Composition, form of production and packaging
Capsules hard gelatinous, size 4, with blue lid and white body; the contents of the capsules are a white or almost white powder, or a white or almost white powder with slices of mass, or a white or almost white powder compressed with a column and decomposing when pressed.
indapamide 2.5 mg
Excipients: microcrystalline cellulose (granulated), lactose monohydrate, corn starch, magnesium stearate, silicon dioxide colloid, titanium dioxide, gelatin, indigo carmine dye.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Antihypertensive drug, diuretic.
Indapamide belongs to the group of non-azide sulfonamides, by pharmacological properties it is close to thiazide-like diuretics. Reduces the tone of smooth arteries musculature, reduces OPSS. The drug has a moderate saluretic and diuretic effects, which are associated with the blockade of the reabsorption of sodium, chlorine, hydrogen ions and, to a lesser extent, potassium ions in the proximal tubules and the cortical segment of the distal tubules of the kidneys. Possessing the ability to selectively block the "slow" calcium channels, increases the elasticity of the walls of the arteries and reduces the OPSS. Helps reduce hypertrophy of the left ventricle of the heart. Does not affect the content of lipids in the plasma (triglycerides, LDL, HDL); does not affect carbohydrate metabolism (including in patients with concomitant diabetes mellitus). The decrease in OPSS is also due to a decrease in the sensitivity of adrenoreceptors of the vascular wall to noradrenaline and angiotensin II, an increase in the synthesis of prostaglandins with vasodilating activity (prostaglandin PgE2 and prostacyclin PgI2). Reduces the production of free and stable oxygen radicals. At appointment in high doses does not influence a degree of depression of a BP, despite of an increase in a diuresis.
The antihypertensive effect is manifested by the end of the first week, remains for 24 hours against the background of a single dose, reaches a maximum 8-12 weeks after the start of the drug.
After ingestion, indapamide is rapidly and completely absorbed from the digestive tract, bioavailability is high (93%). Eating somewhat slows the rate of absorption, but does not affect the completeness of absorption. After taking the drug inside at a dose of 2.5 mg C max in the blood is achieved after 1-2 hours.
Binding to plasma proteins is about 75%. It also binds to the elastin of the smooth muscles of the vascular wall. Has a high V d , passes through the histohematological barriers (including placental), penetrates into breast milk.
Metabolism and excretion
Metabolised in the liver. T 1/2 is an average of 14-18 hours. It is mainly excreted through the kidneys - 60-80% (in most cases - in the form of metabolites, about 5% - unchanged), through the intestine - 20-23%.
In patients with renal insufficiency, pharmacokinetics does not change. Do not cumulate.
- arterial hypertension.
The drug is administered orally, in the morning, regardless of food intake. Capsule should be swallowed without chewing, washed down with water.
Assign 2.5 mg (1 caps.) 1 time / day.
The drug can be used as a monotherapy or in combination with other antihypertensive agents (with beta-adrenoblockers, slow calcium channel blockers, ACE inhibitors). If after 4-8 weeks of treatment the desired therapeutic effect is not achieved, the dose of the drug should not be increased (the risk of side effects increases without increasing the antihypertensive effect). Instead, another antihypertensive drug that is not a diuretic should be added to the treatment regimen. In cases where treatment should begin with the reception of 2 preparations, the dose of Indap remains 2.5 mg in the morning 1 time / day.
On the part of the digestive system: nausea, vomiting, anorexia, dry mouth, abdominal discomfort, gastralgia, constipation or diarrhea, hepatic encephalopathy (against hepatic insufficiency).
From the side of the central nervous system: asthenia, headache, general weakness, increased fatigue, lethargy, lethargy, malaise, vertigo, muscle spasm, nervousness, tension, irritability, agitation; anxiety, insomnia, depression, dizziness, drowsiness.
From the sense organs: conjunctivitis, impaired vision.
From the respiratory system: rhinitis, rarely - cough, pharyngitis, sinusitis.
From the cardiovascular system: orthostatic hypotension, arrhythmia, palpitations, changes in the ECG (hypokalemia).
From the urinary system: nocturia, polyuria, an increase in the incidence of infections.
Allergic reactions: itching, rash, hives, hemorrhagic vasculitis.
On the part of the hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia.
From the laboratory indicators: hypercalcemia, hyperuricemia, hypochloraemia, hyponatremia, hyperglycemia, hypokalemia, increased urea nitrogen in blood plasma, hypercreatininaemia, glucosuria.
Other: flu-like syndrome, chest pain, back pain, decreased potency and / or libido, rhinorrhea, sweating, weight loss, paresthesia in the extremities, exacerbation of systemic lupus erythematosus, pancreatitis.
acute violation of cerebral circulation;
- expressed hepatic (including with encephalopathy) and / or renal failure, anuria;
- simultaneous reception of drugs that extend the QT interval;
- lactose intolerance, galactosemia, glucose absorption impairment syndrome, galactose;
- the period of lactation (breastfeeding);
- age under 18 years (effectiveness and safety not established);
- Hypersensitivity to indapamide, other derivatives of sulfonamides and components of the drug.
Precautions: diabetes mellitus at the stage of decompensation, hyperuricemia (especially accompanied by gout and urate nephrolithiasis), hyponatremia and other disturbances in water-electrolyte metabolism, moderate hepatic and / or renal insufficiency, ascites, IHD, chronic heart failure, QT interval prolongation;hyperparathyroidism.
