Activase


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alteplase (tissue plasminogen activator, recombinant)

Actilyse (UK), Activase, Activase rt-PA (CA), Cathflo Activase

Pharmacologic class: Plasminogen activator

Therapeutic class: Thrombolytic

Pregnancy risk category C

Action

Converts plasminogen to plasmin, which in turn breaks down fibrin and fibrinogen, thereby dissolving thrombus

Availability

Injection: 2-mg single-patient vials; 50-mg, 100-mg vials

Indications and dosages

Lysis of thrombi obstructing coronary arteries in acute myocardial infarction (MI)

3-hour infusion-

Adults: 100 mg I.V. over 3 hours as follows: 60 mg over first hour (give 6 to 10 mg as bolus over first 1 to 2 minutes), then 20 mg I.V. over second hour, then 20 mg I.V. over third hour

Adults weighing less than 65 kg (143 lb): 1.25 mg/kg I.V. in divided doses over 3 hours, not to exceed 100 mg Accelerated infusion-

Adults weighing more than 67 kg (147 lb): Give total dosage of 100 mg as follows: 15 mg I.V. bolus over 1 to 2 minutes, then 50 mg I.V. over next 30 minutes, then 35 mg I.V. over next 60 minutes.

Adults weighing 67 kg (147 lb) or less: 15 mg I.V. bolus over 1 to 2 minutes, followed by 0.75 mg/kg I.V. over next 30 minutes (not to exceed 50 mg), followed by 0.5 mg/kg I.V. over next hour, not to exceed 35 mg

Acute ischemic cerebrovascular accident (CVA)

Adults: 0.9 mg/kg I.V. over 1 hour, to a maximum dosage of 90 mg, with 10% of total dosage given as I.V. bolus within first minute

Acute massive pulmonary embolism

Adults: 100 mg I.V. over 2 hours, followed by heparin

Restoration of function of central venous access device

Adults weighing 30 kg (66 lb) or more: Cathflo Activase-2 mg/2-ml concentration instilled in dysfunctional catheter. If catheter function isn't restored in 120 minutes after first dose, may give second dose.

Adults weighing 10 kg (22 lb) to less than 30 kg: Cathflo Activase-Use 110% of catheter lumen volume not to exceed 2 mg/2-ml concentration instilled in dysfunctional catheter. If catheter function isn't restored in 120 minutes after first dose, may give second dose.

Off-label uses

• Small-vessel occlusion by microthrombi

• Peripheral arterial thromboembolism

Contraindications

• Hypersensitivity to drug or its components (Cathflo Activase)

• Seizures, stroke, aneurysm, intracranial neoplasm, bleeding diathesis

Precautions

Use cautiously in:

• hypersensitivity to anistreplase or streptokinase

• GI or genitourinary bleeding, ophthalmic hemorrhage, organ biopsy, severe hepatic or renal disease

• elderly patients

• pregnant or breastfeeding patients

• children.

Administration

Be aware that intracranial hemorrhage must be ruled out before therapy begins.

To treat acute ischemic CVA, give within 3 hours of initial signs or symptoms.

If uncontrolled bleeding occurs, stop infusion and notify prescriber immediately.

• Give I.V. only, using controlled-infusion pump.

• Reconstitute with unpreserved sterile water for injection. May be further diluted with normal saline solution or D5W.

Adverse reactions

CNS: cerebral hemorrhage, cerebral edema, CVA (with accelerated infusion)

CV: hypotension, bradycardia, recurrent ischemia, pericardial effusion, pericarditis, mitral regurgitation, electromechanical dissociation, arrhythmias, cardiogenic shock, heart failure, cardiac arrest, cardiac tamponade, myocardial rupture, embolization, venous thrombosis

GI: nausea, vomiting, GI bleeding

GU: GU tract bleeding

Hematologic: spontaneous bleeding, bone marrow depression

Musculoskeletal: musculoskeletal pain

Respiratory: pulmonary edema

Skin: bruising, flushing

Other: fever, edema, phlebitis or bleeding at I.V. site, hypersensitivity reaction (including rash, anaphylactic reaction, laryngeal edema), sepsis

Interactions

Drug-drug. Aspirin, drugs affecting platelet activity (such as abciximab, heparin, dipyridamole, oral anticoagulants, vitamin K antagonists): increased risk of bleeding

Drug-diagnostic tests. Blood urea nitrogen: elevated level

Patient monitoring

• Monitor vital signs, ECG, and neurologic status.

