| Title |
Clinical Pharmacokinetic and Pharmacodynamic Profile of Etoricoxib
|
|---|---|
| Published in |
Clinical Pharmacokinetics, September 2012
|
| DOI | 10.2165/00003088-200847110-00002 |
| Pubmed ID | |
| Authors |
Jody K. Takemoto, Jonathan K. Reynolds, Connie M. Remsberg, Karina R. Vega-Villa, Neal M. Davies |
| Abstract |
The NSAID etoricoxib is a selective inhibitor of cyclo-oxygenase 2 (COX-2), approved for treatment of patients with chronic arthropathies and musculoskeletal and dental pain. The rate of absorption of etoricoxib is moderate when given orally (the maximum plasma drug concentration occurs after approximately 1 hour), and the extent of absorption is similar with oral and intravenous doses. Etoricoxib is extensively protein bound, primarily to plasma albumin, and has an apparent volume of distribution of 120 L in humans. The area under the plasma concentration-time curve (AUC) of etoricoxib increases in proportion to increasing oral doses between 5 and 120 mg. The elimination half-life of approximately 20 hours in healthy subjects enables once-daily dosing. Etoricoxib is eliminated following biotransformation to carboxylic acid and glucuronide metabolites that are excreted in urine and faeces, with little of the drug (<1%) being eliminated unchanged in the urine. Etoricoxib is metabolized primarily by the cytochrome P450 (CYP) 3A4 isoenzyme. Plasma concentrations (AUC) of etoricoxib appear not to be different in patients with chronic renal insufficiency compared with individuals who have normal renal function. Compared with healthy subjects, it has been reported that the AUC is increased by approximately 40% in patients with moderate hepatic impairment. No inhibitory effects on CYP2C9, 2C19, 2D6, 2E1 or 3A4 are expected to occur with etoricoxib. Coadministration of etoricoxib with other drugs has been examined only to a limited extent, thus further assessment is necessary. Etoricoxib has been assessed for the management of several specific disease states, including pain, osteoarthritis, and rheumatoid arthritis, and has shown similar efficacy in comparison with traditional NSAIDs (including naproxen, diclofenac and ibuprofen) in these conditions. Etoricoxib has demonstrated a significant reduction in gastrointestinal toxicity compared with many traditional NSAIDs. The renal adverse effects of etoricoxib appear to be similar to those of other NSAIDs, and the cardiovascular adverse effects of this selective COX-2 inhibitor require further clinical scrutiny. Further study is necessary to delineate the relevance of the pharmacokinetic disposition in terms of the clinical benefits and risks of etoricoxib compared with other options in the clinical arsenal. |
Mendeley readers
The data shown below were compiled from readership statistics for 102 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Peru | 1 | <1% |
| Unknown | 101 | 99% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 16 | 16% |
| Student > Master | 14 | 14% |
| Student > Ph. D. Student | 12 | 12% |
| Researcher | 10 | 10% |
| Student > Doctoral Student | 5 | 5% |
| Other | 15 | 15% |
| Unknown | 30 | 29% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 28 | 27% |
| Pharmacology, Toxicology and Pharmaceutical Science | 21 | 21% |
| Chemistry | 9 | 9% |
| Biochemistry, Genetics and Molecular Biology | 3 | 3% |
| Agricultural and Biological Sciences | 2 | 2% |
| Other | 7 | 7% |
| Unknown | 32 | 31% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 31 May 2016.
All research outputs
#8,535,472
of 25,374,917 outputs
Outputs from Clinical Pharmacokinetics
#682
of 1,602 outputs
Outputs of similar age
#64,141
of 187,198 outputs
Outputs of similar age from Clinical Pharmacokinetics
#233
of 450 outputs
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