Adrenalin-Zdorovye, solution for infection 0,18% on 1 ml No. 10

General characteristics. Structure:

International and chemical названия:epinephrine(1R)-1-(3,4digidroksifenil) - 2-metilamino) - ethanol hydrogen (2R,3R) - 2,3-digidroksibutandioat; main physical and chemical properties: transparent colourless liquid; structure: 1 ml of solution contains hydrotartrate Epinephrinum in terms of 100% substance – 1,82 mg; excipients: sodium metabisulphite, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. the Adrenalin-Zdorovye – cardiostimulating, vasoconstrictive, hypertensive, hyper glycemic means. Drug stimulates a-and b-adrenoceptors of various localization. Has the expressed effect on unstriated muscles of internals, cardiovascular and respiratory systems, activates carbohydrate and lipidic metabolism. At the cellular level action is implemented through activation of adenylatecyclase of an internal surface of cellular membranes, increase in level of intracellular tsAMF and entry into a cell of calcium ions. The first phase of action is caused, first of all, stimulation of b-adrenoceptors of various bodies and is shown by tachycardia, increase in cordial emission, excitability and conductivity of a myocardium, arteriolo-and a bronkhodilatation, decrease in a tone of a uterus, inhibition of allergic reactions, mobilization of a glycogen from a liver and fatty acids from fat depos. In the second phase there is an excitement of a-adrenoceptors that leads to vasoconstriction of abdominal organs, skin, mucous membranes (skeletal muscles – to a lesser extent), to increase in arterial pressure (mainly – systolic), the general peripheric resistance of vessels. Efficiency of drug depends on a dose. In very low doses, at rate of administering it is less than 0,01 mkg/kg/min., can reduce arterial pressure owing to vasodilatation of skeletal muscles. At rate of administering of 0,04-0,1 mkg/kg/min. increases the frequency and force of cordial reductions, reduces the general peripheric resistance of vessels; higher than 0,2 mkg/kg/min. – narrow vessels, increases arterial pressure (mainly systolic) and the general peripheric resistance of vessels. 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. 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 a-adrenoceptors of skin, mucous membranes and internals, causes vasoconstriction, reduction in the rate of absorption of mestnoanesteziruyushchy means, increases duration of action and reduces toxic influence of local anesthesia. Stimulation of b2-adrenoceptors is followed by strengthening of removal of potassium from a cell and can lead to a hypopotassemia. 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, improves fabric exchange. Poorly stimulates the central nervous system, shows antiallergic and antiinflammatory action. Suppresses a lactation. The therapeutic effect at intravenous administration develops almost instantly (action duration – 1–2 min.), at hypodermic – in 5–10 min. (the maximum effect – in 20 min.), at intramuscular – time of the beginning of effect variable.

Pharmacokinetics. At intramuscular and hypodermic introduction it is quickly soaked up; the maximum concentration in blood is reached in 3–10 min. Gets through a placental barrier, into breast milk, does not get through a blood-brain barrier. Also catechol-au-methyltransferase (in метанефрин) in cells of a liver, kidneys, a mucous membrane of intestines, axons is metabolized by monoamine oxidase (in vanililmindalny acid). The elimination half-life at intravenous administration makes 1–2 min. Excretion of metabolites is carried out by kidneys. It is allocated with breast milk.

Indications to use:

Allergic reactions of immediate type (bronkhoobstruktion, acute anaphylaxis) developing at use of medicines, serums, hemotransfusion, stings of insects or administration of various allergens; arterial hypotension of various genesis (posthemorrhagic, intoksikatsionny, infectious), an asystolia, a bronchospasm during an anesthesia, a hypoglycemic coma (at insulin overdose). Bleeding of superficial vessels of skin and mucous membranes, including from gums (topical administration).

Route of administration and doses:

Appoint intramusculary, subcutaneously, sometimes – intravenously (kapelno), vnutriserdechno (performing resuscitation at a cardiac standstill), locally. At intramuscular introduction action begins quicker, than at hypodermic. Dosing mode individual. For adults of a dose at intramuscular and hypodermic introduction make, usually 0,3–0,75 ml. The injection can repeat each 10 min. under control of heart rate and arterial pressure before improvement of a condition of the patient. The highest doses at hypodermic introduction: one-time – 1 ml, daily – 5 ml. The patient with critical condition and the expressed disturbances of a hemodynamics enter intravenously slowly, having dissolved 1 ml of drug in 500 ml of isotonic solution of sodium of chloride (rate of administering – 1–4 mkg/min., i.e. 0,3–1,2 ml/min.); at achievement of effect introduction is stopped. Vnutriserdechno is entered at an asystolia if other ways of introduction are unavailable since there is a risk of a cardiac tamponade and pheumothorax. Vnutriserdechno is entered by 0,1–0,2 mg through a special long needle. For children single doses at intramuscular and hypodermic introduction make: till 1 year – 0,1–0,15 ml, 1–4 years – 0,2–0,25 ml, 5–7 years – 0,3–0,4 ml, 8–10 years – 0,4–0,5 ml, are more senior than 10 years – 0,5 ml. Frequency of introductions – 1–3 times a day. Stop of bleedings: apply locally, putting the tampons moistened with drug.

