Dopamine 40 mg / ml concentrate 5 ml of ampoule №5

Dopmin instructions for use

Composition

active substance: 1 ml of concentrate contains dopamine hydrochloride 40 mg;
excipients: sodium metabisulphite (E 223), water for injection.

Dosage form

Concentrate for the preparation of solution for infusion.

Basic physical and chemical properties:

a clear, colorless or yellowish solution.

Pharmacological group

Non-glycosidic cardiotonic agents. Adrenergic and dopaminergic drugs. ATX C01C code A04.

Pharmacological properties

Pharmacodynamics.

In humans, dopamine acts as a catecholamine of natural origin and is the immediate precursor of another catecholamine, norepinephrine. Dopamine releases norepinephrine from sympathetic nerve endings. In addition to effects mediated by norepinephrine, dopamine also has its own pharmacological effect. The most important metabolites of dopamine are MAO (MAO) and catechol-O-methyltransferase (COMT). In small doses (0.5-2 μg / kg / min), dopamine expands renal, mesenteric and coronary vessels by stimulating D1-dopamine receptors (the concentration of intracellular cAMP increases). Dopamine increases renal blood flow, glomerular filtration and renal excretion.

In medium doses (2-10 μg / kg / min), a positive inotropic effect from the heart develops, due to the stimulation of b 1 -adrenoceptors of the myocardium and the ability of dopamine to increase the release of norepinephrine.

In high doses, dopamine also stimulates a 1-adrenoreceptors, which leads to vasoconstriction. Dopamine increases cardiac output, as well as systolic and pulsatile arterial pressure. In small doses, the diastolic pressure increases insignificantly, however, as the dose increases, the peripheral vascular resistance increases, and consequently, the diastolic pressure also increases.

Pharmacokinetics.

The onset of action of dopamine is observed after 1-5 minutes, the drug is quickly distributed in the body tissues (Vd 0.89 l / kg), practically does not penetrate the blood-brain barrier. There is no information on the penetration of dopamine through the placenta. The half-life of dopamine is 1-2 minutes, it usually stops about 10 minutes after the end of the infusion. A significant part of the drug is metabolized initially in MAO (MAO) and catechol-O-methyltransferase (COMT) in the liver and kidneys, and in the blood plasma is inactivated to inactive homovanolic acid metabolites (HVA) and 3,4-dihydroxyphenylacetate (DOPAC). Approximately 25% of the dose of dopamine is transformed into norepinephrine. Most of the dopamine is excreted in the urine in the form of GVK, as well as sulfate and glucuronic compounds. Less than 10% is excreted unchanged. The total clearance of dopamine is approximately 4.4 l / kg / h.

Indications

Heart failure due to acute myocardial infarction (cardiogenic shock).

State of shock after surgery.

Severe infections (infectious toxic shock).

Hypersensitivity reactions (anaphylactic shock).

A marked decrease in blood pressure (severe hypotension) of any genesis.

Contraindications

Hypersensitivity to dopamine or any other component of the drug.

Pheochromocytoma, glaucoma, hyperthyroidism, prostatic hypertrophy with residual urine syndrome, tachyarrhythmia, ventricular fibrillation, hypovolemia (before the start of treatment it is necessary to correct the deficiency of the volume of circulating blood). Avoid anesthesia with cyclopropane and halogenated carbohydrates.

Interaction with other drugs and other interactions

Catechol-O-methyltransferase (COMT) inhibitors, for example, entacapone, can enhance the cardiac effects of catecholamines, including dopamine. The clinical significance of potentiating interaction is not determined. Patients treated with entacapone therapy 1-2 days before dopamine administration should be given low doses of the drug.

Blockers of α- and β-adrenergic receptors. Blockers of α-adrenoreceptors counteract the peripheral vasoconstriction of dopamine, β-adrenergic receptor blockers counteract the effects of dopamine on the heart.

Inhibitors of monoamine oxidase (MAO).

