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Alteplase

ACTIVASE

Pronunciation: AL-te-plays

Alteplase ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Alteplase ballicule

What it isRecombinant tissue plasminogen activator converting plasminogen to plasmin; acute ischemic stroke, STEMI and massive PE.

Why this oneIt dissolves clot that has already formed, which no anticoagulant does.

What limits it⚑ Benefit falls steeply after 4.5 hours in stroke. Intracranial hemorrhage is the price; screen every contraindication before use.

FDA label

FDA dosingPopulationStartTargetMax
Acute ischemic strokeAdults0.9 mg/kg IV (max 90 mg): 10% as bolus over 1 min, remainder over 60 min90 mg total
Acute myocardial infarctionAdultsWeight-based (accelerated or 3-h regimen)100 mg total
Acute massive pulmonary embolismAdults100 mg IV over 2 h100 mg

Renal Undefined

Hepatic Undefined

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

Cost

Alteplase (ACTIVASE)
Strength#/mogeneric $/unitCostPlus
50 mg/vialinjper unitnot offered
100 mg/vialinjper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Alteplase is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskIntracranial hemorrhage; the time window is everything

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Sedation liability0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

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