Acrypamide retard - instructions for use, dose, side effects, contraindications

Excipients: ludypress LCEE [lactose monohydrate 94.7-98.3%, povidone 3-4%] 94.4 mg, hypromellose 42 mg, silicon dioxide colloid 0.7 mg, magnesium stearate 1.4 mg;

composition of the shell: hypromellose 4.83 mg, macrogol-6000 0.14 mg, glycerol 0.28 mg, titanium dioxide 0.91 mg, talc 0.49 mg, lactose monohydrate 0.35 mg.

Description:

The tablets covered with a film cover, round, biconcave, white or white with kremovatym or grayish shade of color.

Pharmacotherapeutic group:Diuretics

ATX: & nbsp

C.03.B.A.11 Indapamide

Pharmacodynamics:

Antihypertensive agent (diuretic, vasodilator). By pharmacological properties is close to thiazide diuretics (violation of reabsorption of sodium ions in the cortical segment of the Henle loop). Increases the excretion of urine ions 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 concentration of lipids in the blood plasma (triglycerides, high and low density lipoproteins); does not affect carbohydrate metabolism (including in patients with concomitant diabetes mellitus). Reduces the sensitivity of the vascular wall to norepinephrine 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. After repeated administration, the therapeutic effect is observed after 1-2 weeks, reaches a maximum of 8-12 weeks and persists up to 8 weeks; after taking a single dose the maximum effect is observed after 24 hours.

Pharmacokinetics:After ingestion quickly and completely absorbed from the gastrointestinal tract. Bioavailability is high (93%). Eating somewhat slows down the speed, but does not affect the amount of absorbed indapamide. The maximum concentration in the blood plasma after taking retard tablets (1.5 mg) is achieved after 12 hours. With repeated administration of fluctuations in the concentration of indapamide in blood plasma in the interval between doses of two doses decrease. Equilibrium concentration is achieved after 7 days of regular intake. The drug is 71-79% bound to blood plasma proteins. It also binds to the elastin of the smooth muscles of the vascular wall. Has a high volume of distribution, passes through the histohematological (including placental) barriers, penetrates into breast milk.

Metabolised in the liver. The half-life of indapamide is an average of 14 hours, the final half-life is 26 hours.

It is excreted from the body by the kidneys (60-70%) mainly in the form of metabolites, through the intestine - 20-23%. In patients with renal insufficiency, pharmacokinetics does not change. Do not cumulate.

Indications:

Arterial hypertension.

Contraindications:

Hypersensitivity to the active and auxiliary components of the drug, derivatives of sulfonamides and thiazide.

Severe hepatic insufficiency (including hepatic encephalopathy), severe renal failure (creatinine clearance less than 30 ml / min), hypokalemia.

Lactose intolerance, galactosemia, glucose / galactose absorption disorder, lactase deficiency.

Pregnancy, lactation, age under 18 years.

Carefully:

Disorders of water-electrolyte balance, hepatic and / or renal failure, hyperuricemia (especially manifested by gout or urate nephrourolythiasis), hyperparathyroidism, diabetes mellitus in decompensation stage.

The drug should be administered with caution to patients receiving therapy with other medications, which may prolong the QT interval (see "Interaction with other drugs").

Dosing and Administration:

Inside, regardless of food intake, with enough liquid. Take the drug preferably in the morning. With arterial hypertension, the drug is taken 1 tablet (1.5 mg) per day.

With insufficient effectiveness after 4-8 weeks, it is advisable to add to the therapy a drug with a different mechanism of action (increasing the dose is inappropriate - in the absence of an increase in antihypertensive effect, there is an increase in side effects).

Side effects:

From the side of the cardiovascular system: orthostatic hypotension, arrhythmia, palpitations, ECG changes, characteristic of hypokalemia.

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

From the digestive system: constipation or diarrhea, dyspepsia (including nausea, vomiting), anorexia, dryness of the oral mucosa, abdominal pain, hepatic encephalopathy (against liver failure), pancreatitis.

From the genitourinary system: infection, nocturia, polyuria.

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

Allergic reactions: pruritus, patchy-papular rash, hives,hemorrhagic vasculitis, angioedema, toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity reactions.

From the hematopoiesis: thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia.

Laboratory indicators: hypercalcemia, hyperuricemia, hypochloraemia, hypokalemia, hyponatremia, hyperglycemia, increased blood urea nitrogen, hypercreatininaemia, glucosuria.

Other: exacerbation of systemic lupus erythematosus.

Overdose:

Symptoms: nausea, vomiting, weakness, marked decrease in blood pressure, dizziness, drowsiness, confusion, respiratory depression, dysfunction of the gastrointestinal tract; in patients with impaired liver function, it is possible to develop a "hepatic" coma.

