Dopamine (Concentrate) Instructions for Use

ATC Code

C01CA04 (Dopamine)

Active Substance

Dopamine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Dopaminomimetic and adrenomimetic drug

Pharmacotherapeutic Group

Cardiotonic agent of non-glycoside structure

Pharmacological Action

Cardiotonic and hypertensive agent. It is an agonist of dopamine receptors and is their endogenous ligand.

In low doses (0.5-3 mcg/kg/min), it acts primarily on dopamine receptors, causing dilation of renal, mesenteric, coronary, and cerebral vessels. Due to its specific effect on peripheral dopamine receptors, it reduces renal vascular resistance, increases renal blood flow, as well as glomerular filtration, sodium ion excretion, and diuresis; dilation of mesenteric vessels also occurs (this effect of dopamine on renal and mesenteric vessels differs from the action of other catecholamines).

In low and medium doses (2-10 mcg/kg/min), it stimulates postsynaptic β₁-adrenergic receptors, which causes a positive inotropic effect and an increase in minute cardiac output. Systolic BP and pulse pressure may increase; while diastolic BP does not change or slightly increases. Total peripheral vascular resistance usually does not change. Coronary blood flow and myocardial oxygen consumption, as a rule, increase.

In high doses (10 mcg/kg/min or more), stimulation of α₁-adrenergic receptors predominates, causing an increase in total peripheral vascular resistance, heart rate, and constriction of renal vessels (the latter can reduce the previously increased renal blood flow and diuresis). Due to the increase in minute cardiac output and total peripheral vascular resistance, both systolic and diastolic BP increase.

The onset of the therapeutic effect occurs within 5 minutes during IV administration and lasts for 10 minutes.

Pharmacokinetics

After IV administration, it is widely distributed in the body, partially penetrating the blood-brain barrier. About 25% of the dose is taken up by neurosecretory vesicles, where hydroxylation occurs and norepinephrine is formed. The apparent V_d is 0.89 L/kg. Plasma protein binding is 50%.

It is rapidly metabolized in the liver, kidneys, and plasma by MAO and catechol-O-methyltransferase to inactive metabolites – homovanillic acid and 3,4-dihydroxyphenylacetate. T_1/2 from plasma is about 2 minutes, from the body is about 9 minutes. It is excreted by the kidneys: about 80% within 24 hours; mainly in the form of metabolites, a small part of the dose (less than 10%) is excreted unchanged.

Indications

Shock of various origins (cardiogenic, postoperative, infectious-toxic, anaphylactic, hypovolemic /only after restoration of circulating blood volume/). Acute cardiovascular failure of various origins, low cardiac output syndrome in cardiac surgery patients, arterial hypotension.

ICD codes

Dosage Regimen

Concentrate

The dose is set individually depending on the severity of shock, the level of BP, and the patient’s response to dopamine administration.

To increase myocardial contractility, it is administered IV drip at 100-250 mcg/min.

During intensive surgical therapy, it is administered at a dose of 300-700 mcg/min; for septic shock – at a dose of 750-1500 mcg/min.

To affect BP, an increase in dose to 500 mcg/min or more is recommended, or norepinephrine is additionally prescribed at a constant dose of dopamine.

The duration of use is determined individually. There is positive experience with infusion lasting up to 28 days. After stabilization of the clinical situation, dopamine is withdrawn gradually.

If cardiac arrhythmias occur, regardless of the doses used, further dose increase is contraindicated.

Adverse Reactions

From the cardiovascular system tachycardia or bradycardia, chest pain, palpitations, increase or decrease in BP, conduction disorders, widening of the QRS complex, vasospasm, increase in left ventricular end-diastolic pressure; when used in high doses – ventricular or supraventricular arrhythmias.

From the digestive system nausea, vomiting, gastrointestinal bleeding.

From the nervous system headache, anxiety, motor restlessness, tremor of the fingers.

From the metabolism polyuria.

Allergic reactions in patients with bronchial asthma – bronchospasm, shock.

Local reactions if dopamine gets under the skin – necrosis of the skin, subcutaneous tissue, possible development of gangrene.

