Active substanceIndapamideIndapamide
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  • Dosage form: & nbspcoated tablets
    Composition:

    1 tablet contains:

    Component name

    Amount, mg

    Active substances:

    Indusapamid

    2,5

    Excipients - to obtain a tablet (without a coat) with a mass of 100 mg:

    Lactose Monohydrate

    72,0

    Microcrystalline cellulose

    10,0

    Corn starch

    10,1

    Magnesium stearate

    0,9

    Polyvinylpyrrolidone

    3,6

    Talc

    0,9

    Excipients - to obtain a tablet (with a coating) of 105 mg:

    Shell composition:

    Hypromellose

    1,873

    Polysorbate 80

    0,828

    Titanium dioxide

    0,728

    Castor oil

    0,230

    Talc

    0,728

    Macrogol-4000

    0,613

    Description:Round, biconvex tablets, without risks, coated with a white coating.On a cross-section the tablet is white or almost white in color.
    Pharmacotherapeutic group:Diuretics
    ATX: & nbsp

    C.03.B.A.11   Indapamide

    Pharmacodynamics:

    A hypotensive agent, a thiazide-like diuretic with a moderate in strength and long duration of action, a benzamide derivative. Has moderate saluretic and diuretic effects, which are associated with blockade of reabsorption of sodium, chlorine, hydrogen ions, and to a lesser extent potassium ions in the proximal tubules and cortical segment of the nephron distal tubule.

    The vasodilator effects and the reduction of the overall peripheral vascular resistance are based on the following mechanisms: a decrease in the reactivity of the vascular wall to norepinephrine and angiotensin II; an increase in the synthesis of prostaglandins with vasodilating activity; oppression of calcium current in the smooth-muscle walls of blood vessels.

    Reduces the tone of the smooth muscles of the arteries, reduces the overall peripheral resistance of the vessels. Helps reduce hypertrophy of the left ventricle of the heart. In therapeutic doses 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 a constant intake of the drug and lasts up to eight weeks; against the background of a single admission the maximum effect is observed after 24 hours.

    Pharmacokinetics:

    Suction. After oral administration, it is quickly and completely absorbed from the gastrointestinal tract (GIT); bioavailability is high (93%).

    Eating somewhat slows the rate of absorption, but does not affect the completeness of absorption. Time to reach the maximum concentration in the blood plasma (TCmax) - 1-2 hours after ingestion. With repeated administration of fluctuations in the concentration of indapamide in blood plasma in the interval between doses of two doses decrease. The equilibrium concentration is established after 7 days of regular intake.

    Distribution. Relationship with blood plasma proteins - 71-79%. It also binds to the elastin of the smooth muscles of the vascular wall. Has a high volume of distribution, passes through the histohematological barriers (including placental), penetrates into breast milk.

    Metabolism. Metabolised in the liver.

    Excretion. The half-life (T1/2) - 18 hours, 60-80% Kidneys derived as metabolites (unchanged output of about 5%), through the intestine - 20%. In patients with renal insufficiency, the pharmacokinetics do not change.Do not cumulate.

    Indications:

    Arterial hypertension.

    Contraindications:

    Hypersensitivity to indapamide and other components of the drug, as well as to other derivatives of sulfonamide, severe renal failure (creatinine clearance less than 30 ml / min), hypokalemia, hepatic encephalopathy or severe liver dysfunction, acute impairment of cerebral circulation, pregnancy, lactation, age up to 18 years of age (effectiveness and safety not established); lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (the drug contains lactose).

    Carefully:

    With violations of the liver and / or kidney function, disturbances of water-electrolyte balance, hyperparathyroidism, in weakened patients or in patients receiving combined therapy with other antiarrhythmics, while taking medications that extend the interval QT (see the section "Interaction with other drugs"), diabetes mellitus, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).

    Pregnancy and lactation:

    During pregnancy, do not prescribe diuretic drugs.Do not use these drugs to treat physiological swelling in pregnancy. Diuretic drugs can cause fetoplacental ischemia and lead to impaired fetal development (hypotrophy). Application of the drug INDAPAMIDE not recommended during pregnancy.

    Indapamide is excreted in breast milk. Given the potential for adverse events in infants, breastfeeding during treatment with the drug INDAPAMIDE Not recommended.

