Names and pronunciation
(al-ti-plaze′) Activase, Activase rt-PA , Cathflo Activase
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Drug reference
(al-ti-plaze′) Activase, Activase rt-PA , Cathflo Activase
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Func. class.: Thrombolytic enzyme Func. class.: Antacid, hypophos- phatemic
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Chem. class.: Tissue plasminogen activator (TPA) Chem. class.: Aluminum product, phosphate binder
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Do not confuse: alteplase/Altace Activase/Cathflo Activase/TNKase
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ACTION: Produces fibrin conversion of plasminogen to plasmin; able to bind to fibrin, convert plasminogen in throm- bus to plasmin, which leads to local fibrinolysis, limited systemic proteolysis ACTION: Neutralizes gastric acidity; binds phosphates in GI tract; these phos- phates are then excreted
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USES: Lysis of obstructing thrombi associated with acute MI, ischemic con- ditions that require thrombolysis (i.e., PE, unclotting arteriovenous shunts, acute ischemic CVA), central venous catheter occlusion (Cathflo) USES: Antacid, hyperphosphatemia in chronic renal failure; adjunct in gastric, peptic, duodenal ulcers; hyperacidity, reflux esophagitis, heartburn, stress ulcer prevention in critically ill, GERD
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Unlabeled uses: Arterial thromboem- bolism, deep vein thrombosis (DVT), occlusion prophylaxis, percutaneous coronary intervention (PCI) Unlabeled uses: GI bleeding
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CONTRAINDICATIONS: Active internal bleeding, history of CVA, severe uncontrolled hypertension, intracranial/ intraspinal surgery/trauma (within 3 mo), aneurysm, brain tumor, platelets <100,000 mm3, bleeding diathesis including INR >1.7 or PR >15 sec, arteriovenous mal- formation, subarachnoid hemorrhage, intracranial hemorrhage, uncontrolled hypertension, seizure at onset of stroke Precautions: Pregnancy, breastfeeding, children, geriatric patients, neurologic defi- cits, mitral stenosis, recent GI/GU bleeding, diabetic retinopathy, subacute bacterial endocarditis, arrhythmias, diabetic hemor- rhage retinopathy, CVA, recent major sur- gery, hypertension, acute pericarditis, hemostatic defects, significant hepatic dis- ease, septic thrombophlebitis, occluded AV cannula at seriously infected site CONTRAINDICATIONS: Hyper- sensitivity to product or aluminum products Precautions: Pregnancy, breastfeeding, geriatric patients, fluid restriction, decreased GI motility, GI obstruction, dehydration, renal disease, sodium- restricted diets, GI bleeding, hypokalemia
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SIDE EFFECTS INTEG: Urticaria, rash SYST: GI, GU, intracranial, retroperitoneal A bleeding, anaphylaxis, fever SIDE EFFECTS GI: Constipation, anorexia, fecal impaction META: Hypophosphatemia
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INTERACTIONS Increase: bleeding—anticoagulants, salicy- lates, dipyridamole, other NSAIDs, abcix- imab, eptifibatide, tirofiban, clopidogrel, ticlopidine, some cephalosporins, plicamy- cin, valproic acid; monitor for bleeding Drug/Herb Increase: risk for bleeding—feverfew, garlic, ginger, ginkgo, ginseng, green tea Drug/Lab Test Increase: PT, APTT, TT INTERACTIONS Decrease: effectiveness of—allopurinol, amprenavir, cephalosporins, corticoste- roids, delavirdine, digoxin, fluoroquinolones, gabapentin, gatifloxacin, H2 antagonists, iron salts, isoniazid, ketoconazole, peni- cillAMINE, phenothiazines, phenytoin, quiNIDine, quinolones, tetracyclines, thy- roid hormones, ticlopidine, anticholiner- gics; separate by at least 4-6 hr Drug/Food Decrease: product effect—high-protein meal
