phenoxybenzamine

Summary

Summary: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.

Top Publications

  1. Vaidyanathan S, Mansour P, Soni B, Hughes P, Singh G. Chronic lymphocytic leukaemia, synchronous small cell carcinoma and squamous neoplasia of the urinary bladder in a paraplegic man following long-term phenoxybenzamine therapy. Spinal Cord. 2006;44:188-91 pubmed
    ..A case report...
  2. Motta P, Mossad E, Toscana D, Zestos M, Mee R. Comparison of phenoxybenzamine to sodium nitroprusside in infants undergoing surgery. J Cardiothorac Vasc Anesth. 2005;19:54-9 pubmed
    ..to compare the effects of a direct-acting arterial dilator, sodium nitroprusside, to an alpha-adrenergic receptor blocker, phenoxybenzamine, in infants with congenital heart defects undergoing cardiac repairs on cardiopulmonary bypass.
  3. Inchiosa M, Kizelshteyn G. Treatment of complex regional pain syndrome type I with oral phenoxybenzamine: rationale and case reports. Pain Pract. 2008;8:125-32 pubmed publisher
    The nonselective alpha-adrenergic antagonist, phenoxybenzamine, has been used in the treatment of neuropathic pain syndromes, specifically, complex regional pain syndrome (CRPS) types I and II...
  4. Mussa S, Guzik T, Black E, Dipp M, Channon K, Taggart D. Comparative efficacies and durations of action of phenoxybenzamine, verapamil/nitroglycerin solution, and papaverine as topical antispasmodics for radial artery coronary bypass grafting. J Thorac Cardiovasc Surg. 2003;126:1798-805 pubmed
    ..b>Phenoxybenzamine, verapamil/nitroglycerin solution, and papaverine have been advocated as topical antispasmodic agents...
  5. Te A. A modern rationale for the use of phenoxybenzamine in urinary tract disorders and other conditions. Clin Ther. 2002;24:851-61; discussion 837 pubmed
    b>Phenoxybenzamine (PBZ) is a nonselective, irreversible alpha-adrenergic receptor antagonist that is approved for the treatment of diaphoresis and hypertension associated with pheochromocytoma...
  6. Chang M, Smith S, Thorpe A, Barratt M, Karim F. Evaluation of phenoxybenzamine in the CFA model of pain following gene expression studies and connectivity mapping. Mol Pain. 2010;6:56 pubmed publisher
    ..The aim of this study was to identify genes altered in this model of osteoarthritic pain and use this information to infer analgesic potential of compounds based on their own gene expression profiles using the Connectivity Map approach...
  7. Guzzetta N. Phenoxybenzamine in the treatment of hypoplastic left heart syndrome: a core review. Anesth Analg. 2007;105:312-5 pubmed
    ..An emerging treatment strategy aimed at improving early mortality is the intraoperative administration of phenoxybenzamine, a profound systemic vasodilator...
  8. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A. Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001;276:31279-84 pubmed
    b>Phenoxybenzamine (PB), a classical alpha-adrenergic antagonist, binds irreversibly to the alpha-adrenergic receptors (ARs)...
  9. Tweddell J, Hoffman G, Fedderly R, Berger S, Thomas J, Ghanayem N, et al. Phenoxybenzamine improves systemic oxygen delivery after the Norwood procedure. Ann Thorac Surg. 1999;67:161-7; discussion 167-8 pubmed
    ..We hypothesized that phenoxybenzamine could achieve a balanced circulation through reduction of systemic vascular resistance.

More Information

Publications62

  1. Parkash J, Kaur G. Potential of PSA-NCAM in neuron-glial plasticity in the adult hypothalamus: role of noradrenergic and GABAergic neurotransmitters. Brain Res Bull. 2007;74:317-28 pubmed
    ..was studied in the proestrous phase of cycling rats treated with alpha-adrenergic receptor blocker phenoxybenzamine (PBZ) and gamma-aminobutyric acid (GABA) by using dual immunohistofluorescent staining and Western blot ..
  2. Kasturi S, Kutikov A, Guzzo T, Smith A, Wein A. Modern management of pheochromocytoma. Nat Clin Pract Urol. 2007;4:630-3 pubmed
    ..A 55-year-old male with poorly controlled hypertension and a history of coronary artery disease presented with a large adrenal mass. The patient also reported a long-standing history of profuse sweating, tinnitus, vomiting and headaches...
  3. Miakotina O, Agassandian M, Shi L, Look D, Mallampalli R. Adenovirus stimulates choline efflux by increasing expression of organic cation transporter-2. Am J Physiol Lung Cell Mol Physiol. 2005;288:L93-102 pubmed
    ..Cells were active in pH-sensitive, reversible transport of choline, a process blocked pharmacologically with phenoxybenzamine, an inhibitor of organic cation transporters (OCT)...
  4. Donoso M, Miranda R, Briones R, Irarrazaval M, Huidobro Toro J. Release and functional role of neuropeptide Y as a sympathetic modulator in human saphenous vein biopsies. Peptides. 2004;25:53-64 pubmed
    ..While guanethidine reduced the overflow of ir-NPY, phenoxybenzamine did not augment NPY release, but increased that of noradrenaline...
  5. Nettesheim O, Hoffken G, Gahr M, Breidert M. [Haematemesis and dysphagia in a 20-year-old woman with congenital spine malformation and situs inversus partialis]. Z Gastroenterol. 2003;41:319-24 pubmed
    ..Drug history revealed that the patient had been treated with the alpha-receptor blocking drug phenoxybenzamine over at least 12 years for bladder dysfunction...
  6. Nakazato Y, Sekine H, Isogaya M, Ito S, Ohga A. Atropine- and hexamethonium-resistant motor response to greater splanchnic nerve stimulation in the dog stomach. J Auton Nerv Syst. 1987;20:35-42 pubmed
    ..This contraction was abolished or reversed to a relaxation after intravenous injection of atropine and phenoxybenzamine. When hexamethonium was further administered, a long lasting contraction appeared in response to the greater ..
  7. Donnerer J, Lembeck F. Heat loss reaction to capsaicin through a peripheral site of action. Br J Pharmacol. 1983;79:719-23 pubmed
    ..application of capsaicin to the nerves of the hind leg and by their chronic denervation, by treatment with phenoxybenzamine and guanethidine, evidence was obtained that reflex withdrawal of sympathetic vasoconstrictor tone mediates ..
  8. Telegdy G, Tiricz H, Adamik A. Involvement of neurotransmitters in urocortin-induced passive avoidance learning in mice. Brain Res Bull. 2005;67:242-7 pubmed
    ..The following receptor antagonists blocked the action of urocortin on consolidation: haloperidol, atropine, phenoxybenzamine, bicuculline, the CRF antagonist CRF9-41 and methysergide...
  9. Jia J, Zeng X, Li Y, Ma S, Bai J. Ephedrine induced thioredoxin-1 expression through ?-adrenergic receptor/cyclic AMP/protein kinase A/dopamine- and cyclic AMP-regulated phosphoprotein signaling pathway. Cell Signal. 2013;25:1194-201 pubmed publisher
    ..induced Trx-1 expression, which was inhibited by propranolol (?-adrenergic receptor inhibitor), but not by phenoxybenzamine (?-adrenergic receptor inhibitor) in rat pheochromocytoma PC12 cells...
  10. Akema T, Chiba A, Kimura F. On the relationship between noradrenergic stimulatory and GABAergic inhibitory systems in the control of luteinizing hormone secretion in female rats. Neuroendocrinology. 1990;52:566-72 pubmed
    ..c.v. injection of NA in estrogen-primed rats. On the other hand, blockade of alpha-adrenergic receptors by phenoxybenzamine did not interfere with the stimulatory effect of an i.c.v. injection of a GABAA antagonist bicuculline...
