Composition, form of production and packaging
Tablets of prolonged action, covered with a film membrane of yellow color, round, biconcave; On the cross-section, two layers are visible, the inner layer (core) is white or almost white.
indapamide 1.5 mg
Excipients: hypromellose (hypromellose 4000) - 42-78.4 mg, lactose monohydrate - 168.5-132.1 mg, silicon dioxide colloid (aerosil) - 1 mg, magnesium stearate - 2 mg.
Sheath composition: hypromellose (hydroxypropylmethylcellulose) 5.94 mg, macrogol (polyethylene glycol 4000) 1.29 mg, talc 462 Ојg, titanium dioxide 1.29 mg, tropeolin O 18 Ојg.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
Diuretic. Antihypertensive drug. By pharmacological properties is close to thiazide diuretics (the mechanism of action is associated with a violation of sodium reabsorption in the cortical segment of the Henle loop). Increases the urinary excretion of sodium and chlorine ions, and to a lesser extent - potassium and magnesium ions. Possessing the ability to selectively block 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 blood plasma (TG, LDL, HDL) and carbohydrate metabolism (including in patients with concomitant diabetes mellitus). Reduces the sensitivity of the vascular wall to norepinephrine (noradrenaline) and angiotensin II, stimulates the synthesis of prostaglandin E 2 , reduces the production of free and stable oxygen radicals.
The antihypertensive effect persists for 24 hours when taking the drug 1 time / day, the optimal therapeutic effect develops by the end of the first week of admission.
After oral intake quickly and completely absorbed from the digestive tract; bioavailability is high (93%). Admission with food somewhat slows the rate of absorption, but does not affect its magnitude. C max is achieved 12 hours after ingestion.
At repeated receptions of fluctuation of concentration of a preparation in a blood plasma in an interval between receptions of two doses decrease. The equilibrium state is established after 7 days of regular admission. Binding to blood plasma proteins - 79%. It also binds to the elastin of the smooth muscles of the vascular wall. Do not cumulate. Has a high V d , penetrates through the histohematological barriers (including placental), excreted in breast milk.
Metabolism and excretion
Metabolised in the liver. T 1/2 - 18 hours. It is excreted by the kidneys mainly in the form of metabolites 60-80% (in an unchanged form is about 5%), through the intestine - 20%.
Pharmacokinetics in special clinical cases
In patients with renal insufficiency, pharmacokinetics does not change.
- arterial hypertension.
Tablets are taken orally, without chewing, squeezed with enough liquid. The daily dose of the drug is - 1.5 mg (1 tab.) 1 time / day (morning).
On the part of the digestive system: nausea, anorexia, dry mouth, gastralgia, vomiting, diarrhea, constipation, abdominal pain, possibly development of hepatic encephalopathy; rarely - pancreatitis.
From the side of the central nervous system: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression; rarely - fatigue, general weakness, malaise, muscle spasm, tension, irritability, anxiety.
On the part of the respiratory system: cough, pharyngitis, sinusitis; rarely rhinitis.
From the cardiovascular system: orthostatic hypotension, changes in the ECG (hypokalemia), arrhythmia, palpitations.
From the urinary system: frequent infections, nocturia, polyuria.
Allergic reactions: rash, hives, itching, hemorrhagic vasculitis.
On the part of laboratory indicators: hyperuricemia, hyperglycemia, hypokalemia, hypochloraemia, hyponatremia, hypercalciuria, elevated plasma urea nitrogen, hypercreatininemia, glucosuria.
On the part of the hemopoietic system: in isolated cases - thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia and hemolytic anemia.
Other: exacerbation of systemic lupus erythematosus.
- severe renal failure (anuria stage);
- severe hepatic (including with encephalopathy) insufficiency;
- lactation period;
- age up to 18 years;
- simultaneous reception of drugs that extend the QT interval;
- hypersensitivity to the drug and other sulfonamide derivatives.
With caution appoint the drug for violations of the liver and / or kidney function, violation of water-electrolyte balance, hyperparathyroidism, patients with an increased interval of QT on ECG or receiving combination therapy, diabetes mellitus in decompensation stage, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution appoint a drug for violations of kidney function.
Contraindicated use of the drug in severe renal failure (anuria stage).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution appoint a drug for violations of liver function
Contraindicated use of the drug in severe hepatic insufficiency (including with encephalopathy).
When the drug is prescribed for patients taking cardiac glycosides, laxative drugs against hyperaldosteronism, as well as to the elderly, regular monitoring of potassium ions and creatinine levels is indicated.
On the background of taking indapamide, the concentration of potassium, sodium, magnesium ions in the blood plasma (electrolyte disturbances may develop), pH, glucose concentration, uric acid and residual nitrogen should be systematically monitored.
The most thorough control is shown in patients with cirrhosis of the liver (especially with edema or ascites due to the risk of developing metabolic alkalosis, which increases the manifestation of hepatic encephalopathy), as well as in coronary artery disease, heart failure and elderly people. 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 determination of the concentration of potassium ions in the blood should be carried out during the first week of application of the drug.
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 ACE inhibitors are prescribed at low initial doses.
When administering indapamide, it must be borne in mind that derivatives of sulfonamides can aggravate the course of systemic lupus erythematosus.
Use in Pediatrics
The effectiveness and safety of the drug in children is not established.
Impact on the ability to drive vehicles and manage mechanisms
In some cases, individual reactions associated with changes in blood pressure are possible, especially at the beginning of treatment and with the addition of another antihypertensive agent. As a result, the ability to perform work that requires increased attention may be reduced.
Symptoms: nausea, vomiting, weakness, dysfunction of the gastrointestinal tract, violations of water and electrolyte balance, 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; if necessary, conduct symptomatic therapy. There is no specific antidote.
When combined with indapamide saluretics, cardiac glycosides, gluco- and mineralocorticoids, tetracosactide, amphotericin B (for intravenous administration), laxatives increase the risk of hypokalemia.
With simultaneous admission with cardiac glycosides, the likelihood of developing digitalis intoxication increases; with calcium preparations - hypercalcemia; with metformin - may aggravate lactic acidosis.
When combined with indapamide, the concentration of lithium ions in the blood plasma increases (by decreasing excretion in the urine); Lithium has a nephrotoxic effect.
When combined with indapamide, it should be noted that astemizole, erythromycin IV, pentamidine, sultopride, terfenadine, vincamine, antiarrhythmic drugs Ia class (quinidine, disopyramide) and III class (amiodarone, brethrium, sotalol) can lead to arrhythmia by type "pirouette".
With the combined use of NSAIDs, GCS, tetracosactide, sympathomimetics reduce the hypotensive effect of indapamide, baclofen - enhances.
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.
When combined with indapamide, ACE inhibitors increase the risk of developing arterial hypotension and / or acute hepatic insufficiency (especially with existing renal artery stenosis).
Indapamide increases the risk of kidney dysfunction when using iodine-containing contrast media in high doses (due to dehydration of the body). Before using iodine-containing contrast agents, patients need to restore fluid loss.
Tricyclic antidepressants and antipsychotic drugs increase the hypotensive effect and increase the risk of developing orthostatic hypotension.
When combined, cyclosporine increases the risk of hypercreatininaemia.
Indapamide 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).
Indapamide enhances 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
List B. The drug should be stored in a dry, protected from light and out of reach of children, at a temperature of no higher than 25 В° C. Shelf life - 3 years.