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Pharmacokinetic Profile of Kineret® (anakinra)
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Bioavailability and Clearance
In healthy subjects (n = 11), anakinra, the active ingredient of Kineret®, was well absorbed after bolus subcutaneous injection, with an absolute bioavailability of 95% at a dosage of 70 mg.
In subjects with rheumatoid arthritis (RA), maximum plasma concentrations of anakinra occurred 3 to 7 hours after subcutaneous administration of Kineret® (anakinra) at clinically relevant dosages (1 to 2 mg/kg; n = 18). The terminal half-life ranged from 4 to 6 hours. A period of five times the plasma half-life of a product is generally believed to allow clearance of the active drug from the body. Therefore with Kineret® this would be thirty hours. In patients with RA, no unexpected accumulation of anakinra was observed in plasma samples following daily subcutaneous doses for up to 24 weeks.1
The influence of demographic covariates on the pharmacokinetics of anakinra was studied using population pharmacokinetic analysis encompassing 341 patients receiving daily subcutaneous injection of Kineret® (anakinra) at dosages of 30, 75 and 150 mg for up to 24 weeks. This analysis demonstrated that the mean plasma clearance value after subcutaneous bolus administration was approximately 14% higher in men than in women, and approximately 10% higher in subjects aged <65 years than in subjects > 65 years. Further analyses showed that the estimated anakinra clearance correlated with increasing creatinine clearance (CLcr) and body weight; however, gender and age did not account for the observed differences in mean plasma clearance.1
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Anakinra has a short half-life of 4 to 6 hours, thereby providing flexible control of therapy
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Special Populations
No dosage adjustment is needed for patients with mild renal impairment (CLcr 50 to 80 mL/minute). In the absence of adequate data, Kineret® (anakinra) should be used with caution in patients with moderate renal impairment (CLcr 30 to 50 mL/minute), and should not be used in patients with severe renal impairment (CLcr <30 mL/minute).1
No dosage adjustment is required for Kineret® (anakinra) therapy in patients with RA who have hepatic impairment.1
Currently there are insufficient data to recommend the use of Kineret® (anakinra) in children and adolescents aged <18 years.1
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Gender and age do not significantly affect the mean plasma clearance of anakinra
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References
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