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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
\_\_\_\_\_\_\_ increases the clearance of zidovudine
Rifampin
26
Primary toxicity of zidovudine
Bone marrow suppresion
27
Drug interactions are a major problem of this drug because it is metabolzied by both CYP3A4 and CYP2D6
Delavirdine
28
Blood levels of Delavirdine are decreased by \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
anatacids, ddI, phenytoinm rifampin and nekfinavir
29
NNRTI than can be given once daily because of its long half life
Efavirenz
30
Approved for treatment-experienced HIV aptients and may be effective against HIV strains resistant to other drugs
Etavirine (a subsrate and an inducer of CYP3A4 and also inhibitss CYP2c9 and CYP2C19)
31
highly protein bound diarylpyrimidine with a long half life of 50h
Rilpivirine (Oral bioavailability dependent on acid gastic environment for optimal absorption)
32
All of the PI are substrates and inhibitors of \_\_\_\_\_\_\_\_\_\_\_
CYP3A4 (ritonavir having tje most pronounced effect)
33
This drug is used in combiantion with ritonavir in treatment experienced patients with resistance to other PIs
Darunavir
34
Contains sulfonamide moiety and should be used with caution in patients with sulfonamide allergy
Darunavir
35
Prodrug, forming amprenavir via its hydrolysis in the GI tract.
Fosaprenavir
36
This PI is characterized by inreased oral absorption in the presence of food, hepatic metabolism via CYP3A4 and short half life
Nelfinavir
37
is a synthetic 36 amino-acid peptide. The drug binds to the gp41 subunit of the viral envelope glycoprotein, preventing the conformational changes.
enfuvirtide
38
pyrimidine derivative that binds integrase an enzyme essential to replciation of both HIV1 and HIV2 inhibiting stand transfer
Raltegravir
39
Mechanism of amantadine and Rimantadine
Inhibit an early step in replication of the the influenza A (not B). They prevent incoating
40
\_\_\_\_\_\_\_\_\_of the core of influenza activates vira; RNA transcriptase
Acidification
41
inhibitors of neuraminidase produced by influenza A and B
Oseltamivir and Zanamivir
42
\_\_\_\_\_supresses HBV replication and improves liver histology and fibrosis
Adefovir
43
Inhibits HBV DNA polymerase. Effective orally, the drug undergoes renal elimination in part via active tubular secretion/
Entecavir
44
nucleoside inhibitor of HIV transceiptase that is active in chronic HBV infection
Lamivudine
45
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
Ribavirin
46
potent, pangenotypic protease inhibitor reversibly binding HCV NS3/4A protease
Grazoprevir
47
Increaed activity of host cell ribonucleases that degrade viral mRNA is one of the actions of \_\_\_\_\_\_\_\_\_\_\_
Interfere alpha
48
If a patient develops pancreatitis from didanosine, what drug is an aceptable substitute?
Lamivudine
49
associated with PR interval prolongation
Atazanavir
50
Prophylaxis for accidental needle prick
Treat with zidovudine plus lamivudine plus ritonavir for 4 weeks
51
A 27 year old nursing mother is diagnsoed with genital herpes. What drug ro be used orally is most likely to be prescribed
Valacyclovir
52
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,
Emtricitabine
53
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
Acyclovir
54
Antiherpes drugs (Acyclovir, valacyclovir, penciclovir, famciclovir)
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, F**amciclovir and valacyclovir**: oral Oral forms cause nauea, diarrhea, and headache. IV acyvlovir may cause renal and CNS toxicity
55
Drugs for CMV (Ganciclovir, Valganciclovir, cidofovir, foscarnet)
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
Antihepatitis Drugs * IFN-a * Adefocir-dipivoxil * entecavir * Lamivudine * talbivudine * ribavarin * sofosbuvir
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
NS5A inhibitors
* daclatasvir * elbasvir * ledipasvir * ombitasvir * velpatasvir
58
NS5B RNA pol inhibitors
Dasabuvir, sofosbuvir
59
NS3/4A protease inhibitors
* Grazoprevir * Paritaprevir * Telaprevir * Boceprevir * Simeprevir
60
Antiinfluenza drugs (Amantadine, Rimantadine, Oseltamivir, Zanamivir, Peramivir)
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
NRTIs
Abacavir, Didanosine, Emtricatabine, lamibudine, stavudine,tenofovir, zalcitabine,zidovudine
62
NNRTIs
Delavirdine Efavirenz Etravirine Nevaripainr Rilpivirine
63
Protease inhibitors
* Atazanavir * Darunavir * Fosamprenavir * Indinavir * Nelfinavir * Ritonavir * Saquinavir * Tipranavir
64
Entry inhibitors
Enfuviritide Mraviroc
65
Integrase inhibitors
Dolutegravir, elvitegravir, raltegravir

I hate DRUGS!! (26 decks)

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