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FA - Microbiology > Micro - Antimicrobials (Antiviral therapy) > Flashcards

Micro - Antimicrobials (Antiviral therapy) Flashcards

Pg. 191-193 in First Aid 2014 Sections include: -Antiviral therapy -Zanamivir, oseltamivir -Ribavirin -Acyclovir, famciclovir, valacyclovir -Ganciclovir -Foscarnet -Cidofovir

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Biology 101 flashcards
1
Q

What are 2 types of HIV antiviral therapy that work on fusion? What part of fusion is inhibited by each?

A

FUSION (1) Attachment: Maraviroc (2) Penetration: Enfuvirtide

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2
Q

What HIV antiviral therapy is an example of an Integrase Inhibitor?

A

Raltegravir

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3
Q

Give 7 examples of protease inhibitors used as HIV antiviral therapy.

A

(1) Lopinavir (2) Atazanavir (3) Darunavir (4) Fosamprenavir (5) Saquinavir (6) Ritonavir (7) Indinavir

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4
Q

What are the 2 types of Reverse transcriptase inhibitors used as HIV Antiviral therapy?

A

NRTIs, NNRTIs

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5
Q

What are 7 examples of NRTIs used as Reverse transcriptase inhibitors in HIV antiviral therapy?

A

NRTIs: (1) Tenofovir (TDF) (2) Emtricitabine (FTC) (3) Abacavir (ABC) (4) Lamivudine (3TC) (5) Zidovudine (ZDV, formerly AZT) (6) Didanosine (ddl) (7) Stavudine (d4T)

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6
Q

What are 3 examples of NNRTIs used as Reverse transcriptase inhibitors in HIV antiviral therapy?

A

NNRTIs: (1) Nevirapine (2) Efavirenz (3) Delavirdine

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7
Q

What are the 4 major categories of drugs used as HIV antiviral therapy?

A

(1) Fusion (2) Integrase inhibitors (3) Protease inhibitors (4) Reverse transcriptase inhibitors

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8
Q

What are the 4 major categories of drugs (based on function of inhibition) used as other (non-HIV) antiviral therapy?

A

(1) Protein synthesis (2) Uncoating (3) Nucleic Acid synthesis (4) Release of progeny virus

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9
Q

What is an example of an antiviral therapy that functions via protein synthesis?

A

Protein synthesis: Interferon-alpha

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10
Q

What are 2 examples of antiviral therapy that functions via inhibition of uncoating?

A

Uncoating: (1) Amantadine (2) Rimantadine

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11
Q

What are the 3 major categories of antiviral therapy that function via inhibition of nucleic acid synthesis? Give at least one example of a drug in each category.

A

Nucleic Acid Synthesis: (1) Guanine nucleotide synthesis - Ribavirin (2) Viral DNA polymerase inhibitors - Foscarnet, Cidofovir (3) Guanosine analogs - Acyclovir, etc., Ganciclovir

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12
Q

What is an example of an antiviral therapy that works via inhibition of guanine nucleotide synthesis? What are 2 viruses treated by this drug?

A

Ribavirin (RSV, HCV)

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13
Q

What are 2 examples of antiviral therapy that work as viral DNA polymerase inhibitors? What are 2 viruses treated by either of these drugs? Which of these 2 viruses is only treated if acyclovir-resistant?

A

(1) Foscarnet (2) Cidofovir; CMV, HSV; HSV is acyclovir-resistant

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14
Q

What are 2 examples of antiviral therapy that work as guanosine analogs? What is at least one virus treated by each of these drugs?

A

(1) Acyclovir, etc (HSV, VZV) (2) Ganciclovir (CMV)

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15
Q

What is the major category of antiviral therapy that works via inhibition of progeny virus?

A

Neuraminidase inhibitors

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16
Q

What are 2 examples of Neuraminidase inhibitors? What are 2 examples of viruses that may be treated by either of these drugs?

A

(1) Zanamivir (2) Oseltamivir; Influenza A, B

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17
Q

For which virus is antiviral therapy that inhibits uncoating (i.e., amantadine/rimantadine) no longer useful, and why?

A

No longer useful for influenza due to high resistance

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18
Q

Draw a visual depicting the following 4 methods of HIV antiviral therapy in a CD4 T cell: (1) Inhibition of Fsion (2) Integrase inhibitors (3) Reverse transcriptase inhibitors (4) Protease inhibitors.

A

See p. 191 in First Aid 2014 for visual on left

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19
Q

Draw a visual depicting the following 4 methods of other (non-HIV) antiviral therapy in mammalian cell: (1) Protein synthesis (2) Inhibition of uncoating (3) Inhibition of nucleic acid synthesis (4) Inhibition of release of progeny virus

A

See p. 191 in First Aid 2014 for visual on right

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20
Q

What is the mechanism of Zanamivir and its effect? What other drug shares this mechanism/effect

A

Inhibit influenza neuraminidase –> decrease the release of progeny virus; Oseltamivir

21
Q

What is the clinical use for Zanamivir and Oseltamivir?

A

Treatment and prevention of both influenza A and B

22
Q

What is the mechanism and effect of Ribavirin?

A

Inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase

23
Q

What are 2 clinical uses of Ribavirin?

A

(1) RSV (2) Chronic hepatitis C

24
Q

What are 2 toxicities associated with Ribavirin?

A

(1) Hemolytic anemia (2) Severe teratogen

25
Q

What kind of drug is Acyclovir? How do cellular enzymes change its form? What is its mechanism? What other 2 drugs are the same as Acyclovir in these ways?

A

Monophosphorylated by HSV/VZV thymidine kinase and not phosphorylated in uninfected cells –> few adverse effects. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inhibits viral DNA polymerase by chain termination; Famciclovir, Valacyclovir

26
Q

To what extent do acyclovir/famiclovir/valacyclovir have adverse effects, and why?

A

Monophosphorylated by HSV/VZV thymidine kinase and not phosphorylated in uninfected cells –> few adverse effects.

27
Q

What are the 2 main viruses for which acyclovir/famiclovir/valacyclovir are used? Against what virus do they have weak activity? In what contexts do they have no activity?

A

HSV and VZV. Weak activity against EBV. No activity against CMV. No effect on latent forms of HSV and VZV.

28
Q

For what HSV-related conditions are acyclovir/famiclovir/valacyclovir clinically used?

A

Used for HSV-induced mucocutaneous and genital lesions as well as encephalitis.

29
Q

How are acyclovir/famiclovir/valacyclovir clinically used in immunocompromised patients?

A

Prophylaxis in immunocompromised patients

30
Q

What is Valacyclovir? How does it compare to acyclovir in terms of bioavailability?

A

Valacyclovir, a prodrug of acyclovir, has better oral bioavailability

31
Q

Of acyclovir/famiclovir/valacyclovir, which is used in the case of herpes zoster?

A

For herpes zoster, use a related agent, famiclovir

32
Q

What are 2 toxicities associated with acyclovir/famiclovir/valacyclovir?

A

(1) Obstructive crystalline nephropathy and (2) Acute renal failure if not adequately hydrated

33
Q

What is the mechanism of resistance against acyclovir/famiclovir/valacyclovir?

A

Mutated viral thymidine kinase

34
Q

What is the mechanism of ganciclovir?

A

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

35
Q

What is the clinical use for ganciclovir?

A

CMV, especially in immunocompromised patients.

36
Q

What is Valganciclovir, and how does it compare to ganciclovir in terms of bioavailability?

A

Valganciclovir, a prodrug of ganciclovir, has better oral bioavailability

37
Q

What are 4 toxicities associated with ganciclovir?

A

(1) Leukopenia (2) Neutropenia (3) Thrombocytopenia (4) Renal toxicity

38
Q

How does ganciclovir compare to acyclovir in terms of toxicity?

A

More toxic to host enzymes than acyclovir.

39
Q

What is the mechanism of resistance against ganciclovir?

A

Mutated CMV DNA polymerase or lack of viral kinase

40
Q

What is the mechanism of foscarnet?

A

Viral DNA polymerase inhibitor that binds the pyrophosphate-binding site of the enzyme; Think: “FOScarnet = pyroFOSphate analog”

41
Q

How is foscarnet different from acyclovir/famiclovir/valacyclovir and ganciclovir?

A

Does not require activation by viral kinase

42
Q

What is the clinical use of foscarnet?

A

CMV retinitis in immunocompromised patients when ganciclovir fails; Acyclovir-resistant HSV

43
Q

What is the toxicity associated with foscarnet?

A

Nephrotoxicity

44
Q

What is the mechanism of resistance against foscarnet?

A

Mutated DNA polymerase

45
Q

What is the mechanism of Cidofovir?

A

Preferentially inhibits viral DNA polymerase.

46
Q

How Cidofovir different from acyclovir/famiclovir/valacyclovir and ganciclovir? Which other antiviral drug also shares this quality?

A

Does not require phosphorylation by viral kinase; Foscarnet

47
Q

What is the clinical use of Cidofovir? What other antiviral drug has the same clinical use?

A

CMV retinitis in immunocompromised patients; Acyclovir-resistant HSV; Foscarnet

48
Q

What kind of half-life does cidofovir have?

A

Long half-life

49
Q

What toxicity does Cidofovir have? What can be done to reduce this toxicity?

A

Nephrotoxicity (coadminister with probenecid and IV saline to decrease toxicity)

FA - Microbiology (43 decks)

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