Urapidil

6 - ( (3 - ( 4 - (2 -methoxyphenyl) - 1-piperazinyl) propyl) amino) - 1,3- dimethyl- 2, 4 ( 1H, 3H) - pyrimidinedion

• 34661-75-1
• 64887-14-5 ( urapidil hydrochloride)

C02CA06

Antihypertensives

α1 -adrenoceptor antagonist

156-158 ° C

Water: 157 mg · l-1 at 25 ° C

Hydrochloride

Attention

520 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Urapidil is an antihypertensive ( blood pressure lowering agent ) from the group of α1 -adrenoceptor antagonists, and is used primarily in acute increases in blood pressure.

• 2.1 pharmacodynamics
• 2.2 pharmacokinetics

Clinical information

Application

Urapidil ( iv ) is an alternative to calcium antagonists and nitrates in hypertensive crisis. Orally, it can be used in the combination therapy of arterial hypertension.

Side effect

Side effects are common ( 1-10 %), nausea, headache and dizziness, rare (< 1%), arrhythmias, fatigue and sweats observed.

Contraindications

During pregnancy and lactation urapidil is contraindicated. However, it is often used as "off label" treatment in pregnancy, especially at a time and manifested under Perfusorgesteuerter hand against preeclampsia. In the case, a maximum daily dose of 24 mg / hour is recommended.

Interactions

Urapidil has an additive effect with all antihypertensive agents, which can lead to a hypotonic circulatory status (based on strong blood pressure reduction ). The effect is enhanced by alcohol consumption. When concomitant administration of antihistamine cimetidine of urapidil serum levels may be increased up to 15%.

Pharmacological properties

Pharmacodynamics

Urapidil mediated via blockade of peripheral postsynaptic α1 - receptors, a decrease in vascular resistance and thus a reduction in systolic and diastolic blood pressure. In addition, it stimulates central serotonin receptors of type 5 -HT1A, creating a counter-reaction ( reflex ) prevents the sympathetic nervous system.

Pharmacokinetics

After the intravenous administration enters a two-phase course of the concentration in the serum is initially conditioned by the distribution process and in the second phase, by elimination. Metabolism occurs mainly in the liver, which mainly ineffective metabolites arise. Excretion is about 70% through the kidneys, the remainder fecal. The plasma half-life is 2.7 hours, much longer in liver and kidney disease, so a dose reduction is necessary in this case. Urapidil penetrates the blood -brain barrier and the placenta.

Trade names

Monopreparations: Ebrantil (D, A, CH), Hypotrit (A ) and generic (D).