Ephedrine (Ephedrine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceEphedrineEphedrine
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  • 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
    • Dosage form: & nbspInjection.
    Composition:

    1 ml of the solution contains:

    active substance: ephedrine hydrochloride - 50 mg, excipient: water for injection.

    Description:

    Transparent colorless liquid.

    Pharmacotherapeutic group:Sympathomimetic tool.
    ATX: & nbsp

    R.03.C.A.02   Ephedrine

    Pharmacodynamics:

    Sympathomimetic, stimulates alpha and beta-adrenergic receptors. Acting on varicose thickening of efferent adrenergic fibers, promotes the release of norepinephrine into the synaptic cleft. In addition, it has a weak stimulating effect directly on adrenoreceptors. It causes vasoconstrictive, bronchodilating and psychostimulating action. Increases the overall peripheral vascular resistance and systemic blood pressure, increases the minute volume of blood, the number of heartbeats and the force of the heart beat, improves the atrioventricular conductivity; increases the tone of skeletal muscles, the concentration of glucose in the blood; inhibits peristalsis of the intestine, dilates the pupil (without affecting accommodation and intraocular pressure).Stimulates the central nervous system, by psycho-stimulating action is close to the phenamine. It inhibits the activity of monoamine oxidase and catecholamine-O-methyltransferase. Has a stimulating effect on alpha-adrenergic receptors of blood vessels in the skin, causing narrowing of dilated vessels, thereby reducing their increased permeability, leading to a decrease in swelling in hives.

    The beginning of the therapeutic effect with intramuscular injection of 25-50 mg - after 10-20 minutes, the duration of action - 0.5-1 hour. With repeated administration with a short interval (10-30 minutes), the pressor effect of ephedrine rapidly decreases (tachyphylaxis, bound with a progressive decrease in the stocks of norepinephrine in varicose thickenings).

    Pharmacokinetics:

    Absorption after intramuscular or subcutaneous administration is rapid.

    In small amounts, it is metabolized in the liver. The half-life at pH 5 of urine is 3 hours, at a pH of 6.3 urine -6 hours.

    It is excreted by the kidneys, mostly unchanged. The amount of the drug taken depends on the pH of the urine and increases when the urine pH shifts to the acid side.

    Indications:

    Arterial hypotension (collapse, shock,surgical interventions, spinal anesthesia, trauma, blood loss, bacteremia, gangloblocking overdose, adrenoblockers and other antihypertensive medications); uncontrolled sympathetic block with various variants of central segmental blockades.

    Contraindications:

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

    If you have any of these diseases, consult a doctor before taking the drug.

    Carefully:

    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, Raynaud's disease; 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.

    If you have any of these diseases, consult a doctor before taking the drug.

    Dosing and Administration:

    Subcutaneously, intravenously and intramuscularly. The method of administration depends on the indications. With an acute decrease in blood pressure, a slow intravenous injection is indicated; with infectious diseases, before spinal anesthesia - subcutaneous or intramuscular injection.

    Intravenously ephedrine apply by spray or drip. When a single-stage injection is slowly injected 0.02-0.05 g (0.4 - 1 ml of a solution with a concentration of 50 mg / ml).

    With drip introduction ephedrine used in isotonic sodium chloride solution in a total dose of 0.06-0.08 g; the amount of isotonic solution is from 100 to 800 ml.

    For subcutaneous administration, 0.02-0.05 g (0.4-1 ml) of a solution with a concentration of 50 mg / ml 1-2 times a day is used.

    To prevent a reduction in blood pressure for spinal anesthesia, 1 ml of a solution with a concentration of 50 mg / ml 10-30 min before the onset of anesthesia is injected under the skin.

    Higher doses of ephedrine for adults with subcutaneous injection: single dose - 0.05 g, daily - 0.1 g.

    Side effects:

    From the nervous system and sensory organs: more often - headache, sleep disturbance; less often - weakness, nervousness, motor anxiety, dizziness; frequency unknown - convulsions, muscle spasms, tremor, numbness of hands or feet, drowsiness; when used in high doses - hallucinations, changes in mood or psyche.

    From the cardiovascular system: less often - angina, bradycardia or tachycardia, palpitation, increase or decrease in blood pressure, at high doses - ventricular arrhythmias; rarely - a feeling of discomfort or pain in the chest; frequency unknown - unusual hemorrhages, hyperemia of the facial skin.

    From the digestive system: more often - nausea, vomiting; less often - dryness or irritation of the mouth or pharynx, loss of appetite; frequency is unknown - heartburn.

    From the urinary system: less often - difficulty and painful urination.

    Local reactions: pain or burning in the place of intramuscular injection.

    Other: less often - increased sweating, pale skin; narrowing of peripheral vessels, allergic reactions, dyspnea or shortness of breath, chills, hyperthermia, dilated pupils, blurred vision.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

    Overdose:

    Symptoms: severe weakness, agitation, insomnia, urinary retention, excessive blood pressure increase, decreased appetite, vomiting, increased sweating, rash.

