Pharmacokinetics of alteplase in the treatment of ischaemic stroke

Expert Opinion on Drug Metabolism and Toxicology

Volumn 8, Issue 2, 2012, Pages 271-281

  Acheampong, Paul ^a   Ford, Gary A ^b  

^a NEWCASTLE UPON TYNE HOSPITALS NHS FOUNDATION TRUST   (United Kingdom)

^b NEWCASTLE UNIVERSITY   (United Kingdom)

Author keywords

alteplase; fibrinolysis; ischaemic stroke; pharmacokinetics; recombinant tissue plasminogen activator; thrombolysis

Indexed keywords

ACETYLSALICYLIC ACID; ALTEPLASE; APIXABAN; APROTININ; CLOPIDOGREL; DABIGATRAN; DESMOTEPLASE; GLYCERYL TRINITRATE; HEPARIN; NICARDIPINE; NITRATE; PLACEBO; RETEPLASE; RIVAROXABAN; STREPTOKINASE; TENECTEPLASE; TRANEXAMIC ACID; UROKINASE;

ACUTE HEART INFARCTION; ANAPHYLAXIS; ANGIONEUROTIC EDEMA; ANTICOAGULATION; ARTICLE; BLEEDING; BLOOD CLOT LYSIS; BRAIN HEMORRHAGE; BRAIN ISCHEMIA; CONTINUOUS INFUSION; DISTRIBUTION VOLUME; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG CONTRAINDICATION; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG TOLERABILITY; HEART FUNCTION; HUMAN; HYPERTENSION; HYPOFIBRINOGENEMIA; HYPOTENSION; LIVER PERFUSION; LUNG EMBOLISM; NONHUMAN; PATHOPHYSIOLOGY; POSTMARKETING SURVEILLANCE; STROKE; THROMBOSIS; TONGUE EDEMA; TREATMENT OUTCOME; TREATMENT RESPONSE;

BRAIN ISCHEMIA; DRUG INTERACTIONS; FIBRINOLYTIC AGENTS; HUMANS; PRODUCT SURVEILLANCE, POSTMARKETING; STROKE; TISSUE PLASMINOGEN ACTIVATOR;

EID: 84856094347     PISSN: 17425255     EISSN: 17447607     Source Type: Journal    
DOI: 10.1517/17425255.2012.652615     Document Type: Article

References (97)

