Ephedrine (Ephedrinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Adreno- and sympathomimetics (alpha-, beta-)

Included in the formulation
  • Ephedrine
    solution w / m in / in d / infusion PC 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Ephedrine hydrochloride injection 5%
    solution inwards 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • АТХ:

    R.03.C.A.02   Ephedrine

    Pharmacodynamics:

    Sympathomimetic (adrenomimetic of indirect action), alkaloid, obtained from various species of ephedra (Ephedra L.) family Ephedra (Ephedraceae). Ephedrine, contained in plants, is a levorotatory isomer. The racemate was synthesized, inferior to the levorotatory isomer.

    After the administration of ephedrine, α- and β-adrenergic receptors are excited: acting on varicose thickening of efferent adrenergic fibers, ephedrine promotes the release of the mediator of noradrenaline into the synaptic cleft. In addition, it has a weak stimulating effect directly on adrenoreceptors.

    It stimulates the activity of the heart (increases the frequency and strength of contractions), facilitates atrioventricular conductivity, increases blood pressure, causes bronchodilator effect, suppresses intestinal peristalsis, dilates the pupil (without affecting accommodation and intraocular pressure), improves skeletal muscle tone, causes hyperglycemia.

    Unlike epinephrine, the effect of ephedrine develops slowly, but lasts longer.With the repeated administration of ephedrine with a small interval (10-30 min), its pressor action rapidly decreases - tachyphylaxis (rapid addiction) occurs, associated with a progressive decrease in norepinephrine stores in varicose thickenings.

    Ephedrine stimulates the central nervous system, by psycho-stimulating action is close to phenamine.

    It inhibits the activity of MAO and catechol-O-methyltransferase.

    Pharmacokinetics:

    Absorption is good. Biotransformation in the liver (slightly). The half-life is 3-6 h (shortening with urine acidification). Elimination by the kidneys, mainly in unchanged form (strengthening with acidification of urine).

    Indications:

    Arterial hypotension in surgical operations (especially with spinal anesthesia), trauma, blood loss, infectious diseases.

    Bronchial asthma and other obstructive airway diseases, vasomotor and allergic rhinitis, sinusitis (for constriction of the vessels of the nasal mucosa), serum sickness, urticaria and other allergic conditions.

    Narcolepsy, enuresis (as a result of the stimulating effect on the central nervous system, sleep becomes less deep, it facilitates spillage when urge to urinate), myasthenia gravis.

    In ophthalmic practice: to expand the pupil with a diagnostic purpose.

    ICD-10

    V.F90-F98.F98.0   Enuresis of inorganic nature

    VI.G70-G73.G70.2   Congenital or acquired myasthenia gravis

    IX.I95-I99.I95   Hypotension

    X.J30-J39.J30.3   Other allergic rhinitis

    X.J30-J39.J30.1   Allergic rhinitis caused by pollen of plants

    X.J30-J39.J30.0   Vasomotor rhinitis

    X.J30-J39.J32   Chronic Sinusitis

    X.J00-J06.J01   Acute Sinusitis

    X.J40-J47.J44   Other chronic obstructive pulmonary disease

    X.J40-J47.J45   Asthma

    XII.L50-L54.L50   Hives

    XXI.Z00-Z13.Z01.0   Examination of eyes and eyesight

    XIX.T80-T88.T80.6   Other serum reactions

    Contraindications:

    Uncontrolled arterial hypertension and tachycardia, hypertrophic obstructive cardiomyopathy, insomnia, pheochromocytoma, ventricular fibrillation.

    Carefully:

    Use with caution in metabolic acidosis, hypercapnia, hypoxia, atrial fibrillation, angle-closure glaucoma, pulmonary hypertension, hypovolemia, myocardial infarction, occlusive vascular diseases (including history): arterial embolism, atherosclerosis, Buerger's disease, frostbite, diabetic endarteritis, disease Reynaud; diseases of the cardiovascular system (including angina pectoris, tachyarrhythmia, ventricular arrhythmia,coronary insufficiency, arterial hypertension), diabetes mellitus, thyrotoxicosis, benign prostatic hyperplasia, simultaneous use of funds for inhalation anesthesia.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Qualitative and well-controlled studies on humans and animals have not been conducted.