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DOSAGE AND ROUTES MI (standard infusion) (Activase) • Adult >65 kg: 100 mg total given over 3 hr as follows: 60 mg given over first hour (6- to 10-mg bolus over 1-2 min), then 20 mg given over second hour, then 20 mg over third hour • Adult <65 kg: 1.25 mg/kg over 3 hr: 0.75 mg/kg over first hour (0.075-0.125 mg/kg given as a bolus over first 1-2 min), then 0.25 mg/kg over second hour, then 0.25 mg/kg over third hour, max 100 mg MI (accelerated infusion) (Activase) • Adult ≥67 kg: 100 mg total dose: give 15-mg IV BOL, then 50 mg over 30 min, then 35 mg over 60 min • Adult <67 kg: 15-mg IV BOL, then 0.75 mg/kg (max 50 mg) over 30 min, then 0.5 mg/kg (max 35 mg) over next 60 min Pulmonary embolism (Activase) • Adult: IV 100 mg over 2 hr, then heparin Acute ischemic stroke (Activase) • Adult/child IV 0.9 mg/kg, max 90 mg; give as INFUSION over 1 hr, give 10% of dose IV BOL over first minute Occluded venous access devices (Cathflo Activase) • Adult/child ≥30 kg: IV 2 mg/2 mL instilled in occluded catheter, may repeat if needed after 2 hr • Child 10-29 kg: IV 110% of lumen volume, max 2 mg/2 mL instilled in oc- cluded catheter, may repeat if needed after 2 hr Deep venous thrombosis (DVT) (Activase) (unlabeled) • Adult: IV 4 mcg/kg/min as 2-hr infu- sion, then 1 mcg/kg/min × 33 hr Percutaneous coronary intervention (PCI) (unlabeled) • Adult: INTRACARDIAC 20 mg over 5 min, then 50 mg over the next 60 min Occlusion prophylaxis (unlabeled) (Cathflo Activase) • Adult/child>30 kg: IV Do not exceed 2 mg in 2 mL; may use up to 2 doses 120 min apart • Adult/child ⬦30 kg: IV 110% lumen volume (max 2 mg/2 mL) in occluded catheter, may repeat after 2 hr DOSAGE AND ROUTES Antacid • Adult: PO 500-1500 mg 3-6× daily, max 6 doses/day Hyperphosphatemia • Adult: PO Suspension 30-40 mL (regu- lar) or 15-20 mL (concentrated) tid-qid • Child: PO 50-150 mg/kg/day in 4-6 divided doses
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Available forms: Powder for injection 50 mg (29 million international units/vial), 100 mg (58 million international units/ vial); Cathflo Activase: lyophilized powder for injection 2 mg Available forms: Suspension 320 mg/5 mL, 450 mg/5 mL, 600 mg/5 mL, 675 mg/5 mL; capsules 475, 500 mg; tablets 300, 500, 600 mg
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Administer: (Activase) Intermittent IV INFUSION route • After reconstituting with provided di- luent, add amount of sterile water for injection (no preservatives) 20-mg vial/20 mL or 50-mg vial/50 mL to make 1 mg/mL, mix by slow inversion or dilute with NaCl, D5W to a concentration of 0.5 mg/mL; 1.5 to <0.5 mg/mL may result in precipitation of product; use 18G needle; flush line with NaCl after administration, give over 3 hr for MI, 2 hr for PE • Pressure for 30 sec to minor bleeding sites; 30 min to sites of arterial puncture followed by pressure dressing; inform prescriber if this does not attain hemo- stasis; apply pressure dressing • Store powder at room temperature or refrigerate; protect from excessive light • Heparin therapy after thrombolytic therapy is discontinued, TT, ACT, or APTT less than 2× control (about 3-4 hr); treat- ment can be initiated before coagulation study results obtained, infusion should be discontinued if pretreatment INR >1.7, PT >15 sec, or elevated APTT is identified • Use reconstituted IV solution within 8 hr or discard • Avoid invasive procedures, injections, rectal temperature • Cathflo Activase: Use product after other options used for declotting a line; reconsti- tute by using 2.2 mL of sterile water pro- vided and injecting in vial, direct flow into powder (1 mg/mL), foam will disappear after standing; swirl, do not shake, solution will be pale yellow or clear, use within 8 hr, instill 2 mL of reconstituted solution into occluded catheter, try to aspirate after 1⁄2 hr; if unable to remove, allow 2 hr, a second dose may be used; aspirate 5 mL of blood to remove clot and product, irrigate with nor- mal saline Administer: 2 tsp (10 mL) will neutral- ize 20 mEq of acid PO route • Give 2 hr before or 6 hr after fluoro- quinolones • Hyperphosphatemia: Give with 8 oz water, meals unless contraindicated • Laxatives or stool softeners if consti- pation occurs, especially for geriatric patients • After shaking suspension NG route • By nasogastric tube if patient unable to swallow