• Maintain strict bed rest.

• Watch for signs and symptoms of bleeding tendency and hemorrhage.

• Monitor patient on Cathflo Activase for GI bleeding, venous thrombosis, and sepsis.

• Evaluate results of clotting studies.

Patient teaching

• As appropriate, explain therapy and monitoring to patient and family.

Activase

(ăk′tə-vās′)
A trademark used for a synthetic tissue plasminogen activator.

Activase®

A proprietary thrombolytic, which is used to manage acute ischaemic strokes. Current guidelines support Activase use in eligible stroke patients within 3 hours of symptom onset. 
Mechanism Activation of fibrinolysis by stimulating conversion of plasminogen to plasmin.

Activase®

A proprietary thrombolytic, which may ↑ survival in TIA victims by 33% Mechanism Activation of the body's fibrinolytic system by stimulating conversion of plasmin from plasminogen, and several other clotting factors. See TIA, tPA.
References in periodicals archive ?
Seedlings growing with water were found to contain an increased (by 5%) amount of ribulose-bisphosphate carboxylase activase and oxygen-evolving enhancer protein 2 (OEE2), whereas expression of oxygen-evolving enhancer protein 1 (OEE1) increased by 8%.
Rubisco activase Expression Levels are Possibly aResult of Circadian Rhythms
Investigators discovered the existence of rubisco activase in 1985 and proved that it activates rubisco.
Arid-Land Agricultural Research Center, has teamed with Rebekka Wachter, associate professor of chemistry and biochemistry at Arizona State University, and Nathan Henderson, her postdoctoral research associate, to crystallize rubisco activase.
El fallo a modo de conclusion, en considerando decimo noveno senala, "Que de conformidad a lo razonado, en el caso a que se refiere el presente recurso, luego de producida la interrupcion de la prescripcion liberatoria con el acto del requerimiento judicial y no habiendose practicado posteriormente diligencia alguna que activase la ejecucion, debe entenderse que, a partir de la fecha misma de dicho requerimiento, comenzo a correr una nueva prescripcion.
Manawadu and her colleagues analyzed patients in the hospital's stroke registry who received alteplase (Activase) between January 2009 and December 2010.
Cabe decir que el reconocimiento historico de esta valiosa obra de creacion realizada por las tres generaciones de ilustrados menorquines a lo largo de mas de setenta anos ha sido desigual, y ha afectado de manera especial la creacion literaria, seguramente porque la transmision textual fue todavia mayoritariamente manuscrita, aunque Menorca contase con una imprenta desde mediados del siglo XVIII y la impresion se activase con el nacimiento de la prensa periodica, en castellano, el 1811.
(33.) One example is Activase, a recombinant tissue plasminogen activator developed by Genentech Inc.
The thrombolytic drugs tested included: alteplase (Cathflo Activase, Genentech, Inc, San Francisco, California), urokinase (Abbokinase, Abbott Laboratories, Abbott Park, Illinois), streptokinase (Streptase, Aventis, Paris, France), tenecteplase (TNKase, Genentech, Inc), and reteplase (Retavase, Boehringer Mannheim, Mannheim, Germany).
This procedure increase photosynthesis efficiency, motivate Rubisco activase complex and gain carbon photosynthesis.
En una palabra, existia un espacio para que la entrada en juego de un fuerte detonador activase la carga, en terminos quimicos por simpatia, como posiblemente sucede en Jordania y puede suceder en Argelia.