Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave; On the cross-section, two layers are visible: the inner layer is white or white with a yellowish tint of color.
indapamide 2.5 mg
Excipients: ludipress, magnesium stearate, silicon dioxide colloid (aerosil), hydroxypropylmethylcellulose, titanium dioxide, polyethylene glycol, talc.
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 2011.
Hypotensive agent (diuretic, vasodilator). According to its pharmacological properties, it is close to thiazide diuretics (disruption of sodium rasabsorbia in the cortical segment of the Henle loop). Increases the urinary excretion of sodium, chlorine 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 overall peripheral vascular resistance. Helps reduce hypertrophy of the left ventricle of the heart. Does not affect the content of lipids in the blood plasma (triglycerides, low-density lipoproteins, high-density lipoproteins); significantly does not affect carbohydrate metabolism, but in the presence of hypokalemia, blood glucose levels may increase. Reduces the sensitivity of the vascular wall to noradrenaline and angiotensin II, stimulates the synthesis of prostaglandin PgE2? and prostacyclin PgI2, reduces the production of free and stable oxygen radicals.
When administered in high doses does not affect the degree of lowering blood pressure, despite an increase in diuresis.
With a systematic admission, the therapeutic effect is observed after 1-2 weeks, reaches a maximum by 8-12 weeks and lasts up to 8 weeks; after taking a single dose the maximum effect is observed after 24 hours. .
After oral administration, it is quickly and completely absorbed from the digestive tract; bioavailability is high (93%). Eating somewhat slows the rate of absorption, but does not affect the amount of absorbed drug. C max in blood plasma is achieved 1-2 hours after taking the drug inside. 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 concentration is established after 7 days of regular intake.
T 1/2 on the average is 14-18 hours, the connection with blood plasma proteins is 71-79%. It also binds to the elastin of the smooth muscles of the vascular wall. Has a high volume of distribution, penetrates through the histohematological barriers (including placental), penetrates into breast milk.
Metabolised in the liver. With urine, 60-80% is excreted in the form of metabolites (in an unchanged form, about 5% is excreted), through the intestine - 20-23%.
In patients with renal insufficiency, pharmacokinetics does not change. Do not cumulate
- arterial hypertension.
Tablets are taken orally, without chewing.
With hypertension, appoint 2.5 mg (1 tablet) 1 time per day in the morning. With insufficient effectiveness after 4-8 weeks, it is advisable to add antihypertensive medications to the therapy with a different mechanism of action (increasing the dose is not advisable - in the absence of a significant increase in the effect, there is an increase in side effects).
From the cardiovascular system: orthostatic hypotension, changes in the ECG (hypokalemia), arrhythmia, palpitations.
From the nervous system: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression; rarely - fatigue, malaise, muscle spasm, tension, irritability, anxiety.
On the part of the digestive system: nausea, vomiting, diarrhea or constipation, decreased appetite, dry mouth, abdominal pain, hepatic encephalopathy (against liver failure), pancreatitis.
From the respiratory system: cough, pharyngitis, sinusitis, rarely - rhinitis.
From the urinary system: infections, nocturia, polyuria.
Allergic reactions: pruritus, patchy-papular rash, hives, hemorrhagic vasculitis.
From the hematopoiesis: thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia
Laboratory indicators: hyperuricemia, hyperglycemia, hypokalemia, hypochloraemia, hyponatremia, hypercalcemia, an increase in the blood plasma of urea nitrogen, hypercreatininemia, glucosuria.
Other: exacerbation of systemic lupus erythematosus.
- severe renal failure (anuria stage);
- severe hepatic insufficiency (including with encephalopathy);
- deficiency of lactase;
- glucose-galactose malabsorption (the preparation contains lactose);
- lactation period;
- age under 18 years (effectiveness and safety not established);
- Hypersensitivity to indapamide, other derivatives of sulfonamides and components of the drug.
With caution: for violations of the liver and / or kidney function, violation of water-electrolyte balance, hyperparathyroidism, patients with an increased QT interval on the ECG, or simultaneous administration of drugs that extend the QT interval, diabetes mellitus at the stage of decompensation, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure. Use with caution in case of impaired renal function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency. Use with caution in case of impaired liver function.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
Use with caution in old age. The elderly are shown regular monitoring of the content of potassium ions and creatinine.
In patients taking cardiac glycosides, laxatives, against the background of hyperaldosteronism, as well as in the elderly, regular monitoring of the content of potassium and creatinine ions is shown.
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 - the risk of metabolic alkalosis, increasing manifestations of hepatic encephalopathy), coronary heart disease, chronic heart failure, and also in the elderly. Patients with an increased QT interval on an electrocardiogram (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 during the first week of treatment.
Hypercalcemia on the background of taking indapamide may be a consequence of previously undiagnosed hyperparathyroidism.
In patients with diabetes mellitus, it is extremely important to control the level of glucose in the blood, especially in the presence of hypokapaemia.
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 arterial hypertension and spontatremia (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.
Derivatives of sulfonamides can aggravate the course of systemic lupus erythematosus (it should be borne in mind when administering indapamide).
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Symptoms: nausea, vomiting, weakness, dysfunction of the gastrointestinal tract, water-electrolyte disorders, in some cases - excessive lowering of 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.
Saluretics (loop, thiazide), cardiac glycosides, gluco- and mineralocorticoids, tetracosactide, amphotericin B (IV), 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.
Increases the concentration of lithium ions in the blood plasma (reduces excretion in the urine), lithium has a nephrotoxic effect.
Astemizole, erythromycin (intravenous), pentamidine, sultopride, terfenadine, vincamine, antiarrhythmic drugs of class 1a (quinidine, dsnopyramide) and class III (amiodarone, brethilia tosylate, sotalol) can lead to pirouette arrhythmia by prolonging the QT interval .
NSAIDs, GCS, tetracosactide, sympathomimetics reduce the hypotensive effect, baclofen - strengthens. Combination with potassium-sparing diuretics can be effective in some patients, however, 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).
Increases the risk of kidney dysfunction when using iodine-containing contrast media in high doses (dehydration of the body). Before using iodine-containing contrast agents, patients need to restore fluid loss.
Imipramine (tricyclic) antidepressants and antipsychotic drugs increase the hypotensive effect and increase the risk of developing orthostatic hypotension.
Cyclosporine increases the risk of hypercreatininaemia.
Reduces the effect of indirect anticoagulants (coumarin or indanedione derivatives) due to an increase in the concentration of clotting factors as a result of a decrease in the volume of circulating blood and increase in their production by the liver (dosage correction may be required).
Strengthens the blockade of the neuromuscular transmission, which develops under the action of nondepolarizing muscle relaxants.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
List B. Store in a dry place, protected from light and out of the reach of children, at a temperature of no higher than 25 В° C. Shelf life - 3 years.