PREGNANCY AND LACTATION
IndapВ® is contraindicated in pregnancy and lactation (breast-feeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe violations of kidney function, anuria. With caution in moderate renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function. With caution in moderate hepatic impairment.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years of age
APPLICATION IN ELDERLY PATIENTS
Elderly people show careful control of the content of potassium and creatinine.
Indapamide is effective for the treatment of patients with arterial hypertension at risk, i.e. with concomitant pathology (diabetes mild to moderate severity or with chronic renal failure, patients with hyperlipidemia).
With prolonged use of indapamide, electrolyte disturbances can sometimes occur, such as hyponatremia, hypokalemia, hypercalcemia, and hypochloraemic alkalosis.These disorders are more often observed in patients with chronic heart failure, liver diseases, with vomiting and diarrhea, as well as in individuals on a salt-free diet, which necessitates the control of blood electrolytes.
Indapamide increases the release of magnesium in the urine, which can lead to hypomagnesemia.
When using indapamide, the uric acid and residual nitrogen content in the blood plasma should also be systematically monitored.
Perhaps the appearance of orthostatic hypotension, which can be provoked by alcohol intake, barbiturates, opioid analgesics, and also by other antihypertensive drugs.
In the case of hypokalemia caused by indapamide, the toxicity of cardiac glycosides may increase. In patients taking cardiac glycosides, laxatives, with hyperaldosteronism, as well as in the elderly, careful monitoring of the potassium and creatinine content is shown.
The most thorough control is indicated in patients with cirrhosis of the liver (especially with edema or ascites - the risk of metabolic alkalosis, increasing manifestations of hepatic encephalopathy), IHD, chronic heart failure, and also in the elderly. Patients with an increased QT interval on the ECG (congenital or developing against a background of a pathological process) also belong to the high-risk group.
The first measurement of the potassium concentration in the blood should be performed within 1 week of treatment.
Hypercalcemia on the background of taking indapamide may be a consequence of previously undiagnosed hyperparathyroidism.
In patients with diabetes, it is extremely important to monitor blood glucose levels, especially when hypokalemia is present.
Significant dehydration can lead to the development of acute renal failure (reduced glomerular filtration). Patients must compensate for the loss of water and at the beginning of treatment carefully monitor the kidney function.
Indapamide can give a positive result in the conduct of doping control.
Patients with hypertension and hyponatremia (due to taking diuretics) need to stop taking diuretics 3 days before the start of taking ACE inhibitors (if necessary, diuretics can be taken a little later) or they are given initial low doses of ACE inhibitors.
Indapamide may worsen the course of systemic lupus erythematosus.
Despite the fact that indapamide has virtually no effect on carbohydrate metabolism, in patients with insulin-dependent diabetes mellitus it is possible to increase the necessary dose of insulin, and for latent diabetes it is necessary to monitor blood glucose.
Symptoms: nausea, vomiting, weakness, dysfunction of the gastrointestinal tract, water-electrolyte disorders, in some cases - excessive decrease in blood pressure, respiratory depression. In patients with cirrhosis, the development of hepatic coma is possible.
Treatment: gastric lavage, correction of water-electrolyte balance, symptomatic therapy. There is no specific antidote.
It is not recommended to use indapamide and lithium drugs simultaneously because of the possibility of developing a toxic effect of lithium against the background of a decrease in its renal clearance.
The combined use of indapamide with astemizole, erythromycin (IV), pentamidine, sultopride, terfenadine, vincamine, antiarrhythmic drugs IA (quinidine, disopyramide) and grade III (amiodarone, brethylium, sotalol) may reduce the hypotensive effect of indapamide and lead to arrhythmia in type "pirouette" due to the synergistic effect (lengthening) on вЂ‹вЂ‹the duration of the QT interval.
NSAIDs, GCS, tetracosactide, adrenostimulants reduce the hypotensive effect, baclofen strengthens.
Saluretics (loop, thiazide), cardiac glycosides, gluco- and mineralocorticosteroids, tetracosactide, laxatives, amphotericin B (IV) increase the risk of hypokalemia.
With simultaneous admission with cardiac glycosides, the likelihood of developing digitalis intoxication increases; with calcium preparations - hypercalcemia; with metformin, aggravation of lactic acidosis is possible.
Combination with potassium-sparing diuretics can be effective in some patients, but the possibility of hypo- or hyperkalemia, especially in patients with diabetes mellitus and renal insufficiency, is not completely excluded.
ACE inhibitors increase the risk of arterial hypotension and / or acute renal failure (especially with existing renal artery stenosis).
Indapamide increases the risk of developing kidney failure when using iodine-containing contrast agents in high doses with dehydration of the body. Before using iodine-containing contrast agents, patients need to restore fluid loss.
Tricyclic antidepressants and antipsychotics can increase the antihypertensive effect of the drug and increase the risk of orthostatic hypotension.
With simultaneous use with cyclosporine, an increase in the level of creatinine in the blood plasma is possible.
Reduces the effect of indirect anticoagulants (coumarin or indanedione derivatives) due to an increase in the concentration of coagulation factors as a result of a decrease in BCC and increase in their production by the liver (dose adjustment may be required).
Strengthens the blockade of the neuromuscular transmission, which develops under the action of nondepolarizing muscle relaxants.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of 15-25 В° C. Shelf life - 3 years.