Block 3 materials (Antivirals) Flashcards
Drugs that are Entry inhibitors?
Maraviroc (Attachment)
Enfuvirtide (Fusion)
Drugs that are Reverse transcriptase inhibitors?
NRTI’s
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF)
Zidovudine (ZDV,
formerly AZT)
NNRTI
Delavirdine
Efavirenz
Nevirapine
Drugs that are integrase inhibitors?
gravir suffix
Dolutegravir
Elvitegravir
Raltegravir
Bictegravir
Drugs that are protease inhibitors?
navir suffix
Atazanavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Ritonavir
Saquinavir
Drugs that are nucleic acid synthesis inhibitors?
1) Guanosine analogs
- Acyclovir, etc (HSV, VZV)
- Ganciclovir (CMV)
2) Adenosine analog
- Remdesivir (SARS-CoV-2)
3) Endonuclease inhibitor
- Baloxavir (influenza virus)
4) Viral DNA polymerase
inhibitors
- Cidofovir &Foscarnet
(HSV* & CMV)
5) Guanine nucleotide synthesis
- Ribavirin (RSV, HCV
Drugs that inhibit progeny release?
Neuraminidase inhibitors
Oseltamivir & Zanamivir (Influenza A & B)
Oseltamivir & Zanamivir
MOA:
Clinical uses:
Adverse effects:
MOA:
Neuraminidase inhibitors that prevent the release of viral progeny
Clinical uses:
Influenza A & B
Adverse effects:
1) Gi upset
2) Exacerbate COPD (Zanamivir)
MOA:
Neuraminidase inhibitors that prevent the release of viral progeny
Clinical uses:
Influenza A & B
Adverse effects:
1) Gi upset
2) Exacerbate COPD (Zanamivir)
Oseltamivir & Zanamivir
Baloxavir
MOA:
Clinical uses:
MOA:
Inhibits cap0snatching endonucleases to reduce viral replication
Clinical use:
Reduce the severity of influenza virus within 48hrs
MOA:
Inhibits cap0snatching endonucleases to reduce viral replication
Clinical use:
Reduce the severity of influenza virus within 48hrs
Baloxavir
Remdesivir
MOA:
Clinical uses:
MOA:
Adenosine analog that inhibits viral RNA-dependent RNA polymerase (reduce viral production)
Clinical use:
SARS-CoV-2 (covid)
MOA:
Adenosine analog that inhibits viral RNA-dependent RNA polymerase (reduce viral production)
Clinical use:
SARS-CoV-2 (covid)
Remdesivir
Acyclovir, Famciclovir, Valacyclovir
MOA:
Clinical uses:
Adverse effects:
Resistance:
MOA:
Guanosine analogs that are phosphorylated by HSV/VZV thymidine kinase to inhibit viral DNA polymerase
Clinical use:
HSV & VZV
Adverse effects:
1) Obstructive crystalline nephropathy
2) Acute kidney injury (hydrate!)
Resistance:
Mutated thymidine kinase
MOA:
Guanosine analogs that are phosphorylated by HSV/VZV thymidine kinase to inhibit viral DNA polymerase
Clinical use:
HSV & VZV
Adverse effects:
1) Obstructive crystalline nephropathy
2) Acute kidney injury (hydrate!)
Resistance:
Mutated thymidine kinase
Acyclovir, Famciclovir, Valacyclovir
Ganciclovir
MOA:
Clinical uses:
Adverse effects:
Resistance:
MOA:
Guanosine analog that is formed by CMV kinase to inhibit viral DNA polymerase to prevent viral replication
Clinical uses:
CMV (HIV/AIDS)
Adverse effects:
1) Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia)
2) Nephrotoxicity
Resistance:
Mutated CMV viral kinase
MOA:
Guanosine analog that is formed by CMV kinase to inhibit viral DNA polymerase to prevent viral replication
Clinical uses:
CMV (HIV/AIDS)
Adverse effects:
1) Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia)
2) Nephrotoxicity
Resistance:
Mutated CMV viral kinase
Ganciclovir
What is the second option if a patient with CMV is resistant to ganciclovir?
