DOBUTAMIN GEXAL

Active material: Doʙutamin
When ATH: C01CA07
CCF: Beta₁-adrenomimetik. Cardio-tonic
ICD-10 codes (testimony): I50.0, I50.1
When CSF: 01.02.03.02
Manufacturer: Hexal AG (Germany)

DOSAGE FORM, COMPOSITION AND PACKAGING

Valium for solution for infusion powder from white to slightly pink in color.

Excipients: mannitol.

530 mg – glass bottles with capacity 20 ml (1) – packs cardboard.

Pharmacological action

Cardiotoniceski drug neglikozidnoj of nature, beta₁-adrenomimetik. Is a racemic mixture, synthetic simpatomimeticeski Amin, related to the structure of izoproterenolu and dopamine. Has a positive inotropic effect on myocardium; moderately increases HEART RATE, increases the impact and minute amounts of heart, reduces round and vascular resistance of lesser circulation. System pressure does not change significantly. The drug causes a decrease in the pressure of filling the ventricles of the heart. Increases coronary blood flow and improves the supply of gaseous oxygen. Increase cardiac output can cause increased perfusion to the kidneys and increase the excretion of sodium and water.

Children increase stroke volume, that occurs under the influence of dobutamine, accompanied by less pronounced decrease round and ventricular filling pressure; There is a more pronounced increase in the HEART RATE and raise HELL.

The effect of the drug is 1-2 minutes after the start of infusions.

Pharmacokinetics

Distribution

In continuous infusions (C)_ss plasma levels achieved after 10-12 m. The Value Of C_ss in the blood of linearly increases with increasing infusion rate. V_d – about 0.2 l / kg.

Metabolism

Dobutamin predominantly metabolized in tissues and in the liver. Metabolism occurs mainly by conjugation with glucuronidase, as well as prior to the formation of pharmacologically inactive 3-o-methyl-dobutamine.

Deduction

T_1/2 is 2-3 m. Plasma clearance does not depend on the minutes of the heart and is 2.4 l/min/m². Report mostly kidneys and jelchew. More 2/3 from the imposed dose excreted news in the form of glukuronidov and 3-o-methyl-dobutamine.

Testimony

- Acute heart failure;

— acute decompensation of chronic heart failure;

- Congestive heart failure (If decompensation; as a temporary adjuvant on the background of standard therapy);

— low cardiac output (How adverse reaction at IVL).

Dosage regimen

The drug is introduced into / in the form of infusions. Due to the small T_1/2 dobutamine infusion should be prolonged, continuous.

The on/in infusion duration depends on clinical effectiveness. At the time of the introduction of Dobutamine Gexal requires constant monitoring of HEART RATE, heart rhythm, the magnitude of HELL, the number of selected urine and speed infusions. Possibly, during treatment should monitor the magnitude of minutes of the heart, central venous pressure and the pressure in the pulmonary capillaries.

Adults the drug is recommended in doses of 2.5-10 µg/kg body weight/min. In some cases, the dose is up to 40 ug / kg / min.

Babies the drug is recommended in doses of 1-15 ug / kg / min. When used in doses ≥ 7.5 mcg/kg/min begins to manifest most side effects (especially the tachycardia). There is evidence, testifying, that the minimum effective dose in children above, than in adults. Maximum carry-dose in children below, than in adults. The caution should produce the necessary dose selection, tk. therapeutic latitude dobutamine in children, apparently, lower.

Recommendations for the infusions of Dobutamine Gexal in different initial doses are presented in table.

* when double concentration, ie. at 2 × 250 mg dobutamine in 50 mL of solvent, You must reduce the recommended dose in 2 times.

Terms of preparation and administration of infusion solution

Dobutamin Gexal is intended only for in/infusions after pre. The speed and duration of Dobutamine Gexal set individually, taking into account the reactions of the patient and the dynamics of gemodinamicakih.

Valium for solution for the infusions originally bred in 10 ml of sterile water for injection, If the product is not fully melted, Add another 10 ml.

If necessary, further dilution of the concentrate dobutamina should use 5% glucose, 0.9% sodium chloride, ringer's solution or a solution of sodium lactate-.

Divorced solution can be stored for 24 no, After that, the solution is not to be applied

Solutions, containing dobutamine infusion, can give a pink coloring, the intensity that will grow over time (as a result of its oxidation), However, the substantial loss of activity and toxicity does not occur. Cooked solutions are not intended for repeated drug selection.

