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Pharmacology > Antivirals > Flashcards

Antivirals Flashcards

1
Q

Patients being treated for HIV should be on at least ______ drugs.

A

3

typically 2 NRTIs and a 3rd drug

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2
Q

What is the MOA of NRTIs (Nuceloside Reverse Transcriptase Inhibitors)?

A

Eliminates action of reverse transcriptase which inhibits the virus from transcribing RNA to DNA

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3
Q

What type of toxicity can NRTIs cause?

A

Mitochondrial

Off target inhibition of mitochondrial DNA polymerase

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4
Q

S/s of NRTIs mitochondrial toxcity:

A 
Peripheral neuropathy 
Lipodystrophy (lipoatrophy)
Lactic acidosis
Hepatic steatosis 
Pancreatitis
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5
Q

How are NRTIs eliminated?

A

Renally

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6
Q

Which NRTI should be used if a patient has renal dysfunction?

A

Abacavir

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7
Q

The NRTIs, Lamivudine and emtricitabine are very commonly used and have _____ toxicity risk.

A

Minimal

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8
Q

The NRTI, tenofovir, carries which type of toxicity risk?

A

Nephrotoxicity

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9
Q

The NRTI, abacavir, has which AE?

A

HSR (pts with HLA B-5701 allele are at greater risk)

Increased risk of MI

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10
Q

Zidovudine (AZT), one of the first NRTIs is still used in patients who have multiple _____ _____ and may cause ______.

A

drug resistance

anemia, neutropenia (d/t BM suppression)

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11
Q

What is the largest concern with patients on NNRTIs (Non-nucleotide Reverse Transcriptase Inhibitors)?

A

DI

CYP450 substrates and induce CYP3A4

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12
Q

SE of NNRTIs include:

A

rash, increased transaminases

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13
Q

What is concern is associated with the long half lives of NNRTIs like Efavirenz?

A

Patients will typically be on two NRTIs and an NNRTI, if regimen is stopped, the NRTIs will exit the body faster than the NNRTI which could have a half life up to 3 weeks. Having only the NNRTI in the body can lead to drug resistance by the virus

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14
Q

AE of the NNRTI Efavirenz include:

A

Teratogenic in 1st trimester
CNS SE
False positive cannabinoid and benzo tests

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15
Q

AE of NNRTI Nevirapine:

A

Hepatotoxicity secondary to HSR

Stevens-Johnson syndrome

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16
Q

AE of the NNRTI Etravirine:

A

2nd gen

Induces CYP3A4, inhibits 2C9(incr warfarin levels) and 2C19 (prevents activation of plavix)

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17
Q

What is the pharmokinetic enhancement of drug levels called?

A

Boosting

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18
Q

Protease inhibitors: lopinavir, saquinavir, darunavir, and tipranavir are always _______
Nelfinavir is _____ ______.

A

boosted

never boosted

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19
Q

How does the PI Ritonavir work to boost other PI’s?

A

Ritonavir is a potent inhibitor of CYP3A4, PI’s are substrates of CYP3A4. By inhibiting CYP3A4 this increases the bioavailability of PIs, decreases elimination of PIs, and results in increased efficacy, and/or a longer dosing interval
(Rotanavir has effect on HIV replication, was used at higher doses to treat HIV in the ‘90’s)

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20
Q

Common DI associated with Ritonavir:

A 
CYP3A4 substrates (increase levels of those drugs also)
Inhibits CYP2D6
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21
Q

Protease Inhibitors DI’s are related to:

A

Substrates of CYP3A4

Inhibitors of CYP3A4

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22
Q

SE of PI use:

A

Dyslipidemia
Increased glucose
GI intolerance

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23
Q

Which drugs are CI for patients using PI’s?

A 
Midazolam, triazolam
Rifampin (potent inducer of 3A4=cancel out effect of ritonavir)
Simvastatin, lovastatin 
Fluticasone
St. John's Wort
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24
Q

The PI Atazanavir should not be used with:

A

acid suppressing agents. Atazanavir needs acidic environment to be absorbed

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25
Q

Which drugs required dose adjustments in patients using PI’s?

