Arifon, pills 2.5mg, 30pcs

Composition

1 tablet contains:

Active ingredient:

indapamide 2.5 mg;

Auxiliary substances:

lactose monohydrate-59.25 mg;

corn starch-20.00 mg;

magnesium stearate-0.75 mg;

povidone-4.00 mg;

talc — 3.5 mg;

Film shell:

glycerol-0.087 mg; macrogol 6000-0.035 mg; magnesium stearate-0.087 mg; hypromellose-1.449 mg; sodium lauryl sulfate-0.017 mg; titanium dioxide-0.278 mg; white beeswax-0.047 mg.

Composition

:  a diuretic.

Pharmaceutical action:  

Antihypertensive agent (diuretic, vasodilator)Pharmacological properties are similar to thiazide diuretics (violation of Na+ reabsorption in the cortical segment of the Henle loop). Increases urinary excretion of Na+, Cl – and to a lesser extent K+ and Mg2+. Having the ability to selectively block “slow” calcium channels, it increases the elasticity of arterial walls and reduces OPSS. Helps to reduce LV hypertrophy of the heart.

It does not affect the content of lipids in plasma (TG, LDL, HDL); it 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 PgE2 and prostacyclin PgI2, reduces the production of free and stable oxygen radicals. When administered in high doses, it does not affect the degree of blood pressure reduction, despite an increase in diuresis.

After repeated use, the therapeutic effect is noted after 1-2 weeks, reaches a maximum by 8-12 weeks and persists for up to 8 weeks; after taking a single dose, the maximum effect is noted after 24 hours

. Pharmacokinetics:  

It is rapidly and completely absorbed from the gastrointestinal tract; bioavailability is high. Food intake slightly slows down the rate of absorption, but does not affect the total amount of absorbed drug. TCmax – 1-2 hours after taking the usual dosage form and 12 hours after taking retard tablets. Cmax after oral use at a dose of 5 mg – 260 ng / ml. With repeated doses, fluctuations in the concentration of the drug in plasma in the interval between 2 doses are reduced. Css is set after 7 days of regular admission.

Plasma protein binding is 71-79%. It also binds to the smooth muscle elastin of the vascular wall. It has a high volume of distribution, passes through histohematic barriers (including placental).

It is metabolized in the liver. T1 / 2-14 h, the final T1 / 2-26 h. 60-70% is excreted by the kidneys in the form of metabolites (about 5-7% is excreted unchanged), and 20-23% is excreted through the intestine. In patients with renal insufficiency, the pharmacokinetics do not change. It doesn’t accumulate.

Indications

Arterial hypertension.

Use during pregnancy and lactation

As a rule, Arifon is not recommended for use during pregnancy, including for the removal of physiological edema. It should be borne in mind that diuretics can cause fetoplacental ischemia and lead to impaired fetal development.

Due to the fact that indapamide is excreted in breast milk, it is also not recommended to prescribe the drug during breastfeeding. If therapy is necessary, breast-feeding should be discontinued.

Contraindications

• hepatic encephalopathy;
• severe renal failure;
• hypokalemia;
• hypersensitivity to sulfonamide derivatives.

Simultaneous use of Arifon and drugs that prolong the QT interval should be avoided.

Interaction

Concomitant use of indapamide and tricyclic antidepressants such as imipramine increases the hypotensive effect and increases the risk of orthostatic hypotension.

With the simultaneous use of thiazide diuretics and calcium salts, hypercalcemia may develop due to a decrease in the excretion of calcium ions in the urine. With the simultaneous use of indapamide and cyclosporine, an increase in the content of creatinine in blood plasma is possible, which is observed even with a normal content of water and sodium ions. With the simultaneous use of thiazide diuretics and lithium preparations, an increase in the concentration of lithium in blood plasma is possible, accompanied by the appearance of signs of overdose, (due to a decrease in the excretion of lithium in the urine).

If it is necessary to prescribe this combination, the concentration of lithium in the blood plasma should be monitored. Concomitant use of diuretics with astemizole, bepridil, erythromycin (IV), halofantrine, pentamidine, sultoprid, terfenadine, vincamine increases the likelihood of arrhythmia of the “pirouette”type. Hypokalemia, bradycardia, or an extended QT interval may contribute to this condition.