    The use of ephedrine during pregnancy and lactation (breastfeeding) is possible only if the potential benefit to the mother exceeds the possible risk to the fetus or baby.

    Dosing and Administration:

    Adults subcutaneously, intramuscularly or intravenously administered 20-50 mg; Inside - 25-50 mg 2-3 times a day.

    For topical application, the dosing regimen is individual.

    Maximum doses: for adults with oral and subcutaneous single dose - 50 mg, daily dose - 150 mg.

    Side effects:

    From the side CNS and peripheral nervous system: headache, sleep disturbance, weakness, nervousness, motor anxiety, dizziness, convulsions, muscle spasms, tremor, numbness in the hands or feet, drowsiness, pupil dilated, blurred vision; when used in high doses - hallucinations, changes in mood or psyche.

    From the side of cardio-vascular system: angina, bradycardia or tachycardia, palpitation, increased or decreased blood pressure, ventricular arrhythmias, a feeling of discomfort or pain in the chest, hemorrhages, hyperemia of the facial skin, narrowing of the peripheral vessels.

    From the side digestive system: nausea, vomiting, dryness or irritation of the mouth or pharynx (with parenteral use), loss of appetite, heartburn.

    From the side urinary system: labored and painful urination.

    Other: increased sweating, pallor of the skin, allergic reactions, dyspnea or shortness of breath, chills, hyperthermia; local reactions - pain or burning in the place of intramuscular injection.

    Overdose:

    Hypertension, arrhythmias, transient bradycardia with transition to tachycardia, myocardial infarction, pulmonary edema, renal failure, metabolic acidosis, dyspnoea, headache, vomiting, unusual pallor, cooling of the skin.

    Treatment is symptomatic.

    Interaction:

    Ephedrine weakens the effect of opioid analgesics and other agents that depress the central nervous system.

    When used simultaneously with non-selective beta-blockers and nitrates, a weakening of the therapeutic effect (blockade of β-adrenergic receptors can lead to the prevalence of alpha-adrenergic activity with a risk of hypertension and a pronounced bradycardia with possible development of cardiac blockade, beta-adrenergic blockade also inhibits beta2-adrenergic bronchodilator effect).

    Funds alkalinizing urine (including antacids containing calcium and magnesium ions, inhibitors of carbonic anhydrase, citrates, sodium hydrogen carbonate), increase the half-life ephedrine and the risk of intoxication.

    When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, agents for inhalation anesthesia (chloroform, enflurane, halothane, isoflurane, methoxyflurane, trichlorethylene), the risk of developing severe ventricular arrhythmias increases; with other sympathomimetics - increased severity of side effects from the cardiovascular system; with antihypertensive drugs (including sympatholytic drugs, diuretics, rauwolfia alkaloids) - a decrease in the hypotensive effect.

    Simultaneous use of beta-adrenomimetics with bronchodilator means, additional excessive stimulation of the central nervous system is possible, which can lead to increased excitability, irritability, insomnia, convulsions, arrhythmias.

    When used simultaneously with reserpine and MAO inhibitors (including furazolidone, procarbazine, selegiline) there may be headache, heart rhythm disturbances, vomiting, sudden and pronounced increase in blood pressure, hyperpyretic crisis; with phenytoin - a sudden decrease in blood pressure and bradycardia (depends on the dose and rate of administration); with drugs of thyroid hormones - mutual reinforcement of action.

    Increases metabolic clearance of glucocorticosteroids, ACTH for prolonged use (correction of their doses may be required). Ergometrine, ergotamine, methylergomethrin, oxytocin increase the vasoconstrictor effect and the risk of occurrence of ischemia and gangrene.

    Levodopa increases the risk of arrhythmias (requires a reduction in the dose of sympathomimetics).

    Enhances the stimulating effect on the central nervous system and the risk of toxic effects of xanthines (including aminophylline, theophylline, caffeine).

    Cocaine enhances the stimulating effect on the central nervous system and the cardiovascular system.

    Special instructions:

    To avoid disturbance of night sleep, do not use ephedrine and containing drugs at the end of the day and at bedtime.

    It is inappropriate to apply for a long time. In connection with the stimulating effect on the central nervous system ephedrine can be a means of abuse.

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