Ebrantil® (Urapidil)

Ebrantil® (active ingredient urapidil) is an antihypertensive with a unique dual mechanism of action: it blocks peripheral alpha-1 receptors and at the same time stimulates central serotonin 5-HT1A receptors. This combination lowers blood pressure without the reflex increase in heart rate that often occurs with other vasodilators.

Urapidil is used for severe high blood pressure that does not respond adequately to other medications. As a solution for injection, it is one of the standard medications for hypertensive emergencies in the emergency department. For oral use, it is available as Ebrantil® extended-release capsules.

Unlike most blood pressure medications, urapidil has no negative effect on metabolism (blood sugar, blood lipids) and may even improve insulin sensitivity.

Urapidil has a dual mechanism of action:

1. Peripheral alpha-1 blockade:

• Blocks alpha-1 receptors on the blood vessels
• Arteries and veins dilate
• Peripheral vascular resistance decreases
• Blood pressure falls

2. Central serotonin effect (5-HT1A agonism):

• Stimulates central 5-HT1A receptors in the brainstem
• Inhibits sympathetic tone centrally
• Prevents the reflex increase in heart rate
• Steady lowering of blood pressure without a racing heart

Advantages of the dual mechanism:

• No reflex tachycardia (unlike pure alpha blockers)
• No sodium retention
• Metabolically neutral (no negative effect on blood sugar/blood lipids)
• May improve insulin sensitivity

Onset of action: Extended-release capsules: after 30-60 minutes. Intravenous: within 5 minutes. Duration of action of the extended-release form: 10-14 hours.

Ebrantil® (urapidil) is suitable for:

• Moderate to severe high blood pressure
• Treatment-resistant high blood pressure (as an add-on medication)
• Hypertensive crises and emergencies (IV)
• Perioperative blood pressure control (IV)

Particularly suitable for:

• High blood pressure with metabolic syndrome
• Diabetes with high blood pressure (metabolically neutral)
• Patients in whom reflex tachycardia is undesirable
• Acute hypertensive episode as emergency therapy

Not suitable:

• Coarctation of the aorta
• Arteriovenous shunts (except hemodynamically insignificant ones)
• Pregnancy and breastfeeding

High blood pressure (oral, extended-release capsules):

• Starting dose: 30 mg twice daily
• Usual dose: 30-60 mg twice daily
• Maximum dose: 180 mg daily (divided into 2 doses)

Hypertensive emergency (intravenous):

• 25 mg slowly IV (over 20 seconds)
• If the effect is insufficient: repeat after 5 minutes
• Maintenance infusion: 9-30 mg/hour

Available strengths:

• 30 mg, 60 mg, 90 mg extended-release capsules (Ebrantil®)
• 25 mg/5 ml, 50 mg/10 ml solution for injection

How to take (extended-release capsules):

• Twice daily (morning and evening)
• Swallow the capsules whole with water
• Do not open or chew
• Regardless of meals

Notes:

• Regular blood pressure and pulse checks
• Move slowly when getting up (orthostatic hypotension possible)
• Watch for dizziness, especially in the first few days
• Do not stop abruptly (taper off slowly)

For emergency use (IV): Only by medical professionals, with blood pressure and ECG monitoring.

Ebrantil® must not be taken in cases of:

• Hypersensitivity to urapidil
• Pregnancy, unless treatment is necessary because of your medical condition

Caution in:

• Hepatic impairment (slowed breakdown)
• Renal impairment (dose adjustment may be needed)
• Older patients (increased sensitivity)
• Heart failure (close monitoring), especially if it has a mechanical cause, e.g. aortic or mitral valve stenosis
• Hypovolemia (greater drop in blood pressure)

Pregnancy and breastfeeding: There is no or only very limited experience with urapidil in pregnant women. Urapidil crosses the placenta to the unborn child, and animal studies have shown harmful effects on reproduction. Use is not recommended in women of childbearing age who are not using contraception. Ebrantil® should not be used during breastfeeding.

Common (1-10%):

• Dizziness
• Headache
• Nausea
• Fatigue

Uncommon (0.1-1%):

• Orthostatic hypotension (especially at the start)
• Gastrointestinal complaints
• Dry mouth
• Nasal congestion
• Sleep disturbances
• Skin rash
• Palpitations

Rare:

• Priapism (persistent erection – emergency!)
• Thrombocytopenia
• Angioedema
• Severe drop in blood pressure

Caution with:

• Other blood pressure-lowering drugs → increased hypotension
• Alpha blockers (doxazosin, tamsulosin) → additive hypotension
• PDE-5 inhibitors (sildenafil, tadalafil) → increased lowering of blood pressure
• Alcohol → increased hypotension
• Cimetidine → increased urapidil levels

Note: Combination with ACE inhibitors is currently not recommended, as there is not yet sufficient experience with it.