Esmolol

When ATH:
C07AB09

Characteristic.

Èsmolola hydrochloride is a white or almost white crystalline powder. It is a relatively hydrophilic compound, highly soluble in water and easily soluble alcohol. Distribution factor (octanol / water) at pH 7,0 is 0,42. Molecular weight - 331,8. It has one asymmetric center and exists as a pair of enantiomeric.

Pharmacological action.
Gipotenzivnoe, antiarrhythmic, antianginalnoe.

Application.

Arterial hypertension, sinus tachycardia, supraventricular tachycardia and tachyarrhythmia (including atrial fibrillation and flutter, incl. during and after surgery), myocardial infarction, unstable angina, thyrotoxic crisis, pheochromocytoma.

Contraindications.

Hypersensitivity, sinusovaya bradycardia (less 45 u. / min), cardiogenic shock, AV block II-III degrees, severe heart failure, sick sinus syndrome, sinoatrialynaya blockade, hypotension (Sad below 90 mm Hg. Art., Dad below 50 mm Hg. Art.), bleeding, gipovolemiя.

Restrictions apply.

Bronchial asthma, эmfizema, chronic obstructive bronchitis, congestive heart failure, diabetes, impairment of renal function; secondary hypertension, vasoconstriction due to hypothermia background, during or after surgery; pregnancy, lactation, childhood (safety and effectiveness in children have not identified), advanced age.

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus. Although adequate and well-controlled studies of safety in pregnant women has not conducted, using esmolol in the last trimester of pregnancy and childbirth was reported on the development of bradycardia in the fetus, continue after the end of infusion drugs. Not recommended for use during breast-feeding (There are no data on the penetration of breast milk).

Side effects.

The frequency of side effects when using esmolol evaluated in 369 patient with supraventricular tachycardia and more than 600 patient during or after surgery, included in clinical trials. Most marked effects were mild and transient. The most significant side effect was hypotension (cm. Precautions). During the post-marketing studies reported fatalities, encountered in clinical conditions, when esmolol was, probably, It used to control ventricular rate (cm. Precautions).

From the nervous system and sensory organs: dizziness (3%), drowsiness (3%), headache (2%), ažitaciâ (2%), confusion (2%), feeling tired (1%); less 1% — slight dizziness, asthenia, paraesthesia, depression, alarm, convulsions, aphronia, taste, vision and speech.

Cardio-vascular system and blood (hematopoiesis, hemostasis): symptomatic hypotension (accompanied by profuse sweating, dizziness) - 12% (Therapy was discontinued in approximately 11% patients, half of which was observed symptomatic hypotension), asymptomatic hypotension — 25%, the peripheral blood circulation (1%); less 1% -pallor, flushing, bradycardia (less 50 beats / min), chest pain, heartbeat, syncope, OF блокада, pulmonary edema. In 2 patients without supraventricular tachycardia, but with severe coronary artery disease (post-myocardial infarction or unstable angina) developed reversible (at the termination of treatment) tyazhelaya bradycardia / sinusovaya pause / asystole.

From the digestive tract: nausea (7%), vomiting (1%); less 1% -dry mouth, dyspepsia, anorexia, constipation, abdominal discomfort.

From the respiratory system: less 1% -nasal congestion, wheezing in the chest, difficulty breathing, breathlessness, bronchospasm.

For the skin: infusion reactions, including inflammation and induration at the injection site (in 8% cases); less 1% is swelling, эritema, discolouration of the skin, burning at the injection site, skin necrosis (when extravasation).

Other: less 1% -fever, Sweating, chills, urinary retention, pain in the interscapular region, coldness of hands and feet, withdrawal.

Cooperation.

Potentiates the effect of non-depolarizing muscle relaxants, cardiodepressive action quinidine, prokaynamyda, disopyramide and verapamil. It increases the risk of bradycardia and hypotension in the background of reserpine. Sympathomimetic and xanthine derivatives weaken (mutually) effects; other antihypertensive drugs — reinforce hypotension. Increases in plasma levels of digoxin; warfarin, morphine and increase the plasma concentration of succinylcholine. Incompatible in the same syringe with other drugs, incl. from 5% solution of sodium bicarbonate.

Overdose.

Symptoms: excessive reduction of blood pressure, bradycardia, PVCs, heart failure, bronchospasm. An overdose of esmolol can cause heart failure.

