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Pharmacology > Anti-Viral Agents > Flashcards

Anti-Viral Agents Flashcards

1
Q

Steps in Viral Replication

A 
Attachment
Entry
Uncoating
Synthesis
Assembly
Release
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2
Q

Prototype of antiviral agents that are phosphorylated intracellularly by a viral kinase that inhibits viral DNA synthesis

A

Acyclovir

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3
Q

MOA of Acyclovir

A

Converted into Acyclovir triphospate to inhibit viral DNA polymerase

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4
Q

Requirement for Acyclovir in its initial phosphorylation

A

Viral kinases

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5
Q

Compare the bioavailability of acyclovir and valacyclovir

A

Acyclovir is MORE bioavailable than valacyclovir

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6
Q

Drug used against herpes virus and does not have an effect on CMV

A

Acyclovir

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7
Q

Adverse effects of Acyclovir

A

Extrapyramidal signs and renal dysfunction secondary to crystalline nephropathy

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8
Q

Drugs that decrease Acyclovir clearance

A

Probenicid and Cemetidine

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9
Q

Compare the serum levels of acyclovir and valacyclovir

A

Valacyclovir > Acyclovir

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10
Q

CSF levels of acyclovir and valacyclovir

A

50%

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11
Q

Treatment of choice for postherpetic neuralgia used for suppression of frequently recurring genital herpes

A

Valacyclovir

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12
Q

Adverse effect of Valacyclovir

A

Seizures at high doses and thrombotic thrombocytopenic purpura

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13
Q

Acyclic guanine nucleoside analog fro Varicella and Genital Herpes

A

Penciclovir

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14
Q

Main clinical use for Famciclovir

A

HSV 1 and 2

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15
Q

Compare the triphosphate activity of Acyclovir and Penciclovir

A

Acyclovir > Penciclovir

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16
Q

Compare the intracellular concentration of Acyclovir and Penciclovir

A

Acyclovir < Penciclovir

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17
Q

Major difference of Famciclovir and Acyclovir

A

Famciclovir does not cause chain termination due to the presence of a 3-OH group

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18
Q

Most common side effects of topical drugs

A

burning sensation, itchiness, erythema

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19
Q

Most common side effects of oral drugs

A

Nausea, vomiting, diarrhea

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20
Q

Major adverse effects of Peniclovir and Famciclovir

A

Testicular toxicity on repeated doses but does not change sperms

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21
Q

MOA of Docosanol

A

Inhibits fusion between plasma membrane and the HSV envelope preventing viral entry

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22
Q

MOA of Trifluridine

A

Irreversible inhibition of thymidylate synthase and DNA synthesis inhibitor

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23
Q

Clinical significance of Trifluridine

A

Keratoconjunctivitis secondary to HSV 1 and 2

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24
Q

Anti-viral activity of Ganciclovir

A

Active against all herpesviruses but especially active against CMV

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25
Q

MOA of Ganciclovir

A

Inhibits viral DNA polymerase and causes chain termination

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26
Q

Clinical indication for Ganciclovir

A

CMV retinitis, CMV prophylaxis and CMV colitis

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27
Q

Adverse effect of Ganciclovir

A

Myelosuppression

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28
Q

Drugs that increase ganciclovir levels

A

Probenecid and Trimethoprim

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29
Q

Drug that increase in level with ganciclovir when used together

A

Didanosine

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30
Q

Clinical indication for ganciclovir

A

CMV retinitis and CMV prophylaxis in organ transplants

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31
Q

Iodinated thymidine analog that inhibits viral DNA synthesis at low concetration

A

Idoxuridine

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32
Q

Clinical indication of Idoxuridine

A

Herpes infections of the eyes but not for systemic viral infections

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33
Q

Clinical indication of Foscarnet

A

CMV retinitis and Acyclovir resistant HSV 2 and VZV in AIDS patient

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34
Q

Adverse effects of Foscarnet

A

Nephrotoxicity and penile ilcerations

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35
Q

MOA of Cidofovir

A

Potent inhibitor and alternative of viral DNA polymerase

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36
Q

Cidofovir is cross-resistant with:

A

Ganciclovir

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37
Q

Two active metabolites of Cidofovir

A

Cidofovir diphosphate

Cidofovir phosphocholine

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38
Q

It has a longer half-life between the 2 metabolites of cidofovir

A

Cidofovir phosphocholine

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39
Q

Cidofovir is administered with what drug to block active tubular secretion

A

Probenecid

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40
Q

Adverse effect of Cidofovir

A

Nephrotoxicity and Fanconi’s anemia

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41
Q

MOA of Fomivirsen

A

Inhibits CMV replication through sequence-specific and non-specific mechanisms

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42
Q

Anti-viral activity of Rimantadine and Amantadine

A

3 antigenic subtypes of influenza A (H1N1, H2N2, H3N2) ONLY

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43
Q

Indication for use of amantadine and rimantadine

A

Prophylaxis and treatment of Influenza A2

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44
Q

Seizure effects of Amantadine and Rimantadine

A

Amantadine > Rimantadine

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45
Q

Adverse effects of Amantadine and Rimantadine

A

CNS toxicity due to Dopamine

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46
Q

MOA of Oseltamivir and Zanamivir

A

Inhibitor of Influenza A and B nueraminidase

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47
Q

Route of Administration of Oseltamivir and Zanamivir

A

Oseltamivir is ORAL and Zanamivir is INHALATIONAL

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48
Q

MOA of Adefovir Dipivoxil

A

Competitive inhibition of DNA polymerase causing chain termination of DNA synthesis

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49
Q

Metabolite of Adefovir and its effect

A

Pivalic acid - causes decrease in carnitine levels

50
Q

Therapeutic effect of Adefovir

A

For chronic HBV infections in decompensated liver disease

51
Q

Adverse effect of Adefovir

A

Nephrotoxicity; lactic acidosis and hepatic steatosis due to mitochondrial dysfunction

52
Q

Interferons produced by nearly all cells with its effects

A

Alpha and Beta IFN; anti-viral and anti-proliferative effect

53
Q

Interferon restricted to T-Lymphocytes and NK Cells with its effects

A

Gamma IFN; less anti-viral and more potent immunoregulatory effect

54
Q

MOA of interferon

A

Transcription, translation, protein processing, virus maturation inhibition

55
Q

Interferon for chronic hepatitis C

A

Interferon alpha 2a

56
Q

Interferon for chronic hepatitis B and C

A

Interferon alpha 2b

57
Q

Adverse effects of interferon

A

Myelosuppression, flu-like symptoms, alopecia, and abortifacient

58
Q

Drugs that cause hematologic toxicity with interferon

A

Zidovudine and Ribavirin

59
Q

Interferon has increased risk of hepatic failure with:

A

Didanosine

60
Q

Interferon has increased risk of BM suppression with:

A

Zidovudine

61
Q

Linear or branched PEG moiety attached to IFN used for chronic Hepatitis C

A

Pegylated interferon

62
Q

Pharmacokinetics of Lamivudine

A

Poor CSF penetration and freely crosses the placenta

63
Q

MOA of Ribavirin

A

Competitive inhibition of GTP-dependent 5’’ capping causing defective replication

64
Q

This drug stays for more than 6 months after administration lethal to pregnant women

65
Q

Adverse effect of Ribavirin

A

Systemic hemolytic anemia; contraindicated in pregnancy

66
Q

Clinical Indication of Palivizuumab

A

Prophylaxis for RSV

67
Q

This drug lacks direct anti-viral effect but induces cytokines and chemokines with anti-viral effects

68
Q

MOA of imiquimod

A

Induction of interferons

69
Q

Drug used as topical for condylomata cuminata and actinic keratosis

70
Q

Adverse effect of Imiquimod

A

Influenza-like syndrome

71
Q

MOA of immunoglobulins

A

Inhibits viral penetration, opsonize viral particles, activate complement, stimulate cell-mediated immunity

