Term
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Definition
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Term
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Definition
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Term
| What modifications are made to the NRTIs? |
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Definition
| All are phosporylated 3 times except for tenofovir: it is cleaved next to its PO4 group, and then phosphorylated one more time. |
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Term
| What are the toxicities of NRTIs? |
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Definition
May be associated with mitochondrial toxicity owing to inhibition of mtDNAP gamma, inc the risk of lactic acidosis with hepatic steatosis, which may be fatal, as well as disorders of lipid metabolism. Treatment should be suspended in the setting of rapidly rising aminotransferase levels, progressive hepatomegaly, or metaboic acidosis of unknown etiology.
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Term
What is the MOA of Didanosine?
MOR?
Toxicity? |
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Definition
MOA – synthetic analog of deoxyadenosine , oral BA 30-40%,
Resistance – L74V mutation , K65R, multiple thymidine analog mutations.
Toxicity – dose dependent. Pancreatitis, other effects: painful peripheral distal neuropathy, D, hepatitis, esophageal ulceration, cardiomyopathy, CNS toxicity
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Term
What is the MOA of Lamivudine?
MOR?
Side effects? |
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Definition
•MOA – inibits HBV DNA polymerase and HIV reverse transcriptase by competing with deoxycytidine triP for incorporation into the viral DNA, chain termination.
•Resistance – chronic therapy with YMDD strain mutations
•SA – HA, N, Dizziness are rare. No evidence of mitochondrial toxicity.
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Term
| What is Lamuvidine typically given in combination with? |
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Definition
| Zidovudine - They are synergistic (less than 1 FIC) |
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Term
| What is the MOA of Abacavir? |
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Definition
| It is a guanosine analog that is well-absorbed. BA 83% |
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Term
| What is the MOA of NNRTIs? |
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Definition
| Bind directly to HIV-I reverse transcriptase resulting in blocking of RNA and DNA dep polymerase . Binding site of NNRTIs is near but distinct from that of NRTIs. |
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Term
- Which form of HIV do NNRTIs affect?
- How are they different than NRTIs?
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Definition
- HIV-1. The do not work against HIV-2.
- They do not compete with nucleosidetriphosphates, and do not need enzymatic P
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Term
| What is the MOR to NNRTIs? |
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Definition
Occurs rapidly with monotherapy. K103N+Y181C mutations confer resistance across all NNRTIs; L1001, Y188C, G109A confer resistance to nevirapine and efavirenz.
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Term
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Definition
| Delviradine, Efavirenz and Nevirapine. |
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