Table 2.
Anticoagulant characteristics.
| Drug | FDA Indications | Dosing* | Mechanism | Half-life* | Metabolism and Renal Clearance | Laboratory Effects† |
|---|---|---|---|---|---|---|
| Dabigatran‡ | NVAF, VTE, VTE prophylaxis | NVAF: 150 mg PO bid, (RD) 75 mg PO bid VTE: 150 mg PO bid VTE prophylaxis: 150 mg PO bid (after THR 110 mg PO × 1 followed by 220 mg PO qd) | Direct thrombin inhibitor | 12–17 h | Hydrolyzed to form dabigatran, the active moiety, further metabolized through conjugation 80% renal clearance | ↔/↑PT/INR, ↑↑ PTT, ECT/dTT, TT, ↔ anti-Xa level |
| Rivaroxaban | NVAF, VTE, VTE prophylaxis, chronic CAD or PAD | NVAF: 20 mg PO qd, (RD) 15 mg PO qd VTE: 15 mg PO bid ×21 days followed by 20 mg qd VTE primary (THR/TKR) or secondary prophylaxis: 10 mg qd Chronic CAD or PAD: 2.5 mg PO bid plus aspirin | Direct Xa inhibitor | 5–11.7 h | Hepatic: primary site by CYP3A4/5, CYP2J2, and hydrolysis 33% renal clearance | ↑↑ PT/INR, ↔/↑PTT, ↑anti-Xa level |
| Apixaban | NVAF, VTE, VTE prophylaxis | NVAF: 5 mg PO bid, (RD) 2.5 mg PO bid VTE: 10 mg PO bid ×7 days followed by 5 mg PO bid VTE primary (THR/TKR) or secondary prophylaxis: 2.5 mg PO bid | Direct Xa inhibitor | 6.8–15.2 h | Hepatic: mainly by CYP3A4 25% renal clearance | ↑ PT/INR, ↔/↑ PTT, ↑anti-Xa level |
| Edoxaban‡ | NVAF, VTE | NVAF: 60 mg PO qd, (RD) 30 mg qd VTE: 60 mg PO qd, (RD) 30 mg qd | Direct Xa inhibitor | 11.5 h | Hepatic: minimal, substrate of P-glycoprotein and CYP3A4 50% renal clearance | ↑ PT/INR, ↔/↑ PTT, ↑anti-Xa level |
| Betrixaban | VTE prophylaxis | VTE prophylaxis: 160 mg PO ×l followed by 80 mg PO qd, (RD) 80 mg ×l followed 40 mg qd | Direct Xa inhibitor | 19–27 h | Substrate of P-glycoprotein 6%−13% renal clearance | ↔/↑ PT/INR, ↔/↑ PTT, ↑anti-Xa level |
| Fonda parinux | VTE, VTE prophylaxis | VTE: 5–10 mgSQqd VTE prophylaxis (THR/TKR/hip fracture, abdominal surgery): 2.5 mg SQ qd | AT–dependent (mediated) selective inhibition of Xa | 17–21 h | 77% renal clearance | ↔ PT/INR, ↔/↑ PTT, ↑anti-Xa level |
| Unfractionated heparin | NVAF and valvular atrial fibrillation, VTE, ACS, critical limb ischemia, DIC | NVAF and valvular atrial fibrillation: 70–80 units/kg IV bolus followed by infusion of 18 units/kg per hour or fixed dose of 5,000 units IV bolus followed by infusion of 1,000 units/h VTE: 80 units/kg IV bolus and then 18 units/kg per hour, or fixed dosing of 5,000 units IV bolus followed by 1,000 units/h VTE prophylaxis: 5,000 units SQ every 8–12 h ACS: 60 units/kg (maximum 4,000 units) followed by an initial infusion of 12 units/kg per hour (maximum 1,000 units/h) DIC: Initial, 10,000 units IV bolus and then 5,000 to 10,000 units every 4–6 h |
AT-dependent (mediated) inactivation of thrombin (IIa) and activated factor X (factor Xa) | 1.5 h | Hepatic and reticuloendothelial system Renally cleared only at higher doses; phagocytosis | ↔ PT/INR, PTT, ↑anti-Xa level |
| Enoxaparin | VTE, VTE prophylaxis, STEMI, unstable angina, and non-Q-wave MI, mechanical heart valve prophylaxis | VTE: 1 mg/kg SQ bid or 1.5 mg/kg SQ qd VTE prophylaxis (THR/TKR/abdominal surgery/medical): 30 or 40 mg SQ qd; 30 mg SQ every 12 h STEMI: 30-mg IV bolus followed 15 min later by 1 mg/kg SQ, MAX 100 mg for the first 2 doses; maintenance, 1 mg/kg SQ bid; plus aspirin or (RD for >75 y) 0.75 mg/kg SC every 12 h (maximum 75 mg for the first 2 doses) only) followed by 0.75 mg/kg dosing for the remaining doses Unstable angina and non‒Q‒wave MI: mechanical heart valve: 40 mg SQ every 24 h OR 1 mg/kg SQ bid (say off label?) |