    Treatment: with excessive hypertensive effect, reduce the rate of administration or the introduction of temporary discontinuation, if ineffective - alpha-blockers short-acting.

    Interaction:

    Weakens the effects of narcotic analgesics and hypnotic drugs.

    Medicines alkalinizing urine (including antacids containing Ca2+ and Mg2+, carbonic anhydrase inhibitors, citrates, sodium hydrogen carbonate), increase the half-life of ephedrine and the risk of intoxication.

    When applied 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 otherssympathomimetic means - 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 with adrenergic bronchodilators can lead to additional excessive stimulation of the central nervous system, which can cause increased excitability, irritability, insomnia, seizures, arrhythmias.

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

    Simultaneous administration with reserpine and monoamine oxidase inhibitors (including furazolidone, procarbazine, selegiline) can cause headache, cardiac arrhythmias, vomiting, sudden and pronounced increase in blood pressure, hyperpyretic crisis; with non-selective beta-blockers and nitrates - the weakening of the therapeutic effect (beta-adrenergic blockade can lead to the prevalence of alpha-adrenergic activity with the risk of hypertension and a pronounced bradycardia with possible development of cardiac blockade, beta-adrenergic blockade also prevents beta2-adrenergic bronchodilator effect); with phenoxybenzamine - strengthening of the hypotensive effect and tachycardia; 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 the metabolic clearance of glucocorticosteroids, adrenocorticotropic hormones during long-term use (dosage adjustment may be required); neurological effects of diatrizoates, iotalamic and yoxaglovic acids. Ergometrine, ergotamine, methylergomethrin, oxytocin increase the vasoconstrictor effect and the risk of occurrence of ischemia and gangrene, as well as severe arterial hypertension, up to intracranial hemorrhage. Doxapram, sympatholytics (guanadrel, guanethidine), mazindol, mecamylamine, methyldopa, trimetaphane, methylphenidate enhance the pressor effect.

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

    Strengthens the stimulating effect (mutually) on the central nervous system of mazindole, methylphenidate.

    Ritodrin enhances (mutually) effects (including side effects).

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

    Special instructions:

    For infusion, a device with a measuring device should be used to regulate the infusion rate. Infusion should be carried out in a large (better in the central) vein. During the treatment period it is recommended to measure blood pressure, urine volume, minute blood volume, electrocardiogram, central venous pressure, pulmonary artery pressure and wedging pressure in the pulmonary capillaries.

    To avoid the development of disturbances of night sleep should not be appointed ephedrine and containing medicines at the end of the day and at bedtime.

    It is recommended to be careful to avoid getting the drug into the circulatory tissues, which can cause necrosis (in the case of the formation of extravasate, infiltrate 10-15 ml of 0.9% NaCl containing 5-10 ml of phentolamine immediately). Excessive doses of myocardial infarction can increase ischemia by increasing the myocardial oxygen demand.

    Whenever possible, hypovolemia should be corrected as soon as possible. Treatment with ephedrine does not replace transfusion of blood, plasma, blood-substituting fluids and / or saline solutions.

    Ephedrine is inexpedient to apply for a long time (narrowing of peripheral vessels, leading to the possible development of necrosis or gangrene).

    When administered to correct arterial hypotension or add a local anesthetic drug during labor / delivery, as well as co-administration with some drugs that stimulate labor activity (for example, vasopressin, ergotamine, ergonovin, metergergonovin), can cause persistent arterial hypertension (up to rupture of cerebral vessels); during spinal anesthesia, it can increase the heart rate in the fetus.

    If the mother's blood pressure exceeds 130/80 mm Hg, ephedrine use is not recommended.

    In connection with the stimulating effect on the central nervous system can be the subject of abuse of drug addicts.

    When discontinuing treatment, the dose should be reduced gradually, since sudden withdrawal of therapy can lead to severe hypotension.If the solution is opaque, you can not enter it. Unused portion should be destroyed.

    Inhibitors of monoamine oxidase, increasing the pressor effect of sympathomimetics, can cause the occurrence of headaches, arrhythmias, vomiting, hypertensive crisis, therefore, when patients take monoamine oxidase inhibitors in the preceding 2-3 weeks, the dose of sympathomimetics should be reduced (up to 1/10 of the usual dose).

    Form release / dosage:Injection.
    Packaging:

    50 mg / ml in ampoules of 1 ml.

    5 ampoules in the outline of the cell.

    1 or 2 contourcell packs with instructions for use in a pack of cardboard.

    20, 50 or 100 contour packagings with 20, 50 or 100 instructions for use in a cardboard box or in a box of corrugated cardboard (for inpatient).

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000377
    Date of registration:25.02.2011
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.10.2015
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