Anti-Virals

Question 1

Oseltamivir, Zanamivir

Answer 1

MAO: inhibit influenza neuroaminidase - dec release of progeny virus

Tx and prevention of flu A and B (w/in 48 hrs symptoms)

Question 2

Acyclovir, Valacyclovir

Answer 2

MAO: Guanosine analogs that must be mono-phos by HSV/VZV thymidine kinase then inhibit viral DNA polymerase by chain termination

Work on HSV and VZV and prophylaxis (weak for EBV and no CMV)

Only on active disease

Resistance: mutated viral thymidine kinase

Question 3

Famciclovir

Answer 3

Same MAO as acyclovir but used for herpes zoster specifically

Question 4

Ganciclovir

Answer 4

MAO: guanosine analog whose 5’ - monophosphate formed by CMV viral kinase then inhibits viral DNA polymerase

For CMV and prophylaxis

Resistance: mutated viral kinase

Question 5

Foscarnet

Answer 5

MAO: pyrophosphate analog that binds pyrophosphate binding site on Viral DNA poly, RNA poly and rev transcriptase to inhibit them (does NOT require kinase)

Uses - CMV retinitis when ganciclovir fails and acyclovir-resistant HSV

Resistance: mutated DNA polymerase

Question 6

Cidofovir

Answer 6

MAO: preferentially inhibits viral DNA poly (does NOT require kinase)

Uses - CMV retinitis when ganciclovir fails and acyclovir-resistant HSV

Long half-life

Question 7

NRTIs

Answer 7

HIV

Abacavir, didadosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine

MAO: nucleoside/ nucleotide analogs that comp inhibit nucleotide binding to reverse transcriptase and terminate DNA chain (lack a 3’ OH group); must be phosphorylated to be active

Tenofovir = nucleoTide (all others nucleoside)

Bone marrow suppression

Zidovudine for prophylaxis and pregnancy

Question 8

NNRTIs

Answer 8

HIV

Delavirdine, Efavirenz, Nevirapine

MAO: bind to reverse transcriptase at site diff from NRTIs and do NOT require phosphorylation to be active

Question 9

Protease Inhibitors

Answer 9

-navirs (no virions)

MAO: inhibits protease from pol gene from cleaving polypeptide into mature new viruses

Ritonavir inhibits CYT P450

Question 10

Integrase Inhibitors

Answer 10

HIV

Raltegravir, Elvitegravir, Dolutegravir (tegra)

MAO: inhibit HIV genome integration ino host cell chromosome bu reversibly inhibiting HIV integrase (also pol gene)

Question 11

Enfuvirtide

Answer 11

HIV

MAO: binds gp41 to inhibit viral entry

Question 12

Maraviroc

Answer 12

HIV

MAO: binds CCR-5 on surface of T cells and monocytes to inhibit interaction w/ gp120

“Maraviroc inhibits the dock”

Question 13

What is the typical HAART therapy regimen?

Answer 13

2 NRTIs + Integrase Inhibitor

Question 14

Interferons (3 types)

Answer 14

MAO: glycoproteins normally synthesized by virus-infected cells

Anti-viral and anti-tumor properties

IFN- alpha = chronic Hep B and C, Kaposi, hairy cell leukemia, condyloma acuminatum, RCC, malignant melanoma

IFN-beta = MS

IFN - gamma = chronic gran disease

Question 15

Ribavirin

Answer 15

MAO: inhibits synthesis of guanine nucleotides by comp inhibiting inosine monophosphate dehydrogenase

Chronic Hep C (+ some RSV)

Question 16

Sofosbuvir

Answer 16

MAO: inhibits Hep C RNA-dep RNA polymerase acting as a chain terminator

For Hep C but do not use alone

Question 17

SImeprevir

Answer 17

MAO: Hep C protease inhibitor

For Hep C but do not use as monotherapy