  11. Feitelson J, Kulenovic E, Beck D, Harris P, Passmore J, Malkani A, et al. Endogenous norepinephrine regulates blood flow to the intact rat tibia. J Orthop Res. 2002;20:391-6 pubmed
    ..Blockade of alpha-adrenergic receptors with phentolamine or phenoxybenzamine attenuated by more than 50% the norepinephrine-induced decrease in bone blood flow...
  12. Cadirci E, Suleyman H, Hacimuftuoglu A, Halici Z, Akcay F. Indirect role of beta2-adrenergic receptors in the mechanism of analgesic action of nonsteroidal antiinflammatory drugs. Crit Care Med. 2010;38:1860-7 pubmed publisher
    ..This study investigates whether the analgesic effects of indomethacin, diclofenac sodium, aspirin, and nimesulide (IDAN; upper case letters of the four drugs we used) are also related to adrenal gland hormones...
  13. Kawarai M, Koss M. Sympathetic control of nasal blood flow in the rat mediated by alpha(1)-adrenoceptors. Eur J Pharmacol. 2001;413:255-62 pubmed
    ..intravenous treatment with the non-selective alpha-adrenoceptor antagonists, phentolamine (5 mg kg(-1)) and phenoxybenzamine (2 mg kg(-1)), as well as with the selective alpha(1)-adrenoceptor antagonist, prazosin (300 microg kg(-1))...
  14. van der Graaf P, Danhof M. On the reliability of affinity and efficacy estimates obtained by direct operational model fitting of agonist concentration-effect curves following irreversible receptor inactivation. J Pharmacol Toxicol Methods. 1997;38:81-5 pubmed
    ..underscored with the analysis of experimental data obtained from the interaction between noradrenaline and phenoxybenzamine in rat isolated aorta...
  15. Asuar Aydillo S. [Current role of intracavernous therapy in the treatment of erectile dysfunction]. Arch Esp Urol. 2002;55:475-82 pubmed
  16. Emerson C, Rainbird A. Use of a 'hospital-at-home' service for patient optimization before resection of phaeochromocytoma. Br J Anaesth. 2003;90:380-2 pubmed
    ..We present a patient with a phaeochromocytoma who was successfully managed preoperatively with phenoxybenzamine in the community by a 'hospital-at-home' service...
  17. Pai R, Conant A, Dihmis W. Treatment with phenoxybenzamine may lead to loss of endothelial viability in radial artery. Ann Thorac Surg. 2008;86:350-1; author reply 351-2 pubmed publisher
  18. Takayanagi I, Ohtsuki H, Saito K, Koike K, Satoh M. Propylbenzilycholine mustard (PrBCM)-sensitive cholinoceptors and contractile response to partial agonist in guinea pig ileal muscle. Jpn J Pharmacol. 1991;56:151-8 pubmed
    ..Carbachol behaves as a partial agonist in the preparation treated with phenoxybenzamine and mainly activates PrBCM-sensitive cholinoceptors, as phenoxybenzamine preferably blocks PrBCM-resistant ..
  19. van der Graaf P, Stam W. Analysis of receptor inactivation experiments with the operational model of agonism yields correlated estimates of agonist affinity and efficacy. J Pharmacol Toxicol Methods. 1999;41:117-25 pubmed
    ..For this purpose, the interaction between noradrenaline and phenoxybenzamine was studied in rat small mesenteric artery using a paired-curve design...
  20. De Oliveira N, Ashburn D, Khalid F, Burkhart H, Adatia I, Holtby H, et al. Prevention of early sudden circulatory collapse after the Norwood operation. Circulation. 2004;110:II133-8 pubmed
    ..The current study examines early outcomes after the Norwood operation in our unit in an attempt to identify variables that may have altered the risk of unexpected circulatory collapse...
  21. Scholten A, Cisco R, Vriens M, Cohen J, Mitmaker E, Liu C, et al. Pheochromocytoma crisis is not a surgical emergency. J Clin Endocrinol Metab. 2013;98:581-91 pubmed publisher
    ..Pheochromocytoma crisis is a feared and potentially lethal complication of pheochromocytoma...
