Dobutamine-MP - instructions for use, dose, side effects, contraindications

Active substanceDobutamineDobutamine

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Dobutamine-MP

concentrate d / infusion

Medresurs, OOO Russia

Dosage form: & nbspTOoncentrat for solution for infusion.

Composition:

1 ml of concentrate for solution for infusion contains:

Active substance: dobutamine hydrochloride 14.0 mg (in terms of dobutamine - 12.5 mg);

Excipients: sodium metabisulphite no more than 0.2225 mg (in terms of sulfur dioxide) not more than 0.1575 mg; 0.5 M solution of hydrochloric acid to pM 3.5; water for injection up to 1 ml.

Description:

Transparent, colorless or slightly colored liquid.

Pharmacotherapeutic group:cardiotonic agent of non-glycosidic structure

ATX: & nbsp

C.01.C.A.07 Dobutamine

Pharmacodynamics:

Dobutamine is a cardiotonic drug of a non-glycosidic nature, beta₁-adrenomimetic. It is a racemate, a synthetic sympathomimetic amine, akin to the structure of isoproterenol and dopamine. Positive inotropic action is associated with a direct stimulatory effect on beta_1-adrenoreceptors of the myocardium. Increases shock (VO) and minute volume of the heart (MOS). Has a weak stimulating effect on beta₂-adrenoceptors, causes a moderate positive chronotropic effect.When used in high doses, a marked tachycardia can be observed. Reduces the overall peripheral vascular resistance (OPSS) and general pulmonary vascular resistance (OLSS). Systemic arterial pressure (BP) in this case can not significantly change, because the decrease in the OPSS is accompanied by an increase in the shock volume. Perhaps both an increase in blood pressure and its reduction. Patients with arterial hypertension who have normal BP figures during the administration of the drug are more prone to vasopressor reaction. Reduces the filling pressure of the ventricles of the heart, increases coronary blood flow and supply of myocardium with oxygen, improves the atrioventricular conductivity. However, like all inotropic drugs, dobutamine increases myocardial oxygen consumption. Increasing MOS, increases renal blood flow and can increase the excretion of sodium and water ions.

In children, an increase in stroke volume is accompanied by a less pronounced decrease in OPSS and the filling pressure of the ventricles of the heart; there is a more pronounced increase in blood pressure and an increase in heart rate.

The onset of action depends on the prescribed dose: with moderate and high doses of 1-2 minutes from the start of the injection; at low dosages, the time of onset of the effect may extend up to 10 minutes.The duration of action is about 5 minutes after the end of the infusion.

With a diagnostic study of ischemia using the "stress-echocardiography": due to a positive inotropic and in particular a positive chronotropic action under dobutamine loading, the demand for myocardium in oxygen increases. In the case of coronary stenosis, a slight increase in coronary blood flow can lead to a limitation of regional perfusion, which is seen on the echocardiogram, as new deviations are observed on the affected segment of the myocardial wall.

Diagnostic study of viability: a viable but hypo- or akinetic myocardium resting on an echocardiogram (in the unconscious state, in a dream) has a functional reserve for compression, which is stimulated primarily by a positive inotropic action caused by dobutamine loading at lower concentrations (5-20 mkg / kg body weight / min). An echocardiogram shows an improvement in systolic compression, i.e. increase the movement of the wall on the affected segment.

Pharmacokinetics:

The volume of distribution is about 0.2 l / kg body weight.Metabolized in tissues and in the liver due to conjugation with glucuronides with the participation of catechol-O-methyltransferase to inactive metabolites. The main metabolite is 3-O-methyldobutamine. Clearance - 2.4 l / min / m². The half-life is about 2 minutes. Derived in the form of metabolites by the kidneys and through the intestine, with kidneys more than 2/3 of the administered dose.

Indications:

Acute congestive heart failure, acute decompensation of chronic heart failure, chronic heart failure (as a temporary adjuvant on the background of standard therapy for decompensation), cardiogenic shock, open heart surgery, surgical intervention, septic shock, increase or maintenance of minute blood volume during an artificial ventilation with a positive residual pressure at the end of expiration.

To conduct a "stress-echocardiography" test as an alternative to a functional test with physical activity.

