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Activase
alteplase
Adult Dosing .
Dosage forms: INJ
acute myocardial infarction
- [accelerated infusion, <67 kg]
- Dose: 15 mg IV x1, then 0.75 mg/kg/dose IV over 30min, then 0.5 mg/kg/dose IV over 60min; Max: 100 mg/total dose
- [accelerated infusion, >67 kg]
- Dose: 15 mg IV x1, then 50 mg IV over 30min, then 35 mg IV over 60min; Max: 100 mg/total dose
- [3h infusion, <65 kg]
- Dose: 0.075 mg/kg/dose IV x1, then 0.675 mg/kg IV over 60min, then 0.5 mg/kg IV over 120min; Max: 100 mg/total dose
- [3h infusion, >65 kg]
- Dose: 60 mg IV over 60min, then 40 mg IV over 120min; Max: 100 mg/total dose; Info: give 6-10 mg of first dose as bolus, then remainder over 60min
acute ischemic stroke
- [0.9 mg/kg/total dose IV over 60min]
- Start: ASAP within 3h of symptom onset; give 10% total dose (0.09 mg/kg/dose) IV x1, then remaining 90% (0.81 mg/kg/dose) IV over 60min; Max: 90 mg/total dose; Info: D/C if pre-tx INR >1.7 or aPTT incr; may give within 3-4.5h of symptom onset if patient <81 yo without diabetes mellitus and prior stroke history, no anticoagulant use, NIHSS score <26, and ischemic injury <33% MCA territory on imaging
acute massive pulmonary embolism
- [100 mg IV over 2h]
renal dosing
- [see below]
- renal impairment: no adjustment
- HD/PD: not defined
hepatic dosing
- [see below]
- mild-moderate impairment: not defined; severe impairment: not defined, caution advised
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- internal bleeding, active
- intracranial aneurysm
- intracranial AVM
- intracranial neoplasm
- intracranial surgery within 3mo
- intraspinal surgery within 3mo
- serious head trauma within 3mo
- ischemic stroke within prior 3mo
- bleeding diathesis
- HTN, severe uncontrolled
- aortic dissection, known or suspected (stroke or MI use)
- intracranial hemorrhage (stroke use)
- subarachnoid hemorrhage (stroke use)
- GI bleeding within 21 days (stroke use)
- GU bleeding within 21 days (stroke use)
- infective endocarditis (stroke use)
- caution: surgery, recent major
- caution: trauma, recent
- caution: intracranial hemorrhage, recent
- caution: internal bleeding within 2-4wk (MI or PE use)
- caution: cerebrovascular disease
- caution: HTN
- caution: pericarditis, acute
- caution: SBE
- caution: LV thrombus
- caution: hemostatic disorder
- caution: ophthalmic condition, hemorrhagic
- caution: thrombophlebitis, septic
- caution: occluded AV cannula at serious infection site
- caution: hepatic impairment, severe
- caution: anticoagulant use, concurrent
- caution: patients >75 yo
Drug Interactions .
Overview
alteplase
thrombolytic
- angioedema
- anticoagulant
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- bleeding, severe
- intracranial hemorrhage
- thromboembolism
- cholesterol embolism
- hypersensitivity reaction
- anaphylaxis
Common Reactions
- bleeding
Safety/Monitoring .
Monitoring Parameters
Stroke: PT/INR, aPTT at baseline, then periodically; BP at baseline, then q15min x2h, then q30min x6h, then q1h x16h; signs/symptoms of hypersensitivity reaction during infusion and for at least 2h after D/C
All Other Indications: PT/INR, aPTT, BP at baseline, then periodically; signs/symptoms of hypersensitivity reaction during infusion and for at least 2h after D/C
Look/Sound-Alike Drug Names
Activase confused with: Retavase; TNKase
alteplase confused with: TNKase
t-pa (synonym for alteplase) confused with: TNKase
Pregnancy/Lactation .
Pregnancy
Clinical Summary
benefits outweigh risks during pregnancy; risk of fetal harm not expected based on limited human data; risk of hemorrhage in pregnant patients during delivery based on drug's mechanism of action
Lactation
Clinical Summary
may use while breastfeeding; no human data available, though risk of infant harm or adverse effects on milk production not expected based on drug properties
Pharmacology .
Metabolism: for alteplase: liver; CYP450: unknown
Excretion: for alteplase: urine; Half-life: <5min (initial), 72min (terminal); Info: >50% elimination occurs during initial phase
Subclass: Stroke ; Thrombolytics, Recombinant Tissue Plasminogen Activators (rtPA)
Mechanism of Action
for alteplase: binds to fibrin and converts tissue plasminogen to plasmin, promoting fibrinolysis
Formulary .
No Formulary Selected
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