Features of use:

The drug should not be administered vnutriarterialno since excessive narrowing of peripheral vessels can lead to a gangrenosis. With care apply at advanced and children's age. At endocardiac introduction it is necessary to control arterial pressure, central venous pressure, pulmonary pressure, heart rate. Introduction of Adrenalina-Zdorovye at depressed cases does not replace hemotransfusion, plasma, blood-substituting liquids and/or saline solutions. Drug is inexpedient to be used is long (the narrowing of peripheral vessels leading to possible development of a necrosis or gangrene). For prevention of arrhythmias at the same time appoint b-adrenoblockers. Data on use at reduced function of kidneys or a liver are absent. Use for correction of hypotension at the time of delivery is not recommended as drug can detain the second stage of childbirth; at introduction in high doses for weakening of reduction of a uterus can cause a long atony of a uterus with bleeding. Lactation period. Feeding by a breast should be stopped.

Side effects:

From cardiovascular system: arterial hypertension, disturbances of a heart rhythm (tachycardia, fibrillation of ventricles), stenocardia, heartbeat, pallor of face skin, a hemorrhagic stroke, a fluid lungs (at high doses). From the central nervous system: headache, alarming state, tremor; seldom – dizziness, sensation of fear, the general weakness, a sleep disorder, psychoneurotic frustration. Allergic reactions: skin rash, multiformny erythema. From digestive tract: nausea, vomiting. From a metabolism: the hypopotassemia, a hyperglycemia are possible. Local reactions: pain or burning in the place of an injection.

Interaction with other medicines:

Antagonists of Epinephrinum are blockers of a-and b-adrenoceptors. Weakens effects of narcotic analgetics and somnolent medicines. At use along with cardiac glycosides, quinidine, tricyclic antidepressants, a dopamine the risk of development of arrhythmias increases; with other sympathomimetic means – strengthening of expressiveness of side effects from cardiovascular system; with anti-hypertensive means (including with diuretics) – decrease in their efficiency. Co-administration with monoamine oxidase inhibitors can cause the sudden and expressed increase in arterial pressure, a headache, heart arrhythmias, vomiting; with nitrates – weakening of their therapeutic action; with phenoxybenzamine – strengthening of hypotensive effect and tachycardia; with Phenytoinum – a sudden lowering of arterial pressure and bradycardia (depends on a dose and rate of administering); with drugs of hormones of a thyroid gland or an Euphyllinum – mutual strengthening of action; with ergot alkaloids – strengthening of vasopressor effect (up to the expressed ischemia and a gangrenosis). Reduces effect of hypoglycemic medicines (including insulin). Can reduce action of hormonal contraceptives, reduce myorelaxation effect of not depolarizing muscle relaxants. At simultaneous use with drugs for the general anesthesia development of life-threatening arrhythmias is possible.

Contraindications:

Hypersensitivity to Epinephrinum to hydrotartrate, arterial or pulmonary hypertension, the expressed atherosclerosis, stenocardia, a serious illness of heart (a myocardial infarction, coronary insufficiency), aneurisms, a tachyarrhythmia, fibrillation of ventricles or auricles, a metabolic acidosis, a hypovolemia, shock of not allergic genesis, occlusal diseases of vessels, a convulsive syndrome, a thyrotoxicosis, a pheochromocytoma, a diabetes mellitus, closed-angle glaucoma, pregnancy. An anesthesia inhalation means for the general anesthesia (Ftorotanum, cyclopropane – danger of developing of arrhythmia)

Overdose:

Symptoms: excessive increase in arterial pressure, a mydriasis, the tachycardia which is replaced by bradycardia, disturbances of a heart rhythm (including fibrillation of auricles and ventricles), a cold snap and pallor of integuments, vomiting, a headache, a metabolic acidosis, a fluid lungs, a myocardial infarction, craniocereberal hemorrhage (especially at elderly patients).

Treatment: termination of administration of drug, introduction of a-and b-adrenoblockers, high-speed nitrates; at heavy complications complex therapy is necessary.

Storage conditions:

To store in the place protected from light at a temperature from 8 °C to 15 °C. To store in the place, unavailable to children.

Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 1 ml of 5 ampoules in a blister strip packaging, No. 5х2 in a pack; on 5 or 10 ampoules in a pack.