Drug information of Anistreplase

Anistreplase


Anistreplase, trade name Eminase, is a thrombolytic drug prescribed to treat acute myocardial infarction.

Mechanism of effect

The drug is an acylated streptokinase-plasminogen complex. The acylation of the drug renders it temporarily inactive, protecting it from plasmin inhibitors. Anistreplase is deacylated following injection, activating the drug to increase thrombolysis by increasing plasminogen's conversion to plasmin. Plasmin breaks down the fibrin of the thrombus to break up the clot and release arterial blockages.

Pharmacodynamic

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.

Pharmacokinetics

Tmax: 0.15 h

Cmax: 5.59

Volume of distribution: 5.90

Clearance: 3.87

Terminal phase elimination half-life: 1.16

Drug indications

For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction

Dosage

30 units IV once over 2 to 5 minutes.

Drug contraindications

Contraindicated in patients with history of severe allergic reaction to anistreplase or streptokinase and in those with active internal bleeding, CVA, recent (within the past 2 months) intraspinal or intracranial surgery or trauma, aneurysm, arteriovenous malformation, intracranial neoplasm, uncontrolled hypertension, or known bleeding diathesis.

Side effects

Adverse reactions
CNS: intracranial hemorrhage.
CV: flushing, ARRHYTHMIAS, conduction disorders, hypotension.
GI: hemorrhage, gum or mouth hemorrhage.
GU: hematuria.
Hematologic: bleeding tendency, bleeding at puncture sites, eosinophilia.
Musculoskeletal: arthralgia.
Respiratory: hemoptysis.
Skin: hematoma, urticaria, pruritus, delayed purpuric rash (2 weeks after therapy).
Other: anaphylaxis

Adrenocorticoids, cefamandole, cefoperazone, cefotetan, corticotropin (long-term therapy), ethacrynic acid, glucocorticoids, plicamycin, valproic acid: May increase risk of severe hemorrhage. Use with extreme caution and monitor patient closely.
Drugs that alter platelet function (including aspirin, dipyridamole, and NSAIDs), heparin, oral anticoagulants: May increase risk of bleeding. Monitor patient closely.

Alerts

Each patient being considered for therapy with anistreplase should be carefully evaluated and anticipated benefits should be weighed against potential risks associated with the therapy.

 In the following conditions, the risks of anistreplase therapy may be increased and should be weighed against the anticipated benefits: Recent (within 10 days) major surgery (e.g., coronary artery bypass graft, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels); cerebrovascular disease; recent gastrointestinal or genitourinary bleeding (within 10 days); recent trauma (within 10 days). Hypertension: systolic BP ³180 mm Hg and/or diastolic ³110 mm Hg; high likelihood of left heart thrombus (e.g., mitral stenosis with atrial fibrillation); subacute bacterial endocarditis; hemostatic defects including those secondary to severe hepatic or renal disease; pregnancy; diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions; septic thrombophlebitis or occluded AV cannula at seriously infected site; advanced age (i.e., over 75 years old); patients currently receiving oral anticoagulants (e.g., warfarin sodium); any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of its location; acute pericarditis.

Points of recommendation

  • Life style changes such as diet, not smoking and exercise are often recommended following a heart attack. It is important to understand what you can do to reduce your risk of a heart attack. Discuss this with your doctor or health care professional.
  • Instruct patient and caregiver to recognize and report signs and symptoms of internal bleeding.
  • Inform patient about importance of strict bed rest.


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