Albarel tablets 1mg, No. 30

Arterial hypertension.

Inside, at the beginning of a meal, 1 table. 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 tab. in the morning, 1 tab. in the evening during meals). The maximum daily dose is 2 mg.

In renal failure with Cl creatinine above 15 ml / min, dose adjustment of the drug is not required.

1 tablet contains 1.544 mg of rilmenidine dihydrogen phosphate, which corresponds to 1 mg of rilmenidine (active substance).

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

Hypersensitivity to rilmenidine and excipients of the drug; depression; severe renal failure (creatinine clearance less than 15 ml / min); pregnancy and breastfeeding; age up to 18 years (efficacy and safety have not been established); lactase deficiency, galactose intolerance, glucose-galactose malabsorption (the drug contains lactose); simultaneous use with sultopride (see section 'Interaction with other medicinal products').

With care: simultaneous use with alcohol, beta-blockers used for the treatment of heart failure (bisoprolol, metoprolol, carvedilol); recent stroke or myocardial infarction.

Trade name: ALBARELЃ

International non-proprietary name: Rilmenidine

Dosage form: tablets

Composition: 1 tablet contains 1.544 mg of rilmenidine dihydrogen phosphate, which corresponds to 1 mg of rilmenidine (active substance).

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

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

PHARMACOTHERAPEUTIC GROUP

Central antihypertensive agent. ATX CODE: —02ј—06

PHARMACOLOGICAL PROPERTIES
PHARMACODYNAMICS

ALBARELЃ, an oxazoline derivative with an antihypertensive effect, has a selective effect on the imidazoline receptors (I1) of the cortical and peripheral vasomotor centers, in particular the renal centers. The 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 (BP).

In patients with arterial hypertension, ALBARELЃ leads to a dose-dependent decrease in systolic and diastolic blood pressure both in the 'lying' and 'standing' positions. It has been shown that the appointment of therapeutic doses of ALBARELЃ (1 mg / day once or 2 mg / day in 2 divided doses) is effective in the treatment of mild to moderate arterial hypertension. It works for 24 hours and is effective during physical exertion. With prolonged use of the drug ALBARELЃ, addiction to the drug does not develop. In therapeutic doses, ALBARELЃ does not lead to fluid and electrolyte retention in the body and does not disturb metabolic balance.

ALBARELЃ retains significant antihypertensive activity 24 hours after administration, while the total peripheral resistance decreases without changes in cardiac output. Myocardial contractility and electrophysiological indices remain unchanged.

ALBARELЃ does not affect orthostatic regulation, in particular in elderly patients, as well as the physiological compensatory response of the heart rate to exercise.

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

ALBARELЃ does not affect the regulation of glucose metabolism, including in patients with type 1 and type 2 diabetes mellitus; does not affect lipid metabolism.

PHARMACOKINETICS
Absorption

The drug is rapidly absorbed. The maximum plasma concentration (3.5 ng / ml) is reached 1.5-2 hours after a single dose of rilmenidine 1 mg orally. Absolute bioavailability is 100% without the effect of 'primary passage' through the liver. Taking the drug simultaneously with food does not affect its bioavailability.

Distribution

The binding of the drug to blood 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.

Withdrawal

It is mainly excreted through the kidneys. 65% of the dose taken is excreted unchanged in the urine. Renal clearance is two-thirds of the total clearance.
The half-life is 8 hours. It does not change with a change in dose or repeated administration of the drug.

Reappointment of the drug

Equilibrium concentration is achieved after 3 days of taking the drug.

Plasma content of ALBARELЃ during long-term administration of the drug

In patients with arterial hypertension receiving ALBARELЃ for 2 years, the concentration of the drug in the plasma remains stable.

In elderly patients

The half-life in patients aged 70 years and older is 13 ± 1 h.

In patients with hepatic impairment

The half-life is 12 ± 1 hours.

In patients with renal impairment

Since the excretion of the drug is carried out mainly by the kidneys, it slows down in such patients, which correlates with creatinine clearance. In patients with severe renal impairment (creatinine clearance less than 15 ml / min), the half-life is approximately 35 hours. Excreted in breast milk.

INDICATIONS FOR USE

Arterial hypertension.

CONTRAINDICATIONS

Hypersensitivity to rilmenidine and excipients of the drug; depression; severe renal failure (creatinine clearance less than 15 ml / min); pregnancy and breastfeeding; age up to 18 years (efficacy and safety have not been established); lactase deficiency, galactose intolerance, glucose-galactose malabsorption (the drug contains lactose); simultaneous use with sultopride (see section 'Interaction with other medicinal products').

With care: simultaneous use with alcohol, beta-blockers used for the treatment of heart failure (bisoprolol, metoprolol, carvedilol); recent stroke or myocardial infarction.

APPLICATION DURING PREGNANCY AND LACTATION

Due to the lack of clinical data, taking the drug ALBARELЃ is contraindicated in pregnant women, although no teratogenic or embryotoxic effects were observed in animal experiments. It is not known whether rilmenidine or its metabolites are excreted in breast milk. The available experimental pharmacodynamic and toxicological data have shown that rilmenidine and its metabolites are excreted in the milk of animals. The risk to newborns and infants cannot be ruled out. The drug ALBARELЃ is not recommended for use during breastfeeding. Effects on Fertility: Reproduction studies in rats did not reveal any effects of rilmenidine on fertility.

