Ephedrine (Solution) Instructions for Use

ATC Code

C01CA26 (Ephedrine)

Active Substance

Ephedrine (BAN)

Clinical-Pharmacological Group

Alpha-, beta-adrenergic agonist

Pharmacotherapeutic Group

Sympathomimetic agent

Pharmacological Action

Ephedrine is a sympathomimetic (indirect-acting adrenomimetic) alkaloid obtained from various species of the Ephedra L. genus of the Ephedraceae family. The ephedrine contained in plants is the levorotatory isomer. The synthetically produced racemate is less active than the levorotatory isomer.

After administration, ephedrine stimulates α- and β-adrenergic receptors: by acting on the varicose thickenings of efferent adrenergic fibers, Ephedrine promotes the release of the neurotransmitter norepinephrine into the synaptic cleft. In addition, it has a weak direct stimulating effect on adrenergic receptors.

It stimulates heart activity (increases the rate and force of contractions), facilitates AV conduction, increases blood pressure, causes a bronchodilator effect, suppresses intestinal peristalsis, dilates the pupil (without affecting accommodation and intraocular pressure), increases skeletal muscle tone, and causes hyperglycemia.

Unlike epinephrine, the effect of ephedrine develops slowly but lasts longer. With repeated administration of ephedrine at short intervals (10-30 minutes), its pressor effect quickly decreases – tachyphylaxis (rapid tolerance) occurs, associated with a progressive decrease in norepinephrine reserves in the varicose thickenings.

Ephedrine stimulates the CNS, and its psychostimulant effect is similar to phenamine.

It inhibits the activity of MAO and COMT.

Pharmacokinetics

It is metabolized in the liver in small amounts. The T_1/2 is 3-6 hours. It is excreted by the kidneys, mainly unchanged.

Indications

Arterial hypotension during surgical operations (especially during spinal anesthesia), trauma, blood loss, infectious diseases, overdose of ganglion-blocking agents, adrenoblockers, and other antihypertensive drugs.

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

Narcolepsy, enuresis (due to the stimulating effect on the CNS, sleep becomes less deep, facilitating awakening when the urge to urinate appears), myasthenia.

ICD codes

Dosage Regimen

Administer Ephedrine solution subcutaneously, intramuscularly, or intravenously as directed by a physician.

For adults, the typical subcutaneous or intramuscular dose is 25 mg to 50 mg. Do not exceed a single dose of 50 mg or a daily dose of 150 mg.

For intravenous administration in acute hypotension, administer 5 mg to 25 mg by slow injection. Repeat doses may be given as needed, not more frequently than every 10 minutes to avoid tachyphylaxis.

For bronchial asthma or obstructive respiratory diseases, administer 25 mg to 50 mg subcutaneously or intramuscularly. The dose may be repeated if necessary.

For prevention of hypotension during spinal anesthesia, administer 25 mg to 50 mg intramuscularly or subcutaneously.

For pediatric patients, the recommended subcutaneous dose is 3 mg/kg/24 hours or 0.2 mL/kg/24 hours, divided into 4 to 6 doses.

Adjust the dosage regimen individually based on clinical response and patient tolerance. Monitor heart rate and blood pressure closely.

Avoid administering the final dose late in the day to prevent insomnia. Avoid long-term use due to the risk of tolerance and dependence.

Adverse Reactions

Nervous system: headache, sleep disturbances, weakness, nervousness, motor restlessness, dizziness, convulsions, muscle spasms, tremor, numbness of the hands or feet, drowsiness; when used in high doses – hallucinations, mental disorders.

Organ of vision: pupil dilation, blurred vision.

Cardiovascular system: angina pectoris, bradycardia or tachycardia, palpitations, increase or decrease in blood pressure, ventricular arrhythmias, feeling of discomfort or chest pain, hemorrhages, facial skin flushing, peripheral vasoconstriction.

Digestive system: nausea, vomiting, dryness or irritation of the mouth or throat, loss of appetite, heartburn.

Urinary system: difficult and painful urination.

Local reactions: pain or burning at the site of intramuscular injection.

Other: increased sweating, pallor of the skin, allergic reactions, shortness of breath or difficulty breathing, chills, hyperthermia.

Contraindications

Hypersensitivity to ephedrine; uncontrolled arterial hypertension, tachycardia, hypertrophic obstructive cardiomyopathy, insomnia, pheochromocytoma, ventricular fibrillation.

Use in Pregnancy and Lactation

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

Special Precautions

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

To avoid disruption of night sleep, Ephedrine and preparations containing it should not be used at the end of the day and before bedtime.

Long-term use is not advisable. Due to its stimulating effect on the CNS, Ephedrine can be a substance of abuse.

Drug Interactions

With simultaneous use, Ephedrine weakens the effect of opioid analgesics and other agents that have a depressant effect on the CNS.

With simultaneous use with non-selective beta-blockers and nitrates – weakening of the therapeutic effect (blockade of β-adrenergic receptors can lead to the predominance of alpha-adrenergic activity with the risk of developing arterial hypertension and pronounced bradycardia with the possible development of heart block; blockade of β-adrenergic receptors also prevents the beta₂-adrenergic bronchodilator effect).

With simultaneous use, urine-alkalinizing agents (including antacids containing calcium and magnesium ions, carbonic anhydrase inhibitors, citrates, sodium bicarbonate) increase the T_1/2 of ephedrine, thereby increasing the risk of intoxication.

With simultaneous use with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, agents for inhalation anesthesia (chloroform, enflurane, halothane, isoflurane, methoxyflurane, trichloroethylene), the risk of developing severe ventricular arrhythmias increases; with other sympathomimetics – increased severity of side effects from the cardiovascular system; with antihypertensive agents (including sympatholytics, diuretics, rauwolfia alkaloids) – reduction of the hypotensive effect.

With simultaneous use with bronchodilator beta-adrenomimetics, additional excessive stimulation of the CNS is possible, which can cause increased excitability, irritability, insomnia, convulsions, arrhythmias.

With simultaneous use with reserpine and MAO inhibitors (including furazolidone, procarbazine, selegiline), headache, cardiac rhythm disturbances, vomiting, sudden and significant increase in blood pressure, hyperpyretic crisis are possible; with phenytoin – sudden decrease in blood pressure and bradycardia (depends on the dose and rate of administration); with thyroid hormone preparations – mutual enhancement of action.

With long-term simultaneous use, Ephedrine increases the metabolic clearance of corticosteroids, ACTH (dose adjustment may be required). Ergometrine, ergotamine, methylergometrine, oxytocin increase the vasoconstrictor effect and the risk of ischemia and gangrene.

With simultaneous use, levodopa increases the risk of developing arrhythmias (a reduction in the dose of the sympathomimetic is required).

With simultaneous use, Ephedrine enhances the stimulating effect on the CNS and the risk of toxic phenomena from xanthines (including aminophylline, theophylline, caffeine).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.