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I hate DRUGS!! > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

1
Q

Guanosine analog active against HSV 1 and 2 and Varicella zoster virus

Activated initially by the viral kinase

A

Acyclovir

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2
Q

Acyclovir is actiavted intially activated by the viral kinase to form_________

A

Acyclovir triphosphate

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3
Q

2 ways acyclovir interferes with viral synthesis

A
  • Competitive substrate for DNA polymerase
  • Chain termination after its incorporation into vital DNA
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4
Q

prodrug convertd to acyclovir by heaptic metabolism after oral adminsitration and reaches plasma levels 3-5 times greater than those achieved acyclovir

A

Valacyclovir

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5
Q

Undergoes activation by viral thymidine kinase and the triphostphate form inhibits DNA polymerase BUT does not cause chain termiantion

A

Penciclovir

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6
Q

prodrug converted to penciclovir by first pass metabolism in the liver

A

Famciclovir

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7
Q

alipathic alcohol that inhibits fusion between the HSV envelope and plasma membranes.

A

Docosanol

  • Prevents viral entry and subsequent replication.
  • Topically, shortens healing time
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8
Q

guanine derivative, triphosphorylated to form a nucleotide that inhibits DNA polymerases of CMV and HSV and cause chain termination

A

Ganciclovir

  • An intraocular implant form of ganciclovir can be used in CMV retinitis
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9
Q

Prodrug of ganciclovir, has high bioavailabity

A

Valganciclovir

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10
Q

phosphonate and is activated exclusively by host cell kinases. The active diphosphonate inhibits DNA polymerase of HSV, CMV and adenovirus and HPV,

A

Cidofovir

  • Effective against CMV retinitis in mucocutaneous HSV
  • Nephrotoxicity is the major dose limiting toxicity
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11
Q

phosphonoformate derivative that does not require phosphorylation for antiviral activity. Not an antimetabolite, inhibits RNA polymerase, DNA polymerase, and HIV reverse transcriptase

A

Foscarnet

  • penetrates well into tissue, including CNS
  • inhibits herpese DNA polymerase in acyclovir resistant strains that are thymidine kinase deficient
  • Nephrotoxic
    • hypocalcemia
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12
Q

adenine analog and has activity against HSV, VZV, and CMV. Used topically for herpes keratitis but has no effeect on genital lesions.

A

VIdarabine

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13
Q

Pyrimidine analogs used topically in HSV1. Too toxic for systemic use

A

Idoxuridine and trifluridine

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14
Q

antisense oligonucleotide that binds to mRNA of CMV, inhibiting early protein synthesis. THe drug is injected intravitreally for treatment of CMV retinitis

A

Fomivirsen

  • causes iritis, vitreatis, increased intraocular pressure and changes in vision
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15
Q

Prototype drug of Nucleoside reverse transcriptae inhibitors

A

Zidovudine

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16
Q

Prototype drug of nonnucleoside reverse transcriptase inhibitors

A

Delabirdine

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17
Q

Protoype drug for Protease inhibitors

A

Indinavir

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18
Q

Prototype of CCR-5 antagonist

A

Maraviroc

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19
Q

Prototype drug of fusion inhibitors

A

Enfuvirtide

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20
Q

Abacavir

A

Guanosine analog. Good oral bioavailability

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21
Q

Dose limiting effect of didanosine

A

Pancreatitis

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22
Q

Didanosine bioavailability is reduced by _________________

A

food and by chelating agents

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23
Q

Dose limiting effect of stavudine

A

Peripheral neuropathy

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24
Q

Nucleotide that acts like NRTIs to competitively inhibit reverse transcriptase

A

Tenofovir

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25
Q

_______ increases the clearance of zidovudine

A

Rifampin

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26
Q

Primary toxicity of zidovudine

A

Bone marrow suppresion

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27
Q

Drug interactions are a major problem of this drug because it is metabolzied by both CYP3A4 and CYP2D6

A

Delavirdine

28
Q

Blood levels of Delavirdine are decreased by ___________________

A

anatacids, ddI, phenytoinm rifampin and nekfinavir

29
Q

NNRTI than can be given once daily because of its long half life

A

Efavirenz

30
Q

Approved for treatment-experienced HIV aptients and may be effective against HIV strains resistant to other drugs

A

Etavirine

(a subsrate and an inducer of CYP3A4 and also inhibitss CYP2c9 and CYP2C19)

31
Q

highly protein bound diarylpyrimidine with a long half life of 50h

A

Rilpivirine

(Oral bioavailability dependent on acid gastic environment for optimal absorption)

32
Q

All of the PI are substrates and inhibitors of ___________

A

CYP3A4

(ritonavir having tje most pronounced effect)

33
Q

This drug is used in combiantion with ritonavir in treatment experienced patients with resistance to other PIs

A

Darunavir

34
Q

Contains sulfonamide moiety and should be used with caution in patients with sulfonamide allergy

A

Darunavir

35
Q

Prodrug, forming amprenavir via its hydrolysis in the GI tract.

A

Fosaprenavir

36
Q

This PI is characterized by inreased oral absorption in the presence of food, hepatic metabolism via CYP3A4 and short half life

A

Nelfinavir

37
Q

is a synthetic 36 amino-acid peptide. The drug binds to the gp41 subunit of the viral envelope glycoprotein, preventing the conformational changes.

