Anti-Viral Agents Flashcards

(121 cards)

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
MOA of Ganciclovir
Inhibits viral DNA polymerase and causes chain termination
26
Clinical indication for Ganciclovir
CMV retinitis, CMV prophylaxis and CMV colitis
27
Adverse effect of Ganciclovir
Myelosuppression
28
Drugs that increase ganciclovir levels
Probenecid and Trimethoprim
29
Drug that increase in level with ganciclovir when used together
Didanosine
30
Clinical indication for ganciclovir
CMV retinitis and CMV prophylaxis in organ transplants
31
Iodinated thymidine analog that inhibits viral DNA synthesis at low concetration
Idoxuridine
32
Clinical indication of Idoxuridine
Herpes infections of the eyes but not for systemic viral infections
33
Clinical indication of Foscarnet
CMV retinitis and Acyclovir resistant HSV 2 and VZV in AIDS patient
34
Adverse effects of Foscarnet
Nephrotoxicity and penile ilcerations
35
MOA of Cidofovir
Potent inhibitor and alternative of viral DNA polymerase
36
Cidofovir is cross-resistant with:
Ganciclovir
37
Two active metabolites of Cidofovir
Cidofovir diphosphate | Cidofovir phosphocholine
38
It has a longer half-life between the 2 metabolites of cidofovir
Cidofovir phosphocholine
39
Cidofovir is administered with what drug to block active tubular secretion
Probenecid
40
Adverse effect of Cidofovir
Nephrotoxicity and Fanconi's anemia
41
MOA of Fomivirsen
Inhibits CMV replication through sequence-specific and non-specific mechanisms
42
Anti-viral activity of Rimantadine and Amantadine
3 antigenic subtypes of influenza A (H1N1, H2N2, H3N2) ONLY
43
Indication for use of amantadine and rimantadine
Prophylaxis and treatment of Influenza A2
44
Seizure effects of Amantadine and Rimantadine
Amantadine > Rimantadine
45
Adverse effects of Amantadine and Rimantadine
CNS toxicity due to Dopamine
46
MOA of Oseltamivir and Zanamivir
Inhibitor of Influenza A and B nueraminidase
47
Route of Administration of Oseltamivir and Zanamivir
Oseltamivir is ORAL and Zanamivir is INHALATIONAL
48
MOA of Adefovir Dipivoxil
Competitive inhibition of DNA polymerase causing chain termination of DNA synthesis
49
Metabolite of Adefovir and its effect
Pivalic acid - causes decrease in carnitine levels
50
Therapeutic effect of Adefovir
For chronic HBV infections in decompensated liver disease
51
Adverse effect of Adefovir
Nephrotoxicity; lactic acidosis and hepatic steatosis due to mitochondrial dysfunction
52
Interferons produced by nearly all cells with its effects
Alpha and Beta IFN; anti-viral and anti-proliferative effect
53
Interferon restricted to T-Lymphocytes and NK Cells with its effects
Gamma IFN; less anti-viral and more potent immunoregulatory effect
54
MOA of interferon
Transcription, translation, protein processing, virus maturation inhibition
55
Interferon for chronic hepatitis C
Interferon alpha 2a
56
Interferon for chronic hepatitis B and C
Interferon alpha 2b
57
Adverse effects of interferon
Myelosuppression, flu-like symptoms, alopecia, and abortifacient
58
Drugs that cause hematologic toxicity with interferon
Zidovudine and Ribavirin
59
Interferon has increased risk of hepatic failure with:
Didanosine
60
Interferon has increased risk of BM suppression with:
Zidovudine
61
Linear or branched PEG moiety attached to IFN used for chronic Hepatitis C
Pegylated interferon
62
Pharmacokinetics of Lamivudine
Poor CSF penetration and freely crosses the placenta
63
MOA of Ribavirin
Competitive inhibition of GTP-dependent 5'' capping causing defective replication
64
This drug stays for more than 6 months after administration lethal to pregnant women
Ribavirin
65
Adverse effect of Ribavirin
Systemic hemolytic anemia; contraindicated in pregnancy
66
Clinical Indication of Palivizuumab
Prophylaxis for RSV
67
This drug lacks direct anti-viral effect but induces cytokines and chemokines with anti-viral effects
Imiquimod
68
MOA of imiquimod
Induction of interferons
69
Drug used as topical for condylomata cuminata and actinic keratosis
Imiquimod
70
Adverse effect of Imiquimod
Influenza-like syndrome
71
