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Pharmacology-PA
Antivirals-Lecture #2
| Question | Answer |
|---|---|
| 1. What is the trade name for Lamivudine? | 3TC |
| 2. T/F The molecular compound of Lamivudine is? | 2',3'-dideoxy-3'-thiacytidine |
| 3. T/F The brand names for Lamivudine are Zeffix, Heptovir, Epivir, and Epivir-HBV. | True |
| 4. What is the MOA of Lamivudine? | terminates synthesis of proviral DNA and inhibits reverse transcriptase of HIV and HBV |
| 5. What is Lamivudine used to treat? | Used for treatment of chronic hepatitis B at a lower dose than for treatment of HIV. |
| 6. T/F Unlike AZT, Lamivudine does not produce bone marrow suppression. | True |
| 7. T/F Combination of zidovudine with lamivudine slows development of zidovudine resistance. | True |
| 8. T/F Long term use of lamivudine unfortunately leads to emergence of a resistant hepatitis B virus (YMDD) mutant. | True |
| 9. What are the drug interactions of Lamivudine? | concurrent administration with TMP/SMX increases bioavailability of lamivudine |
| 10. What are the ADR of Lamivudine? | Pancreatitis |
| 11. T/F Every DNA strand is consisted a nucleotides. | True |
| 12. T/F Nucleotides are monomers that are made of a phosphate, a sugar (deoxyribose) and a heterocyclic base (Thimine, Cytosine -pyrimidines- Adenine, Guanine - purines-). | True |
| 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. | True |
| 14. What is the trade name of Stavudine? | d4T |
| 15. T/F The molecular compound of Stavudine is? | 2'-3'-didehydro-2'-3'-dideoxythymidine |
| 16. What is the MOA of Stavudine? | analog of thymidine that converts to triphosphate form |
| 17. T/F When administering Stavudine, the Intracellular phosphorylation inhibited by AZT prevents co-administration. | True |
| 18. What does Stavudine inhibit? | Inhibits reverse transcriptase and DNA polymerase |
| 19. T/F Stavudine Penetrates the blood-brain barrier. | True |
| 20. What is the ADR of Stavudine? | peripheral neuropathy, renal toxicity |
| 21. What should be taken with caution with the drug Stavudine? | patients with renal impairment |
| 22. What is the trade name for Zalcitabine? | ddC, Hivid |
| 23. T/F The molecular compound of Zalcitabine is? | 2'-3'-dideoxycytidine, ddC and is also called dideoxycytidine. True |
| 24. What is Zalcitabine? | It is a nucleoside analog reverse transcriptase inhibitor (NARTI) |
| 25. T/F Zalcitabine is sold under the trade name Hivid. | True |
| 26. What is the MOA of Zalcitabine? | analog of deoxycytidine converted to triphosphate form which incorporates into viral DNA and inhibits reverse transcriptase |
| 27. T/F In Zalcitabine, competitive inhibitor of dCTP is for the active site of viral reverse transcriptase. | True |
| 28. What does Zalcitabine inhibit? | Inhibits viral and cellular DNA synthesis. |
| 29. How potent is Zalcitabine? | approximately 10 times more potent than zidovudine against HIV |
| 30. What drug decreases the absorption due to Food or antacids? | Zalcitabine |
| 31. What is ADR of Zalcitabine? | rash, stomatitis, peripheral neuropathy, Pancreatitis |
| 32. What does Zalcitabine cause? | causes pancreatitis, rarely fatal |
| 33. T/F Patients who have pancreatitis or a history of pancreatitis, or are at risk for pancreatitis, either should not take zalcitabine or should take it with extreme caution. | True |
| 34. T/F When administering Zalcitabine, what should be monitored? | Serum amylase levels |
| 35. What is the normal range of serum amylase level? | The normal range is 23 to 85 U/L |
| 36. T/F Patients with moderate to severe peripheral neuropathy should not take zalcitabine. | True |
| 37. T/F Patients with renal impairment may be at increased risk of toxicity due to decreased clearance of Zalcitabine through the kidneys. | True |
| 38. What is the tradename for Didanosine? | ddI, Videx, Videx EC |
| 39. T/F The molecular compound of Didanosine is 2',3'-dideoxyinosine. | True |
| 40. What is the MOA Didanosine? | incorporates into the DNA chain, causing termination of chain elongation and inhibits RT. |
| 41. When taking Zalcitabine, what is it not recommended for? | Not recommended for initial treatment of HIV, best for AZT-resistant HIV |
| 42. T/F Didanosine are Acid labile (available in chewable tablets or solution) all oral formulations contained or are compounded with buffering agents to increase the gastric pH. | True |
| 43. How are the chewable tablets of Didanosine? | The chewable tablets were large, fragile, and foul-tasting |
| 44. What does the buffering compound of Didanosine cause? | Buffering compound would cause diarrhea. |
