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| <applet load="" size="480" color="" frame="true" spin="on" Scene ="Tipranavir/Tipranavir/1" align="right" caption="Tipranavir, better known as Aptivus, ([[2o4p]])"/> | | <StructureSection load='' size='340' side='right' caption='Tipranavir, better known as Aptivus, ([[2o4p]])' scene='Tipranavir/Tipranavir/1'> |
| ===Better Known as: Aptivus=== | | ===Better Known as: Aptivus=== |
| * Marketed By: Boehringer-Ingelheim<br /> | | * Marketed By: Boehringer-Ingelheim<br /> |
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| ===Drug Resistance=== | | ===Drug Resistance=== |
| The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]] | | The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]] |
| | | </StructureSection> |
| ===Pharmacokinetics=== | | ===Pharmacokinetics=== |
| {| class="wikitable" border="1" width="52%" style="text-align:center"
| | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> |
| |-
| | <tr> |
| ! 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>
| | <td style="width:100%; vertical-align:top;border-width:0px; border-style:inset"> |
| |-
| | <div style="height:100%; width: 100%"> |
| ! Parameter
| | {{:HIV Protease Inhibitor Pharmacokinetics}} |
| ! [[Ritonavir]]
| | </div> |
| ! [[Tipranavir]]
| | </td> |
| ! [[Indinavir]]
| | </tr> |
| ! [[Saquinavir]]
| | </table> |
| ! [[Amprenavir]]
| |
| ! [[Fosamprenavir]]
| |
| ! [[Lopinavir]]
| |
| ! [[Darunavir]]
| |
| ! [[Atazanavir]]
| |
| ! [[Nelfinavir]]
| |
| |-
| |
| ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
| |
| ! 4.4
| |
| ! ~3
| |
| ! 1.5
| |
| ! 3.7
| |
| ! .98
| |
| ! 1.5-4
| |
| ! 2
| |
| ! .5
| |
| ! 2-4
| |
| ! 3.1
| |
| |-
| |
| ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
| |
| ! 13120
| |
| ! 14600
| |
| ! 8100
| |
| ! 2297
| |
| ! 4901
| |
| ! 4820
| |
| ! 11.9
| |
| ! 2730
| |
| ! ~4393
| |
| ! 4701
| |
| |-
| |
| ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
| |
| ! --
| |
| ! --
| |
| ! 65
| |
| ! 4
| |
| ! --
| |
| ! --
| |
| ! --
| |
| ! --
| |
| ! 68
| |
| ! 20-80
| |
| |-
| |
| ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
| |
| ! 99
| |
| ! >99
| |
| ! 61
| |
| ! 98
| |
| ! 90
| |
| ! 90
| |
| ! 99
| |
| ! 95
| |
| ! 86
| |
| ! 98
| |
| |-
| |
| ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
| |
| ! 4.8
| |
| ! 4.2
| |
| ! 1.2
| |
| ! 4.5
| |
| ! 5.5
| |
| ! 7.7
| |
| ! 6.1
| |
| ! 29.4
| |
| ! 5.3
| |
| ! 3.3
| |
| |-
| |
| ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
| |
| ! 128100
| |
| ! 46500
| |
| ! 20900
| |
| ! 13467
| |
| ! 11999
| |
| ! 35000
| |
| ! 117600
| |
| ! 4746
| |
| ! ~26045
| |
| ! 31906
| |
| |-
| |
| ! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
| |
| ! ~8.4
| |
| ! 32.4
| |
| ! 49.5
| |
| ! 36.7
| |
| ! 56.8
| |
| ! 84.4
| |
| ! 1.7
| |
| ! 32.8
| |
| ! 13.6
| |
| ! 37.3
| |
| |-
| |
| ! Dosage (mg)
| |
| ! 600
| |
| ! 600
| |
| ! 800
| |
| ! 1000
| |
| ! 600
| |
| ! 1400
| |
| ! 280
| |
| ! 400
| |
| ! 400
| |
| ! 1250
| |
| |-
| |
| ! Metabolism
| |
| ! Hepatic (CYP3A4 & CYP2C19)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4 & CYP3A5)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| ! Hepatic (CYP3A4)
| |
| |}
| |
|
| |
|
| ===References=== | | ===References=== |