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Anti HIV drugs


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What are the two major classes of anti HIV drugs?
Antimetabolite inhibitors of RT
Viral aspartate protease inhibitors
Nucleoside reverse transcriptase inhibitors - mechanism
Selective for virally encoded RNA dependent DNA polymerase
Lack a 3’ OH so they cause chain termination
Mechanism of resistance to NRTIs?
Resistance via mutations of the DNA pol gene can result in:
Impairment of NRTI incorporation into DNA
Removal of NRTI from the terminated DNA chain
Mutants that arise during combination therapy are cross-resistant to all NRTIs in clinical use
NNRTIs mechanism?
Bind to a site different from NRTIs
Don’t require phosphorylation to be active and don’t compete with nucleoside triphosphates
Bind to a hydrophobic subdomain near the active site of HIV-RT producing allosteric inhibition, enzyme can no longer bind normal substrate
NNRTIs toxicity?
relatively low, contraindicated in pregnancy
NNRTI drug interactions?
Nevaripine and efavirenz both induce and are metabolized by CYP3A4
Delavirdine is metabolized by and inhibits CYP3A4
How do protease inhibitors work?
Protease cleaves large proteins into function proteins for HIV,
Selective for HIV protease inactive vs human proteases
How are NRTI and NNRTIs used together?
Used in combination to minimize resistance NNRTI + 2NRTIs
How are PIs used with other HIV drugs?
in combination with NRTIs to minimize resistance strains and for synergistic effect
Additive or synergistic effects with NRTIs because they inhibit a late pathway
Toxicity of protease inhibitors?
GI distress, increased bleeding in hemophiliacs, hepatoxicity, metabolic alterations hyperglycemia, hyperlipidemia, insulin resistance, lipodystrophy (wasting or redistribution of fat)
which PIs are least toxic?
Nelfinivir and saquinavir are well-tolerated rotinarvir is poorly tolerated at full dose
Drug interactions of PIs?
Drug interactions drugs that inhibit cytochrome P-450 CYP3A4, increase plasma concentration of PI toxicity
All Pis are substrates and inhibitors of CYP3A4. rotinavir is the most potent and saquinivir the least potent inhibitor.
what is enfurivitide?
Peptide that interferes with virus cell interaction and blocks viral fusion with the CD4 cell membrane
Which class of HIV drugs is contracindicated in pregnancy?
Which drug is good for prevention of vertical transmission?
NRTI - Zidovudine
NNRTI - Nevaripine given at onset of labor

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