Products
Etilefrin is commercially available in drop form (Effortil) and has been approved in many countries since 1958. The combination with dihydroergotamine (Effortil plus) is no longer marketed.
Structure and properties
Etilefrin (C10H15NO2, Mr = 181.23 g/mol) is a racemate and is present in drugs as etilefrine hydrochloride, a white crystalline powder or colorless crystals that are readily soluble in water. Like other sympathomimetics, it is structurally related to epinephrine.
Effects
Etilefrin (ATC C01CA01) has sympathomimetic, positive inotropic, and chronotropic properties. It binds to alpha1 and beta1 adrenoceptors to promote cardiac activity, constrict blood vessels, and increase venous tone.
Indications
Etilefrin is used to treat low blood pressure.
Dosage
According to the SmPC. The drops are usually taken two to three times a day, preferably before meals, with plenty of liquid. Due to its stimulant properties, the drug should not be administered in the late afternoon or evening.
Abuse
Etilefrin can be abused as a stimulant. It is prohibited in athletic competitions according to the doping list.
Contraindications
Full details can be found in the drug label.
Interactions
Drug-drug interactions have been described with sympathomimetics, cardiac glycosides, inhalational anesthetics, dihydroergotamine, beta-blockers, atropine, antidiabetics, and antihypertensives.
Adverse effects
The most common possible adverse effects include headache. Occasionally, palpitations, cardiac arrhythmias, dizziness, tremor, restlessness, insomnia, anxiety, and nausea may occur.
