Adrenaline storage temperature. adrenomimetic agents. epinephrine hydrochloride. Description of the dosage form


Adrenaline is a drug that has a pronounced effect on the cardiovascular system and increases blood pressure.

Composition, release form and analogues

The drug is produced in the form of a solution of Adrenaline hydrochloride and Adrenaline hydrotartrate. The first is made from a white crystalline powder with a slight pinkish tint, which changes under the influence of oxygen and light. In medicine, a 0.1% solution for injection is used. It is prepared with the addition of 0.01 N. hydrochloric acid solution. It is preserved with sodium metabisulphite and chlorobutanol. Adrenaline hydrochloride solution is clear and colorless. It is prepared under aseptic conditions. It is important to note that it cannot be heated.

A solution of adrenaline hydrotartrate is made from a white crystalline powder with a grayish tint, which tends to change under the influence of oxygen and light. It is easily soluble in water and slightly soluble in alcohol. Sterilization takes place at a temperature of +100 °C for 15 minutes.

Adrenaline hydrochloride is available in the form of a 0.01% solution, and Adrenaline hydrotartrate in the form of a 0.18% solution of 1 ml in neutral glass ampoules, as well as in hermetically sealed orange glass bottles of 30 ml - for local use.

1 ml solution for injection contains 1 mg adrenaline hydrochloride. One package contains 5 ampoules of 1 ml or 1 vial (30 ml).

Among the analogues of this drug, the following can be distinguished:

  • Adrenaline hydrochloride-Vial;
  • epinephrine tartrate;
  • epinephrine;
  • epinephrine hydrotartrate.

Pharmacological action of adrenaline

It should be noted that the action of Adrenaline hydrochloride does not differ from the effect of Adrenaline hydrotartrate. However, the difference in relative molecular weight allows the use of the latter in large doses.

When the drug is introduced into the body, an effect on alpha- and beta-adrenergic receptors occurs, which is in many ways similar to the effect of excitation of sympathetic nerve fibers. Adrenaline causes vasoconstriction abdominal cavity, mucous membranes and skin, blood vessels skeletal muscles it narrows to a lesser extent. The drug causes an increase blood pressure.

In addition, the stimulation of cardiac adrenergic receptors, which leads to the use of Adrenaline, contributes to the strengthening and acceleration of heart contractions. This, together with an increase in blood pressure, provokes the excitation of the center of the vagus nerves, which have an inhibitory effect on the heart muscle. As a result, these processes can lead to a slowdown in cardiac activity and arrhythmias, especially under conditions of hypoxia.

Adrenaline relaxes the muscles of the intestines and bronchi, and also dilates the pupils due to the contraction of the radial muscles of the iris, which have adrenergic innervation. The drug increases the level of glucose in the blood and improves tissue metabolism. It also has a positive effect on functional ability skeletal muscle especially when tired.

It is known that adrenaline does not have a pronounced effect on the central nervous system, but in rare cases headaches, anxiety and irritability can be observed.

Indications for the use of Adrenaline

According to the instructions for Adrenaline, the drug should be used in the following cases:

  • Arterial hypotension unresponsive to adequate volumes of replacement fluids (including shock, trauma, surgery to open heart, chronic heart failure, bacteremia, renal failure, overdose medicines);
  • Bronchial asthma and bronchospasm during anesthesia;
  • Bleeding from superficial vessels of the skin and mucous membranes, including gums;
  • asystole;
  • Stop bleeding of various kinds;
  • Allergic reactions of the immediate type that develop when using serums, medicines, blood transfusions, insect bites, consumption of specific food products or due to the introduction of other allergens. Allergic reactions include urticaria, anaphylactic and angioedema;
  • Hypoglycemia caused by an overdose of insulin;
  • Treatment of priapism.

The use of Adrenaline is also indicated for open-angle glaucoma, as well as in cases of eye surgery (for the treatment of swelling of the conjunctiva, in order to dilate the pupil, with intraocular hypertension). The drug is often used when it is necessary to prolong the action of local anesthetics.

Contraindications

According to the instructions for Adrenaline, the drug is contraindicated in:

  • Severe atherosclerosis;
  • Hypertension;
  • bleeding;
  • pregnancy;
  • lactation;
  • Individual intolerance.

Adrenaline is also contraindicated during anesthesia with cyclopropane, halothane and chloroform.

How to use Adrenaline

Adrenaline is injected subcutaneously and intramuscularly (in rare cases - intravenously) at 0.3, 0.5 or 0.75 ml of a solution (0.1%). In ventricular fibrillation, the drug is administered intracardiac, and in cases of glaucoma, a solution (1-2%) in drops is used.

Side effects

According to the instructions for Adrenaline, side effects drugs include:

  • Significant increase in blood pressure;
  • Arrhythmia;
  • Tachycardia;
  • Pain in the region of the heart;
  • Ventricular arrhythmias (at high doses);
  • Headache;
  • dizziness;
  • Nausea and vomiting;
  • Psychoneurotic disorders (disorientation, paranoia, panic behavior, etc.);
  • allergic reactions ( skin rash, bronchospasm, etc.).

Adrenaline drug interactions

Simultaneous use of adrenaline with sleeping pills and narcotic analgesics may weaken the effect of the latter. The combination with cardiac glycosides, antidepressants, quinidine is fraught with the development of arrhythmia, with MAO inhibitors - increased blood pressure, vomiting, headaches, with phenytoin - bradycardia.

Storage conditions

Adrenaline should be stored in a cool dry place, protected from sun rays. The shelf life of the drug is 2 years.

The action of adrenaline when administered to the body is associated with the effect on a- and b-adrenergic receptors and largely coincides with the effects of excitation of sympathetic nerve fibers. 0n causes vasoconstriction of the abdominal organs, skin and mucous membranes; narrows the vessels of the skeletal muscles to a lesser extent. Arterial pressure rises. However, the pressor effect of adrenaline due to the excitation of b-adrenergic receptors is less constant than the effect of norepinephrine. Changes in cardiac activity are complex: by stimulating the adrenoreceptors of the heart, adrenaline contributes to a significant increase and increase in heart rate; at the same time, however, due to reflex changes due to an increase in blood pressure, the center of the vagus nerves is excited, which has an inhibitory effect on the heart; as a result, cardiac activity may slow down. Cardiac arrhythmias may occur, especially in conditions of hypoxia. Adrenaline causes relaxation of the muscles of the bronchi and intestines, dilation of the pupils (due to contraction of the radial muscles of the iris, which have adrenergic innervation). Under the influence of adrenaline, there is an increase in blood glucose and an increase in tissue metabolism. Adrenaline improves the functional capacity of skeletal muscles (especially during fatigue); its action is similar in this respect to the effect of excitation of sympathetic nerve fibers (a phenomenon discovered by L. A. Orbeli and A. G. Ginetsinsky). Adrenaline in therapeutic doses usually does not have a pronounced effect on the central nervous system. However, there may be anxiety, headaches, tremors. In patients with parkinsonism, under the influence of adrenaline, muscle rigidity and tremor increase.

Indications for use:

Acute decrease in blood pressure (collapse), seizures bronchial asthma, hypoglycemia (decrease in blood sugar) due to an overdose of insulin, acute drug allergic reactions, glaucoma (increased intraocular pressure), ventricular fibrillation (chaotic contractions of the heart muscle), etc .; as a vasoconstrictor in otorhinolaryngological (for the treatment of diseases of the ear, throat, nose) and ophthalmic (eye) practice.

Mode of application:

Subcutaneously and intramuscularly, sometimes intravenously 0.3-0.5-0.75 ml of a 0.1% solution. With ventricular fibrillation intracardiac; with glaucoma - 1-2% solution in drops.

Side effects:

Tachycardia (palpitations), heart rhythm disturbance, increased blood pressure; at coronary disease heart attacks of stenocardia are possible.

Contraindications:

Arterial hypertension (persistent rise in blood pressure), severe atherosclerosis, diabetes mellitus, thyrotoxicosis (disease thyroid gland), pregnancy. Adrenaline cannot be used during anesthesia with halothane, cyclopropane.

Release form:

0.1% solution in ampoules of 1 ml in a package of 6 pieces; in vials of 30 ml.

Storage conditions:

List B. In a cool, dark place. Shelf life: 2 years Suprarenin, Suprarenalin, Tonogen.

Compound:

White or slightly pinkish crystalline powder. Changes under the influence of light and atmospheric oxygen. For medical use is produced in the form of a 0.1% solution (Solutio Adrenalini hudrochloridi 0.1%). The solution is prepared with the addition of 0.01 N. hydrochloric acid solution. Preserved with chlorobutanol and sodium metabisulphite; pH 3.0-3.5. The solution is colorless, transparent. Solutions can not be heated, they are prepared under aseptic conditions.

Attention! Before using the drug Adrenaline hydrochloride, you should consult your doctor. This instruction provided in free translation and is intended for informational purposes only. For more information, please refer to the manufacturer's annotation.

Adrenaline belongs to the group of hormonal drugs and is an analogue of the main hormone synthesized by the adrenal medulla - paired endocrine glands found in humans and vertebrates.

Release form and composition

The active substance of the drug is epinephrine (Epinephrinum).

Pharmacological group of adrenaline - hypertensive drugs, adreno- and sympathomimetics (alpha-, beta-).

According to the instructions, Adrenaline hydrochloride is available in two forms:

  • Injection;
  • Solution for external use.

Pharmacological action of adrenaline

Being essentially a neurotransmitter, adrenaline, when introduced into the body, transmits electrical impulses from nerve cell through the synaptic space between neurons, as well as from neurons to muscles. The action of this biologically active chemical associated with the effect on alpha- and beta-adrenergic receptors and largely coincides with the effect of excitation of sympathetic fibers nervous system- parts of the autonomic (otherwise autonomous) nervous system, ganglions which (ganglia) are located at considerable distances from the innervated organs.

According to the instructions, Adrenaline provokes vasoconstriction of the organs located in the abdominal cavity, blood vessels of the skin and mucous membranes. To a lesser extent, there is a narrowing of the vessels of the skeletal muscles. At the same time, blood pressure indicators increase, in addition, the vessels located in the brain expand.

The pressor effect of adrenaline, however, is less pronounced than the effect of the use of norepinephrine, which is due to the excitation of not only α 1 and α 2 -adrenergic receptors, but also β 2 -adrenergic receptors of the vessels.

Against the background of the use of adrenaline hydrochloride, the following are noted:

  • Strengthening and acceleration of contractions of the heart muscle;
  • Facilitation of the processes of atrioventricular (atrioventricular) conduction;
  • Increased automatism of the heart muscle, provoking the development of arrhythmias;
  • Excitation of the X-pair center resulting from an increase in blood pressure cranial nerves(the so-called vagus nerves), which have an inhibitory effect on the activity of the heart, provoking the occurrence of transient reflex bradycardia.

Also, under the influence of Adrenaline, the muscles of the bronchi and intestines relax, the pupils dilate. And since this substance serves as a catalyst for all processes occurring in the body metabolic processes, its application:

  • Increases the level of glucose in the blood;
  • Increases metabolism in tissues;
  • Enhances glucogenesis and glycogenesis;
  • Slows down the processes of glycogen synthesis in skeletal muscles;
  • Promotes increased capture and utilization of glucose in tissues;
  • Increases the level of activity of glycolytic enzymes;
  • It has a stimulating effect on "trophic" sympathetic fibers;
  • Increases the functionality of skeletal muscles;
  • Stimulates the activity of the central nervous system;
  • Increases the level of wakefulness, mental energy and activity.

In addition, Adrenaline hydrochloride is able to have a pronounced anti-allergic and anti-inflammatory effect on the body.

A characteristic feature of Adrenaline is that its use provides an instant derivative effect. Since the drug is an ideal stimulant of cardiac activity, it is indispensable in ophthalmic practice and during surgical operations.

Indications for the use of Adrenaline

The use of Adrenaline, according to the instructions, is advisable in the following situations:

  • When sharp decline blood pressure indicators (with collapse);
  • To relieve symptoms of an attack of bronchial asthma;
  • When a patient develops acute allergic reactions against the background of taking a particular drug;
  • With hypoglycemia (low blood sugar levels);
  • With asystole (a condition that is characterized by the cessation of the activity of the heart with the disappearance of bioelectrical activity);
  • With an overdose of insulin;
  • In open-angle glaucoma (increased intraocular pressure);
  • When chaotic contractions of the heart muscle occur (ventricular fibrillation);
  • For the treatment of otolaryngological diseases as a vasoconstrictor drug;
  • For the treatment of ophthalmic diseases (during surgical operations on the eyes, the purpose of which is to eliminate swelling of the conjunctiva, for the treatment of intraocular hypertension, stop bleeding, etc.);
  • With anaphylactic shock, which has developed as a result of bites of insects and animals;
  • With intense bleeding;
  • During surgical operations.

Because the this drug has a short-term effect, to prolong the time of its action Adrenaline is often combined with a solution of novocaine, dicaine or other anesthetic drugs.

Contraindications

Contraindications to the appointment of adrenaline are:

  • Simultaneous use with cyclopropane, halothane and chloroform (since such a combination can provoke severe arrhythmia);
  • Simultaneous use with oxytocin and antihistamines;
  • Aneurysm;
  • Hypertonic disease;
  • Endocrine disorders (in particular diabetes mellitus);
  • Glaucoma;
  • Atherosclerotic vascular lesions;
  • Hyperthyroidism;
  • The period of pregnancy and lactation.

Method of application and dosage

Since Adrenaline comes in the form of a solution, it can be used in several ways: lubricate skin administered intravenously, intramuscularly and under the skin.

In cases of bleeding, it is used as an external agent, applied to a bandage or swab.

The daily dose of Adrenaline should not exceed 5 ml, and a single injection - 1 ml. In a muscle, vein or under the skin, the agent is injected very slowly and with caution.

In cases where the medicine is required by the child, the dose is calculated based on individual features his body, age and general condition.

In cases where Adrenaline does not have the expected effect, and there is no improvement in the patient's condition, it is recommended to use similar preparations stimulating action, which have a less pronounced toxic effect.

Side effects of adrenaline

It should be remembered that an overdose of Andernaline or its incorrect administration can cause the patient to develop severe arrhythmia and transient reflex bradycardia (a type of violation sinus rhythm, which is accompanied by a decrease in the number of contractions of the heart muscle to 30-50 beats per minute).

In addition, high concentrations of the substance can enhance the processes of protein catabolism.

Analogues

Currently, there are many analogues of Adrenaline. Among them: Stiptirenal, Epinephrine, Adrenin, Paranephrine and many others.

Release form: ampoules of 1 ml of a 0.1% solution, in a package of 6 pieces, in vials of 30 ml of a 0.1% solution (for external use).

Administered subcutaneously, intramuscularly, with extreme severe conditions - intravenously, with ventricular fibrillation and cardiac arrest - intracardiac.

Single doses of 0.1% adrenaline solution for injection are as follows: children under the age of 6 months - 0.1 ml, from 6 to 12 months - 0.15 ml, from 1 year to 3 years 0.2 - 0.25 ml, from 3 to 7 years - 0.3 - 0.5 ml, from 7 to 14 years - 0.6 - 1 ml. The action of the injected adrenaline is characterized by a short duration, since it is quickly destroyed in the body.

At sudden stop heart (for example, reflex, caused by irritation vagus nerve) a 0.1% solution of adrenaline hydrochloride (0.05 ml per one year of a child's life) is injected into the heart cavity of a sick child in combination with the same amount of a 0.1% solution of atropine, with the addition of a 10% solution of calcium chloride - 0.3 - 0.5 ml for one year of life (E. K. Tsybulkin, 1977).

In severe asthma attacks, the appointment of adrenaline is ineffective. Moreover, he provides bad influence on the drainage and ventilation function of the bronchi.

Side effects: tachycardia, cardiac arrhythmias, increased blood pressure.

Contraindications: arterial hypertension, diabetes mellitus, thyrotoxicosis. It is unacceptable to use adrenaline during anesthesia with halothane, cyclopropane, chloroform.

Rp.: Sol. Adrenalini hydrochloridi 0.1% 1 ml
D.t. d. N. 6 in amp.
S. 0.5 ml under the skin during an asthma attack in a 7-year-old child.

« Drug therapy in Pediatrics”, S.Sh. Shamsiev

Alpha, beta adrenomimetic

A drug: ADRENALINE HYDROCHLORIDE SOLUTION 0.1% (ADRENALINE HYDROCHLORIDE RASTVOR 0/1%)

Active ingredient: epinephrine
ATX code: C01CA24
KFG: Alpha, beta adrenomimetic
Reg. number: 70/151/11
Date of registration: 03/17/70
The owner of the reg. Award: ELLARA MC (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

1 ml - ampoules.
30 ml - dark glass bottle.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
The provided scientific information is general and cannot be used to make a decision on the possibility of using a particular medicinal product.

PHARMACHOLOGIC EFFECT

Adrenomimetic, has a direct stimulating effect on? - and? -adrenergic receptors.

Under the action of epinephrine (adrenaline), due to stimulation of ?-adrenergic receptors, an increase in the content of intracellular calcium in smooth muscles occurs. Activation? 1-adrenergic receptors increases the activity of phospholipase C (through G-protein stimulation) and the formation of inositol triphosphate and diacylglycerol. This promotes the release of calcium from the depot of the sarcoplasmic reticulum. Activation? 2-adrenergic receptors leads to the opening calcium channels and increase calcium entry into cells.

Stimulation of ?-adrenergic receptors causes G-protein-mediated activation of adenylate cyclase and an increase in cAMP production. This process is a trigger mechanism for the development of reactions from various target organs. As a result of stimulation? 1-adrenergic receptors in the tissues of the heart is an increase in intracellular calcium. On stimulation? 2-adrenergic receptors, there is a decrease in free intracellular calcium in smooth muscles, due, on the one hand, to an increase in its transport from the cell, and on the other hand, to its accumulation in the depot of the sarcoplasmic reticulum.

It has a pronounced effect on the cardiovascular system. Increases the frequency and strength of heart contractions, stroke and minute volume of the heart. Improves AV conduction, increases automatism. Increases myocardial oxygen demand. Causes vasoconstriction of the abdominal organs, skin, mucous membranes, to a lesser extent - skeletal muscles. Increases blood pressure (mainly systolic), in high doses increases OPSS. The pressor effect can cause a short-term reflex slowing of the heart rate.

Epinephrine (adrenaline) relaxes the smooth muscles of the bronchi, lowers the tone and motility of the gastrointestinal tract, dilates the pupils, and helps to lower intraocular pressure. Causes hyperglycemia and increases plasma free fatty acids.

PHARMACOKINETICS

Metabolized with the participation of MAO and COMT in the liver, kidneys, gastrointestinal tract. T 1/2 is a few minutes. Excreted by the kidneys.

Penetrates through the placental barrier, does not penetrate the BBB.

It is allocated with breast milk.

INDICATIONS

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.

Bronchial asthma (stopping an attack), bronchospasm during anesthesia.

Asystole (including against the background of an acutely developed AV blockade of the III degree).

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

Arterial hypotension unresponsive to adequate volumes of replacement fluids (including shock, trauma, bacteremia, open heart surgery, kidney failure, chronic heart failure, drug overdose).

The need to prolong the action of local anesthetics.

Hypoglycemia (due to an overdose of insulin).

Open-angle glaucoma, with surgical operations on the eyes - swelling of the conjunctiva (treatment), to dilate the pupil, intraocular hypertension.

To stop bleeding.

Treatment of priapism.

DOSING MODE

Individual. Enter s / c, less often - in / m or / in (slowly). Depending on the clinical situation, a single dose for adults can range from 200 mcg to 1 mg; for children - 100-500 mcg. The solution for injection can be used as eye drops.

Topically used to stop bleeding - use tampons moistened with a solution of epinephrine.

SIDE EFFECT

From the side of cardio-vascular system: angina pectoris, bradycardia or tachycardia, palpitations, increase or decrease in blood pressure; when used in high doses - ventricular arrhythmias; rarely - arrhythmia, chest pain.

From the nervous system: headache, anxiety state, tremor, dizziness, nervousness, fatigue, psychoneurotic disorders (psychomotor agitation, disorientation, memory impairment, aggressive or panic behavior, schizophrenia-like disorders, paranoia), sleep disturbance, muscle twitching.

From the side digestive system: nausea, vomiting.

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

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

Others: hypokalemia, increased sweating; local reactions- pain or burning at the injection site.

CONTRAINDICATIONS

Hypertrophic obstructive cardiomyopathy, pheochromocytoma, arterial hypertension, tachyarrhythmia, ischemic heart disease, ventricular fibrillation, pregnancy, lactation, hypersensitivity to epinephrine.

PREGNANCY AND LACTATION

Epinephrine (adrenaline) crosses the placental barrier and is excreted in breast milk.

Adequate and strictly controlled clinical research The safety of epinephrine has not been established. Use during pregnancy and lactation is possible only if the expected benefit of therapy for the mother outweighs the potential risk to the fetus or child.

SPECIAL INSTRUCTIONS

Use with caution in metabolic acidosis, hypercapnia, hypoxia, atrial fibrillation, ventricular arrhythmias, pulmonary hypertension, hypovolemia, myocardial infarction, non-allergic shock (including cardiogenic, traumatic, hemorrhagic), with thyrotoxicosis, occlusive vascular diseases (including a history of arterial embolism, atherosclerosis, Buerger's disease, cold injury, diabetic endarteritis, Raynaud's disease), cerebral atherosclerosis, angle-closure glaucoma, diabetes, Parkinson's disease, convulsive syndrome, prostatic hypertrophy; simultaneously with inhalation drugs for anesthesia (halothane, cyclopropane, chloroform), in elderly patients, in children.

Epinephrine should not be administered intra-arterially, since severe peripheral vasoconstriction can lead to the development of gangrene.

Epinephrine can be used intracoronary in cardiac arrest.

With arrhythmias caused by epinephrine, beta-blockers are prescribed.

DRUG INTERACTIONS

Antagonists of epinephrine are blockers of?- and?-adrenergic receptors.

Non-selective beta-blockers potentiate the pressor effect of epinephrine.

When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, inhalation anesthesia (chloroform, enflurane, halothane, isoflurane, methoxyflurane), cocaine increases the risk of developing arrhythmias (simultaneous use is not recommended, except in cases of emergency); with other sympathomimetic agents - increased severity side effects from the cardiovascular system; with antihypertensive drugs (including diuretics) - a decrease in their effectiveness; with ergot alkaloids - an increase in the vasoconstrictor effect (up to severe ischemia and the development of gangrene).

MAO inhibitors, m-anticholinergics, ganglionic blockers, thyroid hormone preparations, reserpine, octadine potentiate the effects of epinephrine.

Epinephrine reduces the effects of hypoglycemic agents (including insulin), neuroleptics, cholinomimetics, muscle relaxants, opioid analgesics, hypnotics.

At simultaneous application with drugs that prolong the QT interval (including astemizole, cisapride, terfenadine), there is an increase in the duration of the QT interval.