2010/09/17

Albarel

Composition, structure and packing

Tablets are round, biconvex, white, engraved on both sides of the symbol "I".

1 tab. rilmenidine dihydrogen 1.544 mg, which corresponds to the content of rilmenidine 1 mg

Excipients: sodium karboksimetilkrahmal, microcrystalline cellulose, lactose, wax, silicon dioxide, colloidal anhydrous, magnesium stearate, talc, white beeswax.

Clinico-pharmacological group: Selective imidazoline receptor agonists.

Antihypertensives.

Pharmacological action

Antihypertensive drug, a derivative oksazolina. Selectively interacts with imidazoline receptors (I1) of cortical and peripheral vasomotor centers, in particular renal centers. Linking rilmenidine with imidazoline receptors inhibits sympathomimetic activity in both cortical and peripheral centers, which leads to a decrease in blood pressure. Albarel provides a dose-dependent hypotensive effect on systolic and diastolic BP in the supine position and standing.

Shown that the use of the drug Albarel in therapeutic doses (1 or 2 mg / day) effective in treating mild to moderate hypertension. The action of the drug lasts for 24 hours, effective during exercise. Prolonged use of addictive is not developed. In therapeutic doses Albarel not affect the function of the heart, does not cause sodium and water retention, does not violate the metabolic balance. Albarel reduces TPVR without changes in cardiac output. Myocardial contractility and electrophysiological indices remain unchanged. Albarel not cause orthostatic hypotension (including elderly patients) does not violate the compensatory physiological responses of heart rate to physical exercise, no effect on renal blood flow, glomerular filtration and filtration fraction; no effect on carbohydrate and lipid metabolism (in m . hours in patients with insulin and insulin-dependent diabetes mellitus).

Pharmacokinetics

Absorption

After taking the drug inside rilmenidine is rapidly and completely absorbed from the gastrointestinal tract. After receiving a single assay in a dose of 1 mg Cmax in plasma achieved after 1.5-2 h and is 3.5 ng / ml. The absolute bioavailability is 100% not subject to the effect of "first pass" through the liver. Absorption is the same in different patients: interindividual changes are not marked. Simultaneous food intake does not affect the bioavailability.

Distribution

Plasma protein binding is less than 10%. Vd - 5 l / kg. After the repeated application of the equilibrium state is established with the third day of the regular treatment. In patients with hypertension receiving treatment within 2 years, the concentration assay in plasma remains stable. Provided with breast milk.

Metabolism

Albarel biotransformiruetsya slightly.

Metabolites detected in trace amounts in urine and are the result of hydrolysis or oxidation oksazolinovogo ring. These metabolites are not α2-adrenoceptor agonists.

Removing 65% of applied dose excreted unchanged in the urine. Renal clearance is 2 / 3 of the total clearance. T1 / 2 by 8 h does not change when re-appointment.

Pharmacokinetics in special clinical cases of T1 / 2 in persons aged 70 years and older is 13 ± 1 h.

Patients with hepatic insufficiency T1 / 2 was 12 ± 1 h. Since the elimination of the drug occurs mainly by the kidneys in patients with impaired renal function has slowed elimination of the drug, which correlates with the spacecraft. In patients with severe impaired renal function (CC less than 15 ml / min) T1 / 2 is about 35 hours

Statement
hypertension. Dosage regimen recommended dose assay is 1 mg / day (1 tab.) Morning. If blood pressure is reduced enough after one month of treatment, the dose may be increased to 2 mg / day in 2 divided doses (1 tab. In the morning and 1 tab. In the evening during meals). In patients with renal insufficiency mild to moderate severity (spacecraft more than 15 ml / min) did not require correction dose. Treatment is long.

Side effect
From the side of the central nervous system: possible asthenia, insomnia, drowsiness, increased fatigue during physical exertion, and in rare cases - anxiety, depression, convulsions.
Since the cardiovascular system: heart, in isolated cases - cold extremities, orthostatic hypotension.
On the part of the digestive system: epigastric pain, dry mouth, diarrhea, and in rare cases - nausea, constipation.

Dermatological reactions: seldom - skin rash, itching. Other: In isolated cases - peripheral edema, hot flushes, disturbed sexual function.

Side effects are rare, usually mild and are transient.

Contraindications
pronounced depression;
renal failure, severe (CC <15 ml / min);
Pregnancy
lactation (breastfeeding);
Hypersensitivity to the drug.

Pregnancy, Lactation

The drug should not be given during pregnancy and lactation (breastfeeding) because of the lack of sufficient clinical data. In experimental studies have not observed teratogenic and embryotoxic effects.

Application for violations of renal function

In patients with renal insufficiency mild to moderate severity (spacecraft more than 15 ml / min) did not require correction dose.

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

Cautions

Administration of these drugs to patients after a recent stroke, myocardial infarction requires periodic medical monitoring. Thanks to good assay can be assigned to the testimony of elderly patients and patients with concomitant diabetes mellitus.

If you want to stop treatment the dose should be reduced gradually, although it is unlikely that the removal of the drug will be accompanied by any side effects.

Avoid co-administration assay with MAO inhibitors. During the course of treatment is not recommended to drink alcohol. Use in pediatric clinical data on the safety and efficacy of the drug in children under the age of 18 years is not enough, so the drug should not be given this category of patients.

Effects on ability to drive vehicles and management mechanisms Albarel in therapeutic doses has no effect on psychomotor reaction.

If the drug is prescribed in doses exceeding the therapeutic or in combination with drugs, depressing the central nervous system activity, should notify patients - drivers and patients dealing with other potentially dangerous activities, to the possibility of drowsiness.

Overdose

Symptoms: marked hypotension, mental disorders.

Treatment: gastric lavage, then - sympathomimetic therapy. Rilmenidine bad output in hemodialysis.

Drug Interactions

Appointment assay with tricyclic antidepressants reduce its antihypertensive effect.

Effect of assay reinforce vasodilators, diuretics and antihistamines. When combined with the use of drugs, have a depressing effect on the CNS, possibly increased sleepiness.

Terms and Conditions of storage

The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 2 years.