Rilmenidine

Chemical name

2-[(Дициклопропилметил )амино]-2-оксазолин

Gross

C10-H16-N2-O

Characteristics

It is soluble in water and alcohol metilovom, poorly soluble in ethanol.

Of drugs

Drugs, the antihypertensive. Is specific agonist central and peripheral imidazoline (I_1) receptors. Initiation central imidazoline receptors in the heart sossoudodwigatelnom oblong brain by lower impoulsation sympathetic to the pressure and the heart, which leads to a decline in AD and round, reducing variation. Partly antihypertensive activity of stimulation альфа_2-адренергическ��х receptors on the cell membranes of the kernel solitarnogo tract. Impact renin activity and the content of norarenalina, angiotenzina II and aldosterone. Enlisting I_1-imidazolinovykh peripheral receptors in the kidneys, napochechnikah, pancreas, adipose tissue and karotidnykh clubockah accompanied by a number of additional effects. Initiation I_1-imidazolinovykh receptors in the kidneys is reduced reabsorbtion sodium and water, napochechnikah-braking release of catecholamines hromaffinnah cells in the pancreas-an secreta insulin in response to glucose load in adipozitah increased lipoliza in karotidnykh clubockah Increased sensitivity to decrease AD and гипоксии/гиперкапнии. По The double blind �лацебо-контролируемы х research and comparative studies with the standard drugs has antigipertenzivna active in therapeutic doses (1 mg / day one, or 2 mg / day in 2 admission), with mild and moderate degree of hypertension. Dozozawisimo lowers Sad and Dad (at rest and with physical activity), the situation in the patient lying, and standing. Provides prolonged pharmacological effects gipotenzivny significant effect maintained for a period of 24 hours after admission to the dose of 1 mg. With long-term use can reduce the gipotenzivnogo effects and sudden withdrawal is not accompanied by the development of ricochetna hypertension. It does not impair physiological responses manifested climate variation in response to the physical strain. In therapeutic doses virtually no effect on airway diseases, the release of heart, heart электрофизиологическ ие indexes kidney bloodstream, the characteristics clubockova filtering and the filtering �ракции.Предполагаетс я neiroproteguogo existence of the cerebral Ischemia unrelated to the change think Krovotoka.bystro drawn from the blood, C_max plasma (3.5 ng / l) is a 1.5-2 h after a single reception. Bioavailability of 100% (no change in food intake), the effect of the first pass through the liver is missing. Linking blood plasma is less than 10%, the volume of 5 l / kg Metabolized to a small extent with the formation of the products of hydrolysis or oxidation oksazolinovogo ring (found in the urine in trace quantities, and are not agonists альфа_2-адренорецепто��ов). Report mostly kidneys (65% excreted in the urine in an unmodified form). Kidney klirens 2 / 3 common ground. T_1/2-8 hrs (not dependent on the dose and frequency reception). Equilibrium concentration is achieved within 3 days regular reception and later a permanent Urovne.pri insufficient liver function and in patients older T_1/2 grew to 12-13 C.na backdrop of the kidney is slowing down and correlates with the value of Cl creatinine. In severe renal insufficiency (Cl creatinine less than 15 ml / min) T_1/2 is about 35 hours (to be a correction mode).

Indications

Arterial hypertension.

Pregnancy and lactation

Contraindicated during pregnancy, although tests on animals showed teratogenic or embriotoksicskih effects. At the time of treatment should stop breast-feeding (enters breast milk).

Contraindications

Hypersensitivity expressed depression, severe renal insufficiency (Cl creatinine less than 15 ml / min), pregnancy and breast-feeding, child age (not enough clinical experience).

Side-Effects

From the nervous system and sensory organs : drowsiness or insomnia, fatigue, dizziness, weakness and physical loads; Fear, depression, Sudorogi.so the circulatory system and blood : heart, cooling limbs, ortostatical gipotenzia, Priliv.so part of the intestine : dry mouth, pain in epigastria, diarrhoea, nausea, Zapor.so the urogenital system : peripheral oedema, sexual disorders Funktion.so the skin : skin rashes, itching of the skin.

Patient interaction

Effect increase vazodilatatora, mochegonne and antipruritic drugs weakening - Tricyclic antidepressants. Not recommended simultaneous application with MAO inhibitors.

Overdosing

Symptoms : expressed arterial gipotenzia, mental illness, the Soznaniya.lechenie : washing stomach, a simpatomimeticakih funds. Haemodialysis weak.

Precautions

There is a need for extreme caution in patients with sinusova bradikardiei (HR 50 u. / min), the weakness syndrome sinusnogo hub, AV blockade II and the heavy Hepatic. In therapeutic doses does not affect the mind and the ability to concentrate. When the recommended dose or a medical appointment, oppressive central nervous system, may cause feelings of sleepiness (it should be taken into account when appointing people whose professional activity requires quick mental and physical reactions). The treatment should be deleted alcohol.

Dosing and Administration

Inside. The recommended dose of 1 mg / day morning. If, after receiving over one month normalization AD has been reached, dose can be increased to 2 mg / day (1 mg morning and evening with a meal). The treatment is carried out continuously and the long-term. Denial reduce dose gradually.

Literature

1. Gavras A., A. Manolis, Gavras H. paradigm sympathetic suppression system in chronic heart недостаточности//Межд унар. med. Zh-2000-N 3 .- C. 213-216.2. DV Preobrazhensky, A. Sidorenko, Romanov NE Clinical pharmacology major classes of drugs antigipertenziveh / / Consilium Medicum .- 2000 .- T. 2 .- N 3 .- C. 99-127.3. Maiese K., L. Pek, S. Berger, S. Reis Reduction in focal cerebral ischemia by agents acting at imidazole receptors / / J. of Cerebral Blood Flow & Metabolism .- 1992 .- V. 12-N-1 P. 53-63.4. Mizobe T., M. Maze Alfa_2-agonists and Anesthesia / / New Drugs in Anesthesia.-1995 .- V. 33-N-1 P. 81-103.5. Zwieten P. Modulatin of sympathetic outflow by centrally acting antihypertensive drugs / / Cardiovascular Drugs Ther 1996 .- .- V. 10-N-1 P. 283-292.

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