Anti-Virals Flashcards

1
Q

Mechanism of action of Ion Channel Blockers (Adamantane Drugs)

A

Block the viral M2 proton channel, prevent uncoating of influenza virus (early endosome)

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2
Q

<p>Names of Adamantane drugs </p>

A

<p>Rimantadine, Amantadine </p>

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3
Q

Enfuvirtide and Maraviroc act on what type of virus

A

HIV

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4
Q

Enfuvirtide MOA

A

Mimics HR2, binds to HR1 and prevents HR1-HR2 interaction, thus preventing fusion of HIV with CD4 T cell

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5
Q

Maraviroc MOA

A

small molecule antagonist that binds to CCR5. Only blocks strains of HIV that use CCR5 receptor (HIV-1)

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6
Q

Name the 2 antivirals that act as nucleic acid synthesis inhibitors

A

Acyclovir (valacyclovir), Ganciclovir (valganciclovir)

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7
Q

Acyclovir & Ganciclover act on what viruses

A

Herpes simples viruses 1 & 2, Varicella zoster virus, & cytomegalovirus

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8
Q

First step needed prior to acyclovir & ganciclover activity

A

Require metabolic activation to a triphosphate form

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9
Q

MOA of Acyclovir & ganciclover

A

After being metabolically activated to a triphosphate form, acyclovir or ganciclover compete with dGTP for terminal end of growing DNA chain within viral DNA polymerase. After binding to terminal end, traps the polymerase at that location, preventing further chain elongation.

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10
Q

Does acyclovir/ganciclover use host or viral kinase for activation?

A

Viral kinase used for addition of first phosphate group

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11
Q

Route of administration for acyclovir/ganciclover?

A

As a orally absorbed pro drug (valacyclovir/valganciclover)

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12
Q

Name NRTI’s used to treat HIV

A
ABACAVIR
LAMIVUDINE
TENOFOVIR DISOPROXIL
ZIDOVUDINE (AZT)
EMTRICITABINE
didanosine (ddl)
stavudine
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13
Q

Metabolic activation of nucleoside reverse transcriptase inhibitors (NRTIs) occurs by host or viral kinase?

A

Host kinase used for addition of first phosphate group.

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14
Q

NRTI inhibition type (competitive or noncompetitive)?

A

NRTI’s competitively inhibit reverse transcriptase.

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15
Q

Indirect inhibition of polymerase by NRTI has what consequence?

A

NRTIs also inhibit host cell mitochondrial DNA polymerase, causing depletion of mitochondrial DNA and subsequently mitochondrial RNA and peptides involves in ox phos. This ultimately leads to mitochondrial dysfunction, and leads to several toxicities associated with NRTIs.

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16
Q

Name 2 NNRTIs

A

Efavirenz, Nevirapine

17
Q

Where do NNRTIs (efavirenz & nevirapine) bind

A

the hydrophobic pocket in the p66 subunit of HIV-1 reverse transcriptase

18
Q

What does Raltegravir inhibit

A

the catalytic activity of HIV-1,2 encoded integrase –> viral DNA cannot be incorporated into host DNA

19
Q

What are the HIV-1 Protease Inhibitiors?

A

Atazanavir, Ritonavir, amprenavir, indinavir, lopinavir, nelfinavir, saquinavir

20
Q

How do HIV-1 Protease Inhibitors work?

A

They inhibit aspartyl protease enzymes that cleave HIV gag and pol precursor polypeptides that are required for HIV virion maturation

21
Q

Which HIV-1 Protease inhibits CYP activity?

A

Ritonavir inhibits CYP3A4

22
Q

What drugs are used to treat Hepatitis C??

A

Boceprevir, Telaprevir

23
Q

Efavirenz and Nevirapine work on what type of virus?

A

HIV-1 only, not HIV-2

24
Q

Raltegravir acts on what type of virus?

A

HIV-1, HIV-2 –> HIV integrase inhibitor

25
Q

What type of virus does Boceprevir and Telaprevir work on?

A

Hepatitis C

26
Q

What is the MOA of Foscarnet?

A

pyrophosphate anion mimic that binds to pyrophosphate binding site on DNA polymerase and inhibit DNA synthesis

27
Q

What types of viruses does Foscarnet work on?

A

Herpes simplex virus types 1 and 2 (HSV-1, HSV-2)

28
Q

Mechanism of boceprevir and telaprevir

A

Inhibits hepatitis C viral serine proteases needed to cleave viral peptide product into individual proteins –> structural proteins cannot be made

29
Q

Mechanism of oseltamivir and zanamivir

A

Block neuraminidase A and B in influenza so viral particles cannot be released from host cell

30
Q

Mechanism of peginterferon alfa

A

Signals cells to produce proteins that block viral protein synthesis

31
Q

Mechanism of ribavirin

A

Competitively inhibits GTP 5’ capping of viral mRNA in influenza –> viral mRNA rapidly degraded (mainly used for HepC)

32
Q

Mechanism of trifluridine?

A

Irreversibly binds thymidylate synthase and specific DNA polymerases, inhibiting DNA synthesis –> treats herpes simplex in the eye