Indinavir
From Proteopedia
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| - | ! colspan="12" align="center"| HIV Protease Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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> | + | ! colspan="12" align="center"| HIV Protease Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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> |
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! Parameter | ! Parameter | ||
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! Fosamprenavir | ! Fosamprenavir | ||
! Lopinavir | ! Lopinavir | ||
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! Nelfinavir | ! Nelfinavir | ||
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! Lopinavir | ! Lopinavir | ||
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! 4381 | ! 4381 | ||
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! [[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) | ||
| - | ! 4. | + | ! 4.8 |
! 4.2 | ! 4.2 | ||
! 1.8 | ! 1.8 | ||
! 4.5 | ! 4.5 | ||
| - | ! 5. | + | ! 5.5 |
! Fosamprenavir | ! Fosamprenavir | ||
! Lopinavir | ! Lopinavir | ||
| - | ! | + | ! 29.4 |
| - | ! 5. | + | ! 5.3 |
! 3.3 | ! 3.3 | ||
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! Fosamprenavir | ! Fosamprenavir | ||
! Lopinavir | ! Lopinavir | ||
| - | ! | + | ! 4746 |
! ~26045 | ! ~26045 | ||
! 27000 | ! 27000 | ||
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! Fosamprenavir | ! Fosamprenavir | ||
! Lopinavir | ! Lopinavir | ||
| - | ! | + | ! 400 |
! 400 | ! 400 | ||
! 750 | ! 750 | ||
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! Hepatic (CYP3A4) | ! Hepatic (CYP3A4) | ||
! Hepatic (CYP3A4) | ! Hepatic (CYP3A4) | ||
| - | ! | + | ! Hepatic (CYP3A4) |
! Atazanavir | ! Atazanavir | ||
! Nelfinavir | ! Nelfinavir | ||
Revision as of 08:03, 2 December 2010
|
Better Known as: Crixivan
- Marketed By: Merck & Co.
- Major Indication: Human Immunodeficiency Virus Infection
- Drug Class: HIV Protease Inhibitor
- Date of FDA Approval (Patent Expiration): 1996 (2014)
- 2006 Sales:
- Importance:
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Mechanism of Action
Pharmacokinetics
| HIV Protease Inhibitor Pharmacokinetics[1][2][3][4][5][6][7] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Darunavir | Atazanavir | Nelfinavir | |
| Tmax (hr) | 4.4 | ~3 | Indinavir | Saquinavir | .98 | Fosamprenavir | Lopinavir | .5 | 2-4 | Nelfinavir | |
| Cmax (ng/ml) | 13120 | 14600 | Indinavir | 1540 | 4901 | Fosamprenavir | Lopinavir | 2730 | ~4393 | 4381 | |
| Bioavailability (%) | Ritonavir | Tipranavir | 65 | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Darunavir | Atazanavir | Nelfinavir | |
| Protein Binding (%) | 99 | >99 | 61 | 98 | Amprenavir | Fosamprenavir | 99 | Darunavir | Atazanavir | Nelfinavir | |
| T1/2 (hr) | 4.8 | 4.2 | 1.8 | 4.5 | 5.5 | Fosamprenavir | Lopinavir | 29.4 | 5.3 | 3.3 | |
| AUC (ng/ml/hr) | 128100 | 46500 | Indinavir | 16200 | 11999 | Fosamprenavir | Lopinavir | 4746 | ~26045 | 27000 | |
| IC50 (nM) | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Darunavir | Atazanavir | Nelfinavir | |
| Clearance (L/h) | Ritonavir | 32.4 | Indinavir | Saquinavir | 56.76 | Fosamprenavir | Lopinavir | Darunavir | Atazanavir | Nelfinavir | |
| Dosage (mg) | 600 | 600 | Indinavir | Saquinavir | 600 | Fosamprenavir | Lopinavir | 400 | 400 | 750 | |
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Amprenavir | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Atazanavir | Nelfinavir | |
References
- ↑ Goebel FD, MacGregor TR, Sabo JP, Castles M, Johnson PA, Legg D, McCallister S. Pharmacokinetic characterization of three doses of tipranavir boosted with ritonavir on highly active antiretroviral therapy in treatment-experienced HIV-1 patients. HIV Clin Trials. 2010 Jan-Feb;11(1):28-38. PMID:20400409 doi:10.1310/hct1101-28
- ↑ Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.
- ↑ 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.
- ↑ 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.
- ↑ Remmel RP, Kawle SP, Weller D, Fletcher CV. Simultaneous HPLC assay for quantification of indinavir, nelfinavir, ritonavir, and saquinavir in human plasma. Clin Chem. 2000 Jan;46(1):73-81. PMID:10620574
- ↑ Fuster D, Clotet B. Review of atazanavir: a novel HIV protease inhibitor. Expert Opin Pharmacother. 2005 Aug;6(9):1565-72. PMID:16086644 doi:10.1517/14656566.6.9.1565
- ↑ Vermeir M, Lachau-Durand S, Mannens G, Cuyckens F, van Hoof B, Raoof A. Absorption, metabolism, and excretion of darunavir, a new protease inhibitor, administered alone and with low-dose ritonavir in healthy subjects. Drug Metab Dispos. 2009 Apr;37(4):809-20. Epub 2009 Jan 8. PMID:19131522 doi:10.1124/dmd.108.024109