  22. Sabath L, Cornelissen G, Halberg F, Stoynev A, Ikonomov O, Otsuka K. Circadian hypo- and hyper-amplitude-tension (CHAT) associated with putative pheochromocytoma and 12-hourly phenoxybenzamine treatment. Biomed Pharmacother. 2004;58 Suppl 1:S99-106 pubmed
    ..15- to 60-minute intervals over several days, with interruptions, before and after the institution of 10 mg phenoxybenzamine per os every 12 hours (between 7:30 and 8:00 and between 19:30 and 20:00), with continued monitoring over ..
  23. Welch B, Atwell T, Nichols D, Wass C, Callstrom M, Leibovich B, et al. Percutaneous image-guided adrenal cryoablation: procedural considerations and technical success. Radiology. 2011;258:301-7 pubmed publisher
    ..To assess safety, technical success, complications, and hemodynamic changes associated with the adrenal cryoablation procedure...
  24. Telegdy G, Adamik A. The action of orexin A on passive avoidance learning. Involvement of transmitters. Regul Pept. 2002;104:105-10 pubmed
    ..The following receptor blockers were used: haloperidol, phenoxybenzamine, propranolol, atropine, bicuculline, naloxone and nitro-L-arginine, which can block nitric oxide synthase...
  25. Mihai R, Sadler G, Bridge H. Adrenergic blockade with phenoxybenzamine and propranolol in a cohort of 60 patients undergoing surgery for phaeochromocytoma. Eur J Anaesthesiol. 2008;25:508-10 pubmed publisher
  26. Raasch W, Jungbluth B, Schäfer U, Häuser W, Dominiak P. Norepinephrine release is reduced by I(1)-receptors in addition to alpha(2)-adrenoceptors. Ann N Y Acad Sci. 2003;1009:270-3 pubmed
    ..overflow was diminished by moxonidine even when alpha(2)-adrenoceptors were blocked quantitatively using phenoxybenzamine, suggesting an I(1)-receptor-mediated mechanism of noradrenaline release...
  27. Bruynzeel H, Feelders R, Groenland T, van den Meiracker A, van Eijck C, Lange J, et al. Risk Factors for Hemodynamic Instability during Surgery for Pheochromocytoma. J Clin Endocrinol Metab. 2010;95:678-85 pubmed publisher
    ..In addition, efficacy of pretreatment with the alpha-adrenergic receptor (alpha) antagonists phenoxybenzamine (PXB) and doxazosin (DOX) was compared with respect to reduction of intraoperative HD instability.
  28. Li J, French B, Fu P, Bardag Gorce F, French S. Catecholamines are involved in the mechanism of the urinary alcohol level cycle in rats fed ethanol intragastrically at a constant rate. Life Sci. 2004;75:3043-51 pubmed
    ..Propranolol, a beta adrenergic blocker, attenuated the amplitude of the cycle. Phenoxybenzamine, an alpha blocker disrupted the cycle and elevated ethanol to fatal levels...
  29. Zhang C, Hsueh W. PAF-induced bowel necrosis. Effects of vasodilators. Dig Dis Sci. 1991;36:634-40 pubmed
    ..We thus studied the effects of vasodilators in this model. We found that: (1) Phenoxybenzamine, prazosin, ICI 198615 (leukotriene antagonist) and PGE1 counteracted the PAF-induced mesenteric flow ..
  30. Tarasova O, Sjöblom Widfeldt N, Nilsson H. Transmitter characteristics of cutaneous, renal and skeletal muscle small arteries in the rat. Acta Physiol Scand. 2003;177:157-66 pubmed
  31. Conant A, Shackcloth M, Oo A, Chester M, Simpson A, Dihmis W. Phenoxybenzamine treatment is insufficient to prevent spasm in the radial artery: the effect of other vasodilators. J Thorac Cardiovasc Surg. 2003;126:448-54 pubmed
    ..Recently the use of the irreversible alpha-adrenergic antagonist phenoxybenzamine has been proposed...
  32. Amobi N, Guillebaud J, Kaisary A, Lloyd Davies R, Turner E, Smith I. Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens. Eur J Pharmacol. 2003;462:169-77 pubmed
    ..The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]..
