Urapidil
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Non-proprietary name | Urapidil | |||||||||||||||||||||
other names |
6- {3- [4- (2-methoxyphenyl) -1-piperazinyl] propyl} amino-1,3-dimethyl-2,4 (1 H , 3 H -pyrimidinedion) |
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Molecular formula | C 20 H 29 N 5 O 3 | |||||||||||||||||||||
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Molar mass | 387.48 g · mol -1 | |||||||||||||||||||||
Physical state |
firmly |
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Melting point |
156-158 ° C |
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solubility |
Water: 157 mg l −1 at 25 ° C |
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Toxicological data | ||||||||||||||||||||||
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Urapidil is an antihypertensive agent (an antihypertensive agent) from the group of α 1 -adrenoceptor - antagonist , acts primarily on arterial vasodilator (vasodilator), and is primarily in acute blood pressure increases used.
Clinical information
application
Urapidil ( intravenous ) is an alternative to calcium antagonists and nitrates in doses administered via the vein in adults of 10 to 50 mg and more in the hypertensive crisis . Orally it can be used in combination therapy for arterial hypertension .
side effect
Side effects are often (1–10%) nausea , headache and dizziness , rarely (<1%) arrhythmias , fatigue and sweating .
Contraindications
During pregnancy and lactation is contraindicated urapidil. However, it is often used as an "off-label" therapy in pregnancy, especially with long-term administration and under perfusor-controlled administration against manifested preeclampsia . In this 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 situation (excessive decrease in blood pressure). The effect is also increased by drinking alcohol . If the antihistamine cimetidine is administered at the same time , the urapidil serum level can be increased by up to 15%.
Pharmacological properties
Pharmacodynamics
By blocking peripheral, postsynaptic α 1 receptors, Urapidil mediates a decrease in vascular resistance and thus a decrease in systolic and diastolic blood pressure. In addition, it stimulates central serotonin receptors of the 5-HT 1A type , which prevents an adverse reaction ( reflex tachycardia ) of the sympathetic nervous system .
Pharmacokinetics
After intravenous administration, a two-phase course of the concentration in the serum occurs, which is initially caused by distribution processes and in the second phase by elimination. The metabolism takes place mainly in the liver , whereby mainly ineffective metabolites are formed. About 70% of the excretion takes place via the kidneys , the rest in the faeces. The plasma half-life is 2.7 hours, much longer in liver and kidney diseases, which is why a dose reduction is necessary in this case. Urapidil penetrates the blood-brain barrier and crosses the placenta .
Trade names
Monopreparations : Ebrantil (D, A, CH), Hypotrit (A), Eupressyl (F), Mediatensyl (F) and Generika (D).
literature
- Karow, Lang-Roth: General and special pharmacology and toxicology. 14th edition 2005. Self-published.
- Instructions for use and specialist information Ebrantil ® , Altana Pharma, 2002.
Web links
Individual evidence
- ↑ a b c Entry on urapidil in the ChemIDplus database of the United States National Library of Medicine (NLM) .
- ↑ a b data sheet Urapidil hydrochloride from Sigma-Aldrich , accessed on April 25, 2011 ( PDF ).
- ↑ Reinhard Larsen: Anesthesia and intensive medicine in cardiac, thoracic and vascular surgery. (1st edition 1986) 5th edition. Springer, Berlin / Heidelberg / New York et al. 1999, ISBN 3-540-65024-5 , p. 69.
- ↑ Specialist information Ebrantil ® , as of June 2009.