Select a medication above to begin.
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
- 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
- revakinagene taroretcel
- 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 hemorrhage in pregnant pts 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
Join Now to View Patient Handouts!
Create a FREE epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.
Pill Pictures
Join Now to View Pill Pictures!
Create a FREE epocrates Online account to access full-color images of medications within the drug monograph.
Current Members: Sign In.