Saquinavir. Clinical pharmacology and efficacy

Clinical Pharmacokinetics
S Vella, M Floridia

Abstract

Saquinavir is an HIV protease inhibitor with no, or limited, effect on the activity of other structurally related human aspartic proteinases. As with other HIV protease inhibitors, saquinavir inhibits the cleavage of the gag-pol protein substrate leading to the release of structurally defective and functionally inactive viral particles. It is active on both HIV-1 and HIV-2, and also has activity on chronically infected cells and HIV strains resistant to reverse transcriptase inhibitors. Synergy of action has been observed with other antiretroviral drugs. Saquinavir is characterised by a low bioavailability which is further reduced in the fasting state. Metabolism is mainly hepatic through cytochrome P450 (CYP) 3A4, but intestinal metabolism through the same system has also been reported. To achieve higher drug plasma concentrations and increase the antiviral effect, a new formulation of saquinavir with a higher bioavailability has recently been introduced. Higher plasma drug concentrations may also be obtained by combining the drug with CYP blockers, such as ritonavir or ketoconazole. Because of its metabolic interference with the CYP system, saquinavir cannot be coadministered with astemizole, terfenadine or cisapride. Rifampi...Continue Reading

Citations

Nov 4, 2000·Archives of Pharmacal Research·R Samuel, B Suh
Nov 28, 2007·Journal of Neuroimmune Pharmacology : the Official Journal of the Society on NeuroImmune Pharmacology·Dhananjay Pal, Ashim K Mitra
Jun 6, 2000·Advanced Drug Delivery Reviews·X Li, W K Chan
Jun 6, 2000·Advanced Drug Delivery Reviews·G C Williams, P J Sinko
Jun 26, 2001·British Journal of Clinical Pharmacology·C H KoksJ H Beijnen
Aug 10, 2000·British Journal of Clinical Pharmacology·D J Back
Aug 24, 2013·International Journal of Nanomedicine·Sidi YangEmmanuel A Ho
May 1, 2001·Clinical Pharmacokinetics·J Q TranB M Kerr
Apr 18, 2014·International Journal of Nanomedicine·Maria João GomesBruno Sarmento
Apr 20, 2011·Expert Opinion on Drug Metabolism & Toxicology·Mona Arab-AlameddineChantal Csajka
May 9, 2002·Drug Metabolism Reviews·Slobodan Rendic
Jul 28, 2013·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·William J ChiouDaniel A J Bow
Jul 28, 2015·Journal of Pharmaceutical Sciences·Tom De BruynPieter P Annaert
Jan 31, 2006·Life Sciences·Dhananjay Pal, Ashim K Mitra
Aug 10, 2000·British Journal of Clinical Pharmacology·G J MuirheadN Buss
Nov 22, 2005·Expert Opinion on Drug Delivery·Suresh KatragaddaAshim K Mitra
Nov 12, 2013·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Feng LiXiaochao Ma
Mar 5, 2004·British Journal of Clinical Pharmacology·Margit FröhlichWalter E Haefeli
Sep 28, 2004·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Vandana N HiraniJerome M Lasker
Jun 27, 2019·Current Topics in Medicinal Chemistry·Chandrashekhar Voshavar
May 12, 2020·ChemMedChem·André L C S NascimentoMarlus Chorilli
Mar 23, 2011·Drug Metabolism and Drug Interactions·Yamsani Shravan KumarYamsani Madhusudan Rao
Jun 3, 2020·Chemistry : a European Journal·Aysun ÇapcıSvetlana B Tsogoeva
Jun 3, 2021·Pharmaceuticals·Bauso Luana VittoriaAlessandra Bitto
Nov 17, 2009·Advanced Drug Delivery Reviews·José das NevesBruno Sarmento

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antivirals

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Antivirals (ASM)

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Related Papers

Methods in Molecular Biology
Maria Lindgren, Ulo Langel
The Annals of Pharmacotherapy
M J SheltonG D Morse
Antimicrobial Agents and Chemotherapy
David CroteauCHARTER Group
Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology : Official Publication of the International Retrovirology Association
Francesca AweekaRichard W Price
© 2022 Meta ULC. All rights reserved