72
Q

Viral enzyme that synthesizes DNA using viral RNA as template

A

Reverse transcriptase

73
Q

Drugs with high chance of mutation

A

Abacavir
Lamivudine
Emtricitabine

74
Q

Targets of Anti-HIV drugs

A

Virus-cell fusion
Reverse transcription
Proteolytic processing

75
Q

First line agent drug for pregnant women to prevent vertical transmission of HIV

A

Zidovudine

76
Q

Fixed dose combinations used against HIV

A

Zidovudine and Lamivudine OR

Zidovudine and Lamivudine and Abacavir

77
Q

This drug increases Zidovudine’s level

78
Q

Drugs that increase Zidovudine’s level

A

Probenecid
Fluconazole
Atovaquone
Valproic acid

79
Q

Zidovudine is active against

A

HIV 1&2; HTLV 1&2

80
Q

Didanosine is active against

A

HIV 1&2, HTLV 1

81
Q

Adverse effects of Didanosine

A

Peripheral neuropathy and dose-dependent pancreatitis

82
Q

Drugs whose levels decrease when given with Didanosine

A

Ciprofloxacin
Ketoconazole
Itraconazole

83
Q

Drugs that increase didanosine levels

A

Allopurinol

Tenofovir

84
Q

Drugs that decrease didanosine levels

A

Methadone
Atanazavir
Delavirdine

85
Q

Stavudine is active against

86
Q

Adverse effects of Stavudine and Zalcitabine

A

Dose=related peripheral neuropathy, fat atrophy

87
Q

This drug has a more anti-retroviral activity in monocyte-macrophage cell lines

A

Zalcitabine

88
Q

Drugs which increase zalcitabine levels

A

Probenecid

Cimetidine

89
Q

Lamivudine and Tenofovir are active against

A

HIV 1&2; HBV

90
Q

This drug counteracts phosphorylation of Zalcitabine

A

Lamivudine

91
Q

Drugs for pregnant women

A

Lamivudine
Zidovudine
Atazanavir

92
Q

Adverse effect of Abacavir

A

Fatal hypersensitivity syndrome (fever, abdominal pain, GI complaints)

93
Q

Anti-HIV pre-exposure prophylaxis

A

Tenofovir and Emtricitabine

94
Q

Oral solution of this drug contains propylene glycol contraindicated in young children, women, and patients with renal and hepatic failure

A

Emtricitabine

95
Q

Adverse effect of Emtricitabine

A

Hyperpigmentation of skin

96
Q

Anti-viral activity of NNRTI

A

HIV 1 but not HIV 2 and no activity on DNA polymerases

97
Q

MOA of NNRTI

A

Inhibits viral reverse transcriptase and does not require phosphorylation

98
Q

Adverse effects of Nevirapine

A

Dose-limiting toxicity: rash on trunk, face and extremities (SPARES PALMS AND SOLES)

99
Q

NNRTI drug that has reduced efficacy with antacids, PPIs, and H2 blockers

A

Delavirdine

100
Q

Dihydrobenzoxazinone NNRTI

101
Q

Bisheteroarylpiperazine NNRTI

A

Delavirdine

102
Q

Dipyridodiazepinone NNRTI

A

Nevirapine

103
Q

Adverse effect of Efavirenz

A

CNS toxicity

104
Q

Adverse effect of Delavirdine

A

Skin rash (teratogenic)

105
Q

MOA of protease inhibitors

A

Prevent proteolytic cleavage of HIV polyproteins and prevents metamorphosis of HIV virus particles into its adult form

106
Q

Protease inhibitor with least potency to inhibit CYP3A4

A

Saquinavir

107
Q

Adverse effect of saquinavir

A

Prolonged QT interval

108
Q

Protease inhibitor with most potency to inhibit CYP3A4

109
Q

Adverse effect of Ritonavir

A

GI toxicity and dose-dependent hyperTG and hypercholesterolemia

110
Q

Adverse effect of indinavir

A

nephrolithiasis and HIV lipodystrophy syndrome

111
Q

Non-peptidic protease inhibitor

A

Nelfinavir

112
Q

Nelfinavir has increased dose when given with

113
Q

Only protease inhibitor with a sulfonamide moiety

A

Amprenavir

114
Q

Protease inhibitor with greatly increased water solubility and improved oral bioavailability

A

Fosamprenavir

115
Q

This drug is a weak CYP3A4 inhibitor but becomes strong with Ritonavir

116
Q

Azapeptide protease inhibitor contraindicated in patients with hepatic insufficiency and is recommended in pregnant patients

A

Atazanavir

117
Q

Relatively new protease inhibitor with increased risk of intracranial hemorrhage

A

Tipranavir

118
Q

The only available HIV entry inhibitor

A

Enfuvirtide

119
Q

Entry inhibitor accumulated in the cervicovaginal fluid

120
Q

Entry inhibitor accumulated in seminal fluid

121
Q

MOA of Enfuvirtide

A

Binds to gp41 subunit of glycoprotein preventing conformational changes for fusion of viral and cellular membranes

Pharmacology (4 decks)

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