Adrenaline - instructions for use, dose, side effects, contraindications

Excipients: sodium chloride - 8.00 mg, sodium disulfite - 1.00 mg, (sodium metabisulfite) chlorobutanol hemihydrate (chlorobutanol hydrate) equivalent to 5.00 mg chlorobutanol, disodium edetate 0.50 mg, (disodium ethylenediaminetetraacetic acid) glycerol ) - 60,00 mg, hydrochloric - up to pH acid 2,5-4,0, water for injections - up to 1 ml.

Description:

Transparent colorless or slightly colored liquid with a characteristic odor.

Pharmacotherapeutic group:Alpha- and beta-adrenomimetic

ATX: & nbsp

C.01.C.A.24 Epinephrine

Pharmacodynamics:

The effect is due to the activation of the receptor-dependent adenylate cyclase on the inner surface of the cell membrane, increasing the intracellular concentration of cyclic adenosine monophosphate (cAMP) and calcium ions (Ca2 +).

In very low doses, at an administration rate of less than 0.01 μg / kg / min, reduce arterial pressure, due to expansion of the vessels of the skeletal musculature. At a rate of administration of 0.04-0.1 μg / kg / min increases the frequency and strength of heartbeats, the shock volume of blood and the minute volume of blood, reduces the overall peripheral vascular resistance; higher than 0.02 μg / kg / min narrows vessels, raises arterial pressure (mainly, systolic) and a common peripheral vascular resistance. The pressor effect can cause a short-term reflex slowing of heart rate abbreviations.

Relaxes the smooth muscles of the bronchi., Doses above 0.3 μg / kg / min, reduce renal blood flow, blood supply to the internal organs, tone and, motility of the gastrointestinal tract. It dilates the pupils, helps reduce the production of intraocular fluid and intraocular pressure. It causes hyperglycemia (increases glycogenolysis, and gluconeogenesis) and increases the content of free fatty acids in the plasma.

POvercomes the conductivity, excitability and automatism of the myocardium. Increases myocardial oxygen demand.Inhibits the antigen-induced release of histamine and leukotrienes, eliminates spasm, bronchioles, prevents the development of edema mucous membrane.

Acting on α-adrenergic receptors located in the skin, mucous membranes and internal organs, causes vasoconstriction, reduced rate of absorption of local anesthetics, prolongs duration and reduces the toxic effect of local anesthesia.

Stimulation b₂-adrenoceptorsis accompanied by increased excretion of potassium ions (K +) from the cell and can lead to hypokalemia.

With intracavernous injection reduces blood filling of cavernous bodies.

The therapeutic effect develops almost instantaneously with intravenous administration (duration of action is 1-2 minutes), 5-10 minutes after subcutaneous injection (maximum effect after 20 minutes), with intramuscular introduction - the time of onset of the effect is variable.

Pharmacokinetics:

Suction

When intramuscular or subcutaneous injection is well absorbed. Entered parenterally, rapidly destroyed. Also absorbed in endotracheal and conjunctival administration. Time to reach the maximum concentration in the blood. with subcutaneous and.intramuscular injection - 3-10 minutes. Penetrates through placenta, into breast milk, does not penetrate the blood-brain barrier.

Metabolism

Metabolized mainly monoamine oxidase and catechol-O-methyltransferase in the endings of sympathetic nerves and other tissues, as well as in the liver with the formation of inactive metabolites. Half-life with intravenous administration - 1-2 minutes.

Excretion

It is excreted by the kidneys in the main form of metabolites: vanillylmandelic acid, sulfates, glucuronides, and also in a small amount - in unchanged form.

Indications:

· Allergic reactions of immediate type (including urticaria, angioedema, anaphylactic shock), developing with the use of drugs, serums, blood transfusions, eating foods, insect bites or other allergens; asthma of physical effort;

· Bronchial asthma (relief of asthmatic status), bronchospasm during anesthesia;

· Asystole (including on the background of acute development of atrioventricular blockade of the third degree);

· Bleeding from the superficial vessels of the skin and mucous membranes (including gums);

· Arterial hypotension that does not respond to adequate volumes of replacement fluids (including shock, bacteremia, open heart surgery, kidney failure);

· The need to lengthen the action of local anesthetics;

· Episodes full of atrioventricular blockade (with the development of the syncopal condition (Morgagni-Adams-Stokes syndrome));

· Stop bleeding (as a vasoconstrictor).

