Adrenalin-Darnitsa, r-nd/in. амп.по 1 ml No. 10

General characteristics. Structure:

Active ingredient: 1 ml of solution contains tartrate adrenaline (tartrate Epinephrinum) in terms of 100% dry matter of 1,8 mg;
excipients: sodium metabisulphite, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Treats natural hormones. It is formed by methylation of noradrenaline and deposition of newly created adrenaline in chromaffin fabric of marrow of adrenal glands. Adrenomimetik acting on a-and b-adrenoceptors. Bigger affinity shows adrenaline concerning a2-, b2-and b3-of adrenoceptors, smaller to a1-ib1-to adrenoceptors.
Action is caused by activation of adenylatecyclase on an internal surface of a cellular membrane, increase in intracellular concentration of tsAMF and Ca2+. In very low doses at rate of administering arterial pressure owing to vasodilatation of skeletal muscles can reduce less than 0,01 mkg/kg/min. At rate of administering of 0,04-0,1 mkg/kg/min. increases the heart rate and force of cordial reductions, a stroke output of blood and minute volume of blood, reduces the general peripheric vascular resistance; higher than 0,02 mkg/kg/min. – narrow vessels, increases arterial pressure (mainly systolic) and the general peripheric vascular resistance. The pressor effect can cause short-term reflex delay of heart rate. Weakens unstriated muscles of bronchial tubes. Doses higher than 0,3 mkg/kg/min. reduce a renal blood stream, blood supply of internals, a tone and motility of digestive tract. Expands pupils, promotes decrease in products of intraocular liquid and intraocular pressure. Causes a hyperglycemia (strengthens a glycogenolysis and a gluconeogenesis) and increases the content in plasma of free fatty acids. Increases conductivity, excitability and automatism of a myocardium. Increases the need of a myocardium for oxygen. Inhibits the release of a histamine and leukotrienes induced by antigens, eliminates a spasm of bronchioles, prevents edematization of their mucous. Affecting the alpha adrenoceptors located in skin, mucous membranes and internals causes vasoconstriction, reduction in the rate of absorption of mestnoanesteziruyushchy means, increases duration and reduces toxic influence of local anesthesia. Stimulation of b2-adrenoceptors is followed by strengthening of removal of K+ from a cell and can lead to a hypopotassemia. At intrakavernozny introduction reduces a krovenapolneniye of cavernous bodies. The therapeutic effect develops almost instantly at intravenous administration (action duration – 1–2 min.), in 5–10 min. after hypodermic introduction (the maximum effect – in 20 min.), at intramuscular introduction time of the beginning of effect variable.

Pharmacokinetics. Absorption. At intramuscular or hypodermic introduction it is well soaked up. Time of achievement of the maximum concentration in blood (TCmax) at hypodermic and intramuscular introduction – 3–10 min.

Distribution. Gets through a placenta, into breast milk, does not get through a blood-brain barrier.

Metabolism. It is metabolized, mainly, by two enzymes – the catechol-0-methyltransferase turning adrenaline in a liver and other fabrics in метанефрин, and monoamine oxidase with the participation of which it turns into vanililmindalny acid.

Removal. Metabolites are removed generally in the form of conjugates with sulphuric acid and, to a lesser extent, with urine in the form of glucuronides. The elimination half-life (T12) makes 1–2 min.

Indications to use:

Allergic reactions of immediate type: the acute anaphylaxis which developed at use of medicines, serums or contact with allergens. Bronchial asthma – stopping of an attack. A hypoglycemia owing to insulin overdose. Hypopotassemia. Asystolia, cardiac standstill. Lengthening of effect of local anesthetics. Sharply developed AV blockade of the III St.

Route of administration and doses:

Drug is appointed subcutaneously, intramusculary, sometimes intravenously or intravenously kapelno.