| 45. T/F New Videx EC (trade name for Didanosine) formulations uses smaller capsule containing coated microspheres instead of using a buffering compound. | True |
| 46. T/F Didanosine is approved by the FDA for once-a-day dosing. | True |
| 47. T/F Didanosine were the first generic anti-HIV drug marketed in the United States. | True |
| 48. T/F Food substantially reduces didanosine bioavailability, when administered on an empty stomach. | True |
| 49. What is the half-life of Didanosine in the plasma and in intracellular environment? | The half-life in plasma is only 1.5 hours, but 12 hours in the intracellular environment. |
| 50. How is Didanosine eliminated? | Elimination is predominantly renal |
| 51. What is the ADR for Didanosine? | pancreatitis, peripheral neuropathy |
| 52. When administering Didanosine, what drug does it interfere? | May interfere with absorption of other drugs (ketoconazole) |
| 53. What is the trade name for Tenofovir? | Viread |
| 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. | True |
| 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. | True |
| 56. What can Tenofovir cause? | Acute renal failure, fanconi syndrome, proteinuria, and tubular necrosis. |
| 57. What does Tenofovir increase? | It increases didanosine and Atazanavir concentration protease inhibitors |
| 58. What does Protease inhibitors (PIs) target? | Protease inhibitors (PIs) target viral assembly by inhibiting the activity of the HIV-1 protease. |
| 59. T/F HIV protease cleaves nascent polypeptides into mature proteins for final assembly of new virons. | True |
| 60. In Protease Inhibitors, target HIV-1 protease is essential for? | Target HIV-1 protease is essential for the final step of viral replication |
| 61. T/F HIV protease cleaves nascent proteins for final assembly of new virons. | True |
| 62. What are the Protease Inhibitor Agents? | 1-Saquinavir, 2-Ritonavir, 3-Nelfinavir, 4-Amprenavir, 5-Indinavir |
| 63. What is the MOA of Protease Inhibitors? | 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 |
| 64. What is the trade name for Saquinavir? | Invirase, Fortovase |
| 65. T/F Invirase is a poorly-absorbed hard gel capsule which quickly led to viral resistance in many of the pioneer patients. | True |
| 66. T/F Fortovase was a soft gel capsule reformulated for improved bioavailability, which now superseded by Invirase + ritonavir. | True |
| 67. How is Sasquinavir administered? | Oral administration with high fat meals to maximize absorption |
| 68. T/F Oral bioavailability of Saquinavir in both formulations significantly increases when patients also receive ritonavir. | True |
| 69. T/F Ritonavir inhibits the cytochrome P450 3A4 enzyme. | True |
| 70. T/F When Saquinavir is administered with co-administration delavirdine (an NNRTI), the plasma levels increase. | True |
| 71. What are the ADR of Saquinavir? | headache, fatigue, nausea, diarrhea, loose stools, abdominal discomfort, increased LFT’s |
| 72. What is the tradename for Indinavir? | Crixivan |
| 73. T/F Indinavir is well-absorbed orally, and is the least protein bound of all of the protease inhibitors. | True |
| 74. T/F Indinavir requires precise dosing every 8 hours. | True |
| 75. T/F Indinavir is being replaced by newer drugs that are more convenient and less likely to promote resistant virus, such as lopinavir or atazanavir. | True |
| 76. T/F When administering Indinavir, acidic gastric conditions are necessary for absorption. | True |
| 77. What are the ADR for Indinavir? | nausea, vomiting, headache, diarrhea, fatigue, nephrolithiasis, hyperlipidemia, hyperbilirubinemia, lipodystrophy |
| 78. What is the tradename for Ritonavir? | Norvir |
| 79. T/F Ritonavir is no longer utilized as a single PI agent due to excessive side effects. | True |
| 80. T/F Ritonavir is now frequently used to “boost” plasma concentrations of other Protease Inhibitors, which reduced dosages and frequencies. | True |
| 81. T/F Ritonavir’s bioavailability is unaffected by food, but is unpalatable. | True |
| 82. T/F Ritonavir is an inhibitor of cytochrome P450 3A4 enzymes. | True |
| 83. What are the ADR of Ritonavir? | nausea, vomiting, diarrhea, asthenia, headache, circumoral paresthesia, elevated aminotransferase and triglyceride levels, taste alteration |
| 84. T/F One of Ritonavir's side effects is hyperglycemia. | True |
| 85. T/F It appears that Ritonavir directly inhibits the GLUT4 insulin regulated transporter, keeping glucose from entering fat and muscle cells. | True |
| 86. T/F Nelfinavir in combination with lamivudine and zidovudine, decreases viral load by at least 100-fold and increases CD4+ counts. | True |