MAO inhibitors potentiate the effects of dopamine and prolong the action of the drug. With great care, dopamine should be used in patients taking or during the last 2 weeks MAO inhibitors. Such patients should be given a significantly lower dose of dopamine (the initial dose is 1/10 of the conventional therapeutic dose).

Tricyclic antidepressants and maprotiline.

Dopamine increases the amount of norepinephrine released in the nerve endings. Tricyclic antidepressants inhibit the reuptake of norepinephrine in the nerve endings and thereby potentiate the effects of dopamine. For patients taking antidepressants, the dose of dopamine should be reduced in connection with the potentiation of effects. When applying the drug simultaneously with tricyclic antidepressants, hypotension and bradycardia may occur.

Halothane and cyclopropane.

When dopamine is used in combination with halothane, cyclopropane and some other anesthetics that increase the sensitivity of the heart muscle, ventricular arrhythmia and hypertension can develop. The simultaneous use of these drugs should be avoided.

Phenytoin.

With intravenous administration of phenytoin during the infusion of dopamine, arterial hypertension and bradycardia can develop. Care must be taken when injecting simultaneously.

Dopamine should not be used in patients who take ergot alkaloids, because of the risk of excessive peripheral vasoconstriction.

Dopamine can enhance the action of diuretics.

Application features

Different types of hypovolaemia should be corrected before starting dopamine therapy. Hypoxia, hypercapnia and acidosis reduce the effectiveness of the drug and increase the likelihood of side effects, so treatment with dopamine should be carried out in parallel with the correction of these conditions.

Particular attention should be given to patients with organic lesions of the heart and blood vessels, for example

• patients with ischemic heart disease and angina pectoris;
• patients with arterial obliterans (eg, atherosclerosis, thromboembolism, Raynaud's disease, frostbite, diabetic microangiopathy, or Vinivarter-Burger disease)
• patients with arrhythmias.

Due to acute myocardial infarction in shock, low doses of dopamine should be used.

If there is a disproportionate increase in diastolic pressure (i.e., a marked decrease in the stroke volume of the heart), the rate of infusion should be reduced and the patients kept under medical supervision, as this may be due to an increase in peripheral vascular resistance.

Patients with peripheral vascular disease in the history should carefully monitor for any changes in color or temperature of the skin of the extremities.

After surgery in the digestive tract or in patients with hemorrhagic diathesis, there is a risk of bleeding due to redistribution of blood circulation.

The administration of dopamine, even in low doses, should be carried out gradually to prevent unwanted arterial hypotension, which usually passes after an increase in the infusion rate.

It is necessary to constantly adjust the dose of administration depending on the changes in the patient's condition, diuresis, MOK and blood pressure. If the patient receiving dopamine increases diastolic blood pressure (i.e., a marked decrease in the pressure amplitude), he should decrease the rate of administration and should be carefully monitored for further signs of vasoconstrictor activity, but only if the desired effect is achieved. In the case of an excessive increase in diastolic blood pressure, a decrease in diuresis or the appearance of arrhythmia, it is necessary to reduce the dose of dopamine. With the stabilization of heart function and blood pressure, there may be a dose reduction in order to ensure optimal urination.

The introduction of dopamine should be carried out under the control of heart rate, blood pressure, ECG, diuresis, it is recommended to monitor the stroke volume of the heart, ventricular filling pressure, central venous pressure, pulmonary artery pressure.

With prolonged parenteral treatment, in all cases, regardless of the patient's condition, minute volume and laboratory tests, electrolyte and acid-base balance, liver and kidney function should be regularly monitored.

To prevent extravasation, it is recommended to inject dopamine into a large vein. When extravasates appear, prevent necrosis by infiltrating affected tissues with phentolamine. Prevention of ischemia can be carried out by administering phentolamine (5-10 mg of phentolamine in 10-15 ml of 0.9% saline) in a syringe with a thin needle in the affected area.With the termination of infusion, it may be necessary to gradually reduce the dose of dopamine due to the threat of arterial hypotension.

Dopamine should not be given in and in the form of a bolus injection.

