Albarel pills 1 mg №30

pharmachologic effect

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

Albarel^® has a dose-dependent hypotensive effect on systolic and diastolic blood pressure in the supine and standing position. It is shown that the appointment of the drug Albarel^® in therapeutic doses (1 or 2 mg / day) is effective in the treatment of mild and moderate arterial hypertension. The effect of the drug lasts for 24 hours, effective during physical exertion. With prolonged use, addiction does not develop.

In therapeutic doses Albarel^® does not cause a delay of electrolytes and water, does not disturb the metabolic equilibrium.

Albarel^® OPSS unchanged cardiac output. Myocardial contractility and electrophysiological indices remain unchanged.

Albarel^® does not cause orthostatic hypotension (including in the elderly); does not violate the compensatory physiological response of the heart rhythm to physical activity; does not affect the renal blood flow,glomerular filtration or filtration fraction; does not affect lipid and carbohydrate metabolism (including in patients with type 1 and type 2 diabetes).

Pharmacokinetics

Suction

After taking the drug inside rilmenidine is rapidly absorbed. After a single dose of rilmenidine in a dose of 1 mg C_max in plasma it is reached in 1.5-2 hours and amounts to 3.5 ng / ml. Absolute bioavailability is 100%; not affected by the “first pass” effect through the liver. Simultaneous use of the drug with food does not affect its bioavailability.

Distribution

Plasma protein binding is less than 10%. V_d - 5 l / kg. It is excreted in breast milk.

C_ss achieved after 3 days of regular use of the drug. In hypertensive patients receiving albarel^® for 2 years, the plasma concentration of the drug remains stable.

Metabolism

Metabolites are found in trace amounts in the urine and are the result of hydrolysis or oxidation of the oxazoline ring. These metabolites are not α agonists.₂-adrenoreceptors.

Removal

65% of the dose taken is excreted unchanged in the urine. Renal clearance is 2/3 of total clearance.

T_1/2 is 8 hours and does not change when changing the dose or repeated use of the drug.

Pharmacokinetics in Special Patient Groups

T_1/2 in patients aged 70 years and older is 13 ± 1 h.

In patients with hepatic insufficiency T_1/2 makes 12 ± 1 h.

Since the excretion of the drug occurs mainly by the kidneys, in patients with renal failure, there is a slowdown in excretion of the drug, which correlates with the CC value.In patients with severe renal failure (CC less than 15 ml / min) T_1/2 is about 35 h.

Indications

- arterial hypertension.

Dosing regimen

The drug is taken orally, at the beginning of the meal.

The recommended dose is 1 tab. / Day in the morning.

In the absence of a therapeutic effect, the dose of the drug can be increased to 2 tab./day (1 pill in the morning and 1 pill in the evening during the meal). The maximum daily dose is 2 mg.

Have patients with renal insufficiency with CC more than 15 ml / min no dose adjustment required.

Side effect

The frequency of adverse reactions is presented in the following order: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10 000, <1/1000), very rarely (<1/10 000), is unknown (frequency cannot be estimated based on available data).

Psychological: often - anxiety, depression, insomnia.

Nervous system: often - drowsiness, headache, dizziness.

Cardiovascular: often - a feeling of palpitations, cold extremities; infrequently - flushing of the skin of the face, orthostatic hypotension.

Gastrointestinal: often - pain in the epigastric region, dry mouth, diarrhea, constipation; infrequently - nausea.

Dermatological: often - skin itch, rash.

Musculoskeletal system: often - muscle spasms.

From the genital and breast organs: often - sexual dysfunction.

Other: often - asthenia, fatigue, swelling.

Contraindications

- depression;

- renal failure severe (CC <15 ml / min);

- simultaneous use with sultoprid;

- Lactase deficiency, galactose intolerance, glucose-galactose malabsorption syndrome (the preparation contains lactose);

- pregnancy;

- lactation period (breastfeeding);

- age up to 18 years (safety and efficacy not established);

- Hypersensitivity to rilmenidine and auxiliary components of the drug.

WITH caution the drug should be used simultaneously with ethanol, beta-blockers used in the treatment of heart failure (bisoprolol, Metoprolol, carvedilol); after a recent stroke or myocardial infarction.

Use during pregnancy and lactation

Due to the lack of sufficient clinical data, the use of the drug Albarel^® contraindicated during pregnancy, although experimental studies no teratogenic and embryotoxic effects were observed in animals.

It is not known whether rilmenidine or its metabolites are excreted in breast milk. Available experimental and toxicological data have shown that rilmenidine and its metabolites are excreted in breast milk from animals. Risk to infants and babies cannot be excluded. Drug albarel^® not recommended for use during breastfeeding.

