Save up -80% on Darunavir
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Darunavir volume of distribution
Darunavir is 95% protein bound to alpha-1-acid glycoprotein (AAG). Mean volume of distribution is approximately 131L (or 2L/kg), demonstrating moderate distribution to peripheral sites in the body. Darunavir is also a lipophilic compound, as it has higher solubility in organic compared to aqueous solvents.
Discount Cards 16,000+
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Total savings $4,735,080
What is Darunavir
Darunavir is a protease inhibitor used to treat HIV. It acts on the HIV aspartyl protease which the virus needs to cleave the HIV polyprotein into its functional fragments.
Darunavir mechanism of action
Darunavir is a HIV protease inhibitor which prevents HIV replication by binding to the enzyme’s active site, thereby preventing the dimerization and the catalytic activity of the HIV-1 protease. Darunavir selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in virus-infected cells, which prevents the formation of mature infectious virus particles. Structual analyses suggests that the close contact that darunavir has with the main chains of the protease active site amino acids (Asp-29 and Asp-30) is an important contributing factor to its potency and wide spectrum of activity against multi-protease inhibitor resistant HIV-1 variants. Darunavir can also adapt to the changing shape of a protease enzyme because of its molecular flexibility. Darunavir is known to bind to two distinct sites on the enzyme: the active site cavity and the surface of one of the flexible flaps in the protease dimer.
Dosage forms of Darunavir
(3R,3AS,6ar)-hexahydrofuro(2,3-b)furan-3-yl N-((1S,2R)-1-benzyl-2-hydroxy-3-(N(1)-isobutylsulfanilamido)propyl)carbamate (3R,3AS,6ar)-hexahydrofuro(2,3-b)furan-3-yl(1S,2R)-3-(((4-aminophenyl)sulfonyl)(isobutyl)amino)-1-benzyl-2-hydroxypropylcarbamate
Patriot A Division Of Janssen Inc
Human Immunodeficiency Virus
Indication of Darunavir
Darunavir, co-administered with ritonavir, and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) infection in antiretroviral treatment-experienced adult patients, such as those with HIV-1 strains resistant to more than one protease inhibitor.
Toxicity of Darunavir
Some degree of serum aminotransferase elevations occur in a high proportion of patients taking darunavir containing antiretroviral regimens. Moderate-to-severe elevations in serum aminotransferase levels (above 5 times the upper limit of normal) are found in 3% to 10% of patients overall, and rates are higher in patients with HIV-HCV coinfection. In clinical trials of darunavir elevations in serum ALT above 5 times ULN occurred in 2% to 3% of patients, but no subject developed clinically apparent liver injury with jaundice. The serum enzyme elevations during therapy are usually asymptomatic and self-limited and can resolve even with continuation of the medication. Clinically apparent acute liver injury due to darunavir has been reported since its approval and more widescale use, but none have been well characterized for clinical features. The liver injury generally arises after 1 to 8 weeks of therapy and the pattern of serum enzyme elevations is usually, but not always, hepatocellular. Signs of hypersensitivity (fever, rash, eosinophilia) are rare, as is autoantibody formation. The acute liver injury is usually self-limited and resolves within a few weeks of stopping darunavir. However, fatal instances have been reported, at least to the sponsor and monitoring of liver enzymes during therapy is recommended.
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