Epipen (epinephrine) solution for injections 0.3 mg/dose 2 ml. №1 tube

Description

Epipen Storage
active substance: adrenaline (epinephrine);

1 ml of solution contains 1 mg of adrenaline; 1 dose (0.3 ml) contains 0.3 mg of adrenaline;

Epipen Excipients: sodium chloride, sodium metabisulfite (E 223), concentrated hydrochloric acid, water for injections.

Epipen Dosage form
Solution for injection.

Main physical and chemical properties: clear solution without visible inclusions.

Pharmacotherapeutic group
Cardiac drugs. Non-glycosidic cardiotonic drugs. Adrenergic and dopaminergic drugs. Epinephrine. ATX code C01C A24.

Pharmacological properties
Pharmacodynamics. Adrenaline is a catecholamine that stimulates the sympathetic nervous system (alpha and beta receptors) and thus increases heart rate, cardiac output and increases coronary circulation.

The action of adrenaline beta receptors on the smooth muscles of the bronchi causes them to relax, which relieves wheezing and reduces shortness of breath.

Adrenaline is rapidly inactivated, most of the dose of adrenaline is excreted as metabolites in the urine.

Pharmacokinetics.

Adrenaline is a natural substance produced by the cerebral part of the adrenal glands in response to exercise or stress. It is rapidly inactivated mainly by two enzymes: catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). A significant amount of these enzymes is found in the liver, which is important but not essential in the breakdown process. Most of the dose of adrenaline is excreted as metabolites in the urine.

The half-life of adrenaline from blood plasma is 2.5 minutes. However, when administered subcutaneously or intramuscularly, local vasoconstriction delays absorption, so the therapeutic effect is asymptomatic and the duration of action is longer than the expected half-life. It is recommended to gently massage the injection site.

In a pharmacokinetic study of 35 healthy volunteers, grouped according to the degree of subcutaneous fat layer of the thigh and distributed by sex, a single injection of 0.3 mg / 0.3 ml into the outer thigh was administered using a pre-filled Epipen pen and a comparison was made in a crossover study with a dose administered using a hand syringe with needles specially adapted for delivery to the muscle layer. The results showed that in female subjects with a thick subcutaneous fat layer (distance from the skin to the muscles at maximum pressure is> 20 mm) there was a slower absorption of adrenaline, which was reflected in the tendency to decrease the concentration of adrenaline in blood plasma during the first ten minutes after administration (see section “Features of application”). However, the total adrenaline exposure from 0 to 30 min (AUC0-30 min) in all groups of subjects who used pre-filled Epipen pens exceeded the exposure after syringe administration. Importantly, the tendency to increase plasma adrenaline levels after administration with a pre-filled Epipen pen compared to manual intramuscular injection in healthy subjects with well-perfused subcutaneous tissue may not necessarily be extrapolated to patients. with a diagnosis of anaphylactic shock, which may be an outflow of blood from the skin to the leg muscles. Therefore, the possibility of narrowing of the blood vessels of the skin during the injection should be considered.

Patient variability and intraindividual variability were quite high in this study, so no reliable conclusions can be drawn.

Indication
Severe allergic reactions (anaphylaxis), for example: allergic reactions to insect bites, food, drugs, contact with other allergens, as well as idiopathic or exercise-induced anaphylaxis.

Contraindication
There are no known absolute contraindications for the use of Epipen in emergency care for allergic reactions.