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Active ingredients
Rilmenidine
Release form
Pills
Composition
Active ingredient: Rilmenidine (Rilmenidine); Active ingredient concentration (mg): 1
Pharmacological effect
An antihypertensive drug, an oxazoline derivative. Selectively interacts with the imidazoline receptor (I1) of the cortical and peripheral vasomotor centers, in particular the renal centers. The binding of rilmenidine to 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 long-term 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
Absorption; After taking the drug inside rilmenidine is rapidly absorbed. After a single dose of rilmenidine in a dose of 1 mg Cmax in plasma is reached in 1.5-2 hours and is 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%. Vd - 5 l / kg. It is excreted in breast milk .; Css is 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 agonists of 2-adrenoreceptors .; Withdrawal; 65% of the dose taken is excreted unchanged in the urine. Renal clearance is 2/3 of total clearance .; T1 / 2 is 8 hours and does not change with dose change or repeated use of the drug .; Pharmacokinetics in special groups of patients; T1 / 2 in patients aged 70 years and older is 13 ± 1 h; In patients with hepatic insufficiency, T1 / 2 is 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), T1 / 2 is about 35 h.
Indications
Arterial hypertension.
Contraindications
Severe depression. ; Renal failure severe (creatinine clearance <15 ml / min). ;Pregnancy. ; Lactation (breastfeeding). ; Hypersensitivity to the drug.
Use during pregnancy and lactation
Due to the lack of sufficient clinical data, the use of the drug Albarel; contraindicated in pregnancy, although in experimental animal studies, no teratogenic and embryotoxic effects were observed .; 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.
Dosage and administration
The recommended dose of Albarel is 1 mg / day (1 tab.) In the morning. ; If the blood pressure drops not enough after one month of treatment, the dose can be increased to 2 mg / day in 2 doses (1 tablet in the morning and 1 tablet in the evening during the meal). ; Patients with renal insufficiency of mild and moderate severity (creatinine clearance more than 15 ml / min) do not require dose adjustment. ; Treatment is carried out for a long time. ;
Side effects
Side effects are rare, as a rule, mild and transient in nature.; CNS: possible asthenia, insomnia, drowsiness, increased fatigue during exercise; in isolated cases - anxiety, depression, convulsions. From the side of the cardiovascular system: possible heartbeat; in isolated cases - cooling of the limbs, orthostatic hypotension. ; On the part of the digestive system: possible pain in the epigastrium, dry mouth, diarrhea; in rare cases - nausea, constipation. ; Dermatological reactions: rarely - skin rash, itching. ; Other: in isolated cases - peripheral edema, hot flashes, disorder of sexual function. ;
Overdose
Symptoms: pronounced decrease in blood pressure, impaired ability to concentrate. Treatment: conducting sympathomimetic therapy; gastric lavage; with a pronounced decrease in blood pressure - the use of sympathomimetics. Hemodialysis is ineffective.
Interaction with other drugs
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, therefore driving vehicles or working with mechanisms 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, since reduction of the hypotensive effect of rilmenidine is possible .; Caution must be exercised with the simultaneous use of 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 (except for 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, because may increase the hypotensive effect and increased risk of orthostatic hypotension .; It is necessary to 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 that inhibit the action of the central nervous system, such as morphine derivatives (analgesics, antitussive drugs and replacement therapy), benzodiazepines, anxiolytics (in addition to benzodiazepines), sleeping pills, antipsychotics, antihistamines, antidepressants with sedative effects (amitriptyline, doxepin, antihysthetamines, antidepressants with sedative effect (amitriptyline, doxepin, antihysthetamines, antidepressants with sedative effect (amitriptyline, anti-depressants, antihistamines, antidepressants with sedative) , trimipramine), other antihypertensive drugs, baclofen, thalidomide, pizothiphene, indoramine, because possible depression of the central nervous system. Owing to impaired ability to concentrate, driving a car or working with machinery can be dangerous.
special instructions
Do not suddenly stop taking the drug. The dose 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 supervision .; 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 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 the ability to drive motor vehicles and control mechanisms; No specific studies have been carried out on the effect of rilmenidine on the ability to drive vehicles and work with mechanisms. Care must be taken when driving vehicles and working with machinery (risk of developing drowsiness).