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Antivirals

Kaplan

QuestionAnswer
What are the “Antiherpetic drugs” (4) “-ovir” 1. Acyclovir 2. Cidofovir (used in TK negative strains) 3. Ganciclovir 4. Foscarnet (used in TK negative strains)
What is the target/ MOA of the Antiherpetic drugs? INHIBIT DNA POLYMERASE (Or Chain termination by adding fake nucleotide that lacks 3’OH)
How does Acyclovir get activated? Is a PRODRUG/ NUCLEOSIDE —> NUCLEOTIDE (triphosphorylated by viral and human kinases) Viral kinase: viral thymidine kinase (TK) - monophosphorylated
How does resistance to Acyclovir work? HSV strains that LACK THYMIDINE KINASE (TK NEGATIVE strains)
Which Antiherpetic drugs works against TK negative strains ?(2) 1. Cidofovir 2. Foscarnet
What is the clinical use of ACYCLOVIR? (2 virus) 1. Herpes simplex virus (HSV) 2. Varicella-zoster virus (VZV) (Reduce viral shedding in genitalia herpes) Viral shedding= release of viral particles, decreased dt decrease replication
How is postherpatic neuralgia/pain treated? (2 medications) 1. TCAs 2. Gabapentin
Acyclovir Side effects? Crystalluria (pt must stay hydrated)
MOA of Ganciclovir. And work on which viruses (3)? Similar to Acyclovir 1. HSV 2. VZV 3. CMV (retinitis)
Side Effects of Ganiciclovir Bone marrow suppression (hemtotoxic- leukopenia, thrombocytopenia) GANciclovir GANgs up on bone marrow
MOA of Foscarnet Inhibits DNA polymerase. (Not an antimetabolite) (NNRTI= Non-Nucleoside reverse transcriptase inhibitor. It is not a nucleoside so it does not need phosphorylation by kinases, acts directly)
side effects of Foscarnet? (2) 1. Nephrotoxicity 2. Hypocalcemia (tremor and seizure)
What are the group of drugs used to treat HIV? (4) 1. Reverse Transcriptase Inhibitors 2. Protease Inhibitors 3. Integrate Inhibitors 4. Fusion Inhibitors
What are the MOA of Reverse Transcriptase Inhibitors (RTIs)? PRODRUGS that gets triphosphorylated and INHIBIT REVERE TRANSCRIPTASE (by competing w/ natural nucleotides) (Also can cause chain termination)
What are the Reverse transcriptase inhibitors? (3) 1. ZIDOVUDINE, AZT (thymidine analogue) 2. LAMIVUDINE, 3TC (cytosine analogue) 3. EMTRICITABINE ,FTC (cytosine analogue)
Side effect of Zidovudine? Bone marrow suppression (hematoxicity)
side effect of Lamivudine and EMTRICITABINE Least toxic of the RTIs Both should never be used together to avoid competition. *both are CYTOSINE analogues
What is a NtRTI and its structure? TENOFOVIR (not to be confused w a hepatitis drug dt suffix) Structure: already has a phosphate head (only 2 is needed)
What are the NNRTis (non-nucleoside reverse transcriptase inhibitors? (2) and MOA, S/E 1. EFAVIRENZ 2. NEVIRAPINE INHIBIT reverse transcriptase at different site than NRTIs S/E maculopapular rash and vivid dreams
What are the Protease Inhibitors? (4) ”-navirs” 1. Ritonavir 2. Lopinavir 3. Atazanavir 4. Darunavir (Last three are co-formulated w Ritonavir)
MOA of Protease Inhibitors INHIBITS Aspartate protease (pol gene encoded) —> virus cannot mature (Aspartame protease cleaves polypeptides in HIV to form proteins of mature virus core)
Why is Ritonavir and other “-avirs” used together? Bc RITONAVIR is a P450 enzyme inhibitor so it increase the level of the 2nd Protease inhibitor
Side effect of Ritonavir? Syndrome of disordered lipid and CHO (aldehyde) metabolism w central adiposity and insulin resistance
What are the Integrase Inhibitors (1) and MOA? “-tegravirs” 1. Raltegravir MOA: PREVENT INTEGRATION OF VIRAL GENOME IN HOST CELL DNA
What are the Fusion Inhibitors? (2) 1. Maravicor 2. Enfuvirtide BOTH are BACKUP drugs (not really used much)
MOA of MARAVICOR Blocks the binding of the gp120 HIV protein to CCR5 on macrophage surface (to prevent viral entry)
MOA of ENFUVIRTIDE bind to gp41 and inhibits the fusion HIV-1 to CD4+ cells
Difference between NRTIs and NNRTIs? NRTIs NEEDS to be PHOSPHORYLATED, NNRTIs does NOT need to be phosphorylated (Herpes does not need NRTIs because they do not need to be reverse translated)
What is the combination treatment of HIV in pregnancy? 2 NRTIs needs to be combined
What are used as COMPLETE treatment regimes for HIV? Integrase inhibitors + 2 NRTIs
MOA of Zanamivir and Oseltamivir? Inhibit NEURAMINIDASES of Influenza A and B —> decrease viral shedding (less replication, less transmission) (NEURAMINIDASES inhibits virons clumping so that more particles are available for infecting host cells)
What are the Hepatitis C drugs? (3) 1. Simeprevir (NS3/4A) 2. Ledipasvir (NS5A) 3. Sofosbuvir (NS5B)
MOA of Simeprevir Hep C protease inhibitor
MOA of Ledipasvir Inhibits HCV NS5A protein —> decrease RNA replication and secretion
MOA of Sofosbuvir Inhibits RNA polymerase (nucleotide analog) Hep C drug
MOA of Ribavirin (HepC med) Inhibits IMP dehydrogenase and RNA polymerase (Used in Lasa fever and Hanta virus)
Which antiviral drug has “-avir” drugs for AIDS (HIV)
Which antiviral drug has “-ivir” drugs for INFLUENZA
Which antiviral drug has “-ovir” drugs for Oh HERPES!
Created by: DVD27
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