Active substanceDopamineDopamine
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  • Dosage form: & nbspconcentrate for solution for infusion
    Composition:

    In 1 ml (unit of volume)

    In an ampoule with a capacity of 5 ml

    Active substance:

    dopamine hydrochloride

    40 mg

    dopamine hydrochloride

    200 mg

    Excipients:

    sodium disulfite

    10 mg

    sodium disulfite

    50 mg

    water for injections

    up to 1 ml

    water for injections

    up to 5 ml

    Description:Transparent, colorless or slightly yellowish solution.
    Pharmacotherapeutic group:cardiotonic agent of non-glycosidic structure
    ATX: & nbsp

    C.01.C.A.04   Dopamine

    Pharmacodynamics:

    Dopamine is a catecholamine identical to the natural neurotransmitter of the human body, as well as a precursor of norepinephrine. It has a number of pharmacological properties, characteristic for adrenergic substances.

    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 dopamine receptors.

    In low doses (0.5-2 μg / kg / min) acts mainly on dopaminergic receptors, causing the expansion of renal, mesenteric, coronary and cerebral vessels. Expansion of the renal vessels leads to increased renal blood flow, increased glomerular filtration rate, increased diuresis (usually), and elimination of sodium ions.

    There is also an expansion of mesenteric vessels (this effect of dopamine on renal and mesenteric vessels differs from that of other catecholamines).

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

    At high doses (10 μg / kg / min or more) alpha stimulation predominates1-adrenoceptors, causing an increase in OPSS 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 arterial pressure increase. After stopping the introduction, the effect lasts 5-10 minutes.

    Pharmacokinetics:

    The effect of dopamine begins within 1-2 min after intravenous infusion. About 25% of the dose is captured by neurosecretory vesicles, where hydroxylation occurs and norepinephrine is formed. Dopamine quickly and fully distributed in the body (volume of distribution Vd= 0.89 l / kg), with difficulty passes through the blood-brain barrier (BBB). The half-life (T1/2) about 1-2 min (from the plasma 2 min, from the tissues - 9 min).The effect of dopamine is observed within 10 min after the termination of the infusion. Connection with plasma proteins - 50%.

    Metabolised in the liver, kidneys, plasma monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT) to inactive metabolites of homovanilic acid (HVA) and 3,4-dihydroxyphenylacetate (DOPAC).

    The total clearance of dopamine is 4.4 l / kg / h.

    It is excreted by the kidneys with urine in the form of HVA and conjugates (glucuronides, sulfates). In small quantities (less than 10%) is output in unchanged form.

    Indications:

    Shock states of various genesis: cardiogenic shock, postoperative shock, hypovolemic shock (only after recovery of circulating blood volume), infectious-toxic shock, anaphylactic shock.

    Acute cardiovascular failure in various pathological conditions.

    Syndrome of "low cardiac output" in patients after heart operations, acute arterial hypotension.

    Poisoning (to enhance diuresis).

    Contraindications:

    Hypersensitivity to the components of the drug (including other sympathomimetics), idiopathic hypertrophic subaortic stenosis, thyrotoxicosis, pheochromocytoma,closed-angle glaucoma, benign prostatic hyperplasia with clinical manifestations, tachyarrhythmia, ventricular fibrillation of the heart, age under 18 years.

    Carefully:

    Hypovolemia, severe stenosis of the aortic aorta, myocardial infarction, cardiac arrhythmias (ventricular arrhythmias, atrial fibrillation), metabolic acidosis, hypercapnia, hypoxia, arterial hypertension in the "small" circle of blood circulation, occlusive vascular disease in the anamnesis (arterial thromboembolism, atherosclerosis, thromboanginitis obliterans , frostbite, obliterating endarteritis, Raynaud's disease), pregnancy, lactation; bronchial asthma (if a history of increased sensitivity to disulfite), diabetes mellitus.

    Pregnancy and lactation:In pregnant women, use the drug 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).
    Does it penetrate dopamine in breast milk - is unknown.
    Dosing and Administration:

    Intravenously drip, the dose is set individually.

