Instructions for use Valsacor N80
- Instructions for use Valsacor N80
- Form of preparation, its composition and packaging
- Mechanism of action
- Pharmacokinetics of the drug
- Who is it recommended to take?
- When and to whom is it not recommended to take?
- How to use?
- Symptoms of drug overdose and their treatment
- Interaction with other drugs
- Taking the drug during pregnancy and breastfeeding
- Side effects
- Where and how to store?
- Terms of leave from pharmacies
- Walsakor H80 price
Farm Group: The drug for the treatment of hypertension
Form of preparation, its composition and packaging
Valsacor H80 is available in the form of tablets. They are enclosed in a film shell of pink color, have a biconvex oval shape.
1 tablet contains 80 mg of valsartan and 12.5 mg of hydrochlorothiazide, as well as additional substances: MCC, lactose monohydrate, magnesium stearate, croscarmellose sodium, povidone, colloidal silicium dioxide.
The film membrane has the following composition: hypromellose, titanium dioxide (E171), macrogol 4000, red iron oxide and yellow iron oxide (E172) as dyes.
Tablets of the drug are enclosed in blister packs of 14 pcs. on one sheet. Blisters are enclosed in cardboard packs of 2 and 7 pieces.
Mechanism of action
Valsacor H80 is a combined drug containing an angiotensin II receptor blocker and a thiazide diuretic.
Valsartan is a selective antagonist to angiotensin II receptors. It shows selective antagonism specifically to the subtype of AT1 receptors. The consequence of the blocking of these receptors is an increase in the concentration of angiotensin in the blood plasma and, accordingly, an increase in the stimulation of AT2 receptors. It should be remembered that valsartan is not an AT1 receptor agonist and does not inhibit angiotensin-converting enzyme (kinase II), which neutralizes bradykinin. Therefore, there is practically no chance of developing dry cough, a characteristic side effect of ACE inhibitors. Valsartan does not exert a depressing or stimulating effect on other hormones, mediators or ion transport.
Reduction of pressure in hypertension with valsartan passes without changing the heart rate.
Hypotensive action of valsartan develops within 120 minutes after taking a single dose of the drug. The maximum effect is achieved in 4-6 hours and persists throughout the day, which allows you to come to a single reception - this greatly increases the convenience of reception and compliance of the patient. With the subsequent regular use of valsartnam, the greatest result is achieved after 2-4 weeks of use. The effect persists for a long time and does not depend on the dose of the drug. Combination with hydrochlorothiazide makes it possible to accelerate the achievement of an antihypertensive effect.
Valsartan is characterized by the presence of withdrawal syndrome, so you can not stop taking this medication suddenly, because there is a sudden increase in pressure in the bloodstream.
Hydrochlorothiazide - a diuretic, has a thiazide structure. It acts on the distal part of the renal tubules, namely, it reduces the reverse absorption of ion-forming salts such as sodium, potassium, chlorine and magnesium into the blood. Increases the concentration of these substances in the secondary urine, and accordingly decreases in the blood. The reverse effect is on calcium ions and uric acid. Hypotonic effect of the drug is due not only to a decrease in the concentration of salts and the volume of circulating blood, but also by the expansion of arterioles. In this case, hydrochlorothiazide in the case of its reception at normal pressure does not practically change the blood pressure.
The first diuretic effect develops within an hour after admission, reaches a maximum after 4 hours and lasts up to 12 hours. With regular use of a stable antihypertensive effect occurs after 3-4 days, a therapeutically significant result requires the intake of 21-28 days.
Pharmacokinetics of the drug
After taking the valsartan tablet, its rapid absorption in the intestine occurs, but the degree of completeness of the drug in the systemic circulation varies very much. The average bioavailability is approximately 23%. After 2 hours, the maximum concentration is observed in the blood, the accumulative effect is little pronounced. The speed and degree of absorption of the drug do not have sexual differences.
The preparation for 94-97% of the total amount in the blood is transported in a bound form with serum albumins. Plasma clearance is quite low - 2 liters per hour.
Taking the drug with or without food does not change the plasma concentration of the substance in the blood, and therefore does not affect the therapeutic effect. Therefore, valsartan can be taken regardless of food intake.
