アニストレプラーゼ
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/08/13 14:00:52」(JST)
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Anistreplase
Clinical data |
Trade names |
Eminase |
AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
Legal status |
? |
Pharmacokinetic data |
Half-life |
90 minutes |
Identifiers |
CAS number |
81669-57-0 Y |
ATC code |
B01AD03 |
DrugBank |
DB00029 |
KEGG |
D02947 Y |
Chemical data |
Formula |
? |
Mol. mass |
approx. 131,000 g/mol |
Y (what is this?) (verify) |
Anistreplase is a thrombolytic drug.[1][2][3]
Anistreplase has been developed by Beecham as Eminase. It is also known as anisoylated plasminogen streptokinase activator complex (APSAC)
Mechanism
It is a complex of purified human plasminogen and bacterial streptokinase that has been acylated to protect the enzyme's active site. When the drug is administered, the acyl group gets hydrolyzed, thereby freeing the activator complex. It converts plasminogen to plasmin, which in turn degrades fibrin (blood clots) to fibrin split products.
References
- ^ Rawles J (January 1996). "Magnitude of benefit from earlier thrombolytic treatment in acute myocardial infarction: new evidence from Grampian region early anistreplase trial (GREAT)". BMJ 312 (7025): 212–5. doi:10.1136/bmj.312.7025.212. PMC 2350007. PMID 8563585.
- ^ Hannaford P, Vincent R, Ferry S, Hirsch S, Kay C (April 1995). "Assessment of the practicality and safety of thrombolysis with anistreplase given by general practitioners". Br J Gen Pract 45 (393): 175–9. PMC 1239197. PMID 7612317.
- ^ Rawles J, Light J (October 1993). "Loss of quality adjusted days as a trial endpoint: effect of early thrombolytic treatment in suspected myocardial infarction. Grampion Region Early Anistreplase Trial (GREAT)". J Epidemiol Community Health 47 (5): 377–381. doi:10.1136/jech.47.5.377. PMC 1059832. PMID 8289038.
Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)
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Antiplatelet drugs |
Glycoprotein IIb/IIIa inhibitors
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- Abciximab
- Eptifibatide
- Tirofiban
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ADP receptor/P2Y12 inhibitors
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- thienopyridines
- Clopidogrel
- Prasugrel
- Ticlopidine
- nucleotide/nucleoside analogs
- Cangrelor
- Elinogrel
- Ticagrelor
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Prostaglandin analogue (PGI2)
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- Beraprost
- Iloprost
- Prostacyclin
- Treprostinil
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COX inhibitors
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- Acetylsalicylic acid/Aspirin#
- Aloxiprin
- Carbasalate calcium
- Indobufen
- Triflusal
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Thromboxane inhibitors
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- thromboxane synthase inhibitors
- Dipyridamole (+Aspirin)
- Picotamide
- receptor antagonist
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Phosphodiesterase inhibitors
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- Cilostazol
- Dipyridamole
- Triflusal
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Other
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- Cloricromen
- Ditazole
- Vorapaxar
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Anticoagulants |
Vitamin K antagonists
(inhibit II, VII, IX, X)
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- coumarins: Acenocoumarol
- Coumatetralyl
- Dicoumarol
- Ethyl biscoumacetate
- Phenprocoumon
- Warfarin#
- 1,3-Indandiones: Clorindione
- Diphenadione
- Phenindione
- other: Tioclomarol
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Factor Xa inhibitors
(with some II inhibition)
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Heparin group/
glycosaminoglycans/
(bind antithrombin)
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- low molecular weight heparin
- Bemiparin
- Certoparin
- Dalteparin
- Enoxaparin
- Nadroparin
- Parnaparin
- Reviparin
- Tinzaparin
- oligosaccharides
- heparinoid
- Danaparoid
- Dermatan sulfate
- Sulodexide
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Direct Xa inhibitors
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- xabans
- Apixaban
- Betrixaban
- Darexaban
- Edoxaban
- Otamixaban
- Rivaroxaban
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Direct thrombin (IIa) inhibitors
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- bivalent: Hirudin
- Bivalirudin
- Desirudin
- Lepirudin
- univalent: Argatroban
- Dabigatran
- Melagatran‡
- Ximelagatran‡
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Other
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- Antithrombin III
- Defibrotide
- Protein C
- Ramatroban
- REG1
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Thrombolytic drugs/
fibrinolytics |
- plasminogen activators: r-tPA
- Alteplase
- Reteplase
- Tenecteplase
- UPA
- Anistreplase
- Monteplase
- Streptokinase#
- other serine endopeptidases: Ancrod
- Brinase
- Fibrinolysin
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Non-medicinal |
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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cell/phys (coag, heme, immu, gran), csfs
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rbmg/mogr/tumr/hist, sysi/epon, btst
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drug (B1/2/3+5+6), btst, trns
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UpToDate Contents
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English Journal
- Acute ST-segment elevation myocardial infarction: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition).
