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Pharmacology > Antivirals/HIV meds > Flashcards

Antivirals/HIV meds Flashcards

1
Q

This antiviral class prevents late protein synthesis and processing…

A

proteasae inhibitors (HIV)

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2
Q

These drugs prevent viral packaging, assembly and release from the cell

A

neuraminidase inhibitors (flu)

Prisoners who can’t leave their cell say: “Nerd, im in a daze!”

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3
Q

acyclovir, valacyclovir, and docosanol are active against __________

A

HSV/VZV

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4
Q

ganciclovir, valganciclovir, foscarnet, and cidofovir are active against both ________ and _________.

A

CMV and Herpes

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5
Q

ribavarin is the only drug active against what disease?

A

RSV

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6
Q

These three drugs work against influenza

A

oseltamivir, zanamivir, and baloxavir

Sell Tami, and Zane in Biloxi

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7
Q

these three drugs are active against HBV

A

tenofovir, entecavir and lamivudine

“TEL hep b to fuck off!”

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8
Q

These two drugs are active against HCV

A

sofosbuvir/ledipasvir

sofosbuvir/velpatasvir

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9
Q

What is the DOC for VZV?

A

acyclovir/valacyclovir

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10
Q

what is the mechanism by which acyclovir/valacyclovir achieves antiviral status?

A

inhibits DNA synthesis by competing with dGTP.

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11
Q

what type of analogue is acyclovir?

A

guanosine analogue

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12
Q

how does acyclovir receive its first phosphorylation within the cell?

A

using viral thymidine kinase

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13
Q

how is resistance to acyclovir achieved?

A

mutation of thiamine kinase preventing first phosphorylation

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14
Q

what makes valacyclovir attractive in place of acyclovir?

A

because it is a prodrug which is converted to acyclovir, it has a higher bioavailability

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15
Q

what are the adverse effects of acyclovir?

A

nephrotoxicity w/ high IV dose

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16
Q

is acyclovir safe for pregnant patients?

A

yes

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17
Q

This drug inhibits viral fusion to host cell membrane preventing the virus from entering the cell, and is active against HSV

A

docosanol

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18
Q

what is docosanol used for?

A

herpes simplex

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19
Q

what are common side effects for docosanol?

A

skin irritation, headache

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20
Q

these two drugs are guanosine analogues that are activated by viral kinases within the cell which inhibits DNA polymerase

A

ganciclovir/valganciclovir

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21
Q

what are the routes of admin for ganciclovir?

A

ocular implant, oral, IV

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22
Q

what are the routes of admin for valganciclovir?

A

PO only

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23
Q

_______ treats…

PO tx/prophylaxis of CMV/herpes in immuncompromised patients

Oral, IV, ocular implant for CMV retinitis

IV for life threatening CMV

A

ganciclovir

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24
Q

what are the adverse effects of ganciclovir?

A

myelosuppression

CNS: HA, confusion, seizures

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25
Q

what is the mechanism by which foscarnet achieves antiviral status?

A

directly inhibits DNA and RNA polymerase and reverse transcriptase

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26
Q

does foscarnet require phosphorylation to be activated?

A

no

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27
Q

what is the DOC for CMV encephalitis?

A

foscarnet + ganciclovir

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28
Q

what is the DOC for ganciclovir resistant CMV retinitis?

A

foscarnet

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29
Q

what is the DOC for acyclovir/ganciclovir resistant HSV?

A

foscarnet

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30
Q

describe the toxicity of foscarnet…

A

renal toxicity based on creatinine clearance.

hydration reduces toxicity significantly

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31
Q

who should be cautioned to use foscarnet?

A

renal insufficient patients

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32
Q

what is the mechanism of action fo cidofovir?

A

cytosine analogue that inhibits viral DNA polymerase

Cidofovir = cytosine

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33
Q

does cidofovir require viral enzymes for phosphorylation?

A

no, activity can therefore be maintained agasint kinase deficient CMV or HSV

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34
Q

This drug is given for:

IV for CMV retinitis in ganciclovir resistant CMV

IV/topical for acyclovir resistant HSV

A

cidofovir

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35
Q

describe the adverse effects of cidofovir

A

dose dependent nephrotoxicity avoidable by hydration

same SE as acyclovir!

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36
Q

what is the mechanism of action for oseltamivir and zanamivir?