AT-dependent (mediated) selective inhibition of Xa and to a lesser extent thrombin (IIa) | 4.5–7.5 h SQ, 2–4 h IV | Hepatic: primary by desulfation or depolymerization 8%−40% renal clearance |
↔ PT/INR, ↔/↑ PTT, ↑anti-Xa level |
| Dalteparin | VTE prophylaxis, unstable angina, and non-Q-wave MI, mechanical heart valve prophylaxis | VTE in cancer: 200 IU/kg SQ QD ×l mo and then 150 IU/kg SQ qd VTE prophylaxis (THR/abdominal surgery/medical): 2,500–5,000 IU SQ qd UA/NQWMI: 120 IU/kgSQ every 12 h (max 10,000 IU/dose) with concurrent aspirin |
AT-dependent (mediated) selective inhibition of Xa and to a lesser extent thrombin (IIa) | 3–5 h | NA 70% renal clearance |
↔ PT/INR,↔/↑PTT, ↑anti-Xa level |
| Warfarin‡ | NVAF and valvular atrial fibrillation, VTE, VTE prophylaxis (THR/TKR), mechanical heart valve prophylaxis | NVAF and valvular atrial fibrillation: initial 2–5 mg PO qd; adjust dose based on the results of INR VTE and VTE prophylaxis (THR/TKR): initial 2 to 5 mg PO qd; adjust dose based on the results of INR mechanical heart valve: initial 2–5 mg PO qd; adjust dose based on the results of INR |
Blocks the regeneration of vitamin K epoxide, thus inhibiting synthesis of vitamin K-dependent clotting factors, which include factors II, VII, IX, and X, and the anticoagulant proteins C and S proteins C and S | 5–7 days | Hepatic: extensive by CYP2C9 (primary isoenzyme), CYP2C19, CYP2C8, CYP2C18, CYP1A2, and CYP3A4 92% renal clearance |
↑PT/INR, ↔/↑ PTT, anti-Xa level |
NVAF, Nonvalvular atrial fibrillation; VTE, venous thromboembolism; PO, by mouth; bid, twice daily; RD, reduced dose; THR, total hip replacement; qd, once daily; PT, prothrombin time; ECT, Ecarin clotting time; dTT, diluted thrombin time; CAD, coronary artery disease; PAD, peripheral arterial disease; TKR, total knee replacement; SQ, subcutaneous; ACS, acute coronary syndrome; DIC, disseminated intravascular coagulation; IV, intravenous; STEMI, ST-segment elevation myocardial infarction; MI, myocardial infarction; IU, international unit; NQWMI, non-Q-wave myocardial infarction; NA, not applicable.
Assumes normal renal and hepatic function, normal body mass index, and half-lives extended significantly with renal or hepatic failure, depending on the drug.
Laboratory results are not useful unless correlated for a specific drug. Direct oral anticoagulants specifically have varying effects on PT/INR and other laboratory results. Bold up arrows indicate main/significant impact to increase or alter lab result; up arrows indicate likely impact to increase or alter lab result; 2 up arrows indicate significant impact to increase or alter lab result; double sided horizontal arrows indicate may or may not impact lab value; up arrows with double sided horizontal arrow indicates likely impact to increase or alter lab result but also may not alter result.
Requires initial parenteral agent bridge for treatment of acute VTE.