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

The tablets covered with a film cover, round, white or white with a creamy or grayish shade of color, round, biconcave. Roughness is allowed. On the break the tablets are white or almost white in color.

Pharmacotherapeutic group:Diuretics

ATX: & nbsp

C.03.B.A.11 Indapamide

Pharmacodynamics:

Hypotensive 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 excretion in the urine 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 overall peripheral vascular resistance. Helps reduce hypertrophy of the left ventricle of the heart. Does not affect the content of lipids in the 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 noradrenaline and angiotensin II, stimulates the synthesis PgE2 and prostacyclia 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 by 8-12 weeks and lasts up to 8 weeks; after taking a single dose the maximum effect is observed after 24 hours.

Pharmacokinetics:

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract. Bioavailability is high (93%). Eating somewhat slows down the speed, but does not affect the final amount of absorbed drug. The maximum concentration in the blood is reached after 1-2 hours. The maximum concentration after oral administration at a dose of 5 mg is 260 ng / l. At repeated receptions of fluctuation of concentration of a preparation in plasma in an interval between receptions of two doses decrease. Equilibrium concentration is achieved after 7 days of regular intake. The preparation binds to blood plasma proteins by 70-80%. 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. It is excreted from the body by the kidneys (up to 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:

Increased sensitivity to the drug and other derivatives of the sulfonamide, anuria, severe liver failure (including encephalopathy) and / or renal failure, hypokalemia, simultaneous drug prolonging the interval QT, pregnancy, lactation, children under 18 years of age (efficacy and safety not established).

Lactose intolerance, galactosemia, glucose / galactose absorption disorder.

Carefully:

Violations of water-electrolyte metabolism, hepatic and / or renal failure, lengthening of the interval QT, hyperuricemia (especially manifested by gout or urate nephrourolythiasis), hyperparathyroidism.

Dosing and Administration:

Inside, regardless of food intake, with enough liquid. Take the drug preferably in the morning. The daily dose is 1 tablet (2.5 mg).

If the desired therapeutic effect is not achieved after 4-8 weeks of therapy, the dose of the drug should not be increased (an increased risk of side effects without increasing the antihypertensive effect). Instead, it is recommended that another antihypertensive drug that is not a diuretic be included in the drug regimen.If you start treatment with two antihypertensive drugs, the dose of Acrypamide® remains 2.5 mg once in the morning.

Side effects:

From the cardiovascular system: orthostatic hypotension, arrhythmia, palpitations.

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

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

From the genitourinary system: nocturia, polyuria.

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

Allergic reactions: skin itch, patchy-papular rash, hives, hemorrhagic vasculitis.

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

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

Other: exacerbation of systemic lupus erythematosus.

Overdose:

Symptoms: nausea, vomiting, weakness, arterial hypotension, dizziness, drowsiness, confusion, respiratory depression, dysfunction of the gastrointestinal tract; in a patient with impaired liver function, hepatic coma may develop.

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

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 kidney dysfunction when using iodine-containing contrasting drugs in high doses (dehydration of the body). Before using iodine-containing contrast agents, patients need to restore fluid loss.

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 preparations of calcium ions - hypercalcemia; with metformin, aggravation of lactic acidosis is possible.

Astemizole, erythromycin (with intravenous administration), pentamidine, sultopride, terfenadine, wincamine, antiarrhythmic drugs Ia class (quinidine, disopyramide) and III class (amiodarone, brethil tosylate, sotalol) can lead to the development of arrhythmias of the "pirouette" type due to the synergistic effect (lengthening) on the duration of the interval Q-T.

Nonsteroidal anti-inflammatory drugs, glucocorticosteroids, tetracosactide, adrenostimulants reduce the hypotensive 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.

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 hypotensive effect and increase the risk of developing orthostatic hypotension.

Cyclosporine increases 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 taking Acrypamide ® should be systematically monitor the concentration of ions of potassium, sodium, magnesium in the 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. To the group of the raised risk also patients with the increased interval Q-T on ECG (congenital or developed against a background of some pathological process).

The first measurement of the concentration of potassium ions in the blood should be performed within 1 week of treatment.

Hypercalcemia on the background of taking Acrypamid® 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.

Acrypamide ® can give a positive result in the conduct of doping control.

Patients with arterial 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.

It can aggravate the course of systemic lupus erythematosus.

Efficiency and safety in children are not established.

Form release / dosage:

Tablets, film-coated, 2.5 mg.

Packaging:

10 tablets per contour cell pack.

1, 2 or 3 contour mesh packages together with the instruction for use are placed 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:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001371 / 01

Date of registration:28.11.2007

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® (Akripamide®)