Davis's Drug Guide

anistreplase

General

High Alert Medication: This medication bears a heightened risk of causing significant patient harm when it is used in error.

**Off Market Drug**
This medication is no longer available in the United States. Information provided here is for reference purposes only.


Pronunciation
an-EYE-strep-lase

Trade Name(s)

• anisoylated plasminogen–streptokinase activator complex

• APSAC

• Eminase [Canada]



Pregnancy Category
Category C

Ther. class.
thrombolytics

Pharm. class.
plasminogen activators

Indications

• Acute myocardial infarction (MI)

• Pulmonary embolism (PE)

Action

Combines with plasminogen to form activator complexes, then converts plasminogen to plasmin, which is then able to degrade clot-bound fibrin

Therapeutic Effect(s):

• Lysis of thrombi in coronary arteries, with preservation of ventricular function

• Lysis of pulmonary emboli and subsequent restoration of blood flow

Pharmacokinetics

Absorption: Complete after IV administration

Distribution: Unknown

Metabolism and Excretion: Inactivated by binding to plasmin inactivators

Half-life: 70–120 minutes

TIME/ACTION PROFILE (fibrinolysis)

ROUTEONSETPEAKDURATION
IVunknown45 min6 hr†

†Systemic hyperfibrinolytic state may persist for up to 2 days

Contraindication/Precautions

Contraindicated in:

• Active internal bleeding

• History of cerebrovascular accident

• Recent (within 2 months) intracranial or intraspinal injury or trauma

• Intracranial neoplasm, arteriovenous malformation, or aneurysm

• Severe uncontrolled hypertension

• Known bleeding tendencies

• Hypersensitivity; cross-sensitivity with anistreplase and streptokinase may occur



Use Cautiously in:

• Recent (within 10 days) major surgery, trauma, GI or GU bleeding

• Left heart thrombus

• Severe hepatic or renal disease

• Hemorrhagic ophthalmic conditions

• Septic phlebitis

• Previous puncture of a noncompressible vessel

• Subacute bacterial endocarditis or acute pericarditis

• Recent streptococcal infection or previous therapy with anistreplase or streptokinase (within 5 days–6 mo); may produce resistance because of antibody formation; increased dosage requirements may be encountered (anistreplase and streptokinase only)

• Previous therapy with streptokinase or anistreplase (within 12 months); may produce resistance because of antibody formation

OB: Lactation: Pedi: Safety not established

Geri: Increased risk of intracranial bleeding



Exercise Extreme Caution in:

• Patients receiving warfarin therapy

OB: Early postpartum period (10 days)

Adverse Reactions/Side Effects

CNS: INTRACRANIAL HEMORRHAGE.

EENT: epistaxis, gingival bleeding.

Resp: bronchospasm, hemoptysis.

CV: reperfusion arrhythmias, hypotension, RECURRENT ISCHEMIA/THROMBOEMBOLISM.

GI: GI BLEEDING, hepatotoxicity, nausea, RETROPERITONEAL BLEEDING, vomiting.

GU: GU TRACT BLEEDING.

Derm: ecchymoses, flushing, urticaria.

Hemat: BLEEDING.

Local: hemorrhage at injection site, phlebitis at injection site.

MS: musculoskeletal pain.

Misc: ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS, fever.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

Aspirin, other NSAIDs, warfarin, heparin and heparin-like agents, abciximab, eptifibatide, tirofiban, clopidogrel, ticlopidine, or dipyridamole —concurrent use risk of bleeding, although these agents are frequently used together or in sequence

• Effects may be by antifibrinolytic agents, including aminocaproic acid, aprotinin, or tranexamic acid



Drug-Natural Products
anticoagulant effect and bleeding risk with anise, arnica, chamomile, clove, dong quai, fenugreek, feverfew, garlic, ginger, ginkgo, Panax ginseng, licorice, and others

Route/Dosage

IV (Adults): 30 units over 2–5 min.

