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66 Cards in this Set
- Front
- Back
What are the 5 therapeutic targets within the retroviral life cycle?
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1) Chemokine and CD4 receptors
2)Attachment and fusion 3)Reverse Transcriptase 4)Integrase 5)Maturation |
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What is a retrovirus?
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It is any group of viruses that contain two single-strand linear RNA molecules. It carries a genetic blueprint in the form of RNA instead of DNA.
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What does the CD4 receptors on T cells bind with on the surface of the viral particle?
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gp120
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What stabilizes the T cell/viral complex, allowing gp41-mediated fusion of the virus membrane with the target cell membrane?
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CCR5 chemokine
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This glycoprotein mediates fusion of the virus membrane with the target cell membrane?
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gp41
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What is the function of integrase?
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It incorporates viral DNA into the host DNA.
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What functions to copy viral RNA into viral DNA?
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reverse transcriptase
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This functions to clip newly created viral proteins into usable parts to be packaged for assembly.
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Protease
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Name the two HIV drug classes whose MOA is to block the actions of reverse transcriptase.
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NRTIs and NNRTIs
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What is the MOA of Protease Inhibitors?
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block HIV protease
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What is the MOA of Entry Inhibitors?
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They are all designed to prevent the entry of HIV into the cell.
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What are the 5 HIV drug classses?
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*NRTI
*NNRTI *Protease Inhibitors *Entry Inhibitors *Integrase Inhibitor |
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What does NRTI stand for?
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Nucleoside/Nucleotide Reverse Transcriptase Inhibitor
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What does NNRTI stand for?
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Non-nucleoside Reverse Transcriptase Inhibitor
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What are the 8 NRTIs?
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1) Abacavir
2) Didansosine 3) Tenofovir 4)Lamivudine 5) Emtricitabine 6) Zalcitabine 7) Stavudine 8) Zidovudine |
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What are the 4 NNRTIs?
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1) Efavirenz
2) Nevirapine 3)Delavirdine 4)Etravirine |
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What are the 8 Protease Inhibitors?
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1) Atazanavir
2)Darunavir 3) Fosamprenavir 4)Indinavir 5)Lopinavir 6) Nelfinavir 7)Saquinavir 8)Tipranavir |
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What drug class does Indinavir belong to?
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Protease Inhibitor
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What drug class does Raltegravir belong to?
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Integrase Inhibitor
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What drug class does Saquinavir belong to?
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Protease Inhibitor
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What drug class does Maraviroc belong to?
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Entry Inhibitor
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What drug class does Zalcitabine belong to?
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NRTI
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What NRTI is a nucleoTIDE analog and only requires 2 phosphorylations?
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Tenofovir
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Which drug is associated with hypersensitivity syndrome related to the presence of HLA-B*5701?
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Abacavir
We must test for this mutation before starting a patient on this drug. |
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Which NRTI is safe in pregnancy and also approved for HBV?
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Lamivudine
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This drug is not a 1st line choice due to ADRs such as fat wasting, peripheral neuropathy, lactic acidosis, and hepatic steatosis.
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Zalcitabine
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Which 2 NNTRIs are the most potent?
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Efavirenz and Nevirapine
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Which two Protease Inhibitors are sulfonamides?
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Darunavir and Tipranavir
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Redistribution of fat, leading to central obesity is a common side effect of this class of drug?
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Protease Inhibitor
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What class of drug does Enfuvirtide belong to?
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Entry Inhibitor
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Which drug has the side effect of hyperpigmentation of the skin?
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Emtricitabine
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What class of drug does Emtricitabine belong to?
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NRTI
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This protease inhibitor is associated with the least amount of ADRs.
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Atazanavir
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Describe the MOA of Maraviroc
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Maraviroc is an entry inhibitor that targets CCR5. It prevents the binding of gp120. When this happens, gp41 fusion cannot occur. Thus, the virus cannot enter the cell.
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How can resistance occur?
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Resistance can occur with as little as one mutation in the virus, but it usually takes 3 to 5 mutations before the virus is resistant.
Monotherapy with the NNRTIs would almost cause automatic resistance to develop. This is the reason for multiple drug regimines. |
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Injection site reactions are associated with this Entry Inhibitor.
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Enfuvirtide
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What adverse affects are listed in the packet for Raltegravir?
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none
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How are all the NNRTIs eliminated?
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hepatic metabolism
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What NNRTI is associated with psychotic dreams?
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Efavirenz
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Which protease inhibitor is a strong 3A4 inhibitor used sometimes to increase concentrations of other drugs?
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Ritonavir
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Which NRTI was the first nucleoside approved in 1987 and nicknamed AZT?
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Zidovudine
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Which drug is used to prevent transmission during pregnancy, IV during labor, and then syrup given to newborns?
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Zidovudine
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Which NNRTI is teratogenic?
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Efavirenz
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This drug class is associated with developing a rash.
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NNRTIs
Although rare, SJS could happen |
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Which NNRTIs are inducers of 3A4?
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Nevirapine
Efavirenz Etravirine |
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Which NNRTI is an inhibitor of 3A4?
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Delavirdine
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This NNRTI is an inducer and substrate of 2B6 and 3A4.
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Efavirenz
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What is a possible HBV complication with Emtricitabine?
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resistance or flare-up of HBV is possible if Emtricitabine is discontinued and the drug was also being used to tx HBV.
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Which NNRTI has mixed metabolism, but is known as an inducer and inhibitor?
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Etravirine
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Which NRTI can cause dose dependent peripheral neuropathy and pacreatitis?
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Didanosine
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Name the two chemokine receptors.
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CCR5 and CxCr4
Note: CxCr4 is pretty advanced HIV or AIDs and the outlook is not too good. |
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Which NRTI must be a buffered tablet due to its instability in acidic pH?
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Didanosine
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Which class of drugs bind to a hydrophobic pocket in the p66 subunit of reverse transcriptase as part of their MOA?
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NNRTI
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Do NRTIs require phosphorylation to become active?
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yes
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Do NNRTIs require phosphorylation to become active?
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no
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These drugs get incorporated into viral DNA and cause chain termination due to the missing 3' OH.
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NRTIs
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This drug is given as a prodrug called Disoproxil to improve oral absorption.
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Tenofovir
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Which drug is a purine analog of guanosine?
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Abacavir
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Which drug is a purine analog of adenosine?
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Didanosine
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Which drug is a pyrimidine analog of cytidine?
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Lamivudine
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Which drug 2 drugs are pyrimidine analogs of thymidine?
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Zalcitabine and Zidovidine (AZT)
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Which HIV antiviral is associated with myelosuppression?
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Zidovidine (AZT)
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Which Entry Inhibitor targets gp41?
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Enfuvirtide
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Describe the MOA of Enfuviritide
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When Enfuvirtide is introduced into the body, it binds to gp41 and prevents formation of the helix. Now, the virus can no longer enter the cell.
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Which drug class is associated with the side effect of cushingoid appearance and buffalo hump?
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Protease Inhibitors
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Which drug is used for post needlestick prophylaxis?
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Zidovudine (AZT)
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