Indapamide retard-ALSI sustained release pills 1.5mg, 30pcs

Composition

One long acting coated tablet contains:

as an active ingredient:

indapamide-1.5 mg;

excipients:

hypromellose-77.36 mg,

lactose monohydrate (milk sugar) – 119.14 mg,

colloidal silicon dioxide (aerosil) – 1.0 mg,

magnesium stearate-1.0 mg,

hypromellose-2.24 mg,

lactose monohydrate-2.88 mg,

polyethylene glycol-0.80 mg,

titanium dioxide-2.08 mg

Pharmacological action

Antihypertensive agent, a thiazide-like diuretic with moderate and long-lasting effects, a benzamide derivative. It has moderate saluretic and diuretic effects, which are associated with the blockade of reabsorption of sodium, chlorine, hydrogen ions, and to a lesser extent potassium ions in the proximal tubules and cortical segment of the distal nephron tubule. Vasodilating effects and a decrease in total peripheral vascular resistance are based on the following mechanisms: reduced reactivity of the vascular wall to norepinephrine and angiotensin II; increased synthesis of prostaglandins with vasodilating activity; inhibition of the flow of calcium ions into the smooth muscle walls of blood vessels. Reduces the smooth muscle tone of the arteries, reduces the total peripheral vascular resistance. Helps to reduce hypertrophy of the left ventricle of the heart. In therapeutic doses, it does not affect lipid and carbohydrate metabolism (including in patients with concomitant diabetes mellitus). The antihypertensive effect develops at the end of the first/beginning of the second week with constant use of the drug and persists for 24 hours against the background of a single dose.

Indications

Arterial hypertension.

Recommendations for use

Inside, without chewing, with a sufficient amount of liquid, regardless of food intake, mainly in the morning at a dose of 1.5 mg (1 tablet) per day.

If the desired therapeutic effect is not achieved after 4-8 weeks of treatment, it is not recommended to increase the dose of the drug (the risk of side effects increases without increasing the antihypertensive effect). Instead, it is recommended to include another antihypertensive drug that is not a diuretic in the drug treatment regimen.

In cases where treatment is necessary to start with two medications, the dose of Indapamide retard remains equal to 1.5 mg in the morning once a day.

In elderly patients, the plasma creatinine concentration should be monitored taking into account age, body weight and gender, the drug can be used in elderly patients with normal or slightly impaired renal function (see also the section “Contraindications”).

Contraindications

Hypersensitivity to indapamide, other sulfonamide derivatives or other components of the drug, acute cerebrovascular accident, severe renal impairment (creatinine clearance less than 30 ml/min) and/or liver (including those with hepatic encephalopathy), hypokalemia, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established).

These tablets contain lactose monohydrate (milk sugar), and therefore the drug should not be taken by patients with rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

With caution. Use the drug with caution in diabetes mellitus, hyperuricemia (especially accompanied by gout and urate nephrolithiasis), hyponatremia and other water-electrolyte balance disorders, moderate hepatic and/or renal insufficiency, chronic heart failure, hyperparathyroidism, in patients with an extended QT interval on an ECG or receiving concomitant therapy, which may result in prolongation of the QT interval (astemizole, erythromycin (intravenously), pentamidine, sultopride, terfenadine, vincamine (IV), Class IA antiarrhythmic drugs (quinidine, disopramide) and Class III antiarrhythmic drugs (amiodarone, bretilia tosylate).

Side effects

Most adverse reactions (laboratory and clinical parameters) are dose-dependent. The frequency of adverse reactions that may be caused by thiazide-like diuretics, including indapamide, is given in the following gradations: very common (>1/10); often (>>1/100, >><1/10); infrequently (>1/1000, <1/10); infrequently (><1/100); rarely (>1/10000, <1/100); rarely (><1/1000); very rarely (

From the circulatory and lymphatic system. Very rare: thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, hemolytic anemia.

From the central nervous system. Rare: dizziness, fatigue, headache, paresthesia.

From the cardiovascular system. Very rare: arrhythmia, low blood pressure.

From the digestive system. Infrequently: vomiting. Rare: nausea, constipation, dry mouth. Very rare: pancreatitis.

From the urinary system. Very rare: kidney failure.

From the side of the liver and biliary tract. Very rare: impaired liver function.

Unspecified frequency: the possibility of developing hepatic encephalopathy in the case of liver failure.

From the side of the skin. Hypersensitivity reactions, mainly dermatological, in patients with a predisposition to allergic and asthmatic reactions: Common: maculopapular rash. Infrequently: hemorrhagic vasculitis. Very rare: angioedema and / or urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome. Unspecified frequency: may worsen in the presence of acute disseminated lupus erythematosus. Cases of photosensitivity are described.

Laboratory parameters. In clinical studies, hypokalemia (plasma potassium <3.4 mmol/l) was observed in 10% of patients and 3.2 mmol/l in 4% of patients after 4-6 weeks of treatment. After 12 weeks of therapy, the level of potassium in the blood plasma decreased, on average, by 0.23 mmol/l. Very rarely hypercalcemia. Unspecified frequency: Hypokalemia;  Hyponatremia, accompanied by hypovolemia, dehydration and orthostatic hypotension. Simultaneous loss of chlorine ions can lead to compensatory metabolic alkalosis, but the frequency of alkalosis and its severity is not significant; Increased levels of uric acid and glucose in blood plasma.