A

both are neuraminidase inhibitors, which block the release of the virus from infected cells

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37
Q

what is the therapeutic use of oseltamivir and zanamivir?

A

used against influenza A and B

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38
Q

which anti-flu has been approved for bird flu?

A

oseltamavir

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39
Q

what is the route of admin for zanamavir?

A

nasal or oral inhaler approved for pts > 7 yo

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40
Q

This drug may worsen respiratory fxn in COPD, worsen bronchospasm in asthma.

Not recommended for those w/ airway disease.

A

zanamivir (inhaler, nasal spray)

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41
Q

oseltamivir has what adverse effects?

A

NV, better if taken w/ food

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42
Q

This antiviral prevents viral gene transcription by inhibiting endonuclease activity

A

baloxavir/marboxil

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43
Q

what is baloxavir marboxil approved for,

A

approved for influenza A and B

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44
Q

what are the adverse effects of baloxavir marboxil?

A

diarrhea, nausea and headache

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45
Q

This drug is a guanosine analogue that is phosphorylated by host enzymes to inhibit RNA polymerase, and is active against RSV

A

ribavirin

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46
Q

what is the primary use of ribavirin?

A

as an aerosol against RSV and in HCV PO combined w/ interferon

47
Q

When this drug is given PO dose dependent hemolytic anemia can occur

48
Q

When delivered as an aerosol, respiratory depression, cardiac arrest, hypotension can occur?

49
Q

what are the adverse effects when ribavirin is given IV?

A

psychiatric sxs

50
Q

describe the severity of ribavirin’s teratogenic effects…

A

must not conceive a child for at least 6 months after exposure to the drug.

occupational exposure is problematic as a result

51
Q

This drug is an adenosine analogue that inhibits HBV DNA polymerase

52
Q

This HBV drug is a guanosine analogue that inhibits HBV DNA polymerase

53
Q

what is the DOC for HBV?

54
Q

what is a rare adverse effect of entecavir?

A

hepatic encephalopathy

55
Q

what is the mechanism of action of lamivudine?

A

cytosine analogue that inhibits HBV DNA polymerase

56
Q

what is a rare side effect for lamivudine?

A

pancreatitis

57
Q

after more than 5 years of treatment with lamivudine, what can be expected?

A

resistance

58
Q

This drug is uridine analogue that inhibits viral NS5B RNA polymerase, causes termination of DNA

59
Q

This drug inhibits HCV NS5A protein to prevent phosphorylation and replication

A

ledipasvir/velpatasvir

60
Q

what is the DOC for HCV?

A

sofosbuvir/ledipasvir

or

sofosbuvir/velpatasvir

61
Q

what 2 NRTIs are DOC for HAART therapy in HIV?

A

emtricitabine and tenofovir

62
Q

What is a second acceptable NRTI duo to consider for the triple cocktail of HIV therapy?

A

lamivudine and abacavir

63
Q

what 5 drugs are considered nucleoside reverse transcriptase inhibitors?

A

zidovudine, emtricitabine, tenofovir, lamivudine, abacavir

64
Q

This class of drugs are nucleoside analogue requiring 3x phosphorylation to be incorporated into viral DNA to inhibit viral reverse transcriptase

65
Q

Which NRTIs are safe to use in pregnancy?

A

zidovudine, lamivudine

66
Q

which NRTI has good CNS penetration and can be useful for AIDS dementia?

A

zidovudine

67
Q

what is zidovudine commonly combined with?

A

lamivudine (prevent resistance)

68
Q

The major side effects of ______ include:

Initial: CNS- HA, NV, insomnia, myalgia

later: lactic acidosis, hepatotoxicity, myelosuppression

A

zidovudine

69
Q

This drug has the following precautions:

caution when using other drugs that cause myelosuppression like ganciclovir or ribavirin.

A

zidovudine

consider adding epogen or neupogen

70
Q

These two drugs treat HIV via inhibition of reverse transcriptaase?

A

tenofovir and emtricitabine

71
Q

what are two drugs of first choice when treating HIV?

A

tenofovir and emtricitabine in combo

72
Q

what is the mechanism of action for lamivudine in HIV and HBV

A

HIV inhibits reverse transcriptase, HBV inhibits polymerase

73
Q

describe the toxicity of lamivudine

A

very low toxicity

74
Q

is lamivudine safe in preganncy?

75
Q

what drugs are frequently combined with abacavir?

