生物活性

• 描述Prazosin Hydrochloride, an a1-adrenoceptor blocker, has shown some promise in treating chronic PTSD (Posttraumatic stress disorder). Treatment of PTSD with prazosin is usually initiated at a dose of 1 mg, with monitoring for hypotension after the first dose. The dose is then gradually increased to maintenance levels of 2-6 mg at night^[3]. Prazosin has been shown to be effective in the treatment of PTSD trauma-related nightmares, with low side effect profile and abilities to improve both sleep and reduce trauma nightmares^[4]. Prazosin is extensively metabolised by the liver and has high first-pass metabolism and low oral bioavailability. Oral bioavailability of prazosin ranges from 43.5 to 69.3% (mean 56.9%). Prazosin is highly (92 to 97%) bound to human plasma proteins (albumin and alpha 1-acid glycoprotein) and the extent of binding is independent of the plasma concentration of the drug in the range of 20 to 150 ng/mL^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01677767	-	-	Completed	-	India ... more >> Sir Gangaram Hospital New Delhi, Delhi, India, 110060 Ahmedabad Dialysis Centre Ahmedabad, India, 380005 Excel Center Guwahati, India, 781007 ESIS Hospital; Department of Nephrology Kolkata, India, 600054 Vertex Hospital Mumbai, India, 400083 Apollo Indraprastha Hospitals; Nephrology New Delhi, India, 110076 Aditya Birla Memorial Hospital Pune, India, 411033 Collapse <<
  NCT00687388	Benign Prostatic Hyperplasia	Phase 4	Withdrawn(in order to prepare ... more >>a new clinical trial to evaluate with pathological change) Collapse <<	-	Korea, Republic of ... more >> Severance Hospital Seoul, Korea, Republic of, 120-752 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Asan Medical Center Seoul, Korea, Republic of, 138-736 Collapse <<
  NCT01030874	Orthostatic Hypotension ... more >> Falls Collapse <<	Not Applicable	Completed	-	United States, Oregon ... more >> VA Portland Health Care System, Portland, OR Portland, Oregon, United States, 97239 Collapse <<

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• 参考文献

• [1] Baum O, Da Silva-Azevedo L, et al. Endothelial NOS is main mediator for shear stress-dependent angiogenesis in skeletal muscle after prazosin administration. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2300-8.

  [2] Yu CX, Zhu CB, et al. Selective MT(2) melatonin receptor antagonist blocks melatonin-induced antinociception in rats. Neurosci Lett. 2000 Mar 24;282(3):161-4.

  [3] Green B. Prazosin in the treatment of PTSD. J Psychiatr Pract. 2014;20(4):253-259

  [4] Breen A, Blankley K, Fine J. The efficacy of prazosin for the treatment of posttraumatic stress disorder nightmares in U.S. military veterans. J Am Assoc Nurse Pract. 2017;29(2):65-69

  [5] Jaillon P. Clinical pharmacokinetics of prazosin. Clin Pharmacokinet. 1980;5(4):365-376

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