Interaction

Not recommended combinations When used concomitantly with lithium preparations, it is possible to increase the concentration of lithium ions in blood plasma due to a decrease in its excretion from the body by the kidneys, accompanied by the appearance of signs of overdose (nephrotoxic effect), as well as with a salt-free diet (reduced excretion of lithium ions by the kidneys).

Combinations that require special attention.

1. Drugs that can cause a pirouette-type heart rhythm disorder: Class IA antiarrhythmics (quinidine, hydroquinidine, disopyramide), class III antiarrhythmics (amiodarone, dofetilide, ibutilide, bretilia tosylate), sotalol, some antipsychotics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol), others (bepridil, cisapride, difemanil, erythromycin (intravenous use), halofantrin, mizolastine, pentamidine, sparfloxacin, moxifloxacin, vincamine (iv), astemizole. Concomitant use with any of these drugs, especially against the background of hypokalemia, increases the risk of ventricular arrhythmias of the “pirouette”type. Before starting combination therapy with Indapamide retard and the above drugs, the potassium content in the blood plasma should be monitored and, if necessary, corrected. It is recommended to monitor the patient’s clinical condition, as well as the content of blood plasma electrolytes and ECG. In patients with hypokalemia, it is necessary to use drugs that do not provoke the development of arrhythmia of the “pirouette”type.

2. Concomitant use of nonsteroidal anti-inflammatory drugs (NSAIDs) (with systemic use), including selective cyclooxygenase-2 (COX-2) inhibitors, high doses of salicylic acid (3 g / day or more) may reduce the antihypertensive effect of indapamide, the development of acute renal failure in dehydrated patients (due to a decrease in glomerular filtration rate). At the beginning of indapamide therapy, it is necessary to restore the water-electrolyte balance and monitor kidney function.

3. angiotensin converting enzyme (ACE) inhibitors in patients with hyponatremia (especially in patients with renal artery stenosis) increase the risk of hypotension and/or acute renal failure. Patients with arterial hypertension and possibly hyponatremia due to taking diuretics should:

– stop taking the drug 3 days before the start of ACE inhibitor therapy and switch to potassium-sparing diuretics;

– or start ACE inhibitor therapy with low doses, followed by a gradual increase in the dose if necessary. During the first week of ACE inhibitor therapy, monitoring of plasma creatinine concentrations is recommended.

4. Other medications that may cause hypokalemia:

– amphotericin B (IV), – gluco-and mineralocorticosteroids (with systemic use) (see also information in the section “Drug combinations requiring attention”), – tetracosactide (see also information in the section “Combinations of drugs that require attention”) – laxatives that stimulate intestinal motility.

Concomitant use of the above drugs with indapamide increases the risk of hypokalemia (additive effect). If necessary, the content of potassium ions in the blood plasma should be monitored and corrected.

5. Concomitant therapy with baclofen enhances the antihypertensive effect of indapamide.

6. Cardiac glycosides: hypokalemia increases the toxic effect of cardiac glycosides (glycoside intoxication). When using indapamide and cardiac glycosides simultaneously, the content of potassium ions in blood plasma, ECG indicators should be monitored, and, if necessary, therapy should be adjusted.

Drug combinations that require attention.

1. Concomitant use with potassium-sparing diuretics (amiloride, spironolactone, triamterene) is advisable in some patients, but the possibility of hypokalemia is not excluded. Against the background of diabetes mellitus or renal failure, hyperkalemia may develop. It is necessary to monitor the content of potassium ions in the blood plasma, ECG indicators, and, if necessary, adjust therapy.

2. Metformin increases the risk of developing lactic acidosis, as it is possible to develop renal failure while taking diuretics, especially “loop” ones. Metformin should not be taken if the plasma creatinine concentration exceeds 15 mg / l (135 mmol/l) in men and 12 mg/l (110 mmol/l) for women.

3. Concomitant use of high doses of iodine-containing contrast agents against the background of hypovolemia and taking diuretics increases the risk of acute renal failure. It is recommended to restore the water-electrolyte balance of the blood before using the drugs.

4. Tricyclic antidepressants (imipramine-like) and neuroleptics increase the hypotensive effect and the risk of orthostatic hypotension (additive effect).

5. Preparations containing calcium salts increase the risk of hypercalcemia due to a decrease in the excretion of calcium ions by the kidneys.

6. Cyclosporine, tacrolimus – the risk of increasing the concentration of creatinine in blood plasma without changing the concentration of circulating cyclosporine.

7. Glucorticosteroid drugs, tetracosactide (with systemic use) reduce the hypotensive effect (retention of sodium ions and fluid).

Overdose

Symptoms: nausea, vomiting, weakness, impaired gastrointestinal function (nausea, vomiting), water and electrolyte disorders, marked decrease in blood pressure, dizziness, drowsiness, confusion, respiratory depression, polyuria, oliguria up to anuria, patients with impaired liver function may develop hepatic coma.

