alteplase (Rx)

Brand and Other Names:Activase, TPA, more...Cathflo Activase
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

powder for injection (reconstitute before use)

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

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; AHA/ASA 2019 Acute Stroke Guidelines recommend use within 4.5 hr of stroke onset
  • 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)

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

and alteplase

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (2)

            • defibrotide

              defibrotide increases effects of alteplase by pharmacodynamic synergism. Contraindicated. Coadministration of defibrotide is contraindicated with antithrombotic/fibrinolytic drugs. This does not include use for routine maintenance or reopening of central venous lines.

            • prothrombin complex concentrate, human

              alteplase, prothrombin complex concentrate, human. pharmacodynamic synergism. Contraindicated.

            Serious - Use Alternative (2)

            • apixaban

              alteplase and apixaban both increase anticoagulation. Avoid or Use Alternate Drug.

            • zanubrutinib

              alteplase, zanubrutinib. Either decreases toxicity of the other by anticoagulation. Avoid or Use Alternate Drug. Zanubrutinib-induced cytopenias increases risk of hemorrhage. Coadministration of zanubritinib with antiplatelets or anticoagulants may further increase this risk.

            Monitor Closely (72)

            • alfalfa

              alteplase and alfalfa both increase anticoagulation. Modify Therapy/Monitor Closely.

            • American ginseng

              alteplase and American ginseng both increase anticoagulation. Modify Therapy/Monitor Closely.

            • antithrombin alfa

              antithrombin alfa and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • antithrombin III

              antithrombin III and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • argatroban

              argatroban and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • aspirin

              aspirin, alteplase. Either increases toxicity of the other by anticoagulation. Use Caution/Monitor. The need for simultaneous use of low-dose aspirin and anticoagulant or antiplatelet agents are common for patients with cardiovascular disease; monitor closely.

            • aspirin rectal

              aspirin rectal and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate, alteplase. Either increases toxicity of the other by anticoagulation. Use Caution/Monitor. The need for simultaneous use of low-dose aspirin and anticoagulant or antiplatelet agents are common for patients with cardiovascular disease; monitor closely.

            • azficel-T

              azficel-T, alteplase. Other (see comment). Use Caution/Monitor. Comment: Coadministration with anticoagulants or antiplatelets may increase bruising or bleeding at biopsy and/or injection sites; concomitant use not recommended. Decisions regarding continued use or cessation of anticoagulants or antiplatelets should be made by a physician.

            • bivalirudin

              bivalirudin and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • caplacizumab

              caplacizumab, alteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor.

            • celecoxib

              celecoxib and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • choline magnesium trisalicylate

              choline magnesium trisalicylate and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • cinnamon

              alteplase and cinnamon both increase anticoagulation. Use Caution/Monitor. In theory, cinnamon may interact with blood-thinning medications due to the presence of coumarin.

            • cordyceps

              alteplase and cordyceps both increase anticoagulation. Modify Therapy/Monitor Closely.

            • dabigatran

              dabigatran and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely. Both drugs have the potential to cause bleeding. Concomitant use may increase risk of bleeding.

            • dalteparin

              dalteparin and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • danshen

              alteplase and danshen both increase anticoagulation. Modify Therapy/Monitor Closely.

            • devil's claw

              alteplase and devil's claw both increase anticoagulation. Use Caution/Monitor. Devil's claw may have additive anticoagulant activity.

            • diclofenac

              diclofenac and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • diflunisal

              diflunisal and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • dong quai

              alteplase and dong quai both increase anticoagulation. Modify Therapy/Monitor Closely.

            • enoxaparin

              enoxaparin and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • epoprostenol

              alteplase and epoprostenol both increase anticoagulation. Use Caution/Monitor. Coadministration can increase the risk of bleeding, although this did not occur in clinical trials.

            • etodolac

              etodolac and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • fenoprofen

              fenoprofen and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • feverfew

              alteplase and feverfew both increase anticoagulation. Modify Therapy/Monitor Closely.

            • fish oil

              fish oil, alteplase. Other (see comment). Use Caution/Monitor. Comment: Patients taking fish oil and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding. .

            • fish oil triglycerides

              fish oil triglycerides will increase the level or effect of alteplase by anticoagulation. Use Caution/Monitor. Prolonged bleeding reported in patients taking antiplatelet agents or anticoagulants and oral omega-3 fatty acids. Periodically monitor bleeding time in patients receiving fish oil triglycerides and concomitant antiplatelet agents or anticoagulants.