Use Valganciclovir
Foscarnet
MOA:
Clinical uses:
Adverse effects:
Resistance:
MOA:
Viral DNA/RNA polymerase inhibitor & HIV reverse transcriptase inhibitor that binds the pyrophosphate site to activate
(does NOT need kinases to be activated)
Clinical uses:
CMV retinitis (in HIV/AIDS)
Acyclovir-resistant HSV
Adverse effects:
1) Nephrotoxicity
2) Electrolyte abnormalities
3) Seizures
4) Genital ulcers
Resistance:
Mutated DNA polymerase
MOA:
Viral DNA/RNA polymerase inhibitor & HIV reverse transcriptase inhibitor that binds the pyrophosphate site to activate
(does NOT need kinases to be activated)
Clinical uses:
CMV retinitis (in HIV/AIDS)
Acyclovir-resistant HSV
Adverse effects:
1) Nephrotoxicity
2) Electrolyte abnormalities
3) Seizures
4) Genital ulcers
Resistance:
Mutated DNA polymerase
Foscarnet
Cidofovir
MOA:
Clinical uses:
Adverse effects:
MOA:
Inhibits viral DNA polymerase (No viral kinases to activate it)
Clinical uses:
CMV retinitis (HIV/AIDS)
Acyclovir resistant HSV
Adverse effects:
Nephrotoxicity (give with probenecid & IV saline to reduce toxicity)
MOA:
Inhibits viral DNA polymerase (No viral kinases to activate it)
Clinical uses:
CMV retinitis (HIV/AIDS)
Acyclovir resistant HSV
Adverse effects:
Nephrotoxicity (give with probenecid & IV saline to reduce toxicity)
Cidofovir
NRTI’s
MOA:
Clinical uses:
Adverse effects:
“SEAL The DealZ”
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF) - nucleoTide
Zidovudine (ZDV)
Didanosine
Stavudine
MOA: HIV therapy (Nucleoside reverse transcriptase inhibitors)
Competitively inhibits nucleotide binding to reverse transcriptase & terminate DNA chain elongation (because they lack 3’‘OH)
Clinical uses:
HIV 1/2 therapy (HAART)
ZIDOVUDINE - safe to use in preggos
Adverse effects:
1) Bone marrow suppression
2) Peripheral neuropathy
3) Lactic acidosis (nucleoSides)
4) Anemia (zidovudine)
5) Hypersensitivity in people with HLA-B57 (abacavir)
6) Pancreatitis (Didanosine)
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF) - nucleoTide
Zidovudine (ZDV)
Didanosine
Stavudine
MOA: HIV therapy (Nucleoside reverse transcriptase inhibitors)
Competitively inhibits nucleotide binding to reverse transcriptase & terminate DNA chain elongation (because they lack 3’‘OH)
Clinical uses:
HIV 1/2 therapy (HAART)
ZIDOVUDINE - safe to use in preggos
Adverse effects:
1) Bone marrow suppression
2) Peripheral neuropathy
3) Lactic acidosis (nucleoSides)
4) Anemia (zidovudine)
5) Hypersensitivity in people with HLA-B57 (abacavir)
6) Pancreatitis (Didanosine)
NRTI’s
NNRTI’s
MOA:
Clinical uses:
Adverse effects:
Delavirdine
Efavirenz
Nevirapine
MOA: HIV 1 therapy (Non-nucleoside reverse transcriptase inhibitors)
Non-competitively binds HIV reverse transcriptase to inhibit viral DNA synthesis (does NOT need phosphorylation)
Clinical uses:
HIV 1
Adverse effects:
1) Rash (risk of SJS & toxic epidermal necrolysis)
2) Hepatotoxicity
3) Vivid dreams (Efavirenz)
4) Teratogenic
Delavirdine
Efavirenz
Nevirapine
MOA: HIV 1 therapy (Non-nucleoside reverse transcriptase inhibitors)
Non-competitively binds HIV reverse transcriptase to inhibit viral DNA synthesis (does NOT need phosphorylation)
Clinical uses:
HIV 1
Adverse effects:
1) Rash (risk of SJS & toxic epidermal necrolysis)
2) Hepatotoxicity
3) Vivid dreams (Efavirenz)
4) Teratogenic
NNRTI’s
Integrase inhibitors
MOA:
Clinical uses:
Adverse effects:
Bictegravir
Dolutegravir
Elvitegravir
Raltegravir
MOA:
Inhibits HIV genome integration into host cells chromosomes
Clinical uses:
HIV 1& 2 therapy (HAART)
Adverse effects:
1) Myosis/Myopathy (Elevated CK)
Bictegravir
Dolutegravir
Elvitegravir
Raltegravir
MOA:
Inhibits HIV genome integration into host cells chromosomes
Clinical uses:
HIV 1& 2 therapy (HAART)
Adverse effects:
1) Myosis/Myopathy (Elevated CK)
Integrase inhibitors
Protease Inhibitors
MOA:
Clinical uses:
Adverse effects:
Atazanavir
Darunavir
Lopinavir
Ritonavir
MOA:
Inhibit HIV-1 protease (pol gene) to prevent maturation of new viruses
Clinical uses:
HIV 1 & 2 therapy (HAART)
Adverse effects:
1) Hyperglycemia
2) GI upset
3) Lipodystrophy (Cushing’s like disease)
4) Inhibits CYP450 (Ritonavir)
5) Renal toxicity/Hematuria/Nephropathy/Thrombocytopenia (Indinavir)
AVOID Rifampin!
Atazanavir
Darunavir
Lopinavir
Ritonavir
MOA:
Inhibit HIV-1 protease (pol gene) to prevent maturation of new viruses
Clinical uses:
HIV 1 & 2 therapy (HAART)
Adverse effects:
1) Hyperglycemia
2) GI upset
3) Lipodystrophy (Cushing’s like disease)
4) Inhibits CYP450 (Ritonavir)
5) Renal toxicity/Hematuria/Nephropathy/Thrombocytopenia (Indinavir)
AVOID Rifampin!
Protease Inhibitors
Enfuvirtide
MOA:
Clinical uses:
Adverse effects:
MOA:
Binds gp41 on the HIV envelope to inhibit fusion/entry
Clinical use:
HIV 1 therapy
Adverse effects:
1) Skin reaction at injection sites
2) Peripheral neuropathy
MOA:
Binds gp41 on the HIV envelope to inhibit fusion/entry
Clinical use:
HIV 1 therapy
Adverse effects:
1) Skin reaction at injection sites
2) Peripheral neuropathy
Enfuvirtide
Maraviroc
MOA:
Clinical uses:
Adverse effects:
MOA:
Binds CCR-5 on T cell/macrophages surfaces to prevent HIV envelop protein gp120 from docking/entry
Clinical use:
HIV 1 & 2 therapy
Adverse effect:
Hepatotoxicity
MOA:
Binds CCR-5 on T cell/macrophages surfaces to prevent HIV envelop protein gp120 from docking/entry
Clinical use:
HIV 1 & 2 therapy
Adverse effect:
Hepatotoxicity
Maraviroc