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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 w/in 3h of sx 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 w/in 3-4.5h of sx onset if pt <81 yo w/o diabetes mellitus and prior stroke hx, 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 w/in 3mo
- intraspinal surgery w/in 3mo
- serious head trauma w/in 3mo
- ischemic stroke w/in 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 w/in 21 days (stroke use)
- GU bleeding w/in 21 days (stroke use)
- infective endocarditis (stroke use)
- caution: surgery, recent major
- caution: trauma, recent
- caution: intracranial hemorrhage, recent
- caution: internal bleeding w/in 2-4wk (MI or PE use)
- caution: cerebrovascular dz
- 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: pts >75 yo
Drug Interactions .
Overview
alteplase
thrombolytic
- angioedema
- anticoagulant
Contraindicated
- defibrotide
- mifepristone
Avoid/Use Alternative
- anagrelide
- caplacizumab
- collagenase clostridium histolyticum
- danshen
- edoxaban
- enoxaparin
- fondaparinux
- ibritumomab tiuxetan
- lifileucel
- omacetaxine mepesuccinate
- rivaroxaban
- vorapaxar
Monitor/Modify Tx
- acalabrutinib
- ado-trastuzumab emtansine
- aducanumab
- afatinib
- anacaulase topical
- antithrombin
- apixaban
- argatroban
- asparaginase
- aspirin
- avapritinib
- axitinib
- bevacizumab
- binimetinib
- bivalirudin
- brentuximab vedotin
- bromelain
- bromfenac ophthalmic
- cabazitaxel
- cabozantinib
- calaspargase
- cangrelor
- cannabis
- carfilzomib
- cefaclor
- cefadroxil
- cefazolin
- cefdinir
- cefepime
- cefixime
- cefotetan
- cefoxitin
- cefpodoxime
- cefprozil
- ceftazidime
- ceftriaxone
- cefuroxime axetil
- cefuroxime sodium
- celecoxib
- cephalexin
- cilostazol
- citalopram
- clopidogrel
- cysteamine
- dabigatran
- dalteparin
- dasatinib
- deferasirox
- desvenlafaxine
- deuruxolitinib
- diclofenac
- diclofenac ophthalmic
- diclofenac topical
- diflunisal
- dimethyl fumarate
- diosmin
- dipyridamole
- diroximel fumarate
- donanemab
- duloxetine
- encorafenib
- epoprostenol
- eptifibatide
- erlotinib
- escitalopram
- etodolac
- evening primrose oil
- fenoprofen
- fenugreek
- fluoxetine
- flurbiprofen
- flurbiprofen ophthalmic
- fluvoxamine
- fruquintinib
- garlic
- gefitinib
- gemtuzumab ozogamicin
- ginkgo
- heparin
- hydrocortisone
- ibrutinib
- ibuprofen
- ibuprofen lysine
- icosapent ethyl
- iloprost inhaled
- imatinib
- indomethacin
- ketoprofen
- ketorolac
- ketorolac ophthalmic
- lecanemab
- lenvatinib
- levomilnacipran
- magnesium salicylate
- meclofenamate
- mefenamic acid
- meloxicam
- methotrexate
- methyl salicylate topical
- milnacipran
- mitotane
- monomethyl fumarate
- mycophenolate mofetil
- mycophenolic acid
- nabumetone
- naproxen
- nattokinase
- nepafenac ophthalmic
- niacin (vitamin B3)
- nilotinib
- nintedanib
- nusinersen
- omega-3-acid
- oxaliplatin
- oxaprozin
- pacritinib
- paroxetine
- pazopanib
- pegaspargase
- penicillin G
- pentosan polysulfate sodium
- pentoxifylline
- piperacillin
- piroxicam
- pirtobrutinib
- plasminogen, human
- ponatinib
- porfimer
- pralsetinib
- prasugrel
- ramucirumab
- ranibizumab
- regorafenib
- resveratrol
- rifampin
- salsalate
- saw palmetto
- selpercatinib
- selumetinib
- sertraline
- sirolimus albumin-bound
- sorafenib
- sotatercept
- sugammadex
- sulindac
- sunitinib
- testosterone
- ticagrelor
- tipranavir
- tirofiban
- tisotumab vedotin
- tivozanib
- tolmetin
- tovorafenib
- trametinib
- trazodone
- treprostinil
- upadacitinib
- vadadustat
- valproic acid
- vandetanib
- venlafaxine
- vilazodone
- vinpocetine
- vortioxetine
- warfarin
- willow bark
- zanubrutinib
- ziv-aflibercept
Caution Advised
- aminocaproic acid
- benazepril
- fosinopril
- isosorbide dinitrate
- isosorbide mononitrate
- nitroglycerin
- quinapril
- tranexamic acid
Adverse Reactions .
Serious Reactions
- bleeding, severe
- intracranial hemorrhage
- thromboembolism
- cholesterol embolism
- hypersensitivity rxn
- 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; s/sx hypersensitivity rxn during infusion and for at least 2h after D/C
All Other Indications: PT/INR, aPTT, BP at baseline, then periodically; s/sx hypersensitivity rxn 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 maternal hemorrhage 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: liver; CYP450: unknown
Excretion: 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
binds to fibrin and converts tissue plasminogen to plasmin, promoting fibrinolysis
Formulary .
No Formulary Selected
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