Etilefrin

Etilefrin is an active ingredient that is used to treat low blood pressure. It belongs to the group of sympathomimetics and is structurally related to adrenaline. It is present in medicines in the form of etilefrin hydrochloride and is a white crystalline powder. Etilefrin is soluble in water.

Etilefrin is a racemate. A racemate is an active substance that consists of 2 molecules that occur in a 1:1 ratio and behave like image and mirror image. One speaks of the R-(dextrorotatory) enantiomer and S-(levorotatory) enantiomer. Enantiomers do NOT differ in their physical properties such as melting or boiling point. However, they can have the opposite effect. For example, (S)-carvone smells like caraway and (R)-carvone smells like mint. The amino acid (S)-valine tastes bitter, while (R)-valine tastes sweet. For these reasons, both enantiomers are always tested in today's approval procedures for new active ingredients. Sometimes one enantiomer can be converted into the other in the body.

Etilefrin works by binding to the alpha-1 and beta-1 receptors in the blood vessels. Binding of the active substance to the alpha receptors causes the blood vessels to constrict (vasoconstriction). Binding to the beta receptors leads to an increase in the beating force of the heart and an increased heart rate. This increases blood pressure. Additional effects of etilefrin include dilated pupils and dilated bronchi. The active ingredient cannot cross the blood-brain barrier and therefore only has a peripheral effect.

Always take Etilefrin exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose for adults is 3.75-7.5 mg 3 times a day.

The recommended dose for adolescents and children over 6years of age is 1.875-3.75 mg 2-3 times a day.

The usual dose for children up to 6 years of age is 0.75-1.875 mg 2-3 times a day.

Due to the stimulating effect of the active ingredient, it should not be taken from late afternoon onwards, as this can lead to problems falling asleep.

The following side effects may occur:

Frequent:

• Headache
• Gastrointestinal complaints

Occasional:

• Anxiety
• Insomnia
• Muscle tremors
• restlessness
• dizziness
• Cardiac arrhythmia
• High heart rate (tachycardia)
• palpitations
• nausea

Frequency unknown:

• allergic reactions
• Tightness in the chest (angina pectoris)
• Increase in blood pressure
• sweating

Interactions may occur if the following medicines are taken at the same time:

• Guanethidine
• reserpine
• mineralocorticoids
• Thyroid hormones
• Medication for the treatment of bronchial asthma (sympathomimetics)
• tricyclic antidepressants
• MAO inhibitors
• Medication for allergies (antihistamines)
• digitalis preparations
• certain anesthetic gases (halogenated aliphatic hydrocarbons)
• dihydroergotamine
• atropine
• quinidine
• Alpha- and beta-blockers
• Medication for diabetes mellitus

Etilefrin must NOT be taken in the following cases

• if you are allergic to Etilefrin
• high blood pressure (hypertension)
• cardiac arrhythmia with a rapid heart rate (tachycardia)
• in case of derailment of hyperthyroidism
• tumor of the adrenal gland
• increased intraocular pressure (glaucoma)
• in case of urinary bladder emptying disorder
• severe narrowing of the coronary arteries (coronary heart disease)
• for cardiac insufficiency (heart failure)
• in case of disease of the heart muscle (hypertrophic obstructive cardiomyopathy)
• for narrowing of the heart valves or large arteries
• in the event of a temporary drop in blood pressure
• in case of vascular hardening
• when taking MAO inhibitors for depression

Etilefrin is on the doping list as a stimulant.

Etilefrin can be used from birth .

Etilefrin should NOT be taken in the 1st trimester of pregnancy .

In the 2nd and 3rd trimester, Etilefrin should only be used after consultation with your doctor and after careful consideration of the risks and benefits.

Etilefrin should NOT be taken during breastfeeding, as it is not known whether the active substance passes into breast milk.