ADRENALINA HYDROCHLORIDE Grotex solution for injection 0.1% amp.

Instructions for use

ADRENALINA HYDROCHLORIDE Grotex solution for injection 0.1% amp. 1 ml No. 5

Compound

1 ml of the drug contains:

Active substance:

Adrenaline tartrate

in terms of adrenaline (epinephrine) 1.0 mg

Excipients:

Sodium chloride 8.0 mg

Chlorobutanol hemihydrate in terms of

chlorobutanol 5.0 mg

Disodium edetate dihydrate (Trilon B) 0.5 mg

Glycerol anhydrous 60.0 mg

Hydrochloric acid solution 5 M or

sodium hydroxide solution 2 M to pH 2.2-5.0

Water for injection up to 1.0 ml.

Dosage form

injection

Description

Transparent colorless or slightly colored liquid with a characteristic odor.

Pharmacodynamics

The action is due to the activation of receptor-dependent adenylate cyclase on the inner surface of the cell membrane, an increase in the intracellular concentration of cyclic adenosine monophosphate (cAMP) and calcium ions (Ca2 +). At very low doses, at an injection rate of less than 0.01 μg / kg / min, it can reduce blood pressure due to vasodilation of skeletal muscles. At an injection rate of 0.04-0.1 μg / kg / min, it increases the frequency and strength of heart contractions, stroke volume and minute blood volume, decreases total peripheral vascular resistance, pressure (mainly systolic) and total peripheral vascular resistance. The pressor effect can cause a short-term reflex slowdown of the heart rate.

Relaxes the smooth muscles of the bronchi. Doses above 0.3 μg / kg / min reduce renal blood flow, blood supply to internal organs, tone and motility of the gastrointestinal tract.

They dilate the pupils, help to reduce the production of intraocular fluid and intraocular pressure. Causes hyperglycemia (enhances glycogenolysis and gluconeogenesis) and increases plasma free fatty acids.

Increases the conductivity, excitability and automatism of the myocardium. Increases myocardial oxygen demand.

Inhibits antigen-induced release of histamine and leukotrienes, eliminates spasm of bronchioles, prevents the development of edema of their mucous membranes. Acting on β-adrenergic receptors located in the skin, mucous membranes and internal organs, it causes vasoconstriction, a decrease in the rate of absorption of local anesthetics, increases the duration and reduces the toxic effect of local anesthesia.

Stimulation of 2-adrenergic receptors is accompanied by an increase in the excretion of potassium ions (K +) from the cell and can lead to hypokalemia.

With intracavernous administration, it reduces the blood filling of the cavernous bodies. The therapeutic effect develops almost instantly with intravenous administration (duration of action - 1-2 minutes), 5-10 minutes after subcutaneous administration (maximum effect - after 20 minutes), with intramuscular administration - the time of the onset of the effect is variable.

Pharmacokinetics

Suction

When administered intramuscularly or subcutaneously, it is well absorbed. When administered parenterally, it rapidly degrades. It is also absorbed by endotracheal and conjunctival administration. The time to reach the maximum concentration in the blood with subcutaneous and intramuscular administration is 3-10 minutes. It crosses the placenta, into breast milk, does not cross the blood-brain barrier.

Metabolism

It is metabolized mainly by 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. The half-life for intravenous administration is 1-2 minutes.

Withdrawal

It is excreted by the kidneys mainly in the form of metabolites: vanillyl mandelic acid, sulfates, glucuronides. and also in small quantities - unchanged.

Indications for use

- Allergic reactions of immediate type (including urticaria, angioedema, anaphylactic shock), developing with the use of drugs, serums, blood transfusions, food consumption, insect bites or the introduction of other allergens, asthma of physical effort.

- Bronchial asthma (relief of status asthmaticus), bronchospasm during anesthesia.

- Asystole (including against the background of acutely developing grade III atrioventricular block).

- Bleeding from the superficial vessels of the skin and mucous membranes (including the gums).

- Arterial hypotension, not amenable to the influence of adequate volumes of replacement fluids (including shock, bacteremia, open heart surgery, renal failure).

- The need to lengthen the action of local anesthetics.

- Episodes of complete atrioventricular block (with the development of syncope (Morgagni-Adams-Stokes syndrome)).

- Stopping bleeding (as a vasoconstrictor).

Contraindications

Symptoms: excessive increase in blood pressure, tachycardia, alternating with 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 administration, symptomatic therapy - to lower blood pressure - -adrenergic blockers (phentolamine), in case of arrhythmia - -adrenergic blockers (propranolol).

Application during pregnancy and lactation

Use during pregnancy and during breastfeeding is contraindicated.

Side effects

Classification of the incidence of side effects according to the World Health Organization (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 rare (from <, 1/10000, including individual messages).

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

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

From the digestive system: often - nausea, vomiting.

From the urinary system: rarely - difficult and painful urination (with prostatic hyperplasia).

Local reactions: infrequently - pain or burning at the site of intramuscular injection. Allergic reactions: infrequently - angioedema, bronchospasm, skin rash, erythema multiforme.

Others: infrequently - increased sweating, rarely - hypokalemia.

If the side effects indicated in the instructions are aggravated, or you notice any other side effects that are not indicated in the instructions, inform your doctor.

Interaction

Epinephrine antagonists are blockers of α- and β-adrenergic receptors.

The efficacy of epinephrine is reduced in patients with severe anaphylactic reactions taking β-blockers. In this case, salbutamol is used intravenously.

