Indapamide retarde sustained release pills 1.5mg 30pcs

Composition

Pills.

1 tablet contains:

Active ingredient:

indapamide 1.5 mg;

Auxiliary substances:

hypromellose-77.36 mg;

lactose monohydrate (milk sugar) – 119.14 mg;

colloidal silicon dioxide (aerosil) – 1 mg;

magnesium stearate-1 mg;

Opadray II (hypromellose-2.24 mg, lactose monohydrate-2.88 mg, polyethylene glycol-0.8 mg, titanium dioxide-2.08 mg) – 8 mg

Pharmacological action

Pharmacotherapy group:

diuretic.

ATX code:  C 03 VA 11

Pharmacological properties:

Pharmacodynamics

Indapamide is a sulfonamide derivative, similar in pharmacological properties to thiazide diuretics (impaired reabsorption of sodium ions in the cortical segment of the Henle loop). Increases the excretion of sodium, chlorine and, to a lesser extent, potassium and magnesium ions by the kidneys, which is accompanied by an increase in diuresis and a hypotensive effect. The antihypertensive effect persists for 24 hours against the background of a single dose, while there is a moderate increase in diuresis.

Antihypertensive activity is associated with an improvement in the elastic properties of large arteries, a decrease in arterial and total peripheral vascular resistance. Indapamide reduces left ventricular hypertrophy. 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, do not increase the dose of the drug if the recommended dose does not achieve a therapeutic effect.

Indapamide does not affect the content of lipids in blood plasma (triglycerides, low-density lipoproteins, high-density lipoproteins); it does not affect the parameters of carbohydrate metabolism, including in patients with diabetes mellitus.

Pharmacokinetics

Absorption After oral use, it is rapidly and completely absorbed from the gastrointestinal tract; bioavailability is high (93%). Food intake slightly slows down the rate of absorption, but does not affect the amount of absorbed substance. The maximum concentration in blood plasma is reached 12 hours after ingestion of a single dose. With repeated doses, fluctuations in the concentration of the drug in blood plasma in the interval between two doses are reduced.

Distribution of blood protein binding – 79%. The elimination half-life is 14-24 hours (on average,18 hours). Passes through histohematic barriers (including placental), is released into breast milk. The equilibrium concentration is reached after 7 days of taking the drug. No accumulation is observed with repeated use.

Metabolizmindapamide is excreted as inactive metabolites, mainly by the kidneys (70%) and through the intestines (22%).

Patients in the high-risk group In patients with renal insufficiency, the pharmacokinetics of the drug do not change.

Indications

-Arterial hypertension. Contraindications-Hypersensitivity to indapamide, other sulfonamide derivatives or any of the excipients; – Severe renal insufficiency (creatinine clearance less than 30 ml / min); – Hepatic encephalopathy or severe liver function disorders; – Hypokalemia; – Pregnancy, lactation; – Age under 18 years (efficacy and safety have not been established);-Concomitant use of drugs that prolong the QT interval; – Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Contraindications

With caution: Use with caution in patients with impaired liver and/or kidney function, impaired water-electrolyte balance, hyperparathyroidism, patients with an extended QT interval on an ECG or receiving concomitant therapy, diabetes mellitus in the decompensation stage, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).

Side effects

Most adverse reactions are dose-dependent.

From the digestive system: nausea, anorexia, dryness of the oral mucosa, gastralgia, vomiting, diarrhea, constipation, abdominal pain, impaired liver function, hepatic encephalopathy, hepatitis, increased activity of “hepatic” transaminases, pancreatitis.

From the hematopoietic system: hyperuricemia, hyperglycemia, hypokalemia, hypochloremia, hyponatremia, hypomagnesemia, hypercalcemia, increased urea nitrogen in blood plasma, hypercreatininemia, glucosuria, thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, hemolytic anemia.

Allergic reactions: skin rash, angioedema, urticaria, pruritus, toxic epidermal necrolysis, Stevens-Johnson syndrome, hemorrhagic vasculitis.

From the central nervous system: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression, fatigue, general weakness, malaise, muscle spasms, paresthesia, tension, irritability, anxiety.

From the respiratory system: cough, pharyngitis, sinusitis, rhinitis.

From the cardiovascular system: syncope, marked decrease in blood pressure, changes in the electrocardiogram (ECG) (characteristic of hypokalemia), prolongation of the QT interval on the ECG, arrhythmia, arrhythmia of the “pirouette” type, palpitation sensation.

From the urinary system: frequent infections, nocturia, polyuria, renal failure.

Other: exacerbation of systemic lupus erythematosus, photosensitization reaction.