When used concomitantly with cardiac glycosides, the toxic effect of the latter may increase (it is necessary to monitor the level of potassium in the blood plasma and ECG indicators). When used concomitantly with NSAIDs (for systemic use), high doses of salicylates may reduce the hypotensive effect of indapamide.

With significant fluid loss, acute renal failure may develop (due to a sharp decrease in glomerular filtration). If necessary, NSAIDs should be prescribed during Arifon therapy, water loss should be compensated and renal function should be carefully monitored. Concomitant use of indapamide with other drugs that may cause hypokalemia, including amphotericin B (IV), gluco-and mineralocorticoids (with systemic use), tetracosactide, laxatives that stimulate intestinal motility, increases the risk of hypokalemia (requires constant monitoring of the level of potassium in the blood plasma and, if necessary, appropriate treatment).

With the simultaneous use of thiazide diuretics with corticosteroids, tetracosactide for systemic use, a decrease in the hypotensive effect is observed due to the retention of water and sodium ions under the influence of corticosteroids. When indapamide is co-administered with baclofen, the hypotensive effect increases (it is necessary to compensate for water loss and carefully monitor renal function at the beginning of treatment). With the simultaneous use of indapamide and potassium-sparing diuretics (including amiloride, spironolactone, triamterene), the possibility of hypokalemia or hyperkalemia cannot be completely excluded, especially in patients with diabetes mellitus and renal insufficiency.

In such cases, the level of potassium in the blood plasma, ECG parameters should be monitored and, if necessary, therapy should be adjusted. When indapamide is co-administered with ACE inhibitors, hyponatremia in patients receiving ACE inhibitors increases the risk of sudden hypotension and / or acute renal failure (especially in patients with renal artery stenosis). Patients with essential arterial hypertension and reduced levels of sodium ions in the blood plasma due to diuretics should stop taking diuretics 3 days before starting treatment with ACE inhibitors.

In the future, if necessary, the use of diuretics should be resumed. In addition, low, gradually increasing doses of ACE inhibitors are prescribed. In patients with chronic heart failure, treatment should begin with low doses of ACE inhibitors, first reducing the dose of diuretics. In all cases, renal function (plasma creatinine) should be monitored during the first week of ACE inhibitor therapy.

When indapamide is co-administered with antiarrhythmic drugs that can cause pirouette-type arrhythmias (including quinidine, hydroquinidine, disopyramide, amiodarone, bretilium, sotalol), the risk of developing this condition increases (especially against the background of hypokalemia, bradycardia, and initially prolonged QT interval). If it is necessary to prescribe this combination, the level of potassium in the blood plasma and the QT interval should be monitored, adjusting the dosage regimen.

Concomitant use of diuretics and metformin may cause lactic acidosis, which is probably associated with the development of functional renal failure due to the action of diuretics (mostly “loop”). It is not recommended to use metformin in combination with Arifon if the creatinine level exceeds 15 mg / l (135 mmol/l) in men and 12 mg/l (110 mmol/l) for women.

When using iodine-containing radiopaque drugs, it should be borne in mind that the diuretic effect of indapamide increases the risk of developing renal failure. This risk is especially high when using iodine-containing radiopaque substances in high doses. Before using iodine-containing radiopaque substances, patients need to restore fluid loss.

How to take it, course of use and dosage

Inside, preferably in the morning,1 tablet per day.

In the treatment of patients with arterial hypertension, the dose of the drug should not exceed 2.5 mg / day(an increase in the risk of side effects without increasing the antihypertensive effect).

Overdose

Symptoms:  possible disorders of the water-electrolyte balance (hyponatremia, hypokalemia), nausea, vomiting, hypotension, convulsions, dizziness, drowsiness, confusion, polyuria or oliguria, ending in anuria (due to hypovolemia).

Treatment:  urgent measures aimed at removing the drug from the body: washing the gastrointestinal tract and / or prescribing activated carbon, followed by restoring normal water and electrolyte balance.