Availability

Powder for injection: 30 units/vial

Assessment

• Begin therapy as soon as possible after the onset of symptoms

» Monitor vital signs, including temperature, continuously for myocardial infarction. Do not use lower extremities to monitor blood pressure. Notify physician if systolic BP >180 mm Hg or diastolic BP >110 mm Hg. Thrombolytic therapy should not be given if hypertension is uncontrolled. Inform physician if hypotension occurs. Hypotension may result from the drug, hemorrhage, or cardiogenic shock

» Assess patient carefully for bleeding every 15 min during the 1st hr of therapy, every 15–30 min during the next 8 hr, and at least every 4 hr for the duration of therapy. Frank bleeding may occur from sites of invasive procedures or from body orifices. Internal bleeding may also occur (decreased neurologic status; abdominal pain with coffee-grounds emesis or black, tarry stools; hematuria; joint pain). If uncontrolled bleeding occurs, stop medication and notify physician immediately

» Inquire about previous reaction to anistreplase or streptokinase therapy. Assess patient for hypersensitivity reaction (rash, dyspnea, fever, changes in facial color, swelling around the eyes, wheezing). If these occur, inform physician promptly. Keep epinephrine, an antihistamine, and resuscitation equipment close by in the event of an anaphylactic reaction

» Inquire about recent streptococcal infection. Anistreplase and streptokinase may be less effective if administered between 5 days and 12 months of a streptococcal infection

» Assess neurologic status throughout therapy. Altered sensorium or neurologic changes may be indicative of intracranial bleeding



Myocardial Infarction

• Monitor ECG continuously. Notify physician if significant arrhythmias occur. IV lidocaine or procainamide (Pronestyl) may be ordered prophylactically. Monitor cardiac enzymes. Radionuclide myocardial scanning and/or coronary angiography may be ordered 7–10 days after therapy to monitor effectiveness of therapy

» Assess intensity, character, location, and radiation of chest pain. Note presence of associated symptoms (nausea, vomiting, diaphoresis). Administer analgesics as directed. Notify physician if chest pain is unrelieved or recurs

» Monitor heart sounds and breath sounds frequently. Inform physician if signs of CHF occur (rales/crackles, dyspnea, S3 heart sound, jugular venous distention, relieved CVP)



Lab Test Considerations

• Hematocrit, hemoglobin, platelet count, fibrin/fibrin degradation product (FDP/fdp) titer, fibrinogen concentration, prothrombin time, thrombin time, and activated partial thromboplastin time may be evaluated before and frequently during therapy. Bleeding time may be assessed before therapy if patient has received platelet aggregation inhibitors

» Obtain type and crossmatch and have blood available at all times in case of hemorrhage

» Stools should be tested for occult blood loss and urine for hematuria periodically during therapy



Toxicity and Overdose

High Alert: If local bleeding occurs, apply pressure to site. If severe or internal bleeding occurs, discontinue infusion. Clotting factors and/or blood volume may be restored through infusions of whole blood, packed RBCs, fresh frozen plasma, or cryoprecipitate. Do not administer dextran; it has antiplatelet activity. Aminocaproic acid (Amicar) may be used as an antidote

Potential Nursing Diagnoses

• Ineffective tissue perfusion (Indications)

• Risk for injury (Side Effects)

Implementation

High Alert: Overdosage and under-dosage of thrombolytic medications have resulted in patient harm or death. Have second practitioner independently check original order, dosage calculations, and infusion pump settings

• Thrombolytic agents should be used only in settings in which hematologic function and clinical response can be adequately monitored

» Starting two IV lines before therapy is recommended: one for the thrombolytic agent, the other for any additional infusions

» Avoid invasive procedures, such as IM injections or arterial punctures, with this therapy. If such procedures must be performed, apply pressure to all arterial and venous puncture sites for at least 30 min. Avoid venipunctures at noncompressible sites (jugular vein, subclavian site)

» Acetaminophen may be ordered to control fever

Direct IV: Reconstitute with 5 ml of sterile water for injection (direct to sides of vial) and swirl gently; do not shake to minimize foaming. Do not dilute further. Use reconstituted solution within 30 min of preparation

Rate: Administer via IV line or vein over 2–5 min

Y-Site Incompatibility: Do not admix or administer via Y-site injection with any other medications

Patient/Family Teaching

• Explain purpose of medication and the need for close monitoring to patient and family. Instruct patient to report hypersensitivity reactions (rash, dyspnea) and bleeding or bruising

• Explain need for bedrest and minimal handling during therapy to avoid injury. Avoid all unnecessary procedures such as shaving and vigorous tooth brushing

Evaluation/Desired Outcomes

Lysis of thrombi and restoration of blood flow



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