A 
Rifabutin 
Clarithromycin 
Atorvastatin 
Oral contraceptives 
Voriconazole, ketoconazole
Sildenafil, vardenafil, tadalafil 
Anticonvulsants
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26
Q

Which PK enhancer/booster works by inhibiting CYP3A4 but has no effect of HIV replication?

A

Cobicistat

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27
Q

While ritonavir has mainly lipid and GI concerns what potential AE dose cobicistat have?

A

Renal AEs

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28
Q

How do the Integrase Inhibitors Raltegravir and Elvitegravir differ?

A

Raltegravir is metabolized by the glucoronidation pathway so is not renally eliminated and not metabolized by CYP3A4.
Elvitegravir is metabolized by 3A4 and usually boosted by Cobicistat

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29
Q

Which type of HIV meds are given to patients who do not have other options?

A

Fusion inhibitors

CCR5 Inhibitors

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30
Q

How does the fusion inhibitor Enfuviritide work, how is it administered, AE, metabolism?

A

Binds to the gp41 rc to prevent fusion
Injection
AE: injection site reactions
Metabolized via non-CYP450 pathways

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31
Q

What is the MOA and what is different about the CCR5 Inhibitor, Maraviroc?

A

MOA: CCR5 antagonist at the rc on the surface of CD4 cells inhibiting fusion
It is the only drug that has a target of the human cell vs. viral target

32
Q

Which drugs inhibit mature HIV cells?

A

Protease Inhibitors

33
Q

Which drugs inhibit integration in human DNA?

A

Integrase inhibitors

34
Q

Which drugs prevent formation of HIV DNA?

A

NRTIs, NNRTIs

35
Q

Which drugs inhibit fusion of the virus to the host cell?

A

Fusion inhibitors and CCR5 antagonists

36
Q

Herpes viruses are what kinds of viruses?

A

DNA

37
Q

Why is valacyclovir given and what is it converted into?

A

Valacyclovir is a prodrug for acyclovir. It is given because it is more lipophillic, has better bioavailability, and is better absorbed orally.

38
Q

Why is famciclovir given and what is it converted into?

A

Famciclovir is a prodrug for penciclovir. It is more lipophillic and better absorbed orally. Penciclovir is only available topically.

39
Q

What is the MOA of acyclovir and penciclovir?

A

These drugs are selectively activated by HSV and VZV enzymes, thymidine kinase. The drugs are triphosphorylated by the virus, these triphosphorylated metabolites selectively inhibit DNA synthesis halting the viral replication

40
Q

Why is HSV easier to treat?

A

The thymidine kinase produced by HSV when exposed to acyclovir or penciclovir is more efficient

41
Q

How does docosonol work?

A

(Abreva) Prevents fusion of HSV to plasma membranes

42
Q

When do all drugs for the treatment of HSV and VZV work best?

A

Before manifestation of lesions occur. Once lesions occur, drugs do not heal what has already manifested but prevent further lesions

43
Q

What drugs are used topically for herpes labialis?

A

Penciclovir/docosonal

44
Q

What drug is used in the treatment of HSV encephalitis and herpes zoster in immunocompromised patients?

A

IV acyclovir

45
Q

AE of docosonal include:

A

Burning/stinging sensation

46
Q

AE of systemic HSV, VSV agents:

A

GI disturbances
HA
Rash (acyclovir/valcyclovir)
Fatigue (Famciclovir)

47
Q

What DI can occur with acyclovir and penciclovir?

A

Probenecid blocks renal secretion of these drugs

48
Q

What can cause drug resistance in acyclovir/pencyclovir?

A

Thymidine kinase deficiency (virus no longer producing this)
Thymidine kinase mutants (virus producing faulty form)
=drug can no longer be activated

More common in immunocompromised patients
Suspect resistance if patients show poor clinical response to drugs

49
Q

Treatment of CMV includes what antibiotics?

