Dopamine - instructions for use, dose, side effects, contraindications

Cardiotonic, hypertensive, vasodilating,diuretic agent. Excites beta-adrenergic receptors (in small and medium doses) and alpha-adrenergic receptors (in high doses). Improvement of systemic hemodynamics leads to a diuretic effect. Has a specific stimulating effect on postsynaptic dopamine receptors in the smooth muscles of blood vessels and kidneys.

In low doses (0.5-3 μg / kg / min) acts mainly on dopamine receptors, causing the expansion of renal, mesenteric, coronary and cerebral vessels. Expansion of the kidneys leads to increased renal blood flow, increased glomerular filtration rate, increased diuresis and elimination of sodium; There is also an expansion of mesenteric vessels (this effect of dopamine on renal and mesenteric vessels differs from that of other catecholamines).

In low and medium doses (2-10 μg / kg / min) stimulates postsynaptic beta₁-adrenoceptors, which causes a positive inotropic effect and an increase in the minute volume of blood (IOC). Systolic blood pressure (BP) and pulse pressure may increase; the diastolic blood pressure does not change or slightly increases.The total peripheral vascular resistance (OPSS) usually does not change. Coronary blood flow and oxygen consumption of the myocardium, as a rule, increase.

In high doses (10 μg / kg / min or more) alpha stimulation predominates₁-adrenoceptors, causing an increase in OPSS, heart rate (heart rate) and narrowing of the kidney vessels (the latter can reduce previously increased renal blood flow and diuresis). Due to the increase in IOC and OPSS, both systolic and diastolic blood pressure increase.

The beginning of the therapeutic effect is within 5 minutes against the background of intravenous administration and lasts for 10 minutes.

Pharmacokinetics:

Introduced only intravenously. About 25% of the dose is captured by neurosecretory vesicles, where hydroxylation occurs and the norepinephrine. It is widely distributed in the body, partially passes through the blood-brain barrier (BBB). Visible volume of distribution (newborns) - 1,8 l / kg. Connections with blood plasma proteins - 50%.

Metabolized in the liver, kidneys and plasma to inactive metabolites. The half-life of the drug (T_1/2) - adults: from the plasma - 2 min, from the body - 9 min; newborns - 6.9 minutes (within 5-11 minutes).

It is excreted by the kidneys: 80% of the dose - in the form of metabolites for 24 hours, in small amounts - in unchanged form.

Indications:

- Shock of different genesis (cardiogenic shock, postoperative, hypovolemic, infectious-toxic, anaphylactic shock, hypovolemic (only after recovery of circulating blood volume);

- acute cardiovascular insufficiency, the syndrome of "low cardiac output" in cardiosurgical patients, arterial hypotension.

Contraindications:

Hypersensitivity to the drug (including other sympathomimetics), idiopathic hypertrophic subaortic stenosis, thyrotoxicosis, pheochromocytoma, zakratougolnaya glaucoma, benign prostatic hyperplasia with clinical manifestations, tachyarrhythmia, ventricular fibrillation.

It should not be prescribed for arrhythmia in combination with monoamine oxidase inhibitors, with cyclopropane and halogen-containing anesthetics.

Carefully:

Hypovolemia, severe stenosis of the aortic aorta, myocardial infarction, cardiac arrhythmias (ventricular arrhythmias, atrial fibrillation), metabolic acidosis, hypercapnia, hypoxia, hypertension in the "small" circle of blood circulation, occlusive vascular diseases (incl.Atherosclerosis, thromboembolism, thromboangiitis obliterans, obliterating endarteritis, diabetic endarteritis, Raynaud's disease, frostbite), diabetes mellitus, bronchial asthma (if there was a history of increased sensitivity to disulfite), pregnancy, lactation, age 18 years.

Pregnancy and lactation:

In pregnant women, the drug should be used only if the intended benefit to the mother exceeds the potential risk to the fetus (in the experiment, adverse effects on the fetus have been identified) and / or the child.

Does it penetrate dopamine in breast milk is not known.

Dosing and Administration:

Enter intravenously, drip.

Dose set individually, depending on the severity of shock, the magnitude of AD and the patient's response to treatment.

To enhance diuresis and obtain an inotropic effect (an increase in the contractile activity of the myocardium) is administered at a rate of 100-250 μg / min (1.5-3.5 μg / kg / min) (low dose region).

With intensive surgical therapy - 300-700 μg / min (4-10 μg / kg / min) (medium dose area); with septic shock - 750-1500 μg / | min (10.5-21 μg / kg / min) (area of maximum doses).

In order to influence the blood pressure it is recommended to increase the dose to 500 mcg / min or more, or at a constant dose of dopamine is additionally prescribed norepinephrine (norepinephrine) at a dose of 5 μg / min with a body weight of about 70 kg.

If there is a disturbance of the heart rhythm, regardless of the doses used, a further increase in the dose is contraindicated.

Children injected at a dose of 4-6 (maximum 10) μg / kg / min. In contrast to adults, in children the dose should be increased gradually, ie, starting with the lowest dose.

The rate of administration should be selected individually to achieve the optimal response of the patient. Most patients manage to maintain a satisfactory state with doses of less than 20 μg / kg / min. Duration of application: the duration of infusions depends on the individual characteristics of the patient. There is a positive experience of infusion lasting up to 28 days. After the stabilization of the clinical situation, the drug is withdrawn gradually.