Due to the introduction of dopamine, especially patients with obliterating peripheral vascular diseases and / or disseminated intravascular coagulation, severe constriction of the blood vessels may occur, leading to necrosis of the skin and gangrene. It is necessary to ensure close monitoring of the condition of these patients; In case of appearance of signs of peripheral ischemia, dopamine should be discontinued immediately. It is also necessary to monitor the condition of patients with impaired renal or hepatic function.

For patients in a coma, it is necessary to provide airway patency.

A glucose solution should be used with caution in patients with diabetes mellitus.

Use during pregnancy and lactation

The drug should not be used during pregnancy, because information about its safety and effectiveness is not enough.

Dopamine is not excreted in breast milk, and it is also unknown how it affects the baby.

The ability to influence the reaction rate when driving vehicles or other mechanisms

Dopmin is a drug for use in stationary conditions with a very short half-life. After discharge from the hospital, there is no possibility of drug influence on reaction rate when driving or working with other mechanisms.

Dosing and Administration

Doses of Dopmin are determined individually, given the severity of the shock, the patient's reactions to dopamine treatment and side effects. To obtain the desired effect of dopamine on hemodynamics, each patient should be carefully selected by titration. Before the start of the course of treatment, it is necessary to restore the volume of circulating blood.Simultaneously with the use of dopamine, it is not necessary to neglect such necessary additional measures as, for example, control of the electrolyte balance.

If the doctor has not prescribed otherwise, the following doses are recommended.

Adult patients who are likely to respond to moderate maintenance of heart function and circulation, can be administered dopamine at an initial dose of 2-5 mg / kg body weight per minute.

In this case, the severely ill patients should have an initial dose of 5 mg / kg, and if necessary, it can be gradually increased (eg every 15-30 minutes) to 5-10 mg / kg body weight per minute to a maximum of 20-50 mg / kg of body weight per minute.

In most patients, it is possible to achieve a satisfactory state with doses of dopamine below 20 mg / kg body weight per minute. Doses of more than 20 mg / kg body weight per minute can be accompanied by a reduction in renal blood flow.

In the case of increased heart failure, dopamine should be administered as an infusion of not more than 50 mg / kg body weight per minute.

If there is a need for a dose of more than 50 mg / kg body weight per minute, diuresis should be monitored.

It should be preferred to increase the rate of administration of the drug at a lower concentration than the administration of a more concentrated solution.

The following tables show the rate of administration of the drug for different dosages and different initial concentrations.

If 1 ampoule of dopamine is diluted to 50 ml of the infusion solution, 1 ml of this solution contains 4000 μg of dopamine hydrochloride.

doses	50 kg	70 kg	90 kg
2 mg / kg / min	1.5 ml / hr	2.1 ml / hour	2.7 ml / hr
5 mg / kg / min	3.75 ml / hour	5.25 ml / hr	6.75 ml / hr
10 mg / kg / min	7.5 ml / hr	10.5 ml / hr	13.5 ml / hr
20 mg / kg / min	15 ml / hour	21 ml / hr	27 ml / hour
50 mg / kg / min	37.5 ml / hr	52.5 ml / hr	67.5 ml / hr

If 1 ampoule of dopamine is diluted to 500 ml of the infusion solution, 1 ml of this solution contains 400 μg of dopamine hydrochloride.

doses	50 kg	70 kg	90 kg
2 mg / kg / min	15 ml / hour (5 drops / min)	21 ml / hr (7 drops / min)	27 ml / hour (9 drops / min)
5 mg / kg / min	37.5 ml / hr (2.5 drops / min)	52.5 ml / hr (17.5 drops / min)	67.5 ml / hr (22.5 drops / min)
10 mg / kg / min	75 ml / hr (25 drops / min)	105 ml / hr (35 drops / min)	135 ml / hr (45 drops / min)
20 mg / kg / min	150 ml / hr (50 drops / min)	210 ml / hr (70 drops / min)	270 ml / hr (90 drops / min)
50 mg / kg / min	375 ml / hr	525 ml / hr	675 ml / hr

The duration of treatment depends on the clinical condition of the patient and is determined by the doctor.