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Assess: • Treatment is not recommended in patients with acute ischemic stroke >4.5 hr after symptom onset, with mi- nor neurologic deficit, or with rapidly improving symptoms • VS, B/P, pulse, respirations, neurologic signs, temperature at least q4hr; tempera- ture >104°F (40°C) indicates internal bleeding; monitor rhythm; ventricular dys- rhythmias may occur with hyperperfusion; monitor heart, breath sounds, neurologic status, peripheral pulses; assess neuro- logic status, neurologic change may indi- cate intracranial bleeding • For bleeding: during first hour of treat- ment and 24 hr after procedure: hematu- ria, hematemesis, bleeding from mucous membranes, epistaxis, ecchymosis; guaiac all body fluids, stools; do not use 150 mg or more total dose, intracranial bleeding may occur; do not use in severe uncontrolled hypertension, aneurysm, head trauma, for MI, pulmonary embolism; obtain noncon- trast CT of brain or MRI to take out intracra- nial hemorrhage prior to systemic use • Hypersensitivity: fever, rash, itching, chills, facial swelling, dyspnea, notify pre- scriber immediately; stop product, keep resuscitative equipment nearby; mild re- action may be treated with antihistamines • Previous allergic reactions or strepto- coccal infection; alteplase may be less effective • Blood studies (Hct, platelets, PTT, PT, TT, APTT) before starting therapy; PT or APTT must be less than 2× control before starting therapy; TT or PT q3-4hr during treatment • MI: ECG continuously, cardiac en- zymes, radionuclide myocardial scan- ning/coronary angiography; chest pain intensity, character; monitor those with major early infarct signs on CT scan with substantial edema, mass effect, midline shift • PE: pulse, B/P, ABGs, rate/rhythm of respirations • Occlusion: have patient exhale then hold breath when connecting/disconnect- ing syringe to prevent air embolism • Pregnancy/breastfeeding: usually con- sidered contraindicated in pregnancy ex- cept in serious conditions; use cautiously in breastfeeding Assess: • GI pain: location, intensity, duration, character, aggravating, alleviating factors; monitor for blood in stools, emesis, spu- tum in ulcer disease • Phosphate, calcium levels because product is bound in GI system • Hypophosphatemia: anorexia, weak- ness, fatigue, bone pain, hyporeflexia • Constipation; increase bulk in diet if needed, may use stool softeners or laxa- tives; record amount and consistency of stools • Pregnancy/breastfeeding: may use occasionally at recommended dose in pregnancy, breastfeeding
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Evaluate: • Therapeutic response: lysis of thrombi, adequate hemodynamic state, absence of HF, cannula/catheter lack of occlusion Evaluate: • Therapeutic response: absence of GI pain, decreased acidity, healed ulcers, decreased phosphate levels
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CLINICAL CONSIDERATIONS CLINICAL CONSIDERATIONS
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Patient and caregiver information: • The purpose and expected results of the treatment; to report adverse reac- tions, bleeding (OTC) AlternaGel, Alu-Cap, Almagel Plus , Alu-Tab, Amphojel, Basaljel, Diavol Plus , Gelusil , Mucaine Patient and caregiver information: • Not to use for prolonged periods for patients with low serum phosphate or patients on low-sodium diets; to shake liquid well • That stools may appear white or speckled • To check with prescriber after 2 wk of self-prescribed antacid use • To separate from other medications by 2 hr • Hyperphosphatemia: to avoid phos- phate foods (most dairy products, eggs, fruits, carbonated beverages) during product therapy • To notify prescriber of black tarry stools, which may indicate bleeding A
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PHARMACOKINETICS Cleared by liver, 80% cleared within 10 min of product termination, onset imme- diate, half-life 35 min, peak 1 hr PHARMACOKINETICS PO: Onset 20-40 min, duration 1-3 hr, excreted in feces, onset 20-40 min, peak 30 min, duration 1-3 hr
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• Adult/child ≥30 kg: IV 2 mg/2 mL instilled in occluded catheter, may repeat if needed after 2 hr
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• Child 10-29 kg: IV 110% of lumen volume, max 2 mg/2 mL instilled in oc- cluded catheter, may repeat if needed after 2 hr Deep venous thrombosis (DVT) (Activase) (unlabeled)
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• Adult/child>30 kg: IV Do not exceed 2 mg in 2 mL; may use up to 2 doses 120 min apart
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• Adult/child ⬦30 kg: IV 110% lumen volume (max 2 mg/2 mL) in occluded catheter, may repeat after 2 hr DOSAGE AND ROUTES Antacid
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• Child: PO 50-150 mg/kg/day in 4-6 divided doses
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