Names and pronunciation
Xarelto
Source page 1171
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Individual generic drug information
Extracted information for rivaroxaban only.
Xarelto
Source page 1171
Func. class.: Anticoagulant
Source page 1171
Chem. class.: Factor Xa inhibitor
Source page 1171
ACTION: A novel oral anticoagulant R that selectively and potently inhibits coagulation factor Xa
Source page 1171
USES: For deep venous thrombosis (DVT) prophylaxis/treatment, pulmonary embolism (PE), in patients undergoing knee or hip replacement surgery; for stroke prophylaxis and systemic embolism prophylaxis in patients with nonvalvular atrial fibrillation
Source page 1171
Extracted information for rivaroxaban only.
CONTRAINDICATIONS Severe hypersensitivity
Source page 1171
Black Box Warning: Active bleeding Precautions: Pregnancy, breastfeeding, neonates, infants, children, adolescents, geriatric patients, moderate or severe hepatic disease (Child-Pugh Class B or C), hepatic disease associated with coagulop- athy, creatinine clearance <30 mL/min for use as DVT prophylaxis and <15 mL/min for stroke and systemic embolism prophy- laxis in nonvalvular atrial fibrillation, den- tal procedures, aneurysm, diabetes reti- nopathy, diverticulitis, endocarditis, GI bleeding, hypertension, obstetric delivery, peptic ulcer disease, stroke, surgery Black Box Warning: Abrupt discontinua- tion, epidermal/spinal anesthesia Patients, especially those with dental dis- ease, should be instructed in proper oral hygiene, including caution in use of regu- lar toothbrushes, dental floss, toothpicks Black Box Warning: Bleeding: monitor for bleeding, including bleeding during dental procedures (easy bruising, blood in urine, stools, emesis, sputum, epistaxis); there is no specific antidote Black Box Warning: Abrupt discontinu- ation: avoid abrupt discontinuation unless an alternative anticoagulant in those with atrial fibrillation; discontinuing puts patients at an increased risk of thrombotic events; if product must be discontinued for reasons other than pathologic bleeding, consider administering another anticoagulant Black Box Warning: Epidural/spinal anesthesia: epidural or spinal hemato- mas that result in long-term or permanent paralysis may occur in patients who have received anticoagulants and are receiv- ing neuraxial anesthesia or undergoing spinal puncture; epidural catheter should not be removed <18 hr after the last dose of rivaroxaban; do not administer the next rivaroxaban dose <6 hr after the catheter removal; delay rivaroxaban administra- tion for 24 hr if traumatic puncture oc- curs; monitor for neuro changes R • Hepatic/renal disease: increase in ef- fect of product in hepatic disease (Child- Pugh class B or C), hepatic disease with coagulopathy; renal failure/severe renal impairment (creatinine clearance <30 mL/min in DVT prophylaxis and <15 mL/ min for stroke or systemic embolism pro- phylaxis in nonvalvular atrial fibrillation); product should be discontinued in acute renal failure; reduce dose in those with atrial fibrillation and CrCl 15-50 mL/min; monitor renal function periodically (cre- atinine clearance, BUN) • Beers: avoid use in older adults with CCr <30 mL/min; reduce dose in CCr 30-50 mL/min • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; do not breastfeed, excretion unknown; preg- nancy-related hemorrhage may occur Black Box Warning: To report bleeding (bruising, blood in urine, stools, sputum, emesis, heavy menstrual flow); use soft toothbrush, electric shaver • To inform all health care providers of use; to report to prescriber all products used; to take all medication for the dura- tion, exactly as prescribed to prevent clots; to notify prescriber if unable to take so that a different anticoagulant may be used Black Box Warning: To avoid abrupt discontinuation without another blood thinner • To report numbness of extremities, weakness, tingling, contact prescriber immediately (neuraxial anesthesia, spi- nal puncture)
Source pages 1171, 1172, 1173, 1174
SIDE EFFECTS GI: Increased hepatic enzymes, hyperbili- rubinemia, jaundice, nausea, cholestasis, cytolytic hepatitis HEMA: Bleeding, intracranial bleeding, epidural hematoma, GI bleeding, retinal hemorrhage, adrenal bleeding, retroperi- toneal hemorrhage, cerebral hemorrhage, subdural hematoma, epidural hematoma, hemiparesis, thrombocytopenia INTEG: Pruritus, blister, hypersensitivity, anaphylactic reaction, anaphylactic shock SYST: Stevens-Johnson syndrome
Source page 1173
INTERACTIONS Increase: rivaroxaban effect, possible bleeding—ketoconazole itraconazole, ritonavir, lopinavir/ritonavir; conivaptan, clarithromycin, erythromycin, salicylates, NSAIDs, other anticoagulants, thrombo- lytics, platelet inhibitors, niCARdipine, fluconazole Decrease: rivaroxaban effect—carBA Mazepine, phenytoin, rifAMPin Increase: rivaroxaban effect in renal impairment—telithromycin, darunavir, miFEPRIStone, nelfinavir, pantoprazole, posaconazole, saquinavir, tamoxifen, lapatinib, azithromycin, diltiaZEM, verap amil, quiNIDine, ranolazine, dronedar- one, amiodarone, felodipine Drug/Herb Decrease: rivaroxaban effect—St. John’s wort Drug/Food Increase: rivaroxaban effect in renal disease—grapefruit juice
Source page 1173
Extracted information for rivaroxaban only.