1. Hatano S. Experience from a multicentre stroke register: a preliminary report. Bull WHO 1975;54:541-53 (Pubitemid 8114220)
2. Bamford J, Sandercock P, Dennis M, et al. A prospective study of acute cerebrovascular disease in the community: the Oxfordshire Community Stroke Project 1981-86. 1. Methodology, demography and incident cases of first-ever stroke. J Neurol Neurosurg Psychiatry 1988;51(11):1373-80 (Pubitemid 18262958)
3. Lloyd-Jones D, Adams R, Carnethon M, et al. Heart disease and stroke statistics-2009 update: a report from the American Heart Association Statistics Committee and Stroke Statistics Subcommittee. Circulation 2009;119(3):480-6
4. Morbidity and mortality chartbook. NHLBI. Available from: http://www. nhlbi.nih.gov/resources/docs/cht-book. htm [Last accessed 24 December 2010
5. The atlas of heart disease and stroke. WHO. Available from: http://www.who. int/cardiovascular-diseases/resources/atlas/ en [Last accessed 24 December 2010
6. Boerma T, Abou-Zahr C, Kinfu Y, et al. World Health Statistics 2008. World Health Organization, Geneva; 2008
7. Warlow C, Sudlow C, Dennis M, et al. Stroke. See comment. Lancet 2003;362(9391):1211-24
8. Mathers C, Boerma T, Ma Fat D. An update of the global burden of disease in 2004. World Health Organization, Geneva; 2008
9. Roger VL, Go AS, Lloyd-Jones DM, et al. Heart disease and stroke statistics-2011 update: a report from the American Heart Association. Circulation 2011;123(4):e18-e209
10. Ronning OM, Guldvog B. Stroke units versus general medical wards, I: twelve and eighteen-month survival: a randomized, controlled trial. Stroke 1998;29(1):58-62 (Pubitemid 28046942)
11. Stroke Unit Trialists' Collaboration. Organised inpatient (stroke unit) care for stroke. Cochrane Database of Syst Rev 2007;(4):CD000197
12. Langhorne P, Pollock A; Stroke Unit Trialists' Collaboration. What are the components of effective stroke unit care? Age Ageing 2002;31(5):365-71 (Pubitemid 35174525)
13. Hacke W, Kaste M, Bluhmki E, et al. Thrombolysis with alteplase 3 to 4.5 hours after acute ischemic stroke. N Engl J Med 2008;359(13):1317-29.
14. Haley EC Jr, Levy DE, Brott TG, et al. Urgent therapy for stroke. Part II. Pilot study of tissue plasminogen activator administered 91-180 minutes from onset. Stroke 1992;23(5):641-5.
15. The National Institute of Neurological Disorders and Stroke rt-PA Stroke Study Group. Tissue plasminogen activator for acute ischemic stroke. N Engl J Med 1995;333(24):1581-71.
16. Actilyse. European Medicines Agency. Available from: http://www.ema. europa. eu/ema/index.jsp?curl=pages/medicines/ human/referrals/Actilyse/ human-referral-000069.jsp&mid= WC0b01ac0580024e9a&murl=menus/ regulations/regulations. jsp&jsenabled=true [Last accessed 28 December 2010
17. Alteplase Product Approval Information - Licensing Action 6/18/96. FDA. Available from: http://www.fda. gov/Drugs/DevelopmentApprovalProcess/ HowDrugsareDevelopedandApproved/ ApprovalApplications/Therapeutic BiologicApplications/ucm080430.htm [Last accessed 28 December 2010
18. Corporate Chronology. Genentech. Available from: http://www.gene.com/ gene/about/corporate/history/timeline. html [Last accessed 28 December 2010
19. Ischaemic stroke (acute) - alteplase: Final Appraisal Determination. National Institute for Health and Clinical Excellence. Available from: http://www. nice.org.uk/guidance/index.jsp? action=download&o=33971 [Last accessed 28 December 2010
20. Jr, Adams HPdel Zoppo G, Alberts MJ, et al. Guidelines for the early management of adults with ischemic stroke: a guideline from the American Heart Association/American Stroke Association Stroke Council, Clinical Cardiology Council, Cardiovascular Radiology and Intervention Council and the Atherosclerotic Peripheral Vascular Disease and Quality of Care Outcomes in Research Interdisciplinary Working Groups: the American Academy of Neurology affirms the value of this guideline as an educational tool for neurologists. Stroke 2007;38(5):1655-711 (Pubitemid 46691097)
