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 trademark for a commercial form of tissue plasminogen activator (alteplase recombinant).

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 ?
The presence of tetracycline resulted in a decreased concentration of RUBISCO activase, OEE1 and OEE2 (Fig.
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.
Crystallization will allow researchers to study the activase protein more closely, to visualize its structure, and possibly to manipulate its sequence so that it doesn't unravel at higher temperatures.
Lo que permitio que esta memoria se activase con suficiente fuerza y conviccion; aquellas situaciones de violencia de los anos setenta permitieron evocar dicho acontecimiento.
Llego, en tanto, el siglo XIV, un siglo que los augures habian senalado como de presagios funestos, como asi fue: la guerra de los 100 anos, lapeste negra, el cisma de occidente, las grandes sequias seguidas de grandes inundaciones a lo que se anadio la creciente animosidad antisemita; las diferencias eran ahora por motivos economicos: los judios controlaban, segun Baer (18), los dos tercios de los impuestos indirectos y los derechos aduaneros ,tanto interiores como de fronteras y puertos, llegando a una usura considerada irritante; estas y otras razones llevaron a que en el ano 1313, el Sinodo de Zamora activase contra los judios las prescripciones del Concilio de Letran, y seles prohibe ser medicos por la ya desconfianza de sus tratamientos con los cristianos.
TABLE: SIMILAR SOUNDING DRUG NAMES THAT COULD RESULT IN A MEDICATION ERROR Drug Name Confused With Abelcet Amphotericin B Accupril Aciphex Acetazolamide Acetohexamide Aciphex Aricept Aciphex Accupril Activase TNKase Actonel Actos Adderall Inderal Advicor Altocor Aggrastat Argatroban Adapted from Medication Safety Alert.
1 ribulose bisphosphate carboxylase 107 2 chlorophyll a/b-binding protein 13 3 ferredoxin i 13 4 fructose-bisphosphate aldolase 1 12 5 oxygen-evolving enhancer protein 11 6 nonspecific lipid-transfer protein 11 7 plastocyanin 7 8 glyceraldehyde 3-phosphate dehydrogenase 7 9 no similarity 6 10 10-kDa protein precursor 6 11 photosystem I subunit IV 6 12 caffeic acid O-methyltransferase 5 13 ribulose-bisphosphate carboxylase activase 5 14 no similarity 5 15 function unknown 5 16 photosystem II 10-kDa polypeptide 4 17 drought inducible protein 4 18 endopeptidase CIp 4 19 aldo/keto reductase 4 20 no similarity 4 21 Immature-pod Homologous group Putative genes No.
At the time, Activase was administered only after a heart attack due to the "treacherous" risks attendant to the use of the drug prior to a heart attack.
If the catheter remains non-functional after a dwell time of 120 minutes, a second dose can be instilled (Cathflo Activase, Package Insert, 2001).
Cathflow(TM) Activase(R) (Alteplase): Reported positive results of a large-scale Phase III study of safety of Cathflow Activase for treatment of occluded central venous catheters.