The metabolism of valsartan is carried out with the help of the CYP2C9 isoenzyme.
After 9 hours, the concentration of valsartan in the plasma is reduced by a factor of 2 due to excretion through the intestine (70%) and kidneys (30%).
Bioavailability of hydrochlorothiazide after ingestion varies from 60 to 80%, with the maximum concentration observed after 2 hours. With plasma albumins, 40 to 70% of the substance of the bloodstream is bound.
The drug is not subject to metabolic processes and is excreted mainly by the kidneys (over 95%). After 6-15 hours, the concentration of hydrochlorothiazide falls by half.
In patients with impaired renal excretory function, there is no need to adjust the dose since renal clearance is less than a third of the total. Hemodialysis will not be effective, since valsartan is characterized by a high degree of binding to plasma proteins.
More than 80% of valsartan is excreted in the same form with the help of the intestine, therefore the liver does not take a significant part in the metabolism of the substance. Therefore, patients with a non-biliary liver dysfunction should not change the dosage. At the same time, people with biliary cirrhosis or blockage of the bile ducts require correction of doses, since they have a Valsartan AUC doubling.
It is noted that elderly patients are more susceptible to systemic effects of the drug compared with younger ones. However, the clinical significance of this phenomenon has not been established. Systemic clearance of a diuretic in people of young and middle age is higher than that of the elderly.
Who is it recommended to take?
Valsakor H80 take, if necessary, combined therapy of hypertension.
When and to whom is it not recommended to take?
- With severe violations of liver function with stopping of bile outflow
- In the absence of urination
- In severe violations of the kidneys
- With a reduced level of potassium and sodium in the blood
- With an elevated level of calcium and uric acid in the blood
- During pregnancy and lactation
- Persons under 18 years of age
- With increased sensitivity to the components of the drug
- With intolerance to galactose
How to use?
Valsakor H80 tablets are taken regardless of food once a day. The drug can be used as part of the comprehensive treatment of hypertension along with other antihypertensive agents.
It is especially recommended for patients in whom monotherapy with valsartan or hydrochlorothiazide was ineffective. In this case, it is necessary to choose the optimal dose - valsakor H80 1 tab 1 time per day or as much as 2 tablets per day (if a single dose does not bring the normalization of blood pressure). You can also use Valsakor HD160 - 1 tablet per day.
The most pronounced hypotonic effect of H80 valsakor is obtained not earlier than 2-4 weeks of regular admission. In the event that its level is insufficient (lower pressure is 100 or more mm Hg), an increase in the dose to 160/25 mg is permissible, that is, intake of 1 tablet of valsacor HD160, but not earlier than 4-8 weeks after the initiation of therapy .
Patients with renal insufficiency do not require correction of doses.
If the liver function is disrupted, the maximum daily dose of H80 Valsakor is 1 tablet per day.
Elderly patients should not change the dose of the drug.
Symptoms of drug overdose and their treatment
Symptoms of valsartan overdose are a sharp drop in blood pressure, including dizziness, loss of consciousness, development of collapse and a shock state with possible fatal outcome.
Overdose therapy: symptomatic measures - washing the stomach, causing vomiting, taking a horizontal position, replenishing the volume of circulating blood, normalizing the water-electrolyte balance. Conducting hemodialysis is ineffective due to the high degree of binding of the drug to albumin blood.
Symptoms of an overdose of hydrochlorothiazide are associated with the loss of electrolytes: potassium, magnesium, sodium and chlorine. Also, sharp dehydration with the following symptoms is observed: weakness, drowsiness, nausea, heart rhythm disturbance, muscle spasms. If a group of cardiac glycosides was taken together, an increase in arrhythmia is observed.
Therapy is symptomatic.
Interaction with other drugs
The combined use of valsartan with the following preparations did not lead to a change in the efficacy or toxicity of these agents: warfarin, atenolol, digoxin, cimetidine, indomethacin, glibenclamide, hydrochlorothiazide.
Does not interact with drugs inhibitors or cytochrome P450 intuctors, since it is not metabolized in the liver.
