Dopmin

General characteristics. Structure:

Active ingredient: 40 mg of a dopamine of a hydrochloride.

Excipients: sodium metabisulphite (Е 223), water for injections.

Cardiotonic and hypertensive means, is appointed at treatment of various forms of disturbances of a hemodynamics. Along with an inotropic effect the dopamine has the expanding effect on vessels of heart, brain, kidneys, intestines and increases blood circulation in these bodies. Thanks to bystry removal the dopamine does not collect in an organism even at long infusions.

Pharmacological properties:

Pharmacodynamics. The dopamine is the sympathomimetic having direct effect on β-adrenoceptors and mediated - on α-adrenoceptors.......... In an organism the dopamine is a catecholamine of a natural origin and serves as the direct predecessor of other catecholamine - noradrenaline. The dopamine releases noradrenaline from sympathetic nerve terminations. In addition to the effects mediated through action of noradrenaline, the dopamine also possesses own pharmacological action. The most important metabolites of a dopamine are monoamine oxidase (MAO) and catechol-au-methyltransferase (KOMT). Orally the dopamine does not render cardiovascular effect. In small doses (0,5–2 mkg/kg/min.) the dopamine makes the expanding impact on renal, mezenterialny and coronary vessels thanks to stimulation of D1 dopamine of receptors (concentration of intracellular tsAMF increases). The dopamine increases a renal blood stream, glomerular filtering and renal excretion.

In average doses (2–10 mkg/kg/min.) the dopamine renders the positive inotropic effect on heart caused by stimulation β1-адренергических receptors and ability of a dopamine to increase release of noradrenaline.

And more dopamine also stimulates in high doses of 10 mkg/kg/min. α1-адренергические receptors that conducts to vasoconstriction. The dopamine increases cordial emission, and also the general systolic pressure of blood and pulse pressure. In small doses diastolic pressure slightly increases. However with increase in a dose peripheric resistance increases, therefore, also diastolic pressure increases.

Pharmacokinetics. The beginning of action of a dopamine is shown in 1–5 minutes after the beginning of infusion, drug quickly and widely spreads in body tissues (Vd of 0,89 l/kg), practically does not get through a blood-brain barrier. There is no information on penetration of a dopamine through a placenta. The elimination half-life of a dopamine makes 1–2 minutes. It is usually terminated approximately in 10 minutes after the end of infusion. The most part of drug is metabolized originally in monoamine oxidase (MAO) and catechol-au-methyltransferase (KOMT) in a liver, kidneys and plasma is inactivated to inactive metabolites of gomovanilny acid (GVK) and a 3,4-digidroksifenilatsetat (DOFATs). About 25% of a dose of a dopamine turn into noradrenaline. The most part of a dopamine is allocated with urine in the form of GVK, and also sulphatic and glyukuronidny connections. Less than 10% of a dose are allocated in not changed look. The general clearance of a dopamine makes about 4,4 l/kg/h.

Indications to use:

Acute hypotension or the shock caused by a myocardial infarction, an endotoxic septicaemia, injuries or a renal failure. Dekompensirovanny chronic heart failure. As auxiliary therapy - at hypotension which will not respond to treatment, despite of correction of volume of the circulating blood after open heart operations.

Route of administration and doses:

Drug is used strictly on doctor's orders in the conditions of a hospital. After cultivation the dopamine is entered intravenously only in the form of infusions whenever possible into large veins. The usual initial dose of infusion of a dopamine for adults makes 2–5 mkg/kg/min. and can be increased to 5–10 mkg/kg/min. according to reaction. The dopamine in a dose over 20 mkg/kg/min. usually is not applied though doses over 50 mkg/kg/min. can be appointed in hard cases.

When one ampoule (5 ml) of Dopmin, a concentrate for preparation of infusion solution of 40 mg/ml, is added to 100 ml of 0,9% of solution of sodium chloride or to 5% to glucose solution, one drop of the prepared solution contains about 80 mkg of a dopamine (about 96 mkg of a dopamine of a hydrochloride).

Settlement basis: 1 ml to =20 drops.

The prepared solution has to be used within 12 hours.

Features of use:

Drug is not recommended for inclusion in pregnancy time as information on its safety and efficiency is not enough.

Administration of drug during feeding by a breast is safe as drug is inactivated at hit in the child's organism during feeding and has very short half-life.

Children. Information on use for children is absent therefore drug do not apply this category of patients.