| 87. T/F Nelfinavir may be administered with food. | True |
| 88. What is the ADR of Nelfinavir? | diarrhea, nausea, flatulence, rash |
| 89. What is the prodrug of Fosamprenavir? | It is a Prodrug for amprenavir |
| 90. T/F Fosamprenavir slows conversion to amprenavir, which leads to long plasma half-life & permits twice daily dosing (reduced # pills). | True |
| 91. T/F Fosamprenavir offers no clinical advantage over other protease inhibitors. | True |
| 92. What is the ADR of Fosamprenavir? | nausea, diarrhea, vomiting, oral and perioral paresthesia, rash |
| 93. What are other potential users of Protease inhibitors? | Protease inhibitors can be used as anti-protozoals (against malaria and Giardia) and as anti-cancer Agents. |
| 94. T/F NNRTIs are “Non-nukes”. | True |
| 95. What does the Non-nucleoside reverse transcriptase inhibitors (nNRTI) inhibit? | They inhibit reverse transcriptase directly by binding to the enzyme and interfering with its function. |
| 96. T/F Non-Nucleoside Reverse Transcriptase Inhibitors (nNRTI) are highly selective, non-competitive inhibitors of HIV-1 reverse transcriptase. | True |
| 97. T/F Non-Nucleoside Reverse Transcriptase Inhibitors (nNRTI) has no effect on 1-nucleoside triphosphatesm or 2-human DNA polymerases. | True |
| 98. What are the major advantages of nNRTI having no effect of the nucleoside triphosphatesm or human DNA polymerases? | 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 |
| 99. What are the Non-Nucleoside Reverse Transcriptase Inhibitors (nNRTI) Agents? | 1-Atevirdine, 2-Bishetero.arylpiperazine*, 2-Delavirdine, 3-Nevirapine, 4-Efavirenz |
| 100. What is the trade name for Nevirapine? | NVP, Viramune |
| 101. T/F Nevirapine was more effective than placebo in raising CD4 counts and reducing viral load in patients who have had previous antiretroviral therapy. | True |
| 102. T/F Nevirapine is very lipophilic, therefore widely distributed. | True |
| 103. What is the ADR of Nevirapine? | rash, fever, headache, elevated serum transaminases, hepatotoxicity |
| 104. T/F When Nevirapine is administered with NRTIs, no dosage adjustment is necessary. | True |
| 105. T/F Nevirapine increases the metabolism of protease inhibitors, which adjusts dosages. | True |
| 106. Nevirapine increases the metabolism of what drugs? | Increases metabolism of oral contraceptives, ketoconazole, metronidazole, warfarin, quinidine, theophylline |
| 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. | True |
| 108. T/F The addition of Delavirdine to NRTIs is more effective than NRTIs alone and is considered in salvage therapy. | True |
| 109. T/F Delavirdine is extensively plasma protein bound, and the absorption is not affected by the presence of food. | True |
| 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. | True |
| 111. T/F Like Ritonavir, Delavirdine inhibits cytochrome P450 3A4 also. | True |
| 112. What is the ADR of Delavirdine? | rash, nausea, dizziness, Headache |
| 113. T/F Delavirdine is an inhibitor of drug metabolism. | True |
| 114. What drugs increases delavirdine plasma levels? | Fluoxetine and ketoconazole |
| 115. What drugs decrease plasma levels of delavirdine? | Phenytoin, phenobarbital and carbamazepine |
| 116. What is the trade name of Efavirenz? | Sustiva |
| 117. T/F Efavirenz is indicated for initial therapy of HIV-1. | True |
| 118. How is the dosing for Efavirenz? | Once a day dosing |
| 119. T/F Department of HHS Panel on Antiretroviral Guidelines currently recommends Efavirenz in combination with lamivudine/zidovudine (Combivir) or tenofovir/emtricitabine (Truvada) in adults and adolescents. | True |
| 120. What is lamivudine/zidovudine called? | Combivir |
| 121. What is tenofovir/emtricitabine called? | Truvada |
| 122. T/F the treatment of Efavirenz in combination with Combivir or Truvada, results in the increase in CD4 cell count and decreases the viral load. | True |
| 123. T/F Efavirenz is well distributed, including CNS and with a half-life over 40 hours. | True |
| 124. What is the ADR of Efavirenz? | dizziness, headache, loss of concentration, vivid dreams, rash |
| 125. Efavirenz is an inducer of? | Inducer of cytochrome P-450 |
| 126. T/F Two NRTIs plus a PI can be an Initial Therapy. | True |
| 127. T/F Two NRTIs plus a NNRTI can be an Initial Therapy. | True |
| T/F Two NRTIs plus a PI and NNRTI can be an Initial Therapy. | True |
| 128. T/F Two NRTIs and two PIs can be an Initial Therapy. | True |
| 129. T/F Three NRTIs (less potent alternative) can be an Initial Therapy. | True |
| 130. T/F Efavirenz + zidovudine + lamivudine is one of the preferred initial regimens. | True |
