reteplase (Rx)

Frequency Not Defined

Reperfusion arrhythmias, hypotension

Dizziness, fever, severe headache

Anemia, cholesterol embolization, GI/GU bleeding, intracranial hemorrhage

Nausea, vomiting

Cardiac reinfarction

Cardiogenic shock

Muscle pain

Allergic reaction, injection site reaction

Contraindications

Hypersensitivity

Active bleeding, recent CVA, recent intracranial or intraspinal surgery or trauma, intracranial neoplasm, AVM, aneurysm, bleeding diathesis, severe uncontrolled HTN

See thrombolytic indications/contraindications

Cautions

Recent major surgery, cerebrovascular disease, recent GI or GU bleeding, HTN, acute pericarditis, hemostatic defects, severe thrombophlebitis, severe hepatic/renal dysfunction, currently receiving oral anticoagulants, diabetic hemorrhagic retinopathy, elderly

Monitor potential bleeding sites

Cholesterol embolism reported

Ischemic Stroke: may have no benefit if used after 3 hr of onset

Current use of warfarin and INR in high range may increase bleeding risk

Pregnancy Category: C

Lactation: Not known whether drug crosses into breast milk, unlikely patients will be concerned about nursing in indicated circumstances

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Reteplase is the r-PA (recombinant plasminogen activator) with nonglycosylated deletion mutant of wild-type tissue plasminogen activator (tPA); has less high-affinity fibrin binding, longer half-life, & greater thrombolytic potency than tPA

Promotes thrombolysis by converting plasminogen to plasmin which degrades fibrin & fibrinogen

Pharmacokinetics

Half-Life: 13-16 min

Onset: Coronary thrombolysis occurs in 30 min, reaches peak response at 30-90 min

Metabolism: Inactivated by blood components C1 inactivator, alfa-1-antitrypsin, alfa-2-antiplasmin

Excretion: Urine and feces

Plasma clearance: 250-450 mL/min

IV Incompatibilities

Y-site: bivalirudin

Additive, Syringe, Y-site: heparin

IV Preparation

Reconstitute using diluent, needle, syringe & dispensing pin provided to obtain 1 U/mL soln

IV Administration

Bolus over 2 min

Do not admin solutions that are discolored or contain precipitate

Slight foaming may occur

• May need to stand undisturbed for several minutes to dissipate bubbles

Flush before & after each bolus

Line to contain D5W

Stability

Stable for 4 hr at room temp