Side effect

From the hematopoietic system: Platelet dysfunction. Inhibition of platelet aggregation is transitory and manifests itself only with long-term use (infusion over several days) product. In some cases, the observed bleeding petehiale.

CNS: headache, irritability, restlessness.

Cardio-vascular system: in applying the drug in normal therapeutic doses in most cases – increased HEART RATE at 5-15 u. / min; 7-10% – increased systolic hell on 20-50 mmHg. (in patients with higher ad can expect a significant increase in HELL); in some cases – a sudden and pronounced falling of HELL, which return to their original size after dose reduction or cessation of infusion; the development of ventricular arrhythmias or strengthening existing; 5% – dose-dependent jeludockove ekstrasistola; slowing AV conduction and increased frequency of contractions of the ventricles of the heart in patients with atrial shimmer (Therefore, such patients before infuziei needed dobutamine digitalization); 1-3% – angina (especially in elderly patients), heartbeat, nausea; rarely – the small vasoconstriction (first of all in patients, who had previously received beta-adrenoblokatora).

There is a more pronounced in children compared with adults increase HEART RATE and/or magnitude of HELL, as well as more modest decrease pressure in the lung capillaries. Also noted increasing pressure in the lung capillaries, especially in children under the age of 1 year.

From the urinary system: in applying the drug in high doses can frequent craving for urinating.

Metabolism: reduction in the level of potassium in the blood serum; rarely – kaliopenia.

Allergic reactions: rarely – skin rash, fever, eozinofilija.

Local reactions: perhaps – phlebitis in places of infusion; When an accidental paravenozhnykh infiltrates may cause local inflammation of varying degrees of severity; in a few cases – skin necrosis.

Contraindications

-significantly reduced diastolic ventricular relaxation with tamponade heart;

- Aortalnыy stenosis;

-idiopathic gipertroficski subaortalny stenoses;

- Gipovolemiя;

- Simultaneous MAO inhibitors;

- Lactation;

- Pheochromocytoma;

— jeludockove adults, incl. ventricular fibrillation;

- Hypersensitivity to the drug.

Dobutamin doesn't improve hemodynamic parameters, If there are obstacles filling the ventricles and/or outflow of blood from the ventricles.

FROM caution the drug should be used with metabolic azidoze, giperkapnii, hypoxia, taxiaritmii, atrial fibrillation, myocardial infarction (dobutamine in high doses can increase HEART RATE and myocardial contractility and, increasing the need for hospitalization of oxygen, strengthen ischemia), in pulmonary hypertension, occlusive vascular diseases (arterial embolism, atherosclerosis, trombangiite obliterans/disease/Buerger's, cold injury/etc.. When frostbite/, diabetic endarteritis, Raynaud's disease), angle-closure glaucoma, Pregnancy, in children and adolescents under the age of 18 years.

Pregnancy and lactation

Application of dobutamine when pregnancy is possible only in case, if the expected benefit to the mother outweighs the potential risk to the fetus.

If necessary, the use of the drug during lactation breastfeeding should be discontinued at the time of therapy.

Cautions

When conducting continuous infusion duration 72 hours or more may develop tolerance, Therefore, higher doses may be needed to preserve the original effect.

Dissolved in sterile water for injection liofilizat dobutamina before further breeding should be stored at a temperature between 2° c to 8° c, maximum period 48 no, and at room temperature – maximally 6 no.

Further breeding should be done immediately before applying the product. Cooked solution should be used within 24 no, After that, the solution is not to be applied.

Required constant monitoring of HELL, ventricular filling pressure, central venous pressure, pressure in the pulmonary artery, Heart Rate, ECG, body temperature and diuresis, potassium concentration in blood serum.

The treatment should monitor regional increases or decreases coronary blood flow (blood flow in the coronary vessels of the heart), tk. While it is possible to change the need heart of oxygen.

The speed and duration of dobutamine establish according to the patient's reaction, which is defined by the haemodynamic parameters (Heart Rate, the rhythm of the heart, FROM) and if possible, determine the – minute volume of the heart, ventricular filling pressure (central venous, vnutrikapilljarnoe pressure in the small circle of blood circulation and pressure in the left atrium), as well as signs of changes in the pulmonary artery blood and organ blood flow (diuresis, skin temperature and mental state).