Treatment: gastric lavage and / or use of activated charcoal followed by restoration of normal water-electrolyte balance, symptomatic therapy. There is no specific antidote.

Description

Round tablets of biconvex shape, covered with a film-coated white color. On the cross-section – the inner layer is white or white with a creamy tint of color.

Functional features

After oral use, the drug is completely but gradually absorbed from the gastrointestinal tract. Bioavailability is high (93%). Food intake slightly slows down the rate, but does not affect the completeness of absorption. The maximum concentration in blood plasma is reached 12 hours after ingestion of a single dose. The equilibrium concentration is reached after 7 days of regular use. The drug binds to plasma proteins by 70-80%. It has a high volume of distribution, passes through histohematic (including placental) barriers, and penetrates into breast milk. It is metabolized in the liver. The elimination half-life of indapamide is on average 18-26 hours. It is excreted from the body by the kidneys (up to 80%) mainly in the form of metabolites, through the intestines-20%. In patients with renal insufficiency, the pharmacokinetics do not change. It doesn’t accumulate.

Special instructions

Liver function disorders. In patients with hepatic insufficiency, when prescribing thiazide-like diuretics, hepatic encephalopathy may develop, especially if the water-electrolyte balance is disturbed. If it develops, diuretics should be discontinued.

Photosensitivity. When using thiazide-like diuretics, cases of photosensitivity reactions have been reported. If they develop, the drug should be discontinued. Against the background of therapy with Indapamide retard, it is necessary to protect open areas of the body from exposure to sunlight and artificial ultraviolet radiation.

Water-electrolyte balance. Sodium ion content in blood plasma: all diuretics can cause hyponatremia. The level of sodium ions in blood plasma should be measured before starting treatment with Indapamide retard, and then regularly during treatment. Determination of the content of sodium ions in blood plasma should be carried out before starting therapy with Indapamide retard, as well as during therapy. It is important to regularly monitor the level of sodium ions in the blood plasma, because initially hyponatremia may be asymptomatic. The most careful monitoring of the sodium ion content is indicated in elderly patients and patients with cirrhosis of the liver.

Potassium ion content in blood plasma: hypokalemia is the greatest risk when treated with thiazide-like diuretics. Special attention should be paid to the prevention of hypokalemia (less than 3.4 mmol/l) in the following cases: debilitated patients and/or receiving other therapy (antiarrhythmic drugs and drugs that can prolong the QT interval on the ECG), the elderly, patients with cirrhosis of the liver, peripheral edema and ascites; with coronary heart disease and chronic heart failure. Hypokalemia in such patients increases the toxic effect of cardiac glycosides and increases the risk of arrhythmia. An increased risk group also includes patients with an extended QT interval on the ECG. Hypokalemia is a predisposing factor for the occurrence of severe arrhythmia, and especially pirouette-type arrhythmia, which can lead to death. In all these cases, it is necessary to regularly monitor the content of potassium in the blood plasma. The first determination of the potassium content in the blood plasma should be carried out during the first week of therapy with Indapamide retard.

If hypokalemia is detected, appropriate therapy should be performed.

Calcium ion content in blood plasma: thiazide-like and thiazide diuretics can reduce the excretion of calcium ions by the kidneys, leading to minor and / or temporary hypercalcemia. Severe hypercalcemia with Indapamide retard may be a consequence of previously undiagnosed hyperparathyroidism.

You should stop taking diuretics before examining the function of the parathyroid glands.

Concentration of glucose in blood plasma: in patients with diabetes mellitus, especially in the presence of hypokalemia, it is necessary to monitor the concentration of glucose in the blood plasma.

Uric acid: in patients with hyperuricemia, it may increase the frequency of attacks or exacerbation of gout.

Renal function and diuretics. Thiazide and thiazide-like diuretics are fully effective only in patients with normal or slightly reduced (adult plasma creatinine less than 25 mg/l or 220 mmol/L) renal function. Severe hypovolemia can lead to the development of acute renal failure (decreased glomerular filtration rate), which may be accompanied by an increase in the concentration of urea and creatinine in blood plasma. With normal renal function, transient functional renal failure usually passes without consequences. With existing renal failure, the patient’s condition may worsen.

Elderly patients. It is recommended to regularly monitor the concentration of creatinine and potassium in the blood plasma, taking into account the patient’s age, body weight and gender. Indapamide retard can be prescribed to elderly patients with preserved or slightly impaired renal function (creatinine clearance above 30 ml / min).

Athletes.  Indapamide retard can give a positive result during doping control.

Influence on the ability to drive motor vehicles and other complex mechanical means. The use of indapamide retard does not lead to a violation of psychomotor reactions. However, some patients may develop different individual reactions in response to a decrease in blood pressure, especially at the beginning of therapy or when other antihypertensive agents are added to the therapy. In this regard, at the beginning of treatment with Indapamide retard, it is not recommended to drive vehicles or other complex mechanisms that require increased attention.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Indapamide

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets