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alteplase (Rx)Brand and Other Names:Activase, TPA, more...Cathflo Activase

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

powder for injection (reconstitute before use)

  • 2mg (Cathflo Activase)
  • 50mg (Activase)
  • 100mg (Activase)
more...

Acute Myocardial Infarction

Administer as soon as possible after onset of symptoms

Recommended total dose for AMI is based on patient weight, not to exceed 100 mg, regardless of the selected administration regimen (accelerated or 3 hr)

Accelerated infusion (1-1/2 hr)

  • ≤67 kg: 15 mg IVP bolus over 1-2 minutes, THEN 0.75 mg/kg IV infusion over 30 minutes (not to exceed 50 mg), and THEN 0.5 mg/kg IV over next 60 minutes (not to exceed 35 mg over 1 hr) 
  • >67 kg (100 mg total dose infused over 1.5 hr): 15 mg IVP bolus over 1-2 minutes, THEN 50 mg IV infusion over next 30 minutes, and THEN remaining 35 mg over next 60 minutes  

3-hr infusion

  • <65 kg: 0.075 mg/kg IVP bolus over 1-2 minutes, THEN 0.675 mg/kg infused over the rest of the first hr, THEN 0.25 mg/kg IV for the next 2 hr 
  • ≥65 kg: (100 mg total dose infused over 3 hr): 6-10 mg IVP bolus over 1-2 minutes, THEN 50-54 mg infused over the rest of the first hr (ie, 60 mg in 1st hr including 6-10 mg bolus), THEN 20 mg/hr for the next 2 hr 

Pulmonary Embolism

100 mg IV infused over 2 hr; institute parenteral anticoagulation near the end of or immediately following alteplase infusion when the PTT or thrombin time returns to <2x normal

Acute Ischemic Stroke

0.9 mg/kg IV; not to exceed 90 mg total dose; administer 10% of the total dose as an initial IV bolus over 1 minute and the remainder infused over 60 minutes 

Dosing considerations (acute ischemic stroke)

  • Exclude intracranial hemorrhage as the primary cause of stroke signs and symptoms prior to initiation of treatment (see Contraindications)
  • Administer as soon as possible but within 3 hr after onset of symptoms
  • Monitor and control blood pressure during and following administration
  • In patients without recent use of oral anticoagulants or heparin, treatment can be initiated prior to the availability of coagulation study results
  • Discontinue if the pretreatment INR is >1.7 or the aPTT is elevated

Central Venous Catheter Occlusion

Cathflo Activase: 2 mg in 2 mL instilled into occluded catheter

Assess catheter function after 30 minutes of dwell time by attempting to aspirate blood; if unable to aspirate after 120 minutes dwell time, a 2nd dose may be administered and the process repeated

If catheter function restored, aspirate 4-5 mL blood to remove Cathflo Activase and residual clot

Gently irrigate with 0.9% NaCl

Arterial Thrombosis & Embolism (Off-label)

0.05-0.1 mg/kg/hr by transcatheter intra-arterial infusion for 1-8 hours or until lysis of thrombus 

Intracerebral Hemorrhage (Orphan)

Treatment of intraventricular hemorrhage associated with intracerebral hemorrhage

Orphan indication sponsor

  • Daniel F Hanley, MD; Johns Hopkins University, 600 N Wolfe St, Jefferson 1-109; Baltimore, MD 21287

Bronchitis (Orphan)

Orphan designation for treatment of plastic bronchitis

Sponsor

  • Kathleen A Stringer, PharmD, FCCP - Professor; University of Michigan; 428 Church St; Ann Arbor, MI 48109-1065

Dosage Forms & Strengths

powder for injection (reconstitute before use)

  • 2mg (Cathflo Activase)
more...

Central Venous Catheter Occlusion

<30 kg

  • Cathflo Activase: Instill 110% of the internal lumen volume of the catheter; not to exceed 2 mg in 2 mL

≥30 kg

  • Cathflo Activase: 2 mg instilled into occluded catheter
  • Assess catheter function after 30 minutes of dwell time by attempting to aspirate blood; if unable to aspirate after 120 minutes dwell time, a 2nd dose may be administered and the process repeated
  • If catheter function restored, aspirate 4-5 mL blood in patients 10 kg or more (aspirate 3 mL if <10 kg) to remove Cathflo Activase and residual clot
  • Gently irrigate with 0.9% NaCl
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Interactions

Interaction Checker

alteplase and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 
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            Adverse Effects

            1-10%

            Stroke (1.6%)

            Frequency Not Defined

            Accelerated idioventricular rhythm

            Pulmonary edema

            Arterial embolism

            Bruising

            Bleeding

            DVT

            Hypotension

            Intracranial hemorrhage

            GI/GU hemorrhage

            Pulmonary embolism

            Fever/chills

            Nausea/vomiting

            Sensitivity reaction

            Sepsis

            Shock

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            Warnings

            Contraindications

            Acute Ischemic Stroke

            • Do not administer to treat acute ischemic stroke in the following situations in which the risk of bleeding is greater than the potential benefit
              • Current intracranial hemorrhage
              • Subarachnoid hemorrhage
              • Active internal bleeding
              • Recent (within 3 months) intracranial or intraspinal surgery or serious head trauma
              • Presence of intracranial conditions that may increase the risk of bleeding (eg, some neoplasms, arteriovenous malformations, aneurysms)
              • Bleeding diathesis
              • Current severe uncontrolled hypertension

            Acute myocardial infarction or pulmonary embolism

            • Do not administer for treatment of AMI or PE in the following situations in which the risk of bleeding is greater than the potential benefit
              • Active internal bleeding
              • History of recent stroke
              • Recent (within 3 months) intracranial or intraspinal surgery or serious head trauma
              • Presence of intracranial conditions that may increase the risk of bleeding (eg, some neoplasms, arteriovenous malformations, aneurysms)
              • Bleeding diathesis
              • Current severe uncontrolled hypertension

            Cautions

            Use caution in recent major surgery, cerebrovascular disease, HTN, acute pericarditis, hemostatic defects, severe thrombophlebitis, severe hepatic/renal dysfunction

            Avoid intramuscular injections

            Monitor for bleeding; discontinue therapy if serious bleeding occurs

            Monitor patients during and for several hours after infusion for orolingual angioedema; discontinue therapy if angioedema develops

            Cholesterol embolism reported rarely in patients treated with thrombolytic agents

            Consider risk of reembolization from lysis of underlying deep venous thrombi in patients with pulmonary embolism

            Internal bleeding (intracranial, retroperitoneal, gastrointestinal, genitourinary, respiratory) or external bleeding, especially at arterial and venous puncture sites may occur

            Avoid intramuscular injections and trauma to patient while on therapy

            Perform venipunctures carefully and only as required

            Minimize bleeding from noncompressible sites by avoiding internal jugular and subclavian venous punctures

            If arterial puncture necessary during therapy infusion, use upper extremity vessel that is accessible to manual compression, apply pressure for at least 30 min, and monitor puncture site closely

            Patients treated for acute ischemic stroke, with high risk of intracranial hemorrhage, should be treated at facilities that can provide timely access to appropriate evaluation and management of intracranial hemorrhage

            Coronary thrombolysis may result in reperfusion arrhythmias

            Patients who present within 3 hr of stroke symptom onset, should be treated with alteplase unless contraindications exist; longer time window (3-4.5 hr after symptom onset) shown to be safe and efficasious for select individuals; treatment of patients with minor neurological symptoms not recommended

            Alteplase does not treat adequately underlying deep vein thromposis in patients with pulmonary embolism; consider possible risk of re-embolization due to lysis of underlying deep venous thrombi in this setting

            Clinical conditions that increase risk of bleeding for all indications

            • Recent major surgery or procedure, (e.g., coronary artery bypass graft, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels)
            • Cerebrovascular disease or recent intracranial hemorrhage
            • Recent gastrointestinal or genitourinary bleeding
            • Recent trauma
            • Hypertension: systolic BP above 175 mm Hg or diastolic BP above 110 mm Hg
            • High likelihood of left heart thrombus, e.g., mitral stenosis with atrial fibrillation
            • Acute pericarditis
            • Subacute bacterial endocarditis
            • Hemostatic defects including those secondary to severe hepatic or renal disease
            • Significant hepatic dysfunction
            • Pregnancy
            • Diabetic hemorrhagic retinopathy, or other hemorrhagic ophthalmic conditions or patients currently receiving anticoagulants (e.g., warfarin sodium)
            • Septic thrombophlebitis or occluded AV cannula at seriously infected site 
            • Advanced age
            • Any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of its location
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Excretion in milk unknown; use with caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Recombinant human tissue-type plasminogen activator (t-PA); produces local fibrinolysis