The rule of solution preparation: 0.9 dilution is used% solution of sodium chloride, 5% glucose solution, Ringer-lactate solution. In order to prepare a solution for IV infusion 400-800 mg of dopamine should be added to 250 ml of the solvent (dopamine concentration will be 1.6-3.2 mg / ml).Preparation of the infusion solution should be performed immediately before use (stability of the solution is maintained for 24 hours, except for the mixture with Ringer-lactate solution - maximum 6 hours). The solution of dopamine should be clear and colorless.

Side effects:

Co hand cardio-cardiovascular system: less often - angina, tachycardia or bradycardia, palpitation, chest pain, increased or decreased blood pressure, conduction disorders, expansion of the complex QRS (QRS - the first phase of the ventricular complex, which reflects the process of depolarization of the ventricles), vasospasm, an increase in the end diastolic pressure in the left ventricle; when used in high doses - ventricular or supraventricular arrhythmias.

From the digestive system: more often - nausea, vomiting, bleeding from the gastrointestinal tract.

From the central nervous system: more often - headache; less often - anxiety, motor anxiety, tremor of fingers.

Allergic reactions: in patients with bronchial asthma - bronchospasm, shock.

Other: less often - dyspnea, azotemia, piloerection; rarely - polyuria (when administered in low doses).

Local reactions: when the product gets under the skin - necrosis of the skin, subcutaneous tissue.

Overdose:

Symptoms: excessive increase in AD spasm of peripheral arteries, tachycardia, ventricular extrasystole, angina, dyspnoea, headache, psychomotor agitation.

Treatment: in connection with the rapid excretion of dopamine from the body, these phenomena stop with a decrease in dose or discontinuation of administration, with ineffectiveness - short-acting alpha-blockers (with excessive increase in blood pressure) and beta-blockers (with heart rhythm disturbances).

Interaction:

Pharmaceutically incompatible with alkaline solutions (inactivate dopamine), oxidants, iron salts, thiamine (contributes to the destruction of the vitamin B₁).

Sympathomimetic effect is enhanced by adrenostimulants, MAO inhibitors (incl. furazolidone, procarbazine, selegiline), guanetidine (prolongation of duration and enhancement of cardiostimulating and pressor effects); diuretic - diuretics; cardiotoxic effect - inhalation drugs for general anesthesia, hydrocarbon derivatives - such as cyclopropane, chloroform, enflurane, halothane, isoflurane, methoxyflurane (increased risk of severe atrial or ventricular arrhythmias), tricyclic antidepressants, including maprotiline (risk of heart rhythm disturbances, severe hypertension or hyperpyrexia), cocaine, other sympathomimetics; weaken - butyrophenones and beta-blockers (propranolol).

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

With simultaneous application with levodopa - an increased likelihood of arrhythmias; with hormones of the thyroid gland - it is possible to increase the effect of both dopamine and thyroid hormones.

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

Phenytoin can promote the development of arterial hypotension and bradycardia (depends on the dose and rate of administration); alkaloids of ergot - vasoconstriction and development of gangrene.

Compatible with cardiac glycosides (possibly increased risk of cardiac arrhythmias, additive inotropic effect, ECG monitoring required).

Reduces the antianginal effect of nitrates, which in turn can reduce the pressor effect of sympathomimetics and increase the risk of arterial hypotension (simultaneous use is allowed depending on the achievement of the necessary therapeutic effect).

Special instructions:

Before administration to patients in shock, hypovolemia should be corrected by the administration of plasma and other blood-substituting fluids.

Infusion should be performed under the control of diuresis, heart rate, minute blood volume, blood pressure, ECG. Reducing diuresis without concomitant decrease in blood pressure indicates the need to reduce the dose of dopamine.

Inhibitors of monoamine oxidase (MAO), increasing the pressor effect of sympathomimetics, may cause the onset of headache, arrhythmia, vomiting and other manifestations of hypertensive crisis, therefore, in patients who received MAO inhibitors during the last 2-3 weeks, initial dopamine doses should not exceed 10% of the usual dose.

Strictly controlled studies of the use of the drug in patients under the age of 18 years have not been carried out (there are some reports of the occurrence of arrhythmias and gangrene associated with the drug extravasation with iv introduction in this group of patients).

To reduce the risk of extravasation, if possible, should be injected into large veins. To prevent tissue necrosis in the case of extravasal ingestion of the drug, infiltrate 10-15 ml of 0.9% solution of sodium chloride with 5-10 mg of phentolamine.

Purpose of the drug on the background of occlusive peripheral vascular diseases and / or DIC (disseminated intravascular disseminated intravascular coagulation) in history can cause a sudden and pronounced vasoconstriction, which leads to skin necrosis and gangrene (should be carefully monitored, and when the detection characteristics of peripheral ischemia administration stop immediately).

Form release / dosage:

Concentrate for the preparation of a solution for infusions, 5 mg / ml, 10 mg / ml, 20 mg / ml and 40 mg / ml.

Packaging:In ampoules of neutral glass to 5 ml.

10 ampoules are placed in a box of cardboard. By 5, 10 ampoules per pack of cardboard with partitions or grilles, or a separator of their cardboard or sack paper.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film without coating.

For 1 or 2 contour squares in a pack of cardboard.Each instruction pack or box is supplied with instructions for use, ampoule knife or ampoule ceramic scapper (if using ampoules with notches, dots or rings, the ampoule opener or scarifier does not insert).

Storage conditions:

In a dry place, protected from light and out of reach of children, at a temperature not exceeding 25 ° C.

Shelf life:

4 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001589/08

Date of registration:14.03.2008 / 26.11.2014

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Representation: & nbspBIOCHEMICAL JSC BIOCHEMICAL JSC Russia

Information update date: & nbsp20.01.2016

Illustrated instructions

Instructions

Dopamine (Dopamin)