Antiviral Drugs Flashcards

1
Q

how does herpesviruses facilitate effective drug therapy?

A
  • replication continues over long periods
  • encode enzymes for their own replication
  • participate in drug activation
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2
Q

two drugs used to prevent and treat influenza A, and the difference between them

A
  • amantadine and oseltamivir
  • amantadine is treatment and prophylaxis of influenza A ONLY, while oseltamivir is treatment and prevention of both influenza A and B
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3
Q

oseltamivir: use and mechanism

A
  • prophylaxis and treatment of influenza A and B

- inhibits influenza neuraminidases and interferes with viral release and penetration

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4
Q

ophthalmic herpes simplex

A

trifluridine

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5
Q

herpes simplex not ophthalmic

A

acyclovir, foscarnet, famciclovir, penciclovir

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6
Q

acyclovir: use, mechanism

A
  • systemic and genital herpes simplex

- activated by herpes enzymes and acts as a competitive inhibitor of dGTP and as a chain terminator

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7
Q

acute herpes zoster (shingles)

A

famciclovir

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8
Q

recurrent genital herpes

A

famciclovir

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9
Q

famciclovir: uses, mechanism

A
  • acute herpes zoster (shingles), recurrent genital herpes
  • mechanism similar to acyclovir, prodrug activated to penciclovir which is then phosphorylated to inhibit DNA polymerase
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10
Q

drugs that treat CMV infection

A

ganciclovir, foscarnet

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11
Q

ganciclovir: use, mechanism, side effect

A
  • CMV retinitis and prophylaxis
  • similar mechanism to acyclovir, nucleoside analog whose triphosphate form inhibits DNA synthesis and terminates DNA elongation
  • bone marrow suppression
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12
Q

antiviral drugs that have bone marrow suppression as side effect

A

GRZ (bone marrow suppression is a GRiZzly side effect): ganciclovir, zidovudine (AZT), and ribavirin

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13
Q

acyclovir-resistant herpes simplex

A

foscarnet

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14
Q

foscarnet: uses, mechanism, side effects

A
  • CMV, acyclovir-resistant herpes simplex
  • inhibits DNA polymerase, does not require conversion to triphosphate form to be active
  • side effects: renal damage, seizures (limits use)
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15
Q

drugs approved for hepatitis B and HIV

A

lamivudine and tenofovir

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16
Q

drugs used to treat hepatitis B

A

lamivudine, tenofovir, and alpha-interferons

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17
Q

mechanism of lamivudine and tenofovir when treating hepatitis B

A

inhibit reverse transcriptase domain of hepatitis B DNA polymerase

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18
Q

RSV infections (mostly children)

A

ribavirin

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19
Q

most effective treatment for hepatitis C

A

boceprevir + PEG-interferon-alpha + ribavirin

20
Q

RSV infections (mostly children) and hepatitis C

A

ribavirin

21
Q

ribavirin: uses, mechanism, side effect

A
  • RSV infection and hepatitis C
  • interferes with viral mRNA synthesis by inhibiting GMP/GTP synthesis and capping of viral mRNA
  • side effect: bone marrow suppression
22
Q

alpha interferons: uses

A

venereal warts, hepatitis B and C (used in combination with ribavirin and boceprevir for hepatitis C)

23
Q

boceprevir: use, mechanism

A
  • hepatitis C (in combination with ribavirin and PEG-interferon-alpha)
  • inhibits NS3 protease of hepatitis C, blocks formation of infectious virus
24
Q

zidovudine: what it is, mechanism, side effects

A
  • NRTI (nucleoside inhibitors of reverse transcriptase) for treatment of HIV
  • nucleoside analog that is phosphorylated –> inhibits reverse transcriptase –> acts as a DNA chain terminator
  • side effects: bone marrow suppression, lactic acidosis, hepatic steatosis
25
Q

tenofovir: what it is, uses, mechanism, side effects

A

-NRTI
-combination therapy for HIV; hepatitis B
-nucleoTide prodrug that competes for incorporation into DNA –> chain termination
side effects: lactic acidosis, hepatic steatosis

26
Q

lamivudine: what it is, uses, mechanism, side effects

A
  • NRTI
  • AZT-resistant HIV; hepatitis B
  • nucleoside analog inhibitor of reverse transcriptase
  • side effects: lactic acidosis, hepatic steatosis
27
Q

side effects common to NRTIs

A

lactic acidosis, hepatic steatosis

28
Q

lactic acidosis, hepatic steatosis

A

NRTIs: zidovudine, tenofovir, lamivudine, abacavir

29
Q

efavirenz: what it is, use, mechanism

A
  • NNRTI
  • part of multi-drug therapy for HIV
  • disrupts active site of reverse transcriptase
30
Q

lopinavir: use, mechanism, side effects

A
  • treats HIV in combination with reverse transcriptase inhibitors
  • protease inhibitor, so prevents viral aspartic protease from cleaving Gag-pol polypeptide into separate functional proteins
  • side effects: diabetes (elevated glucose), altered lipid metabolism (increased triglycerides and cholesterol)
31
Q

protease inhibitor

A

lopinavir

32
Q

used to boost levels of other HIV drugs by blocking their metabolism by CYP3A

A

ritonavir

33
Q

enfuvirtide: use, mechanism

A
  • for HIV-1 only (both CXCR4 and CCR5 strains)

- binds to gp41 subunit of HIV glycoprotein and blocks membrane fusion to CD4 T cells

34
Q

difference between enfurvitide and maraviroc

A

maraviroc has a narrow spectrum of use, only treats CCR5-tropic HIV-1

35
Q

maraviroc: use, mechanism, side effects

A
  • treatment of CCR5-tropic HIV-1
  • CCR5 co-receptor antagonist that blocks entry of HIV into cells
  • side effects: hepatotoxicity, cardiovascular events
36
Q

raltegravir: use, mechanism

A
  • treatment of HIV-1

- inhibits HIV-1 integrase, thereby preventing integration of HIV-1 DNA into the genome

37
Q

drugs used in treatment of HIV-1

A

enfurvitide, maraviroc (CCR5-tropic only), raltegravir

38
Q

integrase inhibitor

A

raltegravir

39
Q

treatment of only CCR5-tropic HIV-1

A

maraviroc

40
Q

when is it urgent to start HAART therapy?

A

CD4<350

41
Q

NNRTI

A

efavirenz

42
Q

zidovudine (AZT)-resistant HIV

A

lamivudine

43
Q

amantadine: use, mechanism

A
  • prophylaxis and therapy for influenza A ONLY

- blocks viral uncoating by interfering with M2 protein

44
Q

ritonavir: use

A

used to boost levels of other HIV drugs by blocking their metabolism by CYP3A

45
Q

NRTIs

A

zidovudine, tenofovir, lamivudine