21. Recommendations for stroke management. European Stroke Organisation. Available from: http:// www.eso-stroke.org/recommendations. php?cid=9&sid=1 [Last accessed 28 December 2010
22. Albers GW, Olivot J. Intravenous alteplase for ischaemic stroke. Lancet 2007;369(9558):249-50 (Pubitemid 46136466)
23. National sentinel stroke audit. Royal College of Physicians, London. Available from: http://www.rcplondon.ac.uk/ resources/national-sentinel-stroke- audit [Last accessed 24 December 2010
24. Murray V, Norrving B, Sandercock PA, et al. The molecular basis of thrombolysis and its clinical application in stroke. J Intern Med 2010;267(2):191-208
25. The multicenter acute stroke trial - Europe study group. Thrombolytic therapy with streptokinase in acute ischemic stroke. N Engl J Med 1996;335(3):145-50
26. Furlan A, Higashida RT, Wechsler L, et al. Intra-arterial prourokinase for acute ischemic stroke. The PROACT II study: a randomized controlled trial. Prolyse in Acute Cerebral Thromboembolism. JAMA 1999;282(21):2003-11
27. Ogawa A, Mori E, Minematsu K, et al. Randomized trial of intraarterial infusion of urokinase within 6 hours of middle cerebral artery stroke: the middle cerebral artery embolism local fibrinolytic intervention trial (MELT) Japan. Stroke 2007;38(10):2633-9 (Pubitemid 47493996)
28. Fields JD, Khatri P, Nesbit GM, et al. Meta-analysis of randomized intra-arterial thrombolytic trials for the treatment of acute stroke due to middle cerebral artery occlusion. J Neuro Intervent Surg 2011;3:151-5
29. Hacke W, Albers G, Al-Rawi Y, et al. The Desmoteplase in Acute Ischemic Stroke Trial (DIAS): a phase II MRI-based 9-hour window acute stroke thrombolysis trial with intravenous desmoteplase. Stroke 2005;36(1):66-73 (Pubitemid 40054177)
30. Furlan AJ, Eyding D, Albers GW, et al. Dose Escalation of Desmoteplase for Acute Ischemic Stroke (DEDAS): evidence of safety and efficacy 3 to 9 hours after stroke onset. Stroke 2006;37(5):1227-31 (Pubitemid 43731867)
31. Activase. Genentech. Available from: http://www.gene.com/gene/products/ information/cardiovascular/activase/insert. jsp#top [Last accessed 29 December 2010
32. Nordt TK, Bode C. Thrombolysis: newer thrombolytic agents and their role in clinical medicine. Heart 2003;89(11):1358-62 (Pubitemid 37311107)
33. Rijken DC, Collen D. Purification and characterization of the plasminogen activator secreted by human melanoma cells in culture. J Biol Chem 1981;256(13):7035-41
34. Therapeutic Drugs. In: Dollery C, editor. 2nd edition. Churchill Livingstone, Edinburgh; 1999
35. Alteplase IV: AHFS Drug Information. Medicines Complete. Available from: http://www.medicinescomplete.com/ [Last accessed 21 June 2011]
36. Brenner S. The molecular evolution of genes and proteins: a tale of two serines. Nature 1988;334(6182):528-30
37. ENZYME entry: EC 3.4.21.68. Swiss Institute of Bioinformatics. Available from: http://www.expasy.org/cgi-bin/ nicezyme.pl?3.4.21.68 [Last accessed 29 December 2010
38. Tanswell P, Seifried E, Su PC, et al. Pharmacokinetics and systemic effects of tissue-type plasminogen activator in normal subjects. Clin Pharmacol Ther 1989;46(2):155-62. (Pubitemid 19219951)
39. Collen D, Bounameaux H, De Cock F, et al. Analysis of coagulation and fibrinolysis during intravenous infusion of recombinant human tissue-type plasminogen activator in patients with acute myocardial infarction. Circulation 1986;73(3):511-17 (Pubitemid 16133030)