Contraindications:

Hypersensitivity to dobutamine, its components and derivatives. Any pathological conditions and diseases when there is a mechanical obstruction to the filling of the heart chambers and / orexpulsion of blood from the ventricles (cardiac tamponade, hypertrophic obstructive cardiomyopathy, subaortic stenosis, severe forms of aortic stenosis). Constrictive pericarditis.

Severe hypovolemia.

Ventricular arrhythmias (including ventricular fibrillation), fosochromocytoma.

Simultaneous use of monoamine oxidase inhibitors (MAO).

Contraindications for the performance of the test "stress-echocardiography"

Acute myocardial infarction (within the previous 10 days), unstable angina, stenosis of the left coronary artery stenosis, hemodynamically significant narrowing of the left ventricular output, hypertrophic obstructive cardiomyopathy, hemodynamically significant valvular heart disease, coronary heart disease, developmental predisposition or clinical history significant or chronic arrhythmias (in particular, ventricular paroxysmal tachycardia), severe obstruction, acute pericarditis, myocarditis, and endocarditis, aortic dissection, arterial hypertension, obstruction to filling the ventricle (compressive pericarditis, pericardial tamponade), hypersensitivity to dobutamine (in the anamnesis),blockade of the bundle of the Hisnia, heart valve defects, aortic stenosis, or other cardiovascular diseases, in which tests with physical exertion are contraindicated, with atropine (taking into account contraindications to the use of atropine).

Carefully:

Metabolic acidosis, hypercapnia, hypoxia, tachyarrhythmia, atrial fibrillation, myocardial infarction (high doses of dobutamine can increase the heart rate and myocardial contractility and, increasing myocardial oxygen demand, increase ischemia), hypovolemia, pulmonary arterial hypertension, occlusive vascular disease (arterial thromboembolism , Buerger's disease), Raynaud's disease, atherosclerosis, cold trauma, incl. frostbite, diabetic endarteritis, age under 18 years, angle-closure glaucoma, pregnancy.

Pregnancy and lactation:

The use of the drug Dobutamine-MP in pregnancy is possible only if the intended benefit for the mother exceeds the estimated risk for the fetus and / or child.

If you need to take the drug during the period of breastfeeding, you should stop breastfeeding while the drug is being treated.

Dosing and Administration:

In the absence of other appointments adults it is recommended to inject 2.5-10 μg per 1 kg of body weight per minute. In some cases, the dosage may be up to 40 μg per 1 kg of body weight per minute.

Children it is recommended to administer in doses from 1 to 15 μg per 1 kg of body weight per minute (the minimum effective dose for children is often higher than for adults, while the maximum dose for children is lower than for adults).

Rules for preparing an infusion solution: concentrate for infusion dilute 5% solution of dextrose (glucose), 0.9% solution of sodium chloride or Ringer's lactate solution.

Dobutamine-MP should be administered only in the form of permanent intravenous infusions. Given the short half-life of the drug, the infusion should be continuous. After the preparation of the solution containing dobutamine, the solution is administered intravenously via a needle or an intravenous catheter using an infusion system for drip infusion. When using highly concentrated solutions, it is necessary to use special dosing devices, infusion pumps or automatic syringe pumps.Tables 1 and 2 show the rates of administration of solutions containing various concentrations of dobutamine.

Table 1. Doses for infusion pumps (1 ampoule, which includes 125 mg dobutamine in 50 ml infusion solution)

Dosage in ml / hour	The rate of administration	Patient's body weight
Dosage in ml / hour	The rate of administration	60 kg	80 kg
Low	2.5 μg / kg / min	3,6	4,8
Average	5.0 μg / kg / min	7,2	9,6
High	10.0 μg / kg / min	14,4	19,2

Table 2. Doses for infusion systems (125 mg dobutamine per 500 ml solvent)

Dosage in ml / hour	The rate of administration	Body mass the patient
		60 kg		80 kg
Low	2.5 μg / kg / min	36		48
Average	5.0 μg / kg / min	72		96
High	10.0 μg / kg / min	144	192

If the concentration is doubled (for example, 250 mg dobutamine per 500 ml solution), the rate of administration should be halved.

