Ephedrine
Ephedrine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Ephedrine
ATX code: R03CA02
Active ingredient: ephedrine (Ephedrine)
Manufacturer: Federal State Unitary Enterprise "Moscow Endocrine Plant" (Russia)
Description and photo update: 2020-29-04
Ephedrine is a sympathomimetic drug that is highly effective in the treatment of arterial hypotension.
Release form and composition
Dosage form - solution for injection: colorless, transparent (in a cardboard box 1 or 2 cell contour packages containing 5 ampoules with 1 ml of solution at a dose of 50 mg / ml, and instructions for use of Ephedrine).
Composition of 1 ml solution:
- active substance: ephedrine hydrochloride - 50 mg;
- auxiliary component: water for injection.
Pharmacological properties
Pharmacodynamics
Ephedrine is one of the sympathomimetics that have a stimulating effect on α- and β-adrenergic receptors. It promotes the release of norepinephrine into the synaptic cleft by acting on the varicose thickening of efferent adrenergic fibers. Also, the substance weakly stimulates adrenergic receptors.
Pharmacological actions of Ephedrine:
- psychostimulating, bronchodilating and vasoconstrictor effect;
- increased total peripheral vascular resistance and systemic blood pressure;
- an increase in the minute blood volume, strength and number of heart contractions;
- improvement of atrioventricular conduction;
- increased skeletal muscle tone;
- increased blood glucose;
- inhibition of intestinal peristalsis;
- dilation of the pupil (this effect has no effect on intraocular pressure and accommodation);
- stimulation of the central nervous system (ephedrine is close to phenamine in its psychostimulating effect);
- inhibition of the activity of catechol-O-methyltransferase and monoamine oxidase;
- stimulation of α-adrenergic receptors of blood vessels in the skin, which leads to a narrowing of the dilated vessels and a decrease in their increased permeability, which causes a decrease in edema in urticaria.
With intramuscular (i / m) administration of the drug at a dose of 25 to 50 mg, the therapeutic effect begins after 10–20 minutes and lasts for 0.5–1 hours. In cases of repeated administration of ephedrine with an interval of 10–30 minutes, its pressor the effect quickly decreases (tachyphylaxis develops, associated with a progressive decrease in norepinephrine reserves in varicose thickenings).
Pharmacokinetics
Ephedrine after subcutaneous (s / c) or intramuscular (i / m) administration is rapidly absorbed. The liver is metabolized in small amounts. Its half-life at a urine pH of 5 is 3 hours, at a urine pH of 6.3 - 6 hours.
Excretion is carried out mainly unchanged by the kidneys. The amount of drug excreted depends on the pH of the urine and increases with a shift in pH towards the acidic side.
Indications for use
- arterial hypotension, which can be caused by bacteremia, blood loss, trauma, spinal anesthesia, surgery, shock, collapse, overdose of adrenergic blockers, ganglion blockers and other antihypertensive drugs and other factors;
- uncontrolled sympathetic block against the background of various variants of central segmental blockades.
Contraindications
Absolute:
- uncontrolled tachycardia and arterial hypertension;
- hypertrophic obstructive cardiomyopathy;
- pheochromocytoma;
- insomnia;
- ventricular fibrillation;
- established hypersensitivity to the components of the drug.
Relative (the use of Ephedrine solution requires special care and careful medical supervision):
- occlusive vascular disease, including in history, including Raynaud's disease, diabetic endarteritis, frostbite, Buerger's disease, atherosclerosis, arterial embolism;
- atrial fibrillation;
- hypoxia;
- hypercapnia;
- metabolic acidosis;
- hypovolemia;
- angle-closure glaucoma;
- myocardial infarction;
- pulmonary hypertension;
- thyrotoxicosis;
- pathologies of the cardiovascular system, including arterial hypertension, coronary insufficiency, ventricular arrhythmia, tachyarrhythmia, angina pectoris;
- diabetes;
- benign prostatic hyperplasia;
- combination therapy with drugs for inhalation anesthesia;
- pregnancy;
- lactation period.
Ephedrine, instructions for use: method and dosage
Ephedrine Injection Solution is intended for intravenous, subcutaneous and intravenous (intravenous) administration.
