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step 1 microbiology > antivirals > Flashcards

antivirals Flashcards

1
Q

HIV fusion inhibition

A

attachment: maravirocpenetration: enfuvirtide

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2
Q

HIV inTEGRAse inhibition

A

doluTEGRAvir, elviTEGRAvir, ralTEGRAvir

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3
Q

HIV protease inhibition

A

atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, ritonavir, saquinavir

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4
Q

HIV reverse transcriptase inhibition

A

NRTIS, NNRTI

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5
Q

NRTIs

A

abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine

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6
Q

NNRTIs

A

delaviridine, efavirenz, nevirapine

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7
Q

HBV, HCV protein synthesis inhibition

A

INF-a (binds via PKR)

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8
Q

uncoating (influenza)

A

amantadine, rimantadine(no longer used, high resistance)

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9
Q

Guanosine analogs

A

acyclovir (HSV, VZV)Ganciclovir (CMV)

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10
Q

viral DNA polymerase inhibitors

A

cidofovir (HSV)foscarnet (CMV)

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11
Q

guanine nucleoside synthesis inhibitor

A

ribavirin (RSV, HCV)

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12
Q

release of progeny inhibitors

A

neuraminidase inhibitors (Oseltamivir, Zanamivir) in flu A,B

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13
Q

Ganciclovir MOA

A

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

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14
Q

Ganciclovir use

A

CMV, esp. in IC pts.

Valganciclovir, prodrug of ganciclovir, has better oral bioavailability

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15
Q

Ganciclovir ADR

A

bone marrow suppression (leukopenia, neutropenia, thrombocytopenia); renal toxicity

more toxic to host than acyclovir

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16
Q

Ganciclovir resistance

A

mutated viral kinase

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17
Q

Foscarnet MOA

A

Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor.

Binds to pyrophosphate-binding site of enzyme.

*Does not require any kinase activation

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18
Q

Foscarnet use

A

CMV retinitis in IC patients when ganciclovir fails; acyclovir-resistant HSV

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19
Q

Foscarnet ADR

A

nephrotoxicity, electrolyte abnormalities lead to seizures

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20
Q

Foscarnet Mech of resistance

A

mutated DNA polymerase

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21
Q

Cidofovir MOA

A

preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinase

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22
Q

Cidofovir use

A

CMV retinitis in IC patients;

acyclovir-resistant HSV.

Long-half life

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23
Q

Cidofovir ADR

A

nephrotoxicity (coadmin w/ probenecid and IV saline to dec)

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24
Q

HIV triple therapy

A

2 NRTIs and preferably an integrase inhibitor

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25
Q

NRTIs MOA (HIV)

A

competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group)

26
Q

NRTI make-up

A 
nucleoSides that need to be phosphorylated to be active
 except Tenofovir (nucleoTide)
27
Q

Zidovudine (ZDV) use

A

general prophylaxis and during pregnancy to dec risk of fetal transmission

28
Q

NRTI toxicity

A

bone marrow suppression, peripheral neuropathy

29
Q

NRTI bone marrow suppression TX

A

granulocyte colony-stimulating factor and EPO

30
Q

NRTI nucleoside ADR

A

lactic acidosis

31
Q

ZDV ADR

32
Q

didanosine ADR

A

pancreatitis

33
Q

Abacavir contraindication

A

pt has HLA-B*5701 mutation

34
Q

NNRTIs MOA (HIV)

A

bind to reverse transcriptase at site different from NRTIs. Do not require phosphorylation to be active or compete with nucleotides

35
Q

NNRTI ADR

A

rash and hepatotoxicity

36
Q

NNRTIs contraindicated in pregnancy

A

delavirdine and efavirenz

37
Q

Efavirenz ADR

A

vivid dreams and CNS sx

38
Q

Protease Inhibitors (-navir) MOA (HIV)

A

assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into their functional parts. *thus protease inhibitors prevent maturation of new viruses

39
Q

Ritonavir use

A

“boosts” other drug concentrations by inhibiting p450

40
Q

Protease inhibitor ADR

A

hyperglycemia, GI intolerance, lipodystrophy (Cushing-like syndrome)

41
Q

Indinavir ADR

A

nephropathy, hematuria

42
Q

what drug should never be used with protease inhibitors?

A

Rifampin (potent CYP/UGT inducer) bc it decreases protease inhibitor concentration

43
Q

integrase inhibitors MOA

A

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

44
Q

integrase inhibitors ADR

A

inc. creatine kinase

45
Q

Enfuvirtide MOA

A

fusion inhibitor

binds gp41, inhibiting viral entry

46
Q

Enfuvirtide ADR

A

skin rxn at injection site

47
Q

Maraviroc MOA

A

binds CCR-5 on surface of T cells/monocytes, inhibiting interaction with gp120

48
Q

Interferons MOA

A

glycoproteins norm synthesized by virus-infected cells, exhibiting wide range of antiviral and antitumoral properties

49
Q

INF-a use

A

chronic HBV and HCV; Kaposi sarcoma; hairy cell leukemia; condyloma acuminatum; renal cell carcinoma; malignant melanoma

50
Q

INF-b use

A

multiple sclerosis

51
Q

INF-y use

A

chronic granulomatous disease

52
Q

interferons ADR

A

flu-like symptoms, depression, neutropenia, myopathy

53
Q

Ribavirin (HCV) MOA

A

inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase

54
Q

Ribavirin use

A

chronic HCV, RSV

55
Q

Ribavirin ADR

A

hemolytic anemia, severe teratogen

56
Q

RSV tx in kids

A

palivizumab

57
Q

Sofosbuvir MOA

A

inhibits HCV RNA-dependent RNA polymerase acting asa chain terminator

58
Q

Sofosbuvir use

A

chronic HCV in combo w/ ribavirin

don’t use as monotherapy

59
Q

Sofosbuvir ADR

A

fatigue, HA, nausea

60
Q

Simeprevir MOA

A

HCV protease inhibitor; prevents viral replication

61
Q

Simeprevir use

A

chronic HCV in combo w/ ledipasvir (NS5A inhibitor)

don’t use as monotherapy

62
Q

Simeprevir ADR

A

photosensitivity rxns, rash

step 1 microbiology (7 decks)

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