Carrying out "stress echocardiography"

With the help of the infusomat, intravenously injected dobutamine in increasing doses from 5, 10, 20, 30 to 40 μg / kg / min with an interval of 3 minutes. If in the third minute of the maximum dose (40 mcg / kg / min) the criteria for stopping the sample can not be reached, then 1-1.5 mg of atropine (0.25-0.3 for 4 minutes) is additionally given, with continued infusion dobutamine. Thus, the duration of the last step (40 μg / kg / min) can be up to 7 minutes with the total duration of the sample19 minutes. Atropine can be introduced and in the penultimate stage of the sample (30 μg / kg / min), if the increase in heart rate is low. To stop the action of dobutamine use infusion beta-blockers.

The criteria for stopping the sample with dobutamine are: achieving submaximal heart rate, increasing arterial pressure more than 240/120 mm Hg. or lowering blood pressure by more than 20 mm Hg. in comparison with the initial, the development of an intense typical attack of angina, the appearance of menacing cardiac arrhythmias, the appearance of conduction disorders, the appearance of new or worsening of existing violations of local contractility in two neighboring segments, the development of a global decline in contractility.

Carrying out a pharmacological test of "stress echocardiography" with dobutamine is allowed only by properly qualified personnel, with proper precautions and availability of the equipment and equipment needed for resuscitation and intensive care.

Side effects:

Adverse events are presented in accordance with the WHO classification: very often more than 1/10, often more than 1/100 and less than 1/10,infrequently more than 1/1000 and less than 1/100, rarely more than 1/10000 and less than 1/1000, very rarely less than 1/10000, frequency unknown - insufficient data to determine the frequency of development.

Many side effects depend on the prescribed dosage, however, when using low and medium doses, they rarely develop.

From the cardiovascular system: often - ventricular tachycardia, ventricular arrhythmia, increase or decrease in blood pressure, palpitation, in patients with acute myocardial infarction, high doses of dobutamine may increase ischemia, increasing the need for myocardium in oxygen; infrequently ventricular fibrillation; rarely - myocardial infarction.

From the nervous system: often - headache; infrequent - irritability, motor anxiety.

From the respiratory system: often shortness of breath; rarely - bronchospasm.

From the digestive system: often - nausea, vomiting.

On the part of the organs of hematopoiesis: rarely - eosinophilia, with prolonged use a transient decrease in the aggregation capacity of platelets.

From the skin: rarely - skin rash; frequency not known - skin necrosis.

From the side of metabolism: rarely - hypokalemia.

Other: rarely - fever, local reactions in the form of phlebitis.

Possible complications and side effects during the stress test with dobutamine:

From the side of the cardiovascular system: very often - violations of the rhythm of the heart of low gradation, supraventricular tachycardia, a decrease in systolic blood pressure more than 20 mm Hg; often - an increase in systolic blood pressure of more than 220 mm Hg; infrequently - ventricular tachycardia, ventricular fibrillation, myocardial infarction.

From the nervous system: very often - a headache.

From the respiratory system: very often - shortness of breath.

Children have a more pronounced increase in heart rate and / or blood pressure than adults and a more pronounced decrease in the pressure in the pulmonary capillaries. There was also an increase in pressure in the pulmonary capillaries, especially in children under the age of 1 year.

Overdose:

Symptoms. Excessive positive inotropic and chronotropic effects of the drug can cause arterial hypertension, myocardial ischemia, supraventricular and ventricular tachyarrhythmias and ventricular fibrillation.As a result of the widening of peripheral vessels, hypotension is possible. In addition, nausea, vomiting, tremor, anxiety, decreased appetite, headache, palpitations, angina pectoris, nonspecific cardialgia.

Treatment. In case of an overdose, it is necessary to temporarily stop the administration of dobutamine and, if necessary, immediately begin measures to maintain vital functions (intubation of the trachea, artificial ventilation of the lungs, cardiopulmonary resuscitation). It is necessary to carefully monitor the water-electrolyte balance and the gas composition of the blood. In severe ventricular arrhythmias, lidocaine and beta-adrenoblockers, with a marked increase in blood pressure, intravenous administration of short-acting alpha-blockers is possible.

Interaction:

The simultaneous use of dobutamine with nitrates or sodium nitroprusside is accompanied by a more pronounced increase in MOS, a decrease in OPSS and ventricular filling pressure than with separate use of drugs.

