Pharmacology and Laboratory Testing of the Oral Xa Inhibitors

Samama, M; Meddahi, Sadia; Samama, Charles Marc

doi:10.1016/j.cll.2014.06.009

Cited by 23 publications

(18 citation statements)

References 51 publications

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“…Rivaroxaban is one third renally excreted and is not dialyzable [32]. It is therefore not recommended in patients with significant renal insufficiency (CrCl <15 mL/min).…”

Section: Rivaroxabanmentioning

confidence: 95%

“…Apixaban levels can be assessed by measuring chromogenic anti-factor Xa activity. Although apixaban may prolong the PT and aPTT, these tests are very insensitive to its effects and should not be used for apixaban monitoring [32,33]. Given the drug's short half-life, there can be wide variation in drug levels depending on the time of testing after a given dose.…”

Section: Apixabanmentioning

confidence: 98%

“…Although rivaroxaban prolongs the prothrombin time (PT) and the activated partial thromboplastin time (aPTT), the PT provides only a qualitative assessment of rivaroxaban levels (and the international normalized ratio (INR) should never be used for this purpose) and the aPTT is very insensitive to the drug. Measurement of chromogenic anti-factor Xa is the most reliable way to assess drug levels [32,33]. Given rivaroxaban's short half-life, there can be wide variation in drug levels depending on the time of testing after a given dose [33].…”

Section: Rivaroxabanmentioning

confidence: 99%

“…Peak levels are achieved 3-4 h after administration, and the half-life is 10-14 h [32]. Apixaban is metabolized by cytochrome P34A, 25 % renally excreted, and not dialyzable.…”

Section: Apixabanmentioning

confidence: 99%

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Using New Oral Anticoagulants in Patients Undergoing Major Orthopedic Surgery

Bass

2015

Curr Rheumatol Rep

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Four new oral anticoagulants (NOAC), apixaban, rivaroxaban, edoxaban, and dabigatran, are now available in the USA; however, only apixaban and rivaroxaban are FDA approved for the prevention of venous thromboembolism following orthopedic surgery. Apixaban, rivaroxaban, and edoxaban's anticoagulant activity can be measured using a chromogenic anti-factor Xa assay but there is no widely available means of measuring dabigatran blood levels. None of the NOAC has an antidote. Dabigatran is 80% renally excreted, and patients with atrial fibrillation taking dabigatran for stroke prevention should stop the drug 4-5 days prior to major orthopedic surgery. Apixaban, rivaroxaban, and edoxaban should be held for 48 h preoperatively in this setting.

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“…Rivaroxaban is one third renally excreted and is not dialyzable [32]. It is therefore not recommended in patients with significant renal insufficiency (CrCl <15 mL/min).…”

Section: Rivaroxabanmentioning

confidence: 95%

Section: Apixabanmentioning

confidence: 98%

Section: Rivaroxabanmentioning

confidence: 99%

“…Peak levels are achieved 3-4 h after administration, and the half-life is 10-14 h [32]. Apixaban is metabolized by cytochrome P34A, 25 % renally excreted, and not dialyzable.…”

Section: Apixabanmentioning

confidence: 99%

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Using New Oral Anticoagulants in Patients Undergoing Major Orthopedic Surgery

Bass

2015

Curr Rheumatol Rep

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“…These direct FXa inhibitors are rivaroxaban (BAY 59‐7939), apixaban (BMS‐52247‐01), and edoxaban (DU‐176b). The pharmacokinetic and pharmacodynamic (PK/PD) properties of these drugs have recently been summarized 7. Both apixaban and rivaroxaban have predictable dose‐dependent pharmacokinetic (PK) properties.…”

mentioning

confidence: 99%

A Systems Pharmacology Model for Predicting Effects of Factor Xa Inhibitors in Healthy Subjects: Assessment of Pharmacokinetics and Binding Kinetics

Zhou

Huntjens

Gilissen

2015

CPT Pharmacometrics Syst. Pharmacol.

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Factor Xa (FXa) emerged as a promising target for effective anticoagulation and several FXa inhibitors are now available for the prevention of venous thromboembolism. However, in previously reported pharmacokinetic/pharmacodynamic (PK/PD) models, the complex coagulation processes and detailed information of drug action are usually unclear, which makes it difficult to predict clinical outcome at the drug discovery stage. In this study, a large‐scale systems pharmacology model was developed based on several published models and clinical data. It takes into account all pathways of the coagulation network, and captures drug‐specific features: plasma pharmacokinetics and drug‐target binding kinetics (BKs). We aimed to predict the anticoagulation effects of FXa inhibitors in healthy subjects, and to use this model to compare the effects of compounds with different binding properties. Our model predicts the clotting time and anti‐FXa effects and could thus serve as a predictive tool for the anticoagulant potential of a new compound.

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Management of Chronically Anticoagulated Patients

Levy¹

2020

Trauma Induced Coagulopathy

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Pharmacology and Laboratory Testing of the Oral Xa Inhibitors

Cited by 23 publications

References 51 publications

Using New Oral Anticoagulants in Patients Undergoing Major Orthopedic Surgery

Using New Oral Anticoagulants in Patients Undergoing Major Orthopedic Surgery

A Systems Pharmacology Model for Predicting Effects of Factor Xa Inhibitors in Healthy Subjects: Assessment of Pharmacokinetics and Binding Kinetics

Management of Chronically Anticoagulated Patients

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