Albarel, pills 1mg, 30pcs

Composition

1 tablet contains:

Active ingredient:

rilmenidine 1 mg;

Auxiliary substances:

sodium carboxymethyl starch-4.5 mg;

MKC — 33,646 mg;

lactose — 47 mg;

paraffin solid — 0,155 mg;

silicon dioxide colloidal anhydrous — 0.23 mg;

magnesium stearate — 0.9 mg;

talc 2 mg;

beeswax white — 0.025 mg

Pharmacological action

Pharmacodynamics

ALBAREL derived oxazoline, selectively interacts with imidazoline receptors (I1) 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), due to a decrease in total peripheral resistance.

ALBARELLE has a dose-dependent antihypertensive effect on systolic and diastolic blood pressure in the supine and standing positions.

Double-blind placebo-controlled studies and comparative studies with reference drugs revealed the antihypertensive effectiveness of ALBARELLE in therapeutic doses (1 mg per day in one dose or 2 mg per day in two doses)in mild and moderate arterial hypertension. With this dosage regimen, the antihypertensive effect was maintained for 24 hours throughout the entire study period. In long-term studies, there was no weakening of the antihypertensive effect.

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

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

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

ALBAREL does not affect carbohydrate and fat metabolism, including in patients with type I and type II diabetes mellitus.

Pharmacokinetics

Suction

Suction occurs:

fast: maximum plasma concentration (3.5 ng/ml) is reached in 1 1/2-2 hours after a single dose of ALBAREL at a dose of 1 mg;

completely: absolute bioavailability is 100% without the effect of first passage through the liver;

the same in different patients: no interindividual changes were noted.

Simultaneous food intake does not affect bioavailability when using the recommended therapeutic doses.

Distribution

Binding to plasma proteins is less than 10%.

Metabolism

ALBAREL is very poorly metabolized. The 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 adrenergic receptors.

Excretion

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

The elimination half-life is 8 hours. It doesn’t change when you re-assign it. The duration of the pharmacological effect is longer, the antihypertensive effect is significantly maintained for 24 hours after taking ALBAREL at a dose of 1 mg per day.

After reappointment

Stabilization of the plasma concentration is achieved from the third day of regular use of the drug and remains at the same level in the future.

Long-term monitoring of plasma levels

In patients with arterial hypertension who have been treated for 2 years, the concentration of ALBARELLE in plasma remains stable.

In elderly patients

, pharmacokinetic studies in patients aged 70 years and older have shown that the half-life is 13+ / -1 hours.

In patients with hepatic insufficiency

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

In patients with renal insufficiency

Since the elimination of ALBAREL is mainly renal, in such patients there is a slowdown in the elimination of the drug, which correlates with the value of creatinine clearance. In patients with severe renal insufficiency (creatinine clearance less than 15 ml / min), the elimination half-life is approximately 35 hours.

Indications

Arterial hypertension.

Use during pregnancy and lactation

During pregnancy: ALBARELLE is contraindicated in pregnant women, although no teratogenic or embryotoxic effects have been observed in animal experiments.

During breast-feeding: since ALBAREL is excreted in breast milk, its use is not recommended during the feeding period.

Contraindications

• Hypersensitivity to the drug
• Severe depression
• Severe renal insufficiency (creatinine clearance less than 15 ml / min)

Side effects

Side effects are rare.

They are usually mild and transient: asthenia, palpitations, insomnia, drowsiness, increased fatigue during exercise, epigastric pain, dry mouth, diarrhea, skin rash and, in exceptional cases, cold extremities, orthostatic hypotension, fear, depression, itching, peripheral edema, convulsions, nausea, constipation and hot flashes.

Interaction

Concomitant use of ALBARELLE with MAO inhibitors is not recommended.

use of ALBARELLE with tricyclic antidepressants reduces its antihypertensive effect.

How to take, course of use and dosage

It is taken orally.

The recommended dose is 1 tablet per day in the morning. If blood pressure decreases insufficiently after one month of treatment, the dose can be increased to 2 tablets per day with a double dose (one tablet in the morning and one tablet in the evening during meals).

Due to its good tolerability, ALBAREL can be prescribed to elderly patients with arterial hypertension and patients with diabetes mellitus with arterial hypertension. In case of renal insufficiency, if the creatinine clearance is greater than 15 ml / min, no dose adjustment is required. Treatment should be prolonged.

If it is necessary to stop treatment, the dose should be reduced gradually, although it is unlikely that discontinuation of the drug will be accompanied by any side effect.

Overdose

In the case of taking a large amount of the drug, the expected symptoms may be: severe arterial hypotension, mental disorders. In addition to gastric lavage, sympathomimetic agents can be used.

ALBAREL is poorly excreted by hemodialysis.

Special instructions

For patients with recent stroke or myocardial infarction, the appointment of ALBARELLE requires periodic medical monitoring. Alcohol intake is not recommended during treatment with ALBAREL. In case of renal insufficiency, if the creatinine clearance is greater than 15 ml / min, no dose adjustment is required.

Due to the lack of sufficient clinical data, ALBAREL should not be prescribed to children.

Impact on the ability to drive vehicles and work on machine tools

Double-blind placebo-controlled studies did not show any effect of ALBARELLE in therapeutic doses on psychomotor status. If the drug is prescribed in higher than therapeutic doses or in combination with medications that inhibit the activity of the central nervous system, drivers and operators should be warned about the possibility of drowsiness.

Form of production

Tablets

Storage conditions

At temperatures below 30 °C

Shelf life

2 years

Active ingredient

Rilmenidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Hypertension