Urania

Prevention of VTE in adults who have undergone elective hip or knee replacement surgery. Prevention of stroke & systemic embolism in adults w/ non-valvular atrial fibrillation (NVAF), w/ ≥1 risk factors eg, prior stroke or transient ischaemic attack (TIA); ≥75 yr; HTN; DM; symptomatic heart failure (NYHA class ≥II). Treatment of DVT & pulmonary embolism (PE), & prevention of recurrent DVT & PE in adults.

Prevention of stroke & systemic embolism in NVAF 5 mg bid. Reduce to 2.5 mg bid in NVAF patients w/ at least 2 of the following characteristics: Age ≥80 yr, body wt ≤60 kg, or serum creatinine ≥1.5 mg/dL (133 micromol/L). Patient w/ severe renal impairment (CrCl 15-29 mL/min) 2.5 mg bid. Treatment of DVT & PE 10 mg bid for the 1st 7 days followed by 5 mg bid. Max daily dose: 20 mg. Prevention of recurrent DVT & PE 2.5 mg bid, initiated following completion of 6 mth of treatment w/ 5 mg bid or w/ another anticoagulant. Patient undergoing cardioversion 5 mg bid for at least 2.5 days before cardioversion to ensure adequate anticoagulation. Initiate w/ 2.5 mg bid for at least 2.5 days if patient meets criteria for dose reduction. If cardioversion is required before administration of 5 doses, 10 mg loading dose should be given, followed by 5 mg bid. Reduce to 5 mg loading dose followed by 2.5 mg bid if patient meets criteria for dose reduction. Loading dose should be administered at least 2 hr before cardioversion.

May be taken with or without food: Swallow whole w/ water. Patient unable to swallow whole tab: Crush tab & suspend in water, or 5% glucose in water (G5W), or apple juice or mixed w/ apple puree & immediately administer orally. Alternatively, crush tab & suspend in 60 mL of water or G5W & immediately deliver through a nasogastric tube. Crushed tab is stable in water, G5W, apple juice, & apple puree for up to 4 hr.

Hypersensitivity. Active clinically significant bleeding. Hepatic disease associated w/ coagulopathy & clinically relevant bleeding risk. Lesion or condition if considered a significant risk factor for major bleeding including current or recent GI ulceration, presence of malignant neoplasms at high risk of bleeding, recent brain or spinal injury, recent brain, spinal or ophth surgery, recent intracranial haemorrhage, known or suspected oesophageal varices, arteriovenous malformations, vascular aneurysms or major intraspinal or intracerebral vascular abnormalities. Concomitant treatment w/ other anticoagulants eg, unfractionated heparin, LMWH (enoxaparin, dalteparin), heparin derivatives (fondaparinux), oral anticoagulants (warfarin, rivaroxaban, dabigatran) except under specific circumstances of switching anticoagulant therapy.

Haemorrhagic risk; discontinue if severe haemorrhage occurs. Concomitant use w/ other platelet aggregation inhibitors following surgery are not recommended. Limited experience when used in combination w/ antiplatelet agents in patients w/ acute coronary syndrome &/or undergoing percutaneous coronary intervention after haemostasis is achieved. Not recommended in patients w/ prosthetic heart valves w/ or w/o atrial fibrillation; history of thrombosis who are diagnosed w/ antiphospholipid syndrome; patients w/ CrCl <15 mL/min or undergoing dialysis; severe hepatic impairment. Discontinue treatment at least 48 hr prior to elective surgery or invasive procedures w/ moderate or high risk of bleeding; discontinue at least 24 hr prior to elective surgery or invasive procedures w/ low risk of bleeding. Not recommended as alternative to unfractionated heparin in patients w/ pulmonary embolism who are haemodynamically unstable or may receive thrombolysis or pulmonary embolectomy. Patients w/ active cancer; severe renal impairment (CrCl 15-29 mL/min); mild or moderate hepatic impairment; elevated liver enzymes ALT/AST >2 times ULN or bilirubin ≥1.5 times ULN; low body wt (<60 kg); elderly. Not recommended w/ concomitant strong inhibitors of both CYP3A4 & P-gp eg, azole-antimycotics (eg, ketoconazole, itraconazole, voriconazole, posaconazole) & HIV PIs (eg, ritonavir). Caution w/ concomitant use of strong inducers of both CYP3A4 & P-gp (eg, rifampicin, phenytoin, carbamazepine, phenobarb, St. John's wort) for the prevention of stroke & systemic embolism in NVAF patients & for the prevention of recurrent DVT & PE; do not concomitantly use for the treatment of DVT & PE. Preferable to avoid during pregnancy. Discontinue breast-feeding or discontinue/abstain from therapy during lactation. Safety & efficacy in childn & adolescents <18 yr have not been established.

Anaemia; haemorrhage, haematoma; epistaxis; nausea, GI haemorrhage. Prevention of stroke & systemic embolism in NVAF patients: Eye haemorrhage (including conjunctival haemorrhage); hypotension (including procedural hypotension). Treatment of DVT & PE, & prevention of recurrent DVT & PE: Thrombocytopenia; mouth haemorrhage.

Increased AUC & C_max w/ strong inhibitors of both CYP3A4 & P-gp, eg, azole-antimycotics (eg, ketoconazole, itraconazole, voriconazole & posaconazole) & HIV PI (eg, ritonavir). Decreased AUC & C_max w/ strong inducer of both CYP3A4 & P-gp (eg, rifampicin, phenytoin, carbamazepine, phenobarb or St. John's wort). Increased bleeding risk w/ anticoagulants, platelet aggregation inhibitors, SSRIs/SNRIs & NSAIDs; GPIIb/IIIa receptor antagonists, dipyridamole, dextran or sulfinpyrazone) or thrombolytic agents. Additive effect on anti-Factor Xa activity was observed in combination w/ enoxaparin. Reduced exposure w/ activated charcoal.

Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)

B01AF02 - apixaban ; Belongs to the class of direct factor Xa inhibitors. Used in the treatment of thrombosis.

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