40. Brott TG, Haley EC Jr, Levy DE, et al. Urgent therapy for stroke. Part I. Pilot study of tissue plasminogen activator administered within 90 minutes. Stroke 1992;23(5):632-40.
41. Gimple LW, Gold HK, Leinbach RC, et al. Correlation between template bleeding times and spontaneous bleeding during treatment of acute myocardial infarction with recombinant tissue-type plasminogen activator. Circulation 1989;80(3):581-8 (Pubitemid 19231392)
42. Mori E, Minematsu K, Nakagawara J, Yamaguchi T. Factors predicting outcome in stroke patients treated with 0.6 mg/kg alteplase: evidence from Japan Alteplase Clinical Trial (J-ACT). J Stroke Cardiovasc Dis. In Press, Corrected Proof 2011;20(6):517-22
43. Tebbe U, Tanswell P, Seifried E, et al. Single-bolus injection of recombinant tissue-type plasminogen activator in acute myocardial infarction. Am J Cardiol 1989;64(8):448-53. (Pubitemid 19214571)
44. Baugham RA. Pharmacokinetics of tissue plasminogen activator. In: Sobel BE, Collen D, Grossbard EB, editors. Tissue plasminogen activator in thrombolytic therapy. 1st edition. Marcel Dekker, New York; 1987. p. 41-53
45. Verstraete M. Pharmacokinetics of APSAC, TPA and SCU-PA. In: Julian D, Kubler W, Noris W et al. (eds). Thrombolysis in Cardiovascular Disease. Marcel Dekker, New York,1989. p69-86
46. Seifried E, Tanswell P, Ellbruck F, et al. Pharmacokinetics and haemostatic status during consecutive infusions of recombinant tissue-type plasminogen activator in patients with acute myocardial infarction. Thromb Haemost 1989;61(3):497-501 (Pubitemid 19168163)
47. Garabedian HD, Gold HK, Leinbach RC, et al. Comparative properties of two clinical preparations of recombinant human tissue-type plasminogen activator in patients with acute myocardial infarction. J Am Coll Cardiol 1987;9(3):599-607 (Pubitemid 17024583)
48. Tanswell P, Tebbe U, Neuhaus KL, et al. Pharmacokinetics and fibrin specificity of alteplase during accelerated infusions in acute myocardial infarction. J Am Coll Cardiol 1992;19(5):1071-5
49. Verstraete M, Bounameaux H, De Cock F, et al. Pharmacokinetics and systematic fibrinogenolytic effects of recombinant human tissue-type plasminogen activator (rt- PA) in humans. J Pharmacol Exp Ther 1985;235(2):506-12 (Pubitemid 16248752)
50. Nilsson T, Wallen P, Mellbring G. In vivo metabolism of human tissue-type plasminogen activator. Scand J Haematol 1984;33(1):49-53 (Pubitemid 14087693)
51. Tanswell P, Seifried E, Stang E, Krause J. Pharmacokinetics and hepatic catabolism of tissue-type plasminogen activator. Arzneimittelforschung 1991;41(12):1310-19.
52. Kane I, Sandercock P. Alteplase: thrombolysis for acute ischemic stroke. Therapy 2005;2(5):709-16 (Pubitemid 41447759)
53. Wu Z, Van der Werf F, Stassen T, et al. Pharmacokinetics and coronoary thrombolytic properties of two human tissue-type plasminogen activator variants lacking the finger-like, growth factor-like, and first kringle domains (amino acids 6- 173) in a canine model. J Cardiovasc Pharmacol 1990;16(2):197-203 (Pubitemid 20222640)
54. Beebe DP, Aronson DL. Turnover of human tissue plasminogen activator (tPA) in rabbits. Thromb Res 1986;43(6):663-74 (Pubitemid 16049221)
55. Emeis JJ, cvan den Hoogen CM, Jense D. Hepatic clearance of tissue-type plasminogen activator in rats. Thromb Haemost 1985;54(3):661-4 (Pubitemid 16195313)
56. Eppler S, Senn T, Gilkerson E, Modi NB. Pharmacokinetics and pharmacodynamics of recombinant tissue-type plasminogen activator following intravenous administration in rabbits: A comparison of three dosing regimens. Biopharm Drug Dispos 1998;19(1):31-8 (Pubitemid 28064489)