MOA of immunoglobulins
Inhibits viral penetration, opsonize viral particles, activate complement, stimulate cell-mediated immunity
72
Viral enzyme that synthesizes DNA using viral RNA as template
Reverse transcriptase
73
Drugs with high chance of mutation
Abacavir Lamivudine Emtricitabine
74
Targets of Anti-HIV drugs
Virus-cell fusion Reverse transcription Proteolytic processing
75
First line agent drug for pregnant women to prevent vertical transmission of HIV
Zidovudine
76
Fixed dose combinations used against HIV
Zidovudine and Lamivudine OR | Zidovudine and Lamivudine and Abacavir
77
This drug increases Zidovudine's level
Phenytoin
78
Drugs that increase Zidovudine's level
Probenecid Fluconazole Atovaquone Valproic acid
79
Zidovudine is active against
HIV 1&2; HTLV 1&2
80
Didanosine is active against
HIV 1&2, HTLV 1
81
Adverse effects of Didanosine
Peripheral neuropathy and dose-dependent pancreatitis
82
Drugs whose levels decrease when given with Didanosine
Ciprofloxacin Ketoconazole Itraconazole
83
Drugs that increase didanosine levels
Allopurinol | Tenofovir
84
Drugs that decrease didanosine levels
Methadone Atanazavir Delavirdine
85
Stavudine is active against
HIV 1&2
86
Adverse effects of Stavudine and Zalcitabine
Dose=related peripheral neuropathy, fat atrophy
87
This drug has a more anti-retroviral activity in monocyte-macrophage cell lines
Zalcitabine
88
Drugs which increase zalcitabine levels
Probenecid | Cimetidine
89
Lamivudine and Tenofovir are active against
HIV 1&2; HBV
90
This drug counteracts phosphorylation of Zalcitabine
Lamivudine
91
Drugs for pregnant women
Lamivudine Zidovudine Atazanavir
92
Adverse effect of Abacavir
Fatal hypersensitivity syndrome (fever, abdominal pain, GI complaints)
93
Anti-HIV pre-exposure prophylaxis
Tenofovir and Emtricitabine
94
Oral solution of this drug contains propylene glycol contraindicated in young children, women, and patients with renal and hepatic failure
Emtricitabine
95
Adverse effect of Emtricitabine
Hyperpigmentation of skin
96
Anti-viral activity of NNRTI
HIV 1 but not HIV 2 and no activity on DNA polymerases
97
MOA of NNRTI
Inhibits viral reverse transcriptase and does not require phosphorylation
98
Adverse effects of Nevirapine
Dose-limiting toxicity: rash on trunk, face and extremities (SPARES PALMS AND SOLES)
99
NNRTI drug that has reduced efficacy with antacids, PPIs, and H2 blockers
Delavirdine
100
Dihydrobenzoxazinone NNRTI
Efavirenz
101
Bisheteroarylpiperazine NNRTI
Delavirdine
102
Dipyridodiazepinone NNRTI
Nevirapine
103
Adverse effect of Efavirenz
CNS toxicity
104
Adverse effect of Delavirdine
Skin rash (teratogenic)
105
MOA of protease inhibitors
Prevent proteolytic cleavage of HIV polyproteins and prevents metamorphosis of HIV virus particles into its adult form
106
Protease inhibitor with least potency to inhibit CYP3A4
Saquinavir
107
Adverse effect of saquinavir
Prolonged QT interval
108
Protease inhibitor with most potency to inhibit CYP3A4
Ritonavir
109
Adverse effect of Ritonavir
GI toxicity and dose-dependent hyperTG and hypercholesterolemia
110
Adverse effect of indinavir
nephrolithiasis and HIV lipodystrophy syndrome
111
Non-peptidic protease inhibitor
Nelfinavir
112
Nelfinavir has increased dose when given with
Rifabutin
113
Only protease inhibitor with a sulfonamide moiety
Amprenavir
114
Protease inhibitor with greatly increased water solubility and improved oral bioavailability
Fosamprenavir
115
This drug is a weak CYP3A4 inhibitor but becomes strong with Ritonavir
Lopinavir
116
Azapeptide protease inhibitor contraindicated in patients with hepatic insufficiency and is recommended in pregnant patients
Atazanavir
117
Relatively new protease inhibitor with increased risk of intracranial hemorrhage
Tipranavir
118
The only available HIV entry inhibitor
Enfuvirtide
119
Entry inhibitor accumulated in the cervicovaginal fluid
Maraviroc
120
Entry inhibitor accumulated in seminal fluid
Atanovir
121
MOA of Enfuvirtide
Binds to gp41 subunit of glycoprotein preventing conformational changes for fusion of viral and cellular membranes