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.
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral |
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| ECHA InfoCard | 100.047.377 |
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| Formula | C20H29N5O3 |
| Molar mass | 387.484 g·mol−1 |
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Medical uses
editD/T and reperfusion injuries
editUrapidil has been determined to aid in the recovery of torsion detorsion (T/D) injuries in ovaries and testes, as well as ischemia-reperfusion (I/R) renal injuries. Both of these conditions are directly associated with one another as T/D injuries commonly lead to ischemia, or the lack of blood flow.[7][8][9] Urapidil is able to reduce inflammatory response, apoptosis and act as an antioxidant through a variety of pathways.[8] During the detorsion phase of an injury, reperfusion, or the restoration of blood flow is important, but can also cause injuries to the affected tissue through apoptosis and the generation of ROS.[8][7] Oxidative stress also plays a vital role in D/T and I/R injuries and is marked by malondialdehyde, or MDA, levels.[7][9] MDA can also contribute to tissue damage, particularly by encouraging polymerization and cross-linking of the membranes of the affected cells.[8] Through various studies performed within the past decade, it has been found that urapidil can treat T/D and I/R injuries, particularly stemming from autophagy, apoptosis, and inflammation, by elevating levels of SOD, TAS, and GPx within the cell.[8][9] Both SOD and GPx help to counteract the negative effects of ROS which injures tissue through lipid peroxidation and by damaging DNA.[8] Additionally, urapidil has the ability to counteract autophagy by lowering the quantity of autophagosome marker LC3B and caspase-3 which also plays a critical role in autophagy regulation.[8]
See also
editReferences
edit- ^ Ramage AG (April 1991). "The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors". British Journal of Pharmacology. 102 (4): 998–1002. doi:10.1111/j.1476-5381.1991.tb12290.x. PMC 1917978. PMID 1855130.
- ^ Eltze M (October 1979). "Investigations on the mode of action of a new antihypertensive drug, urapidil, in the isolated rat vas deferens". European Journal of Pharmacology. 59 (1–2): 1–9. doi:10.1016/0014-2999(79)90018-9. PMID 228944.
- ^ Verberne AJ, Rand MJ (1984). "Pharmacological activities of the antihypertensive drug urapidil in the rat". Clinical and Experimental Pharmacology & Physiology. 11 (4): 407–411. doi:10.1111/j.1440-1681.1984.tb00289.x. PMID 6097380. S2CID 22522953.
- ^ Schoetensack W, Bruckschen EG, Zech K (1983). "Urapidil". New Drugs Annual: Cardiovascular Drugs. p. 19.
- ^ Verberne AJ, Rand MJ (January 1985). "Effect of urapidil on beta-adrenoceptors of rat atria". European Journal of Pharmacology. 108 (2): 193–196. doi:10.1016/0014-2999(85)90725-3. PMID 2984023.
- ^ Ramage AG (1990). "Influence of 5-HT1A receptor agonists on sympathetic and parasympathetic nerve activity". Journal of Cardiovascular Pharmacology. 15 (Suppl 7): S75–S85. doi:10.1097/00005344-199001001-00010. PMID 1702490.
- ^ a b c Erdoğan DG, Tanyeli A, Güler MC, Eraslan E, Çomaklı S, Doğanay S (2022). "Beneficial Effects of Urapidil against Renal Ischemia Reperfusion-Related Renal Injury". Southern Clinics of Istanbul Eurasia. 33 (2): 198–202. doi:10.14744/scie.2022.89421.
- ^ a b c d e f g Güler MC, Tanyeli A, Erdoğan DG, Eraslan E, Çomaklı S, Polat E, et al. (July 2021). "Urapidil alleviates ovarian torsion detorsion injury via regulating oxidative stress, apoptosis, autophagia, and inflammation". Iranian Journal of Basic Medical Sciences. 24 (7): 935–942. doi:10.22038/ijbms.2021.57196.12736. PMC 8528257. PMID 34712424.
- ^ a b c Meštrović J, Pogorelić Z, Drmić-Hofman I, Vilović K, Todorić D, Popović M (March 2017). "Protective effect of urapidil on testicular torsion-detorsion injury in rats". Surgery Today. 47 (3): 393–398. doi:10.1007/s00595-016-1388-3. PMID 27444029.