57. Tiefenbrunn AJ, Robinson AK, Kurnik PB, et al. Clinical pharmacology in patients with evolving myocardial infarction of tissue-type plasminogen activator produced by recombinant DNA technology. Circulation 1985;71(1):110-16 (Pubitemid 15164769)
58. Ford GA, Ahmed N, Azevedo E, et al. Intravenous alteplase for stroke in those older than 80 years old. Stroke 2010;41(11):2568-74.
59. Reuvers M. Anticoagulant and fibrinolytic drugs. In: Schaefer C, Peters P, Miller RK, editors. Drugs during pregnancy and lactation: Treatment options and risk assessment. 2nd edition. Academic Press, Great Britain; 2007. p. 248
60. Schaefer C. Anticoagulants and fibrinolytics. In: Schaefer C, Peters P, Miller RK, editors. Drugs during pregnancy and lactation: Treatment options and risk assessment. 2nd edition. Academic Press, Great Britain; 2007. p. 697
61. Romeo F, Rosano GMC, Martuscelli E, et al. Concurrent nitroglycerin administration reduces the efficacy of recombinant tissue-type plasminogen activator in patients with acute anterior wall myocardial infarction. Am Heart J 1995;130(4):692-7.
62. ISIS-4 (Fourth International Study of Infarct Survival) Collaborative Group. Lancet 1995;345(8951):669-82
63. Gruppo Italiano per lo Studio della Soprawivenza nell' Infarto Miocardio. Lancet 1994;343(8906):1115-22
64. Ribo M, Alvarez-Sabin J, Montaner J, et al. Temporal profile of recanalization after intravenous tissue plasminogen activator. Stroke 2006;37(4):1000-4, 697
65. Delgado-Mederos R, Rovira A, Alvarez-Sabin J, et al. Speed of tPA-induced clot lysis predicts DWI lesion evolution in acute stroke. Stroke 2007;38:955-60 (Pubitemid 46568458)
66. Naranja IC, Portilla-Cuenca JC, Caballero PEJ, et al. Fatal intracerebral hemorrhage associated with administration of recombinant tissue plasminogen activator in a stroke patient on treatment with dabigatran. Cerebrovasc Dis 2011;32:614-15
67. Dempfle CE, Hennerici MG. Fibrinolytic treatment of acute ischemic stroke for patients on new oral anticoagulant drugs. Cerebrovasc Dis 2011;32:616-19
68. Wahlgren N, Ahmed N, Davalos A, et al. Thrombolysis with alteplase for acute ischaemic stroke in the Safe Implementation of Thrombolysis in Stroke-Monitoring Study (SITS-MOST): an observational study. Lancet 2007;369(9558):275-82 (Pubitemid 46138121)
69. Diedler J, Ahmed N, Sykora M, et al. Safety of intravenous thrombolysis for acute ischemic stroke in patients receiving antiplatelet therapy at stroke onset. Stroke 2010;41:288-94
70. Lexicomp Online. Lexi-interact. Available from: http://www.uptodate.com/ crlsql/ interact/frameset.jsp [Last accessed 16 January 2011
71. Lees KR, Bluhmki E, Von Kummer R, et al. Time to treatment with intravenous alteplase and outcome in stroke: an updated pooled analysis of ECASS, ATLANTIS, NINDS and EPITHET trials. Lancet 2010;375(9727):1695-703
72. Wardlaw JM, Murray V, Berge E, Del Zoppo GJ. Thrombolysis for acute ischaemic stroke. Cochrane Database of Syst Rev 2009;(4):CD000213
73. Bhatia R, Hill MD, Shobha N, et al. Low rates of acute recanalization with intravenous recombinant tissue plasminogen activator in ischemic stroke: real-world experience and a call for action. Stroke 2010;41(10):2254-8
74. Lee KY, Han SW, Kim SH, et al. Early recanalization after intravenous administration of recombinant tissue plasminogen activator as assessed by preand post-thrombolytic angiography in acute ischemic stroke patients. Stroke 2007;38(1):192-3 (Pubitemid 46035627)
75. Engelter ST, Bonati LH, Lyrer PA. Intravenous thrombolysis in stroke patients of > or = 80 versus (Pubitemid 44614151)
76. Mishra NK, Ahmed N, Andersen G, et al. Thrombolysis in very elderly people: controlled comparison of SITS International Stroke Thrombolysis Registry and Virtual International Stroke Trials Archive. BMJ 2010;341:c6046