Contraindications:

Hypersensitivity to any of the components of the drug, hypertension, severe atherosclerosis (including cerebral atherosclerosis), hypertrophic obstructive cardiomyopathy, tachyarrhythmia, ischemic heart disease, ventricular fibrillation, atrial fibrillation, ventricular arrhythmias, chronic heart failure grade 3-4, myocardial infarction, pheochromocytoma, thyrotoxicosis, diabetes mellitus, acute and chronic arterial insufficiency (including in the anamnesis-arterial embolism, atherosclerosis, diseases Burger, diabetic endarteritis, Raynaud's disease), hypovolemia, metabolic acidosis, hypercapnia, hypoxia, pulmonary hypertension, shock, non-allergic genesis (including cardiogenic,traumatic, hemorrhagic), cold trauma, Parkinson's disease; organic lesions of the brain, angle-closure glaucoma, seizure syndrome, prostatic hyperplasia, age under 18 years (except for conditions directly threatening life), pregnancy, lactation, simultaneous use of inhalation for general anesthesia (halothane), epinephrine in combination with local anesthetics are not used for local anesthesia of the fingers and toes due to the risk of ischemic tissue damage.

In urgent conditions, all contraindications are relative.

Carefully:

Hyperthyroidism, old age.

For the prevention of arrhythmias against the background, the use of the drug is prescribed. beta-blockers.

Pregnancy and lactation:see the section "Contraindications".

Dosing and Administration:

Subcutaneously, intramuscularly, intravenously drip.

Allergic reactions of immediate type (anaphylactic shock): intravenously slowly 0.1-0.25 mg diluted in 10 ml of 0.9% sodium chloride solution, if necessary continue intravenous drip introduction at a concentration of 1: 10,000.In the absence of immediate, life threatening, intramuscular or subcutaneous injection of 0.3-0.5 mg is preferred, if necessary, repeated administration 10-20 minutes up to 3 times.

Bronchial asthma: subcutaneously 0.3-0.5 mg, if necessary, repeated doses can be administered every 20 minutes up to 3 times, or intravenously, 0.1-0.25 mg with dilution at a concentration of 1: 10,000.

With asystole: intracardiac 0.5 mg (diluted with 10 ml of 0.9% sodium chloride solution or other solution); during resuscitation - 0.5-1 mg (in diluted form) intravenously every 3-5 minutes. If the patient is intubated, endotracheal instillation is possible - doses should be 2-2.5 times the dose for intravenous administration.

Stop bleeding - Locally in the form of tampons moistened with a solution of the drug.

With arterial hypotension: intravenously drip 1 μg / min, the rate of administration can be increased to 2-10 μg / min.

To lengthen the action of local anesthetics: in a concentration of 0.005 mg / ml (the dose depends on the type of anesthetic used), for spinal anesthesia 0.2-0.4 mg.

Morgagni-Adams-Stokes Syndrome (bradyiothymic form) in a dose of 1 mg in 250 ml of 5% glucose solution intravenously, gradually increasing the infusion rate until a minimum sufficient number of heartbeats is reached.

As a vasoconstrictor: intravenously drip 1 μg / min; the rate of administration can be increased to 2-10 μg / min:

Application in children's practice:

Newborns (asystole): intravenously, 10-30 mcg / kg every 3-5 min, slowly.

For children: older than 1 month: intravenously, 10 mcg / kg (later every 3-5 minutes, 100 μg / kg is administered (after administration of at least 2 standard doses, higher doses of 200 μg / kg can be used every 5 minutes). Endotracheal administration can be used.

Children with anaphylactic shock: subcutaneously or intramuscularly at 0.01 mg / kg (maximal - up to 0.3 mg), if necessary, the administration of these doses is repeated every 15 minutes (up to 3 times).

Children with bronchospasm: subcutaneously 10 μg / kg (maximal - up to 0.3 mg), doses are repeated every 15 min if necessary; (up to 3-4 times) or every 4 hours.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10;

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000,

very rarely from <1/10000, including individual messages.

From the cardiovascular system: infrequently - angina, bradycardia or tachycardia, palpitations, increased or decreased arterial - pressure, at high doses - ventricular arrhythmias (including ventricular fibrillation); rarely - arrhythmia, chest pain, pulmonary edema.

From the nervous system: often - headache, anxiety, tremor; tic, infrequent - dizziness, nervousness, fatigue, nausea, vomiting, personality disorders (psychomotor agitation, disorientation, memory impairment, psychotic disorders: aggressive or panic behavior, schizophreniform disorders, paranoia), sleep disturbance, muscle twitching.

From the digestive system: often - nausea, vomiting.

From the side of the urinary system: rarely - - difficulty and painful urination (with hyperplasia of the prostate gland).

Local reactions: infrequently - pain or burning in the place of intramuscular injection.

Allergic reactions: infrequently - angioedema, bronchospasm, skin rash, erythema multiforme.

Other: infrequently - increased sweating; rarely - hypokalemia.

If the side effects indicated in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: excessive increase. arterial pressure, tachycardia, followed by bradycardia, rhythm disturbances (including atrial and ventricular fibrillation),coldness and pallor of the skin, vomiting, headache, metabolic acidosis, myocardial infarction, craniocerebral hemorrhage (especially in elderly patients), pulmonary edema, death.

Treatment: stop the introduction, symptomatic therapy - to lower blood pressure - α-adrenoblockers (phentolamine), with arrhythmias - b-adrenoblockers (propranolol).