DOSAGE AND APPLICATION

The tablets are 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 with meals). The maximum daily dose is 2 mg.
In renal failure with creatinine clearance above 15 ml / min, dose adjustment is not required.

OVERDOSE

Symptoms: The most common symptoms are a marked decrease in blood pressure and impaired concentration. Treatment: carrying out symptomatic therapy. In addition to gastric lavage, with a pronounced decrease in blood pressure, the recommended treatment includes the use of sympathomimetics. Hemodialysis is ineffective.

INTERACTION WITH OTHER DRUGS

The simultaneous use of the drug ALBARELЃ with the following drugs is contraindicated (see section 'Contraindications'):

Х with sultopride, due to an increased risk of ventricular arrhythmias, in particular pirouette-type arrhythmias.

The simultaneous use of the drug ALBARELЃ with the following drugs is not recommended (see section: 'Special instructions'):

Х with ethanol, as alcohol increases the sedative effect of the drug: due to impaired concentration, driving or working with machinery can be dangerous. Drinking alcoholic beverages and taking medications containing alcohol should be avoided.

Х with beta-blockers 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 centrally acting antihypertensive drugs can be dangerous for patients with heart failure taking beta-blockers and vasodilators.

Х with MAO (monoamine oxidase) inhibitors: the antihypertensive effect of rilmetidine can be partially reduced.

With the simultaneous use of the drug ALBARELЃ with the following drugs, care should be taken:

Х with baclofen: enhances the antihypertensive effect, the dose of the antihypertensive drug may need to be adjusted and blood pressure control is necessary;

Х with beta-blockers: a significant increase in blood pressure in the event of a sudden cessation of taking a centrally acting antihypertensive drug. Avoid sudden discontinuation of a centrally acting antihypertensive drug; clinical monitoring is necessary;

Х with drugs that cause arrhythmias of the 'pirouette' type (with the exception of sultopride): increased risk of ventricular arrhythmias. ECG monitoring and medical supervision are required;

- with class IA antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide);

- with class III antiarrhythmic drugs (amiodarone, dofetilide, ibutilide), sotalol.

Х with certain antipsychotics: phenothiazines (chlorpromazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpride, tiapride), butyrophenones (droperidol, haloperidol) and other neuroleptics (pimozide).

Х with other drugs: bepridil, cisapride, diphemanil, intravenous erythromycin, halofantrine, mizolastine, moxifloxacin, pentamidine, intravenous spiramycin, intravenous vincamine.

Х with tricyclic antidepressants, the antihypertensive effect of rilmenidine may be slightly reduced.

Х with other antihypertensive drugs: increased antihypertensive effect. The risk of orthostatic hypotension is increased.

With the simultaneous administration of the drug ALBARELЃ with the following drugs, possible interactions should be considered:

Х with alpha-adrenobase locators: increased antihypertensive action, the risk of orthostatic hypotension is increased.

Х with amifostine: increased antihypertensive action.

Х with corticosteroids, tetracosactide (systemic use) (with the exception of hydrocortisone, used as replacement therapy for chronic cortical adrenal insufficiency): weakening of the antihypertensive effect (water / sodium retention in the body caused by corticosteroids).

Х with antipsychotics, imipramine and tricyclic antidepressants: increased antihypertensive action and the risk of orthostatic hypotension (cumulative effect).

Х with other drugs that depress the effect of the central nervous system (central nervous system): morphine derivatives (analgesics, antitussives and substitution therapy), benzodiazepines, anxiolytics other than benzodiazepines, hypnotics, antipsychotics, sedative antagonists of histamine H1-receptors, sedative antidepressants , mianserin, mirtazapine, trimipramine), other antihypertensive drugs, baclofen, thalidomide, pizotifen, indoramine: CNS depression. Driving or operating machinery can be hazardous due to impaired concentration.

SPECIAL INSTRUCTIONS
Do not stop taking the drug suddenly. The dose of the drug should be reduced gradually.
As with the use of other antihypertensive drugs, taking ALBARELЃ by patients who have recently had vascular diseases (stroke or myocardial infarction) requires regular medical supervision.
During the course of treatment, it is not recommended to consume alcoholic beverages (see the section 'Interaction with other medicinal products'). The simultaneous use of the drug ALBARELЃ with beta-blockers used for the treatment of heart failure (bisoprolol, metoprolol, carvedilol) is not recommended (see the section 'Interaction with other medicinal products'). The simultaneous use of the drug ALBARELЃ with MAO inhibitors is not recommended (see the section 'Interaction with other medicinal products'). Due to the possibility of orthostatic hypotension, elderly patients should be warned about the possibility of falls.

The drug ALBARELЃ contains lactose.
The drug should not be administered to patients with rare hereditary diseases - galactose intolerance, hereditary lactase deficiency or glucose-galactose nonabsorption syndrome.

Effects on the ability to drive vehicles and use mechanisms
There have been no specific studies of the effects of rilmenidine on the ability to drive vehicles and work with mechanisms. Care must be taken when driving and operating machinery (risk of drowsiness).

RELEASE FORM

Tablets 1 mg.
10 tablets in a PA blister / aluminum foil / PVC // aluminum foil 1, 2 or 3 blisters together with instructions for use in a cardboard box.

STORAGE CONDITIONS

Store at temperatures below 30 ? C. Keep out of the reach of children!

SHELF LIFE

2 years.
Do not use the drug after the expiration date printed on the package.

TERMS OF RELEASE FROM PHARMACIES

On prescription