    Dosing and Administration:

    Tablets are taken orally, without chewing.

    Daily dose - 1 tablet of the drug INDAPAMIDE 1 time a day (in the morning), with plenty of liquid.

    When treating patients with hypertension, the dose of the drug should not exceed 2.5 mg (increased risk of side effects without increasing antihypertensive effect).

    Elderly patients

    In elderly patients, plasma concentrations of creatinine should be monitored, taking into account age, body weight and sex.

    A drug INDAPAMIDE in a dose of 2.5 mg / day (1 tablet) can be administered to elderly patients with normal or slightly impaired renal function (see section "Contraindications").

    Severe renal insufficiency

    The drug is contraindicated (see the section "Contraindications").
    Side effects:

    Most adverse reactions (laboratory and clinical indicators) are dose-dependent.

    The incidence of adverse reactions that may 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 (> 1/10000, <1/1000); very rarely (<1/10000); frequency (frequency can not be calculated from available data). The incidence of adverse reactions is given in accordance with the classification of the World Health Organization.

    From the blood and lymphatic system: rarely - Thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia, hemolytic anemia.

    From the central nervous system: rarely - dizziness, fatigue, headache, asthenia, paresthesia; frequency, unspecified - faint.

    From the cardiovascular system: rarely: arrhythmia, marked decrease in blood pressure; frequency, unspecified - Arrhythmia of the type "pirouette" (possibly with a fatal outcome), increasing the interval QT on the ECG (see section "Special instructions").

    From the digestive system: infrequently - vomiting; rarely - nausea, constipation, dryness of the oral mucosa; rarely - pancreatitis.

    From the urinary system: rarely - Renal failure.

    From the liver and bile ducts: rarely - a violation of the liver. Unspecified frequency: the possibility of developing hepatic encephalopathy in the case of liver failure (see the sections "Contraindications", "Special instructions"), hepatitis.

    From the skin:

    Hypersensitivity reactions, mainly dermatological, in patients with a predisposition to allergic and asthmatic reactions: often - maculopapular rash; infrequently - hemorrhagic vasculitis; rarely - angioedema and / or urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome; frequency, unspecified - Possible worsening of the course of the disease in patients with acute form of disseminated lupus erythematosus. Cases of photosensitivity reactions are described.

    Laboratory indicators:

    Rarely: hypercalcemia.

    Unspecified frequency:

    - increased activity of "liver" transaminases;

    - reduction of potassium content and development of hypokalemia, especially significant for patients at risk (see section "Special instructions");

    - hyponatremia, accompanied by hypovolemia, dehydration and orthostatic hypotension. Simultaneous loss of chloride ions can lead to compensatory metabolic alkalosis, however, the frequency of development of alkalosis and its severity is negligible;

    - Increase in the concentration of uric acid and glucose in the blood plasma.

    Thiazide and thiazide-like diuretics should be used with caution in patients with gout and diabetes mellitus.

    Overdose:

    Symptoms

    Signs of acute drug poisoning are primarily associated with a violation of the water-electrolyte balance (hyponatremia, hypokalemia). Symptoms of overdose may include nausea, vomiting, abnormal gastrointestinal function, convulsions, dizziness, drowsiness, confusion, polyuria or oliguria leading to anuria (due to hypovolemia), in some cases - excessive reduction in blood pressure, respiratory depression.In patients with cirrhosis, the development of the hepatic coma is possible.

    Treatment

    Emergency measures are limited to removing the drug from the body: gastric lavage and / or the appointment of activated charcoal, followed by the restoration of the water-electrolyte balance. There is no specific antidote.

    Interaction:

    Unwanted combination of drugs

    Lithium preparations

    With simultaneous use of indapamide and lithium preparations, an increase in the concentration of lithium in blood plasma can be observed due to a decrease in its excretion, accompanied by the appearance of signs of an overdose. If necessary, diuretic drugs can be used in combination with lithium preparations, while carefully choosing the dose of drugs, regularly monitoring the lithium content in blood plasma.

    A combination of drugs that requires special attention

    Drugs that can cause arrhythmia such as "pirouette":

    - antiarrhythmic drugs IA class (hydroquinidine (quinidine), disopyramide), antiarrhythmic drugs of III class (amiodarone, dofetilide, ibutilide), sotalol;

    - Some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoroperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol);

    - others: beprideil, cisapride, difemannil, erythromycin (iv), halofantrine, misolastine, pentamidine, sparfloxacin, moxifloxacin, astemizole, wincamine (w / w).