            • flurbiprofen

              flurbiprofen and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • fondaparinux

              fondaparinux and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • forskolin

              alteplase and forskolin both increase anticoagulation. Modify Therapy/Monitor Closely. Forskolin may cause bleeding due to additive platelet inhibition.

            • garlic

              alteplase and garlic both increase anticoagulation. Modify Therapy/Monitor Closely.

            • ginger

              alteplase and ginger both increase anticoagulation. Use Caution/Monitor.

            • ginkgo biloba

              alteplase and ginkgo biloba both increase anticoagulation. Modify Therapy/Monitor Closely.

            • green tea

              green tea, alteplase. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of bleeding.

            • heparin

              heparin and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • horse chestnut seed

              alteplase and horse chestnut seed both increase anticoagulation. Modify Therapy/Monitor Closely.

            • ibrutinib

              ibrutinib will increase the level or effect of alteplase by anticoagulation. Use Caution/Monitor. Ibrutinib may increase the risk of hemorrhage in patients receiving antiplatelet or anticoagulant therapies and monitor for signs of bleeding.

            • ibuprofen

              ibuprofen and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • ibuprofen IV

              ibuprofen IV and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • imatinib

              imatinib, alteplase. Either increases toxicity of the other by Other (see comment). Modify Therapy/Monitor Closely. Comment: Imatinib may cause thrombocytopenia; bleeding risk increased when imatinib is coadministered with anticoagulants, NSAIDs, platelet inhibitors, and thrombolytic agents.

            • indomethacin

              indomethacin and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • ketoprofen

              ketoprofen and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • ketorolac

              ketorolac and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • ketorolac intranasal

              ketorolac intranasal and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • meclofenamate

              meclofenamate and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • mefenamic acid

              mefenamic acid and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • melatonin

              melatonin increases effects of alteplase by anticoagulation. Use Caution/Monitor. Melatonin may decrease prothrombin time.

            • meloxicam

              meloxicam and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • nabumetone

              nabumetone and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • naproxen

              naproxen and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • nitroglycerin rectal

              nitroglycerin rectal decreases effects of alteplase by Other (see comment). Use Caution/Monitor. Comment: Caution should be observed in patients receiving nitroglycerin during t-PA therapy. IV administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. .

            • omega 3 carboxylic acids

              omega 3 carboxylic acids, alteplase. Other (see comment). Use Caution/Monitor. Comment: Patients taking omega-3 acids and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding.

            • omega 3 fatty acids

              omega 3 fatty acids, alteplase. Other (see comment). Use Caution/Monitor. Comment: Patients taking omega-3-fatty acids and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding. .

            • oxaprozin

              oxaprozin and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • panax ginseng

              alteplase and panax ginseng both increase anticoagulation. Modify Therapy/Monitor Closely.

            • piroxicam

              piroxicam and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • reishi

              alteplase and reishi both increase anticoagulation. Modify Therapy/Monitor Closely.

            • reteplase

              alteplase and reteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • rivaroxaban

              rivaroxaban, alteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Avoid concurrent use of rivaroxaban with other anticoagulants due to increased bleeding risk other than during therapeutic transition periods where patients should be observed closely. Monitor for signs/symptoms of blood loss.

            • salicylates (non-asa)

              salicylates (non-asa) and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • salsalate

              salsalate and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • Siberian ginseng

              alteplase and Siberian ginseng both increase anticoagulation. Modify Therapy/Monitor Closely.

            • sulindac

              sulindac and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • tenecteplase

              alteplase and tenecteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            • ticagrelor

              ticagrelor, alteplase. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.

            • tolmetin

              tolmetin and alteplase both increase anticoagulation. Use Caution/Monitor. Potential for increased risk of bleeding, caution is advised.

            • tranexamic acid oral

              tranexamic acid oral, alteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

            • vorapaxar

              alteplase, vorapaxar. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Coadministration of anticoagulants, antiplatelets, or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding.

            • vortioxetine

              alteplase, vortioxetine. Either increases effects of the other by anticoagulation. Use Caution/Monitor.

            • warfarin

              warfarin and alteplase both increase anticoagulation. Modify Therapy/Monitor Closely.

