Names and pronunciation
(are-ga-troe′ban)
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Drug reference
(are-ga-troe′ban)
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Func. class.: Anticoagulant
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Chem. class.: Direct thrombin inhibitor
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Do not confuse: argatroban/Aggrastat
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ACTION: Direct inhibitor of thrombin; it reversibly binds to thrombin active site
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USES: Anticoagulation prevention/ treatment of thrombosis in heparin- induced thrombocytopenia; adjunct to percutaneous coronary intervention (PCI) in those with history of HIT, deep vein thrombosis, pulmonary embolism
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CONTRAINDICATIONS: Hyper- sensitivity, overt major bleeding Precautions: Pregnancy, breastfeeding, children, intracranial bleeding, renal function impairment, hepatic disease, severe hypertension, after lumbar punc- ture, spinal anesthesia, major surgery/ trauma, congenital/acquired bleeding, GI ulcers, abrupt discontinuation
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SIDE EFFECTS A CNS: Fever, intracranial bleeding, head- ache CV: Atrial fibrillation, coronary thrombo- sis, MI, myocardial ischemia, coronary occlusion, ventricular tachycardia, brady- cardia, chest pain, hypotension GI: Nausea, vomiting, abdominal pain, diarrhea, GI bleeding HEMA: Bleeding SYST: Anaphylaxis
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INTERACTIONS Increase: bleeding risk—antiplatelets, NSAIDs, salicylates, dipyridamole, clopi- dogrel, ticlopidine, heparin, warfarin, glycoprotein IIb/IIIa antagonists (abcix- imab, tirofiban, eptifibatide), thrombo- lytics (alteplase, reteplase, urokinase, tenecteplase), other anticoagulants; avoid using concurrently Drug/Herb Increase: bleeding risk—ginger, garlic, ginkgo, horse chestnut Drug/Lab Decrease: HB/Hct
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DOSAGE AND ROUTES Prevention/treatment of thrombosis (heparin-induced thrombocytopenia) • Adult: CONT IV INFUSION 2 mcg/ kg/min; adjust dose until steady-state aPTT is 1.5-3 × initial baseline, max 100 sec, max dose 10 mcg/kg/min Hepatic dose • Adult: CONT INFUSION 0.5 mcg/kg/ min; adjust rate based on aPTT Percutaneous coronary intervention (PCI) in HIT • Adult: IV INFUSION 25 mcg/kg/min and bolus of 350 mcg/kg given over 3-5 min, check ACT 5-10 min after bolus completed, proceed if ACT >300 sec; if ACT <300 sec, give another 150 mcg/kg blous, increase infusion rate to 30 mcg/kg/min, recheck ACT in 5-10 min; if ACT >450 sec, decrease infusion rate to 15 mcg/kg/min, recheck ACT in 5-10 min; when ACT is therapeutic, continue for duration of procedure
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Available forms: Injection 100 mg/mL (2.5 mL; must dilute 100-fold), 50 mg/50 mL, 125 mg/125 mL
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Administer: • Avoid all IM injections that may cause bleeding IV, direct route • For PCI: 350 mg/kg blous and continu- ous infusion of 25 mcg/kg/min; check ACT 5-10 min after bolus Intermittent IV INFUSION route • Dilute in 0.9% NaCl, D5W, LR to a fi- nal concentration of 1 mg/mL; dilute each 2.5-mL vial 100-fold by mixing with 250 mL of diluent, mix by repeated inver- sion of the diluent bag for 1 min; may briefly be slightly hazy • Protect from sunlight • Dosage adjustment may be made after review of aPTT, max 10 mcg/kg/min
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Assess: • Obtain baseline aPTT prior to treat- ment, do not start if aPTT ratio ⬧2.5, then aPTT 4 hr after initiation of treat- ment and at least daily thereafter; if aPTT is above target, stop infusion for 2 hr, then restart at 50%, take aPTT in 4 hr; if below target, increase infusion rate of 0.21 mg/kg/hr without checking for co- agulation abnormalities, do not use with other parenteral anticoagulants • Bleeding: gums; petechiae; ecchymo- sis; black, tarry stools; hematuria/epistax- is; decreased B/P, Hct; vaginal bleeding, possible hemorrhage • Anaphylaxis: dyspnea, rash during treatment • Fever, skin rash, urticaria • Pregnancy/breastfeeding: if preg- nancy is planned or suspected; if preg- nant, use only if benefits outweigh fetal risk; do not breastfeed, excretion un- known
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Evaluate: • Therapeutic response: prevention of thrombosis
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Reason for product, expected re- sults • To use a soft-bristle toothbrush to avoid bleeding gums; avoid contact sports; use electric razor; avoid IM injection • To report any signs of bleeding: gums, under skin, urine, stool; trouble breath- ing, wheezing, skin rash • Pregnancy/breastfeeding: to notify prescriber if planning to become preg- nant, breastfeeding • Not to use OTC meds, herbal products unless approved by prescriber • To notify prescriber of hepatic/GI dis- ease, recent surgery, injury
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PHARMACOKINETICS Metabolized in liver, distributed to extra- cellular fluid, 54% plasma protein bind- ing, half-life 39-51 min, excreted in feces, peak 1-2 hr (anticoagulant action)
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• Adult: CONT IV INFUSION 2 mcg/ kg/min; adjust dose until steady-state aPTT is 1.5-3 × initial baseline, max 100 sec, max dose 10 mcg/kg/min Hepatic dose
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• Adult: CONT INFUSION 0.5 mcg/kg/ min; adjust rate based on aPTT Percutaneous coronary intervention (PCI) in HIT
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• Adult: IV INFUSION 25 mcg/kg/min and bolus of 350 mcg/kg given over 3-5 min, check ACT 5-10 min after bolus completed, proceed if ACT >300 sec; if ACT <300 sec, give another 150 mcg/kg blous, increase infusion rate to 30 mcg/kg/min, recheck ACT in 5-10 min; if ACT >450 sec, decrease infusion rate to 15 mcg/kg/min, recheck ACT in 5-10 min; when ACT is therapeutic, continue for duration of procedure
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