Orthostatic hypotension and hypotensive states, including anesthesia-associated hypotension, hypovolemic shock (with volume expanders) and vasovagal syncope, per locally approved indications.
Also known as: Effortil
Hengstmann JH 1975 (PMID 9300) — physiological disposition of etilefrine in man.
Hengstmann JH 1975 (PMID 9300) — physiological disposition of etilefrine in man.
Etilefrine + epinephrine: potentiation of sympathomimetic effect — risk of arrhythmias and hypertension.
The Prontuário Terapêutico documents in the etilefrine monograph that simultaneous administration with other sympathomimetic substances may potentiate the effect (section 3.2.4). Etilefrine is a direct and indirect sympathomimetic (beta-1 agonist with an alpha component) and epinephrine stimulates alpha and beta receptors: the additive combination increases the risk of tachycardia, arrhythmias, hypertension and myocardial ischaemia. The risk scenario is mainly the administration of epinephrine during anaesthesia or resuscitation in patients who took etilefrine (often used as a decongestant or in shock). The practical guidance is to avoid combining sympathomimetics; if unavoidable, monitor blood pressure, heart rate and rhythm, and use the lowest effective epinephrine dose.
Etilefrine + epinephrine: sympathomimetic potentiation — risk of tachyarrhythmias and hypertension.
The Prontuário Terapêutico documents in the etilefrine monograph (3.2.4): "The effect may be potentiated if etilefrine is given simultaneously with other sympathomimetic substances". Epinephrine and etilefrine are both sympathomimetic — the additive combination increases the risk of tachycardia, arrhythmias and hypertension.
Monitor for signs of adrenergic excess (palpitations, tremor, chest pain, arrhythmias).
Tachyarrhythmia, hypertensive crisis or chest pain with the combination.
Avoid combining sympathomimetics; if unavoidable, monitor blood pressure, heart rate and rhythm.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Etilefrine, 3.2.4 ; approved Epinephrine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=73d75fc4-c386-4c26-8c35-339e5fa2a1e3
Etilefrine + salbutamol: potentiation of sympathomimetic effect — risk of tachycardia and tremor.
The Prontuário Terapêutico documents in the etilefrine monograph (3.2.4) the potentiation of effect when administered simultaneously with other sympathomimetic substances. Salbutamol is a beta-2 agonist used in asthma and COPD; the combination with etilefrine (beta-1 sympathomimetic with an alpha component) has additive effects — tachycardia, tremor and possible hypokalaemia, especially at high doses or with frequent inhalations. The risk is higher in the cardiac patient and in the asthmatic on chronic bronchodilators. The practical guidance is to monitor heart rate and adrenergic symptoms, consider dose adjustment and monitor serum potassium in prolonged therapy.
Etilefrine + salbutamol: sympathomimetic potentiation — risk of tachycardia and tremor.
The Prontuário Terapêutico documents the potentiation between etilefrine and other sympathomimetic substances (3.2.4). Salbutamol (beta-2 agonist) and etilefrine have additive sympathomimetic effects — tachycardia, tremor and possible hypokalaemia.
Monitor tachycardia, tremor and serum potassium.
Symptomatic tachycardia or disabling tremor with the combination.
Monitor heart rate and adrenergic symptoms in the combination; consider dose adjustment.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Etilefrine, 3.2.4
Etilefrine has low oral bioavailability (first-pass effect); food does not clinically alter its pharmacokinetics.
May be taken with or without food.
Hengstmann JH, Weyand U, Dengler HJ. The pharmacokinetics of etilefrine in man. Eur J Clin Pharmacol 1975 (PMID 9300): https://pubmed.ncbi.nlm.nih.gov/9300/
Caffeinated drinks can potentiate the stimulant effects (tachycardia, tremor) of etilefrine.
Moderate caffeine intake during treatment.
Hengstmann JH, Weyand U, Dengler HJ. The pharmacokinetics of etilefrine in man. Eur J Clin Pharmacol 1975 (PMID 9300): https://pubmed.ncbi.nlm.nih.gov/9300/
Etilefrine, being a sympathomimetic, is contraindicated in severe hypertension because of the risk of a hypertensive crisis.
Do not use in patients with severe or uncontrolled hypertension.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Etilefrine
Data on etilefrine use in pregnancy are limited; use only if the benefit outweighs the risk.
Avoid in the 1st trimester; use at delivery must balance the pressor effect.
No sufficient data on excretion into breast milk; consider an alternative.
In women of childbearing age, rule out pregnancy before starting long-term treatment.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Etilefrine ; Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 1, Drugs and Pregnancy: Contraindicated.
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Sympathomimetic with direct action on alpha and beta-adrenergic receptors: increases peripheral vascular resistance (alpha effect) and cardiac contractility and rate (beta effect), raising blood pressure. The pressor effect is rapid and short-lived.
Direct agonism of adrenergic receptors, with predominant vasopressor effect; the pharmacodynamic response correlates with the amount of drug in the central compartment.
Complete enteral absorption (~80% of the dose recovered in urine); extensive first-pass effect results in ~55% bioavailability of unchanged drug.
The main metabolite is the phenolic sulfate (conjugation); a very small proportion is excreted as hydroxymandelic acid. ~80% of the dose is excreted in urine after oral or IV administration.
Predominant half-life ~2 h, consistent with a two-compartment model; volume of distribution (Vd beta) of ~160 L.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
