Anistreplase

1. Anistreplase Drugbank ID : DB00029 Protein chemical formula : C2569H3928N746O781S40 Protein average weight : 59042.3000

2. Description : Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized (freeze-dried) formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl group is chemically conjugated to a complex of bacterial-derived streptokinase and human Plasma-derived Lys-plasminogen proteins. Indication: For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction Pharmacodynamics : Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.

3. Mechanism of action : Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots. Targets : Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1 Affected organisms : Humans and other mammals .

4. Categories : Fibrinolytic Agents and Thrombolytic Agents Sequence : SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP

5. Brands : Eminase Company : WulfingPharma GmbH Description : It is an inactive derivative of a fibrinolytic (thrombolytic) enzyme composed of streptokinase and lys-plasminogen in which the catalytic center of the enzymatic complex is temporarily blocked by a p-anisoyl group. Used for/Prescribed for : For use in the management of ( acute myocardial infarction) AMI in adults for the lysis of thrombi obstructing coronary arteries, the reduction of infarct size, the improvement of ventricular function following AMI, and the reduction of mortality associated with AMI. Formulation : Each unit-dose vial of sterile lyophilized, white to off-white powder contains: anistreplase 30 units, dimethylsulfoxide <3 mg, sodium hydroxide <0.2 mg and the following buffers or stabilizers: p-amidinophenyl-p'-anisate (acylating agent) 150 µg, mannitol 100 mg, L-lysine 46 mg, human serum albumin 30 mg, glycerol <2 mg and Þge-aminocaproic acid 1.2 mg. Preservative-free. Form : dry powder Route of administration : intravenous injection

6. Dosage :The recommended dose is 30 units of anistreplase administered only by i.v. injection over 2 to 5 minutes into an i.v. line or vein. Contraindication : allergic, active internal bleeding; history of cerebrovascular accident (CVA); patients receiving other i.v. thrombolytic agents; recent (within 2 months) intracranial or intraspinal surgery or trauma, intracranial neoplasm, arteriovenous malformation, or aneurysm; known bleeding diathesis; severe, uncontrolled hypertension, recent traumatic cardiopulmonary resuscitation; recent severe trauma Drug interaction :The use of anistreplase with other cardioactive drugs has not been studied. In addition to bleeding associated with heparin and vitamin K antagonists, drugs that alter platelet function (such as ASA and dipyridamole) may increase the risk of bleeding if administered prior to anistreplase therapy

7. References :http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20%28General%20Monographs-%20E%29/EMINASE.html http://www.drugs.com/mmx/eminase.html