Before starting treatment in patients with hypovolemia, the volume of blood should be restored. Given that dopamine improves atrial-ventricular conduction, cardiac glycosides should be administered to patients with atrial fibrillation and a rapid ventricular response before prescribing dopamine.

When treating patients who are in the unconscious state, due to the risk of aspiration, it is necessary to control the patency of the airways. Patients with increased pre- and postnagruzki to reduce the burden on the heart recommended the additional use of nitroglycerin.

Before administration, the drug must be diluted. The dilution volume is 1 ampoule per 250 ml or 500 ml of any of the solutions recommended for use.

Dopamine should not be added to 5% sodium bicarbonate solution or other alkaline solution, as this leads to inactivation of the drug.

The infusion solution must be prepared immediately before use, using only clear solutions that do not change color after adding dopamine.

Infusion, if possible, should be performed using a central venous catheter.

The prepared solution should be used within 12:00. A mixture of Ringer's solution with lactate should be used within 6:00.

Children

Information on the use of dopamine for children is not available, so do not prescribe this age category of patients.

Overdose

Clinical signs of a dopamine overdose correspond to sympathomimetic hyperactivity, including excessive blood pressure and vasoconstriction. Since the half-life of dopamine is very short, stopping the infusion is sufficient to eliminate overdose symptoms. If necessary, administer phentolamine.

When high doses are used, the a-receptor excitation is increased in combination with the antagonistic effect of β-receptors, vasoconstrictor effects are observed at the end.

Symptoms: excessive increase in blood pressure, tachycardia, arrhythmia, increased diastolic pressure in the left ventricle followed by pulmonary edema, angina attacks (especially in patients with heart failure), indeterminate pain in the chest, palpitations, nausea, vomiting, sensation of cold extremities, cyanosis.

Adverse Reactions

Adverse reactions are dose-dependent. When the drug is used in large doses, the risk of arrhythmia and vasoconstriction increases. With accidental ingestion of the drug from the vessels into the tissue, local necrosis is possible.

Infections and infestations.

Rarely gangrene.

From the side of the psyche

Infrequent anxiety.

Nervousness, anxiety.

From the side of the nervous system.

Often a headache.

From the side of the organs of sight.

Rarely: mydriasis.

From the cardiovascular system.

Often heart palpitations, extrasystole, tachycardia, chest pain, arterial hypotension, vasoconstriction, ectopic heart rhythm.

Infrequent cardiac conduction disorders, bradycardia, QRS complex expansion, hypertension (especially with overdose).

Aberrant ventricular conduction, arrhythmia, atrioventicular block, myocardial ischemia, supraventricular tachycardia, sinus tachycardia or ventricular tachycardia, increased ventricular pressure, tremor of fingers.

From the skin and subcutaneous tissue.

Rarely pilorektsiya.

From the respiratory system.

Often shortness of breath.

From the gastrointestinal tract.

Often, nausea, vomiting.

From the kidneys and urinary system.

Rarely azotemia.

Others.

Bleeding, polyuria, hypersensitivity reactions, reactions at the site of administration.

Patients with a history of arterial arteries (arteriosclerosis, arterial embolism, Raynaud's disease, cold trauma, such as frostbite, diabetic microangiopathy, or Vinivarter-Burger disease) should carefully monitor any skin color changes or skin temperature of the extremities. The presence of changes in skin color or skin temperature may be signs of further deterioration of the skin blood circulation.

In patients with respiratory failure, hypoxemia observed increase in inherent increased alveolar hypoventilation circulation areas (pulmonary shunt built).

Excipients sodium metabisulfite in very rare cases can cause severe hypersensitivity reactions and bronchospasm.

Shelf life

3 years.

Storage conditions

Store at a temperature not higher than 25 ° C in its original packaging. Keep out of the reach of children.

Incompatibility

Due to the inactivation of the drug can not be added to alkaline solutions such as sodium bicarbonate.

Packaging

To 5 ml in an ampoule; 5 ampoules in a cardboard box.

Category of leave

On prescription.