Albarel^® (Tablets) Instructions for Use

Marketing Authorization Holder

Egis Pharmaceuticals PLC (Hungary)

Manufactured By

Les Laboratoires Servier Industrie (France)

Packaging and Quality Control Release

EGIS Pharmaceuticals, PLC (Hungary)

ATC Code

C02AC06 (Rilmenidine)

Active Substance

Rilmenidine (Rec.INN registered by WHO)

Dosage Form

Albarel®

Tablets 1 mg: 10, 20 or 30 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, round, biconvex, with an engraving on both sides of the tablet in the form of the sign “H”.

Excipients: sodium carboxymethyl starch – 4.5 mg, microcrystalline cellulose – 33.646 mg, lactose monohydrate – 47 mg, hard paraffin – 0.155 mg, colloidal anhydrous silicon dioxide – 0.23 mg, magnesium stearate – 0.9 mg, talc – 2 mg, white beeswax – 0.025 mg.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Selective imidazoline receptor agonist. Antihypertensive drug

Pharmacotherapeutic Group

Antihypertensive agents; centrally-acting antiadrenergic agents; imidazoline receptor agonists

Pharmacological Action

Antihypertensive agent, belongs to the group of oxazolines. It selectively binds to imidazoline I₁ receptors of central and peripheral (predominantly renal) vasomotor centers. The binding of rilmenidine to imidazoline receptors inhibits the sympathomimetic activity of cortical and peripheral centers and leads to a decrease in blood pressure.

It causes a dose-dependent decrease in systolic and diastolic blood pressure, and acts in both the lying and standing positions of the patient.

At therapeutic doses, the duration of action is 24 hours.

Pharmacokinetics

After oral administration, it is rapidly absorbed (food intake has practically no effect on the rate and extent of absorption). C_max (3.5 ng/ml) is determined 1.5-2 hours after a single dose of 1 mg of rilmenidine, bioavailability is 100%. Plasma protein binding is less than 10%. V_d – 5 l/kg. Only a small part of the absorbed active substance is metabolized (metabolites are pharmacologically inactive). It is excreted mainly by the kidneys – 65% unchanged. Renal clearance is 2/3 of the total. T_1/2 is about 8 hours, does not depend on the dose and duration of administration. C_ss is established after 3 days. In elderly patients (over 70 years old), T_1/2 increases to 13 hours, in patients with hepatic insufficiency – to 12 hours, in patients with chronic renal failure (creatinine clearance 15 ml/min) – to 35 hours. It is excreted in breast milk.

Indications

Essential arterial hypertension.

ICD codes

Dosage Regimen

Administer the tablets orally, swallowed whole with a sufficient amount of water.

Initiate therapy at the recommended starting dose of 1 mg once daily.

Take the daily dose in the morning.

After a treatment period of one month, evaluate the therapeutic response.

If the expected antihypertensive effect is not achieved, increase the dose to 2 mg per day.

Administer the 2 mg daily dose as 1 mg twice daily, typically in the morning and evening.

Do not exceed the maximum daily dose of 2 mg.

For patients with moderate renal impairment (creatinine clearance 15-30 ml/min), exercise caution; the need for dose adjustment should be individually assessed.

In elderly patients, initiate treatment at the standard starting dose of 1 mg once daily; monitor for potential adverse reactions due to possible prolonged elimination half-life.

Conduct long-term treatment under regular medical supervision to monitor blood pressure control and tolerability.

Adverse Reactions

From the cardiovascular system: palpitations; in isolated cases – cold extremities, orthostatic hypotension, hot flushes.

From the central nervous system: insomnia, drowsiness, weakness during physical exertion; in isolated cases – anxiety, depression, convulsions.

From the digestive system: pain in the epigastric region, dry mouth, diarrhea; in isolated cases – nausea, constipation.

Dermatological reactions: skin rash, edema; in isolated cases – itching.

Other: in isolated cases – sexual dysfunction.

Contraindications

Severe depression, chronic renal failure (creatinine clearance <15 ml/min), pregnancy, lactation, hypersensitivity to rilmenidine.

Use in Pregnancy and Lactation

Should not be used during pregnancy. If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided, because Rilmenidine may be excreted in breast milk. Experimental studies have shown that Rilmenidine does not have a teratogenic or embryotoxic effect.

Use in Renal Impairment

Contraindicated in chronic renal failure (creatinine clearance <15 ml/min).

Pediatric Use

The safety and efficacy of rilmenidine in children have not been established, therefore use is not recommended.

Special Precautions

Patients after a stroke and myocardial infarction require periodic medical examination during treatment.

Rilmenidine should not be used in severe renal failure (creatinine clearance less than 15 ml/min).

The use of rilmenidine in combination with MAO inhibitors is not recommended.

Alcohol consumption is not recommended during treatment.

Use in pediatrics

The safety and efficacy of rilmenidine in children have not been established, therefore use is not recommended.

Effect on the ability to drive vehicles and operate machinery

According to clinical studies, Rilmenidine in therapeutic doses (1-2 mg/day) does not affect the ability to concentrate. If the therapeutic dose is exceeded or when used in combination with drugs that can reduce the ability to concentrate, drowsiness may occur. This should be taken into account when using rilmenidine in patients engaged in potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug Interactions

With simultaneous use with vasodilators, diuretics and antihistamines, the antihypertensive effect of rilmenidine is enhanced.

With simultaneous use with tricyclic antidepressants, the antihypertensive effect of rilmenidine is reduced.

With simultaneous use with drugs that have a depressant effect on the central nervous system, drowsiness may be enhanced.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.