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Flashcards in Antivirals Deck (31):
1

Atazanavir

Protease inhibitor

2

Lopinavir

Protease inhibitor

3

Darunavir

Protease inhibitor

4

Fosamprenavir

Protease inhibitor

5

Saquinavir

Protease inhibitor

6

Ritonavir

Protease inhibitor

*Cytochrome P-450 inhibitor

7

Tenofovir

Nucleotide Reverse Transcriptase Inhibitor

8

Emitricitabine

Nucleoside Reverse Transcriptase Inhibitor

9

Abacavir

Nucleoside Reverse Transcriptase Inhibitor

10

Lamivudine

Nucleoside Reverse Transcriptase Inhibitor

11

Zidovudine

Nucleoside Reverse Transcriptase Inhibitor

*Used for general prophylaxis & during pregnancy to reduce risk of fetal transmission

Additional SE: megaloblastic anemia

12

Didanosine

Nucleoside Reverse Transcriptase Inhibitor

13

Stavudine

Nucleoside Reverse Transcriptase Inhibitor

14

Nevirapine

Non-nucleoside Reverse Transcriptase Inhibitor

15

Efavirenz

Non-nucleoside Reverse Transcriptase Inhibitor

Teratogenic

16

Delavirdine

Non-nucleoside Reverse Transcriptase Inhibitor

16

Elvitegravir

Integrase Inhibitor

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase

SE: hypercholesterolemia

17

Zanamivir

Inhibits influenza neuraminidase, decreasing the release of progeny virus

Tx: both influenza A and B

18

Elvitegravir

Integrase Inhibitor

19

Amantadine

Blocks viral penetration/ uncoating (M2 protein)

Prophylaxis and treatment for Influenza A; treats Parkinson's

Toxicity: ataxia, dizziness, slurred speech

Mechanism of Resistance: mutated M2 protein

Rimantidine is a derivative w/ fewer CNS side effects (Doesn't cross BBB)

20

Oseltamivir

Inhibits influenza neuraminidase, decreasing the release of progeny virus

Tx: both influenza A and B

22

Ribavirin

Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase

Tx: RSV, chronic hepatitis C

SE: Hemolytic anemia. Severe teratogen

23

Acyclovir

Monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inhibits viral DNA polymerase by chain termination.

Tx: HSV, VZV, EBV. No effect on latent HSV/VZV.

Valacyclovir (produg) has better oral bioavailability. For herpes zoster use famciclovir.

Mechanism of resistance: lack of viral thymidine kinase

24

Ganciclovir

5'-monophosphate formed by a CMV viral kinase. Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhibits viral DNA polymerase.

Tx: CMV, especially in immunocompromised patients.

Valganciclovir (produg) has better oral bioavailability.

Toxicity: Leukopenia, neutropenia, thrombocytopenia, renal toxicity. More toxic to host enzymes than acyclovir.

Mechanism of resistance: Mutated CMV DNA polymerase OR lack of viral kinase

25

Foscarnet

Viral DNA polymerase inhibitor that binds pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase.

Tx: CMV retinitis in immunocompromised pts when ganciclovir fails; acyclovir-resistant HSV

Toxicity: Nephrotoxicity

Mechanism of resistance: Mutated DNA polymerase

26

Cidofovir

Preferentially inhibits viral DNA polymerase. Does NOT require phosphorylation by viral kinase.

Tx: CMV retinitis in immunocompromised patients; acyclovir-resistant HSV. Long half life.

Toxicity: Nephrotoxicity (coadminister w/ probenecid)

27

Protease inhibitors

Prevent maturation of new viruses (HIV-1 protease cleaves polypeptide products of HIV mRNA into functional parts & allows assembly of virions)

SE: hyperglycemia, GI intolerance, lipodystrophy

28

NRTIs

Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack a 3'-OH group)
*activated by thymidine kinase phosphorylation

SE: bone marrow suppression, peripheral neuropathy

29

NNRTIs

Bind to reverse transcriptase at a site different from NRTIs
*don't require phosphorylation for activation!

30

Integrase Inhibitors

Inhibit HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase

SE: hypercholesterolemia

31

Enfuvirtide

Fusion inhibitor

Selectively binds gp41 and prevents entry of HIV genome into unaffected CD4+ cells