Alteplase

Molecular formula C2736H4U4N9,40824845 Molecular weight 59050.0 CAS Registry No. 105857-23-6 

Sample preparation 100 p.L Formulation + 300 u.L 20 mM dithiothreitol in mobile phase, heat at 37° for 15 min, inject a 25 pL aliquot. 

Mobile phase 200 mM pH 6.8 NaH2P04 containing 0.1% sodium dodetyl sulfate Flow rate 0.35 Injection volume 25 Detector UV 214 

du M6e, C.P.R.C. Stability and activity of alteplase with injectable drugs commonly used in cardiac therapy. Am.J.Health-Syst.Pharm., 1995, 52, 1904-1909 

Mobile phase Gradient. MeCN 0.1% trifluoroacetic add from 0 100 to 60 40 over 90 min Flow rate 1 Ipjection volume 200 Detector UV 210 

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Tissue plasminogen activator (alteplase t-PA) is a serine protease that is released into the circulation from vascular endothelium under conditions of injury or... 

Clark WM, Wissman S, Albers GW, Jhamandas JH, Madden KP, Hamilton S. Recombinant tissue-type plasminogen activator (Alteplase) for ischemic stroke 3 to 5 hours after symptom onset. The ATLANTIS Study a randomized controlled trial. Alteplase Thrombolysis for Acute Noninterventional Therapy in Ischemic Stroke. JAMA 1999 282 2019-2026 [see comment]. 

The NINDS rt-PA smdy was divided into two parts. NINDS part I included 291 patients and NINDS part II included 333 patients. In both parts, acute ischemic stroke patients presenting within 3 hours of symptom onset were randomized to placebo versus treatment with the human rt-PA Alteplase (Activase). The dose was 0.9 mg/kg (maximum dose 90 mg), with 10% of the total dose given as a bolus and the remaining 90% infused over 60 minutes. Inclusion and exclusion criteria for both parts are listed in Table 3.2. These criteria are now the standard clinical criteria used to determine IV rt-PA eligibility in acute stroke patients. 

Three large randomized trials, the European Cooperative Acute Stroke Study (ECASS) parts I and II, and the Alteplase Thrombolysis for Acute Noninterven-tional Therapy in Ischemic Stroke (ATLANTIS), have investigated the efficacy of IV rt-PA in acute stroke beyond the 3-hour window. All three studies showed high rates of sICH complicating rt-PA treatment, and no overall efficacy of rt-PA. 

E, Davis S, Donnan G, Schneider D, Diez-Tejedor E, Trouillas R Randomised double-blind placebo-controlled trial of thrombol3ffic therapy with intravenous alteplase in acute ischaemic stroke (ECASS II). Second European-Australasian Acute Stroke Study Investigators. Lancet. 1998 352 1245-1251. 

Clark WM, Albers GW, Madden KR Hamilton S. The rtPA (alteplase) 0- to 6-hour acute stroke trial, part a (a0276g) results of a double-bhnd, placebo-controlled, multicenter study. Thrombolytic Therapy in Acute Ischemic Stroke Study Investigators. Stroke. 2000 31 811-816. 

Albers GW, Bates VE, Clark WM, Bell R, Verro P, Hamilton SA. Intravenous tissue-type plasminogen activator for treatment of acute stroke The Standard Treatment with Alteplase to Reverse stroke (STARS) study. JAMA. 2000 283 1145-1150. 

OR 1.81, 95% Cl 1.46-2.24), most of which were related to symptomatic intracranial hemorrhage (OR 3.37, 95% Cl 2.68. 22). In addition, a pooled analysis of six major randomized placebo-controlled IV rt-PA stroke trials (Alteplase Thrombolysis for Acute Noninterventional Therapy in Ischemic Stroke (ATLANTIS) I and II, European Cooperative Acute Stroke Study (ECASS) I and II, and NINDS I and II), including 2775 patients who were treated with IV rt-PA or placebo within 360 minutes of stroke onset, confirmed the beneht up to 3 hours and suggested a potential beneht beyond 3 hours for some patients. The pattern of a decreasing chance of a favorable 3-month outcome as the time interval from stroke onset to start of treatment increased was consistent with the findings of the original NINDS study. ... 

Junghans U, Seitz RJ, Wittsack HJ, Aulich A, Siebler M. Treatment of acute basilar artery thrombosis with a combination of systemic alteplase and tirofiban, a nonpeptide platelet glycoprotein Ilb/HIa inhibitor report of four cases. Radiology 2001 221 795-801. 

Reperfusion of Stroke Safety Study Imaging Evaluation-2 Adjunctive Treatment to Standard Alteplase Therapy of Ischemic Stroke. Presented at the 29th International Stroke Conference Fehmary 2004. 

Alteplase, reteplase, or tenecteplase preferred over strepto kinase in ... 

Alteplase 0.6 mg/kg (maximum of 50 mg) over 2-15 min may be utilized if the patient is hemodynamically unstable or in cardiac arrest... 

Patients who are otherwise eligible (except blood pressure) for alteplase, should have their blood pressure lowered cautiously to a systolic <185 mmHg and a diastolic <110 mmHg... 

Patient otherwise eligible for alteplase (except for blood pressure)... 

Ability to begin alteplase therapy within 3 h of CVA onset... 

Alteplase Administration Protocol for Cerebrovascular Accident Indication... 

No antiplatelet agents or anticoagulants should be administered for 24 h following the completion of alteplase (tPA) infusion... 

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