Raltegravir
From Proteopedia
(Difference between revisions)
| Line 1: | Line 1: | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
| - | {| class="wikitable" border="1" width=" | + | {| class="wikitable" border="1" width="40%" style="text-align:center" |
|- | |- | ||
! colspan="12" align="center"| Retroviral Integrase Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] <ref>A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.</ref><ref>doi: 10.1128/AAC.01543-07</ref> | ! colspan="12" align="center"| Retroviral Integrase Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] <ref>A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.</ref><ref>doi: 10.1128/AAC.01543-07</ref> | ||
Revision as of 18:38, 6 December 2010
Pharmacokinetics
| Retroviral Integrase Inhibitor Pharmacokinetics [1][2] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Raltegravir | Elvitegravir | |||||||||
| Tmax (hr) | 1.8 | 2-4 | |||||||||
| Cmax (ng/ml) | 4253 | 2070 | |||||||||
| Bioavailability (%) | 32 | ~30 | |||||||||
| Protein Binding (%) | 83 | N/A | |||||||||
| T1/2 (hr) | 10.8 | 7.6 | |||||||||
| AUC (ng/ml/hr) | 10168 | 21200 | |||||||||
| Dosage (mg) | 400 | 150 | |||||||||
| Metabolism | Hepatic - (UGT1A1) | Hepatic - (CYP3A4) | |||||||||
- ↑ A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.
- ↑ Iwamoto M, Wenning LA, Petry AS, Laethem M, De Smet M, Kost JT, Breidinger SA, Mangin EC, Azrolan N, Greenberg HE, Haazen W, Stone JA, Gottesdiener KM, Wagner JA. Minimal effects of ritonavir and efavirenz on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother. 2008 Dec;52(12):4338-43. Epub 2008 Oct 6. PMID:18838589 doi:10.1128/AAC.01543-07