Admission together with drugs that raise the level of potassium in the blood, threatens the development of hyperkalemia, so you should be careful.
The use of other antihypertensive drugs, as well as diuretics can greatly enhance the hypotonic effect.
The intake of valsartan with lithium preparations leads to a marked increase in the concentration of these ions in the blood and increase their toxicity. Therefore, in this case, it is worthwhile to conduct regular monitoring of the lithium content in the blood.
The joint administration of a thiazide diuretic with barbiturates, anesthetics and ethanol can lead to orthostatic hypotension.
It is necessary to adjust the dose of hypoglycemic agents in the case of joint intake with hydrochlorothiazide.
Angi-hypertensive drugs when taken together with hydrochlorothiazide result in the summation of effects.
The group of cardiac glycosides together with hydrochlorothiazide aggravates the arrhythmia caused by the lowered level of potassium and magnesium.
Increases the hypoglycemic effect of beta-blockers.
The use of drugs that remove uric acid along with hydrochlorothiazide leads to an increase in the concentration of acid in the blood. Therefore, dosage adjustments may be required.
The effect of muscle relaxants like tubocurarine increases.
Antibiotics of the tetracycline group together with hydrochlorothiazide lead to an increase in the level of urea in the blood.
NSAIDs reduce the diuretic effect and can lead to the development of kidney failure.
The intake of calcium preparations leads to an increase in the concentration of this mineral in the blood, which distorts the results of the examination of the parathyroid glands.
Taking the drug during pregnancy and breastfeeding
Taking medications related to angiotensin receptor blockers during pregnancy is strictly prohibited, as it can cause a number of toxic effects on the development of the fetus. If, however, the use of H80 Walsakor was allowed in the process of bearing pregnancy, the ultrasound of the bones of the skull and the kidneys of the fetus should be immediately performed.
In the case of conception planning, a patient who regularly uses H80 Valsacor should find an alternative substitute for this prescription, always with safety in mind. If during the reception of the drug the fact of pregnancy was established, it is necessary to immediately stop taking.
There is no reliable information about the ingestion of valsartan into breast milk, but during the tests it was confirmed that the drug has entered the milk of lactating rats. The content of hydrochlorothiazide in breast milk was also established when it was taken. Therefore, it is necessary to stop feeding if necessary to use the Hals.
: слабость, головокружение, утомляемость, бессонница, головные боли, депрессивные состояния, невралгия. From the side of the central nervous system : weakness, dizziness, fatigue, insomnia, headaches, depressive conditions, neuralgia.
: назофарингит , кашель, ринит, синусит. On the part of the respiratory organs : nasopharyngitis, cough, rhinitis, sinusitis.
: резкое падение АД, нарушение ритма, боль в груди, отеки. From the heart and blood vessels : a sharp drop in blood pressure, rhythm disturbance, chest pain, swelling.
: расстройство, диспепсические явления, нарушение аппетита, воспаление поджелудочной железы, остановка оттока желчи. On the part of the gastrointestinal tract : frustration, dyspepsia, anorexia, pancreatic inflammation, stopping the outflow of bile.
: высыпания, фоточувствительность, облысение. From the skin : rashes, photosensitivity, baldness.
: боли в спине и в суставах конечностей, боли мышцах, воспаление суставов. From the musculoskeletal system : pain in the back and in the joints of the limbs, muscle pain, inflammation of the joints.
: инфекции, учащение мочеиспускания, дисфункция почек. On the part of the urinary system : infection, increased frequency of urination, kidney dysfunction.
: снижение полового влечения, импотенция. From the genitals : a decrease in sexual desire, impotence.
: воспаление конъюнктивы, ухудшение зрения , шумы ушах. From the sense organs : inflammation of the conjunctiva, deterioration of vision, noises of the ears.
Where and how to store?
Valsakor H80 is stored for no more than 2 years from the date of manufacture in a dark, dry place at a temperature of up to 30 ° C. Keep away from children.
Terms of leave from pharmacies
Valsacor H80 belongs to the list of prescription drugs.
Walsakor H80 price
Valsacor N80 tablets 80mg + 12.5mg - 250-300 rub.