Population pharmacokinetics and pharmacodynamics of enoxaparin in unstable angina and non‐ST‐segment elevation myocardial infarction

• DOI: 10.1046/j.1365-2125.2003.01904.x
• Publication Date: 2003-09-12T09:29:15Z
• Authors: René Bruno; Pascale Baille; Sylvie Retout; Nicole Vivier; Christine Veyrat‐...; Ger‐Jan Sanderink; Richard Becker; Elliott M. Antman
• Keywords: Unstable angina; Pharmacodynamics; Enoxaparin sodium

Aims A major concern with any antithrombotic therapy is an increase in the risk of haemorrhage. The aim this study was to analyse population pharmacokinetics and pharmacokinetic/pharmacodynamic (PK/PD) relationships for enoxaparin patients unstable angina (UA) non‐ST‐segment elevation myocardial infarction (NSTEMI), which may help predict Methods Anti‐factor Xa (anti‐Xa) activity measured as marker concentration 448 receiving drug a single 30‐mg intravenous bolus followed by 1.0 or 1.25 mg kg −1 subcutaneously twice day. pharmacokinetic analysis conducted individual estimates clearance area under curve were tested prognostic factors occurrence haemorrhagic episodes. Results Basic PK parameters 0.733 l h [95% confidence interval (CI) 0.698, 0.738], distribution volume 5.24 (95% CI 4.20, 6.28) elimination half‐life 5.0 h. Enoxaparin significantly related patient weight creatinine clearance, only independent predictor experiencing both all (10.7%, P = 0.0013) (2.2%, 0.0004) events. 30 ml min associated decrease 27% compared that median 88 , 1.5‐ 3.8‐fold ‘all’ ‘major’ episodes, respectively. Conclusions depends on body weight, and, therefore, weight‐adjusted dosing recommended minimize interpatient variability exposure importance increased haemorrhage decreasing renal function must be weighed against benefit treatment UA NSTEMI.