Interaction

NOT RECOMMENDED COMBINATIONS-Lithium productsin the simultaneous use of indapamide and lithium preparations, an increase in the concentration of lithium in the blood plasma may occur due to a decrease in its excretion, accompanied by signs of overdose. If necessary, diuretic drugs can be prescribed in combination with lithium preparations, and the dose of drugs should be carefully selected, constantly monitoring the lithium content in the blood plasma.

COMBINATIONS THAT REQUIRE SPECIAL CAUTION-Drugs that can cause arrhythmia of the “pirouette” type-Class IA antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide);-class III antiarrhythmic drugs (amiodarone, dofetilide, ibutilide), sotalol;-some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluorperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol);-others: bepridil, cisapride, difemanil, erythromycin (iv), halofantrin, mizolastine, pentamidine, sparfloxacin, moxifloxacin, astemizole, vincamine (iv).

Increased risk of ventricular arrhythmias, especially pirouette-type arrhythmias (risk factor – hypokalemia). It is necessary to determine the potassium content in the blood plasma and, if necessary, adjust it before starting combination therapy with indapamide and the above drugs. It is necessary to monitor the patient’s clinical condition, monitor the content of blood plasma electrolytes, and ECG indicators.

Patients with hypokalemia should be prescribed drugs that do not cause arrhythmia of the “pirouette”type. – Nonsteroidal anti-inflammatory drugs (with systemic use), including selective cyclooxygenase-2 (COX-2) inhibitors, high doses of salicylates (≥3 g / day)

It is possible to reduce the antihypertensive effect of indapamide. With significant fluid loss, acute renal failure may develop (due to a decrease in glomerular filtration). Patients should be compensated for fluid loss and renal function should be carefully monitored at the beginning of treatment.

-Angiotensin converting enzyme (ACE)inhibitors The use of ACE inhibitors in patients with a reduced level of sodium ions in the blood (especially in patients with renal artery stenosis) is associated with the risk of sudden arterial hypotension and/or acute renal failure.

Patients with arterial hypertension and possibly reduced, due to taking diuretics, the content of sodium ions in the blood plasma should:

– stop taking diuretics 3 days before starting treatment with an ACE inhibitor. In the future, if necessary, the use of diuretics can be resumed; – or start therapy with an ACE inhibitor at low doses, followed by a gradual increase in the dose, if necessary. In patients with chronic heart failure, treatment with ACE inhibitors should be initiated at low doses, with possible preliminary reductions in diuretic doses.

In all cases, during the first week of taking ACE inhibitors in patients, it is necessary to monitor renal function (plasma creatinine concentration). -Other drugs that can cause hypokalemia: amphotericin B (IV), gluco-and mineralocorticosteroids (with systemic use), tetracosactide, laxatives that stimulate intestinal motility Increased risk of hypokalemia (additive effect). It is necessary to regularly monitor the content of potassium in the blood plasma, if necessary, correction. Special attention should be paid to patients receiving concomitant cardiac glycosides. It is recommended to use laxatives that do not stimulate intestinal motility. – Baclofen is marked by an increase in the hypotensive effect. Patients should be compensated for fluid loss and renal function should be carefully monitored at the beginning of treatment. – Cardiac glycosides

Hypokalemia increases the toxic effect of cardiac glycosides. When indapamide and cardiac glycosides are used concomitantly, the potassium content in the blood plasma, ECG parameters should be monitored, and, if necessary, therapy should be adjusted.

DRUG COMBINATIONS REQUIRING ATTENTION-Potassium-sparing diuretics (amiloride, spironolactone, triamterene)Combination therapy with indapamide and potassium-sparing diuretics is appropriate in some patients, but the possibility of hypokalemia (especially in patients with diabetes mellitus and renal insufficiency) or hyperkalemia is not excluded. It is necessary to monitor the potassium content in the blood plasma, ECG indicators and, if necessary, adjust therapy. – Metformin-functional renal failure, which can occur against the background of diuretics, especially “loop”, with simultaneous use of metformin increases the risk of lactic acidosis. Metformin should not be prescribed if the creatinine concentration exceeds 15 mg / l (135 mmol/l) in men and 12 mg/l (110 mmol/l) for women. – Iodine-containing contrast agents

Dehydration of the body while taking diuretics increases the risk of acute renal failure, especially when using high doses of iodine-containing contrast agents. Before using iodine-containing contrast agents, patients need to compensate for fluid loss. – Tricyclic antidepressants, antipsychotics (neuroleptics)Drugs of these classes enhance the antihypertensive effect of indapamide and increase the risk of orthostatic hypotension (additive effect). – Calcium saltswith simultaneous use, hypercalcemia may develop due to a decrease in the excretion of calcium ions by the kidneys. – Cyclosporine, tacrolimus It is possible to increase the concentration of creatinine in blood plasma without changing the concentration of circulating cyclosporine, even with normal fluid and sodium ions. – Corticosteroids, tetracosactide (for systemic use)Reduced hypotensive effect (fluid retention and sodium ions as a result of corticosteroids).

