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STEP 1 > Antivirals/HIV drugs > Flashcards

Antivirals/HIV drugs Flashcards

1
Q

Mechanism of oseltamivir/zanamivir

A

inhibits influenza neuraminidase –> decreased release of progeny virions

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2
Q

Use of oseltamivir/zanamivir

A

treat and prevent both influenza A and B within 72 hrs

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3
Q

Mechanism of acyclovir, famciclovir, valacyclovir

A

guanosine analogs
monophosphorylated by HSV/VZV thymidine kinase and not phosphorylated in uninfected cells –> few adverse effects
triphosphate formed by cellular enzymes
preferentially inhibit viral DNA polymerase by chain termination

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4
Q

Use of acyclovir, famciclovir, valacyclovir

A

HSV - against mucocutaneous and genital lesions and encephalitis
VZV
weak against EBV

prophylaxis in immunocompromised patients
no effect on latent HSV or VZV

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5
Q

What do use for herpes zoster?

A

famciclovir

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6
Q

What is special about valacyclovir

A

prodrug of acyclovir and has better bioavailability

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7
Q

Toxicity of acyclovir, famciclovir, valacyclovir

A

obstructive crystalline nephropathy and acute renal failure if not adequately hydrated

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8
Q

Mechanism of resistance of acyclovir, famciclovir, valacyclovir

A

mutated viral thymidine kinase

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9
Q

Mechanism of ganciclovir

A

5’-monophosphate formed by a CMV viral kinase
guanosine analog
triphosphate formed by cellular kinase
preferentially inhibits viral DNA polymerase by chain termination

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10
Q

Use of ganciclovir

A

CMV, especially in immunocompromised pts

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11
Q

What is valganciclovir?

A

prodrug of ganciclovir with better oral bioavailability

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12
Q

Toxicity of ganciclovir

A

leukopenia, neutropenia, thrombocytopenia, renal toxicity

more toxic to host enzymes than acyclovir

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13
Q

Mechanism of resistance of ganciclovir

A

mutated viral kinase

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14
Q

Mechanism of foscarnet

A

viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor
binds to pyrophosphate-binding site on enzyme
NO activation required by viral kinase

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15
Q

Use of foscarnet

A

CMV retinitis in immunocompromised pts when ganciclovir fails
acyclovir-resistant HSV

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16
Q

Toxicity of foscarnet

A

nephrotoxicity, electrolyte abnormalities (hypo- or hypercalcemia, hypo- or hyperphosphatemia, hypokalemia, hypomagnesemia) can lead to seizures

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17
Q

Mechanism of resistance of foscarnet

A

mutated DNA polymerase

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18
Q

Mechanism of cidofovir

A

preferentially inhibits viral DNA polymerase

dose not require phosphorylation by viral kinase

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19
Q

Use of cidofovir

A

CMV retinitis in immunocompromised patients
acyclovir-resistant HSV
long half-life

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20
Q

Toxicity of cidofovir

A

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

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21
Q

What is the standard HART regimen?

A

2 NRTIs + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor

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22
Q

Name the protease inhibitors

A

“-navir”

atazanavir
darunavir
fosamprenavir
indinavir
lopinavir
ritonavir
saquinavir
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23
Q

Mechanism of protease inhibitors

A

assembly of virions depends on HIV-1 protease (pol genes), which cleaves the polypeptide produces of HIV mRNA into their functional parts
thus, protease inhibitors prevent maturation of new viruses

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24
Q

Ritonavir and p450

A

INHIBITS cyt p450

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25
Q

Toxicity of protease inhibitors

A

hyperglycemia
GI intolerance (nausea, diarrhea)
lipodystrophy
neuropathy, hematuria (indinavir)

26
Q

Rifampin and protease inhibitors

A

rifampin AMPs up the cyt p450 enzymes and thus can lower protease inhibitor concentrations

27
Q

Name the NRTIs

A 
abacavir
didanosine
emtricitabine
lamivudine
stavudine
tenofovir
zidovudine
28
Q

Mechanism of NRTIs

A

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

29
Q

Which of the NRTIs is nucleotides?

A

Tenofovir

30
Q

What do need to do to NRTIs that are nucleosides?

A

need to be phosphorylated to be active

31
Q

Use of zidovudine

A

general prophylaxis

PREGNANCY

32
Q

Toxicity of NRITs

A 
bone marrow suppression (give G-CSF and Epo)
peripheral neuropathy
lactic acidosis (nucleoside)
anemia (ZDV)
pancreatitis (didanosine)
33
Q

Name the NNRTIs

A

Delavirdine
Efavirenz
Nevirapine

34
Q

Mechanism of NNRTIs

A

bind to reverse transcriptase at site different from NRTIs

do NOT require phosphorylation to be active or compete with nucleotides

35
Q

Toxicity of NNRTIs

A

rash and hepatotoxicity are common to all

36
Q

Toxicity of efavirenz

A

rash and hepatotoxicty

vivid dreams and CNS symptoms

37
Q

Contraindication of efavirenz and delavirdine

A

do NOT use in pregnancy

38
Q

Name the integrase inhibitor

A

raltegravir

39
Q

Mechanism of integrase inhibitor

A

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

40
Q

Toxicity of integrase inhibitor

A

increased creatine kinase

41
Q

Mechanism of enfuvirtide

A

binds gp41, inhibiting viral entry

42
Q

Toxicity of enfuvirtide

A

skin reaction at injection site

43
Q

Mechanism of maraviroc

A

binds CCR5 on surface of T cells/monocytes inhibiting interaction with gp120

44
Q

Mechanism of interferons

A

glycoprotein normally synthesized by virus-infect cells

exhibits antiviral and antihumoral properties

45
Q

Use of interferon-alpha

A

chronic hepatitis B and C, Kaposi sarcoma, hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma

46
Q

Use of interferon-beta

A

multiple sclerosis

47
Q

Use of interferon-gamma

A

chronic granulomatous disease

48
Q

Toxicity of interferons

A

neutropenia, myopathy

49
Q

Drugs to treat hepatitis C

A

ribavirin, simeprevir, sofosbuvir

50
Q

Mechanism of ribavirin

A

inhibits synthesis of guanine nucleotides by competitely inhibiting inosine monophosphate dehydrogenase

51
Q

Use of ribavirin

A

chronic HCV, also RSV (palivizumab preferred in children)

52
Q

Toxicity of ribavirin

A

hemolytic anemia

severe teratogen

53
Q

Mechanism of simeprevir

A

HCV protease inhibitor

prevents viral replication

54
Q

Use of simeprevir

A

chronic HCV in combo with ribavirin and peginterferon alfa

55
Q

Can use simeprevir as monotherapy?

A

NO

56
Q

Toxicity of simeprevir

A

photosensitivity reactions, rash

57
Q

Mechanism of sofosbuvir

A

inhibits HCV RNA-dependent RNA polymerase acting as a chain terminator

58
Q

Use of sofosbuvir

A

chronic HCV in combo with ribavirin +/- peginterferon alfa

59
Q

Can you use sofosbuvir as monotherapy?

A

NO

60
Q

Toxicity of sofosbuvir

A

fatigue, headache, nausea

STEP 1 (26 decks)

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