Indinavir: Difference between revisions
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* 2009 Sales: $200 Million | * 2009 Sales: $200 Million | ||
* Importance: At the time of its approval, it was far more powerful than prior antiretroviral drugs. Has subsequently been largely replaced with newer drugs which are less likely to promote resistance, such as [[Lopinavir]] and [[Atazanavir]] | * Importance: At the time of its approval, it was far more powerful than prior antiretroviral drugs. Has subsequently been largely replaced with newer drugs which are less likely to promote resistance, such as [[Lopinavir]] and [[Atazanavir]] | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and diseases. | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
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{| class="wikitable" border="1" width="52%" style="text-align:center" | {| class="wikitable" border="1" width="52%" style="text-align:center" | ||
|- | |- | ||
! colspan="12" align="center"| HIV Protease Inhibitor [[ | ! colspan="12" align="center"| HIV Protease Inhibitor [[Pharmacokinetics]]<ref>PMID:20400409</ref><ref>Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.</ref><ref>L. Veronese et al. Single-Dose Pharmacokinetics of Amprenavir, a Human Immunodeficiency Virus Type 1 Protease Inhibitor, in Subjects with Normal or Impaired Hepatic Function. Antimicrob Agents Chemother. 2000 April; 44(4): 821–826.</ref><ref>J. Ford, et al. Intracellular and Plasma Pharmacokinetics of Saquinavir-Ritonavir, Administered at 1,600/100 Milligrams Once Daily in Human Immunodeficiency Virus-Infected Patients. Antimicrob Agents Chemother. 2004 July; 48(7): 2388–2393.</ref><ref>PMID:10620574</ref><ref>PMID:16086644</ref><ref>PMID:19131522</ref><ref>PMID: 10952482</ref><ref>PMID:16338276</ref><ref>PMID:19729375</ref><ref>PMID:12668574</ref><ref>PMID:17255144</ref><ref>PMID:10858338</ref> | ||
|- | |- | ||
! Parameter | ! Parameter | ||
| Line 32: | Line 32: | ||
! [[Nelfinavir]] | ! [[Nelfinavir]] | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ||
! 4.4 | ! 4.4 | ||
! ~3 | ! ~3 | ||
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! 3.1 | ! 3.1 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
! 13120 | ! 13120 | ||
! 14600 | ! 14600 | ||
| Line 56: | Line 56: | ||
! 4701 | ! 4701 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! -- | ! -- | ||
! -- | ! -- | ||
| Line 68: | Line 68: | ||
! 20-80 | ! 20-80 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
! 99 | ! 99 | ||
! >99 | ! >99 | ||
| Line 80: | Line 80: | ||
! 98 | ! 98 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! 4.8 | ! 4.8 | ||
! 4.2 | ! 4.2 | ||
| Line 92: | Line 92: | ||
! 3.3 | ! 3.3 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
! 128100 | ! 128100 | ||
! 46500 | ! 46500 | ||
| Line 104: | Line 104: | ||
! 31906 | ! 31906 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h) | ||
! ~8.4 | ! ~8.4 | ||
! 32.4 | ! 32.4 | ||