Various types of hypovolemia have to be skorrigirovana before performing therapy a dopamine. During infusion it is necessary to carry out continuous monitoring of blood pressure, an ECG, speed of release of urine. The hypoxia, a hypercapnia and acidosis reduce efficiency of a dopamine and increase probability of side effects therefore treatment by a dopamine has to be carried out together with correction of these states. Infusion of a dopamine can be reduced or stopped at excessive increase in blood pressure, decrease in a diuresis, development of arrhythmia. At accidental hit of drug from vessels in fabric the local necrosis is possible. At the same time immediately it is necessary to make local infiltration by phentolamine in saline solution (5–10 ml of phentolamine in 10–15 ml of 0,9% chloride sodium solution).

At the termination of infusion there can be a need for a gradual dose decline of a dopamine because of risk of developing of arterial hypotension.
Sodium excipient seldom or never can lead metabisulphite to heavy reactions of hypersensitivity and a bronchospasm.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Dopmin – drug for use in stationary conditions with very short half-life. After an extract from a hospital an opportunity to influence speed of response at control of motor transport and work with other mechanisms will be absent.

Side effects:

Side reactions are dozozavisimy. At use of drug in high doses the risk of developing of arrhythmia and vasoconstriction increases. At accidental hit of drug from vessels in fabric the local necrosis is possible.

Widespread side reactions:
Nervous system: headache.
Cardiovascular system: the accelerated heartbeat, an extrasystole, tachycardia, pain behind a breast, arterial hypotension, vasoconstriction, an ectopic cordial rhythm.
Respiratory organs: диспноэ.
System of digestion: nausea, vomiting.

Not widespread side reactions:
Disturbances of mentality: alarm.
Cardiovascular system: disturbance of cordial conductivity, bradycardia, expansion of the QRS complex, arterial hypertension (especially at overdose).

Exceptional cases:
Infections: gangrene.
Organ of sight: mydriasis.
Cardiovascular system: ventricular premature ventricular contraction.
Urinary system: azotemia.
Skin: piloerektion.

Interaction with other medicines:

Inhibitors catechin-au-methyltransferase (KOMT), for example, энтакапон, can exponentiate chronotropic and aritmogenny effects of catecholamines, including a dopamine. Clinical value of exponential interaction is not defined. Patients who received therapy entakapony in 1-2 days prior to introduction of a dopamine have to receive lower doses.

Blockers α-and β-adrenoceptors.......... Blockers of α-adrenoceptors counteract peripheral vasoconstriction of a dopamine, blockers of β-adrenoceptors ((((((((((пропанолол and метопролол) counteract action of a dopamine on heart.

Monoamine oxidase inhibitors (MAO). MAO - important enzymes of a catabolism of catecholamines in an organism. MAO inhibitors exponentiate effects of a dopamine and prolong effect of drug. Carefully it is necessary to apply a dopamine to treatment of patients who accept MAO inhibitors (an initial dose 1/10 from the standard therapeutic dose).

Tricyclic antidepressants and Maprotilinum. The dopamine increases quantity of the released noradrenaline in nerve terminations. Tricyclic antidepressants inhibit the return capture of noradrenaline in nerve terminations that exponentiates effects of a dopamine. For the patients accepting antidepressants, the dose of a dopamine can be reduced in connection with potentiation of effects.

Halothane and cyclopropane. At use of a dopamine ventricular arrhythmia and hypertensia can develop in combinations with the halothane, cyclopropane and some other anesthetics increasing sensitivity of a cardiac muscle. It is necessary to avoid combined use of these drugs.

Phenytoinum. At intravenous administration of Phenytoinum during infusion of a dopamine arterial hypertension and bradycardia can develop. Be careful at simultaneous introduction.

The dopamine should not be applied to the patients applying ergot alkaloids in connection with risk of emergence of excessive narrowing of peripheral vessels.
The dopamine can strengthen effect of diuretic drugs.

Contraindications:

Pheochromocytoma, nekorrigirovanny tachyarrhythmia, tendency to fibrillation of ventricles, thyrotoxicosis, hypersensitivity to acting or to any of excipients. It is necessary to avoid anesthesia cyclopropane or halogenated hydrocarbons.

Overdose:

Clinical signs of overdose of a dopamine correspond to a sympathomimetic hyperactivity. But as the dopamine elimination half-life in an organism very short, is enough termination of infusion for elimination of symptoms of overdose. In need of treatment of excessive vasoconstriction and arterial hypertension enter phentolamine.

Storage conditions:

To store at the room temperature (15–25 °C). To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 5 ml in an ampoule; on 5 ampoules in cardboard packaging.