生物活性

• 描述Phentolamine mesylate (OraVerse), a nonselective a-adrenergic blocking drug, is the first therapeutic agent marketed for the reversal of soft-tissue anaesthesia and the associated functional deficits resulting from an intraoral submucosal injection of a local anaesthetic containing a vasoconstrictor^[3]. Phentolamine mesylate (PM) is widely used to reverse local anesthesia after dental procedures. PM substantially reduced the time to recovery of normal sensation and function after local anesthesia in routine dental treatment^[4]. Phentolamine leads to an increase in FBM (fetal breathing movements) by preferentially antagonizing presynaptic alpha 2-adrenoreceptors over postsynaptic alpha 1-adrenoreceptors. This influence of phentolamine on FBM may be secondary to its effect on ECoG (electrocortical activity). Promotion of LV-ECoG by catecholamines is mediated via an alpha 1-independent mechanism^[5]. Phentolamine mesylate, at dosages from 0.4 to 0.8 mg in adults and adolescents and at dosages from 0.2 to 0.4 mg in children aged 4 to 11 years, has been proven to be safe. Its ability to block a-adrenergic receptors on blood vessels induces vasodilation and enhances the redistribution of the local anesthetic away from the injection site^[6].
• 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
  NCT03240822	Urologic Injuries ... more >> Genital Diseases, Male Amputation Collapse <<	Phase 1	Recruiting	December 2025	United States, North Carolina ... more >> Wake Forest School of Medicine Recruiting Winston-Salem, North Carolina, United States, 27104 Contact: Mary-Clare Day, RN BSN    336-713-1343    Mday@wakehealth.edu Collapse <<
  NCT01422616	Ischemic Stroke ... more >> High Blood Pressure Collapse <<	Phase 3	Recruiting	February 2019	Australia, New South Wales ... more >> Royal Prince Alfred Hospital Recruiting Sydney, New South Wales, Australia, 2050 Contact: Craig S Anderson, MD    +61 2 933 4500    canderson@georgeinstitute.org.au Collapse <<
  NCT00226096	CVA (Cerebrovascular Accident)... more >> Cerebral Hemorrhage Intracranial Hemorrhages Collapse <<	Not Applicable	Completed	-	Australia, New South Wales ... more >> Concord Hospital Concord, New South Wales, Australia, 2138 Gosford Hospital Gosford, New South Wales, Australia, 2250 St George Hospital Kogarah, New South Wales, Australia, 2217 John Hunter Hospital Newcastle, New South Wales, Australia, 2310 St Vincent's Hospital Sydney, New South Wales, Australia, 2010 Royal Prince Alfred Hospital Sydney, New South Wales, Australia, 2050 Westmead Hospital Westmead, New South Wales, Australia, 2145 Australia, South Australia Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 Australia, Victoria Royal Melbourne Hospital Melbourne, Victoria, Australia, 3050 St Vincent's Hospital Melbourne, Victoria, Australia, 3065 Box Hill Hospital Melbourne, Victoria, Australia, 3128 Alfred Hospital Melbourne, Victoria, Australia, 3181 Austin Health Melbourne, Victoria, Australia Monash Medical Centre Melbourne, Victoria, Australia Australia, Western Australia Sir Charles Gairdner Hospital Perth, Western Australia, Australia, 6009 China Regional Coordinating Centre: Peking University First Hospital Beijing, China, 100034 Hospitals in China, c/o The George Institute China Beijing, China Regional Coordinating Centre: Centre for Epidemiological Studies and Clinical Trials, Ruijin Hospital, Shanghai Institute of Hypertension, Shanghai Second Medical University Shanghai, China, 200025 New Zealand North Shore Hospital Auckland, New Zealand Christchurch Hospital Christchurch, New Zealand Collapse <<

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• 参考文献

• [1] Moore PA, Hersh EV, et al. Pharmacokinetics of lidocaine with epinephrine following local anesthesia reversal with phentolamine mesylate. Anesth Prog. 2008 Summer;55(2):40-8.

  [2] Traish A, Gupta S, et al. Phentolamine mesylate relaxes penile corpus cavernosum tissue by adrenergic and non-adrenergic mechanisms. Int J Impot Res. 1998 Dec;10(4):215-23.

  [3] Yagiela JA. What's new with phentolamine mesylate: a reversal agent for local anaesthesia?. SAAD Dig. 2011;27:3-7

  [4] Daubländer M, Liebaug F, Niedeggen G, Theobald K, Kürzinger ML. Effectiveness and safety of phentolamine mesylate in routine dental care. J Am Dent Assoc. 2017;148(3):149-156

  [5] Giussani DA, Moore PJ, Bennet L, Spencer JA, Hanson MA. Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero. J Physiol. 1995;486 (Pt 1)(Pt 1):249-255

  [6] Hersh EV, Lindemeyer RG. Phentolamine mesylate for accelerating recovery from lip and tongue anesthesia. Dent Clin North Am. 2010;54(4):631-642

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