Antivirals Flashcards
- Oseltamivir
- Zanamivir
- Acyclovir
- Famciclovir
- Valacyclovir
Ganciclovir
Foscarnet
Cidofovir
NRTIs (mechanism)
Nucleoside Reverse Transcriptase Inhibitors.
NRTIs (clinical)
Nucleoside Reverse Transcriptase Inhibitors.
Integrase Inhibitors
The Tegravirs.
Protease Inhibitors (mechanism)
Protease Inhibitors (clinical use)
NS5A Inhibitors
NS5B Inhibitors
NS3/4A Inhibitors
Oseltamivir is structurally and analog of what?
Sialic acid analogs.
Off-target adverse effect of Ganciclovir?
- Bone marrow supression
- Nephrotoxicity
Most likely reason for resistance to Acyclovir (HSV/VZV) and Ganciclovir (CMV):
- Resistance to viral thymidine kinase (acyclovir)
- Resistance to CMV kinase (ganciclovir)
Foscarnet’s 3 actions & structure:
Pyrophosphate analog
Inhibits:
1. viral DNA polymerase
2. viral RNA polymerase
3. HIV reverse transcriptase
Acyclovir’s action & structure?
Guanosine analog.
Inhibits
* Viral DNA Polymerase
Cidofovir’s action & structure:
Cytidine monophsophate analog.
Inhibits:
* Cellular kinases (NOT viral kinases)
NRTI drug names
- Abacavir
- Zidovudine
- Emtricitabine
- Lamivudine
- Dianosine
- Stavudine
- Tenofovir
What’s special about the NRTI Tenofovir?
It doesn’t require phosphorylation because it already comes in a nucleotide form.
Distinguishing Didanosine from the other 6 NRTIs?
Pancreatitis.
Distinguishing Zidovudine from the other 6 NRTIs?
Bone marrow suppression & anemia.
- Can be reversed with G-CSF and EPO
Distinguishing Abacavir from the other 6 NRTIs?
Hypersensitivity (Type 4) with HLA B57:01 allele
NNRTIs (mechanism)
NNRTIs (clinical)
How do NRTIs work?
They are competitive inhibitors of Reverse Transcriptase.
* Nuceloside analogs that pretend to be DNA building blocks
* Fit into the enzyme’s active site
How do NNRTIs work?
They bind Reverse Transcriptase at a location different from the active site (where NRTIs bind).
NNRTI drug names
- Efavirenz
- Nevirapine
- Delavirdine
Efavirenz (NNRTI) has what interesting side effect?
Vivid dreams.
HAART regimen.
Usually 3 drugs
* 2 NRTIs
* Integrase or Protein Inhibitor
Distinguishing Integrase Inhibitors from the other antiviral therapies?
Myositis in patients
* Increase in creatine kinase on bloodwork
Also, it is actively against both HIV-1 & HIV-2.
Protease Inhibitor drug names
- Atazanavir
- Darunavir
- Indinavir
- Lopinavir
- Ritonavir
- Saquinavir
- Fosamprenavir
Entry Inhibitors
* Enfuvirtide
Antiviral peptide that targets viral fusion.
Entry Inhibitors
* Maraviroc
Antiviral peptide that targets viral fusion.
Indinavir (protease inhibitor) is known to cause what specific adverse effects?
- Renal Toxicity
- Thrombocytopenia
Adverse profile for the Protease Inhibitor class:
- Hyperglycemia – can cause diabetes
- GI Upset
- Cushing-like syndrome (CYP-450 enzymes)
- **Avoid use of rifampin **(TB drug) due to CYP450 induction
Ritonavir (protease inhibitor) is known to cause what specific adverse effect?
Inhibits CYP-450 enzymes
* May be used to “boost” the concentration of other drugs metabolized by the liver.
CCR-5 is present on which cells?
Monocytes and macrophages
For which virus are NS5A, NS5B, & NS3/4A Inhibitors prescribed?
Hepatitis C virus.
NS5A Inhibitors
* Ledipasvir
* Ombitasvir
* Velpatasvir
NS5B Inhibitors
* Sofosbuvir
* Dasabuvir
NS3/4A Inhibitors
* Grazoprevir
* Simeprevir
What exactly do NS5B Inhibitors target to inhibit viral replication?
Inhibition of viral RNA-dependent RNA polymerase.
What exactly do NS5A Inhibitors target to inhibit viral replication?
Inhibition of viral phosphoprotein (NS5A).
What exactly do NS3/4A Inhibitors target to inhibit viral replication?
NS3/4A, a viral protease.