Depending on the indications, the method of drug administration is selected. Against the background of infectious pathologies and before spinal anesthesia, it is used s / c or i / m; with an acute decrease in blood pressure - slowly IV.
The drug is injected into a vein by drip or jet. With a single-stage injection, 0.02-0.05 g (0.4-1 ml of the drug with a concentration of 50 mg per 1 ml) is injected slowly in a stream.
In cases of drip injection, 0.06–0.08 g of ephedrine is mixed with 100–800 ml of isotonic sodium chloride solution.
When 0.02–0.05 g (0.4–1 ml) of the drug is injected under the skin at a concentration of 50 mg per 1 ml, it is administered 1–2 times a day.
In spinal anesthesia, in order to prevent a decrease in blood pressure, 1 ml of a solution at a concentration of 50 mg per 1 ml is injected 10–30 minutes before the start of anesthesia.
The maximum single dose for adults with subcutaneous injection is 0.05 g, the daily dose is 0.1 g.
Side effects
The development of the following undesirable side reactions from systems and organs with parenteral administration of Ephedrine is possible:
- nervous system and sensory organs: very often - sleep disturbance, headache; often - dizziness, restlessness, nervousness, weakness; with an unknown frequency - drowsiness, numbness of the upper or lower extremities, tremors, muscle spasms, cramps; with the introduction of high doses - a change in the psyche, emotional lability, hallucinations;
- cardiovascular system: often - increase / decrease in blood pressure, palpitations, tachycardia, angina pectoris, bradycardia; rarely - pain or discomfort in the chest; with an unknown frequency - facial skin hyperemia, unusual hemorrhages; with the introduction of high doses - ventricular arrhythmia;
- digestive system: very often - nausea, vomiting; often - loss of appetite, throat irritation or dry mouth; with an unknown frequency - heartburn;
- urinary system: often - painful and difficult urination;
- local reactions: burning or pain at the site of the i / m injection;
- others: often - blurred vision, dilated pupils, hyperthermia, chills, shortness of breath or shortness of breath, allergic reactions, narrowing of peripheral vessels, pallor of the skin, increased sweating.
In case of aggravation of any of the above side effects or the development of other negative effects that are not described in the instructions, you need to consult a doctor.
Overdose
The main symptoms are: skin rash, increased sweating, vomiting, decreased appetite, excessive increase in blood pressure, urinary retention, insomnia, agitation, severe weakness.
Therapy: when an excessive hypertensive effect occurs, the rate of administration is reduced or the use of Ephedrine is temporarily discontinued. If this method is ineffective, short-acting α-blockers are prescribed.
special instructions
In the drip method of intravenous administration of the solution, an instrument with a measuring device is used to regulate the infusion rate. Ephedrine should be injected into a large vein, preferably a central vein.
During therapy, it is important to measure pulmonary artery pressure, pulmonary capillary wedge pressure, central venous pressure, electrocardiogram, blood minute volume, urine volume, and blood pressure.
Ephedrine is not recommended for use at bedtime and at the end of the day to avoid nighttime sleep disturbances.
The solution must be injected carefully and do not allow it to enter the perivascular tissues outside the vascular bed, as this can lead to their necrosis (when extravasate is formed, immediately infiltrate 10-15 ml of 0.9% sodium chloride solution containing 5-10 ml of phentolamine). Higher doses in the setting of myocardial infarction can increase ischemia by increasing myocardial oxygen demand.
If possible, hypovolemia should be corrected before starting treatment. Drug therapy is not a substitute for transfusions of blood, plasma, blood substitutes, and / or saline solutions.
Long-term courses of Ephedrine use are inappropriate, since they can contribute to the narrowing of peripheral vessels, leading to the possible development of gangrene or necrosis.
The use of Ephedrine to correct arterial hypotension during labor / delivery (added to a local anesthetic solution) or in combination with certain drugs to stimulate labor (to methylergonovine, ergonovine, ergotamine, vasopressin, etc.) can lead to persistent arterial hypertension. up to rupture of cerebral vessels. During spinal anesthesia, there is sometimes an increase in the fetal heart rate. When the mother's blood pressure is more than 130/80 mm. rt. Art. the drug is not used.
Since the substance stimulates the central nervous system, it can be abused by drug addicts.
Cancellation of therapy should be carried out gradually, as otherwise severe hypotension may appear.