Studies of the reproductive function of rats did not reveal the effect of rilmenidine on fertility.

Application for violations of kidney function

In patients with renal insufficiency with CC more than 15 ml / min, no dose adjustment is required.

Contraindicated in severe renal failure (CC <15 ml / min).

Use in children

Clinical data on the safety and efficacy of the drug in children under the age of 18 not enough, so the drug should not be prescribed to this category of patients.

Use in elderly patients

Albarel^® can be prescribed for indications in elderly patients.

special instructions

Do not suddenly stop taking the drug. The dose of the drug should be reduced gradually.

As with the use of other antihypertensive drugs, the appointment of the drug Albarel^® patients after a recent stroke or myocardial infarction require regular medical monitoring.

Simultaneous use of the drug Albarel^® with beta-blockers used for the treatment of heart failure (bisoprolol, metoprolol, carvedilol) is not recommended.

Simultaneous use of the drug Albarel^® with MAO inhibitors is not recommended.

Alcohol is not recommended during the course of treatment.

In connection with the possibility of orthostatic hypotension, elderly patients should be warned about the possibility of falls.

The drug contains lactose, so it should not be prescribed to patients with rare hereditary diseases such as galactose intolerance, hereditary lactase deficiency, or glucose-galactose malabsorption syndrome.

Influence on ability to drive motor transport and control mechanisms

No specific studies have been carried out on the effect of rilmenidine on the ability to drive vehicles and work with machinery. Care must be taken when driving vehicles and working with machinery (risk of developing drowsiness).

Overdose

Symptoms: pronounced decrease in blood pressure, impaired ability to concentrate.

Treatment: sympathomimetic therapy; gastric lavage; with a pronounced decrease in blood pressure - the use of sympathomimetics. Hemodialysis is ineffective.

Drug interaction

The simultaneous use of the drug Albarel is contraindicated^® with sultoprid due to the increased risk of ventricular arrhythmias, in particular pirouette-type arrhythmias.

Not recommended for simultaneous use with:

- ethanol, because Alcohol increases the sedative effect of the drug, as a result of which the concentration of attention is disturbed, so driving a car or working with machinery can be dangerous. The use of alcoholic beverages and medication containing ethanol should be avoided;

- with beta-blockers used in heart failure (bisoprolol, Carvedilol, metoprolol), because lowering the tone of the central division of the sympathetic nervous system and the vasodilating effect of antihypertensive drugs can be dangerous for patients with heart failure taking beta-blockers and vasodilators;

- with MAO inhibitors, sincereduction of the hypotensive effect of rilmenidine is possible.

Caution should be exercised while using the drug Albarel^® with:

- Baclofen, it enhances the antihypertensive effect, you may need a dose adjustment of the antihypertensive drug, you need to control blood pressure;

- beta-blockers because of the possibility of a significant increase in blood pressure in the event of a sudden cessation of administration of an antihypertensive drug of central action. A sudden discontinuation of the centrally acting antihypertensive drug should be avoided, clinical monitoring should be undertaken;

- drugs that cause arrhythmia of the "pirouette" type (with the exception of sultopride), since the risk of ventricular arrhythmias increases: antiarrhythmic drugs of class IA (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, dofetilide, ibutilide), sotalol. ECG monitoring and medical observation required;

- certain neuroleptics, such as phenothiazines (chlorpromazine, levomepromazine, thioridazine), benzamides (amisulide, sulpride, tiaprid), butyrophenones (droperidol, haloperidol), others (pimozide);

- other drugs such as bepridil, cisapride, diphemanil, Erythromycin (w / w), halofantrine, mizolastine, moxifloxacin, pentamidine, spiramycin (w / w), vincamine (w / w);

- tricyclic antidepressants, because the hypotensive effect of rilmenidine may be slightly reduced;

- other antihypertensive drugs, becausemay increase the hypotensive effect and increased risk of orthostatic hypotension.

You should consider the possible interaction with the simultaneous use of the drug Albarel^® with:

- alpha-blockers due to increased hypotensive action and increased risk of orthostatic hypotension;

- Amifostine, because may increase antihypertensive action;

- corticosteroids (with the exception of Hydrocortisone, used as replacement therapy for chronic cortical adrenal insufficiency), tetracosactide (for systemic use), because possible weakening of the antihypertensive effect due to the retention of water / sodium in the body caused by corticosteroids;

- neuroleptics, imipramine and tricyclic antidepressants due to increased antihypertensive effects and the risk of orthostatic hypotension (cumulative effect);

- other means suppressing the action of the central nervous system, such as morphine derivatives (analgesics, antitussive drugs)