Albarel - instructions for use, doses, side effects, contraindications

Active substanceRilmenidineRilmenidine

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Dosage form: & nbsppills

Composition:1 tablet contains 1.544 mg of rilmenidine dihydrogen phosphate, which corresponds to 1 mg of rilmenidine (active, substance). Auxiliary substances: sodium carboxymethyl starch 4.5 mg, microcrystalline cellulose 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.

Description:Round biconvex tablets of white color with engraving on both sides of the tablet in the form of the sign "H".

Pharmacotherapeutic group:Hypotensive central action.

ATX: & nbsp

C.02.A.C Imidazoline receptor agonists

C.02.A.C.06 Rilmenidine

Pharmacodynamics:

ALBAREL®, an oxazoline derivative with an antihypertensive effect, exerts selective effect on imidazoline receptors (I₁) cortical and peripheral vasomotor centers, in particular kidney centers / Binding of rilmenidine to imidazoline receptors (I₁) suppresses the sympathomimetic activity of both cortical and peripheral centers, which leads to a decrease in blood pressure (HELL).

In patients with arterial hypertension, ALBAREL® leads to a dose-dependent decrease in systolic and diastolic blood pressure both in the "lying" and "standing" positions.It was shown that the appointment of therapeutic doses of ALBAREL® (1 mg / day once or 2 mg / day in 2 doses) is effective in the treatment of mild to moderate degree of arterial hypertension. Operates for 24 hours and is effective during exercise. With prolonged use of the drug ALBAREL®, the addiction to the drug does not develop.

In therapeutic doses, ALBAREL® does not lead to fluid retention and electrolytes in the body and does not disturb the metabolic balance.

ALBAREL® retains significant antihypertensive activity 24 hours after admission, with a reduction in overall peripheral resistance without changes in cardiac output. Myocardial contractility and electrophysiological indices remain unchanged.

ALBAREL® does not affect orthostatic regulation, in particular in elderly patients, and also on the physiological compensatory response of the heart rhythm to physical activity.

ALBAREL® does not alter renal blood flow, glomerular filtration or filterable fraction.

Pharmacokinetics:Suction
The drug is rapidly absorbed. The maximum concentration in blood plasma (3.5 ng / ml) is achieved after 1.5-2 hours after a single dose of rilmenidine in a dose of 1 mg orally.Absolute bioavailability is 100% without the effect of "primary transmission" through the liver. Taking the drug simultaneously with food does not affect its bioavailability.
Distribution
Binding of the drug to plasma proteins is less than 10%. The volume of distribution is 5 l / kg.
Metabolism
Metabolites are found in trace amounts in urine and are the result of hydrolysis or oxidation of the oxazoline ring. These metabolites are not alpha-2 adrenergic receptor agonists.
Excretion
It is mainly excreted through the kidneys. 65% of the accepted dose is excreted unchanged in the urine. Kidney clearance is two-thirds of the total clearance.
The half-life is 8 hours. It does not change when the dose is changed or repeated administration of the drug.
Repeated administration of the drug
Equilibrium concentration is achieved after 3 days of taking the drug.
The content of the drug ALBAREL® in blood plasma with long-term drug intake
In patients with arterial hypertension receiving ALBAREL® for 2 years, the concentration of the drug in the plasma remains stable.
In elderly people
The half-life in patients aged 70 years and older is 13 ± 1 h.
Patients with hepatic insufficiency
The half-life is 12 ± 1 hours.
In patients with renal insufficiency
Since the excretion of the drug is carried out mainly by the kidneys, in such patients it slows down, which correlates with the creatinine clearance. In patients with severe renal failure (creatinine clearance less than 15 ml / min), the elimination half-life is approximately 35 hours.
Excreted in breast milk.

Indications:Arterial hypertension.

Contraindications:Hypersensitivity to rilmenidine and excipients of the drug; depression; severe renal failure (creatinine clearance less than 15 ml / min); pregnancy and lactation; age under 18 years (effectiveness and safety not established); deficiency of lactase, lactose intolerance, glucose-galactose malabsorption (the preparation contains lactose); simultaneous application with sultopride.

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:Due to the lack of clinical data, ALBAREL® is contraindicated in pregnancy, although there have been no teratogenic or embryotoxic effects in animal experiments.
Because the rilmenidine is excreted in breast milk, it is not recommended to appoint it during the period of breastfeeding.

Dosing and Administration:Tablets should be taken orally at the beginning of a meal, 1 tablet a day in the morning.
In the absence of a therapeutic effect, the dose of the drug can be increased to 2 tablets per day (1 tablet in the morning, 1 tablet in the evening during a meal). The maximum daily dose of 2 mg.
With renal failure with creatinine clearance above 15 ml / min, dose adjustment is not required.