Treatment: giving patients Trendelenburg, oxygen therapy, in / in a liquid (if no edema); simptomaticheskaya therapy: When bradikardii introduction atropine sulfate, isoproterenol or dobutamine (possible use of epinephrine or transvenous pacing conduct); in heart failure-in/appointment of cardiac glycosides and/or diuretics; hypotension is a vasoconstrictor (epinephrine, norepinephrine, Dopamine, doʙutamin) under the control of blood pressure; PVCs are diluted in / with the introduction of lidocaine or phenytoin, bronchospasm is in/with the introduction of beta₂-adrenomimetikov (isoproterenol) or xanthine derivatives. Perhaps I / O assignment of glucagon to correct bradycardia or hypotension.

Dosing and Administration.

B /. Dose set by introducing a series of loading and maintenance doses.

When arrhythmias — in/in infuzionno 0,5 mg/kg/min for 1 m (nagruzochnaya dose), then - 0,05 mg/kg/min for 4 m (maintenance dose). If the response is adequate, dose maintained and periodically adjusted, if necessary; with no effect by the end of 5 min — spend a re-review: in/in infuzionno 0,5 mg/kg/min for 1 m (nagruzochnaya dose), then - 0,1 mg/kg/min for 4 m (maintenance dose) continue to repeat the sequence of infusions with increasing each maintenance dose on 0,05 mg/kg/min to obtain the desired effect. After reaching the effect of loading dose can not be administered, (a) increased supports to reduce to 0,025 mg / kg 1 min or less. The interval between dose increases may be extended to 10 m.

For hypertension or arrhythmia during or after operations-in/0.25-0.5 mg/kg/min (the initial dose) and in/in infuzionno- 0,05 mg/kg/min for 4 m (maintenance dose). In the absence of the effect of re-, to 4 time, observing the sequence of infusions and increasing each additional dose on 0,05 mg / kg. Maximum dose for adults 0,2 mg / kg / min. Babies with supraventricular arrhythmias in/in infuzionno 0,05 mg/kg/min, followed by an increase as necessary every 10 minutes to 0,3 mg / kg / min.

Precautions.

When using esmolol requires careful and constant medical supervision and ECG monitoring, FROM, Heart rate and other indicators.

Gipotenziya. In clinical studies, 25-50% of patients, treated with esmolol, hypotension was observed, usually defined as Garden below 90 mm Hg. Article. and/or dad below 50 mm Hg. Article. About 12% Patients were mainly symptomatic hypertension (mainly sweating, dizziness). Hypotension can occur at any dose, but is dose-dependent, Therefore, the dose over 200 mcg/kg/min are not recommended. Particularly careful control of blood pressure is required in patients with low baseline blood pressure before treatment. By reducing the dose or termination of infusion hypotension disappears, typically for 30 m.

Heart failure. At the first signs or symptoms of heart failure, esmolol should be abolished and, if necessary, conduct specific therapy. The use of esmolol for control of ventricular rate in patients with supraventricular arrhythmias should be performed with caution, if a patient has impaired hemodynamics or in case of reception other substances, which reduce peripheral resistance, cardiac filling, cardiac contractility, Distribution of the electric pulse in the myocardium, because, despite the rapid onset of action and effect development esmolol, several reported cases of lethal use of esmolol, probably to control ventricular rate.

Tachycardia and / or hypertension during and after surgery. Esmolol is not recommended in patients with secondary hypertension, associated with vasoconstriction due to hypothermia.

Bronchospastic diseases. As a cardioselective blocker esmolol, it can be used in patients with diseases bronhospasticheskimi, but with caution, carefully titrating the dose to achieve the lowest effective. In the case of bronchospasm infusion should be stopped immediately; if necessary, They can be used beta₂-stimulants, but with very great caution, If patients have experienced rapid ventricular rate.

Diabetes mellitus and hypoglycemia. Keep in mind the possibility of masking signs of hypoglycemia (tachycardia, hypertension) patients with diabetes. Against the background of aggravated allergic history may be more severe hypersensitivity reactions and the lack of therapeutic effect of conventional doses of epinephrine. At a concentration of more than 10 mg/ml possibly irritated tissue. If the infusion of a local reaction, administration should be discontinued and resume elsewhere.

Cautions.

Solution at a concentration of 250 mg/ml must be diluted before use. Infusion solution (concentration 10 mg / ml) prepare by adding 5 g (20 ml of a solution with concentration 250 mg / ml) èsmolola in a bottle with a liquid for the on/in the volume 500 ml (pre aseptically removed therefrom 20 ml). Cooked solution is stored 24 hours at room temperature; it should not be frozen. It is not recommended to use needles-butterflies.

Cooperation