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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:
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 ...
Side effects from the pill, part of Roche's $2.7 billion acquisition of Carmot in December, were mostly gastrointestinal (GI), like those associated with similar drugs.
Nelfinavir belongs to the class of drugs known as protease inhibitors (PIs) and like other PIs is almost always used in combination with other antiretroviral drugs. Nelfinavir is an orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (K i = 2 nM) and is widely prescribed in combination with HIV reverse transcriptase ...
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 ...
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