Valsacor hd160 coated pills 160mg + 25mg N30
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Active ingredients
Valsartan + Hydrochlorothiazide
Release form
Pills
Composition
Valsartan 160 mg hydrochlorothiazide 25 mg adjuvants: microcrystalline cellulose, lactose monohydrate, magnesium stearate, croscarmellose sodium, povidone, silicon dioxide, colloidal anhydrous. iron oxide red (e172).
Pharmacological effect
Combined antihypertensive drug. Valsartan is a selective antagonist of angiotensin II receptors, non-protein nature. It has a selective antagonistic effect on receptors of the AT1 subtype. The consequence of the blockade of AT1 receptors is an increase in plasma concentrations of angiotensin II, which can stimulate unlocked receptors of the AT2 subtype, which balances the effects associated with stimulation of the AT1 receptors. Valsartan does not have agonistic activity against the AT1 receptors. Its affinity for receptors of the AT1 subtype is approximately 20,000 times greater than that for receptors of the AT2 subtype. Valsartan does not inhibit ACE, also known as kininase II, which converts angiotensin I to angiotensin II and destroys bradykinin. Due to the lack of effect on ACE, the effects of bradykinin and substance P are not potentiated, therefore, when taking antagonists of apiotensin II receptors, the development of dry cough is unlikely. Valsartan does not interact and does not block the receptors of other hormones or ion channels that are involved in regulating the function of the cardiovascular system. When treating arterial hypertension, valsartan lowers blood pressure without affecting heart rate. After ingesting a single dose of valsartan, the antihypertensive effect develops within 2 hours , and the maximum decrease in blood pressure is achieved within 4-6 hours. The antihypertensive effect of valsartan persists for 24 hours. With repeated prescriptions of valsartan, the maximum decrease in blood pressure, regardless of dose, is up to Tigana 2-4 weeks and is maintained at that level during prolonged therapy. Combination with hydrochlorothiazide allows to achieve a significant additional reduction AD.Vnezapnoe discontinuation of valsartan is not accompanied by withdrawal (sharp rise in blood pressure or other adverse clinical effects) .Gidrohlorotiazid - thiazide diuretic, diuretic effect which is associated with impaired reabsorption of sodium, chlorine, potassium, magnesium,water in the distal nephron; delays the excretion of calcium ions, uric acid. It has a hypotensive effect, which is caused by the expansion of arterioles. Virtually no effect on normal blood pressure. The diuretic effect develops within 1-2 hours after taking the drug inside, reaches a maximum after 4 hours and lasts for 6-12 hours. The antihypertensive effect occurs after 3-4 days, but to achieve optimal therapeutic effect may take 3-4 weeks.
Pharmacokinetics
Valsartan Absorption Valsartan is rapidly absorbed after oral administration, but the extent of absorption varies widely. The average absolute bioavailability of valsartan is 23%. The time required to reach Cmax - 2 hours. When taking valsartan with food, the AUC is reduced by 48%. However, 8 hours after ingestion, plasma concentrations of valsartan taken on an empty stomach or with food are the same. Reducing AUC is not accompanied by a clinically significant decrease in the therapeutic effect of valsartan, so the drug can be used regardless of the meal. Distribution When the drug is taken orally once a day, its accumulation is negligible. Plasma concentrations of valsartan are the same in men and women. Valsartan is actively associated with serum proteins (94-97%), mainly with serum albumin. The equilibrium Vd of the drug is small, about 17 liters. Plasma clearance is relatively low (approximately 2 l / h) when compared with hepatic blood flow (approximately 30 l / h). Metabolism and elimination Metabolized using the isoenzyme CYP 2C9. T1 / 2 is 9 hours. Excreted mainly unchanged through the intestines (70%) and kidneys (30%). Pharmacokinetics in special clinical situations Considering that renal clearance is only 30% of the total clearance, patients with impaired renal function do not Correction of doses of the drug is required. Since the degree of binding of valsartan to plasma proteins is high, its removal during hemodialysis is unlikely. About 83% of valsartan is excreted through the intestine, mostly in unchanged form. Valsartan does not undergo significant biotransformation, therefore its systemic action does not correlate with the degree of impaired liver function. Therefore, in patients with hepatic insufficiency of nonbiliary origin and in the absence of cholestasis, no change in the dose of valsartan is required. In patients with biliary cirrhosis or obstruction of the biliary tract, the AUC of valsartan is increased approximately 2 times.Valsakor ND160 is not recommended for patients with impaired liver function. Some elderly patients have a slightly greater systemic effect of valsartan compared with young volunteers; however, it is not established whether these differences have clinical significance. Systemic clearance of hydrochlorothiazide is reduced in elderly patients compared with young. Hydrochlorothiazide Absorption and distribution After ingestion, the absorption of hydrochlorothiazide is 60-80%. Cmax of hydrochlorothiazide in the blood is achieved 2 hours after ingestion. Plasma protein binding is 40-70%. Metabolism and elimination Hydrochlorothiazide is not metabolized and is rapidly excreted in the urine (more than 95%). T1 / 2 is 6-15 hours.