Do not use an opaque solution. The remaining unused part of the drug must be destroyed.
The combined use of ephedrine with monoamine oxidase inhibitors, due to the increase in the latter of the pressor effect of the drug, may cause the appearance of vomiting, arrhythmias, headaches and hypertensive crisis. In this regard, when taking monoamine oxidase inhibitors in the previous 14-21 days, the dose of sympathomimetic is reduced (up to 1/10 of the usual dose).
Application during pregnancy and lactation
Ephedrine during pregnancy and during breastfeeding can only be prescribed for strict indications in cases where the benefits of therapy outweigh the existing risk.
Drug interactions
The effect of drugs / substances on ephedrine when used together:
- drugs that alkalinize urine, including sodium bicarbonate, citrates, carbonic anhydrase inhibitors, antacids containing calcium and magnesium: increase its half-life and the likelihood of developing intoxication;
- oxytocin, methylergometrine, ergotamine, ergometrine: increase the vasoconstrictor effect and the risk of gangrene, ischemia and severe arterial hypertension, up to intracranial hemorrhage;
- methylphenidate, trimetaphan, methyldopa, mecamylamine, mazindol, sympatholytics (guanethidine, guanadrel), doxapram: increase the pressor effect of ephedrine;
- levodopa: increases the likelihood of developing arrhythmias (requires a reduction in the dose of the drug);
- ritodrin: increases the pharmacological efficacy of ephedrine, including enhances unwanted side reactions (this effect is mutual);
- antihypertensive drugs, including sympatholytics, diuretics, rauwolfia alkaloids: reduce the hypotensive effect;
- nonselective β-adrenergic blockers and nitrates: weaken the therapeutic effect (the blockade of β-adrenergic receptors can serve as the prevalence of α-adrenergic activity with the risk of arterial hypertension and pronounced bradycardia with the probable appearance of heart block. β-adrenergic blockade also prevents β-adrenergic action of bronchodilator);
- preparations of thyroid hormones: enhance the effect of ephedrine (this effect is mutual);
- phenoxybenzamine: enhances the hypotensive effect of ephedrine; development of tachycardia can be noted.
The effect of ephedrine on drugs / substances when used together:
- hypnotics, narcotic analgesics: weakens the effects;
- ioxagloic and iothalamic acids, diatrizoates: enhances their neurological effect;
- adrenocorticotropic hormones, glucocorticosteroids: with prolonged treatment, increases metabolic clearance (correction of their doses may be required);
- methylphenidate, mazindol: the stimulating effect on the central nervous system increases (this effect is mutual);
- xanthines, including theophylline, oxtriphylline, diphylline, caffeine, aminophylline: increases the stimulating effect on the central nervous system and the risk of toxic effects;
- cocaine: enhances the stimulating effect on the cardiovascular and central nervous system.
Combinations to be taken into account:
- dopamine, tricyclic antidepressants, quinidine, cardiac glycosides, drugs for inhalation anesthesia (trichlorethylene, methoxyflurane, isoflurane, halothane, enflurane, chloroform): the risk of severe ventricular arrhythmias increases;
- other sympathomimetic drugs: the severity of adverse events from the cardiovascular system increases;
- adrenergic bronchodilator drugs: additional excessive stimulation of the central nervous system is possible, which in some cases leads to arrhythmias, convulsions, insomnia, irritability, increased excitability;
- reserpine and monoamine oxidase inhibitors (including selegiline, procarbazine, furazolidone): the development of vomiting, headache, hyperpyretic crisis, sudden and pronounced increase in blood pressure, cardiac arrhythmias is possible;
- phenytoin: blood pressure suddenly drops and bradycardia is noted.
Analogs
Ephedrine analogues are Ephedrine hydrochloride solution for injection 5%, Adrenaline, Adrenaline-SOLOpharm, Adrenaline hydrochloride-Vial, Norepinephrine, Norepinephrine Agetan, Norepinephrine, Epidject, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ephedrine
There are few reviews of Ephedrine confirming its clinical efficacy.
Price for Ephedrine in pharmacies
The price of Ephedrine is unknown because the drug is not available in pharmacies. The approximate cost of an analogue of the drug - Ephedrine hydrochloride solution for injection 5% (in a package of 10 ampoules of 1 ml) is from 480 to 490 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
