Dobutamine Hexal, lyophilizate, 250 mg

Indications

Acute heart failure, exacerbation (acute decompensation) of chronic heart failure, chronic heart failure (as a temporary adjuvant during primary therapy), low heart volume (as a side effect of artificial ventilation with positive residual expiratory pressure).

Pharmacological effect

Pharmaceutical group:

cardiotonic drug of non-glycoside structure.

Pharmaceutical action:

Dobutamine Hexal is a cardiotonic drug of non-glycoside nature, a beta1-adrenergic agonist. It is a racemate, a synthetic sympathomimetic amine, structurally related to isoproterenol and dopamine. Has a positive inotropic effect on the myocardium; moderately increases heart rate, increases stroke and minute volumes of the heart, reduces peripheral vascular resistance and vascular resistance of the pulmonary circulation. The system pressure does not change significantly. The drug causes a decrease in the filling pressure of the ventricles of the heart. Increases coronary blood flow and improves oxygen supply to the myocardium. Increased cardiac output may cause increased renal perfusion and increased excretion of sodium and water.

In children, the increase in stroke volume, which is observed under the influence of dobutamine, is accompanied by a less pronounced decrease in peripheral vascular resistance and ventricular filling pressure; at the same time, there is a more pronounced increase in heart rate and increase in blood pressure.

The effect of the drug develops 1-2 minutes after the start of the infusion.

Pharmacokinetics:

Distribution
With continuous infusions, Css in blood plasma is achieved in 10-12 minutes. The amount of Css in the blood increases linearly with increasing infusion rate. Vd – about 0.2 l/kg.

Metabolism
Dobutamine is metabolized primarily in tissues and in the liver. Metabolism occurs primarily through conjugation with glucuronides, as well as to the formation of pharmacologically inactive 3-O-methyl-dobutamine.

Removal
T1/2 is 2-3 minutes. Plasma clearance does not depend on cardiac output and is 2.4 l/min/m2. It is excreted primarily by the kidneys and bile. More than 2/3 of the administered dose is excreted by the kidneys in the form of glucuronides and 3-O-methyl-dobutamine.

Special instructions

With continuous administration of Dobutamine HEXAL (more than 72 hours), the phenomenon of tolerance may develop (increasing the dosage of the drug is necessary).

Active ingredient

Dobutamine

Composition

1 bottle contains dobutamine hydrochloride 250 mg.

Contraindications

Hypersensitivity, idiopathic hypertrophic subaortic stenosis, pericardial tamponade, aortic stenosis, hypovolemia, concomitant use of MAO inhibitors, breastfeeding.

Side Effects

From the nervous system and sensory organs: headache.

From the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia (including ventricular), atrial fibrillation, pain in the heart and chest, palpitations, shortness of breath, increased blood pressure, hypotension, hypokalemia (very rare), transient inhibition of platelet aggregation (with long-term use), petechial bleeding, phlebitis.

From the gastrointestinal tract: nausea.

From the skin: skin necrosis (at the injection site).

Allergic reactions: rarely – skin rash, fever, bronchospasm, eosinophilia, etc.), polyuria (with high doses).

Interaction

When taking beta-blockers concomitantly, due to competitive inhibition of receptors, the catecholaminergic effects of dobutamine may be weakened. The predominant alpha-adrenergic effects contribute to peripheral vasoconstriction with a subsequent increase in blood pressure.

With simultaneous blockade of α-adrenergic receptors, the predominant beta-adrenergic stimulating effects in this case can cause tachycardia and peripheral vasodilation.

The simultaneous use of nitroglycerin or sodium nitroprusside, especially with ischemic heart disease, helps to increase cardiac output and reduce systemic vascular resistance and ventricular filling pressure. Heart rate and blood pressure increase slightly or do not change.

The use of dobutamine in patients with diabetes mellitus may cause a higher need for insulin. Therefore, patients with diabetes should monitor their glucose levels.

Concomitant use of ACE inhibitors and dobutamine in high doses can lead to an increase in cardiac output caused by an increase in myocardial oxygen demand. This can lead to heart pain and arrhythmia.

In combination with dopamine, there is usually no additional increase in cardiac output, which is possible with the use of dobutamine alone. However, such a combination increases systemic blood pressure, increases renal blood flow, sodium excretion and diuresis, and also prevents an increase in ventricular filling pressure.

Concomitant use of MAO inhibitors is contraindicated, because in this case, life-threatening side effects may develop (hypertensive crisis, collapse, heart rhythm disturbances and intracranial bleeding).

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

Ergometrine, ergotamine, methylergometrine, oxytocin increase the vasoconstrictor effect and the risk of ischemia and gangrene, as well as severe arterial hypertension, including intracranial hemorrhage.

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

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

There are no clear indications about the interaction of dobutamine with digitalis, furosemide, spironolactone, lidocaine, isosorbide dinitrate, morphine, atropine, heparin, protamine sulfate, potassium chloride, folic acid and paracetamol.

Pharmaceutical incompatibility

Inhalational anesthetics derived from hydrocarbons (including chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial or ventricular arrhythmias (increase the sensitivity of the myocardium to sympathomimetics).

Do not mix dobutamine solution with alkaline solutions (for example, 5% sodium bicarbonate solution), solutions containing both sodium bisulfate and ethanol, with acyclovir, aminophylline, bretylium, calcium chloride, calcium gluconate, cefamandole formate, cephalothin sodium salt, cefazolin sodium salt, diazepam, digoxin, ethacrynic acid (sodium salt), furosemide, sodium heparin, hydrocortisone sodium succinate, insulin, potassium chloride, magnesium sulfate, penicillin, phenytoin, streptokinase, verapamil.

Overdose

Symptoms: nausea, vomiting, loss of appetite, tremor, anxiety, rapid heartbeat, tachycardia, tachyarrhythmia, ventricular fibrillation, excessive increase in blood pressure, myocardial ischemia, cardialgia, headache, shortness of breath, anginal or nonspecific chest pain.

Treatment: discontinuation of drug administration, tracheal intubation to ensure ventilation and blood oxygenation. In case of excessive increase in blood pressure – intravenous administration of short-acting alpha-blockers; in case of ventricular tachyarrhythmia – propranolol or lidocaine. In case of accidental ingestion – activated charcoal (more effective than gastric lavage and induction of vomiting). Hemo- and peritoneal dialysis, forced diuresis, hemosorption using activated carbon are ineffective.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Manufacturer

Wasserburger Arzneumittelwerk GmbH, Germany