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PharmU6 > Antivirals > Flashcards

Antivirals Flashcards

1
Q

What is the mechanism of action of the nucleoside reverse transcriptase inhibitors (NRTI’s)?

A

Viral DNA chain termination via inhibition of reverse transcriptase enzyme

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2
Q

Name the NRTIs (Nucleoside reverse transcriptase inhibitors…

A 
Zidovudine
Lamivudine
Emtrictabine
Tenofovir
Abacavir
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3
Q

What are the side effects of tenofovir?

A

nephrotoxicity

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4
Q

What are the side effects of abacavir?

A

HSR

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5
Q

What are the side effects of Lamivudine/emtricitabine

A 
HA
N/V
Rash
Neutropenia
Pancreatitis
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6
Q

What are the side effects of zidovudine?

A

Anemia

Granulocytopenia

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7
Q

What is the major side effect of all NRTIs?

A

Lactic acidosis

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8
Q

Name the NNRTIs (Non-Nucleoside Reverse transcriptase inhibitors…

A

Efavirenz
Nevirapine
Rilpivirine
Etravirine

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9
Q

What are the NRTIs used for?

A

HIV

HBV–Lamivudine/Emtricitabine/Tenofovir

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10
Q

What is the mechanism of action of the NNRTIs (Non-Nucleoside Reverse transcriptase inhibitors?

A

Inhibit reverse transcriptase through direct enzyme inhibition

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11
Q

What are the common side effects of Efavirenze (NNRTI)?

A

CNS symptoms
Vivid dreams
Drowsiness
Teratogenic

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12
Q

What are the common side effects of Nevirapine (NNRTI)?

A

Rash

Hepatitis–including hepatic necrosis

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13
Q

What are the common side effects of Etravirine (NNRTI)?

A

Rash

Increased LFTs

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14
Q

What are the common side effects of Rilpivirine (NNRTI)?

A

Rash

QT prolongation

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15
Q

What are the NNRTIs used for?

A

HIV

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16
Q

Name the HIV protease inhibitors…

A 
Ritonavir
Fosamprenavir
Atazanavir
Darunavir
Lopinavir
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17
Q

What is the mechanism of action of the protease inhibitors?

A

Bind within active pocket of protease inhibiting binding of virus–without protease cleavage, virus cannot cause infection

Prevent cleavage of protein chain into functional subuntis

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18
Q

What is the primary use of Ritonavir

A

At low doses enhances blood levels of other PI’s when given together

P4503A4 inhibition in the liver and gut

Reduces frequency of dosing
Improves adherence/reduce ADRs
Improves ability to suppress strains of resistant virus
Improve regimen efficacy

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19
Q

What are the side effects of the protease inhibitors?

A

Metabolic toxicities

  • Dyslipidemia
  • Hyperglycemia
  • Lipodystrophy
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20
Q

What is the mechanism of action of enfuvirtide?

A

Peptide molecule that binds directly to the HR1 region of gp41–> Preventing viral cell entry

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21
Q

What are the HIV viral entry inhibitors?

A

Enfuvitide and Maraviroc

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22
Q

What are the side effects of Enfuvirtide?

A

Injection site reaction

23
Q

What is the mechanism of action of Maraviroc?

A

CCR5 Antagonist–HIV uses CCR5 as a co-receptor necessary to enter T-cells

24
Q

What are the side effects of Maraviroc?

A

Hepatotoxicity

25
Q

What is the mechanism of action of the integrase inhibitors?

A

Inhibit the viral enzyme integrase–which is necessary for insertion of viral DNA into human genomic DNA

26
Q

What are the 3 integrase inhibitors used to tx HIV?

A

Raltegravir
Elvitegravir
Dolutegravir

27
Q

What are the goals of HAART?

A

Suppression of viral load
Restoration of immune function–increase CD4 count
Improve quality of life
Reduce HIV-related morbidity and mortality
Minimize risk for antiretroviral resistance–Resistance only occurs during replication–so goal is to keep CD4 count up to prevent replication of virus

28
Q

What is the mechanism of action of Interferon?

