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Table 1 Clinical profile of NOACs [7]

From: NOACs: an emerging class of oral anticoagulants-a review article

Anticoagulant Dabigatran Rivaroxaban Apixaban Edoxaban
Mechanism of action Direct thrombin inhibitor Direct factor Xa inhibitor Direct factor Xa inhibitor Direct factor Xa inhibitor
Prodrug Yes No No No
Absorption Rapid Rapid 3-4 h Rapid
Bioavailability 6% 66% w/o food Up to 100% with food 50% 62%
Half-life 12–17 h 5-9 h(young) 11-13 h(elderly) 12 h 9-11 h
Vd 50–70 L 50 L 21 L 107 L
Time to reach max. plasma conc. 0.5–2 h 2-4 h 1-4 h 1-2 h
Protein binding 35% 92-95% 87% 55%
Liver metabolism No Yes Yes Minimal
Renal excretion 80% 35% 25% 50%
Gastro-intestinal tolerability Dyspepsia No Problem No Problem No Problem
Absorption with food No effect 39% & above No effect 6-22% more
Effect of diet Delays absorption; time to reach peak level extends to 4 h Peak levels attain at 3 h on fasting and 4 h with food. Factor Xa inhibition higher with food No effect on exposure No effect on exposure
Effect of age Bioavailability is 1.7–2 times high in elders Bioavailability is greater in elderly with half-life 11-13 h with no difference in concentration Exposure is 32% greater in patients above 65 years of age Exposure is 32% greater in patients over 65 years of age
Effect of body weight None Weight < 50 kg have 24% increased exposure & weight > 120 kg have 24% reduced exposure Weight < 50 kg have 20-30% increased exposure & weight > 120 kg have 20-30% reduced exposure Weight < 50 kg have 20-30% increased exposure & weight > 120 kg have 20-30% reduced exposure
Effect of renal impairment Severely impaired; 6 times higher exposure with half-life 28 h Similar increase in exposure with moderate or severe renal impairment No effect on peak concentration. Increase in exposure of 16, 29, and 44% for creatinine clearance of 51–80, 30–50, and 15–29% ml/min, respectively. No effect on peak concentration. Increase in exposure of 16, 29, and 44% for creatinine clearance of 51–80, 30–50, and 15–29% ml/min, respectively.
Effect of hepatic impairment None with Child-Pugh classification B Significantly increased on exposure with Child-Pugh classification B No change in exposure with Child-Pugh classification A or B No change in exposure with Child-Pugh classification A or B
Doses 75 mg, 110 mg, 150 mg 2.5 mg, 10 mg, 15 mg, 20 mg 2.5 mg, 5 mg 15 mg, 30 mg, 60 mg
Dosing Two times a day One time a day Two times a day One time a day
Dosage form Capsule Tablet Tablet Tablet
ADR > 10% gastro-intestinal symptoms (like dyspepsia); 1–10% gastritis, esophagitis; < 1% allergic oedema, thrombocytopenia >1 0% haematologic and oncologic haemorrhage; 1–10% pruritus, abdominal pain; < 1% angioedema, cholestasis > 10% haematologic and oncologic haemorrhage; 1–10% haematuria, epistaxis; < 1% hyper-sensitivity reaction, haematoma > 10% haematologic and oncologic haemorrhage; 1–10% skin rash, anaemia; < 1% intra cranial haemorrhage, interstitial pulmonary disease
Contra indications Serious hyper-sensitivity reactions Serious hyper-sensitivity reactions Serious hyper-sensitivity reactions Serious hyper-sensitivity reactions