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Pronunciation |
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(a
NISS tre
plase) |
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U.S. Brand
Names |
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Eminase® |
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Generic
Available |
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No |
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Synonyms |
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Anisoylated Plasminogen Streptokinase Activator Complex; APSAC |
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Pharmacological Index |
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Thrombolytic Agent |
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Use |
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Management of acute myocardial infarction (AMI) in adults; lysis of thrombi
obstructing coronary arteries; reduction of infarct size |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to anistreplase or streptokinase; active internal bleeding;
history of CVA; recent (within 2 months) intracranial or intraspinal surgery or
trauma, intracranial neoplasm, arteriovenous malformation, or aneurysm; known
bleeding diathesis; severe uncontrolled hypertension |
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Warnings/Precautions |
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Concurrent heparin anticoagulation can contribute to bleeding; pay careful
attention to all potential bleeding site. I.M. injections and nonessential
handling of the patient should be avoided. Venipunctures should be performed
carefully and only when necessary. If arterial puncture is necessary use an
upper extremity vessel that can be manually compressed. If serious bleeding
occurs then the infusion of anistreplase and heparin should be stopped.
Coronary thrombolysis may result in reperfusion arrhythmias. Hypotension,
occasionally severe, can occur (not from bleeding or anaphylaxis). Follow
standard MI management. Rare anaphylactoid reactions can occur. Cautious repeat
administration in patients who have received anistreplase or streptokinase
within 1 year (antistreptokinase antibody may decrease effectiveness or risk of
allergic reactions). Safety and efficacy in pediatric patients have not been
established. |
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Adverse
Reactions |
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As with all drugs which may affect hemostasis, bleeding is the major adverse
effect associated with anistreplase. Hemorrhage may occur at virtually any site.
Risk is dependent on multiple variables, including the dosage administered,
concurrent use of multiple agents which alter hemostasis, and patient
predisposition. Rapid lysis of coronary artery thrombi by thrombolytic agents
may be associated with reperfusion-related atrial and/or ventricular
arrhythmias.
Central nervous system: Intracranial hemorrhage (1%)
Cardiovascular: Hypotension (10.4%)
Gastrointestinal: Gastrointestinal hemorrhage (2%), gingival hemorrhage (1%)
Genitourinary: Hematuria (2.4%)
Hematologic: Hematoma (2.8%)
Local: Bleeding at puncture sites (4.6%)
Respiratory: Hemoptysis (2.2%)
<1% (Limited to important or life-threatening symptoms): Anaphylactic
reaction, anaphylactoid reaction, bronchospasm, angioedema, urticaria, pruritus,
flushing, rash (sometimes with delayed appearance 1-2 weeks after treatment),
eosinophilia, arthralgia, pedal edema, proteinuria, vasculitis,
Guillain-Barré syndrome, adult respiratory distress
syndrome, epistaxis, anemia, ocular hemorrhage
<10% (Unknown causal relationship): Chills, fever, headache, shock,
cardiac rupture, emboli, nausea, vomiting, diaphoresis, purpura,
thrombocytopenia, elevated transaminases, arthralgia, agitation, dizziness,
paresthesia, tremor, vertigo, dyspnea, pulmonary edema |
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Drug
Interactions |
|
Aminocaproic acid (antifibrinolytic agent) may decrease effectiveness.
Drugs which affect platelet function (eg, NSAIDs, dipyridamole, ticlopidine,
clopidogrel, IIb/IIIa antagonists) may potentiate the risk of hemorrhage; use
with caution.
Heparin and aspirin: Use with aspirin and heparin may increase the risk of
bleeding. However, aspirin and heparin were used concomitantly with anistreplase
in the majority of patients in clinical studies. Aspirin was not associated with
an increased rate of hemorrhagic CVAs in clinical trials.
Warfarin or oral anticoagulants: Risk of bleeding may be increased during
concurrent therapy. |
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Stability |
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Store between 2°C and 8°C
(36°F to 46°F); discard solution 30
minutes after reconstitution if not administered; do not shake
solution |
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Mechanism of
Action |
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Activates the conversion of plasminogen to plasmin by forming a complex
exposing plasminogen-activating site and cleavage of a peptide bond that
converts plasminogen to plasmin; plasmin being capable of thrombolysis, by
degrading fibrin, fibrinogen and other procoagulant proteins into soluble
fragments, effective both outside and within the formed
thrombus/embolus |
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Pharmacodynamics/Kinetics |
|
Duration of action: Fibrinolytic effect persists for 4-6 hours following
administration
Metabolism: Anistreplase is an acylated complex of streptokinase with
lys-plasminogen; one of the purposes of this acylation is to extend the serum
circulating time of anistreplase; because deacylation of the complex occurs more
rapidly than dissociation, fibrinolytic activity is controlled by the rate of
deacylation rather than of dissociation
Half-life: 70-120 minutes |
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Usual Dosage |
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Adults: I.V.: 30 units injected over 2-5 minutes as soon as possible after
onset of symptoms |
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Cardiovascular
Considerations |
|
It is important that in using thrombolytic therapy in an institution, that
the protocol for that institution be followed closely, particularly in terms of
dosage, adjunctive heparin therapy, and monitoring of coagulation profiles. It
is important that consideration of preceding recent thrombolytic therapy be
taken into account when invasive procedures, particularly intravascular
procedures, are undertaken. It is important that close clinical monitoring be
carried out to ensure efficacy of therapy. Failure of therapy may require
emergent cardiac catheterization and interventional therapy. Reperfusion after
successful thrombolysis may be associated with rapid resolution of EKG changes
and restoration of cardiac function. However, reperfusion arrhythmias may also
manifest. |
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Mental Health: Effects
on Mental Status |
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None reported |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause hypotension which may be exacerbated by
psychotropics |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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I.V. administration for cardiac emergencies: Patient instruction should be
appropriate to situation. Following infusion, absolute bedrest is important;
call for assistance changing position. You will have increased tendency to
bleed; avoid razors, scissors or sharps, and use soft toothbrush or cotton
swabs. Report back pain, abdominal pain, muscle cramping, acute onset headache,
chest pain, or bleeding. |
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Nursing
Implications |
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Drug should not be used for any condition in which bleeding constitutes a
significant hazard or would be particularly difficult to
manage |
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Dosage Forms |
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Powder for injection, lyophilized: 30
units |
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