| 131. T/F Efavirenz + tenofovir + emtricitabine is one of the preferred initial regimens. | True |
| 132. T/F Lopinavir boosted with ritonavir + zidovudine + lamivudine is one of the preferred initial regimens. | True |
| 133. T/F Lopinavir boosted with ritonavir + tenofovir + emtricitabine. is one of the preferred initial regimens. | True |
| 134. T/F Part of the monitoring therapy, Plasma HIV RNA is monitored for load reduction below detectable levels. | True |
| 135. T/F CD4 cell counts are done to assess immune status of patient. | True |
| 136. T/F Initially, monitoring performed every 4 weeks for immune status of patients. | True |
| 137. How long does the undetectable HIV RNA need to be monitored? | Every 3 Months |
| 138. T/F One of the results of treatment failure is when less than a 10 fold reduction of viral load is after 4-6 weeks. | True |
| 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. | True |
| 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). | True |
| 141. T/F One of the results of treatment failure is when there is persistent decline of CD4 cells or clinical Deterioration. | True |
| 142. What does Fusion Inhibitors interfere with? | 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) |
| 143. What do the Immune stimulators do? | It uses the body’s chemical messengers to stimulate an immune response (Interleukin 2, HIV-1 Immunogen, Reticulose) |
| 144. What does the Fusion/attachment inhibitors Entry inhibitors (or fusion inhibitors) interfere with? | It interferes with binding, fusion and entry of HIV-1 to the host cell by blocking one of several targets. |
| 145. What are the two currently available agents in the class of Fusion? | Maraviroc and enfuvirtide |
| 146. What do Integrase Inhibitors inhibit? | They inhibit HIV integrase enzyme, which is a key step in the reproduction cycle of HIV (Zintevir) |
| 147. What are the other Integrase Inhibitors? | Thalidomide, Hydroxyurea, Interferon |
| 148. T/F Integrase inhibitors inhibit the enzyme integrase, which is responsible for integration of viral DNA into the DNA of the infected cell. | True |
| 149. T/F There are several integrase inhibitors currently under clinical trial, and Raltegravir became the first to receive FDA approval in October 2007. | True |
| 150. What is the first drug to target the CCR5 coreceptor on the surface of the cell? | Maraviroc |
| 151. What is the first drug in the integrase inhibitor class? | Raltegravir |
| 152. T/F Etravirine is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) "with clear activity against some NNRTI-resistant viruses." | True |
| 153. T/F There are 6 things to consider when choosing the Choice of drug. | True |
| 154. T/F One of the considerations of DOC is that there are now approx 20 approved anti-HIV drugs and more in development (see page 16 of the i-Base guide). | True |
| 155. T/F One of the considerations of DOC is that some are more potent than others. | True |
| 156. T/F One of the considerations of DOC is that a few cannot be used together (ex: d4T and AZT). | True |
| 157. T/F One of the considerations of DOC is that recent studies and guidelines recommend using: 2 NRTIs + 1 NNRTI or 2 NRTIs + 1 PI-based on combination as being most effective: 1-[AZT / 3TC / efavirenz] or 2-[AZT / 3TC / lopinavir/r (Kaletra)] | True |
| 158. T/F One of the considerations of DOC is that there are other combinations that are better for some people. | True |
| 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. | True |
| 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. | True |
| 161. T/F Regarding Inhibiting mother-child transmission, the mother should receive single-dose Nevirapine (NVP) when entering labor. | True |
| 162. T/F Regarding Inhibiting mother-child transmission, the mother should receive AZT+3TC for one week following delivery. | True |
| 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. | True |
| 164. T/F Regarding Mother-child Transmission, Complementary measures include caesarian section and formula feeding. | True |
| 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%. | True |
| 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. | True |
| 167. T/F In HIV Treatment, Once resistance develops it never reverses. | True |
| 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. | True |
| 169. T/F During HIV replication, error-prone Reverse Transcriptase produces frequent mutations. | True |
| 170. T/F Most of the mutations are insignificant, but some will produce resistance to specific drugs. | True |
| 171. What is the main cause of resistance? | poor adherence |
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