Other shortness of breath, azotemia, piloerection, when administered in low doses – polyuria.

Contraindications

Hypersensitivity to dopamine; hypertrophic obstructive cardiomyopathy, pheochromocytoma, thyrotoxicosis; tachyarrhythmia, ventricular fibrillation, closed-angle glaucoma; simultaneous use of cyclopropane and hydrocarbon derivatives for inhalation anesthesia, ergot alkaloids; children and adolescents under 18 years of age.

With caution hypovolemia, myocardial infarction, cardiac arrhythmias (ventricular arrhythmias, atrial fibrillation), severe aortic stenosis, metabolic acidosis, hypercapnia, hypoxia, arterial hypotension in the pulmonary circulation, obliterating vascular diseases (including atherosclerosis, thromboembolism, obliterating thromboangiitis, obliterating endarteritis, diabetic endarteritis, Raynaud’s disease, frostbite), diabetes mellitus; pregnancy, breastfeeding period.

Use in Pregnancy and Lactation

During pregnancy, Dopamine is used only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age (efficacy and safety have not been established).

Special Precautions

Dopamine improves atrioventricular conduction, so patients with atrial fibrillation should be given cardiac glycosides before using dopamine; hypoxia, hypercapnia, and acidosis reduce the effectiveness of dopamine, increasing the likelihood of side effects.

Before administering dopamine to patients in a state of shock, hypovolemia should be corrected by administering plasma and other blood-substituting fluids. Infusion should be carried out under the control of diuresis, minute cardiac output, BP, ECG, heart rate. A decrease in diuresis without a concomitant decrease in BP indicates the need to reduce the dose of dopamine. MAO inhibitors, increasing the pressor effect of sympathomimetics, can cause headache, arrhythmia, vomiting, and other manifestations of a hypertensive crisis, so in patients who have received MAO inhibitors within the last 2-3 weeks, the initial doses of dopamine should be no more than 10% of the usual dose.

To reduce the risk of extravasation, Dopamine should be administered into large veins whenever possible.

The use of dopamine against the background of obliterating diseases of peripheral vessels and/or a history of disseminated intravascular coagulation syndrome can cause a sharp and pronounced vasoconstriction, leading to skin necrosis and gangrene (careful monitoring should be carried out, and if signs of peripheral ischemia are detected, dopamine administration should be stopped immediately).

Drug Interactions

With simultaneous use with diuretics, the diuretic effect of dopamine is enhanced.

With simultaneous use of MAO inhibitors (including furazolidone, procarbazine, selegiline), guanethidine, an increase in the intensity and duration of the cardiostimulating and pressor effects of dopamine is possible.

Administration of dopamine against the background of taking tricyclic antidepressants (including maprotiline) leads to an enhancement of its effects (tachycardia, arrhythmia, severe arterial hypertension may develop).

With simultaneous use with guanadrel, the sympathomimetic effect is enhanced.

There is a report of the development of severe arterial hypotension with simultaneous use of dopamine with phenytoin.

With simultaneous use with inhalation agents for general anesthesia, hydrocarbon derivatives (including cyclopropane, chloroform, enflurane, halothane, isoflurane, methoxyflurane), the risk of developing severe cardiac arrhythmias increases.

Other sympathomimetics, as well as cocaine, enhance the cardiotoxic effect.

Butyrophenone derivatives, beta-adrenergic blockers reduce the effect of dopamine.

Dopamine reduces the hypotensive effect of guanadrel, guanethidine, methyldopa, rauwolfia alkaloids (the latter prolong the effect of dopamine).

With simultaneous use with levodopa – increased risk of arrhythmias.

With simultaneous use with thyroid hormones – it is possible to enhance the effect of both dopamine and thyroid hormones.

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

With simultaneous use with cardiac glycosides, an increased risk of cardiac arrhythmias is possible, an additive positive inotropic effect.

It reduces the antianginal effect of nitrates, which in turn can reduce the pressor effect of sympathomimetics and increase the risk of arterial hypotension.

Pharmaceutically incompatible with alkaline solutions (inactivate Dopamine), oxidizing agents, iron salts, thiamine (promotes the destruction of vitamin B₁).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.