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etilefrine, combinations

C01CA51

Forms & Strengths

Oral tablets: 2.5 mg to 5 mg
Oral drops: 7.5 mg/mL
Intravenous/Intramuscular injection: 10 mg/mL
Combination formulations with analeptics or autonomic agents vary by region

Adult Dosing

Oral: 5 mg to 10 mg 3 times daily
Oral drops: 15 to 20 drops 3 times daily
Acute hypotension (IM/IV): 2.5 mg to 5 mg administered slowly; may be repeated as needed

Pediatric Dosing

Safety and efficacy in children are not fully established
Oral drops (when used): Dosage adjusted by age, typically 2 to 5 drops 2 to 3 times daily for younger children, and up to 10 drops for adolescents, under strict clinical supervision

Indications

Orthostatic hypotension and circulatory dysregulation
Hypotensive states associated with autonomic dysfunction
Management of acute hypotensive episodes during anesthesia or surgery

Mechanism of Action

Direct stimulation of alpha-1 and beta-adrenergic receptors
Increases cardiac output and venous return through vasoconstriction
Elevates both systolic and diastolic blood pressure

Contraindications

Hypersensitivity to etilefrine or sympathomimetic amines
Severe hypertension and thyrotoxicosis
Phaeochromocytoma
Angle-closure glaucoma
First trimester of pregnancy and lactation
Severe coronary artery disease and recent myocardial infarction

Adverse Reactions

Palpitations, tachycardia, and cardiac arrhythmias
Hypertension and headache
Anxiety, tremor, and restlessness
Nausea and sweating

Drug Interactions

Monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants can potentiate the pressor response, risking severe hypertension
Beta-blockers may antagonize the cardiovascular effects of etilefrine and lead to severe vasoconstriction via unopposed alpha-adrenergic activity
Halogenated hydrocarbon anesthetics increase myocardial sensitivity to sympathomimetics, raising arrhythmia risks

Curated Content: Needs Vetting Before Put to Clinical Use