    The usual starting dose is 2-5 μg / kg / min, depending on the result, the dose can be increased to 5-10 μg / kg / min.

    Doses of more than 20 μg / kg / min are rarely used, but in severe cases the doses may be increased to 50 μg / kg / min.

    The rule of solution preparation: to dilute the concentrate to prepare a solution for infusions 40 mg / ml use 0.9% solution of sodium chloride, 5% solution of dextrose. The resulting solution contains about 80 μg of dopamine in 1 ml (corresponding to 96 μg of dopamine hydrochloride). 1 ml of the resulting solution = 20 drops.

    The resulting (reconstituted) solution should be used within 12 hours.
    Side effects:

    From the cardiovascular system: tachycardia or bradycardia, chest pain, increased or decreased blood pressure, conduction disorders, expansion of the complex QRS, vasospasm; when used in high doses - arrhythmia.

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

    From the nervous system: headache, anxiety, tremor.

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

    Other: shortness of breath, azotemia, piloerection; rarely - polyuria.

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

    Overdose:

    Symptoms: excessive increase in blood pressure, spasm of the 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 inefficiency - short-acting alpha-blockers.

    Interaction:

    Pharmaceutically incompatible with alkaline solutions, oxidizing agents, iron salts, thiamine (contributes to the destruction of the vitamin).

    Sympathomimetic effect strengthen adrenostimulators, MAO inhibitors (prolongation of duration and enhancement of cardiostimulating and pressor effects), guanethidine; diuretic - diuretics; cardiotoxic - Enhance drugs for inhalation of general anesthesia, derivatives of hydrocarbons, cyclopropane (increased risk of severe atrial or ventricular arrhythmias), tricyclic antidepressants,maprolithin (risk of heart rhythm disturbances, severe hypertension or hyperpyrexia), cocaine; weaken the butyrophenones and beta-blockers (propranolol).

    Ergot ergot and derivatives (ergometrine, ergotamine, methylergomethrin) and oxytocin increase the vasoconstrictor effect of dopamine and the risk of occurrence of ischemia and gangrene, as well as severe arterial hypertension, up to intracranial hemorrhage.

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

    Dopamine SNandantianginal 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).

    With simultaneous application with levodopa, the probability of arrhythmias increases; with hormones of the thyroid gland - it is possible to strengthen the actions of both dopamine and thyroid hormones.

    Phenytoin can promote the development of arterial hypertension and bradycardia (depends on the dose and rate of administration).

    When combined with cardiac glycosides, an increased risk of cardiac arrhythmias, an additive inotropic effect (electrocardiogram monitoring is required) is possible.

    Special instructions:

    Before administering to patients in shock, hypovolemia should be corrected by the administration of plasma and other blood substitutes. Infusion should be performed under the control of diuresis, minimal blood volume (IOC), blood pressure (BP), ECG. Reducing diuresis without arterial hypotension indicates the need to reduce the dose.

    Patients who received drugs from the MAO inhibitor group during the last 2-3 weeks, the initial dopamine doses should not exceed 10% of the usual dose.

    To reduce the risk of extravasation, if possible, should be injected into large veins. To prevent tissue necrosis in case of extravasal ingestion of the drug, 10-15 ml of a 0.9% solution of isotonic sodium chloride with 5-10 mg of phentolamine should be immediately infiltrated.
    Form release / dosage:Concentrate for the preparation of a solution for infusions, 40 mg / ml.
    Packaging:

    5 ml concentrate for solution for infusion into transparent ampoules of colorless glass type 1, with a break point of blue color.

    5 ampoules are placed in sealed plastic pallets.

    1 pallet together with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of 15 to 25 ° C, in a place protected from light.

    Keep out of the reach of children.

    Shelf life:

    5 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N016107 / 01
    Date of registration:01.12.2009
    The owner of the registration certificate:Orion CorporationOrion Corporation Finland
    Manufacturer: & nbsp
    Representation: & nbspORION CORPORATION ORION PHARMA ORION CORPORATION ORION PHARMA Finland
    Information update date: & nbsp20.01.2016
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