A

enfuvirtide

38
Q

pyrimidine derivative that binds integrase an enzyme essential to replciation of both HIV1 and HIV2 inhibiting stand transfer

A

Raltegravir

39
Q

Mechanism of amantadine and Rimantadine

A

Inhibit an early step in replication of the the influenza A (not B). They prevent incoating

40
Q

_________of the core of influenza activates vira; RNA transcriptase

A

Acidification

41
Q

inhibitors of neuraminidase produced by influenza A and B

A

Oseltamivir and Zanamivir

42
Q

_____supresses HBV replication and improves liver histology and fibrosis

A

Adefovir

43
Q

Inhibits HBV DNA polymerase. Effective orally, the drug undergoes renal elimination in part via active tubular secretion/

A

Entecavir

44
Q

nucleoside inhibitor of HIV transceiptase that is active in chronic HBV infection

A

Lamivudine

45
Q

inhibits the replication of a wide range of DNA and RNA viruses, including influena A and B, parainfluenza, RSV, paramyxoviruses, HCV and HIV.

Drug inhibits guanosine triphosphate formation, prevents capping of viral mRNA

A

Ribavirin

46
Q

potent, pangenotypic protease inhibitor reversibly binding HCV NS3/4A protease

A

Grazoprevir

47
Q

Increaed activity of host cell ribonucleases that degrade viral mRNA is one of the actions of ___________

A

Interfere alpha

48
Q

If a patient develops pancreatitis from didanosine, what drug is an aceptable substitute?

A

Lamivudine

49
Q

associated with PR interval prolongation

A

Atazanavir

50
Q

Prophylaxis for accidental needle prick

A

Treat with zidovudine plus lamivudine plus ritonavir for 4 weeks

51
Q

A 27 year old nursing mother is diagnsoed with genital herpes. What drug ro be used orally is most likely to be prescribed

A

Valacyclovir

52
Q

Oral formulations of this drug should not be used in a pregnant AIDS patients because they contain propylene glycol, Once of the characterisitc adverse effects of the drug is hyperpigmentation of the palms of the hands and soles of the feet,

A

Emtricitabine

53
Q

more than 90% of this drug is excreted in the urine in tact form. Because its urinary solubility is low, aptients should be well hydrated to prevent nephrotoxicity

A

Acyclovir

54
Q

Antiherpes drugs

(Acyclovir, valacyclovir, penciclovir, famciclovir)

A

Activated by viral thymidine kinase (TK) to forms that inhibit viral DNA polymerase

Treatment and prophylaxis for HSV1,2 and VSV. None of these drugs is active agains TK strains

Acyclovir: topical , oral, IV. Penciclovir: topical, Famciclovir and valacyclovir: oral

Oral forms cause nauea, diarrhea, and headache. IV acyvlovir may cause renal and CNS toxicity

55
Q

Drugs for CMV

(Ganciclovir, Valganciclovir, cidofovir, foscarnet)

A

Viral activation of ganciclovir to form inhibitbiting DNA polymerase; no viral bioactivation of cidofovir and foscarnet

Treatment of CMV infections in immunosuppression and organ transplantation

Ganciclovir: oral, IV, intraocular forms. Valganciclovir: oral, Cidofovir, foscarnet: IV

Ganciclovir: BOne marrow suppression, hepatic and neurologic dysfunction. Cidofovir and foscarnet: nephrotoxic Foscarnet: CNS effects and electrolyte imbalance

56
Q

Antihepatitis Drugs

  • IFN-a
  • Adefocir-dipivoxil
  • entecavir
  • Lamivudine
  • talbivudine
  • ribavarin
  • sofosbuvir
A

Degrades viran RNA via actiavation of host cell RNAse (IFNa). Inhibition of HBV polymerase (others), Multiple antiviral actions (ribavarin)

Suppressive treatment of HBV (all drugs except ribavirin). Treatment of HCV (sofosbuvirm ribavarin +/- IFN a)

IFN-a: Parenteral. Adefovir, entercavir, lamivudine, sofosbuvir and ribavirin: oral. Ribavirin: inhalational

SE: IFN–a: alopecia, myalgia, depression, flu-like syndrome. Adefovir: Lactic acidosis, renal and heaptic toxicity. Ribavirin: anemia, teratogen

57
Q

NS5A inhibitors

A
  • daclatasvir
  • elbasvir
  • ledipasvir
  • ombitasvir
  • velpatasvir
58
Q

NS5B RNA pol inhibitors

A

Dasabuvir, sofosbuvir

59
Q

NS3/4A protease inhibitors

A
  • Grazoprevir
  • Paritaprevir
  • Telaprevir
  • Boceprevir
  • Simeprevir
60
Q

Antiinfluenza drugs

(Amantadine, Rimantadine, Oseltamivir, Zanamivir, Peramivir)

A

Amantadine and rimantadine: block of M2 proton channels. Oseltamivir and zanamivir inhibit neuraminidase

M2 blcoksers virtually obsolete. Others prophylaxis vs most current flu starins and shorten symptoms

Oral forms except zanamivir (inhalational)

SE: oseltamivir and peramivir: GI effects Delirum in patients with active influenza. ZanamivirL bronchospasm in asthmatics

61
Q

NRTIs

A

Abacavir, Didanosine, Emtricatabine, lamibudine, stavudine,tenofovir, zalcitabine,zidovudine

62
Q

NNRTIs

A

Delavirdine

Efavirenz

Etravirine

Nevaripainr

Rilpivirine

63
Q

Protease inhibitors

A
  • Atazanavir
  • Darunavir
  • Fosamprenavir
  • Indinavir
  • Nelfinavir
  • Ritonavir
  • Saquinavir
  • Tipranavir
64
Q

Entry inhibitors

A

Enfuviritide

Mraviroc

65
Q

Integrase inhibitors

A

Dolutegravir, elvitegravir, raltegravir

I hate DRUGS!! (26 decks)

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