Antivirals Flashcards by William Hannay

Release of Progeny Virus

Neuraminidase inhibitors

Zanamivir and Oseltamivir (Flu A and B)

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Nucleic acid synthesis

Guanine nucleotide synthesis: Ribavirin (RSV + HCV)

Viral DNA Polymerase inhibitors: Foscarnet and Cidofovir (HSV and CMV)

Guanosine analogs: Ayclovir, etc (HSV,VZV)
Ganciclovir (CMV)

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Uncoating

Amantadine and Rimantadine

No longer used

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Protein Synthesis

IFN-a

HBV & HCV

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Fusion (HIV)

Attachment: Maraviroc

Penetration: Enfuvirtide

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Reverse Transcriptase inhibitors (HIV)

NRTIs
Tenofovir (TDF)
Emtricitabine (FTC)
Abacavir (ABC)
Lamivudine (3TC)
Zidovudine (ZDV, use to be AZT)
Didanosine (ddl)
Stavudine (d4T)

NNRTIs
Nevirapine
Efavirenz
Delavirdine

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Integrase inhibitors

Raltegravir

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Protease inhibitors

Lopinavir
Atazanavir
Darunavir
Fosamprenavir
Squinavir
Ritonavir
Indinavir

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Zanamivir/Oseltamivir

Inhibits influenza Neuramidase. Decrease release of progeny

Influenza A and B

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Ribavirin

Inhibits gaunaine nulceotides by competitively inhibiting IMP dehydrogenase

RSV, Chronic Hep C

Hemolytic anemia. Severe Teratogen

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Acyclovir, Famciclovir, Valacyclovir (Guanosine analogs)

Monophosphylated by HSV/VZV thymidine kinase, but not uninfected cells

Guanosine analogs. Triphosphate formed by cellular enzymes. (incorporated to viral DNA)
Preferentially inhibits viral DNA polymerase by chain termination

HSV, VZV, weak against EBV and nothing in CMV.

Mucocutaneous and genital lesions, encephalitis.

Prophylaxis in immunocompromized.

Only in primary infection, not latent.

Vala is a prodrug to acyclo. increase bio avaialbility

HZ –> Famciclovir, releated

Can cause Obstructive cystalline nephropathy, ARF.

Resistance from mutated viral thymidine kinase

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Ganciclovir

Guanosine analog, but different thymidine kinase*

5 monophosphate formed by CMV viral kinase

Guanosine analong

Triphosphate by cellular kinase.

Preferential to viral DNA polymerase

CMV. Especially immunocompromised

Valganciclovir –> prodrug with better oral

Leukopenia, neutropenia, thrombocytopenia, renal toxicity.
More so than acyclovir

Resistance: Mutated CMV DNA polymerase or lack of viral kinase

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Foscarnet

Viral DNA polymerase inhibitor that binds to pyrophosphate binding site of the enzyme

Fos = pyroFOSphate analog

Does not require viral kinase activation.

CMV retinitis w/ ganciclovir fail or acyclovir reisstant HSV

Nephrotoxicity, anemia, bad side effects

Resistance from mutated DNA polymerase

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Cidofovir

Preferentially inhibits viral DNA polymerase, doesn’t need viral kinase

CMV retintis in immunocompromised patients; acyclovir resistant HSV. long 1/2 life

Nephrotoxicity. Coadminister w/ probenecid and IV saline

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HAART

When AIDS defininig illness or

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Protease inhibitors

“Navir”

Assembly of virion depends onf HIV-1 (pol) gene. Cleaves polypeptides.

Ritonavir can boost other drug concentrations (inhibits c P450)

Hyperglycemia, hyperlipidemia, GI intolerance, lipidystrophy.

Nephropathy, hematuria w/ Indinavir

Atazanavir –> stones/hyperbili

Indinavir –> stones

Ritonavir –> pancreatitis

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NRTIs

Abacavir (ABC) (HLA B570
Didanosine (ddI) Pancreatitis/ Hep steatosis
Emtricitabine (FTC)
Lamivudine (3TC)
Stavudine (d4T)
Tenofovir (TDF) - NtRTI
Zidovuide (ZDV/AZT) (anemia, GI, Pregnancy)

Competively inhibits nucleotide binding to RT. Terminates DNA chain.

Requires Thymidine Kinase - Tenofovir

Tenofovir is a nucleotide.

BM suppression (reverse w/ G-CSF and EPO),
peripheral neuropathy
Lactic acidosis (nucleosides)
Rash (nucleotides)

ZDV –> anemia.

ZDV in pregnancy and general prophylaxis (occupation)

ddI –> Pancreatitis

NNRTIs

Don’t need phosphorylation/thymidine kinase

Efavirenz (neuropsych)
Nevirapine
Delavirdine

Bind to RT at different site. Noncompetetive

Rash, hepatotoxicity

Vivid dreams/CNS in efavirenz.

Delavirdine and efavirenz contraindicated in pregnancy

Integrase inhibitors

Raltegravir

Inhibits genome intergration

Hypercholesterolemia, hyperglycemia (metabolic), pancreatitis, hepatotoxicity

Fusion inhibitors

Enfuvirtide (gp41) –> viral entry

Maraviroc (CCR5) –> viral attachment

Skin reactions
at injection sites

can be X4 virus, dont’ give it

Atazanavir

Protease inhibitor

Stones, hyperbilirubinemia

Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Darunavir

Protease inhibitor

Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Fosamprenavir

Protease inhibitor

Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Indinavir

Protease inhibitor

Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Stones, Nephropathy, hematuria

Lopinavir

Protease inhibitor Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Ritonavir

Protease inhibitor Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy Inhibits p-450

Saquinavir

Protease inhibitor Hyperglycemia, GI intolerance (nausea/diarrhea), lipodystrophy

Abacavir

NRTI (ABC) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ```

Didanosine

NRTI (ddI) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ``` Pancreatitis, hepatosteatosis

Emtricitabine

NRTI (FTC) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ```

Lamivudine

NRTI (3TC) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ```

Satuvidine

NRTI (d4T) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ```

Tenofovir

NRTI (TDF) ``` BM suppression (reverse w/ G-CSF and EPO) Rash, peripheral neuropathy, ```

Zidovudine

NRTI (ZDV) ``` BM suppression (reverse w/ G-CSF and EPO) Lactic acidosis, peripheral neuropathy, ``` Pregnancy/prophylaxis. Anemia

Efavirenz

NNRTI Rash, hepatotoxicity Vivid dreams and CNS symptoms not for pregnancy

Nevirapine

NNRTI Rash, hepatotoxicity

Delavirdine

NNRTI Rash, hepatotoxicity Not for pregnancy

Interferons

Glycoproteins. Synthesized in viral infected cells, wide range of antitumor and antiviral properties Neutropenia and myopathy

IFN-a

Chronic Hep B, Hep C Kaposi sarcoma, Hairy cell leukemia, conyloma acuminatum, RCC, MM

IFN-B

IFN-y

CGD