Tipranavir: Difference between revisions
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* 2009 Sales: N/A | * 2009 Sales: N/A | ||
* Importance: It was the ninth [[HIV Protease]] inhibitor approved by the FDA for treatment of HIV. It is a very potent inhibitor, and is often recommended for patients who have become resistant to other treatments, but also has a relatively harsh side-effect profile. | * Importance: It was the ninth [[HIV Protease]] inhibitor approved by the FDA for treatment of HIV. It is a very potent inhibitor, and is often recommended for patients who have become resistant to other treatments, but also has a relatively harsh side-effect profile. | ||
* | * 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 | ||
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! [[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 | ||
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! 4701 | ! 4701 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! -- | ! -- | ||
! -- | ! -- | ||
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! 20-80 | ! 20-80 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
! 99 | ! 99 | ||
! >99 | ! >99 | ||
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! 98 | ! 98 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! 4.8 | ! 4.8 | ||
! 4.2 | ! 4.2 | ||
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! 3.3 | ! 3.3 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
! 128100 | ! 128100 | ||
! 46500 | ! 46500 | ||
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! 31906 | ! 31906 | ||
|- | |- | ||
! [[ | ! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h) | ||
! ~8.4 | ! ~8.4 | ||
! 32.4 | ! 32.4 |