How to take, course of use and dosage

Inside,1 tablet per day, preferably in the morning. The tablet should be swallowed whole, without chewing, washed down with water. Increasing the dose does not increase the antihypertensive effect, but increases the diuretic effect. Elderly patients.

In elderly patients, plasma creatinine concentrations should be monitored based on age, body weight, and gender. Indapamide retard can be used in elderly patients with normal or slightly impaired renal function.

Overdose

Indapamide, even in doses up to 40 mg, i. e. 27 times more than the therapeutic dose, does not have a toxic effect. Signs of acute poisoning with the drug are primarily associated with a violation of the water-electrolyte balance (hyponatremia, hypokalemia).

Clinical symptoms of overdose may include nausea, vomiting, decreased blood pressure, seizures, dizziness, drowsiness, confusion, polyuria or oliguria leading to anuria (due to hypovolemia).

Treatment: gastric lavage, and / or intake of activated charcoal, followed by restoration of water and electrolyte balance. There is no specific antidote.

Special instructions

Liver function disorders

When using thiazide and thiazide-like diuretics in patients with impaired liver function, hepatic encephalopathy may develop, especially in the case of impaired water-electrolyte balance. In this case, diuretics should be discontinued immediately.

Photosensitivity reactionin the background of taking thiazide and thiazide-like diuretics, cases of photosensitivity reactions have been reported (see “Side effect”). If photosensitivity reactions develop while taking the drug, treatment should be discontinued. If it is necessary to continue diuretic therapy, it is recommended to protect the skin from exposure to sunlight or artificial ultraviolet rays.

Water-electrolyte balance-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 severe consequences. Regular monitoring of the sodium ion content is necessary, since initially a decrease in the sodium content in the blood plasma may not be accompanied by the appearance of pathological symptoms. The most careful monitoring of the sodium ion content is indicated for patients with cirrhosis of the liver and elderly patients (see the sections “Side effects” and “Overdose”). -The content of potassium ions in the blood plasma

When treated with thiazide and thiazide-like diuretics, the main risk is a sharp decrease in the potassium content in the blood plasma and the development of hypokalemia. The risk of hypokalemia should be avoided (/k) in patients of the following categories: elderly, debilitated or receiving combined drug therapy with other antiarrhythmic drugs and drugs that may increase the QT interval, patients with cirrhosis of the liver, peripheral edema or ascites, coronary heart disease, heart failure. Hypokalemia in these patients increases the toxic effect of cardiac glycosides and increases the risk of arrhythmias. In addition, the increased risk group includes patients with an extended QT interval, and it does not matter whether this increase is caused by congenital causes or the action of medications. Hypokalemia, as well as bradycardia, is a condition that contributes to the development of severe arrhythmias and, especially, arrhythmias of the “pirouette” type, which can lead to death. In all the cases described above, it is necessary to regularly monitor the content of potassium in the blood plasma. The first measurement of potassium ions in the blood should be carried out within the first week after the start of treatment. If hypokalemia occurs, appropriate treatment should be prescribed.

-Blood calcium content It 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 the content of calcium in the blood plasma. Severe hypercalcemia may be a consequence of previously undiagnosed hyperparathyroidism.

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

-Blood glucose level It is necessary to monitor the concentration of glucose in the blood in patients with diabetes mellitus, especially in the presence of hypokalemia.

Uric acid in patients with gout may increase the frequency of seizures or worsen the course of gout.

Diuretics and function Renal thiazide and thiazide-like diuretics are fully effective only in patients with normal or slightly impaired renal function (adult plasma creatinine concentrations below 25 mg / l or 220 mmol/L). In elderly patients, the normal concentration of creatinine in blood plasma is calculated taking into account age, body weight and gender.

It should be borne in mind 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 sodium ions against the background of taking diuretics. As a result, the concentration of urea and creatinine in the blood plasma may increase. If the kidney function is not impaired, such temporary functional renal failure usually passes without consequences, but with pre-existing renal failure, the patient’s condition may worsen.

Athletes The Active ingredient included in the preparation Indapamide retard can give a positive result during doping control in athletes.

Influence on the ability to drive vehicles and mechanisms:

The effect of the substances that make up 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 case, the ability to drive vehicles or other mechanisms may be reduced.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf life

3 years

Active ingredient

Indapamide

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets