Arifon retard pills 1,5mg N30
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Active ingredients
Indapamide
Release form
Pills
Composition
Indapamide 1.5 mg adjuvants: lactose monohydrate - 124.5 mg, hypromellose - 64 mg, magnesium stearate - 1 mg, povidone - 8.6 mg, silicon dioxide anhydrous colloid - 0.4 mg film composition: glycerol - 0.219 mg, hypromellose - 3.642 mg, macrogol 6000 - 0.219 mg, magnesium stearate - 0.219 mg, titanium dioxide - 0.701 mg.
Pharmacological effect
An antihypertensive (diuretic) drug, a sulfonamide derivative containing an indole ring. In terms of pharmacological properties, indapamide is close to thiazide diuretics, whose action is associated with inhibition of the reverse absorption of sodium ions in the cortical segment of the nephron loop. Indapamide increases the excretion of sodium ions, chlorine and, to a lesser extent, potassium and magnesium ions with urine, which is accompanied by increased diuresis and causes an antihypertensive effect. In clinical studies of phase II and III, using indapamide in monotherapy in doses that do not have a pronounced diuretic effect , the hypotensive effect was demonstrated, which persisted for 24 hours. The antihypertensive effect of indapamide is associated with an improvement in the elasticity of large arteries, a decrease in the resistance of arterial vessels and OPSS. The drug helps to reduce the hypertrophy of the left ventricle of the heart. Thiazide and thiazide-like diuretics at a certain dose reach a plateau of therapeutic effect, while the frequency of side effects continues to increase with further increase in the dose of the drug. Therefore, one should not increase the dose of the drug if a therapeutic effect is not achieved when taking the recommended dose. In short, medium and long-term studies involving patients with arterial hypertension, it was shown that indapamide does not affect lipid metabolism (including triglycerides, cholesterol, LDL and HDL) and on the indicators of carbohydrate metabolism (including in patients with diabetes).
Pharmacokinetics
Absorption In pills of drug Arifon retard, the active substance is in a special carrier matrix, which ensures a gradual controlled release of indapamide in the gastrointestinal tract. The released indapamide is rapidly and completely absorbed from the gastrointestinal tract.Food intake slightly increases the time of absorption of the drug, without affecting the completeness of absorption. Cmax in plasma is reached 12 hours after ingestion of a single dose. With repeated administration, fluctuations in the concentration of the drug in the blood plasma in the interval between administration of the drug are smoothed out. There is individual variability of drug absorption. Distribution Plasma binding to plasma proteins is about 79%. Css is reached after 7 days of regular use. When the drug is taken again, its accumulation is not observed. Metabolism and elimination Indapamide undergoes biotransformation and is excreted as inactive metabolites, mainly with urine - 70% and feces - 22% .T1 / 2 is 14-24 hours (average 18 hours). Pharmacokinetics in special clinical situations, the pharmacokinetic parameters of the drug Arifon retard do not change in patients with renal insufficiency.
Indications
- arterial hypertension.
Contraindications
- renal failure severe (CC less than 30 ml / min); - hepatic encephalopathy; - severe liver dysfunction; - hypokalemia; - hypersensitivity to indapamide, other sulfonamide derivatives or to any of the excipients. Due to the fact that the composition of the drug includes lactose, Arifon retard is not recommended for patients with lactose intolerance, galactosemia, glucose-galactose malabsorption. The drug should be prescribed with caution in disorders of the liver and kidneys, disorders of water and electrolyte , weakened patients or patients receiving combined therapy with other antiarrhythmic drugs, diabetes, elevated uric acid, hyperparathyroidism, patients with a prolonged QT interval. Because of the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents in age under 18 years old.
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
As a rule, diuretic drugs should not be prescribed during pregnancy. Do not use these drugs to treat physiological edema during pregnancy. Diuretic drugs can cause placental ischemia and lead to impaired fetal development. Due to the fact that indapamide is excreted in breast milk, the use of the drug during breastfeeding is not recommended.
Dosage and administration
Assign inside on 1 tab. / Day, preferably in the morning. The pill should be swallowed whole, not chewed, squeezed with water. When treating patients with arterial hypertension, increasing the dose of the drug does not increase the antihypertensive effect, but enhances the diuretic effect. Elderly patients should be monitored for plasma creatinine level, taking into account age, body weight and sex. retard at a dose of 1.5 mg / day (1 tab.) can be administered to elderly patients with normal or slightly impaired renal function.
Side effects
Most adverse reactions (laboratory and clinical indicators) are dose-dependent. The frequency of adverse reactions that can be caused by thiazide-like diuretics, including indapamide, is given in the form of the following gradation: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10,000, <1/1000); very rarely (<1/10 000); unspecified frequency (frequency cannot be calculated from available data). From the hematopoietic system: very rarely - thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, hemolytic anemia. From the CNS and peripheral nervous system: rarely - asthenia, vertigo, paresthesia, headache pain; unspecified frequency - fainting. From the side of the cardiovascular system: very rarely - arrhythmia, pronounced decrease in blood pressure unspecified frequency - pirouette type arrhythmia (possibly fatal). On the digestive system: infrequently - vomiting; rarely - nausea, constipation,dryness of the oral mucosa; very rarely - pancreatitis. From the side of the liver and biliary tract: very rarely - impaired liver function; unspecified frequency - hepatic encephalopathy and hepatitis may develop in patients with hepatic insufficiency. From the urinary system: very rarely - renal insufficiency. allergic and asthmatic reactions: often - maculo-papular rash; infrequently - hemorrhagic vasculitis; very rarely - angioedema and / or urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome; unspecified frequency - in patients with acute form of systemic lupus erythematosus may worsen the course of the disease; Cases of photosensitivity reactions are described. Laboratory indicators: in clinical studies, hypokalemia (plasma content of potassium less than 3.4 mmol / l) was observed in 10% of patients and less than 3.2 mmol / l in 4% of patients after 4-6 weeks of treatment. After 12 weeks of therapy, the plasma concentration of potassium decreased, on average, by 0.23 mmol / l. Hypercalcemia has been very rarely observed. Unspecified frequency: 1) a decrease in the content of potassium and the development of hypokalemia, especially significant for patients at risk; 2) hyponatremia, accompanied by hypovolemia, dehydration and orthostatic hypotension. Simultaneous hypochloraemia can lead to a compensatory metabolic alkalosis (the probability and severity of this effect is low); 3) increase in the concentration of uric acid and glucose in the blood: thiazide and thiazide-like diuretics should be used with caution in patients with gout and diabetes mellitus; 4) increase in the QT interval on the ECG; 5) increased activity of hepatic transaminases.
Overdose
Indapamide even in very high concentrations (up to 40 mg, ie, 27 times the therapeutic dose) does not have a toxic effect. Symptoms of acute drug poisoning are primarily associated with impaired water and electrolyte balance (hyponatremia, hypokalemia). Nausea, vomiting, decrease in blood pressure, convulsions, dizziness, drowsiness,confusion, polyuria or oliguria, leading to anuria (due to hypovolemia). Treatment: urgent measures aimed at removing the drug from the body: gastric lavage and / or the appointment of activated carbon, followed by the restoration of normal water-electrolyte balance.
Interaction with other drugs
Non-recommended combination of drugs. In the case of simultaneous use of indapamide and lithium preparations, an increase in plasma lithium concentration may be observed due to a decrease in its excretion, accompanied by the appearance of signs of overdose. If necessary, diuretic drugs can be used in combination with lithium drugs, and the dose of drugs should be carefully selected, constantly monitoring the lithium content in the blood plasma. Combinations requiring special controlPreparations capable of causing pirouette-type arrhythmia: - Class I antiarrhythmic drugs (quinidine, hydroquinidine, Disopyramide); - Class III antiarrhythmic drugs (amiodarone, sotalol, dofetilide, ibutylide); - some antipsychotics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trift rperazin), benzamide (amisulpride, sulpirid), sulpirida, tiaprida, butyrophenone (droperidol), haloperidol; other (w / w). Hypopotassemia increases the risk of ventricular arrhythmias, especially pirouette-type arrhythmias. The level of potassium in the blood plasma should be determined and, if necessary, adjusted before starting the combination therapy with indapamide and the above mentioned drugs. It is necessary to monitor the patient’s clinical condition, monitor plasma electrolyte levels, ECG indicators. Patients with hypokalemia should use drugs that do not cause pirouette-type arrhythmia. When used simultaneously with NSAIDs (for systemic use), including selective COX-2 inhibitors, high doses of salicylates (more than 3 g / day), may decrease the antihypertensive action of indapamide. With significant fluid loss, acute renal failure may develop (due to a decrease in glomerular filtration).If necessary, the appointment of NSAIDs during therapy with Arifon retard should compensate for the loss of water and carefully monitor kidney function. With simultaneous use of indapamide with ACE inhibitors, hyponatremia in patients receiving ACE inhibitors increases the risk of sudden arterial hypotension and / or acute renal failure (especially renal artery stenosis). Patients with arterial hypertension and reduced due to the intake of diuretics sodium ions in the blood plasma should: - 3 days before the start of treatment with ACE inhibitors, stop taking diuretics. In the future, if necessary, resume diuretics; or start therapy with ACE inhibitors with low, gradually increasing doses of ACE inhibitors. In chronic heart failure, treatment should be started with low doses of ACE inhibitors, having previously reduced the dose of diuretics. In all cases, in the first week of taking ACE inhibitors, it is necessary to monitor kidney function (creatinine content in the blood plasma). With simultaneous use of indapamide with other drugs that can cause hypokalemia, including. with amphotericin B (w / w), gluco-and mineralocorticoid (with systemic use), tetracosactide, laxatives that stimulate intestinal motility, increases the risk of hypokalemia due to the additive effect (requires constant monitoring of the level of potassium in blood plasma and, if necessary, his correction). Special attention should be paid to patients who are simultaneously receiving cardiac glycosides. It is recommended to use laxatives that do not stimulate intestinal motility. At simultaneous use of indapamide with baclofen, there is an increase in the hypotensive effect (it is necessary to compensate for water loss and at the beginning of treatment to carefully monitor kidney function). to monitor the level of potassium in the blood plasma and ECG indicators and, if necessary, adjust the therapy). tions that require special treatment vnimaniyaOdnovremennaya indapamide and potassium-sparing diuretics suitable for some patients, but it does not exclude the possibility of hypokalemia (especially in patients with diabetes and patients with renal insufficiency) or hyperkalemia.It is necessary to monitor the level of potassium in the blood plasma, ECG indicators and, if necessary, adjust therapy. Functional renal failure, which can occur against the background of diuretics, especially loop, while the appointment of metformin increases the risk of lactic acidosis. It is not recommended to use metformin in combination with Arifon retard with creatinine levels above 15 mg / l (135 μmol / l) in men and 12 mg / l (110 μmol / l) in women. Dehydration of the body while taking diuretic drugs increases the risk of development acute renal failure, especially when using iodine-containing contrast agents in high doses. Patients need to compensate for fluid loss before using iodine-containing contrast agents. With simultaneous use of indapamide and tricyclic antidepressants, antipsychotic drugs, there is an increase in the hypotensive effect of indapamide and an increased risk of orthostatic hypotension (additive effect). excretion of calcium ions with urine. With simultaneous use of thiazide diur ticks with cyclosporine and tacrolimus may increase creatinine levels in blood plasma without changing the concentration of circulating cyclosporine, even with normal content of fluid and sodium ions. GCS influence.
special instructions
Liver dysfunction In the appointment of thiazide and thiazide-like diuretics in patients with impaired liver function, hepatic encephalopathy may develop, especially in the case of electrolyte imbalance. In this case, diuretic intake should be stopped immediately. Photosensitivity Instances of thiazide and thiazide-like diuretics have been reported, cases of photosensitivity reactions have been reported. In the case of the development of photosensitivity reactions in patients receiving the drug should stop treatment. If necessary, continue therapy with diuretics, it is recommended to protect the skin from exposure to sunlight or artificial ultraviolet rays. The content of sodium ions in the blood plasma. Before starting treatment, it is necessary to determine the content of sodium ions in the blood plasma.While taking the drug, this indicator should be regularly monitored. All diuretic drugs can cause hyponatremia, sometimes leading to extremely serious consequences. Requires constant monitoring of the content of sodium ions, because an initial decrease in sodium concentration in the blood plasma may not be accompanied by the appearance of pathological symptoms. The most careful control of the content of sodium ions is indicated for patients with cirrhosis of the liver and the elderly. Content of potassium ions in blood plasma When treating with thiazide and thiazide-like diuretics, the main risk is a sharp decrease in the level of potassium in the blood plasma and the development of hypokalemia. It is necessary to avoid the risk of hypokalemia (<3.4 mmol / l) in patients of the following categories: elderly, debilitated or receiving combined drug therapy with other antiarrhythmic drugs and drugs that can increase the QT interval, patients with cirrhosis, peripheral edema or ascites, ischemic heart disease , heart failure. Hypokalemia in these patients increases the toxic effect of cardiac glycosides and increases the risk of arrhythmias. In addition, patients with an increased QT interval are considered to be at increased risk, and it does not matter if this increase is caused by congenital causes or the effect of drugs. Hypopathy, as well as bradycardia, is a condition conducive to the development of severe arrhythmias and, especially, ventricular arrhythmias such as pirouette, which can be fatal. In all the cases described above, it is necessary to regularly monitor the content of potassium in the blood plasma. The first measurement of the concentration of potassium ions in the blood must be carried out during the first week after the start of treatment. When hypokalemia occurs, appropriate treatment should be prescribed. Calcium content in plasma should be borne in mind that thiazide and thiazide-like diuretics can reduce the excretion of calcium ions by the kidneys, leading to a slight and temporary increase in plasma calcium concentration. Severe hypercalcemia may be due to a previously undiagnosed hyperparathyroidism. Diuretic drugs should be discontinued before examining the function of the parathyroid glands. Glucose content in blood plasma It is necessary to control the blood glucose level in patients with diabetes mellitus,especially in the presence of hypokalemia. Uric acid Patients with gout may increase the frequency of seizures or aggravate gout. below 25 mg / l or 220 µmol / l). In elderly patients, normal plasma creatinine levels are calculated based on age, body weight and gender. It should be noted that at the beginning of treatment, patients may experience a decrease in glomerular filtration rate due to hypovolemia, which, in turn, is caused by loss of fluid and ions sodium while taking diuretic drugs. As a result, urea and creatinine concentrations may increase in blood plasma. If the kidney function is not impaired, such temporary functional renal failure usually passes without consequences, however, with the existing renal failure, the patient's condition may deteriorate. Sportsmen Indapamide can give a positive result when carrying out doping control in athletes. control mechanismsThe action of substances that are part of the drug Arifon retard, does not lead to a violation of psychomotor reactions. However, in some people, various individual reactions may develop in response to a decrease in blood pressure, especially at the beginning of therapy or when other antihypertensive drugs are added to the therapy. In this case, the ability to drive a car or other mechanisms can be reduced.