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{{Drugbox
{{Drugbox
| IUPAC_name       =  
| IUPAC_name = 6-({3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl}amino)-1,3-dimethylpyrimidine-2,4(1''H'',3''H'')-dione
| image            =
| image = Urapidil.png
| CAS_number        =
| ATC_prefix        = C02
| ATC_suffix        = CA06
| PubChem          = 5639&
| DrugBank          =
| chemical_formula  = C20H29N5O3
| molecular_weight  = 387.47596
| bioavailability  =
| protein_bound    =
| metabolism        =
| elimination_half-life =
| excretion        =
| pregnancy_AU      =  <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US      =  <!-- A / B            / C / D / X -->
| pregnancy_category= 
| legal_AU =  <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA =  <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US =  <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status      =
| routes_of_administration =
}}
{{CMG}}


<!--Clinical data-->
| tradename = 
| Drugs.com = {{drugs.com|international|urapidil}}
| pregnancy_category = 
| legal_status = Rx-only
| routes_of_administration = Oral


<!--Pharmacokinetic data-->
| bioavailability = 
| metabolism = 
| elimination_half-life = 
| excretion = 


'''Urapidil''' is a [[sympatholytic]] drug.
<!--Identifiers-->
| CAS_number = 34661-75-1
| CAS_supplemental = <br />64887-14-5 ([[Hydrochloride|HCl]])
| ATC_prefix = C02
| ATC_suffix = CA06
| PubChem = 5639
| ChemSpiderID = 5437
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = A78GF17HJS
| ChEMBL = 279229


<!--Chemical data-->
| C=20 | H=29 | N=5 | O=3
| molecular_weight = 387.48 g/mol
| smiles = O=C1\C=C(/N(C(=O)N1C)C)NCCCN3CCN(c2ccccc2OC)CC3
}}
__NOTOC__
{{SI}}
{{CMG}}


{{Antihypertensives and diuretics}}
==Overview==
'''Urapidil''' is a [[sympatholytic]] [[antihypertensive]] [[drug]]. It acts as an [[alpha-1 adrenoceptor|α<sub>1</sub>-adrenoceptor]] [[receptor antagonist|antagonist]] and as an [[5-HT1A receptor|5-HT<sub>1A</sub> receptor]] [[agonist]]<ref name="pmid1855130">{{cite journal |author=Ramage AG |title=The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors |journal=Br. J. Pharmacol. |volume=102 |issue=4 |pages=998–1002 |date=April 1991 |pmid=1855130 |pmc=1917978 |doi= |url=}}</ref> Although an initial report suggested that urapidil was also an [[alpha-2 adrenoceptor|α<sub>2</sub>-adrenoceptor]] [[agonist]],<ref name="pmid228944">{{cite journal|author=Eltze M |title=Investigations on the mode of action of a new antihypertensive drug, urapidil, in the isolated vas deferens |journal=Eur. J. Pharmacol. |volume=59 |pages=1–9 |year=1979 |doi= 10.1016/0014-2999(79)90018-9|url=|pmid=228944|issue=1–2}}</ref> this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum.<ref name="pmid6097380">{{cite journal |author=Verberne AJM, Rand MJ |title=Pharmacological activities of the antihypertensive drug urapidil in the rat |journal=Clin. Exp. Pharmacol. Physiol. |volume=11 |pages=407–412 |year=1984 |doi= 10.1111/j.1440-1681.1984.tb00289.x|url= |pmid=6097380 |issue=4}}</ref> Unlike some other [[alpha-1 adrenoceptor|α<sub>1</sub>-adrenoceptor]] [[receptor antagonist|antagonists]], urapidil does not elicit reflex tachycardia, and this may be related to its weak [[beta-1 adrenoceptor|β<sub>1</sub>-adrenoceptor]] [[receptor antagonist|antagonist]] activity,<ref name="">{{cite book |author=Schoetensack W, Bruckschen EG, Zech K |title=Urapidil |pages=19 |year=1983 |doi= |url= |work=New Drugs Annual: Cardiovascular Drugs}}</ref><ref name="pmid2984023">{{cite journal |author=Verberne AJM, Rand MJ |title=Effect of urapidil on β-adrenoceptors of rat atria |journal=Eur. J. Pharmacol. |volume=108 |pages=193–196 |year=1985 |doi= 10.1016/0014-2999(85)90725-3|url= |pmid=2984023 |issue=2}}</ref> as well as its effect on cardiac vagal drive.<ref name="pmid1702490">{{cite journal |author=Ramage AG |title=Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity |journal=J. Cardiovasc. Pharmacol. |volume=15 |pages=S75–S85 |year=1990 |doi= |url= |pmid=1702490}}</ref> Urapidil is currently not approved by the [[Food and Drug Administration|U.S. Food and Drug Administration]], but it is available in [[Europe]].


[[de:Urapidil]]
== See Also ==
[[pl:Urapidil]]
* [[Naftopidil]]


== References ==
{{Reflist|2}}


[[Category:Drugs]]
{{Antihypertensives}}
{{Adrenergics}}
{{Serotonergics}}
{{Piperazines}}


{{WH}}
[[Category:Alpha blockers]]
{{WS}}
[[Category:Antihypertensive agents]]
[[Category:Cardiovascular Drugs]]
[[Category:Drug]]

Revision as of 23:25, 24 July 2014

Urapidil
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC20H29N5O3
Molar mass387.48 g/mol
3D model (JSmol)

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist[1] Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist,[2] this was not substantiated in later studies that demonstrated it was devoid of agonist actions in the dog saphenous vein and the guinea-pig ileum.[3] Unlike some other α1-adrenoceptor antagonists, urapidil does not elicit reflex tachycardia, and this may be related to its weak β1-adrenoceptor antagonist activity,[4][5] as well as its effect on cardiac vagal drive.[6] Urapidil is currently not approved by the U.S. Food and Drug Administration, but it is available in Europe.

See Also

References

  1. ↑ Ramage AG (April 1991). "The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors". Br. J. Pharmacol. 102 (4): 998–1002. PMC 1917978. PMID 1855130.
  2. ↑ Eltze M (1979). "Investigations on the mode of action of a new antihypertensive drug, urapidil, in the isolated vas deferens". Eur. J. Pharmacol. 59 (1–2): 1–9. doi:10.1016/0014-2999(79)90018-9. PMID 228944.
  3. ↑ Verberne AJM, Rand MJ (1984). "Pharmacological activities of the antihypertensive drug urapidil in the rat". Clin. Exp. Pharmacol. Physiol. 11 (4): 407–412. doi:10.1111/j.1440-1681.1984.tb00289.x. PMID 6097380.
  4. ↑ Schoetensack W, Bruckschen EG, Zech K (1983). Urapidil. New Drugs Annual: Cardiovascular Drugs. p. 19.
  5. ↑ Verberne AJM, Rand MJ (1985). "Effect of urapidil on β-adrenoceptors of rat atria". Eur. J. Pharmacol. 108 (2): 193–196. doi:10.1016/0014-2999(85)90725-3. PMID 2984023.
  6. ↑ Ramage AG (1990). "Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity". J. Cardiovasc. Pharmacol. 15: S75–S85. PMID 1702490.

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