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Common side effects include nausea, vomiting, diarrhea, and feeling tired. [4] More serious side effects include problems with QT prolongation, heart block, high blood lipids, and liver problems. [4] It appears to be safe in pregnancy. [4] It is in the protease inhibitor class and works by blocking the HIV protease. [4]
These protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. Protease inhibitors that have been developed and are currently used in clinical practice include:
Nelfinavir is a protease inhibitor: it inhibits HIV-1 and HIV-2 proteases. HIV protease is an aspartate protease which splits viral protein molecules into smaller fragments, and it is vital to both the replication of the virus within the cell, and also to the release of mature viral particles from an infected cell.
The drug binds to and inhibits CYP3A4, so a low dose can be used to enhance other protease inhibitors. This discovery drastically reduced the adverse effects and improved the efficacy of protease inhibitors and HAART. [35] [36]. However, because of the general role of CYP3A4 in xenobiotic metabolism, dosing with ritonavir also affects the ...
Common side effects include headache, nausea, yellowish skin, abdominal pain, trouble sleeping, and fever. [2] Severe side effects include rashes such as erythema multiforme and high blood sugar. [2] Atazanavir appears to be safe to use during pregnancy. [2] It is of the protease inhibitor (PI) class and works by blocking HIV protease. [2]
Protease inhibitors can alter adipocyte metabolism causing lipodystrophy, a common side effect associated with the use of most HIV protease inhibitors. Many mechanisms have been proposed, for example inhibition of adipocyte differentiation , triglyceride accumulation and increased lipolysis .
The first HIV protease inhibitor approved by the FDA was saquinavir, which was designed to target wild-type HIV-1 protease. [27] However, this inhibitor is no longer effective due to resistance-causing mutations on the HIV-1 protease structure. The HIV genome has high plasticity, so has been able to become resistant to multiple HIV-1 protease ...
Indinavir (IDV; trade name Crixivan, made by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV/AIDS. It is soluble white powder administered orally in combination with other antiviral drugs. The drug prevents protease from functioning normally.
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