- Goodman SG, Menon V, Cannon CP, Steg G, Ohman EM, Harrington RA; American College of Chest Physicians.Author information St. Michael's Hospital, Division of Cardiology, 30 Bond Street, Queen, Toronto, Ontario, Canada. goodmans@smh.toronto.on.caErratum inChest. 2008 Oct;134(4):892. AbstractThis chapter about fibrinolytic, antiplatelet, and antithrombin treatment for acute ST-segment elevation (STE) myocardial infarction (MI) is part of the American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Grade 1 recommendations are strong and indicate that the benefits do, or do not, outweigh risks, burden, and costs. Grade 2 suggests that individual patient values may lead to different choices (for a full understanding of the grading see the chapter by Guyatt et al, CHEST 2008; 133[suppl]:123S-131S). Among the key recommendations in this chapter are the following: for patients with ischemic symptoms characteristic of acute MI of < or = 12 h in duration and persistent STE, we recommend that all undergo rapid evaluation for reperfusion (primary percutaneous coronary intervention [PCI] or fibrinolytic) therapy and have a reperfusion strategy implemented promptly after contact with the health-care system (Grade 1A). For patients with ischemic symptoms characteristic of acute MI of < or = 12 h in duration and persistent STE, we recommend administration of streptokinase, anistreplase, alteplase, reteplase, or tenecteplase over no fibrinolytic therapy (all Grade 1A). For patients with symptom duration < or = 6 h, we recommend the administration of alteplase or tenecteplase over streptokinase (both Grade 1A). We recommend aspirin over no aspirin therapy followed by indefinite therapy (Grade 1A); we also recommend clopidogrel in addition to aspirin for up to 28 days (Grade 1A). In addition to aspirin and other antiplatelet therapies, we recommend the use of antithrombin therapy (eg, unfractionated heparin (UFH), enoxaparin, or fondaparinux) over no antithrombin therapy (Grade 1A), including for those patients receiving fibrinolysis (and regardless of which lytic agent is administered), primary PCI, or patients not receiving reperfusion therapy.
- Chest.Chest.2008 Jun;133(6 Suppl):708S-775S. doi: 10.1378/chest.08-0665.
- This chapter about fibrinolytic, antiplatelet, and antithrombin treatment for acute ST-segment elevation (STE) myocardial infarction (MI) is part of the American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Grade 1 recommendations are strong and indicate tha
- PMID 18574277
- Finite element modeling and experimental characterization of crosstalk in 1-D CMUT arrays.
- Bayram B, Kupnik M, Yaralioglu GG, Oralkan O, Ergun AS, Lin DS, Wong SH, Khuri-Yakub BT.Author information Edward L. Ginzton Laboratory, Stanford University, CA 94305, USA. bbayram@gmail.comAbstractCrosstalk is the coupling of energy between the elements of an ultrasonic transducer array. This coupling degrades the performance of transducers in applications such as medical imaging and therapeutics. In this paper, we present an experimental demonstration of guided interface waves in capacitive micromachined ultrasonic transducers (CMUTs). We compare the experimental results to finite element calculations using a commercial package (LS-DYNA) for a 1-D CMUT array operating in the conventional and collapsed modes. An element in the middle of the array was excited with a unipolar voltage pulse, and the displacements were measured using a laser interferometer along the center line of the array elements immersed in soybean oil. We repeated the measurements for an identical CMUT array covered with a 4.5-microm polydimethylsiloxane (PDMS) layer. The main crosstalk mechanism is the dispersive guided modes propagating in the fluid-solid interface. Although the transmitter element had a center frequency of 5.8 MHz with a 130% fractional bandwidth in the conventional operation, the dispersive guided mode was observed with the maximum amplitude at a frequency of 2.1 MHz, and had a cut-off frequency of 4 MHz. In the collapsed operation, the dispersive guided mode was observed with the maximum amplitude at a frequency of 4.0 MHz, and had a cut-off frequency of 10 MHz. Crosstalk level was lower in the collapsed operation (-39 dB) than in the conventional operation (-24.4 dB). The coverage of the PDMS did not significantly affect the crosstalk level, but reduced the phase velocity for both operation modes. Lamb wave modes, A0 and S0, were also observed with crosstalk levels of -40 dB and -65 dB, respectively. We observed excellent agreement between the finite element and the experimental results.
