Hematology and Oncology Book

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t-PAAka: tPA, Alteplase, Activase

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  1. See Also
    1. Thrombolytic
  2. Dose
    1. Myocardial Infarction
      1. Bolus: 15 mg IV THEN
      2. Next: 0.75 mg/kg (max 50 mg) over 30 minutes THEN
      3. Next: 0.5 mg/kg (max 35 mg) over next 60 minutes
      4. Administer adjunctive Heparin concurrently
        1. See Thrombolysis
    2. Acute Ischemic Cerebrovascular Accident
      1. Calculate total dose: 0.9 mg/kg (max 90 mg)
      2. Bolus: Give 10% total dose as IV bolus over 1 minute
      3. Next: Give remainder of total dose over 60 minutes
    3. Acute Pulmonary Embolus
      1. Dose: 100 mg IV over 2 hours
      2. Restart Heparin when PTT below twice normal
  3. Disadvantages (compared with other Thrombolytics)
    1. Cost: $1200
    2. Increased bleeding risk
      1. 3-4% greater risk of bleeding in older than age 75
    3. Re-occludes earlier than other Thrombolytics
      1. Needs Heparin concurrently and afterward
  4. Advantages (compared with other Thrombolytics)
    1. Probably reperfuses arteries earlier
    2. Superior in large, anterior Myocardial Infarctions

Alteplase (C0032143)

Definition (MSH)A proteolytic enzyme in the serine protease family found in many tissues which converts PLASMINOGEN to PLASMIN. It has fibrin-binding activity and is immunologically different from URINARY PLASMINOGEN ACTIVATOR. The primary sequence, composed of 527 amino acids, is identical in both the naturally occurring and synthetic proteases. EC 3.4.21.68.
Definition (PDQ)A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, recombinant tPA increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42033&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42033&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C39607" NCI Thesaurus)
Definition (NCI)Tissue Plasminogen Activator isoforms 1 (562-aa, 63-kD), 2 (291-aa, frameshifted with distinct C-terminus), and 3 (516-aa, deleted Ex4) are encoded by human PLAT Gene (Peptidase S1 Family). EGF-like, fibronectin I, and kringle domains mediate fibrin, LRP1, annexin II, and cytokeratin 8 binding. TPA also binds to laminin, fibronectin, and mannose receptor. Inhibited by PAI-1, serine protease TPA is widely expressed as an active single chain, then secreted, and cleaved by plasmin, tissue kallikrein, or factor XA to a fully active disulfide linked A/B-protein; N-heavy chain and C-light chain. Important in cell migration and tissue remodeling, TPA activates (increased by fibrin or heparin) plasminogen to fibrinolytic plasmin conversion by hydrolyzing a specific Arg-Val bond. Altered activity causes hyper- or hypofibrinolysis. (from LocusLink, Swiss-Prot, OMIM, and NCI)
Definition (NCI)Tissue plasminogen activator (PLAT) is a serine protease that activates the proenzyme plasminogen to plasmin, which in turn is responsible for fibrinolytic activity. PLAT is synthesized in vascular endothelial cells as a single polypeptide chain. Proteolytic cleavage of the single chain protein at a centrally located arginine-isoleucine bond by plasmin gives rise to a 2-chain disulfide-linked form, composed of the N-terminally derived heavy chain and the C-terminal light chain.
Definition (NCI)A secreted serine protease which converts the proenzyme plasminogen to plasmin, a fibrinolytic enzyme. Tissue-type plasminogen activator is synthesized as a single chain which is cleaved by plasmin to a two chain disulfide linked protein. This enzyme plays a role in cell migration and tissue remodeling. Increased enzymatic activity causes hyperfibrinolysis, which manifests as excessive bleeding; decreased activity leads to hypofibrinolysis which can result in thrombosis or embolism. (from LocusLink)
Definition (NCI)A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, recombinant tPA increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism. (NCI05)
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) , Enzyme (T126)
MSHD010959
EnglishAlteplase, Alteplase - chemical, ALTEPLASE PREPARATION, Plasminogen activator tissue type, PLAT, recombinant tissue plasminogen activator, rt-PA, rt-PA preparation, T Plasminogen Activator, T-PA, T-PA - tissue-type plasminogen activator, t-PA preparation, T-Plasminogen Activator, Tissue Activator D 44, Tissue Activator D-44, Tissue Plasminogen Activator, Tissue plasminogen activator preparation, Tissue Type Plasminogen Activator, Tissue-Type Plasminogen Activator, Tissue-type plasminogen activator preparation, TPA, TTPA
Spanishactivador del plasminogeno - T, activador del plasminogeno histico, activador del plasminogeno tisular, alteplasa, preparado con activador del plasminogeno tisular, preparado de activador del plasminogeno tipo tisular, preparado de activador tisular del plasminogeno, preparado de rt-PA, preparado de t-PA, preparado de TPA, TPA
Parent ConceptsBlood Coagulation Factor (C0005789), Plasminogen Activator (C0032144), Serine Protease (C0036734), Fibrinolytic Agents (C0016018), Alteplase (C0032143), Hydrolase (C0020289), Duplicate concept (C1274013), Plasminogen activator agent (C1636198)
SourcesCSP, LNC, MSH, MTH, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Activase (C0701942)

ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) , Enzyme (T126)
MSHD010959
EnglishActivase, Alteplase Genentech Brand, Genentech Brand of Alteplase, Hoffmann La Roche Brand of Alteplase, Hoffmann-La Roche Brand of Alteplase
SourcesMSH, MTH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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