sympatholytic A sympatholytic (sympathoplegic) drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). They are indicated for various functions; for example, t ...

antihypertensive Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myocardial infa ...

drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.5-HT_1A receptor

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

. Although an initial report suggested that urapidil was also an α₂-adrenoceptor

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

, 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. Unlike some other α₁-adrenoceptor

antagonists An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.tachycardia Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal ...

, and this may be related to its weak β₁-adrenoceptor

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain. as well as its effect on cardiac vagal drive. Urapidil is currently not approved by the

U.S. Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

, but it is available in

Europe Europe is a continent located entirely in the Northern Hemisphere and mostly in the Eastern Hemisphere. It is bordered by the Arctic Ocean to the north, the Atlantic Ocean to the west, the Mediterranean Sea to the south, and Asia to the east ...

.

Medical uses

D/T and reperfusion injuries

Urapidil 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. Urapidil is able to reduce inflammatory response, apoptosis and act as an antioxidant through a variety of pathways. 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. Oxidative stress also plays a vital role in D/T and I/R injuries and is marked by malondialdehyde, or MDA, levels. MDA can also contribute to tissue damage, particularly by encouraging polymerization and cross-linking of the membranes of the affected cells. 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. Both SOD and GPx help to counteract the negative effects of ROS which injures tissue through lipid peroxidation and by damaging DNA. 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. Urapidil 25mg-5ml vials yellow background

Urapidil 25mg-5ml vials yellow background

References

{{Piperazines 5-HT1A agonists Alpha-1 blockers Beta blockers Chemical substances for emergency medicine Piperazines Lactams Pyrimidines 2-Methoxyphenyl compounds

Medical uses

D/T and reperfusion injuries

See also

References