  33. Pinto J, Assanasen P, Baroody F, Naureckas E, Naclerio R. Alpha-adrenoreceptor blockade with phenoxybenzamine does not affect the ability of the nose to condition air. J Appl Physiol (1985). 2005;99:128-33 pubmed
    ..capacity, we raised the temperature through alpha-adrenoreceptor blockade by intranasally administering phenoxybenzamine. We hypothesized that blocking alpha-adrenoreceptors during inhalation of cold, dry air would lead to an ..
  34. Toda H, Maruyama H, Budgell B, Kurosawa M. Responses of dorsal spinal cord blood flow to noxious mechanical stimulation of the skin in anesthetized rats. J Physiol Sci. 2008;58:263-70 pubmed publisher
    ..The responses of SCBF to pinching of the ipsilateral hindpaw persisted both after treatment with phenoxybenzamine and after spinalization at the C1-2 level, whereas the responses to pinching at other sites disappeared...
  35. Sato M, Kawatani M. Effects of noradrenaline on cytosolic concentrations of Ca(2+) in cultured corpus cavernosum smooth muscle cells of the rabbit. Neurosci Lett. 2002;324:89-92 pubmed
    ..The NA (10 microM)-induced [Ca2+]i increase was dose-dependently inhibited by phenoxybenzamine (1 nM-1 microM). The inhibition was 71% at 0.1 microM and was completely made at 1 microM...
  36. Weintraub Z, Alvaro R, Baier R, Cates D, Nowaczyk B, Martino C, et al. Effect of norepinephrine on fetal breathing in sheep. Biol Neonate. 1998;73:60-8 pubmed
    ..could enhance fetal breathing during administration of oxygen, or 100% O2 plus cord occlusion, and if phenoxybenzamine would reverse these changes...
  37. Martinez Arizala A, Holaday J, Long J. Cardiovascular responses to intrathecal vasopressin in conscious and anesthesized rats. Am J Physiol. 1989;256:R193-200 pubmed
    ..administration of the V1-receptor antagonist d(CH2)5[Tyr(Me)2]AVP (V1-ANT) but are not blocked by intravenous phenoxybenzamine, hexamethonium, or [Sar1, Thr8]angiotensin II, an angiotensin II antagonist...
  38. Rau T, Kothiwal A, Rova A, Rhoderick J, Poulsen D. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int J Mol Sci. 2014;15:1402-17 pubmed publisher
    b>Phenoxybenzamine (PBZ) is an FDA approved ?-1 adrenergic receptor antagonist that is currently used to treat symptoms of pheochromocytoma. However, it has not been studied as a neuroprotective agent for traumatic brain injury (TBI)...
  39. Yu Y, Koss M. Alpha2-adrenoceptors do not mediate reflex mydriasis in rabbits. J Ocul Pharmacol Ther. 2004;20:479-88 pubmed
    ..The alpha-adrenergic antagonist, phenoxybenzamine (0.3 mg/kg, intravenously (i.v...
  40. Drummond P. The effect of sympathetic activity on thermal hyperalgesia in capsaicin-treated skin during body cooling and warming. Eur J Pain. 2001;5:59-67 pubmed
    ..To investigate this issue, the noncompetitive alpha-(alpha) adrenergic antagonist phenoxybenzamine was introduced by iontophoresis into the skin of 16 healthy volunteers either before or after the topical ..
  41. Hocking B, Westerman R. Radiofrequency electrocution (196 MHz). Occup Med (Lond). 1999;49:459-61 pubmed
    ..His symptoms were partly alleviated with ultra-sound therapy, phenoxybenzamine and glyceryl trinitrate patches locally applied, but after several months he continues to have some symptoms...
  42. Martin J, Knuepfer M, Beinfeld M, Westfall T. Mechanism of pressor response to posterior hypothalamic injection of neuropeptide Y. Am J Physiol. 1989;257:H791-8 pubmed
    ..Pretreatment of rats with 2.0 mg/kg (iv) of phenoxybenzamine, or 7...