Indications
- arterial hypertension (in patients for whom combination therapy is indicated).
Contraindications
- severe liver dysfunction; biliary cirrhosis and obstruction of the biliary tract (cholestasis); - mild and moderate liver dysfunctions of nonbiliary origin (for a given dose of the drug); - anuria, pronounced renal dysfunction (CC less than 30 ml / min (0.5 ml / sec)); - hemodialysis; - hypokalemia, hyponatremia, hypercalcemia or hyperuricemia with clinical manifestations, refractory to adequate therapy; - galactose intolerance, lactase deficiency lapp or glucose impaired glucose / galactose syndrome; - age up to 18 years (ef efficacy and safety of valsartan in children not established); - pregnancy; - lactation period; - hypersensitivity to valsartan, hydrochlorothiazide, sulfonamide derivatives and other components of the drug. Use caution while using potassium, potassium-sparing diuretics, potassium-containing substitutes for food salts and other drugs that can increase the level of potassium in the blood (for example, heparin), chronic heart failure, IV functional class according to the NYHA classification, chechnya failure (QC more than 30 ml / min (0.5 ml / sec)), moderate liver dysfunction, bilateral or unilateral stenosis of the renal arteries or stenosis of the artery of a single kidney, condition after kidney transplantation, conditions accompanied by a decrease in BCC and / or sodium ions ( includingdiarrhea, vomiting), primary hyper aldosteronism, aortic and mitral valve stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), systemic lupus erythematosus, hypersensitivity to other angiotensin II receptor antagonists, allergic reactions and bronchial asthma.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
The use of angiotensin II receptor antagonists is not recommended in the first trimester of pregnancy. The drug is contraindicated in the II and III trimesters of pregnancy, because the use in the II and III trimesters of pregnancy can cause fetotoksicheskie effects (reduced renal function, oligohydramnios, delayed ossification of the fetal skull bones) and neonatal toxic effects (renal failure, hypotension, hyperkalemia). If, nevertheless, the drug was used in the II and III trimesters of pregnancy, then an ultrasound of the kidneys and bones of the fetus should be performed. When planning a pregnancy, it is recommended that the patient be switched to alternative antihypertensive therapy taking into account the safety profile. When confirming pregnancy, Valsacor ND160 should be canceled as soon as possible. data on the allocation of valsartan in breast milk. However, it is known that valsartan penetrates the milk of lactating rats. Hydrochlorothiazide is excreted in breast milk. Therefore, if necessary, therapy with Valsacor ND160 during lactation should be canceled breastfeeding.
Dosage and administration
The drug is taken orally, regardless of the meal, the multiplicity of reception - 1 time / day. Valsacor ND160 can be combined with other antihypertensive drugs. Treatment should be started with minimal doses of the drug. For patients who have not reached the target level of blood pressure on the background of monotherapy (valsartan at a dose of 160 mg or hydrochlorothiazide at a dose of 25 mg), a fixed combination of doses - Valsacor ND160 (160/25 mg) 1 time / day is recommended. The maximum antihypertensive effect of the drug Valsacor ND160 (160/25 mg) develops within 2-4 weeks. Patients with impaired renal function (CC more than 30 ml / min (0.5 ml / sec)) do not need to change the dose of the drug. Valsacor ND160 is not recommended for patients with impaired liver function. The maximum recommended daily dose of valsartan in patients with mild or moderate liver dysfunctions of nonbiliary origin is 80 mg (1 tab. / Day of Valsacor H80). For elderly patients, dose adjustment is not required.
