Moxonidine

Chemical name

4-Хлор-5-(2-имидазолин-2-��ламино)-6-метокси-2-мет илпиримидин

Gross

C9-H12-Cl-N5-O

Of drugs

Drugs, the antihypertensive. Yes connects central imidazoline receptors (I_1) responsible for TVR and reflex control of the sympathetic nervous system (located in ventero-lateralnom Division oblong brain). Is agonist pre - and postsinapticakih альфа_2-адренорецепто��ов.Быстро and almost completely absorbed in the digestive tract. Absolute bioavailability-88%. C_max (1,3-2,0 mg / l) is within 1 h. Linking plasma protein-5,8-7,9%, the average distribution-1,4-3 l / kg About 10% becomes 2 metabolita low specific activity. Mean plasma T_1/2 2-3 hours The Cl is 0.77 l / kg fat-67%. The urine unchanged to see 58-60% imposed Dozy.interval between C_max achievement and expressed AD decline of 2-4 hrs Single ingesting lead to the fall of AD alone at an average rate of 10%, with a load - 7.7%. Duration of more than 12 hours (slow return of the central nervous system and for a long time decreases the adrenalin plasma). In kursovom admission to the dose of 0.2 mg 1-2 times / day reduces Sad at 27-29 mm Hg, Dad, at 15-19 mm Hg Decreases suffering cardiac left heart, reduces signs miocardialland fibrosis, mikroarteriopatii, normalizes capillary blood diseases. Impact round, lung vascular resistance, content in the blood renin and angiotenzina II, and via norarenalina alone and load predserdnyi natriyureticski factor (for a load), aldosterone. Decreases tissue resistance to insulino, stimulates the release of growth hormone.

Indications

Arterial hypertension; The metabolic syndrome.

Contraindications

Hypersensitivity, weakness syndrome sinusnogo unit of sinoatrialna and AV conduction II extent aetiology less than 50 strokes per minute, heavy rhythm of the heart, heart failure (IV functional class NYHA), the unstable stenocardia expressed human liver and kidneys, human peripheral blood (obliteriruty proper receptacles lower limbs with the syndrome peremejateisa hromota, Reynaud disease), Parkinson's disease, depressive moods, epilepsy, glaucoma, pregnancy, breast-feeding (at the end of treatment), adolescence (up to 16 years).

Side-Effects

Brown mouth (early treatment), fatigue, weakness, headaches, dizziness, oppression CNS and peripheral edema.

Patient interaction

Do (mutually) effect etc. gipotenziveh preparations deprimiruth funds (alcohol, tranquilizers, barbiturates, neiroleptiki).

Overdosing

Symptoms : hypotension, dry mouth, rapid heartbeat, weakness, Sonlivosti.lechenie : symptomatic. As a specific antidote impose idazoxan (imidazolinov antagonist).

Precautions

Be wary when using renal failure (because of a possible increase plasma concentration) : the creatinine level of less than 60 ml / min dose reduced by half, below 30 ml / min, overturned. During treatment excludes alcohol, it is not recommended (especially at the beginning of treatment) Work with requiring increased attention and responsiveness.

Dosing and Administration

Inside, during or after delivery, the initial dose of 0.2 mg once a day, the average therapeutic dose of 0.4 mg / day, in the reception 1-2 with a maximum daily dose of 0.6 mg.

Literature

1. Bochenkov Brown Agonists imidazoline receptors in the treatment of hypertension (review) / In : : Issues in clinical pharmacology and pharmacotherapy in internal organs disorders. Metro : UK MMA them. I. M. department, 1996 .- C. 36-43.2. Olbinskaya LI, Bochenkov Brown Experience with the agonist imidazoline receptors moksonidina (Zinta), with the long-term treatment of high blood pressure in patients with diabetes mellitus type II / / Mountain. pharmacology and therapy .- 2000 .- T. 9 .- N 3 .- C. 58-60.3. Thostova hearings, Proshin AY, Belousov B. Gipotensus effectiveness tinta (moksonidina) in patients with mild and moderate hypertension / / Mountain. pharmacology and pharmacotherapy-1998 .- T. 7-N 1-C 36-42.

All products of this group

Moxonidine

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