Side effects:From the cardiovascular system: a feeling of palpitations, orthostatic hypotension.
From the side of the central nervous system: asthenia, insomnia, drowsiness, excessive fatigue with exercise, anxiety, depression.
From the digestive system: gastralgia, dryness of the oral mucosa, diarrhea, nausea, constipation.
From the skin: skin rash, itchy skin.
Other: cold extremities, violation of sexual function, edematous syndrome, seizures, "hot flashes" of blood to the skin of the face.

Overdose:Symptoms: a marked decrease in blood pressure and psycho-emotional lability, a disorder of consciousness.
Treatment: gastric lavage and symptomatic therapy. Hemodialysis is ineffective.

Interaction:Contraindicated simultaneous use of the drug ALBAREL® with sultopride, due to the increased risk of ventricular arrhythmia, in particular arrhythmias such as "pirouette."
It is not recommended to use simultaneously with:
- ethanol, as spirits contribute to increased sedative effect,
- with beta-adrenoblockers used in heart failure (bisoprolol, carvedilol, metoprolol): a decrease in the tone of the central part of the sympathetic nervous system and the vasodilating effect of antihypertensive drugs can be dangerous for patients with heart failure who take beta-blockers and vasodilators.
Caution should be exercised when using ALBAREL® simultaneously with:
- baclofen: increases the antihypertensive effect, it may be necessary to correct the dose of the antihypertensive drug;
- beta-blockers: a significant increase in blood pressure in the event of a sudden discontinuation of an antihypertensive drug. Avoid sudden discontinuation of an antihypertensive drug;
- drugs that cause arrhythmia of the "pirouette" type (with the exception of sultopride): an increased risk of ventricular arrhythmia. ECG monitoring and medical supervision are necessary;
- antiarrhythmic drugs IA class (quinidine, hydroquinidine, disopyramide);
- antiarrhythmic drugs of III class (amiodarone, dofetilide, ibutilide), sotalol;
- certain neuroleptics: phenothiazines (chlorpromazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpride, tiapride), butyrophenones (droperidol, haloperidol) other neuroleptics (pimozide);
- other preparations: bepridil, cisapride, difemanyl, erythromycin intravenous, halofantrine, misolastine, moxifloxacin, pentamidine, spiramycin intravenously, wincamine intravenously.
It is necessary to take into account possible interactions with simultaneous reception of ALBAREL® with:
- alpha-adrenoblockers: increased hypotensive effect, increased, risk of orthostatic hypotension,
- amifostine: increased antihypertensive action,
- corticosteroids, tetracosactide (systemic administration) (with the exception of hydrocortisone used as a substitute therapy for chronic cortical adrenal insufficiency): weakening of antihypertensive action (water retention / sodium in the body caused by corticosteroids),
- antipsychotics, imipramine and tricyclic antidepressants: increased antihypertensive action and the risk of orthostatic hypotension (cumulative effect),
- other drugs affecting the central nervous system: morphine derivatives (analgesics, antitussives and substitution therapy), benzodiazepines, anxiolytics in addition to benzodiazepines, hypnotics, neuroleptics, sedative antagonists of histamine H receptors, sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), other antihypertensive drugs, baclofen, thalidomide, pizotifen, indoramin: oppression of the central nervous system.

Special instructions:Taking ALBAREL® with patients who have recently undergone vascular disease (stroke or myocardial infarction) requires regular medical supervision.
During the course of treatment is not recommended to drink alcoholic beverages.
Due to the lack of sufficient clinical data, the drug is not recommended for children under 18 years of age.
Due to good tolerability it is possible to use both in elderly patients and in patients with arterial hypertension and concomitant diabetes mellitus.
The drug should be taken for a long time. The drug should be canceled gradually, despite the fact that the withdrawal of the drug does not lead to a sharp increase in blood pressure.

Effect on the ability to drive transp. cf. and fur:It is advisable to use caution when driving vehicles or mechanisms, as with increasing the dose of the drug or in combination with drugs that reduce the ability to concentrate, therapy with ALBAREL® can be accompanied by a decrease in the ability to concentrate.

Form release / dosage:Tablets 1 mg.

Packaging:For 10 tablets in a blister of PA / aluminum foil / PVC / / aluminum foil.
1, 2 or 3 blisters together with instructions for use in a cardboard bundle.

Storage conditions:Store below 30 ° C. Keep out of the reach of children!

Shelf life:2 years.
Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013071 / 01

Date of registration:23.12.2011

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS Pharmaceutical Plant, ZAO Hungary

Laboratories Servier France

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp09.10.2015

Illustrated instructions

Instructions

Albarel® (Albarel®)