TRASYLOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRASYLOL (TRASYLOL).
Aprotinin is a serine protease inhibitor that forms reversible enzyme-inhibitor complexes with trypsin, plasmin, kallikrein, and chymotrypsin, thereby inhibiting fibrinolysis and reducing perioperative blood loss.
| Metabolism | Aprotinin is metabolized predominantly by proteolytic degradation in the kidney; less than 10% is excreted unchanged in the urine. |
| Excretion | Primarily renal excretion; 70-80% of aprotinin is eliminated unchanged in urine within 48 hours; minor biliary/fecal elimination (<5%). |
| Half-life | Terminal elimination half-life approximately 2 hours (alpha phase) and 10-12 hours (beta phase); prolongation in renal impairment. |
| Protein binding | Approximately 40-60% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.4 L/kg; indicates limited extravascular distribution and high binding to tissue proteases. |
| Bioavailability | Not applicable for oral route (degraded in GI tract); intravenous bioavailability is 100%. |
| Onset of Action | Intravenous: immediate (within minutes); direct application to surgical field: within seconds. |
| Duration of Action | Biological effects persist for up to 6-8 hours after a single dose; antifibrinolytic effect lasts approximately 4-6 hours; clinical duration guides redosing during surgery. |
1,000,000 KIU (kallikrein inhibitor units) IV loading dose over 10 minutes, followed by 250,000 KIU/hour continuous IV infusion during surgery; also 1,000,000 KIU added to cardiopulmonary bypass circuit prime volume.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustments recommended; use caution in patients with severe renal impairment (CrCl <30 mL/min) due to limited data. |
| Liver impairment | No specific Child-Pugh based adjustments defined; consider cautious use in severe hepatic impairment (Child-Pugh C) due to altered protein binding. |
| Pediatric use | Not established; use is not recommended in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor renal function and bleeding risk due to age-related physiological changes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRASYLOL (TRASYLOL).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not established. Caution advised; consider risk of neonatal bleeding. |
| Teratogenic Risk | FDA Category B. No evidence of teratogenicity in animal studies. Insufficient human data; avoid use in first trimester unless essential. Risk of fetal hemorrhage with maternal use near term due to anticoagulant effects. |
| Fetal Monitoring |
■ FDA Black Box Warning
TRASYLOL (aprotinin) was voluntarily withdrawn from the U.S. market in 2008 due to safety concerns including increased risk of death, renal failure, congestive heart failure, and stroke. The FDA recommends use only in specific research settings under a special protocol.
| Serious Effects |
["Hypersensitivity to aprotinin or any component of the formulation","Re-exposure within 6-12 months (due to high risk of anaphylaxis)","Pre-existing renal dysfunction (e.g., serum creatinine >2.0 mg/dL or dialysis dependence)","Concurrent use of other anticoagulants or antiplatelet agents (relative)","Pregnancy (Category B, but risk-benefit should be considered)"]
| Precautions | ["Risk of anaphylactic reactions, especially upon re-exposure within 6 months","Increased risk of renal toxicity including acute renal failure","Increased risk of thrombotic events such as stroke and myocardial infarction","Contraindicated in patients with known hypersensitivity to aprotinin","Should not be used in patients with pre-existing renal impairment or undergoing deep hypothermic circulatory arrest"] |
Loading safety data…
| Monitor coagulation parameters (PT, aPTT, fibrinogen), renal function, and signs of bleeding. Fetal monitoring for distress during labor if used near term. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data lacking. |