Clinical Pharmacokinetics and Pharmacodynamics of Allopurinol and Oxypurinol
@article{Day2007ClinicalPA, title={Clinical Pharmacokinetics and Pharmacodynamics of Allopurinol and Oxypurinol}, author={Richard Osborne Day and Garry G Graham and Mark Hicks and Andrew J. McLachlan and Sophie Lena Stocker and Kenneth Mapson Williams}, journal={Clinical Pharmacokinetics}, year={2007}, volume={46}, pages={623-644} }
Allopurinol is the drug most widely used to lower the blood concentrations of urate and, therefore, to decrease the number of repeated attacks of gout. Allopurinol is rapidly and extensively metabolised to oxypurinol (oxipurinol), and the hypouricaemic efficacy of allopurinol is due very largely to this metabolite.The pharmacokinetic parameters of allopurinol after oral dosage include oral bioavailability of 79 ± 20% (mean ± SD), an elimination half-life (t1/2) of 1.2 ± 0.3 hours, apparent oral…
153 Citations
The population pharmacokinetics of allopurinol and oxypurinol in patients with gout
- Medicine, BiologyEuropean Journal of Clinical Pharmacology
- 2013
The pharmacokinetic model provides a means of predicting the allopur inol dose required to achieve target oxypurinol plasma concentrations for patients with different magnitudes of renal function, different body mass and with or without concomitant diuretic use.
Pharmacokinetics and comparative bioavailability of allopurinol formulations in healthy subjects
- MedicineClinical pharmacology in drug development
- 2014
The two allopurinol formulations were considered bioequivalent, based on the rate and extent of absorption, and both formulations were well tolerated.
Pharmacokinetic and Pharmacodynamic Interaction Between Allopurinol and Probenecid in Patients with Gout
- MedicineThe Journal of Rheumatology
- 2011
Coadministration of allopurinol with probenecid had a significantly greater hypouricemic effect than alloporinol alone despite an associated reduction of plasma oxypurinols concentrations.
Pharmacokinetic and Pharmacodynamic Interaction between Allopurinol and Probenecid in Healthy Subjects
- MedicineClinical pharmacokinetics
- 2008
Coadministration of allopurinol and probenecid to healthy subjects had a greater hypouricaemic effect than either alloporinol or probenacid alone, despite a reduction in plasma oxypurinl concentrations when the drugs were taken concomitantly.
Clinical Pharmacokinetics and Pharmacodynamics of Febuxostat
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- 2016
The pharmacokinetic parameters of febuxostat after multiple oral dose administration are not affected by mild to moderate hepatic impairment, and there is no consensus on whether renal impairment has any effect on the pharmacokinetics of feBUXostat.
The pharmacokinetics of oxypurinol in people with gout.
- Medicine, BiologyBritish journal of clinical pharmacology
- 2012
This first established pharmacokinetic model provides a tool to achieve target oxypurinol plasma concentrations, thereby optimizing the effectiveness and safety of allopur inol therapy in gouty patients with various degrees of renal impairment.
Optimizing Therapy With Allopurinol: Factors Limiting Hypouricemic Efficacy
- Medicine, BiologyThe American journal of the medical sciences
- 2008
Clinical aspects of the use of the hypouricemic drug allopurinol are examined, finding that the initial use of an anti-inflammatory drug or low-dose colchicine decreases but does not eliminate the development of acute attacks of gout during the initiation of therapy with allopURinol.
Individualising the dose of allopurinol in patients with gout
- MedicineBritish journal of clinical pharmacology
- 2017
Using the nomogram, the maintenance dose of allopurinol estimated to reach target concentrations can be predicted from UP, unlike previous studies which required CLCR or diuretic use as covariates to be included.
Allopurinol: insights from studies of dose–response relationships
- MedicineExpert opinion on drug metabolism & toxicology
- 2017
This review covers the metabolism and pharmacokinetics of allopurinol and its active metabolite, oxypur inol and how these factors affect the plasma concentrations of urate at initiation and during long-term therapy with allopURinol.
How much allopurinol does it take to get to target urate? Comparison of actual dose with creatinine clearance-based dose
- MedicineArthritis Research & Therapy
- 2018
A wide range of R+ doses are required to achieve target SU, and four easily obtained clinical variables (baseline SU, CrCL, weight, and allopurinol dose) may be helpful to predict allopURinol doses.
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