click below
click below
Normal Size Small Size show me how
Antivirals
Kaplan
| Question | Answer |
|---|---|
| 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! |