Interaction:

Epinephrine antagonists are α- and β-adrenoreceptor blockers.

The efficacy of epinephrine has been reduced in patients with severe anaphylactic reactions taking b-adrenoblockers. In this case, intravenously apply salbutamol.

Application in conjunction with other adrenomimetics can enhance the effect of epinephrine.

Weakens the effects of narcotic analgesics and hypnotics.

When used concomitantly with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, agents for inhalation anesthesia (enflurane, halothane, isoflurane, methoxyflurane), the risk of arrhythmias increases with cocaine (together it should be used very carefully or not at all); with other adrenomimetics - increased severity of side effectseffects from the side, cardiovascular system; with antihypertensive agents - reducing their effectiveness.

With diuretics - it is possible to increase the pressor effect of epinephrine. Simultaneous use with drugs inhibiting monoamine oxidase (procarbazine, selegiline, and furazolidone,) can cause a sudden and pronounced increase in blood pressure, hyperpyretic crisis, headache, cardiac arrhythmias, vomiting; with nitrates - weakening of their therapeutic effect; with phenoxybenzamine - increased hypotensive effect and tachycardia; with phenytoin - a sudden decrease in blood pressure and bradycardia (depends on the dose and rate of administration); with preparations of hormones, thyroid gland - mutual reinforcement of action; with drugs prolong the QT-interval (including astemizole, cisapride, terfenadine) - lengthening QT-interval; with diatrizoatami, iotalamovoy or yoksaglovoj acids - intensification of neurologic effects; with alkaloids of ergot - increased vasoconstrictor effect (up to pronounced ischemia and development of gangrene).

Reduces the effect of insulin and other hypoglycemic drugs.

Special instructions:

A random intravenous injection of epinephrine can cause a sharp increase in blood pressure.

Increased blood pressure when injecting the drug can cause attacks of angina pectoris. Epinephrine can cause the constriction of capillaries of the kidneys, thereby reducing diuresis.

For infusion, a device with a measuring device should be used to regulate the infusion rate.

Infusion should be carried out in a large (better in the central) vein.

Intra-cardinally administered with asystole, if other methods are not available, because there is a risk of cardiac tamponade and pneumothorax.

During the treatment, it is recommended to determine the concentration of potassium ions (K +) in the blood serum, measure blood pressure, diuresis, minute volume of circulation, electrocardiogram, central venous pressure, pulmonary artery pressure and wedge pressure in the pulmonary capillaries. Excessive doses for myocardial infarction, may enhance ischemia by increasing the myocardial oxygen demand.

Increases the glycemia, in, the connection, with which diabetes requires higher doses of insulin and sulfonylurea derivatives.

With endotracheal injection, the absorption and final concentration of the drug in the plasma can be unpredictable.

The introduction of epinephrine in shock, states does not replace transfusion of blood, plasma, blood-substituting fluids and / or saline solutions.

Epinephrine is inexpedient to apply for a long time (narrowing of peripheral vessels, leading to the possible development of necrosis or gangrene).

Strictly controlled studies of the use of epinephrine in pregnant women have not been conducted. Statistically consistent, the relationship between the appearance of malformations and inguinal hernia in children whose mothers were used epinephrine during the first trimester or throughout the pregnancy, there was also reported in one case about the occurrence of anoxia, in the fetus, after intravenous administration - the mother of epinephrine.

Use to correct low blood pressure during labor is not recommended because it can delay the second stage of labor; when administered in large doses to reduce uterine contractions, may cause a prolonged atony of the uterus with bleeding.

Can be used in children with cardiac arrest, but caution should be used.

When discontinuing, treatment of the dose should be reduced gradually, because sudden abolition of therapy can lead to a decrease in blood pressure.

Easily destroyed by alkylating agents and oxidizing agents, including chlorides, bromides, nitrites, iron salts, peroxides.

If the solution has acquired a pinkish or brown color or contains a sediment it can not be injected. Unused portion should be destroyed.

Effect on the ability to drive transp. cf. and fur:

After applying the drug, the doctor must individually, in each case, decide whether to admit the patient to the management of transport or to engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions

Form release / dosage:Solution for injection 1 mg / ml.

Packaging:

Into ampoules of 1 ml. 5 ampoules per contour cell pack.

For 1 or 2 contour packs with instruction on the use of the drug, a knife or scarifier ampullum in a pack of cardboard.

For 20, 50 or 100 contour cell packs with 20, 50 or 100 instructions for the use of the drug, respectively, with knives or scribers ampoule into boxes of cardboard or boxes of corrugated cardboard (for inpatient).

When packing ampoules with notches, rings and break points, knives or scarifier ampoules do not.

Storage conditions:

In the dark place at a temperature of no higher than 15 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-001849

Date of registration:30.12.2011/09.09.2014

Expiration Date:Unlimited

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Information update date: & nbsp04.02.2017

Illustrated instructions

Instructions

Adrenalin (Adrenaline)