Rilmenidine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

I1-imidazoline receptor agonists

Included in the formulation

Albarel®

pills inwards

EGIS ZAO Pharmaceutical Plant Hungary

АТХ:

C.02.A.C Imidazoline receptor agonists

C.02.A.C.06 Rilmenidine

Pharmacodynamics:

Antihypertensive drug, an oxazoline derivative. Selectively interacts with imidazoline receptors (I₁) cortical and peripheral vasomotor centers, in particular kidney centers. The binding of rilmenidine to imidazoline receptors inhibits the sympathomimetic activity of both cortical and peripheral centers, which leads to a reduction in blood pressure.

Rilmenidine has a dose-dependent hypotensive effect on systolic and diastolic blood pressure in a supine and standing position. It has been shown that the administration of rilmenidine at therapeutic doses (1 or 2 mg / day) is effective in the treatment of mild to moderate arterial hypertension. The effect of the drug persists for 24 hours, is effective during exercise. With prolonged use, addiction does not develop.

In therapeutic doses rilmenidine does not affect the function of the heart, does not cause delay of sodium and water, does not disturb the metabolic balance.

Rilmenidine reduces OPSS without changes in cardiac output. Myocardial contractility and electrophysiological indices remain unchanged.

Rilmenidine does not cause orthostatic hypotension (including in elderly people); does not violate the compensatory physiological reaction of the heart rhythm to the physical load; does not affect renal blood flow, glomerular filtration or filtration fraction; does not affect carbohydrate and lipid metabolism (including in patients with insulin-dependent and non-insulin-dependent diabetes mellitus).

Pharmacokinetics:

After taking the drug inside rilmenidine quickly and completely absorbed from the digestive tract. After a single dose of rilmenidine at a dose of 1 mg C_max in plasma is achieved after 1.5-2 hours and is 3.5 ng / ml. Absolute bioavailability is 100%; is not exposed to the effect of "first passage" through the liver. Absorption occurs identically in different patients: interindividual changes are not noted. Simultaneous food intake does not affect bioavailability. 65% of the accepted dose is excreted unchanged in the urine. Kidney clearance is 2/3 of the total clearance.

Half-lifeis 8 hours; Do not change when reappointed.

Indications:

Arterial hypertension.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

Contraindications:

Hypersensitivity, depression, chronic renal failure (CC <15 ml / min), pregnancy, breast-feeding, children's age (lack of sufficient clinical experience).

Carefully:Simultaneous use with alcohol, beta-adrenoblockers, used for the therapy of heart failure (bisoprolol, metoprolol, carvedilol); recently suffered stroke or myocardial infarction.

Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. Do not apply! There is no information on the penetration into breast milk. Do not apply!

Category of recommendations FDA is not defined.

Dosing and Administration:

The recommended dose of rilmenidine is 1 mg / day (1 tab.) In the morning.

If the BP does not decrease enough after one month of treatment, the dose can be increased to 2 mg / day in 2 divided doses (1 table in the morning and 1 tablet in the evening during meals).

In patients with mild and moderate renal insufficiency (QC more than 15 ml / min), dose adjustment is not required.

Treatment is long.

Side effects:

From the side of the central nervous system: possible asthenia, insomnia, drowsiness,increased fatigue during exercise; in isolated cases - anxiety, depression, convulsions.

From the cardiovascular system: palpitation is possible; in isolated cases - cold extremities, orthostatic hypotension.

From the digestive system: possible pain in the epigastrium, dry mouth, diarrhea; in isolated cases - nausea, constipation.

Dermatological reactions: rarely - skin rash, itching.

Other: in isolated cases - peripheral edema, hot flashes, sexual dysfunction.

Side effects are rarely seen, as a rule, are poorly expressed and have a transitory character.

Overdose:Symptoms: severe arterial hypotension, mental disorder, impaired consciousness.
Treatment: gastric lavage, the introduction of sympathomimetic drugs. Hemodialysis is ineffective.

Interaction:

The appointment of rilmenidine with tricyclic antidepressants reduces its antihypertensive effect.

The effect of rilmenidine is enhanced by vasodilators, diuretics and antihistamines.

When combined with drugs that have an inhibitory effect on the central nervous system, it may increase sleepiness.

Special instructions:

Central I agonist₁-imidazoline receptors of long-acting, insufficiently studied means.

Rilmenidine (1-2 mg / day 2 times a day) and moxonidine (0.2-0.4 mg / day once a day) are comparable in effectiveness (47-50% of participants - normalization of blood pressure) and safety in patients with mild and moderate hypertension (200 participants, RCT, double-blind).

In therapeutic doses does not affect psychomotor reactions. If the drug is prescribed in doses exceeding the therapeutic dose, or in combination with drugs depressing the central nervous system, patients, drivers and patients engaged in other potentially hazardous activities, should be warned about the possible occurrence of drowsiness.

Instructions

Rilmenidine (Rilmenidinum)

Arterial hypertension.