DOSAGE AND ROUTES DVT prophylaxis (knee or hip replacement) • Adult: PO 10 mg/day × 12 days after knee replacement surgery or × 35 days after hip replacement; administer the ini- tial dose ≥6-10 hr after surgery once hemostasis has been established DVT/PE treatment/reduction of risk • Adult: PO 15 mg bid with food × 21 days, then 20 mg daily for a total of 6 mo, may continue after 6 mo to reduce risk Stroke prophylaxis and systemic embolism prophylaxis (with nonval- vular atrial fibrillation) • Adult: PO 20 mg/day with evening meal (CrCl >50 mL/min) Converting from warfarin to rivaroxaban • Discontinue warfarin and start riva roxaban when INR is <3 Converting from another anticoagulant other than warfarin to rivaroxaban • Start rivaroxaban 0-2 hr before the next scheduled evening administration of anticoagulant (omit that dose of antico- agulant); for continuous infusion of un- fractionated heparin, stop the infusion and initiate rivaroxaban simultaneously Converting from rivaroxaban to another anticoagulant with rapid onset (not warfarin) • Discontinue rivaroxaban and give the first dose of the other anticoagulant (oral or parenteral) at the time that the next dose of rivaroxaban would have been administered Hepatic dose • Adult: PO Child-Pugh class B or C: avoid use Renal dose • Adult: PO (nonvalvular atrial fibrilla- tion) CCr 15-50 mL/min 15 mg daily; CCr <15 mL/min avoid use; (treatment/pro- phylaxis of DVT/pulmonary embolism) CCr <30 mL/min avoid use
Source page 1172
Available forms: Tabs 2.5, 10, 15, 20 mg; granules for oral suspension 1 mg/ mL; tablet starter pack 15-20 mg
Source page 1172
Administer: • For DVT prophylaxis: give daily with- out regard to food; give initial dose ≥6-10 hr after surgery when hemostasis has been established • For stroke/systemic embolism proph- ylaxis: give daily with evening meal • If dose is not given at correct time, give as soon as possible on the same day • 15-, 20-mg tabs should be taken with food; for those unable to swallow whole, tabs may be crushed, mixed with apple- sauce; immediately following administra- tion, instruct to eat; crushed tabs are stable in applesauce for up to 4 hr • 10-mg tab can be taken without regard to food; all doses ≥15 mg should be given with food Nasogastric (NG) tube or gastric feeding tube: • Confirm gastric placement of tube • Crush 15- or 20-mg tab, suspend in 50 mL of water, and administer via NG or gastric feeding tube • Enteral feeding should immediately follow administration of a crushed dose • Crushed tabs are stable in water for up to 4 hr Missed doses • Patients receiving 15 mg BID should take their missed dose immediately to ensure intake of 30 mg per day; two 15- mg tabs may be taken at once followed by the regular 15 mg BID dose the next day • For patients receiving once-daily dos- ing, take the missed dose as soon as it is remembered • Store at room temperature
Source page 1172
Extracted information for rivaroxaban only.
Assess:
Source page 1173
Evaluate: • Prevention of DVT, stroke, and sys- temic embolism
Source page 1174
CLINICAL CONSIDERATIONS
Source page 1173
Patient and caregiver information: • To report if pregnancy is planned or suspected; not to breastfeed
Source page 1174
Extracted information for rivaroxaban only.
PHARMACOKINETICS Bioavailability 80%-100%, protein bind- ing (92%-95%) albumin, excreted in urine 66% (36% unchanged, 30% metab- olites), 28% in feces (7% unchanged, 21% metabolites), unchanged drug excreted in urine (via active tubular secretion, glomerular filtration); terminal elimination half-life 5-9 hr, peak 2-4 hr; increased effect in hepatic/renal disease, Japanese patients, increased terminal half-life in geriatric patients
Source page 1173
Filter the extracted dose blocks for this individual drug.
DVT prophylaxis (knee or hip replacement)
• Adult: PO 10 mg/day × 12 days after knee replacement surgery or × 35 days after hip replacement; administer the ini- tial dose ≥6-10 hr after surgery once hemostasis has been established DVT/PE treatment/reduction of risk
Candidate age grouping · source page 1172
DVT prophylaxis (knee or hip replacement)
• Adult: PO 15 mg bid with food × 21 days, then 20 mg daily for a total of 6 mo, may continue after 6 mo to reduce risk Stroke prophylaxis and systemic embolism prophylaxis (with nonval- vular atrial fibrillation)
Candidate age grouping · source page 1172
DVT prophylaxis (knee or hip replacement)
• Adult: PO 20 mg/day with evening meal (CrCl >50 mL/min) Converting from warfarin to rivaroxaban
Candidate age grouping · source page 1172
DVT prophylaxis (knee or hip replacement)
• Adult: PO Child-Pugh class B or C: avoid use Renal dose
Candidate age grouping · source page 1172
DVT prophylaxis (knee or hip replacement)
• Adult: PO (nonvalvular atrial fibrilla- tion) CCr 15-50 mL/min 15 mg daily; CCr <15 mL/min avoid use; (treatment/pro- phylaxis of DVT/pulmonary embolism) CCr <30 mL/min avoid use
Candidate age grouping · source page 1172