  43. Van Maanen E, Banning J, Roebel L, Morgan J. Dopamine and norepinephrine increase venous return by stimulating alpha and beta adrenoceptors in the dog. J Cardiovasc Pharmacol. 1988;11:627-34 pubmed
    ..b>Phenoxybenzamine virtually abolished the venous responses to the lowest doses of both agonists and diminished the venous ..
  44. Darroch S, Gardner A, Vong Y, Choo L, Mitchelson F. Effect of temperature reduction on responsiveness to cholinomimetics in the taenia caeci of the guinea-pig. J Auton Pharmacol. 1991;11:109-19 pubmed
    ..was similar to the KA value for the partial agonist obtained in experiments with the irreversible antagonist phenoxybenzamine (2.5 microM). It was also similar to the KB value determined at 18 degrees C (3...
  45. Oo A, Conant A, Chester M, Dihmis W, Simpson A. Temperature changes stimulate contraction in the human radial artery and affect response to vasoconstrictors. Ann Thorac Surg. 2007;83:126-32 pubmed
    ..necessitating the routine use of topically applied vasodilators, such as glyceryl trinitrate, papaverine, phenoxybenzamine, or calcium channel antagonists, in theatre...
  46. Dugas G, Fuller J, Singh S, Watson J. Pheochromocytoma and pregnancy: a case report and review of anesthetic management. Can J Anaesth. 2004;51:134-8 pubmed
    ..To describe a patient diagnosed with pheochromocytoma in the third trimester of pregnancy and discuss the perioperative and anesthetic management...
  47. Pérez Rivera A, Fink G, Galligan J. Increased reactivity of murine mesenteric veins to adrenergic agonists: functional evidence supporting increased alpha1-adrenoceptor reserve in veins compared with arteries. J Pharmacol Exp Ther. 2004;308:350-7 pubmed
    ..in veins was due to a greater alpha-adrenoceptor reserve, vessels were incubated with the alkylating agent phenoxybenzamine (PBZ; 0.3, 3, 10, and 30 nM)...
  48. Miller A, Glasel J. Comparative sequence and immunochemical analyses of murine monoclonal anti-morphine antibodies. J Mol Biol. 1989;209:763-78 pubmed
    ..The possible importance of additional contact amino acids, tryptophan, aspartic and/or glutamic acids, is discussed...
  49. Habbe N, Ruger F, Bojunga J, Bechstein W, Holzer K. Urapidil in the preoperative treatment of pheochromocytomas: a safe and cost-effective method. World J Surg. 2013;37:1141-6 pubmed publisher
    ..Perioperative ?1-receptor-blockade with orally administered phenoxybenzamine or intravenous urapidil therefore is a standard procedure in the treatment regime prior to surgery.
  50. Braga F, Mota I. Homologous passive cutaneous anaphylaxis (PCA) in mice and heterologous PCA induced in rats with mouse IgE. Immunology. 1976;30:655-69 pubmed
    ..This fact seems to indicate that the physiological mechanism operating in mouse mast cells are different from those operating in rat mast cells...
  51. Pan D, Li H, Zeng Z. [The discussion of standards for clinical functional gradation and preoperative preparation of pheochromocytoma]. Zhonghua Wai Ke Za Zhi. 2004;42:1089-92 pubmed
    ..To discuss the standards for clinical functional gradation and preoperative preparation of pheochromocytoma...
  52. Srinivasan C, Sachdeva R, Morrow W, Gossett J, Chipman C, Imamura M, et al. Standardized management improves outcomes after the Norwood procedure. Congenit Heart Dis. 2009;4:329-37 pubmed publisher
    ..We studied the impact of a standardized management protocol for neonates undergoing NP...
  53. Dipp M, Nye P, Taggart D. Phenoxybenzamine is more effective and less harmful than papaverine in the prevention of radial artery vasospasm. Eur J Cardiothorac Surg. 2001;19:482-6 pubmed
    ..The major drawback of the radial artery is its proclivity to spasm. Both papaverine and phenoxybenzamine have been recommended as topical vasodilators in clinical practice...