            Promotes thrombolysis by converting plasminogen to plasmin; plasmin degrades fibrin and fibrinogen

            Absorption

            Onset: Coronary thrombolysis occurs in 30 min; reaches peak response at 60 min

            Peak plasma time: 20-40 min

            Distribution

            Vd: 27-53 L

            Metabolism

            Rapidly cleared from circulation by liver

            Metabolites: Degradation products (constituent amino acids of alteplase)

            Elimination

            Initial half-life: 5 minutes (free, unbound form)

            Terminal half-life: 72 minutes

            Total body clearance: 34.3-38.4 mL/hr

            Excretion: Urine

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            Administration

            Vial Reconstitution

            Use only the accompanying sterile water for injection (without preservatives); do not use bacteriostatic water for injection

            Reconstitute using aseptic technique

            Do not add other medication to resulting solution

            Reconstitute no more than 8 hr before use (does not contains antibacterial preservatives)

            Slight foaming is not unusual; let stand undisturbed for several minutes to allow large bubbles to dissipate

            Inspect parenteral drug products for particulate matter and discoloration prior to administration whenever solution and container permit

            Activase may be administered as reconstituted at 1 mg/mL or further diluted immediately before administration in an equal volume of 0.9% NaCl or D5W, to yield a concentration of 0.5 mg/mL, using either PVC bags or glass vials

            Avoid excessive agitation during dilution; mix by gently swirling and/or slow inversion

            50-mg vials

            • Do not use if vacuum is not present
            • Using a large bore needle (eg, 18 gauge) and a syringe, reconstitute by adding the contents of the accompanying 50 mL vial of sterile water for injection (SWFI) to the 50 mg vial, directing the SWFI stream into the lyophilized cake

            100-mg vials

            • The 100 mg vials do not contain vacuum
            • Using the transfer device provided, reconstitute by adding the contents of the accompanying 100 mL vial of SWFI to the 100 mg vial
            • 1. Use aseptic technique
            • 2. Remove the protective flip-caps from 1 vial of Activase and 1 vial of SWFI
            • 3. Open the package containing the transfer device by peeling the paper label off the package
            • 4. Remove the protective cap from 1 end of the transfer device and keeping the vial of SWFI upright, insert the piercing pin vertically into the center of the stopper of the vial of SWFI
            • 5. Remove the protective cap from the other end of the transfer device; do NOT invert the vial of SWFI
            • 6. Hold the vial of Activase upside down, position it so that the center of the stopper is directly over the exposed piercing pin of the transfer device, and push the vial of Activase down so that the piercing pin is inserted through the center of the Activase vial stopper
            • 7. Invert the 2 vials so that the vial of Activase is on the bottom (upright) and the vial of SWFI is upside-down, allowing the SWFI to flow down through the transfer device; allow the entire contents of the vial of SWFI to flow into the Activase vial (approximately 0.5 mL of SWFI will remain in the diluent vial)
            • 8. Remove the transfer device and the empty SWFI vial from the Activase vial and discard
            • 9. Swirl gently to dissolve the Activase powder; do NOT shake

            Bolus Dose Preparation

            Prepare the bolus dose in 1 of the following ways

            50-mg vials

            • Remove the appropriate volume from the reconstituted vial (1 mg/mL) using a syringe and needle
            • If this method is used with the 50 mg vials (contains vacuum), the syringe should not be primed with air and the needle should be inserted into the vial stopper

            100-mg vials

            • If the 100 mg vial (no vacuum) is used, the needle should be inserted away from the puncture mark made by the transfer device
            • Remove the appropriate volume from a port (second injection site) on the infusion line after the infusion set is primed
            • Program an infusion pump to deliver the appropriate volume as a bolus at the initiation of the infusion

            Cathflo Activase preparation

            Reconstitute 2 mg vial by adding 2.2 mL SWI (do not use bacteriostatic water for injection); yields final concentration of 1 mg/mL

            Mix by gently swirling until completely dissolved; complete dissolution occurs within 3 minutes; do NOT shake

            Use within 8 hr if stored at room temperature

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Select a class to view formulary status for similar drugs

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