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Epinephrine is an alpha and beta stimulant. At the cellular level, the effect is due to the activation of adenylate cyclase on the inner surface of the cell membrane, an increase in the level of intracellular cAMP and the entry of Ca2 + into the cell. Increases heart rate and heart rate, shock and minute release, increases conductivity, excitability and automatism of the myocardium. Increases myocardial oxygen demand. It constricts the vessels of the abdominal organs, skin, mucous membranes, and to a lesser extent, skeletal muscles. Increases blood pressure (mainly systolic), in high doses increases round fist. The pressure effect can cause a short-term reflex slowing of the heart rate. Relaxes the smooth muscles of the bronchi. Lowers the tone and motility of the digestive tract. It expands the pupils, helps reduce the production of intraocular fluid and intraocular pressure. It causes hyperglycemia and increases the content of free fatty acids in the plasma.
- Allergic reactions of immediate type (including anaphylactic shock), developing with the use of drugs, serums and other drug allergens, bronchial asthma (relief of an attack);
- hypoglycemia (due to insulin overdose), hypokalemia;
- asystole, cardiac arrest, bleeding (arrest), lengthening the action of local anesthetics;
- AV block III stage (acutely developed);
- open-angle glaucoma.
1 ml of solution contains:
Active substance: epinephrine hydrochloride 1 mg.
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Dosage and Administration
Parenteral: with anaphylactic shock and other allergic reactions, hypoglycemia - s / c, less often - IM or / in slow; for adults - for 0.2–0.75 ml, for children - for 0.1–0.5 ml; Higher doses for adults with s / c administration: single - 1 ml, daily - 5 ml.
With an attack of bronchial asthma in adults - s / to 0.3–0.7 ml.
With cardiac arrest- intracardiac 1 ml.
Locally: to stop bleeding - swabs moistened with a solution of the drug; a few drops are added to the solution of local anesthetics immediately before administration.
Tachycardia, arrhythmias (eliminate beta-blockers), ventricular fibrillation, angina, increased blood pressure, pulmonary edema, anxiety, dizziness, headache, tremor, nausea, increased muscle rigidity and tremor (in patients with parkinsonism).
Hypersensitivity, arterial hypertension, angina pectoris, marked atherosclerosis, cardiac asthma, aneurysm, diabetes mellitus, thyrotoxicosis, pregnancy, angle-closure glaucoma; the state of general anesthesia (caused by ftorotan, cyclopropane, chloroform - due to the risk of arrhythmias).
Antagonists of epinephrine are alpha and beta adrenoreceptor blockers. Reduces the effectiveness of diuretics, insulin, antipsychotics, M- and H-cholostimulants, muscle relaxants. Efficiency increases when combined with M-anticholinergics, MAO inhibitors, ganglioblokatorami, uterine tone stimulants, thyroid preparations, rauwolfia alkaloids. Enhances the effect of aminophylline and thyroid drugs.
For infusion, a device with a measuring device should be used to control the rate of infusion.
Infusions should be carried out in a large (preferably in the central) vein.
Intracardially injected during asystole, if other methods are not available, because there is a risk of cardiac tamponade and pneumothorax.
During the treatment period, it was recommended to determine the concentration of K + in the serum, the measurement of blood pressure, diuresis, IOC, ECG, central venous pressure, pulmonary artery pressure and wedging pressure in the pulmonary capillaries.
Excessive doses in myocardial infarction can increase ischemia by increasing myocardial oxygen demand.
Increases glycemia, and therefore, diabetes requires higher doses of insulin and sulfonylurea derivatives.
With endotracheal administration, absorption and final plasma concentration of the drug may be unpredictable.
Introduction of epinephrine in shock conditions does not replace blood transfusion, plasma, blood-substituting liquids and / or saline solutions.
Epinephrine is not advisable 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 consistent relationship was established between the occurrence of deformities 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 iv administration of the mother epinephrine. Epinephrine should not be used for pregnant women with blood pressure above 130/80 mm Hg. Experiments on animals have shown that when administered in doses 25 times higher than the recommended dose for humans, it causes a teratogenic effect.
