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Antivirals-Lecture #2

Quiz yourself by thinking what should be in each of the black spaces below before clicking on it to display the answer.
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Question
Answer
show 3TC  
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2. T/F The molecular compound of Lamivudine is?   show
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3. T/F The brand names for Lamivudine are Zeffix, Heptovir, Epivir, and Epivir-HBV.   show
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4. What is the MOA of Lamivudine?   show
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show Used for treatment of chronic hepatitis B at a lower dose than for treatment of HIV.  
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show True  
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7. T/F Combination of zidovudine with lamivudine slows development of zidovudine resistance.   show
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8. T/F Long term use of lamivudine unfortunately leads to emergence of a resistant hepatitis B virus (YMDD) mutant.   show
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show concurrent administration with TMP/SMX increases bioavailability of lamivudine  
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10. What are the ADR of Lamivudine?   show
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show True  
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show True  
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13. T/F The combination of a sugar and an heterocyclic base is a nucleoside. When a phosphate is added to the molecule, a nucleotide is created.   show
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show d4T  
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15. T/F The molecular compound of Stavudine is?   show
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show analog of thymidine that converts to triphosphate form  
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17. T/F When administering Stavudine, the Intracellular phosphorylation inhibited by AZT prevents co-administration.   show
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show Inhibits reverse transcriptase and DNA polymerase  
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19. T/F Stavudine Penetrates the blood-brain barrier.   show
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show peripheral neuropathy, renal toxicity  
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21. What should be taken with caution with the drug Stavudine?   show
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show ddC, Hivid  
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23. T/F The molecular compound of Zalcitabine is?   show
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show It is a nucleoside analog reverse transcriptase inhibitor (NARTI)  
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25. T/F Zalcitabine is sold under the trade name Hivid.   show
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26. What is the MOA of Zalcitabine?   show
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27. T/F In Zalcitabine, competitive inhibitor of dCTP is for the active site of viral reverse transcriptase.   show
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show Inhibits viral and cellular DNA synthesis.  
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29. How potent is Zalcitabine?   show
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show Zalcitabine  
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31. What is ADR of Zalcitabine?   show
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32. What does Zalcitabine cause?   show
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show True  
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show Serum amylase levels  
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35. What is the normal range of serum amylase level?   show
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show True  
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show True  
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38. What is the tradename for Didanosine?   show
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39. T/F The molecular compound of Didanosine is 2',3'-dideoxyinosine.   show
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40. What is the MOA Didanosine?   show
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show Not recommended for initial treatment of HIV, best for AZT-resistant HIV  
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show True  
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43. How are the chewable tablets of Didanosine?   show
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44. What does the buffering compound of Didanosine cause?   show
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45. T/F New Videx EC (trade name for Didanosine) formulations uses smaller capsule containing coated microspheres instead of using a buffering compound.   show
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show True  
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show True  
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show True  
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show The half-life in plasma is only 1.5 hours, but 12 hours in the intracellular environment.  
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50. How is Didanosine eliminated?   show
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51. What is the ADR for Didanosine?   show
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52. When administering Didanosine, what drug does it interfere?   show
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53. What is the trade name for Tenofovir?   show
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54. T/F Tenofovir is also available in a fixed-dose combination with emtricitabine in a product with the brand name Truvada for once-a-day dosing.   show
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55. T/F Emtricitabine, which is marketed in combination with Tenofovir that makes Truvada, is also marketed as a single compound product called Emtriva, also by Gilead.   show
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56. What can Tenofovir cause?   show
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show It increases didanosine and Atazanavir concentration protease inhibitors  
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show Protease inhibitors (PIs) target viral assembly by inhibiting the activity of the HIV-1 protease.  
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show True  
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60. In Protease Inhibitors, target HIV-1 protease is essential for?   show
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61. T/F HIV protease cleaves nascent proteins for final assembly of new virons.   show
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62. What are the Protease Inhibitor Agents?   show
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show Reversibly inhibit the proteinase that is essential for the final step of viral proliferation HIV Protease in the fully open conformation, about to bind a protease inhibitor  
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64. What is the trade name for Saquinavir?   show
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65. T/F Invirase is a poorly-absorbed hard gel capsule which quickly led to viral resistance in many of the pioneer patients.   show
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66. T/F Fortovase was a soft gel capsule reformulated for improved bioavailability, which now superseded by Invirase + ritonavir.   show
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show Oral administration with high fat meals to maximize absorption  
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show True  
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69. T/F Ritonavir inhibits the cytochrome P450 3A4 enzyme.   show
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70. T/F When Saquinavir is administered with co-administration delavirdine (an NNRTI), the plasma levels increase.   show
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show headache, fatigue, nausea, diarrhea, loose stools, abdominal discomfort, increased LFT’s  
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show Crixivan  
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73. T/F Indinavir is well-absorbed orally, and is the least protein bound of all of the protease inhibitors.   show
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show True  
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show True  
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show True  
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77. What are the ADR for Indinavir?   show
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78. What is the tradename for Ritonavir?   show
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79. T/F Ritonavir is no longer utilized as a single PI agent due to excessive side effects.   show
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show True  
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show True  
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82. T/F Ritonavir is an inhibitor of cytochrome P450 3A4 enzymes.   show
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show nausea, vomiting, diarrhea, asthenia, headache, circumoral paresthesia, elevated aminotransferase and triglyceride levels, taste alteration  
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show True  
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show True  
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show True  
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show True  
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show diarrhea, nausea, flatulence, rash  
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show It is a Prodrug for amprenavir  
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90. T/F Fosamprenavir slows conversion to amprenavir, which leads to long plasma half-life & permits twice daily dosing (reduced # pills).   show
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91. T/F Fosamprenavir offers no clinical advantage over other protease inhibitors.   show
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show nausea, diarrhea, vomiting, oral and perioral paresthesia, rash  
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show Protease inhibitors can be used as anti-protozoals (against malaria and Giardia) and as anti-cancer Agents.  
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show True  
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95. What does the Non-nucleoside reverse transcriptase inhibitors (nNRTI) inhibit?   show
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show True  
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97. T/F Non-Nucleoside Reverse Transcriptase Inhibitors (nNRTI) has no effect on 1-nucleoside triphosphatesm or 2-human DNA polymerases.   show
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show Major advantages are the there is a lack of cross-resistance with nucleoside reverse transcriptase inhibitors and there is a lack of effect on the host blood cell precursors  
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show 1-Atevirdine, 2-Bishetero.arylpiperazine*, 2-Delavirdine, 3-Nevirapine, 4-Efavirenz  
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show NVP, Viramune  
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show True  
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show True  
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103. What is the ADR of Nevirapine?   show
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show True  
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105. T/F Nevirapine increases the metabolism of protease inhibitors, which adjusts dosages.   show
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show Increases metabolism of oral contraceptives, ketoconazole, metronidazole, warfarin, quinidine, theophylline  
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107. T/F Delavirdine has efficacy that is lower than other NNRTIs, especially efavirenz, and has an inconvenient schedule, which is why it is omitted from initial therapy.   show
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show True  
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109. T/F Delavirdine is extensively plasma protein bound, and the absorption is not affected by the presence of food.   show
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110. T/F The complex set of drug interactions make the place of Delavirdine in second-line and salvage therapy is unclear, that is why it’s rarely used.   show
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show True  
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show rash, nausea, dizziness, Headache  
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113. T/F Delavirdine is an inhibitor of drug metabolism.   show
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show Fluoxetine and ketoconazole  
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115. What drugs decrease plasma levels of delavirdine?   show
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116. What is the trade name of Efavirenz?   show
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117. T/F Efavirenz is indicated for initial therapy of HIV-1.   show
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118. How is the dosing for Efavirenz?   show
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show True  
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120. What is lamivudine/zidovudine called?   show
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121. What is tenofovir/emtricitabine called?   show
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show True  
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show True  
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show dizziness, headache, loss of concentration, vivid dreams, rash  
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show Inducer of cytochrome P-450  
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show True  
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127. T/F Two NRTIs plus a NNRTI can be an Initial Therapy.   show
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show True  
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show True  
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show True  
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130. T/F Efavirenz + zidovudine + lamivudine is one of the preferred initial regimens.   show
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show True  
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132. T/F Lopinavir boosted with ritonavir + zidovudine + lamivudine is one of the preferred initial regimens.   show
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133. T/F Lopinavir boosted with ritonavir + tenofovir + emtricitabine. is one of the preferred initial regimens.   show
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show True  
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show True  
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136. T/F Initially, monitoring performed every 4 weeks for immune status of patients.   show
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show Every 3 Months  
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show True  
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139. T/F One of the results of treatment failure is when there is failure to reach undetectable viral load after 4-6 months of treatment.   show
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140. T/F One of the results of treatment failure is when there is detection of virus after initial complete suppression of viral load (resistance).   show
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141. T/F One of the results of treatment failure is when there is persistent decline of CD4 cells or clinical Deterioration.   show
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show Fusion Inhibitors interfere with the interactions that enable membrane fusion between the virus, or an HIV-infected cell and an uninfected cell, reducing replication (AMD-3100, FP-21399)  
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show It uses the body’s chemical messengers to stimulate an immune response (Interleukin 2, HIV-1 Immunogen, Reticulose)  
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show It interferes with binding, fusion and entry of HIV-1 to the host cell by blocking one of several targets.  
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145. What are the two currently available agents in the class of Fusion?   show
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146. What do Integrase Inhibitors inhibit?   show
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show Thalidomide, Hydroxyurea, Interferon  
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show True  
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show True  
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150. What is the first drug to target the CCR5 coreceptor on the surface of the cell?   show
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151. What is the first drug in the integrase inhibitor class?   show
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152. T/F Etravirine is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) "with clear activity against some NNRTI-resistant viruses."   show
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153. T/F There are 6 things to consider when choosing the Choice of drug.   show
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show True  
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show True  
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156. T/F One of the considerations of DOC is that a few cannot be used together (ex: d4T and AZT).   show
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show True  
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158. T/F One of the considerations of DOC is that there are other combinations that are better for some people.   show
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159. T/F One of the considerations of DOC is that every drug has different advantages and disadvantages, and newer drugs are being used as first line therapy.   show
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160. T/F Regarding Inhibiting mother-child transmission, the WHO guidelines state that pregnant women should start Zidovudine (AZT) from 28 weeks or as soon as possible from that point.   show
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161. T/F Regarding Inhibiting mother-child transmission, the mother should receive single-dose Nevirapine (NVP) when entering labor.   show
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show True  
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163. T/F Regarding Inhibiting mother-child transmission, the child should be given single dose Nevirapine immediately after delivery and daily Zidovudine until one week old.   show
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show True  
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165. T/F Regarding Mother-child Transmission, in some settings, the interventions have succeeded in reducing the risk of infection from 25% to about 1%.   show
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166. T/F In HIV Treatment, the treatment with less than 3 drugs or missing doses (even one dose a week) will lead to resistance, and the combination will fail.   show
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show True  
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168. T/F In HIV Treatment, Resistance to one drug or drug combination is associated with increased likelihood of resistance to the next combination (cross-resistance) between most drugs in each class.   show
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show True  
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show True  
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171. What is the main cause of resistance?   show
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