Treatment: gastric lavage and / or reception of activated carbon, correction of water-electrolyte balance, symptomatic therapy. There is no specific antidote.

With a significant reduction in blood pressure, the patient should be placed in the "lying" position on the back with raised legs, if necessary, correct hypovolemia (for example, intravenous infusion of 0.9% sodium chloride solution).

Interaction:

Increases the concentration of lithium ions in the blood plasma (decreased excretion in the urine), lithium has a nephrotoxic effect.

Increases the risk of violations of kidney fiction when using iodine-containing contrast media in high doses (dehydration of the body). Before using iodine-containing contrast agents, patients need to restore the volume of circulating blood.

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 adjustment may be required).

Strengthens the blockade of the neuromuscular transmission, which develops under the action of nondepolarizing muscle relaxants.

Saluretics (loop, thiazide), cardiac glycosides, glucocorticosteroids and mineralocorticosteroids, tetracosactide, amphotericin B (with intravenous administration), laxative drugs increase the risk of hypokalemia.

With simultaneous admission with cardiac glycosides, the likelihood of developing digitalis intoxication increases; with calcium preparations - hypercalcemia; with metformin - the risk of development of lactic acidosis increases.

Astemizole, erythromycin (with intravenous administration), pentamidine, sultopride, terfenadine, wincamine, antiarrhythmic drugs of IA class (quinidine, disopyramide) and III class (amiodarone, brethil tosylate), sotalol, some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol), other (bepridil, cisapride, difemanyl, halofantrine, misolastine, sparfloxacin, moxifloxacin) can lead to the development of pirouette-type arrhythmias due to the synergistic effect (lengthening) on the duration of the QT interval.

Non-steroidal anti-inflammatory drugs, including selective inhibitors of cyclooxygenase-2 (COX-2), high doses of acetylsalicylic acid (3 g / day or more), glucocorticosteroids, tetracosactide, adrenostimulants reduce the antihypertensive effect, baclofen - Strengthens.

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.

Angiotensin converting enzyme (ACE) inhibitors increase the risk of arterial hypotension and / or acute renal failure (especially with existing renal artery stenosis).

Imipramine (tricyclic) antidepressants and antipsychotic drugs (neuroleptics) increase the antihypertensive effect and increase the risk of developing orthostatic hypotension.

Cyclosporine and tacrolimus increase the risk of hypercreatininaemia.

Special instructions:

In patients taking cardiac glycosides, laxative drugs, against hyperaldosteronism, as well as in the elderly, careful monitoring of the content of potassium and creatinine ions is shown.

Against the background of the drug should be systematically monitor the content of ions of potassium, sodium, magnesium in the blood plasma (may cause electrolyte disorders), pH, the concentration of glucose, uric acid and residual nitrogen. The most thorough control is indicated in patients with cirrhosis of the liver (especially with edema or ascites - the risk of developing metabolic alkalosis, enhancing the manifestation of hepatic encephalopathy), coronary heart disease, chronic heart failure, and 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 concentration of potassium ions in blood plasma should be performed within 1 week of treatment.

Hypercalcemia associated with the administration of the drug Acrypamide® retard may be a consequence of previously undiagnosed hyperparathyroidism.

In patients with diabetes, it is extremely important to monitor the concentration of glucose in the blood plasma, especially in the presence of hypokalemia.

A significant decrease in the volume of circulating blood can lead to the development of acute renal failure (decreased glomerular filtration rate). Patients need to compensate for fluid loss, and at the beginning of treatment carefully monitor kidney function.

Acrypamide® retard can give a positive result in doping control. Patients with hypertension and hyponatremia (due to taking diuretics) should stop taking diuretics 3 days before the initiation of angiotensin-converting enzyme (ACE) inhibitors (if necessary, diuretics can be taken a little later) or they are given initial low doses of ACE inhibitors.

In patients with elevated uric acid concentration in blood plasma, the frequency of gout attacks may increase with therapy.

With the use of thiazide-like diuretics, cases of the development of photosensitivity reactions were noted. If they develop, the drug should be discontinued. On the background of therapy with the drug Acrypamide® retard, it is necessary to protect the exposed areas of the body from exposure to sunlight and artificial ultraviolet radiation.

It can aggravate the course of systemic lupus erythematosus:

Efficiency and safety in children are not established.

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

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

Form release / dosage:Tablets of prolonged action, film-coated, 1.5 mg.

Packaging:

For 10 tablets in a planar cell package.

3 or 6 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001136

Date of registration:04.08.2011

Expiration Date:Unlimited

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp03.07.2017

Illustrated instructions

Instructions

Acrypamide® retard (Akripamide® retard)