CATHFLO ACTIVASE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CATHFLO ACTIVASE (CATHFLO ACTIVASE).
Tissue plasminogen activator that converts plasminogen to plasmin, leading to fibrinolysis.
| Metabolism | Primarily hepatic metabolism; not well characterized. |
| Excretion | Primarily hepatic metabolism; renal excretion of inactive metabolites accounts for <5% of the dose. Biliary/fecal elimination is minimal (<1%). |
| Half-life | Initial half-life: 4–6 minutes (alpha phase); terminal half-life: 30–50 minutes (beta phase). Clinical context: Rapid clearance from plasma; effects on fibrinogen depletion persist for 12–24 hours. |
| Protein binding | Approximately 50% bound to plasma proteins (primarily fibrinogen and albumin). Binding is concentration-dependent due to fibrin affinity. |
| Volume of Distribution | 0.08–0.15 L/kg (approximately 5–10 L in a 70 kg adult). Clinical meaning: Confined largely to plasma compartment; limited extravascular distribution. |
| Bioavailability | Intravenous: 100% (only route). Not administered orally due to extensive first-pass metabolism (>95% degradation). |
| Onset of Action | Intravenous bolus: restoration of catheter function within 2–5 minutes. Intravenous infusion (for acute MI): lysis begins within 20–30 minutes. |
| Duration of Action | Fibrinolytic effect: 4–6 hours post-dose; restoration of catheter patency persists for the life of the catheter (typically days to weeks). Clinical notes: Clot dissolution occurs rapidly; reocclusion may occur if underlying thrombus persists. |
2 mg via intracatheter instillation, dwell for 2 hours, then aspirate; may repeat once if occlusion persists. For occluded central venous access devices only.
| Dosage form | VIAL |
| Renal impairment | No dose adjustment required for renal impairment; drug is cleared primarily by the liver. |
| Liver impairment | No specific Child-Pugh based adjustments; use caution in severe hepatic impairment due to increased bleeding risk. |
| Pediatric use | Weight <30 kg: 2 mg per lumen; weight ≥30 kg: 2 mg per lumen, same adult regimen. Safety and efficacy in neonates not established. |
| Geriatric use | No specific dose adjustment based on age alone; monitor for bleeding events as elderly may have higher bleeding risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CATHFLO ACTIVASE (CATHFLO ACTIVASE).
| Breastfeeding | Unknown if excreted in human milk; likely due to low molecular weight. M/P ratio not established. Consider discontinuing breastfeeding or drug based on importance to mother. |
| Teratogenic Risk | Insufficient human data; animal studies not conducted. As a thrombolytic agent, risk of hemorrhage during first trimester may cause pregnancy loss. Second/third trimester: risk of placental abruption, preterm labor, fetal hemorrhage. Use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: RISK OF BLEEDING. Activase (alteplase) can cause significant, sometimes fatal, bleeding. Do not use in patients with active internal bleeding, recent stroke, or other bleeding risks.
| Serious Effects |
Active internal bleeding, recent intracranial or intraspinal surgery, recent stroke, known bleeding diathesis, severe uncontrolled hypertension, recent head trauma.
| Precautions | Bleeding risk including intracranial hemorrhage; monitor for bleeding; avoid in patients with recent surgery, trauma, or coagulopathy; risk of cholesterol embolism. |
| Food/Dietary | No known food interactions. Maintain normal diet unless otherwise instructed. |
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| Monitor for signs of bleeding (e.g., placental abruption, vaginal bleeding), fetal distress via electronic fetal monitoring, and uterine activity. Assess maternal coagulation parameters (fibrinogen, PT, aPTT). |
| Fertility Effects | No human data on fertility impact; no animal studies. Theoretical risk of ovarian hemorrhage; not expected to impair fertility long-term. |
| Clinical Pearls |
| CATHFLO ACTIVASE (alteplase) is used to restore patency to occluded central venous access devices. Do not use if known or suspected catheter-related infection or thrombosis. Administer as a 2 mg instillation; clamp for 1 hour, then aspirate. Do not administer if patient has active bleeding or recent stroke. Use with caution in patients with risk of bleeding. After instillation, do not flush vigorously; gentle aspiration is key. |
| Patient Advice | This medication is used to unblock your central line catheter. · You may feel a temporary pinch or pressure during instillation. · Inform your healthcare provider immediately if you experience pain, swelling, or bleeding at the catheter site. · Do not attempt to flush the catheter yourself after the medication is given. · You may be asked to wait for up to an hour while the medication works. |