Indinavir: Difference between revisions
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! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
! Ritonavir | |||
! Tipranavir | |||
! Indinavir | |||
! Saquinavir | |||
! Amprenavir | |||
! Fosamprenavir | |||
! Lopinavir | |||
! Ritonavir | |||
! Darunavir | |||
! Atazanavir | |||
! Nelfinavir | |||
|- | |||
! Clearance (nM) | |||
! Ritonavir | ! Ritonavir | ||
! Tipranavir | ! Tipranavir | ||
Revision as of 07:06, 2 December 2010
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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] | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Tmax (hr) | 2.67 | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Cmax (ng/ml) | 5444 | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Bioavailability (%) | Ritonavir | Tipranavir | 65 | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Protein Binding (%) | 99 | Tipranavir | 61 | 98 | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| T1/2 (hr) | 4 | Tipranavir | 1.8 | 7-12 | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| AUC (ng/ml/hr) | 58000 | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| IC50 (nM) | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Clearance (nM) | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Dosage (mg) | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Metabolism | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
References
- ↑ Gallicano K, Foster B, Choudhri S. Effect of short-term administration of garlic supplements on single-dose ritonavir pharmacokinetics in healthy volunteers. Br J Clin Pharmacol. 2003 Feb;55(2):199-202. doi: , 10.1046/j.1365-2125.2003.01736.x. PMID:12580992 doi:https://dx.doi.org/10.1046/j.1365-2125.2003.01736.x