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Raltegravir
From Proteopedia
(Difference between revisions)
(New page: ===Pharmacokinetics=== {| class="wikitable" border="1" width="52%" style="text-align:center" |- ! colspan="12" align="center"| Retroviral Integrase Inhibitor [[Pharmaceutical_Drugs#Pharma...) |
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{| class="wikitable" border="1" width="52%" style="text-align:center" | {| class="wikitable" border="1" width="52%" style="text-align:center" | ||
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| - | ! 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> | + | ! 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> |
|- | |- | ||
! Parameter | ! Parameter | ||
| Line 13: | Line 13: | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ||
| - | ! | + | ! 4253 |
! 2070 | ! 2070 | ||
|- | |- | ||
| Line 21: | Line 21: | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
| - | ! | + | ! 83 |
! Elvitegravir | ! Elvitegravir | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
| - | ! | + | ! 10.8 |
! 7.6 | ! 7.6 | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
| - | ! | + | ! 10168 |
! 21200 | ! 21200 | ||
| - | |- | ||
| - | ! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h) | ||
| - | ! Raltegravir | ||
| - | ! Elvitegravir | ||
|- | |- | ||
! Dosage (mg) | ! Dosage (mg) | ||
| - | ! | + | ! 400 |
! 150 | ! 150 | ||
|- | |- | ||
! Metabolism | ! Metabolism | ||
| - | ! | + | ! Hepatic - (UGT1A1) |
! Hepatic - (CYP3A4) | ! Hepatic - (CYP3A4) | ||
|} | |} | ||
Revision as of 18:31, 6 December 2010
Pharmacokinetics
| Retroviral Integrase Inhibitor Pharmacokinetics [1][2] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Raltegravir | Elvitegravir | |||||||||
| Tmax (hr) | 1.8 | Elvitegravir | |||||||||
| Cmax (ng/ml) | 4253 | 2070 | |||||||||
| Bioavailability (%) | Raltegravir | Elvitegravir | |||||||||
| Protein Binding (%) | 83 | Elvitegravir | |||||||||
| T1/2 (hr) | 10.8 | 7.6 | |||||||||
| AUC (ng/ml/hr) | 10168 | 21200 | |||||||||
| Dosage (mg) | 400 | 150 | |||||||||
| Metabolism | Hepatic - (UGT1A1) | Hepatic - (CYP3A4) | |||||||||