Side effects
From the side of the central nervous system and peripheral nervous system: often - general weakness; sometimes - increased fatigue, asthenia, dizziness, incl. postural, vertigo, insomnia; rarely - headache, depression, paresthesia, neuralgia; very rarely - fainting (when used after myocardial infarction). On the part of the respiratory system: often - nasopharyngitis; sometimes - infections of the upper respiratory tract, rhinitis, sinusitis, cough; very rarely - respiratory distress syndrome with pneumonitis and pulmonary edema. From the side of the cardiovascular system: sometimes - chest pain; often - marked reduction in blood pressure and orthostatic hypotension; very rarely, arrhythmias; potentially possible - peripheral edema. From the digestive system: often - diarrhea; sometimes nausea, dyspepsia, abdominal pain; rarely - gastroenteritis, loss of appetite, constipation, hyperbilirubinemia, increased activity of hepatic transaminases; very rarely - pancreatitis, intrahepatic cholestasis, jaundice. On the skin side: rarely - skin rash, photosensitivity; very rarely - alopecia. From the musculoskeletal system: sometimes - pain in the back, limbs, sprain and tears of ligaments and muscles or muscle tendons, arthritis, arthralgia; rarely - myalgia, muscle weakness, muscle cramps. From the urinary system: sometimes - decreased libido, impotence (less than 1%), urinary tract infections, viral infections, increased frequency of urination; rarely - hypercreatininemia,increasing the concentration of serum urea nitrogen; very rarely - impaired renal function. For the senses: sometimes - impaired vision; rarely - ringing in the ears, konyunktivit.Allergicheskie reactions: very rarely - angioedema, urticaria, skin rash, itching, hypersensitivity reactions, including serum sickness, and necrotizing vasculitis, toxic epidermal necrolysis (Lyell's syndrome), lupus-like reactions, exacerbation of SLE. From the hemopoietic system: rarely - anemia, incl. hemolytic, leukopenia, agranulocytosis, bone marrow suppression, decrease in hemoglobin and hematocrit, neutropenia, thrombocytopenia (sometimes with purpura). From the laboratory parameters: often - hyperkalemia, hypokalemia, hyponatremia, hypomagnemia, hypercalcemia, hyperacumia, hypokalemia, hyponatremia, hypomagneemia, hypercalcemia, hypokalemia, hyponatremia, hypomagneemia, hypercalcemia, hyperacumia, hypokalemia, hyponatremia, hypomagnemia very rarely - nosebleeds.
Overdose
Valsartan Symptoms: pronounced decrease in blood pressure, which can lead to dizziness, collapse and / or shock with death. Treatment: symptomatic, it is recommended to induce vomiting and flush the stomach, the appointment of activated carbon. With the development of arterial hypotension, it is necessary to give the patient a horizontal position with raised legs, fill the BCC and correct the impaired water-electrolyte balance. Hemodialysis is ineffective. Hydrochlorothiazide Symptoms: the most frequent symptoms are due to electrolyte deficiency (hypokalemia, hypochloremia, hyponatremia) and dehydration due to excessive diuresis (nausea, drowsiness, arrhythmia, muscle spasm). With simultaneous intake of cardiac glycosides, hypokalemia may aggravate the course of arrhythmias. Treatment: symptomatic.
Interaction with other drugs
ValsartanKlinicheski significant pharmacokinetic interactions with drugs cimetidine, warfarin, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, valsartan glibenclamide not otmecheno.Poskolku not exposed to significant metabolism, it should not expect significant drug interactions associated with the induction or inhibition of cytochrome R450.Odnovremenny receiving potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium-containing food additives,drugs that increase the level of potassium in the blood serum (ACE inhibitors, heparin, cyclosporine), can lead to hyperkalemia, and therefore care must be taken. Simultaneous use with other antihypertensive drugs, including diuretics, leading to increased hypotensive effect. When simultaneously taking lithium preparations and angiotensin II receptor antagonists, there have been cases of a reversible increase in serum lithium ions and an increase in its toxicity. It is recommended that blood levels of lithium ions be monitored regularly. Hydrochlorothiazide C thiazide diuretics Drugs such as ethanol, barbiturates and opioid analgesics may potentiate the risk of orthostatic hypotension. Hypoglycemic agents (for oral administration and insulin): may require correction of the dose of hypoglycemic agents. agents: additive effect. Holinolytics (for example, atropine, biperiden) increase the bioavailability of thiazide diuretics. Colestiramine and colestipol: in the presence of anionic exchange resins, the absorption of hydrochlorothiazide decreases. HCS, ACTH, laxatives, amphotericin B, carbenoxolone, benzathine benzylpenicillin, salicylic acid and salicylates: it is possible to reduce the electrolyte content, in particular hypokalemia, it is recommended to regularly monitor the content of potassium ions in the blood. (quinidine, hydroquinidine, disopyramide), class