ALBAREL
Active material: Rilmenidine
When ATH: C02AC06
CCF: Selective imidazoline receptor agonist. Antihypertensive drugs
ICD-10 codes (testimony): I10
When CSF: 01.09.01.02
Manufacturer: EGG PHARMACEUTICALS Plc (Hungary)
Pharmaceutical form, composition and packaging
Pills round, lenticular, white, with the engraving on both sides of the sign “I”.
| 1 tab. | |
| rilmenidine dihydrogen phosphate | 1.544 mg, |
| that corresponds to the contents of rilmenidine | 1 mg |
Excipients: sodium carboxymethyl, microcrystalline cellulose, lactose, paraffin, Colloidal anhydrous silica, magnesium stearate, talc, white beeswax.
10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
Pharmacological action
Antihypertensive drugs, oksazolina derivative. Selectively interacts with imidazolinovymi receptors (I1) cortical and peripheral vasomotor centers, in particular kidney centers. Linking with rilmenidine imidazolinovymi receptors ingibiruet sympathomimetic activity as cortical, and peripheral centres, that leads to lower HELL.
Albarel® has a dose-dependent hypotensive effect on systolic and diastolic HELL lying and standing. Displaying, that use of the drug Albarel® at therapeutic doses (1 or 2 mg / day) effective in treating mild to moderate hypertension. The product lasts for 24 no, effective exercise. With long-term use, addictive is not.
In therapeutic doses, Albarel® does not affect heart function, no delays sodium and water, does not violate the metabolic balance.
Albarel® impact round without changes of cardiac output. Airway diseases and electrophysiological indexes remain unchanged.
Albarel® does not cause orthostatic hypotension (incl. the elderly); does not violate the compensatory physiological responses of heart rate on exercise; does not affect kidney blood, clubockovu filtering or filtration fraction; has no effect on carbohydrate and lipid metabolism (incl. patients with insulinzawisimam and non-insulin-dependent diabetes mellitus).
Pharmacokinetics
Absorption
After taking the drug inside rilmenidin rapidly and completely absorbed from the digestive tract. After one reception Albarela® dose 1 mg Cmax plasma achieved through 1.5-2 h and is 3.5 ng / ml. The absolute bioavailability of 100%; not exposed to the effect of “first pass” through the liver. Absorption occurs identically among different patients: mezhindividualnye changes are not marked. Simultaneous eating does not affect the bioavailability.
Distribution
Plasma protein binding is less than 10%. Vd – 5 l / kg.
After reapplying the equilibrium is established from the third day of a regular dose. In patients with arterial hypertension, receiving treatment for 2 years, Albarela concentration® plasma remains stable.
Provided with breast milk.
Metabolism
Albarel® biotransformiroetsa slightly. Metabolites are found in trace quantities in urine and are the result of hydrolysis or oxidation of oksazolinovogo rings. These metabolites are not agonists α2-adrenoreceptorov.
Deduction
65% the dose appears in an unmodified form with urine. Renal clearance is 2/3 of the total clearance.
T1/2 is 8 no; does not change when the reappointment.
Pharmacokinetics in special clinical situations
T1/2 among persons aged 70 years of age and older is 13 ± 1 h.
In patients with liver failure T1/2 makes 12 ± 1 h.
Because drug excretion occurs mainly kidneys, in patients with the human kidney excretion of the drug a slowdown, that correlates with the size of the CC. In patients with acute violations of the kidney (CC less than 15 ml / min) T1/2 is about 35 no.
Testimony
- Arterial hypertension.
Dosage regimen
The recommended dose of Albarela® is 1 mg / day (1 tab.) morning.
If HELL is reduced insufficient after one month of treatment, the dose can be increased to 2 mg / day 2 admission (1 tab. morning and 1 tab. in the evening during meals).
In patients with renal insufficiency, mild (QC more 15 ml / min) It does not require correction dose.
Treatment is long-term.
Side effect
CNS: possible fatigue, insomnia, drowsiness, increased fatigue during exercise; in a few cases – anxiety, depression, convulsions.
Cardio-vascular system: Maybe heartbeat; in a few cases – cold extremities, orthostatic hypotension.
From the digestive system: There may be pain in the epigastria, dry mouth, diarrhea; in a few cases – nausea, constipation.
Dermatological reactions: rarely – skin rash, itch.
Other: in a few cases – peripheral edema, tides, disorder of sexual function.
Side effects are rare, usually, mild and transitory nature are.
Contraindications
-depression;
- Severe renal insufficiency (CC<15 ml / min);
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug.
Pregnancy and lactation
The drug should not be appointed during pregnancy and lactation (breast-feeding) due to the lack of sufficient clinical data.
IN experimental studies not observed teratogenic and embryotoxic effects.
Cautions
In appointing the drug patients after recently suffering a stroke, myocardial infarction requires periodic medical monitoring.
Thanks to good endurance Albarel® You can assign according to elderly patients and patients with concomitant diabetes mellitus.
If necessary, the treatment dose should be reduced gradually, Although it is unlikely, that the Elimination of the drug will be accompanied by any side effects.
Not recommended simultaneous appointment Albarela® MAO inhibitors.
During the course of treatment is not recommended to consume alcohol.
Use in Pediatrics
Clinical data on the safety and effectiveness of the drug in children and adolescents under the age of 18 years insufficiently, Therefore, the drug should not be prescribed to patients in this category.
Effects on ability to drive vehicles and management mechanisms
Albarel® in therapeutic doses does not affect psychomotor reactions. If the drug is prescribed in doses, exceeding therapeutic, or in combination with drugs, oppressive CENTRAL NERVOUS SYSTEM activity, You should warn patients – drivers and patients, involved in other potentially hazardous activities, the possible occurrence of sleepiness.
Overdose
Symptoms: severe hypotension, mental disorders.
Treatment: gastric lavage; then – simpatomimeticheskaja therapy. Rilmenidin bad displayed by hemodialysis.
Drug Interactions
Appointment Of Albarela® tricyclic antidepressants reduces its antihypertensive effect.
Effect Of Albarela® increase vazodilatatora, diuretics and antihistamines.
When coupled with the use of drugs, have a depressing effect on the CNS, may increase drowsiness.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 2 year.
