage of treatment валсартан + captopril, monotherapies valsartany and monotherapies by captopril was confirmed with a combination at the patients accepting blockers of β-adrenoceptors..........
Care when using a triple combination of APF inhibitors, blockers of β-adrenoceptors is necessary for patients with heart failure and a valsartana.
Period of pregnancy and feeding by a breast. Considering the mechanism of action of antagonists of angiotensin II, it is impossible to exclude risk for a fruit at use of a vasartan during pregnancy.
As well as other drugs exerting direct impact on renin-angiotensin-aldosteronovuyu system валсартан should not be applied during pregnancy. If pregnancy is revealed during treatment by drug, reception of a valsartan needs to be stopped as soon as possible.
It is unknown whether gets валсартан into breast milk. Therefore use of drug during feeding is not recommended by a breast.
Children. Safety and efficiency of use of a valsartan for children is not established yet therefore drug is not used in pediatric practice.
Ability to influence speed of response at control of vehicles or work with other mechanisms. At reception of a valsartan, as well as other anti-hypertensive means, it is recommended to be careful at control of vehicles and work with exact mechanisms.

Side effects:

Frequency of emergence of side reactions is estimated as follows: very often — ≥1/10; often — ≥1/100, <1/10; sometimes — ≥1/1000, <1/100; seldom — ≥1/10 000, <1/1000; very seldom — <1/100 000.
Infections and invasions: often — viral infections; seldom — upper respiratory tract infections, pharyngitises, sinusitis; very seldom — rhinitis.
From system of a hemopoiesis: often — a neutropenia; very seldom — thrombocytopenia.
From immune system: very seldom — hypersensitivity reactions, including a serum disease.
Disbolism: sometimes — гиперкалиемия*.
Disturbances of mentality: sometimes — sleeplessness, decrease in a libido.
From a nervous system: often — postural dizziness *; seldom — вертиго; very seldom — a headache **.
From an organ of sight and hearing: sometimes — вертиго.
From cardiovascular system: often — orthostatic hypotension, arterial hypotension **; very seldom — a vasculitis.
From respiratory system: sometimes — cough.
From a GIT: sometimes — diarrhea, an abdominal pain; very seldom — nausea **.
From skin and hypodermic cellulose: very seldom — rash, an itch.
From a musculoskeletal system: sometimes — a dorsodynia; very seldom — an arthralgia, a mialgiya.
From urinogenital system: very seldom — a renal failure **.
General disturbances: sometimes — weakness, an adynamy, hypostasis.
There are messages on existence of side reactions:
* at symptoms of heart failure;
** at heart failure (it is frequent — dizziness, a renal failure, arterial hypotension; sometimes — a headache, nausea).
In rare instances administration of drug can influence results of laboratory researches, for example decrease in level of hemoglobin and an indicator of a hematocrit is possible.
At certain patients with AG sometimes noted substantial increase of level of creatinine in a blood plasma, potassium and the general bilirubin. Messages on separate cases of increase in indicators of function of a liver are received.
At some patients with heart failure creatinine level in a blood plasma, and also potassium level in a blood plasma and an urea nitrogen in blood increased.
Therefore at treatment by drug Diokor Solo it is necessary to control periodically the above-stated indicators and to introduce amendments during treatment.
No special monitoring of laboratory parameters is required for the patients with essential hypertensia receiving therapy valsartany.

Interaction with other medicines:

Medicinal interaction of drug which would have clinical value is not revealed. Treat drugs which investigated in clinical tests: Cimetidinum, warfarin, furosemide, digoxin, атенолол, indometacin, hydrochlorothiazide, амлодипин, Glibenclamidum.
As Diokor Solo substantially is not metabolized, clinically significant interaction between medicines in the form of metabolic induction or oppression of system of P450 cytochrome at the combined use with valsartany is noted. In spite of the fact that валсартан has high extent of linkng with proteins of a blood plasma, the researches in vitro did not show any interaction at this level with a number of molecules which also have high extent of linkng with proteins, namely with diclofenac, furosemide and warfarin.
Simultaneous use with kaliysberegayushchy diuretics (for example Spironolactonum, Triamterenum, amiloride), the additives of potassium or substitutes of salt containing potassium can lead to increase in level of potassium in a blood plasma and to increase in content of creatinine in a blood plasma at patients with heart failure. It is necessary to be careful when the combined treatment is necessary.

Contraindications:

Hypersensitivity to a valsartan or any of drug components; period of pregnancy and feeding by a breast; children's age.

Overdose:

Owing to overdose of drug the expressed arterial hypotension can develop that can lead to consciousness oppression, a collapse, shock. If drug was accepted recently, it is necessary to cause vomiting. At hypotension a usual method of therapy is in/in injection of physiological solution.
It is improbable that валсартан it is possible to bring out of an organism by a hemodialysis in connection with its linkng with proteins of a blood plasma.