Special instructions

When prescribing Arifon to patients with diabetes mellitus, it is extremely important to monitor glucose levels, especially in the presence of hypokalemia. In patients with high uric acid content, there is a tendency to increase the number of gout attacks.

When prescribing thiazide diuretics to patients with hepatic insufficiency, hepatic encephalopathy may develop.In such cases, the drug should be discontinued immediately.

Thiazide diuretics show their full effectiveness only in the absence of violations or with moderate violations of renal function (blood creatinine content less than 25 mg/l or 220 mmol/l).

In elderly patients, the normal level of creatinine in blood plasma is calculated taking into account the age, body weight and gender of the patient according to the Cockcroft formula:

CLcr=(140-age /in years/) x body weight (kg)/0.814 x plasma creatinine (mmol / l).

This formula is used to calculate creatinine levels in men, and for women, the final result should be multiplied by 0.85.

It should be borne in mind that at the beginning of treatment, patients may experience a decrease in glomerular filtration due to hypovolemia, which is caused by the loss of water and sodium ions against the background of taking diuretics. As a result, the concentration of urea and creatinine in the blood plasma may increase. If kidney function is not impaired, such temporary renal failure usually passes without consequences. However, if you already have kidney failure, the patient’s condition may worsen.

Against the background of Arifon therapy, an exacerbation of disseminated lupus erythematosus is possible.

Before starting treatment, the content of sodium ions in the blood plasma should be determined. During treatment, regular monitoring of this indicator is necessary, since initially a decrease in the concentration of sodium in the blood plasma may not be accompanied by the appearance of pathological symptoms. Especially often, such an analysis should be performed in patients with cirrhosis of the liver and in the elderly.

When using thiazide diuretics, the main risk is a sharp decrease in the content of potassium ions and the development of hypokalemia. In a certain category of patients, especially the elderly, weakened or receiving concomitant therapy, with cirrhosis of the liver with developed edema or ascites, CHD, chronic heart failure, it is necessary to avoid the development of hypokalemia ( Hypokalemia, as well as bradycardia, is a condition that contributes to the development of severe cardiac arrhythmias, especially the “pirouette” type, which often leads to fatal outcomes. In all the cases described above, it is necessary to determine the content of potassium ions in the blood plasma more often. The first measurement of the potassium ion concentration in the blood should be carried out within the first week after the start of treatment.

If hypokalemia occurs, appropriate treatment should be prescribed, while avoiding the use of drugs that cause pirouette-type arrhythmias. If such a rhythm disorder occurs, antiarrhythmic drugs should not be used, but an artificial rhythm driver should be installed.

It should be borne in mind that thiazide diuretics can reduce the excretion of calcium ions in the urine, which leads to minor and temporary hypercalcemia. Severe hypercalcemia may be a consequence of previously undiagnosed hyperparathyroidism. Diuretics should be discontinued before starting a parathyroid function study.

If it is necessary to prescribe laxatives against the background of Arifon therapy, drugs that do not affect intestinal motility should be prescribed.

Against the background of taking indapamide, a positive result is possible during doping control in athletes. An increase in the dose of thiazide diuretics above the optimal one is not accompanied by an increase in the antihypertensive effect, but may be accompanied by the occurrence of pronounced adverse reactions. If therapy with thiazide diuretics does not lead to the desired therapeutic effect, the dose of the drug should not be increased.

When used concomitantly with other antihypertensive drugs, the dose of Arifon should be reduced, at least at the beginning of treatment.

Use in pediatrics

Due to the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents under 18 years of age.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect of the substances that make up Arifon does not lead to a violation of psychomotor reactions. However, it should be borne in mind that in some cases, individual reactions may occur with a decrease in blood pressure (especially at the beginning of therapy or with a combination of several antihypertensive drugs). In this case, the ability to perform work that requires increased attention and speed of psychomotor reactions may be reduced.

Form of production

Pills.

Storage conditions

The drug should be stored in a dry place at a temperature not exceeding 30°C.

Shelf life

5 years

Active ingredient

Indapamide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension