Adrenalin

Adrenaline is a stimulator of α-, as well as β-adrenoreceptors.

[1]

Indications Adrenalin

The medicine is indicated for the elimination of anaphylaxis and laryngeal edema due to allergies (as well as other allergic reactions with an immediate type of development), to eliminate attacks of bronchial asthma and to treat the consequences of an insulin overdose.

Locally appointed in a complex treatment with local anesthetic drugs, as well as to stop the bleeding.

[2], [3], [4], [5]

Release form

It is available as an injection in ampoules (1 ml) or for local use. One package contains 5 ampoules with a volume of 1 ml or 1 bottle with a volume of 30 ml.

[6], [7]

Pharmacodynamics

The drug is an adrenostimulator. The effect of the active component of epinephrine stimulates α-adrenoreceptors, thereby increasing the amount of intracellular calcium present in the smooth muscle. Due to the activation of α1-adrenoreceptor activity, the activity of phospholipase type C (through stimulation of G protein activity) also increases, as well as the formation of inositol triphosphate with diacylglycerol. As a result, calcium is released from the intracellular stores (sarcoplasmic reticulum cisterns). Due to the activation of the action of α2-adrenoreceptors, calcium channels are released and the rate of calcium entry into the cells is increased.

By stimulating the activity of β-adrenergic receptors, the activation of the adenylate cyclase function, as well as the enhancement of cAMP production, occurs due to the action of G-protein. This process is a catalyst for the occurrence of reactions from a variety of target organs.

Stimulation of the activity of β1-adrenergic receptors inside the cardiac tissues allows to increase the level of intracellular calcium, and stimulation of the activity of β2-adrenoreceptors reduces the level of free matter inside the smooth muscles. On the one hand, this is due to an increase in its excretion from the cell, while on the other hand, its concentration in the intracellular stores (cisterns of the sarcoplasmic reticulum).

Intensively affects the cardiovascular system - increases strength with the frequency of cardiac contractions, and besides this, it's minute with shock volumes. It improves AV-conduction processes, as well as automatism. Strengthens the need for oxygen in the myocardium. In addition, it narrows the vessels of the peritoneum, mucous membranes and skin, and (less significantly) skeletal muscles. Increases the level of blood pressure (mainly systolic), but also significantly increases the OPSS. Due to pressor impact, a short reflex slowing of the heart rate is possible.

Epinephrine allows you to relax the smooth muscles in the bronchi, reduces the motor and tone of the gastrointestinal tract, and besides it decreases the intraocular pressure and promotes the dilatation of the pupils. It can cause the development of hyperglycemia, and also increases the concentration of free fatty acids inside the plasma.

[8], [9], [10], [11]

Pharmacokinetics

Metabolism of the active substance occurs in the kidneys, liver, and gastrointestinal tract, with the participation of COMT with MAO. Half-life lasts only a few minutes. Excretion occurs through the kidneys.

The active component passes through the barrier of the placenta, and also through the BBB. In addition, it is able to penetrate into breast milk.

[12]

Dosing and administration

You need to administer the medicine parenterally. In the case of anaphylaxis and other allergic reactions, as well as hypoglycemia - is administered subcutaneously (occasionally intramuscularly or intravenously slowly). For adults, the dosage is 0.2-0.75 ml, and for children 0.1-0.5 ml. Maximum dosage subcutaneously for adults 1 ml (single) and 5 ml (daily).

In the case of bronchial asthma, adults need to inject subcutaneously 0.3-0.7 ml of the solution. In case of cardiac arrest, the drug is administered intracardiac at a dosage of 1 ml.

[18], [19], [20], [21], [22]

Use Adrenalin during pregnancy

Since epinephrine is able to pass through the placenta and into the mother's milk, Adrenaline is not recommended for use in pregnancy or lactation. The use is permitted only in cases where the possible benefit to the mother is higher than the risk of developing negative consequences for the child or the fetus.

Contraindications

Among the contraindications:

• obstructive form of hypertrophic cardiomyopathy;
• elevated blood pressure;
• pheochromocytoma;
• tachyarrhythmia;
• ventricular fibrillation;
• IHD;
• individual intolerance of the active component of drugs - epinephrine.

[13], [14], [15]

Side effects Adrenalin

After using the medicine, such adverse reactions can develop:

• organs of the cardiovascular system: tachycardia or bradycardia, as well as angina, problems with palpitation, a decrease or increase in blood pressure. If used in a large dosage, ventricular arrhythmia may develop. Occasionally there are pain in the sternum, as well as arrhythmia;
• organs of the National Assembly: headaches and dizziness, a sense of anxiety, a sense of fatigue, nervousness, and tremors. In addition, psychoneurotic disorders (disoriented state, psychomotor agitation, memory problems, panic or aggression, schizophrenia-like disorders, and paranoia), sleep problems and muscle twitching;
• organs of the digestive system: vomiting with nausea;
• organs of the urinary system: single can be observed painful with difficulty urination (in case of prostate hyperplasia);
• allergies: bronchial spasms, Quincke edema, skin rashes and erythema multiforme;
• others: increased sweating, development of hypokalemia. Among the local reactions - burning and pain at the site of intramuscular injection.

[16], [17]

Interactions with other drugs

The agents blocking the action of α-, as well as β-adrenoreceptors are antagonists of the active component of epinephrine.

Non-selective β-blockers increase the pressor effect of epinephrine.

As a result of the connection with cardiac glycosides, and in addition tricyclics, quinidine, and also dopamine, cocaine and drugs used in inhalation anesthesia (such as enflurane, isoflurane, chloroform, and halothane and methoxyflurane), the risk of arrhythmia increases. Therefore, taking them at the same time is not recommended, exceptions are only cases of acute necessity.

When combined with other sympathomimetics, the severity of adverse reactions from the organs of the cardiovascular system increases.

In combination with antihypertensive drugs (among them also diuretics) - their drug efficacy is weakened.

Combined therapy with ergot alkaloids increases the vasoconstrictive effect of drugs (can go to the development of gangrene, as well as severe ischemia).

MAO inhibitors, n-cholinolytics, m-holinoblokatory, and in addition to this drug hormones thyroid, octadine and reserpine increase the effect of epinephrine.

Epinephrine weakens the effect of antidiabetic drugs (among them insulin), cholinomimetic drugs, neuroleptics, narcotic analgesics, as well as muscle relaxants and hypnotics.

A combination with medications that extend the QT interval (among such cisapride, astemizole and terfenadine), further increases its length.

[23], [24], [25]

Storage conditions

The medicine is contained in standard conditions for medicines - a dark dry place. Temperature regime - no more than 15 ° C.

[26], [27]

Shelf life

Adrenaline is allowed to be used for 36 months from the date of manufacture of the medicine.

[28], [29], [30]