When used during lactation, the risk and benefit should be assessed due to the high likelihood of side effects in the baby.
Application for the correction of hypotension during labor is not recommended, as it may delay the second stage of labor; when administered in large doses to weaken the contraction of the uterus, it can cause long-lasting atony of the uterus with bleeding.
Can be used in children with cardiac arrest, but care must be taken, since the dosing schedule requires 2 different concentrations of epinephrine.
When discontinuing treatment, the dose should be reduced gradually, since sudden withdrawal of therapy may lead to severe hypotension.
Easily destroyed by alkalis and oxidizing agents.
If the solution has acquired a pinkish or brown color or contains a precipitate, it cannot be injected. Unused parts should be destroyed.
Symptoms: excessive increase in blood pressure, tachycardia, alternating bradycardia, arrhythmias (including atrial and ventricular fibrillation), coldness and pallor of the skin, vomiting, headache, metabolic acidosis, myocardial infarction, brain cranial hemorrhage (especially in elderly patients) , pulmonary edema, death.
Treatment: stop the introduction, symptomatic therapy - to reduce blood pressure - alpha-blockers (phentolamine), with arrhythmias - beta-blockers (propranolol).
- Brand name: Adrenalin
- Active ingredient: Epinephrine
- Dosage form: Injection
- Manufacturer: Moscow Endocrine Plant
- Country of Origin: Russia
Studies and clinical trials of Epinephrine (Click to expand)
- Variation in epinephrine and cortisol excretion rates associated with behavior in an Australian Aboriginal community
- Enantiomeric separation of d-/l-norepinephrine and -epinephrine by high-performance liquid chromatography with a β-cyclodextrin type chiral stationary phase
- Stereoselective modification of circular dichroism spectra of rat lung β-adrenoceptor protein preparation by enantiomers of epinephrine
- Epinephrine prevents nitric oxide/peroxynitrite induced apoptosis of neuronal cells through β-adrenergic receptor activation
- Epinephrine absorption after different routes of administration in an animal model
- Metabolic effects induced by epinephrine in Rana Balcanica erythrocytes under normoxic and hypoxic conditions
- Identification of and observations on epinephrine and norepinephrine containing cells in the adrenal medulla
- Stability of the intra-epithelial component of the blood-testis barrier in epinephrine-induced testicular degeneration in Syrian hamsters
- Epinephrine potentiation of arachidonate-induced aggregation of cyclooxygenase-deficient platelets
- Effect of epinephrine on fibrinogen receptor exposure by aspirin-treated platelets and platelets from concentrates in response to ADP and thrombin
- Deficient elevation of the cytoplasmic calcium ion concentration by epinephrine in epinephrine-insensitive platelets of patients with myeloproliferative disorders
- Evidence for retrograde degeneration of epinephrine neurons in Alzheimer's disease
- Loss of C1 and C3 epinephrine-synthesizing neurons in the medulla oblongata in parkinson's disease
- The action of epinephrine on the blood vessels of cortisone-treated animals
- Effects of cortisone and epinephrine on hepatic and myocardial glycogen of mice and rats
- Effects of cortisone and epinephrine on the glycogen of skeletal muscles of mice
- Is epinephrine administration by sublingual tablet feasible for the first-aid treatment of anaphylaxis? A proof-of-concept study
- Epinephrine for the treatment of anaphylaxis: do all 40 mg sublingual epinephrine tablet formulations with similar in vitro characteristics have the same bioavailability?
- Sensitive determination of protein based on the fluorescence enhancement effect of terbium (III)–epinephrine–protein–sodium dodecylsulfate system
- Enhanced chemiluminescence of lucigenin with epinephrine in cationic surfactant micelles containing periodate
- Sensitive determination of epinephrine in pharmaceutical preparation by flow injection coupled with chemiluminescence detection and mechanism study
- Effect of the geometry of microfabricated flow reactors on chemiluminescent detection of epinephrine with lucigenin
- Epinephrine-induced MMP expression is different between skeletal fibroblasts and myoblasts
- Resolution of refractory no-reflow with intracoronary epinephrine