    Increased ventricular arrhythmia risk, especially arrhythmias such as "pirouette" (risk factor - hypokalemia)

    It is necessary to determine the content of potassium in the blood plasma and, if necessary, adjust it before starting the combination therapy with indapamide and the above drugs. It is necessary to monitor the clinical condition of the patient, control of blood plasma electrolytes, electrocardiogram (ECG) parameters.

    Patients with hypokalemia should use drugs that do not cause arrhythmia such as "pirouette".

    Non-steroidal anti-inflammatory drugs (for systemic administration), including selective inhibitors of COX-2 (cyclooxygenase-2), high doses of salicylates (≥3 g / day)

    It is possible to reduce the antihypertensive effect of indapamide.

    With a significant loss of fluid, acute renal failure may develop (due to a decrease in glomerular filtration rate).Patients need to compensate for fluid loss and at the beginning of treatment carefully monitor kidney function.

    Angiotensin converting enzyme (ACE) inhibitors

    The administration of ACE inhibitors to patients with a reduced concentration of sodium ions in the blood (especially patients with renal artery stenosis) is accompanied by a risk of sudden arterial hypotension and / or acute renal failure.

    Patients with hypertension and possibly reduced, due to the intake of diuretics, the content of sodium ions in the blood plasma is necessary: 3 days before the start of treatment with an ACE inhibitor, stop taking diuretics. In the future, if necessary, the reception of diuretics can be resumed. Or start therapy with an ACE inhibitor from low doses, with subsequent a gradual increase in the dose, if necessary.

    In chronic heart failure, treatment with ACE inhibitors should begin with low doses with the possible preliminary reduction of doses of diuretics.

    In all cases, in the first week of taking ACE inhibitors in patients, it is necessary to monitor renal function (creatinine concentration in the blood plasma).

    Other drugs that can cause hypokalemia: amphotericin B (IV), gluco- and mineralocorticosteroids (for systemic administration), tetracosactide), laxatives that stimulate bowel motility

    Increased risk of hypokalemia (additive effect).

    Regular monitoring of the potassium content in the blood plasma is necessary; if necessary - its correction. Particular attention should be given to patients who simultaneously receive cardiac glycosides. It is recommended to use laxatives that do not stimulate intestinal motility.

    Baclofen

    There is an increase in anti-hypertensive effect.

    Patients need to compensate for fluid loss and at the beginning of treatment carefully monitor kidney function.

    Cardiac glycosides

    Hypokalemia increases the toxic effect of cardiac glycosides.

    With the simultaneous use of indapamide, and cardiac glycosides cccontrols the content of potassium in the blood plasma, the parameters of the ECG, and, if necessary, adjust the therapy.

    A combination of drugs that requires attention

    Potassium-sparing diuretics (amiloride, spironolactone, triamterene, eplerenone (a derivative of spironolactone))

    Combination therapy with indapamide and potassium-sparing diuretics is suitable in some patients, but the possibility of hypokalemia (especially in patients with diabetes mellitus and patients with renal insufficiency) or hyperkalemia is not ruled out.

    It is necessary to monitor the potassium content in the blood plasma, the parameters of the ECG and, if necessary, adjust the therapy.

    Metformin

    Functional renal failure, which can occur against the background of diuretics, especially "loop", with the simultaneous administration of metformin increases the risk of developed lactic acidosis.

    No should be applied metformin, if the creatinine concentration exceeds 15 mg / L (135 μmol / L) in men and 12 mg / L (110 μmol / L) in women.

    Iodine-containing contrast agents

    Dehydration of the body against the background of 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 must compensate for fluid loss.

    Trand cyclic antidepressants, antipsychotics (antipsychotics)

    Preparations of these classes increase the antihypertensive effect of indapamide and increase the risk of orthostatic hypotension (additive effect).

    Salts of calcium

    With simultaneous administration, it is possible to develop hypercalcemia due to a decrease in excretion of calcium ions by the kidneys.

    Cyclosporin, tacrolimus

    It is possible to increase the concentration of creatinine in the blood plasma without changing the concentration of circulating cyclosporine, even with a normal content of liquid and sodium ions.

