Antivirals Flashcards

1
Q

Atazanavir

A

Protease inhibitor

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2
Q

Lopinavir

A

Protease inhibitor

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3
Q

Darunavir

A

Protease inhibitor

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4
Q

Fosamprenavir

A

Protease inhibitor

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5
Q

Saquinavir

A

Protease inhibitor

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6
Q

Ritonavir

A

Protease inhibitor

*Cytochrome P-450 inhibitor

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7
Q

Tenofovir

A

Nucleotide Reverse Transcriptase Inhibitor

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8
Q

Emitricitabine

A

Nucleoside Reverse Transcriptase Inhibitor

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9
Q

Abacavir

A

Nucleoside Reverse Transcriptase Inhibitor

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10
Q

Lamivudine

A

Nucleoside Reverse Transcriptase Inhibitor

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11
Q

Zidovudine

A

Nucleoside Reverse Transcriptase Inhibitor

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

Additional SE: megaloblastic anemia

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12
Q

Didanosine

A

Nucleoside Reverse Transcriptase Inhibitor

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13
Q

Stavudine

A

Nucleoside Reverse Transcriptase Inhibitor

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14
Q

Nevirapine

A

Non-nucleoside Reverse Transcriptase Inhibitor

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15
Q

Efavirenz

A

Non-nucleoside Reverse Transcriptase Inhibitor

Teratogenic

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16
Q

Delavirdine

A

Non-nucleoside Reverse Transcriptase Inhibitor

16
Q

Elvitegravir

A

Integrase Inhibitor

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

SE: hypercholesterolemia

17
Q

Zanamivir

A

Inhibits influenza neuraminidase, decreasing the release of progeny virus

Tx: both influenza A and B

18
Q

Elvitegravir

A

Integrase Inhibitor

19
Q

Amantadine

A

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
Q

Oseltamivir

A

Inhibits influenza neuraminidase, decreasing the release of progeny virus

Tx: both influenza A and B

22
Q

Ribavirin

A

Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase

Tx: RSV, chronic hepatitis C

SE: Hemolytic anemia. Severe teratogen

23
Q

Acyclovir

A

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
Q

Ganciclovir

A

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
Q

Foscarnet

A

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
Q

Cidofovir

A

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
Q

Protease inhibitors

A

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
Q

NRTIs

A

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
Q

NNRTIs

A

Bind to reverse transcriptase at a site different from NRTIs

*don’t require phosphorylation for activation!

30
Q

Integrase Inhibitors

A

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

SE: hypercholesterolemia

31
Q

Enfuvirtide

A

Fusion inhibitor

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