In cases, When the average AD is less than 70 mmHg., and, of course, left ventricular diastolic pressure is not increased, hypovolemia can be present, that must be corrected before the introduction of dobutamine. If HELL remains low or continue to decline during injection, Despite the adequate amount of diastolic pressure and blood minute volume, You should consider the use of dopamine or norepinephrine.

Dobutamine is not recommended as a support for gipovolemicheskom shock.

In some cases with chronic heart insufficiency under decompensation, along with dobutamine shows appointment peripheral vasodilators (incl. sodium nitroprusside, nitroglycerin).

Overdose

Symptoms: nausea, vomiting, loss of appetite, tremor, anxiety, cardiopalmus, tachycardia, integuments, ventricular fibrillation, excessive ad, myocardial ischemia, kardialgija, headache, breathlessness, anginosnaya or non-specific chest pain.

Treatment: cessation of drug administration, tracheal intubation to ensure ventilation and oxygenation of the blood. If excessive raising HELL – in/in the introduction of the Alfa-adrenoblokatorov short-acting, When ventricular tahiaritmii-propranolol or lidocaine. In the event of accidental ingestion – Activated carbon (more effective gastric lavage and inducing vomiting). Diagnostic- E pyeritonyealinyi dialysis, diurez, hemosorbtion with the use of activated charcoal is ineffective.

Drug Interactions

While receiving beta-adrenoblokatorov due to competitive inhibition of the receptors kateholaminergicheskie effects dobutamine may be weakened. Predominant while Alpha adrenergic effects contribute to peripheral vazokonstrikcii with the subsequent increase in ad.

While the blockade of α-adrenoceptor prevailing in this case, the beta-adrenostimulirujushhie effects may cause tachycardia and peripheral vasodilation.

The simultaneous use of nitroglycerin or sodium nitroprusside, especially in IBS, helps to increase the minutes of the heart and reducing systemic vascular resistance and ventricular filling pressure. HR and ad while slightly increasing or not changed.

Application of dobutamine in patients with diabetes mellitus can cause a higher need for insulin. Therefore, diabetics should monitor the level of glucose.

Simultaneous reception of ACE inhibitors and dobutamine in high doses can lead to an increase in minutes of the heart, caused by increased myocardial oxygen demand. This can lead to pain in the heart and arrhythmia.

In combination with dopamine normally no additional growth in minutes of the heart, What is possible when applying one dobutamine. However, this combination improves ad system, increases kidney bloodstream, the excretion of sodium and diurez, and also prevents increased ventricular filling pressure.

The simultaneous admission of MAO inhibitors is contraindicated, tk. in this case, perhaps threatening side effects (hypertensive crisis, collapse, cardiac arrhythmias and intracranial bleeding).

Tricyclic antidepressants, maprotilin, cocaine, doxapram, guanadrel, guanethidine, reinforce pressornyi effect and risk of kardiotoksicheskih side effects.

Ergometrine, ergotamin, methylergometrine, Oxytocin increases the vasoconstrictor effect and the risk of ischemia and gangrene, and severe hypertension, until intracranial hemorrhage.

Levodopa increases the risk of arrhythmias (require lower doses simpatomimetika).

Tireoidnye hormones increase (mutually) effect and the associated risk of coronary insufficiency (especially in koronarnom cattle).

There are no clear indications about the interaction of drugs naperstanki dobutamine, furosemidom, spironolactone, lidokainom, Isosorbide dinitratom, morphine, atropynom, geparinom, protamine sulphate, potassium chloride, folic acid and paracetamol.

Pharmaceutical incompatibility

73.21 anaesthetics derivatives of hydrocarbons (incl. chloroform, enfluran, halothane, izofluran, metoksifluran) increase the risk of severe or predserdnykh jeludockovh arrhythmias (increase the sensitivity of myocardial simpatomimetikam).

You cannot mix a solution of dobutamine with alkaline solutions (eg, 5% a solution of sodium bicarbonate), solutions, contain both sodium bisulfate, and ethanol, acyclovir, aminofillinom, bretiliem, calcium chloride, calcium glukonatom, formiatom zefamandola, zefalotina sodium salt, Cefazolin sodium salt, diazepamom, digoksinom, ethacrynic acid (sodium), furosemidom, heparin sodium, hydrocortisone sodium suktinatom, insulinom, potassium chloride, magnesium sulphate, penicillin, phenytoin, streptokinase, verapamil.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.

After the dissolution of the product can be stored for 24 h at a temperature from 2° to 8° c or over 6 h at a temperature of no higher than 25° c.