Adrenaline

Adrenaline is a stimulant of α- and β-adrenergic receptors.

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Indications Adrenaline

The drug 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), for the elimination of attacks of bronchial asthma and the treatment of the consequences of insulin overdose.

It is prescribed locally for complex treatment together with local anesthetic drugs, as well as to stop bleeding that has occurred.

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Release form

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

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Pharmacodynamics

The drug is an adrenergic stimulant. The effect of the active component epinephrine stimulates α-adrenoreceptors, thereby increasing the amount of intracellular calcium in the smooth muscles. Due to the activation of α1-adrenoreceptors, the activity of phospholipase type C increases (by stimulating the activity of G-protein), as well as the formation of inositol triphosphate with diacylglycerol. As a result, calcium is released from intracellular depots (cisterns of the sarcoplasmic reticulum). Due to the activation of α2-adrenoreceptors, calcium channels are released and the rate of calcium entry into cells increases.

By stimulating the activity of β-adrenoreceptors, G-protein-mediated activation of adenylate cyclase function occurs, as well as increased cAMP production. This process is a catalyst for the occurrence of reactions from various target organs.

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

It has an intensive effect on the cardiovascular system - it increases the force and frequency of heart contractions, and in addition, its minute and stroke volumes. It improves the processes of AV conduction, as well as automatism. It increases the oxygen demand of the myocardium. In addition, it constricts the vessels of the peritoneum, mucous membranes and skin, as well as (less significantly) skeletal muscles. It increases the level of blood pressure (mainly systolic), and in addition, it significantly increases the OPSS index. Due to the pressor effect, a reflex short-term slowdown in heart rate is possible.

Epinephrine relaxes smooth muscles in the bronchi, reduces motility and tone of the gastrointestinal tract, and also reduces intraocular pressure and promotes pupil dilation. It can cause hyperglycemia and increases free fatty acid concentrations in plasma.

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Pharmacokinetics

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

The active component passes through the placental barrier, as well as the BBB. In addition, it is able to penetrate into breast milk.

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Dosing and administration

The drug should be administered parenterally. In case of anaphylaxis and other allergic reactions, as well as hypoglycemia, it is administered subcutaneously (rarely intramuscularly or intravenously slowly). For adults, the dosage is 0.2-0.75 ml, and for children - 0.1-0.5 ml. The maximum subcutaneous dosage for adults is 1 ml (single) and 5 ml (daily).

In case of a bronchoasthmatic attack, adults should be administered 0.3-0.7 ml of the solution subcutaneously. In case of cardiac arrest, the medicine is administered intracardially in a dosage of 1 ml.

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Use Adrenaline during pregnancy

Since epinephrine can pass through the placenta and into breast milk, Adrenaline is not recommended for use during pregnancy or lactation. Use is permitted only in cases where the potential benefit to the mother is higher than the risk of developing negative consequences for the child or fetus.

Contraindications

Among the contraindications:

• obstructive form of hypertrophic cardiomyopathy;
• high blood pressure;
• pheochromocytoma;
• tachyarrhythmia;
• ventricular fibrillation;
• IHD;
• individual intolerance to the active component of the drug – epinephrine.

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Side effects Adrenaline

After using the medicine, the following side effects may develop:

• cardiovascular system: tachycardia or bradycardia, as well as angina pectoris, problems with heartbeat, decrease or increase in blood pressure. In case of use in high dosage, ventricular arrhythmia may develop. Occasionally, pain in the sternum, as well as arrhythmia, occurs;
• organs of the nervous system: headaches and dizziness, anxiety, fatigue, nervousness, and tremor. In addition, psychoneurotic disorders (disorientation, psychomotor agitation, memory problems, manifestations of panic or aggression, disorders similar to schizophrenia, and a feeling of paranoia), sleep problems and muscle twitching;
• digestive system organs: vomiting with nausea;
• urinary system organs: painful urination with difficulty may be observed occasionally (in case of prostate hyperplasia);
• allergies: bronchospasms, Quincke's edema, skin rashes and erythema multiforme;
• others: increased sweating, development of hypokalemia. Local reactions include burning and pain at the site of intramuscular injection.

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Interactions with other drugs

Agents that block the action of α- and β-adrenergic receptors are antagonists of the active component of epinephrine.

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

As a result of the combination with cardiac glycosides, and also tricyclics, quinidine, as well as dopamine, cocaine and drugs used in inhalation anesthesia (such as enflurane, isoflurane, chloroform, as well as halothane and methoxyflurane), the risk of arrhythmia increases. Therefore, it is not recommended to take them simultaneously, except in cases of acute need.

When combined with other sympathomimetics, the severity of side effects from the cardiovascular system increases.

In combination with antihypertensive drugs (including diuretics), their medicinal effectiveness is weakened.

Combined use with ergot alkaloids increases the vasoconstrictive effect of the drug (may lead to the development of gangrene, as well as severe ischemia).

MAO inhibitors, n-anticholinergics, m-anticholinergics, and in addition to this, thyroid hormone medications, octadine and reserpine enhance the effects of epinephrine.

Epinephrine weakens the effects of antidiabetic drugs (including insulin), cholinomimetic drugs, neuroleptics, narcotic analgesics, as well as muscle relaxants and sleeping pills.

Concomitant use with drugs that prolong the QT interval (including cisapride, astemizole and terfenadine) further increases its length.

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Storage conditions

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

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Shelf life

Adrenaline is permitted to be used for 36 months from the date of manufacture of the drug.

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