The combined use of dobutamine and dopamine leads to a more significant increase in blood pressure (a dose-dependent effect of dopamine),increased renal blood flow (stimulation of dopaminergic receptors of renal vessels) and a decrease or absence of changes in ventricular filling pressure.

Alpha-adrenoblockers and drugs with alpha-adrenoblocking activity reduce the hypertensive effect of dobutamine.

Beta-adrenoblockers in small doses contribute to narrowing of the arteries; in high doses show antagonism with dobutamine effects, reduce the positive inotropic effect, there may be an increase in OPSS.

Dobutamine reduces the hypotensive effect of diuretics. The appointment with angiotensin-converting enzyme inhibitors can lead to increased oxygen consumption in the myocardium, the appearance of pain in the heart and arrhythmias.

When combined with halogenated inhalation anesthetics, it should be borne in mind that halothane sensitizes the myocardium to the arrhythmogenic effects of sympathomimetics.

Tricyclic antidepressants, maprotiline, cocaine, doxapram, guanadrel, guanethidine, increase the pressor effect and the risk of cardiotoxic side effects.

Levodopa increases the risk of arrhythmias (requires a reduction in the dose of sympathomimetics).

Cardiac glycosides increase (mutually) inotropic effect and the risk of arrhythmia (caution should be exercised).

Thyroid hormones increase (mutually) the effect and the associated risk of coronary insufficiency (especially in coronary atherosclerosis).

Contraindicated simultaneous administration of MAO inhibitors, since in this case, development of life threatening side effects (hypertensive crisis, collapse, cardiac rhythm disturbance and intracranial hemorrhages) is possible.

The use of dobutamine in diabetic patients can cause a higher need for insulin. Therefore, patients with diabetes should monitor the concentration of glucose in the blood.

Pharmaceutically incompatible with alkaline solutions (5% sodium bicarbonate solution) or any other alkaline solution, as well as with solutions containing sodium bisulfate or ethanol; with aminophylline, acyclovir, brethylium, calcium chloride and gluconate, cefamandol formate, sodium salts of cephalothin, cefazolone, ethacrynic acid, diazepam, digoxin, furosemide, heparin and its salts, hydrocortisone sodium succinate, human insulin, potassium chloride, magnesium sulfate, penicillin, phenytoip, streptokinase, verapamil.

Special instructions:

Continuous infusion of 72 hours or more may result in the development of tolerance, so higher doses may be needed to maintain the initial effect.

Solutions containing dobutamine, can give a pink color, the intensity of which will increase with time (due to its oxidation, however, there is no significant loss of activity and no increase in toxicity).

With the use of the drug Dobutamin-MR, continuous monitoring of the parameters of hemodynamics (heart rate, blood pressure), diuresis, potassium content in the blood serum is mandatory.

With a significant increase in heart rate, it is necessary to reduce the dose of the drug.

If blood pressure remains low or continues to decrease during drug administration, consideration should be given to the possibility of using dopamine or norepinephrine.

In the case of chronic heart failure, it is possible to appoint peripheral vasodilators.

MAO inhibitors, increasing the pressor effect of sympathomimetics, can cause the occurrence of headaches, arrhythmias, vomiting, hypertensive crisis, therefore, when patients take MAO inhibitors in the previous 2-3 weeks, the dose of sympathomimetics should be reduced (up to 10% of the usual dose).

It is not recommended to use the drug as an auxiliary therapy for hypovolemic shock.

It is possible to distort the results when determining the concentration of chloramphenicol by HPLC (high-performance liquid chromatography).

In the case of a previous therapy of angina pectoris, during the "stress-echocardiographic" study, the response to the load may be less pronounced or absent altogether.

Form release / dosage:

Concentrate for solution for infusion, 12.5 mg / ml.

Packaging:

For 10 ml in ampoules of colorless glass. For each ampoule, the label is self-adhesive.

5 ampoules per plastic contour mesh package.

2 contour squares with the instruction are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002158

Date of registration:26.07.2013 / 22.04.2014

Expiration Date:26.07.2018

The owner of the registration certificate:Medresurs, OOOMedresurs, OOO Russia

Manufacturer: & nbsp

GU Russian Cardiology Research and Production Complex MH RF - branch Experimental production of medico-biological preparations Russia

Information update date: & nbsp11.11.2016

Illustrated instructions

Instructions

Dobutamine-MP (Dobutamin-MR)