A

Ganciclovir
Valganciclovir
Cidofivir
Foscarnet

50
Q

Cidovir and Foscarnet can also be used to treat what?

A

Acyclovir-resistant HSV

51
Q

What is the prodrug for ganciclovir?

A

Valganciclovir

52
Q

MOA of ganciclovir:

A

Once triphosphorylated to its active form, it inhibits viral DNA synthesis by inhibiting viral DNA polymerase

53
Q

AE of ganciclovir:

A

**Anemia, neutropenia, thrombocytopenia

GI disturbances

54
Q

Ganciclovir does have HSV activity but has cross-resistance with _______.

A

acyclovir

55
Q

MOA of Cidofivir:

A

Inhibits viral DNA synthesis by inhibiting DNA polymerase

56
Q

MOA of Foscarnet:

A

Inhibits DNA polymerase and reverse transcriptase

57
Q

Why are Cidofivir and Foscarnet active against acyclovir resistant HSV?

A

Their activation is not dependent on thymidine kinase

58
Q

One common adverse effect for both Cidofivir and Foscarnet is:

A

Nephrotoxicity

59
Q

Fever, N/V/D, anemia can also be associated with which drug used in the treatment of CMV and acyclovir-resistant HSV?

A

Foscarnet

60
Q

What DI is present with Cidofivir?

A

Probenecid blocks renal secretion

61
Q

Indications for use of Ribavirin: (3)

A
  1. Symptomatic relief in young children with influenze A and B
  2. RSV pneumonia (inhalation)
  3. Chronic Hep C inf (most common)
62
Q

MOA of Ribavirin:

A

Inhibits viral-specific RNA synthesis

Inhibits formation of viral proteins/enzymes necessary for replication

63
Q

AE of Ribavirin:

A
  • Serious: cardiac arrest, apnea, bacterial pneumonia, pulmonary deterioration
  • **Anemia, neutropenia, thrombocytopenia (may require Epo)
  • Rash, conjunctivitis
64
Q

What should female patients be counseled about regarding ribavirin?

A

Category X: teratogenic

Use 2 forms of birth control during and for 6mos after discontinuation of treatment

65
Q

In what patients is inhaled ribavirin contraindicated?

A

Vented patients

66
Q

How is PO ribavirin eliminated?

A

Renally

67
Q

Adamantanes: Amantadine and Rimantidine were at one time used for the prophylaxis and treatment of influenza ____. Why are they not used often?

A

A

CDC advises against use d/t resistance

68
Q

What is the MOA of Adamantanes?

A

Interference with viral attachment and uncoating

69
Q

What other disease can Amantadine be effective against and why?

A

Parkinson’s
Causes the release of dopamine
(AE: ataxia, nightmares, insomnia)

70
Q

Neuraminidase Inhibitors, the most commonly used antivirals to treat influenza, include:

A

Oseltamivir (Tamiflu)

Zanamivir (Relenza)

71
Q

Oseltamivir(Tamiflu) and Zanamivir (Relenza) are effective against:

A

Influenza A and B, pandemic H1N1, H5N1 (avian influenza)

Treatment and prophylaxis

72
Q

MOA of neuraminidase inhibitors:

A

Inhibits neuraminidase, preventing budding from the host cell (halting reproduction)
Prevents spread of infection

73
Q

When should neuraminidase inhibitors be given?

A

First 48hrs of s/s to limit number of days with s/s

74
Q

Oseltamivir (Tamiflu): route of administration, AE, type of drug

A

PO
prodrug
AE: N/V, serious skin and hypersensitivity reactions, neuropsychiatric side effects

75
Q

Zanamavir (Relenza): Route of administration, AE

A

Oral inhalation

AE: Cough, bronchospasm in patients with asthma and COPD

76
Q

When is Peramivir (IV) given?

A

To patients in the ICU who cannot take oral or inhaled agents

Pharmacology (48 decks)

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