Antivirals COPY Flashcards
What classes of drugs are used to treat HIV infections AND WHICH PARTS OF the HIV INFECTION PROCESSS ARE AFFECTED
ATTACHMENT AND ENTRY(1. Entry inhibitors e.g. enfuviratide, maraviroc)REPLICATION( 2. Nucleoside/nucleotide reverse transcriptase inhibitors e.g. zidovudine 3. Non-nucleoside RT inhibitors e.g. efavirenz)
INTEGRATION(4. Integrase inhibitors e.g. raltegravir) ASSEMBLY AND RELEASE( 5. Protease inhibitors e.g. saquinavir)
Which antivirals are used to treat HIV? How do they work?
- Nucleoside reverse transcriptase inhibitors - target HIV RT (zidovudine) + nucleotide RT inhibitors 2. Protease inhibitors - prevent HIV proteases from cleaving emerging proteins required for development of a mature virion (saquinavir) w/ low dose Ritonavir reduces PI metabolism , so it isco-administered as ‘booster’3. Non-nucleotide RT inhibitors (nnRTIs) - inhibit RT activity by allosteric inhibition (efavirenz) 4. Viral entry inhibitors - enfuvirtide prevents fusion of HIV w/host membrane by binding to glycoprotein GP41; maraviroc blocks CCR5 chemokine receptor which HIV uses to enter macrophages 5. Integrase inhibitors - target HIV integrase protein, which allows HIV DNA to be incorporated into host DNA (raltegravir)
Which antivirals are used to treat hepatitis?
Chronic HBV: - . Then nucleotide RTi (tenofovir) w/Pegylated interferon (peginterferon) alpha SOMETIMES.
Chronic HCV: - Peginterferon + nucleotide analogue (ribavirin) - Protease(enzyme that helps in release of the virus from host) inhibitor (boceprevir)
Distinguish between different types of virus and describe how they use the host cell to replicate
HIV: retrovirus, leukocytes Hepatitis: DNA (hep b-still uses reverse transcriptase for some steps - not fully understood)and RNA viruses(hepC), hepatocytes Herpes Simplex: dsDNA virus (•Surrounded by tegument & enclosed in a lipid bilayer) Influenza: ssRNA virus
Which antivirals are used to treat herpes?
Nucleoside RT inhibitor Acyclovir(nucleoside analogue)
How does HIV use the host cell to replicate?
- Attachment and entry - viral membrane proteins (HIV glycoprotein 120) interact w/leukocyte membrane receptors (CD4/CCR5/CXCR4, GP41 penetrates host cell membrane); viral capsid endocytosis 2. Replication + integration - in cytoplasm, RT converts viral RNA to DNA; DNA transported into nucleus + integrated into host DNA by viral integrase 3. Assembly + release - host cell’s machinery used to produce viral RNA + essential proteins; Gag precursor encodes all viral structural proteins; HIV protease cleaves Gag precursor protein; virus assembled within cell; mature virion released
Which antivirals are used to treat influenza? How do they work?
Influenza neuraminidase inhibitor e.g. Oseltamivir inhibits neuraminidase –> virus can’t be released from the host cell and is destroyed there.
Genral viral structure