            Minor (1)

            • ceftaroline

              ceftaroline increases effects of alteplase by Other (see comment). Minor/Significance Unknown. Comment: Cephalosporins with a methylthiotetrazole (MTT) side ring (eg, cefotetan, cefoperazone) are more frequently associated with hypoprothrombinemic activity.

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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

            Hypersensitivity

            Cerebral edema

            Cerebral herniation

            Seizure

            Ischemic stroke

            Thromboembolism

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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 or prior intracranial hemorrhage
              • Subarachnoid hemorrhage suspected
              • Active internal bleeding
              • Stroke within 3 months
              • 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
            • Ischemic stroke within 3 months except when within 4.5 hr
            • 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)
            • Significant closed head or facial trauma with radiographic evidence of brain injury or facial trauma within 3 months
            • Bleeding diathesis
            • Aortic dissection
            • Current severe uncontrolled hypertension
            • Prior intracranial hemorrhage

            Cautions

            Catheter dysfunction may be caused by a variety of conditions other than thrombus formation, such as catheter malposition, mechanical failure, constriction by a suture, and lipid deposits or drug precipitates within the catheter lumen; considers these types of conditions before administering treatment

            Because of risk of damage to vascular wall or collapse of soft-walled catheters, vigorous suction should not be applied during attempts to determine catheter occlusion

            Avoid applying excessive pressure when agent is instilled into catheter; such force could cause rupture of catheter or expulsion of clot into circulation

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

            Hypersensitivity, including urticaria, angioedema and anaphylaxis, reported in association with therapy; monitor patients during and for several hours after infusion for hypersensitivity; if signs of hypersensitivity occur, e.g. anaphylactoid reaction or angioedema develops, discontinue therapy and promptly institute appropriate therapy

            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; may present with pancreatitis, cerebral infarction, acute renal failure, gangrenous digits, hypertension, rhabdomyolysis, or retinal artery oclusion

            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 efficacious for select individuals; treatment of patients with minor neurological symptoms not recommended

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

            Use with caution in presence of known or suspected infection in catheter; using agent in patients with infected catheters may release a localized infection into the systemic circulation; as with all catheterization procedures, use care to maintain aseptic technique

            Bleeding

            Agent has not been studied in patients known to be at risk for bleeding events that may be associated with use of thrombolytics; exercise caution with patients who have active internal bleeding or who have had any of the following within 48 hours: surgery, obstetrical delivery, percutaneous biopsy of viscera or deep tissues, or puncture of non-compressible vessels

            Exercise caution with patients who have thrombocytopenia, other hemostatic defects (including those secondary to severe hepatic or renal disease), or any condition for which bleeding constitutes a significant hazard or would be particularly difficult to manage because of its location, or who are at high risk for embolic complications (e.g., venous thrombosis in the region of the catheter)

            Death and permanent disability reported in patients who have experienced stroke and other serious bleeding episodes when receiving pharmacologic doses of a thrombolytic

            Should serious bleeding in a critical location (e.g., intracranial, gastrointestinal, retroperitoneal, pericardial) occur, therapy should be stopped and the drug should be withdrawn from the catheter

            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

            Published studies and case reports on alteplase use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes; alteplase is embryocidal in rabbits when intravenously administered during organogenesis at clinical exposure for AMI, but no maternal or fetal toxicity was evident at lower exposure in pregnant rats or rabbits; the most common complication of thrombolytic therapy is bleeding; pregnancy may increase this risk; drug should be used during pregnancy only if potential benefit justifies potential risk to fetus

            Lactation

            There are no data on presence of alteplase in human milk, effects on breastfed infant, or on milk production

            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.

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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

            BRAND FORM. UNIT PRICE PILL IMAGE
            Activase intravenous
            -
            50 mg vial
            Activase intravenous
            -
            100 mg vial
            Activase intravenous
            -
            100 mg vial
            Cathflo Activase intra-catheter
            -
            2 mg vial
            Cathflo Activase intra-catheter
            -
            2 mg vial

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Select a drug:
            Patient Education
            alteplase intravenous

            NO MONOGRAPH AVAILABLE AT THIS TIME

            USES: Consult your pharmacist.

            HOW TO USE: Consult your pharmacist.

            SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Consult your pharmacist.

            DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: No monograph available at this time.

            MISSED DOSE: Consult your pharmacist.

            STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

            Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            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.
            Additional Offers
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.