- IEEE transactions on ultrasonics, ferroelectrics, and frequency control.IEEE Trans Ultrason Ferroelectr Freq Control.2007 Feb;54(2):418-30.
- Crosstalk is the coupling of energy between the elements of an ultrasonic transducer array. This coupling degrades the performance of transducers in applications such as medical imaging and therapeutics. In this paper, we present an experimental demonstration of guided interface waves in capacitive
- PMID 17328339
- Plasminogen activators: a comparison.
- Baruah DB, Dash RN, Chaudhari MR, Kadam SS.Author information Department of Quality Assurance Techniques, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune-411038, India.AbstractThrombolytic drugs play a crucial role in the management of patients with acute myocardial infarction, pulmonary embolism, deep vein thrombosis, arterial thrombosis, acute thrombosis of retinal vessel, extensive coronary emboli, and peripheral vascular thromboembolism. Recognition of the importance of fibrinolytic system in thrombus resolution has resulted in the development of different fibrinolytic agents. Now a days several newer plasminogen activators with different pharmacokinetic and pharmacodynamic properties have been developed to treat thrombotic disease, which are fibrin specific with prolonged half-life and can be administered as a single bolus.
- Vascular pharmacology.Vascul Pharmacol.2006 Jan;44(1):1-9. Epub 2005 Nov 7.
- Thrombolytic drugs play a crucial role in the management of patients with acute myocardial infarction, pulmonary embolism, deep vein thrombosis, arterial thrombosis, acute thrombosis of retinal vessel, extensive coronary emboli, and peripheral vascular thromboembolism. Recognition of the importance
- PMID 16275118
Japanese Journal
- Changes in Mortality of Acute Myocardial Infarction as a Function of a Changing Treatment during the Last Two Decades.
- Claessens Christophe,Claessens Philip,Claessens Marc,Verschueren Roger,Claessens Jan
- Japanese Heart Journal 41(6), 683-695, 2000
- … The mortality rate dropped from 10.57% in the coumarine group and from 14.95% in the heparin group to 5.41% in the alteplase group, to 4.95% in the anistreplase group and 4.00% in the streptokinase subgroup. …
- NAID 130000070680
- Quantification of the benefit of earlier thrombolytic therapy : Five year results of the Grampian region early anistreplase Trial (GREAT)
- Are the Various Thrombolytic Agents Equally Effective in the Treatment of Acute Transmural Myocardial Infarction?
- CLAESSENS Jan,HASELDONCKX Christiane
- Japanese Heart Journal 33(4), 413-421, 1992
- … Our study concerns a group of 160 patients with an acute transmural myocardial infarction, 60 of whom were treated with anistreplase, 52 with streptokinase and 48 with alteplase. … Statistically, the administration of anistreplase was associated with a significantly higher frequency of ventricular arrhythmias in comparison to the other thrombolytic agents, whereas after subsequent coronary angiography, the anistreplase group revealed a significantly lower number of completely occluded coronary arteries. …
- NAID 130000765888
Related Links
- anistreplase /an·is·trep·lase/ (an″is-trep´lās) a thrombolytic agent used to clear coronary vessel occlusions associated with myocardial infarction. anistreplase, a plasminogen activator. indication This drug is used in acute MI for lysis ...
- Anistreplase information including symptoms, causes, diseases, symptoms, treatments, and other medical and health issues. ... Introduction: Anistreplase Description of Anistreplase Anistreplase: An acylated inactive complex of ...
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- 血栓溶解薬、遺伝子組換えプラスミノーゲン活性化因子