Action
Converts plasminogen to plasmin, an enzyme that degrades fibrin clots and lyses thrombi and emboli
Availability
Powder for injection: 250,000, 750,000, and 1.5 million international units/vial
Indications and dosages
➣ Acute evolving transmural myocardial infarction
Adults: 1.5 million international units by I.V. infusion over 1 hour as soon as possible after symptom onset. For intracoronary infusion, 20,000 international units by I.V. bolus via coronary catheter, followed by infusion of 2,000 international units/minute over 1 hour (total of 140,000 international units).
➣ Deep-vein thrombosis (DVT)
Adults: Loading dose of 250,000 international units by I.V. infusion over 30 minutes, followed by 100,000 international units/hour I.V. for 72 hours. Begin therapy as soon as possible after thrombotic symptoms begin (preferably within 7 days).
➣ Pulmonary emboli
Adults: Loading dose of 250,000 international units by I.V. infusion over 30 minutes, then 100,000 international units/hour I.V. for 24 hours (or 72 hours if concurrent DVT is suspected). Begin therapy as soon as possible after thrombotic symptoms begin (preferably within 7 days).
➣ Arterial thrombosis or emboli
Adults: Loading dose of 250,000 international units by I.V. infusion over 30 minutes, then 100,000 international units/hour I.V. for 24 to 72 hours. Begin therapy as soon as possible after thrombotic symptoms begin (preferably within 7 days).
Contraindications
• Hypersensitivity to drug or anistreplase
• Cerebrovascular accident, intracranial or intraspinal surgery within past 2 months
• Active internal bleeding
• Intracranial neoplasm
• Severe, uncontrolled hypertension
Precautions
Use cautiously in:
• severe hepatic or renal disease, recent major surgery or trauma, obstetric delivery, acute pericarditis, infectious endocarditis, atrioventricular malformation or aneurysm, suspected thrombus in left side of heart, septic thrombophlebitis or occluded arteriovenous cannula at seriously infected site
• conditions in which bleeding may be hard to manage (such as organ biopsy, peptic ulcer, previous puncture of noncompressible blood vessel)
• history of cerebrovascular disease
• use of drug within past 2 years
• concurrent anticoagulant use
• elderly patients
• pregnant or breastfeeding patients.
Administration
See Before giving, make sure hydrocortisone is available to treat allergic reaction and aminocaproic acid is available to treat excessive bleeding.
See As ordered, give test dose of 100 international units intradermally to check for hypersensitivity. Wheal-and-flare response within 20 minutes indicates probable allergy.
• To reconstitute, add 5 ml of normal saline solution or dextrose 5% in water to each vial, then dilute again to 45 ml. Roll vial gently between hands; don't shake.
• If necessary, dilute further to 50 ml in plastic container or to 500 ml in glass bottle.
• Don't mix with other drugs or give other drugs through same I.V. line.
Adverse reactions
CNS: headache, intracranial hemorrhage
CV: hypotension, arrhythmias
EENT: periorbital swelling
GI: nausea, vomiting, GI hemorrhage
GU: hematuria
Hematologic: anemia, bleeding tendency
Musculoskeletal: musculoskeletal pain
Respiratory: minor breathing difficulties, bronchospasm, apnea
Skin: urticaria, itching, flushing
Other: bleeding at puncture sites, delayed hypersensitivity reaction
Interactions
Drug-drug. Anticoagulants, aspirin, dipyridamole, indomethacin, phenylbutazone: increased risk of bleeding
Drug-diagnostic tests. Hemoglobin: decreased value
International Normalized Ratio, transaminases: increased values
Partial thromboplastin time (PTT), prothrombin time (PT): prolonged
Patient monitoring
• Monitor vital signs and neurologic status carefully after giving test dose and throughout therapy.
See Watch for signs and symptoms of hypersensitivity reaction. Stop drug if these occur.
• Check for bleeding every 15 minutes for first hour, every 30 minutes for next 7 hours, then every 4 hours.
See Stop therapy and contact prescriber immediately if excessive bleeding occurs.
• Assess neurologic status closely. Watch for indications of intracranial bleeding.
• Handle patient gently and sparingly. If necessary, pad bed rails to prevent injury.
• Monitor pulse rate every hour. Also monitor distal circulation.
• Monitor PTT, PT, plasma thrombin time, hemoglobin, hematocrit, and platelet count.
• Avoid giving I.M. injections during therapy.
Patient teaching
• Tell patient why he's receiving drug.
See Teach patient to recognize and immediately report signs or symptoms of hypersensitivity reaction or excessive bleeding.
• Instruct patient to report unusual bruising or bleeding. Teach him safety measures to avoid bruising and bleeding.
• Advise patient that he'll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.