A

lamivudine or zidovudine

76
Q

This drug has the following serious toxicities.

serious hypersensitivity, SJS.

screen for HLA-B-5701

A

abacavir

“lose your BACK w/ abacavir. HLA B testing needed”

77
Q

what can happen if you discontinue abacavir therapy due to hypersensitivity and then restart the drug?

A

fatal consequences

78
Q

what are the two major, serious side effects of all NRTIs?

A

lactic acidosis and hepatotoxicity

79
Q

what is the mechanism of action for the NNRTIs?

A

bind directly to inhibit viral reverse transcriptase

80
Q

what are the 2 NNRTIs?

A

efavirenz and rilpivirine

81
Q

which of the NNRTIs is DOC for initial therapy?

82
Q

what should you combine efavirenz with?

A

nucleoside analogues

83
Q

what are two major cautions of efavirenz use?

A

CYP3A4 inducer which reduces effectiveness of OC

and

teratogenic

84
Q

which NNRTI do you use in pregnant patients?

A

rilpivirine

85
Q

This drug is not recommended for HIV pts w/ hepatitis because it can increase liver enzymes…

A

rilpivirine

86
Q

what is the common suffix of protease inhibitors and what is the one exception?

A

avir suffix, abacavir is the exception as an NRTI

87
Q

These drugs bind to proteases to inhibit function. prevents maturation of viral particles

A

protease inhibitors

88
Q

protease inhibitors must be combined with what class of HIV antiretroviral in order to prevent mutations/resistance?

89
Q

what metabolizes protease inhibitors?

90
Q

due to the metabolism by CYP3A4, protease inhibitors are often combined with what drug to decrease PI metabolism?

A

combined with ritonavir which is a potent inhibitor of 3A4

91
Q

what drugs will decrease PI levels?

A

3A4 inducers like rifampin, rifabutin, st. john’s wort

92
Q

what are the common adverse effects of protease inhibitors?

A

altered body fat distribution, insulin resistance, increased cholesterol, spontaneous bleeding w hemophilia

93
Q

ritonavir is used for what purpose?

A

inhibits CYP3A4 to increase bioavailability of protease inhibitors

94
Q

what drugs should not be combined with ritonavir?

A

saquinavir, metronidazole, cephalosporins, or isoniazid

95
Q

what shouldn’t ritonavir be given with saquinavir?

96
Q

why shouldn’t ritonavir be combined with metronidazole or cephalosporins?

A

disulfiram like reaction

97
Q

which protease inhibitor is DOC?

98
Q

Which two PIs contain sulfa and should be avoided in sulfa allergy?

A

darunavir, tipranavir

99
Q

which protease inhibitor is drug of second choice?

A

atazenavir

100
Q

what advantage does atazenavir have with respect to the adverse effects of other protease inhibitors?

A

less effect on body fat distribution

101
Q

This PI causes nephrolithiasis and hyperbilirubinemia mitigated by hydration

102
Q

why can’t you combine saquinavir with ritonavir?

A

QT prolongation

103
Q

what is unique about tipranavir?

A

it is a non-peptide PI

104
Q

This drug should be considered for treatment experienced HIV patients who have PI resistant strains

A

tipranavir

105
Q

what combination of tipranavir should be avoided for patients with head trauma?

A

tipranovir and ritonavir increases risk of intracranial hemorrhage

106
Q

This drug can cause liver toxicity, especially in HBV, HCV coinfection

A

tipranavir

107
Q

This drug binds to gp41 of the viral envelope, preventing fusion to the target cell

A

enfuvirtide

108
Q

The only parenteral antiretroviral

A

enfuvirtide

109
Q

what infection has an increased risk when taking enfuvirtide?

A

bacterial pneumonia

110
Q

This drug prevents viral fusion by binding to CCR5 receptor in CD4 T-Cells

111
Q

This drug can only be used for CCR5-trophic HIV for whom no other treatment has been effective

112
Q

What must be performed prior to administration of maraviroc?

A

testing to ensure CCR5-trophic infection. will not work on CXCR4 or mixed tropism

113
Q

This drug is an integrase inhibitor that blocks the integrase enzyme needed for viral replication

A

dolutegravir

“dolute the integrase!”

114
Q

when should you consider dolutegravir?

A

tx resistant patients where other drugs aren’t working

Pharmacology (6 decks)

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