Antivirals Flashcards
Early inhibitors of HIV
Maraviroc, Enfuvirtide
Name the drug:
Binds CCR5 allosterically –> blocks transmission
Maraviroc
Name the drug:
Binds N peptide sequence on HIV gp41 –> blocks hairpin formation –> block membrane fusion events
Enfuvirtide
AZT (zidovudine)
1st nucleoside RT inhibitor (polymerase inhibitor)
Which of the following is not an NRTI? A. Abacavir B. Tenofovir C. Emtricitabine D. Lamivudine
B. Tenofovir is nucleotide RT inhibitor (NtRTI): adenosine analog
A. Abacavir: guanosine analog
C. Emtricitabine: cytosine analog
D. Lamivudine: cytosine analog
Name the type of drug:
Bind to allosteric site on RT –> decrease mobility of RT –> inhibit polymerase
activity
Non nucleoside RT inhibitors against HIV
Dolutegravir is what type of drug?
Integrase inhibitor against HIV
Darunavir is what type of drug?
Protease inhibitor against HIV
What type of drugs blocks maturation of virus particle?
Protease inhibitors
Inhibit cleavage of gag and gag-pol polyproteins
Name the drugs involved in HAART therapy
3 drugs: 2 nucleoside RT inhibitors + protease inhibitor OR non- nucleoside RT inhibitor OR integrase inhibitor
Name the drugs involved in ART therapy
2 NRTI + inhibitor (protease, integrase or NNRTI) + pharmacokinetic enhancer (ritonavir)
T/F: Acyclovir is preferred over valacyclovir
False. Acyclovir has short half life in blood and poorly absorbed orally. Valacyclovir can be sustained at higher levels in blood.
Acyclovir and valacyclovir are what type of drugs?
Nucleoside analog alpha herpesvirus inhibitors
T/F: Acyclovir and valacyclovir are administered as a prodrug and must be activated by viral nucleotide kinase
False. Activated by viral nucleoSIDE kinase (thymidine kinase)
Name the drug interaction that all HSV inhibitors have
some HIV NRTIs (Tenofovir). Elevates levels. Must adjust dosages
T/F: Cidofovir are administered as a prodrug and must be activated by viral nucleotide kinase
False. It is activated by cellular kinase. This is an advantage b/c it doesn’t need activation by virus encoded thymidine kinase. Works with TK - or TK altered strains of HSV
Name the drug:
Diacetyl ester prodrug of penciclovir: acyclic guanine derivative –> allows short chain extension but still causes chain termination
Famciclovir
Nucleoside analog against alpha herpes
Name the drug:
- Acyclic nucleoside phosphonates derivatives of cytosine
- Converted to active by cellular kinases –> don’t need activation by virus encoded thymidine kinase –> retain activity against TK negative or TK-altered strains of HSV
Cidofovir
Which of the following is TRUE about Foscarnet?
A. It is a nucleoside analog alpha herpesvirus inhibitors
B. It is a competitive inhibitor of HSV DNA polymerase
C. Binds indirectly to pyrophosphate-binding sites of HSV DNA polymerase
D. It is 100x more selective for viral vs cellular polymerase
D
A. Non-nucleoside analog
B. Noncompetitive inhibitor
C. Binds directly
Name the 5 drugs currently approved to treat CMV
Ganciclovir Valganciclovir Foscarnet Cidofovir Fomivirsen
NICE JOB! That one is a doozy…
Name the drug:
Hydroxymethylated derivative of acyclovir used intravenously to treat CMV, HSV, VZV
Ganciclovir
Name the drug:
Antisense RNA against CMV
Treats CMV retinitis
Fomivirsen
Amantadine, Rimatadine
Type of drug
Viral uncoating inhibitors against influenza virus
Zanamivir, Oseltamivir
Type of drug
Neuraminidase inhibitor against influenza virus
Name the drug:
RSV monoclonal ab therapy: prophylactic treatment for infants/children
Palivizumab
Ribavirin
Type of drug
Guanosine analog against RSV
Name the drug:
Best broad spectrum antiviral
Ribavirin
Simeprevir
Type of drug
Protease inhibitor against Hep C
Direct acting antiviral agents
Parataprevir
Type of drug
Protease inhibitor against Hep C
Direct acting antiviral agents
Sofosbuvir
Type of drug
Polymerase inhibitor against Hep C
Direct acting antiviral agents
Ombitasivir
Type of drug
Phosphoprotein against Hep C
Direct acting antiviral agents
Dasabuvir
Type of drug
Polymerase inhibitor against Hep C
Direct acting antiviral agents
Lidipasvir
Type of drug
Phosphoprotein against Hep C
Direct acting antiviral agents
Standard of care today for Chronic Hep C
Combo of protease inhibitors (simeprevir, ritonavir)/polymerase (sofosbuvir) +/- ribavirin NO interferon Very effective (100%) and expensive
Name 2 non nucleoside RT inhibitors
Efavirenz
Nevirapine