Acute anaphylaxis: intravenously slowly 0,5 ml of 40% of solution of glucose divorced in 20 ml. Further, if necessary, continue intravenous drop administration with a speed of 1 mkg/min. for what 1 ml of solution of adrenaline dissolve in 400 ml of isotonic sodium of chloride or 5% of glucose. When the condition of the patient allows, intramuscular or hypodermic introduction is more preferable than 0,3-0,5 ml in the diluted or undiluted look.

Bronchial asthma: subcutaneously 0,3–0,5 ml in the diluted or undiluted look. In need of repeated introduction it is possible to enter this dose every 20 min. (to 3 times). Perhaps intravenous administration of 0,3-0,5 ml in the diluted look.

As a vasoconstrictor enter intravenously kapelno with a speed of 1 mkg/min. (with possible increase up to 2–10 mkg/min.).

At an asystolia: enter vnutriserdechno 0,5 ml diluted in 10 ml of 0,9% of solution of sodium of chloride. During the resuscitation actions – on 1 ml (in the diluted look) intravenously slowly each 3–5 min.

At an asystolia at newborns: intravenously to 10-30 mkg/kg there are each 3–5 min., slowly.

To children at an acute anaphylaxis: subcutaneously or intramusculary – on 10 mkg/kg (as much as possible – to 0,3 mg). If necessary introduction is repeated every 15 min. (to 3 times).

To children at a bronchospasm: subcutaneously 10 mkg/kg (as much as possible – to 0,3 mg). If necessary introduction is repeated by each 15 min. (to 3–4 times) or each 4 h.

Incompatibility.

Not to mix in one syringe with solutions of acids and alkalis because of possible chemical interaction of active ingredient.

Features of use:

Vnutriserdechno is entered at an asystolia if other ways of its elimination are unavailable, at the same time there is an increased risk of development of a cardiac tamponade and pheumothorax.

In case of need performing infusion it is necessary to use the device with measuring adaptation for the purpose of regulation of speed of infusion. Infusion should be carried out to large, it is better in central, a vein.

When performing infusion definition of concentration of K+ in blood serum, measurement of arterial pressure, a diuresis, the IOC, an ECG, the central venous pressure, pulmonary pressure and pressure of jamming in pulmonary capillaries is recommended.

In case of need of use of drug at a myocardial infarction, it is necessary to remember that adrenaline can strengthen ischemia due to increase in need of a myocardium for oxygen.

Use of drug for patients with a diabetes mellitus increases a glycemia in this connection, higher doses of insulin or derivatives of sulphonylurea are required.

At endotracheal introduction absorption and final concentration of drug in plasma can be unpredictable.

Administration of adrenaline at shock not of the allergic nature does not replace hemotransfusion, plasma, blood-substituting liquids and/or saline solutions.

It is undesirable to apply adrenaline it is long as the narrowing of peripheral vessels leading to development of a necrosis or gangrene is possible.

At the treatment termination the dose of adrenaline should be reduced gradually since sudden cancellation of therapy can lead to heavy hypotension.

Use during pregnancy or feeding by a breast.

Strictly controlled researches on use of adrenaline for pregnant women were not conducted. Statistically proved interrelation of emergence of uglinesses and inguinal hernia at children to whose mothers appointed adrenaline during the I trimester or throughout all pregnancy is established. It was reported also about emergence of an anoxia at a fruit after intravenous administration of adrenaline of mother.

Experiences on laboratory animals showed that at administration of adrenaline in the doses, by 25 times exceeding recommended for the person the teratogenic effect develops.

Use of adrenaline for correction of hypotension at the time of delivery can detain the second stage of childbirth. At introduction to women in labor of adrenaline for weakening of reduction of a uterus the long atony of a uterus with bleeding can develop.

