Names and pronunciation
Brilinta
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Individual generic drug information
Extracted information for ticagrelor only.
Brilinta
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Func. class.: Platelet inhibitor
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Chem. class.: ADP receptor antago- nist
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ACTION: Reversibly binds to the platelet receptor, preventing platelet activation
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USES: Arterial thromboembolism prophylaxis in acute coronary syndrome (ACS) (unstable angina, acute MI), including in patients undergoing percutaneous coronary intervention (PCI), stroke
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Extracted information for ticagrelor only.
CONTRAINDICATIONS: Hyper- sensitivity, severe hepatic disease
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Black Box Warning: Bleeding, intracra- nial bleeding Precautions: Pregnancy, breastfeeding, infants, neonates, children, GI bleeding, hepatic disease, abrupt discontinuation Black Box Warning: Coronary artery bypass graft surgery (CABG), surgery, abrupt discontinuation, aspirin coadmin- istration Black Box Warning: Increase: bleeding risk—CYP3A4 inhibitors (ketoconazole, itraconazole, voriconazole, clarithromy- cin, telithromycin, nefazodone, ritonavir, lopinavir, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, delavirdine, isonia- zid, dalfopristin, quinupristin, tipranavir); cycloSPORINE, anticoagulants, atazana- vir, thrombolytics Increase: effect of—simvastatin, lovastatin Increase: bleeding risk—NSAIDs, antico- agulants, platelet inhibitors Decrease: ticagrelor action—CYP3A4 inducers (rifAMPin, dexamethasone, phe- nytoin, carBAMazepine, PHENobarbital) Increase or decrease: digoxin Drug/Lab Test Increase: serum creatinine Black Box Warning: Bleeding: assess for bleeding that may occur when aspi- rin is combined with this product; some bleeding can be fatal, usually aspirin doses >100 mg/day; watch for frank bleeding, hypotension; avoid with active bleeding, history of intracranial hemor- rhage Black Box Warning: CABG: do not use in those undergoing CABG; discontinue ≥5 days before surgery Black Box Warning: Aspirin coadmin- istration: use with 75-100 mg of aspirin/ day, avoid higher doses; ticagrelor efficacy is decreased with aspirin >100 mg/day Black Box Warning: Abrupt discontinu- ation: do not discontinue abruptly; may increase risk for MI, stent thrombosis, death • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may be fetal toxic; do not breastfeed, excretion unknown Black Box Warning: To notify prescriber of chills, fever, bruising, bleeding; not to use aspirin >100 mg/day • Not to use any prescription, OTC prod- ucts, herbs without approval of prescriber; products with aspirin, NSAIDs may cause bleeding; to be taken with aspirin; pre- scriber will order, do not alter dose • To notify all health care providers of product use • That product can be taken without re- gard to meals • That it may take longer for bleeding to stop • To notify prescriber if pregnancy is planned or suspected, not to breastfeed
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SIDE EFFECTS CNS: Headache, dizziness, fatigue CV: Hypertension, hypotension, chest pain, atrial fibrillation, bradyarrhythmias, syncope, ventricular pauses, HF GI: Nausea, diarrhea HEMA: Serious, fatal bleeding MISC: Back pain, hyperuricemia, gynecomastia RESP: Dyspnea, cough
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INTERACTIONS
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Extracted information for ticagrelor only.
DOSAGE AND ROUTES Acute coronary syndrome • Adult: PO loading dose 180 mg with aspirin (usually 325 mg PO); then give 90 mg bid with aspirin 75-100 mg/day, do not give maintenance doses of aspirin >100 mg/day MI prophylaxis • Adult: PO 60 mg bid with aspirin 75- 100 mg daily
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Available forms: Tab 60, 90 mg
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Administer: PO route • May be taken without regard to food • Discontinue 5-7 days before surgery • May be crushed (90 mg tab) and mixed with purified water, 100 mL (PO) or 50 mL (NG); ensure entire dose is given by flushing mortar, syringe, NG tube with 2 additional 50 mL of water • Store at room temperature, in original container in dry place
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Extracted information for ticagrelor only.
Assess: • Thromboembolism: Monitor CBC with differential with platelet count baseline and periodically during treatment
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Evaluate: • Prevention of thromboembolism
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take only as prescribed; not to skip or double doses; if a dose is missed, to take next dose at scheduled time
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Extracted information for ticagrelor only.
PHARMACOKINETICS Absolute bioavailability 36%, protein binding (>99%), metabolism by CYP3A4, weak P-glycoprotein substrates and inhibitors, elimination for product and metabolite are hepatic and biliary, 84% excreted in feces, 16% in urine, half-life is 7 hr for ticagrelor, 9 hr for metabolite, maximum inhibition of platelet aggrega- tion (IPA) effect 2 hr, maintained ≥8 hr, peak 1.5 hr product, 2.5 hr metabolite
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Filter the extracted dose blocks for this individual drug.
Acute coronary syndrome
• Adult: PO loading dose 180 mg with aspirin (usually 325 mg PO); then give 90 mg bid with aspirin 75-100 mg/day, do not give maintenance doses of aspirin >100 mg/day MI prophylaxis
Candidate age grouping · source page 1288
Acute coronary syndrome
• Adult: PO 60 mg bid with aspirin 75- 100 mg daily
Candidate age grouping · source page 1288