Arifam (indapamide) tablets with modified release 1.5 mg/10 mg. №30

Ingredients

active substances: indapamide, amlodipine;

1 tablet contains:

• 1.5 mg of indapamide and 6.935 mg of amlodipine besylate, corresponding to 5 mg of amlodipine, or 13.87 mg of amlodipine besylate, corresponding to 10 mg of amlodipine;

excipients: hypromellose 4000 (E 464), lactose monohydrate, magnesium stearate (E 572), povidone (E 1201), colloidal anhydrous silicon dioxide, calcium hydrogen phosphate, microcrystalline cellulose (E 460), croscarmellose sodium (E 468), corn starch pregelatinized; film shell: glycerin (E 422), hypromellose (E 464), macrogol 6000, magnesium stearate (E 572), titanium dioxide (E 171), iron oxide red (E 172) (Arifam® 1.5 mg/10 mg) .

Medicinal form

Tablets with modified release.

The main physical and chemical properties:

Arifam 1.5 mg/5 mg: a tablet covered with a white film coating, round in shape, embossed on one side.

Arifam 1.5 mg/10 mg: a pink film-coated tablet, round in shape, embossed on one side.

Pharmacotherapeutic group

Blockers of calcium channels and diuretics. Amlodipine and diuretics. ATX code C08G A02.

Pharmacological properties

Pharmacodynamics.

Mechanism of action

Indapamide is a sulfonamide derivative with an indole ring, pharmacologically related to thiazide diuretics, which acts by inhibiting sodium reabsorption in the cortical segment of the kidneys. It increases urinary excretion of sodium and chloride and to a lesser extent potassium and magnesium, thus increasing urine output and providing an antihypertensive effect.

Amlodipine is an inhibitor of the influx of calcium ions from the group of dihydropyridines (a blocker of slow calcium channels or an antagonist of calcium ions), which prevents the transmembrane influx of calcium ions into the smooth muscles of the myocardium and blood vessels. The mechanism of antihypertensive action of amlodipine is its ability to relax vascular smooth muscles.

Pharmacodynamic effects

Phase II and III clinical studies demonstrated that the antihypertensive effect lasts 24 hours when indapamide is used as monotherapy. This effect is manifested in doses in which diuretic properties are minimal. The antihypertensive effect of indapamide is associated with improvement of arterial elasticity, reduction of arteriole resistance and general peripheral vascular resistance. Indapamide reduces left ventricular hypertrophy.

If the recommended dose is exceeded, the therapeutic effect of thiazide and thiazide-like diuretics does not increase, while the number of side effects increases. If there is no effect from the treatment, the dose should not be increased.

Also, in the course of short-, medium- and long-term studies involving patients with arterial hypertension, it was demonstrated that indapamide:

• does not affect the metabolism of lipids (triglycerides, low- and high-density lipoproteins);
• does not affect carbohydrate metabolism, even in diabetics with arterial hypertension.

In patients with arterial hypertension, taking amlodipine 1 time per day provides a clinically reliable reduction in blood pressure during 24 hours both in the supine and standing position. Due to the slow onset of action of amlodipine, its use does not lead to acute hypotension. Amlodipine has not been associated with any metabolic side effects or changes in plasma lipids, so it can be used in patients with asthma, gout and diabetes.

Indication

Treatment of essential hypertension in patients requiring treatment with indapamide and amlodipine at doses available in fixed combinations.

Arifam’s contraindications

• Hypersensitivity to active substances, other sulfonamides, dihydropyridine derivatives or any auxiliary substances of the drug;
• severe renal failure (creatinine clearance < 30 ml/min);
• hepatic encephalopathy or severe liver dysfunction;
• hypokalemia;
• breastfeeding period;
• severe hypotension;
• shock (including cardiogenic);
• obstruction of the exit from the left ventricle (for example, severe aortic stenosis);
• heart failure with unstable hemodynamics after acute myocardial infarction.

Dosage and Administration

For oral use.

One tablet per day once, preferably in the morning before meals. The tablet is swallowed whole, without chewing, with water. The maximum daily dose is 1 tablet (1.5 mg/10 mg).

The use of a fixed combination is not intended to initiate therapy.

If it is necessary to change the dosage, individual titration of each of the components of the combination should be carried out.

Special groups of patients

Patients with impaired renal function. In severe renal impairment (creatinine clearance < 30 ml/min), treatment with the drug is contraindicated. No adjustment of the recommended dose is required for patients with mild to moderate renal impairment.

Elderly patients.

In elderly patients, Arifam should be used taking into account kidney function.

Patients with impaired liver function. Treatment with the drug is contraindicated in severe liver function disorders. For patients with impaired liver function of mild and moderate severity, recommendations for the dosage of amlodipine have not been established, so the dose should be selected with caution and treatment should be started with the lowest dose.