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Flashcards in Antiviral Therapy Deck (63):
1

Zanamivir, oseltamivir mech

inhibit influenza neuraminidase : decrease the release of progeny virus

2

Zanamivir, oseltamivir clinical use

Treatment and prevention of both influenza A and B

3

Ribavirin Mech

Inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate DH

4

clinical use of Ribavirin

RSV, Chronic Hep C

5

Ribavirin toxicity/SE

Hemolytic anemia. Severe teratogen.

6

Acyclovir, famciclovir, valacyclovir mech

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

7

Acyclovir, famciclovir, valacyclovir clinical use

HSV and VZV; HSV-induced mucocutaneous and genital lesions as well as for encephalitis. Prophylaxis in immunocompromised patients. No effect on latent forms of HSV and VZV.

8

Acyclovir, famciclovir, valacyclovir have weak activity against what virus?

EBV

9

Acyclovir, famciclovir, valacyclovir has NO activity against what virus?

CMV

10

What is a prodrug of acyclovir? what is its advantage?

Valacyclovir; better bioavailability!

11

What is the treatment for herpes zoster?

Famciclovir! (I took this, wasn't a hug fam of zoster haha)

12

Acyclovir, famciclovir, valacyclovir Toxicity

Obstructive crystalline nephropathy and acute renal failure if not adequately hydreated

13

What is the mech of resistance to acyclovir, famciclovir, valacyclovir?

Mutate viral thymidine kinase

14

Ganciclovir mech

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

15

Ganciclovir Clinical use

CMV, especially in immunocompromised patients. Valganciclovir, a prodrug of ganciclovir, has better oral bioavailability

16

Ganciclovir Toxicity

Leukopenia, neutropenia, thrombocytopenia, renal toxicity. More toxic to host enzymes than acyclovir

17

What is the mech of resistance to Ganciclovir?

Mutated CMV DNA polymerase or lack of viral kinase

18

Foscarnet mech

Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase.

19

What is the mneumonic for foscarnet?

Foscarnet = pyrofosphate analog

20

Foscarnet (2) clinical uses?

1) CMV retinitis in immunocompromised patietns when ganciclovir FAILS; 2) acyclovir-resistant HSV

21

Foscarnet toxicity?

Nephrotoxicty

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What is the mech of resistance to Foscarnet?

Mutated DNA polymerase

23

Cidofovir mech

Preferentially inhibits viral DNA pol. Does not require phosphorylation by viral kinase.

24

What is the clinical use of Cidofovir?

CMV retinitis in immunocompromised patients; acyclovir-resistant HSV.

25

Does Cidofovir have a long or short half life?

long

26

When is HAART initiated?

when patients present with AIDS defining illness, low CD4 counts (

27

What is the HAART regimen?

2 nucleoside reverse transcriptase inhibitors (NRTIs) + 1 non-nucleoside reverse transcriptase inhibitor (NNRTI) OR 1 protease inhibitor or 1 integrase inhibitor

28

What are the Protease inhibitors? stating the suffix is good fucking enough

Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Ritonavir, Saquinavir

29

Mech of protease inhibitors

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

30

Which protease effects metabolism of other drugs? how?

Ritonavir can boost other drug concentrations by inhibiting CYP-450.

31

Navir tease a protease

haha

32

Protease inhibitor Toxicity

Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy. Nephropathy.

33

What protease can cause hematuria?

Indinavir

34

What are the Nucleoside Reverse transcription inhibitors?

Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine (ZDV, formerly AZT)

35

What is the mech of NRTIs?

Competively inhibit nucleotide binding to reverse transcriptae and terminate the DNA chain (lack a 3'OH group). The nucleosides need to be phosphorylated to be active

36

Which NRTI is actually a nucleotide?

Tenofovir

37

Which NRTI is used for general prophylaxis and during pregnancy to decrease the risk of fetal transmission?

ZDV

38

Toxicity of NRTI's

Bone marrow suppression (can be reversed with granulocyte colony-stimulating factor and erythropoietin, peripheral neuropathy, lactic acidosis (nucleosides), rash (non-nucleosides), anemia (ZDV), pancreatitis (didanosine).

39

NNRTIs

Efavirenz, Nevirapine, Delavirdine

40

Efavirenz, Nevirapine, Delavirdine mech

Bind to reverse transcriptae at site different from NRTIs. Do no require phosphorylation to be active or compete with nucleotides.

41

Efavirenz Nevirapine, Delavirdine SE/Toxicity profile

Rash and hepatotoxicty are common to all NNRTIs. Vivid dreams and CNS symptoms are common with efavirenz. Delavirdine and efavirenz are contraindicated in pregnancy

42

What is the integrase inhibitor?

Raltegravir

43

Raltegravir mech

Inhibits HIv genome integration into host cell chromosome by reversibly inhibiting HIV integrae

44

Raltegravir SE/toxicity

Hypercholestrolemia

45

What are the fusion inhibitors?

Enfuvirtide, Marviroc

46

Enfuvirtide mech

binds gp41, inhibiting viral entry

47

Maraviroc mech

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

48

Skin reaction at injection site is a SE of which drug?

Enfuvirtide

49

What are interferons?

Glycoproteins normally synthesize by virus-infected cells

50

What is the mech of interferons?

antivrial and antitumoral properties

51

IFN-alpha clinical usage?

Chronic Hep B & Hep C, Kaposi Sarcoma, Hairy cell leukemia, condyloma acuminatum, renal cell carcinoma, malignant melanoma

52

IFN-beta

multiple sclerosis

53

IFN-gamma

Chronic granulomatous disease

54

Interferon toxicity

Neutropenia, myopathy

55

Antibiotics to avoid in pregnancy + adverse effect?

The following are examples.....

56

Sulfonamides

Kernicterus

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Aminoglycosides

Ototoxicty

58

Fluoroquinolones

Cartilage damage

59

Clarithromycin

Embryotoxic

60

Tetracyclines

Discolored teeth, inhibition of bone growth

61

ribavirin

Teratogenic

62

Griseofulvin

Teratogenic

63

Chloramphenicol

Gray Baby