77. Group, The NINDS t-PA Stroke Study, Generalized efficacy of t-PA for acute stroke. Subgroup analysis of the NINDS t-PA Stroke Trial. Stroke 1997;28:2119-25
78. Meretoja A, Putaala J, Tatlisumak T, et al. Off-Label thrombolysis is not associated with poor outcome in patients with stroke. Stroke 2010;41:1450-8
79. Stroke Trials Registry. The Internet Stroke Center. Available from: http:// www.strokecenter.org/trials/TrialDetail. aspx?tid=81 [Last accessed 29 January 2011
80. Lee M, Hong KS, Saver JL. Efficacy of intra-arterial fibrinolysis for acute ischemic stroke: Meta-analysis of randomized controlled trials. Stroke 2010;41(5):932-7
81. Ciccone A, Valvassori L, Ponzio M, et al. Intra-arterial or intravenous thrombolysis for acute ischemic stroke? The SYNTHESIS pilot trial. J Neuro Interv Surg 2010;2(1):74-9
82. IMS II Trial Investigators. The Interventional Management of Stroke (IMS) II Study. Stroke 2007;38(7):2127-35
83. Wahlgren N, Ahmed N, Eriksson N, et al. Multivariable analysis of outcome predictors and adjustment of main outcome results to baseline data profile in randomized controlled trials: Safe Implementation of Thrombolysis in Stroke-MOnitoring STudy (SITSMOST). Stroke 2008;39(12):3316-22
84. Pereira AC, Martin PJ, Warburton EA. Thrombolysis in acute ischaemic stroke. Postgrad Med J 2001;77(905):166-71 (Pubitemid 32205058)
85. Prescription Medicine Brands. Boehringer Ingelheim. Available from: http://www.boehringer-ingelheim.co.uk/ products/prescription.html [Last accessed 14 February 2011
86. Ludlam CA, Bennett B, Fox KA, et al. Guidelines for the use of thrombolytic therapy. Haemostasis and Thrombosis Task Force of the British Committee for Standards in Haematology. Blood Coagul Fibrinolysis 1995;6(3):273-85
87. Engelter ST, Fluri F, Buitrago-Tellez C, et al. Life-threatening orolingual angioedema during thrombolysis in acute ischemic stroke. J Neurol 2005;252(10):1167-70 (Pubitemid 41443614)
88. Hill MD, Barber PA, Takahashi J, et al. Anaphylactoid reactions and angioedema during alteplase treatment of acute ischemic stroke. CMAJ 2000;162(9):1281-4 (Pubitemid 30304328)
89. Hill MD, Lye T, Moss H, et al. Hemi-orolingual angioedema and ACE inhibition after alteplase treatment of stroke. Neurology 2003;60(9):1525-7 (Pubitemid 36554818)
90. Laubinger R, Guthke K, Erdmann U, Klein U. Angioneurotic orolongual edema associated with the use of rt-PA following a stroke. Anaesthesist 2007;56(10):1024-7 (Pubitemid 350059751)
91. Molinaro G, Gervais N, Adam A. Biochemical basis of angioedema associated with recombinant tissue plasminogen activator treatment: an in vitro experiemental approach. Stroke 2002;33(6):1712-16 (Pubitemid 34619983)
92. Ottomeyer C, Sick C, Hennerici MG, Szabo K. Orolingual angioedema associated systemic thrombolysis with rt-PA: An underestimated side effect. Nervenarzt 2009;80(4):459-63
93. Rafii MS, Koenig M, Ziai WC. Orolingual angioedema associated with ACE inhibitor use after rtPA treatment of acute stroke. Neurology 2005;65(12):1906 (Pubitemid 43970108)
94. De Keyser J, Gdovinova Z, Uyttenboogaart M, et al. Intravenous alteplase for stroke: beyond the guidelines and in particular clinical situations. Stroke 2007;38(9):2612-18 (Pubitemid 47329647)
95. Leonhardt G, Gaul C, Nietsch HH, et al. Thrombolytic therapy in pregnancy. J Thromb Thrombolysis 2006;21(3):271-6 (Pubitemid 43676785)
96. Wiese KM, Talkad A, Mathews M, Wang D. Intravenous recombinant tissue plasminogen activator in a pregnant woman with cardioembolic stroke. Stroke 2006;37(8):2168-9 (Pubitemid 44309923)
97. Yamaguchi Y, Kondo T, Ihara M, et al. Intravenous recombinant tissue plasminogen activator in an 18-week pregnant woman with embolic stroke. Rinsho Shinkeigaku 2010;50(5):315-19.