Esmolol

Chemical name

(+)-4-[2-Гидрокси-3-[(1-мети лэтил)амино]пропокси]��ензолпропановой acid methyl ester (as hydrochloride)

Gross

C16-H25-N-O4

Of drugs

The drugs-gipotenzivne, antiaritmicescoe, antianginalnoe. Does beta_1-adrainoretseptora has cardioseleguoe act his own and simpatomimeticescoy мембраностабилизирую щей activity. Has negative chrono, foreign, and dromo- batmotroponoe effect. Suppress automaticity sinusnogo unit lengthens refrakterny period and slowing down on the AV node. Stops central sympathetic impulsaciu and reduces sensitivity of peripheral tissues to kateholaminam. Decreases Patient, airway diseases, consumption heart oxygen (antianginalny effect), heart and the release of AD. Antianginalny and antigipertenzivny effect takes 10 to 20 minutes after the end of Infuzii.pri in / in the introduction associated with protein to 55% in erythrocytes rapidly hydrolyses esterazami to free acid metabolita (activity is 1 / 1500 of an esmolola), and methanol. T_1/2-9 minutes free acid metabolita 3.7 p (with kidney failure increased 10 times). Equilibrium concentration in the blood is within 5 min using load dose and after 30 minutes without it. Report the news in the form of Metabolita.v doses, exceeding the maximum support for the men in eight times (rabbits) and 30 times (rats) to toxic effect on the organism mother, increases frequency rezorbtion and foetal deaths.

Indications

Arterial hypertension, tachycardia (including sinusovu), and fibrillace fibrillation predserdy of which during and after operations; tireotoksicski kriz, myocardial infarction, feohromotsytoma unstable stenocardia.

Restrictions on the use of

Bronchial asthma, emphysema, chronic bronchitis obstruguy, female heart failure, diabetes, the kidney function; Secondary hypertension, during or after operations caused vazokonstrikciei, in the face of hypothermia; pregnancy, breast-feeding, Children age (safety and efficacy of the use of children to be determined), old age.

Pregnancy and lactation

Adequate and well-controlled studies of safety in pregnant women did not. Is not recommended during breast-feeding (no evidence of penetration in breast milk).

Contraindications

Hypersensitivity, sinusova aetiology (less than 45 u. / min), cardiogenny shock AV blockade degree II expressed heart failure, weakness syndrome sinusnogo unit sinoatrialnaya blockade arterial gipotenzia (Sad below 90 mm Hg, Dad below 50 mm Hg), bleeding, gipovolemia.

Side-Effects

From the nervous system and sensory organs : the concern (3%), drowsiness (3%), headache (2%), ajitation (2%), sputannosti consciousness (2%), feeling fatigue (2%); less than 1%, dizziness, fatigue, paresthesia, depression, convulsions, the thinking, taste, and the Reci.so the circulatory system and blood (blood, gemostaz) : gipotenzia (symptomatic 12%, asymptomatic 25%) the peripheral blood (1%); less than 1% aetiology, rapid heartbeat, sinkope, AV blockade asistolia testing, collapse, black lungs, throm, tide of blood to Licu.so part of the intestine : nausea (7%), vomiting (1%); less than 1% dry mouth, diarrhoea phenomenon anorexia, constipation, pain in Zivote.so the respiratory system : less than 1% zalojennosti nose, the pain and hripa in the chest, difficulty in breathing, shortness of breath, Bronhospazm.so the Skin : less than 1% akrozianoz, lips or staining of skin, eritematosnye skin, necrosis of the skin (with ekstravazace). From the reproductive organs : less than 1% oedema, the Mocheispuskania.prochie : infusion reaction (8% of the skin, swelling at the site of), increased body temperature, sweating, chills, pain in mejlopaterny area away wrists and feet syndrome lifting.

Specific guidance

Solution concentration of 250 mg / ml of a dilute it. Troop solution (concentration of 10 mg / ml) prepared by the addition of 5 g (20 mL solution with a concentration of 250 mg / ml) in esmolola feet with the liquid in / with a volume of 500 ml (tentatively aseptic conditions of the strip 20 ml). Cooked solution stored 24 hours at room temperature; Not freeze. Is not recommended to use iglami-babockami.

Patient interaction

Potenziruet effect nedepoliarizuth miorelaksantov, cardiodepressivne the hinidina, procainamide, and dizopiramida verapamila. It increases the risk of bradikardii and hypotension in the face rezerpina. Simpatomimetiki and derivatives xantina weaken (mutually) effects; Gipotenzivee other drugs are added hypotension. Increases the level of digoxin in plasma; Warfarin, morphine and suktinilholin increase plasma concentration. Incompatible in one sprite with a 5% solution of sodium carbonates and other means.

Overdosing

Symptoms : aetiology, jeludockove ekstrasistola, heart failure, Bronhospazm.lechenie : giving patients the Trendelenburga, oxygen, in / in a liquid (in the absence of swelling light); symptomatic therapy : if bradikardii - atropine sulfate, or isoproterenol dobutamin (possibly use epinephrine or a transvenozna elektrocardiostimulyatsii); in heart failure, heart glycosides and / or dioretiki; with hypotension - sossoudossoujiwate funds (epinephrine, norapinefrin, dopamine, dobutamin) under the supervision of AD; jeludockove ekstrasistola kupiruyutza lidohammo or fenitoinom, bronhospazm - �ета_2-адреномиметикам и (isoproterenol), or derivative xantina. Possibly in / in a glukagona to remove bradikardii or hypotension.

Precautions

There is a need for careful and constant medical monitoring (ECG, AD curves, etc.). Experience with the application of the Paediatric practice limited. It should be borne in mind the possibility of masking signs gipoglikemii (tachycardia, hypertension) in patients with diabetes mellitus. Against the backdrop of aggravated allergologicaki history of the most serious manifestation of the reactions гиперчувствительност и and the lack of therapeutic effect of the usual dose epinephrine. The concentration of more than 10 mg / ml may irritate tissue. If Infusion is a local response to a cease and resume in the other.

Dosing and Administration

Dose set by the series of stress and supporting doses. In adults, in / in infuzionno 0.5 mg / kg / min for 1 min (loading dose), then 0.05 mg / kg / min for 4 min (supporting dose). If the response is adequate dose maintained and periodically, if necessary, adjust; in the absence of effect by the end of the 5th mines re-test : in / in infuzionno 0.5 mg / kg / min for 1 min (loading dose), followed by 0.1 mg / kg / min for 4 min (supporting dose), and repeat the sequence of infusions with the increase in support each dose 0.05 mg / kg / min to obtain the desired effect. After reaching effects overload dose is not recommended, and the increase in support reduced to 0,025 mg / kg in 1 min or less. The interval between doses increases may extend to 10 minutes. With hypertension or arrhythmia during or after operations, in / in the 0.25 mg / kg / min (initial dose), and / infuzionno in-0.05 mg / kg / min for 4 min (supporting dose). In the absence of re-effect until 4 times with consistency infusions and increasing every next supportive dose of 0.05 mg / kg Maximum supporting dose for adults 0.2 mg / kg / min. Children with najeludockova dichotomy / infuzionno in 0.05 mg / kg / min, followed by an increase, if necessary, every 10 minutes to 0.3 mg / kg / min.

Literature

DV Preobrazhensky, A. Sidorenko, Romanov NE, Shatunov IM Clinical pharmacology major classes of drugs antigipertenziveh / / Consilium Medicum-2000. T.-2-N 3-S. 99-127.

Directory → Wegetotropona funds → Adrainoliticaskie funds → Beta-adrenoblokatora → Esmolol