    Corticosteroid preparations, tetracosactide (for systemic administration)

    Reduction of antihypertensive action (fluid retention and sodium ions due to the action of corticosteroids).

    Special instructions:

    Dysfunction of the liver

    With the appointment of thiazide and thiazide-like diuretics in patients with impaired hepatic function, it is possible to develop hepatic encephalopathy, especially in the case of violations of the water-electrolyte balance. In this case, the taking of diuretics should be stopped immediately.

    Fosmosis

    Against the background of taking thiazide and thiazide-like diuretics, cases of development of photosensitivity reactions were reported (see the "Side effect" section).In the case of the development of reactions photosensitivity against the background of taking the drug should stop treatment. If it is necessary to continue therapy with diuretics, it is recommended to protect the skin from exposure to sunlight or artificial ultraviolet rays.

    Water-electrolyte balance

    Content of sodium ions in blood plasma:

    Before the start of treatment it is necessary to determine the content of sodium ions in the blood plasma. Against the background of taking the drug should regularly monitor this figure. All diuretics can cause hyponatremia, which sometimes leads to extremely serious consequences. It is necessary to regularly monitor the content of sodium ions, 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 control of the sodium ion content is indicated in patients with cirrhosis of the liver and elderly people (see "Side effect" and "Overdose" sections).

    The content of potassium ions in blood plasma:

    With thiazide and thiazide-like diuretics, the main risk is a sharp decrease in potassium in the blood plasma and development of hypokalemia.It is necessary to avoid the risk of developing hypokalemia (<3.4 mmol / l) in elderly patients who are weakened or are receiving concomitant drug therapy with other antiarrhythmic drugs and drugs that may increase the QT interval, patients with cirrhosis, peripheral edema or ascites, ischemic disease heart, heart failure. Hypokalemia in these patients increases the toxic effect of cardiac glycosides and increases the risk of arrhythmias.

    In addition, the high-risk group includes patients with an increased interval QT, it does not matter whether this increase is due to innate causes or effects of drugs.

    Hypokalemia, as well as bradycardia, is a condition that promotes the development of severe arrhythmias and, especially, pirouette-type arrhythmias, which can lead to death. In all the cases described above, it is necessary to regularly monitor the potassium content in the blood plasma. The first measurement of the potassium content in the blood should be carried out within the first week after the start of treatment. When hypokalemia occurs, appropriate treatment should be prescribed.

    Calcium in the blood plasma:

    It should be borne in mind that thiazide and thiazide-like diuretics can reduce the excretion of calcium by the kidneys, leading to a slight and temporary increase in the content of calcium in the blood plasma. Expressed hypercalcemia may be a consequence of previously not diagnosed hyperparathyroidism.

    It is necessary to cancel the reception of diuretic drugs before the study of the function of parathyroid glands.

    Concentration of glucose in blood plasma:

    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:

    Patients with gout may increase the incidence of attacks or exacerbate the course of gout.

    Diuretic drugs and kidney function:

    Thiazide and thiazide-like diuretics are effective only in patients with normal or slightly impaired renal function, creatinine plasma concentrations in adults below 25 mg / L or 220 μmol / L in adults. In elderly patients, the normal concentration of creatinine in the blood plasma is calculated taking into account age, body weight and sex.

    It should be borne in mind that at the beginning of treatment, patients may experience a decrease in the glomerular filtration rate due to hypovolemia, which in turn is caused by the loss of fluid and sodium ions on the background of taking diuretic drugs. As a consequence, the blood plasma can increase the concentration of urea and creatinine. If the kidney function is not impaired, such a temporary functional kidney failure, as a rule, passes without consequences, but with the existing renal failure the patient's condition may worsen.

    Application in athletes

    The active substance, which is a part of the preparation INDAPAMIDE, can give a positive result in the conduct of doping control in athletes.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions (risk of dizziness, drowsiness).

    Form release / dosage:

    The tablets covered with a cover, 2,5 mg.

    Packaging:

    10 tablets per contour cell packaging made of polyvinylchloride and aluminum foil.

    1, 2, 3, 4, 5 contour mesh packages together with instructions for use are placed in a pack of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003095
    Date of registration:17.07.2015 / 16.05.2016
    Expiration Date:17.07.2020
    The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp03.11.2017
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