III antiarrhythmic drugs (amiodarone, dofetilide, ibutilide), sotalol, some antipsychotics (thioridazine, chlorpro azine, levomeprosy w / c): the risk of developing arrhythmias of the pirouette type against the background of possible hypokalemia and hypomagnesemia. Control of the content of potassium ions in the blood is recommended. Cardiac glycosides: risk of developing arrhythmias on the background of hypokalemia and hypomagnesemia. Beta-adrenoblockers and diazoxide: increased hypoglycemic effect of these agents. Urikozuricheskie means (probenecid, sulfinpyrazon,allopurinol): an increase in the concentration of uric acid in the blood is possible, as well as an increase in the frequency of hypersensitivity reactions to allopurinol; if necessary, dose adjustment of uricosuric drugs. Pressor amines (for example, epinephrine, norepinephrine): the effect of pressor amines may be reduced. Amantadine: the risk of side effects of amantadine increases. .Miorelaxants of non-depolarizing type of action (for example, tubocurarine): increased effect of muscle relaxants. Cyclosporine: the risk of hyperuricemia and gout increases bnyh oslozhneniy.Tetratsikliny (except doxycycline): Risk of increase of urea concentration in serum krovi.Metildopa: describes cases hemolytic anemii.Lity: diuretics reduce renal clearance of lithium and increase the risk of toxic action of lithium; control of the lithium content in the blood is recommended. NPVP (including COX-2 inhibitors, salicylic acid, indole acetic acid derivatives): the diuretic, natriuretic and hypotensive effects of diuretics may decrease, acute renal failure may develop. Simultaneous intake with calcium preparations, vitamin D may lead to increased levels of calcium ions in the blood, which can distort the results of the study of the function of the parathyroid glands.
special instructions
Patients with severe chronic heart failure in the stage of decompensation or other conditions accompanied by RAASP stimulation of the drug Valsacor ND160 in this group of patients are usually accompanied by a more pronounced decrease in blood pressure, however, following the guidelines for dose selection, treatment rarely requires discontinuation due to arterial hypotension. Therapy with Valsacor ND160 should be carried out with caution. Due to the suppression of the RAAS activity in some patients, the development of a renal dysfunction may develop. In severe chronic heart failure, oliguria and / or progressive azotemia may develop, up to (in rare cases) acute renal failure and / or death (in rare cases). In patients with chronic heart failure, regular monitoring of renal function is necessary, with simultaneous administration of a combination of three classes of drugs - ACE inhibitors, beta-blockers and angiotensin II receptor antagonists (AT1).May be prescribed in combination with other drugs prescribed after myocardial infarction: thrombolytics, acetylsalicylic acid, beta-blockers and statins. Patients with hyponatremia and / or reduced OCSU patients with severe hyponatremia and / or reduced BCC, for example, due to the administration of large doses diuretics, in rare cases, at the beginning of therapy with Valsacor ND160, severe arterial hypotension may develop. Before starting treatment, it is recommended to correct violations of water and electrolyte balance, in particular, by reducing the dose of diuretics. With the development of arterial hypotension with clinical manifestations, it is necessary to give the patient a horizontal position with the legs elevated, fill the BCC and correct the disturbances of water and electrolyte balance. Therapy with Valsacor ND160 can be continued only after stabilization of blood pressure indicators. Renal artery stenosis The safety of using Valsacor ND160 in patients with bilateral or unilateral stenosis of the renal arteries and stenosis of the single kidney has not been established (elevation of serum concentrations of urea and creatinine is possible). patients with impaired renal function (CC more than 30 ml / min (more than 0.5 ml / sec)) do not require changes in the dose of the drug. It is recommended to periodically monitor the content of potassium ions, the concentration of creatinine and uric acid in the serum. There is no experience with Valsacor ND160 in patients with recently transferred kidney transplantation. Liver function impairment It is recommended that patients with impaired liver function take no more than 80 mg of valsartan per day. Primary hyperaldosteronism Valsacor ND160 is not recommended for patients with primary hyperadosteronism. diuretics. Other metabolic disorders. Thiazide diuretics can alter glucose tolerance and increase serum glucose. centering cholesterol, triglycerides, and uric acid. Valsacor ND160 contains lactose, so the drug should not be prescribed to patients with hereditary galactose intolerance, lapp deficiency in lappase or glucose-galactose impaired absorption syndrome. and work with other complex mechanisms that require increased attention, becausemay develop dizziness or weakness on the background of arterial hypotension.