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.
No documented drug–drug interactions for this medicine.
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
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.
