Albarel, tablets 1 mg 30 pcs

Pharmacodynamics

ALBAREL, an oxazoline derivative, selectively interacts with imidazoline receptors (I1) of brain and peripheral vasomotor structures and kidneys. Binding of rilmenidine to imidazoline receptors (I1) inhibits sympathomimetic activity, which leads to a decrease in blood pressure (BP), by reducing total peripheral resistance.

ALBAREL exhibits dose-dependent hypotensive effects on systolic and diastolic BP in the prone and standing position.

Double-blind placebo-controlled studies and comparative studies with reference drugs have demonstrated the antihypertensive efficacy of ALBAREL at therapeutic doses (1 mg daily in one sitting or 2 mg daily in two sitting) for mild to moderate arterial hypertension. With this dosing regimen, the hypotensive effect was maintained for 24 hours throughout the duration of the study. No attenuation of the hypotensive effect was noted in long-term studies.

In therapeutic doses ALBAREL does not affect cardiac function and does not lead to sodium and water retention.

ALBAREL does not cause orthostatic phenomena, including in elderly persons. It does not interfere with the physiological response manifested by changes in heart rate in response to physical activity.

ALBAREL does not affect renal blood flow, glomerular filtration or filtration fraction.

ALBAREL has no effect on carbohydrate and fat metabolism, including in patients with diabetes types I and II.

Pharmacokinetics

Intake

Intake:

Quickly: maximum plasma concentration (3.5 ng/mL) is reached 1 1/2 to 2 hours after a single dose of 1 mg of ALBAREL;

full: Absolute bioavailability is 100% with no effect of first passage through the liver;

different between patients: no interindividual variation noted.

Simultaneous ingestion does not affect bioavailability using the recommended therapeutic doses.

Distribution

The binding to plasma proteins is less than 10%.

Metabolism

ALBAREL is very poorly metabolized. Metabolites are found in trace amounts in the urine and are the result of hydrolysis or oxidation of the oxazoline ring. These metabolites do not bind to alpha-2 adrenoreceptors.

Elimation

ALBAREL is mainly excreted via the kidneys: 65% of the administered dose is excreted unchanged in the urine. Renal clearance represents two-thirds of total clearance.

The elimination half-life is 8 hours. It does not change with repeated administration. The duration of the pharmacological effect is longer; the hypotensive effect is significantly maintained for 24 hours after administration of ALBAREL at a dose of 1 mg per day.

After repeated administration

Plasma concentration stabilization is achieved from the third day of regular drug administration and is maintained at the same level thereafter.

Long-term monitoring of plasma levels

In patients with arterial hypertension who have been treated for 2 years, plasma concentrations of ALBAREL remain stable.

In elderly patients

Pharmacokinetic studies in patients aged 70 years and older have shown a half-life of 13+/-1 hours.

In patients with impaired liver function

The half-life is 12+/-1 hours.

In patients with impaired renal function

Because excretion of ALBAREL is primarily renal, these patients have slower drug excretion which correlates with the creatinine clearance value. In patients with severe renal insufficiency (creatinine clearance less than 15 ml/min) the elimination half-life is approximately 35 hours.

Indications

Hypertension (high blood pressure)

Arterial hypertension.

Active ingredient

Rilmenidine

Composition

1 tablet contains:

The active ingredient:

rilmenidine 1 mg;

Associates:

sodium carboxymethyl starch – 4.5 mg;

MCC – 33.646 mg;

lactose – 47 mg;

solid paraffin – 0.155 mg;

Colloidal anhydrous silica – 0.23 mg;

Magnesium stearate – 0.9 mg;

Talc, 2 mg;

White beeswax, 0.025 mg.