A

Induce interferon-stimulating genes to establish antiviral state within cells

Used for HCV–old

29
Q

What are the side effects of interferon?

A

Flu-like symptoms
Cytopenias
Depression
Fatigue

30
Q

What is the mechanism of action of Ribavirin?

A

Nucleoside analog–competes with viral nucleotides and cause chain termination

Used fro HCV–old

31
Q

What are the side effects of Ribavirin?

A

Hemolytic anemia–very high risk!!

Tetratogenic

32
Q

Name the NS5B polymerase inhibitors?

A

Sofosbuvir

Paritaprevir

33
Q

What is the mechanism of action of the NS5B inhibitors used for HCV?

A

Compete with viral nucleotide to cause viral chain termination of HCV RNA

Inhibitor of HCV NS5B RNA-dependent RNA polymerase–once phosphorylated, competes with natural viral nucleotide (uridine) to cause chain termination of HCV RNA

34
Q

Name the HCV NS5A inhibitors…

A

Ledipasvir
Daclatasvir
Ombitasvir

35
Q

What is the mechanism of action of the HCV NS5A inhibitors?

A

Inhibit the viral phosphoprotein, NS5A, that is required for viral replication

36
Q

Name the NS3/4A protease inhibitors…

A

Simeprevir
Bocepravir
Telapravir

37
Q

What is the mechanism of action of the NS3/4A protease inhibitors?

A

Prevent viral maturation through the inhibition of protein synthesis

38
Q

Why are acyclovir and penciclovir only phosphorylated/active within infected cells?

A

Because phosphorylation requires viral thymidine kinase

39
Q

What antiviral is used for the treatment and prophylaxis of CMV infection?

A

Ganciclovir

40
Q

What is the mechanism of action of Ganciclovir?

A

After phosphorylation in infected cell–causes viral DNA chain termination

41
Q

What is the mechanism of action of acyclovir?

A

After phosphorylation by cellular enzymes–acyclovir triphosphate competes with DNA analogues to cause viral DNA chain termination

42
Q

What is acyclovir used for?

A

HSV and VZV

43
Q

What is a prodrug of acyclovir?

A

Valacyclovir–converted to acyclovir after oral administration

44
Q

Why is penciclovir given topically?

A

Very poor bioavailability

MOA–similar to acyclovir

45
Q

What is a prodrug for penciclovir?

A

Famciclovir–administered orally

46
Q

What are the side effects of acyclovir and penciclovir?

A

CNS changes and renal dysfunction possible when used at higher doses

47
Q

What are the side effects of ganciclovir?

A

Neutropenia and thrombocytopenia

48
Q

What antiviral is a pyrophosphate congener and is broad spectrum–used for HSV/VZV/CMV and HIV?

A

Foscarnet–used when resistance occurs with others

49
Q

What is the mechanism of action of Foscarnet?

A

Directly inhibits herpesvirus DNA polymerase or HIV reverse transcriptase

50
Q

What are the side effects of Foscarnet?

A

Nephrotoxicity–1/3 of pts
Electrolyte/metabolic abnormalities
CNS side effects–tremor, irritability, seizures, hallucinosis
Myelosuppression

51
Q

What is the mechanism of action of Oseltamivir, Zanamivir, and Peramivir?

A

Inhibit viral neuraminidase–an enzyme critical in penetration of respiratory tract mucus and in the release of virus from infected cells –prevent viral release from host cells

Active against both influenza A and B

52
Q

What are the side effects seen with the neuraminidase inhibitors used to tx the flu–Oseltamivir, Zanamivir, and Peramivir?

A

Neuropsychiatric toxicity
GI side effets
Bronchospasm with zanamivir

53
Q

Which neuraminidase inhibitor should not be used if a pt has asthma?

A

Zanamivir–inhaled therapy and can cause bronchospasm

54
Q

Which neuraminidase inhibitor is reserved for therapy among critically ill pts?

A

Peramivir

PharmU6 (7 decks)

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