The use in conjunction with other adrenergic agonists can enhance the effect of epinephrine. Weakens the effects of narcotic analgesics and sleeping pills.

When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, means for inhalation anesthesia (enflurane, halothane, isoflurane, methoxyflurane), cocaine, the risk of arrhythmias increases (together they should be used very carefully or not at all), with other adrenomimetics - strengthening the severity of side effects from the cardiovascular system, with antihypertensive drugs - a decrease in their effectiveness.

With diuretics, an increase in the pressor effect of epinephrine is possible.

Simultaneous use with drugs that inhibit monoamine oxidase (procarbazine, selegiline, as well as furazolidone) can cause a sudden and pronounced increase in blood pressure, hyperpyretic crisis, headache, cardiac arrhythmias, vomiting, with nitrates - a weakening of their therapeutic effect, with phenoxybenzamine - an increase in hypotensive effect and tachycardia: with phenytoin - a sudden decrease in blood pressure and bradycardia (depending on the dose and rate of administration), with preparations of thyroid hormones - mutual enhancement of the action, with drugs that prolong the QT interval (including astemizole, cisapride, terfenadine) - lengthening of the QT interval, with diatriazoates, iothalamic or ioxaglic acids - increased neurological effects, with ergot alkaloids - increased vasoconstrictor effect (up to severe ischemia and the development of gangrene).

Reduces the effect of insulin and other hypoglycemic drugs.

Method of administration and dosage

Subcutaneously, intramuscularly, intravenously.

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 at a concentration of 1: 10000. In the absence of an immediate threat to life, intramuscular or subcutaneous administration of 0.3-0.5 mg is preferable, if necessary, repeated administration after 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 at 0.1-0.25 mg with a dilution at a concentration of 1: 10000.

With asystole: intracardiac 0.5 mg (diluted with 10 ml of 0.9% sodium chloride solution or another solution), during resuscitation measures - 0.5-1.0 mg (diluted) intravenously every 3-5 minutes. If the patient is intubated. endotracheal instillation is possible - doses should be 2-2.5 times higher than doses for intravenous administration.

Stopping bleeding: topically in the form of tampons moistened with a solution of the drug.

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

To lengthen the action of local anesthetics: at 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 (bradyarrhythmic form): at a dose of 1 mg in 250 ml of 5% glucose solution intravenously, gradually increasing the infusion rate until the minimum sufficient number of heartbeats is achieved.

As a vasoconstrictor: intravenous drip 1 mcg / min, the rate of administration can be increased to 2-10 mcg / min.

Application in children's practice:

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

Children older than 1 month: intravenously, 10 μg / kg (subsequently, if necessary, every 3-5 minutes, 100 μg / kg is administered (after the administration of at least 2 standard doses, higher doses can be used every 5 minutes - 200 μg / kg) Endotracheal injection can be used.

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

Children with bronchospasm: subcutaneously 10 μg / kg (maximum - up to 0.3 mg), doses, if necessary, repeat every 15 minutes (up to 3-4 times) or every 4 hours.

Overdose

Symptoms: excessive increase in blood pressure, tachycardia, alternating with 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 administration, symptomatic therapy - to lower blood pressure - -adrenergic blockers (phentolamine), in case of arrhythmia - -adrenergic blockers (propranolol).

special instructions

Accidental intravenous administration of epinephrine can cause a sharp increase in blood pressure.

An increase in blood pressure with the introduction of the drug can cause attacks of angina pectoris. Epinephrine can cause constriction of the kidney capillaries, thereby reducing urine output.

When infusing, an instrument with a measuring device should be used to regulate the infusion rate.

Infusion should be carried out into a large (preferably central) vein.

Intracardially is introduced during asystole, if other methods are not available, because there is a risk of developing cardiac tamponade and pneumothorax.

During the treatment period, it is recommended to determine the concentration of potassium ions (K +) in the blood serum, to measure blood pressure, urine output, cardiac output, electrocardiogram, central venous pressure, pulmonary artery pressure and pulmonary capillary wedge pressure.

Exсessive doses in myocardial infarction can increase ischemia by increasing myocardial oxygen demand.

Increases glycemia, and therefore in diabetes mellitus, higher doses of insulin and sulfonylurea derivatives are required.

With endotracheal administration, absorption and final plasma concentration of the drug may be unpredictable.

Administration of epinephrine in shock conditions is not a substitute for transfusion of blood, plasma, blood-substituting fluids and / or saline solutions.

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

There are no strictly controlled studies of the use of epinephrine in pregnant women. A statistically regular relationship was established between the occurrence of malformations and inguinal hernia in children whose mothers used epinephrine during the first trimester or throughout pregnancy; it was also reported in one case about the occurrence of anoxia in the fetus after intravenous administration of epinephrine to the mother.

The use for the correction of low blood pressure during childbirth is not recommended, since it can delay the second stage of labor, when administered in large doses to weaken the contraction of the uterus, it can cause prolonged uterine atony with bleeding.

Can be used in children in cardiac arrest, but use caution.

When discontinuing treatment, the dose should be reduced gradually. sudden discontinuation 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 turned pinkish or brown in color or contains sediment, it should not be injected. The unused portion should be destroyed.

Influence on the ability to drive vehicles and use mechanisms

After using the drug, the doctor must individually, in each specific case, decide on the patient's admission to driving or engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

Solution for injection 1 mg / ml.

Conditions of dispensing from pharmacies

On prescription

Storage conditions

Store at a temperature not exceeding 15 C.

Keep out of the reach of children.

Best before date

3 years. Do not use after the expiration date!