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66 Cards in this Set

  • Front
  • Back
What are the 5 therapeutic targets within the retroviral life cycle?
1) Chemokine and CD4 receptors
2)Attachment and fusion
3)Reverse Transcriptase
4)Integrase
5)Maturation
What is a retrovirus?
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.
What does the CD4 receptors on T cells bind with on the surface of the viral particle?
gp120
What stabilizes the T cell/viral complex, allowing gp41-mediated fusion of the virus membrane with the target cell membrane?
CCR5 chemokine
This glycoprotein mediates fusion of the virus membrane with the target cell membrane?
gp41
What is the function of integrase?
It incorporates viral DNA into the host DNA.
What functions to copy viral RNA into viral DNA?
reverse transcriptase
This functions to clip newly created viral proteins into usable parts to be packaged for assembly.
Protease
Name the two HIV drug classes whose MOA is to block the actions of reverse transcriptase.
NRTIs and NNRTIs
What is the MOA of Protease Inhibitors?
block HIV protease
What is the MOA of Entry Inhibitors?
They are all designed to prevent the entry of HIV into the cell.
What are the 5 HIV drug classses?
*NRTI
*NNRTI
*Protease Inhibitors
*Entry Inhibitors
*Integrase Inhibitor
What does NRTI stand for?
Nucleoside/Nucleotide Reverse Transcriptase Inhibitor
What does NNRTI stand for?
Non-nucleoside Reverse Transcriptase Inhibitor
What are the 8 NRTIs?
1) Abacavir
2) Didansosine
3) Tenofovir
4)Lamivudine
5) Emtricitabine
6) Zalcitabine
7) Stavudine
8) Zidovudine
What are the 4 NNRTIs?
1) Efavirenz
2) Nevirapine
3)Delavirdine
4)Etravirine
What are the 8 Protease Inhibitors?
1) Atazanavir
2)Darunavir
3) Fosamprenavir
4)Indinavir
5)Lopinavir
6) Nelfinavir
7)Saquinavir
8)Tipranavir
What drug class does Indinavir belong to?
Protease Inhibitor
What drug class does Raltegravir belong to?
Integrase Inhibitor
What drug class does Saquinavir belong to?
Protease Inhibitor
What drug class does Maraviroc belong to?
Entry Inhibitor
What drug class does Zalcitabine belong to?
NRTI
What NRTI is a nucleoTIDE analog and only requires 2 phosphorylations?
Tenofovir
Which drug is associated with hypersensitivity syndrome related to the presence of HLA-B*5701?
Abacavir

We must test for this mutation before starting a patient on this drug.
Which NRTI is safe in pregnancy and also approved for HBV?
Lamivudine
This drug is not a 1st line choice due to ADRs such as fat wasting, peripheral neuropathy, lactic acidosis, and hepatic steatosis.
Zalcitabine
Which 2 NNTRIs are the most potent?
Efavirenz and Nevirapine
Which two Protease Inhibitors are sulfonamides?
Darunavir and Tipranavir
Redistribution of fat, leading to central obesity is a common side effect of this class of drug?
Protease Inhibitor
What class of drug does Enfuvirtide belong to?
Entry Inhibitor
Which drug has the side effect of hyperpigmentation of the skin?
Emtricitabine
What class of drug does Emtricitabine belong to?
NRTI
This protease inhibitor is associated with the least amount of ADRs.
Atazanavir
Describe the MOA of Maraviroc
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.
How can resistance occur?
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.
Injection site reactions are associated with this Entry Inhibitor.
Enfuvirtide
What adverse affects are listed in the packet for Raltegravir?
none
How are all the NNRTIs eliminated?
hepatic metabolism
What NNRTI is associated with psychotic dreams?
Efavirenz
Which protease inhibitor is a strong 3A4 inhibitor used sometimes to increase concentrations of other drugs?
Ritonavir
Which NRTI was the first nucleoside approved in 1987 and nicknamed AZT?
Zidovudine
Which drug is used to prevent transmission during pregnancy, IV during labor, and then syrup given to newborns?
Zidovudine
Which NNRTI is teratogenic?
Efavirenz
This drug class is associated with developing a rash.
NNRTIs

Although rare, SJS could happen
Which NNRTIs are inducers of 3A4?
Nevirapine
Efavirenz
Etravirine
Which NNRTI is an inhibitor of 3A4?
Delavirdine
This NNRTI is an inducer and substrate of 2B6 and 3A4.
Efavirenz
What is a possible HBV complication with Emtricitabine?
resistance or flare-up of HBV is possible if Emtricitabine is discontinued and the drug was also being used to tx HBV.
Which NNRTI has mixed metabolism, but is known as an inducer and inhibitor?
Etravirine
Which NRTI can cause dose dependent peripheral neuropathy and pacreatitis?
Didanosine
Name the two chemokine receptors.
CCR5 and CxCr4

Note: CxCr4 is pretty advanced HIV or AIDs and the outlook is not too good.
Which NRTI must be a buffered tablet due to its instability in acidic pH?
Didanosine
Which class of drugs bind to a hydrophobic pocket in the p66 subunit of reverse transcriptase as part of their MOA?
NNRTI
Do NRTIs require phosphorylation to become active?
yes
Do NNRTIs require phosphorylation to become active?
no
These drugs get incorporated into viral DNA and cause chain termination due to the missing 3' OH.
NRTIs
This drug is given as a prodrug called Disoproxil to improve oral absorption.
Tenofovir
Which drug is a purine analog of guanosine?
Abacavir
Which drug is a purine analog of adenosine?
Didanosine
Which drug is a pyrimidine analog of cytidine?
Lamivudine
Which drug 2 drugs are pyrimidine analogs of thymidine?
Zalcitabine and Zidovidine (AZT)
Which HIV antiviral is associated with myelosuppression?
Zidovidine (AZT)
Which Entry Inhibitor targets gp41?
Enfuvirtide
Describe the MOA of Enfuviritide
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.
Which drug class is associated with the side effect of cushingoid appearance and buffalo hump?
Protease Inhibitors
Which drug is used for post needlestick prophylaxis?
Zidovudine (AZT)