Side effects:

At use of drug are possible following collateral реакции:со the parties of cardiovascular system: stenocardia, bradycardia or tachycardia, heart consciousness, increase or lowering of arterial pressure; at high doses – ventricular arrhythmias; seldom – arrhythmia, thorax pain;

from a nervous system: headache, alarming state, tremor, dizziness, nervousness, fatigue, psychoneurotic frustration, psychomotor excitement, disorientation, memory disturbance, agressive or panic behavior, shizofrenopodobny frustration, paranoia, sleep disorder, muscular twitchings;

from the alimentary system: nausea, vomiting;

from an urinary system: seldom – complicated and an urodynia (at a prostate hyperplasia);

local reactions: pain or burning in the place of an intramuscular injection;

allergic reactions: Quincke's disease, bronchospasm, skin rash, mnogoformny erythema;

others: a hypopotassemia, the increased sweating.

Interaction with other medicines:

Adrenaline weakens effects of narcotic analgetics and somnolent medicines. At use along with cardiac glycosides, quinidine, tricyclic antidepressants, a dopamine, means for an inhalation anesthesia (chloroform, энфлуран, a halothane, изофлуран, метоксифлуран), cocaine the risk of development of arrhythmias increases.

At combined use with other sympathomimetic means – strengthening of expressiveness of side effects from cardiovascular system.

At combined use with anti-hypertensive means, including diuretics – decrease in their efficiency.

Co-administration with MAO inhibitors, including furasolidone, Procarbazinum, селегилин, can cause the sudden and expressed increase in arterial pressure, hyperpyrexial crisis, a headache, heart arrhythmias, vomiting.

At combined use with nitrates weakens their therapeutic action.

At combined use with phenoxybenzamine strengthening of hypotensive effect and tachycardia develops.

At combined use with Phenytoinum the sudden lowering of arterial pressure and bradycardia which depend on a dose and rate of administering of adrenaline develops.

At combined use with drugs of hormones of a thyroid gland perhaps mutual strengthening of action.

At combined use with astemizoly, tsizapridy, terfenadiny lengthening of a Q-T-interval on an ECG is possible.

At combined use with Diatrizoatums, yotalamovy or yoksaglovy acids – strengthening of neurologic effects.

At combined use with alkaloids of an ergot strengthening of vasopressor effect up to the expressed ischemia and a gangrenosis is possible.

Adrenaline reduces efficiency of insulin and other hypoglycemic medicines.

Contraindications:

Hypersensitivity to drug components. Hypertrophic subaortic stenosis (GOKMP), pheochromocytoma. Arterial hypertension. Tachyarrhythmia. Coronary heart disease. Fibrillation of ventricles. Fibrillation of auricles, ventricular arrhythmia. Metabolic acidosis. Hypercapnia, hypoxia. Pulmonary hypertensia. Hypovolemia. Myocardial infarction. Shock of not allergic genesis: cardiogenic, traumatic, hemorrhagic. Thyrotoxicosis. Occlusal diseases of vessels: arterial embolism, atherosclerosis, Thrombangiitis obliterans, cold injury, diabetic endarteritis, Raynaud's disease. Cerebral atherosclerosis. Closed-angle glaucoma. Parkinson's disease. Convulsive syndrome. Prostatauxe. The general anesthesia using inhalation means: Ftorotanum, cyclopropane, chloroform. Pregnancy, lactation period.

Overdose:

Symptoms: fear, concern, tremor, disturbances of a cordial rhythm, headache. Brain hemorrhages owing to sharp increase in arterial pressure are possible. At introduction in high doses (the minimum lethal dose at hypodermic introduction of 10,0 ml of 0,18% of solution) the mydriasis, substantial increase of arterial pressure, tachycardia with possible transition to fibrillation of ventricles develops.

Treatment: the overdose of adrenaline can be eliminated with use α-and β-adrenoblockers, high-speed nitrates. At heavy complications complex therapy is necessary. At arrhythmia appoint parenteral administration of β-adrenoblockers..........

Storage conditions:

To store in the place, unavailable to children, in original packaging, at a temperature not above 15 °C.

Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule; on 10 ampoules in packaging.