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16 Cards in this Set
- Front
- Back
Know the NRTIs:
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- nucleoside phosphorylated to 5'triphosphate by cellular enzymes.
- Inhibit the activity of RT by competing with dNTP and by incorporated with nascent viral DNA, RESULTING IN Dna termination. |
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Resistance to NRTIs AND a.e.?
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- from RT mutations.
A.E.: LACTIC ACIDOSIS, HEPATIC STEATOSIS. |
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What are some A.E.:
- Zidovudine: - Abacavir - Didanosin, Stavudine, Zalcitabine - Didanosine, Stavudine - Didanosine: |
Zidovudine: anemia, neutropenia.
Abacavir: Fatal hypersensitivity reactions Didanosine, Stavudine, Zalcitabine: Peripheal Neuropathy. Didanosine, Stavudine: pancretitis Didanosine: Fat redistribution and retinal changes and optic neuritis Zalcitabine Ulceration: buccal mucosa, soft palate, tongue, pharnyx. |
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Drug-Drug Interactions:
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- Stavudine + Zidovudine = intracellular activation.
- Lamivudine + Zalcitabine = interfering with its phosphorylation. - Ethanol + abacvir = increase conc. - Didanosin + zalcitabine = increase peripheal neuropathy. |
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NNRTIs MOA:
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- Block RT activity by binding adjacent to the enzyme's binding site -> induces conformational changes.
- metabolized by CYP 450 |
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NNRTIs drug names:
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- Nevirapine (Viramune)
- Delavirdine (Rescriptor) - Efavirenz (Sustiva) |
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Most common A.E. for all NNRTIS?
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RASH.
Nevirapine: Stevens-Johnsons Syndrome and hepatitis. Efavirenz: HA, dizziness, abnormal dreams, impaired conc., PSYCHIATRIC DISTURBANCES. - tetrogenic - increased liver enzymes Delavirdine: increased liver enzymes. |
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Protease Inhibitors: (avir)
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HIV proteases is essential for viral polyproteins (gag and gag-pol) into active viral enzymes (RT, integrase, protease) and structural proteins.
- Binds REVERSIBLY to active site of protease. |
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PI:
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- poor oral bioavailability
- all under go metabolism by CYP3A4 and p-glycoprotein - extensivily binds to plasma protein. |
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PI Adverse Effects:
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Hyperglycemia
Hyperlipidemia Fat Redistribution Increased Liver Enzymes GI nausea, vomiting, Diarrhea. |
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Atazanavir A.E.:
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- PR interval prolongation of ECG.
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Ritonavir and Tipranivir combo:
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1. fatal and non-fatal intracranial hemorrhage
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Ritonavir and tipranivir:
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- hepatitis and hepatic decompensation
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ritonavir can cause;
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- crsytalluria, renal colic, nephrlithiasis.
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Fusion inhibitors:
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- Enfuviritide (Fuzeon)
binds to gp41 - given in combo with other drugs - protein binding is high. - |
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A.E. of Enfuviritide:
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- Local injection site reactions:
- Pneumonia - Allergic Reaction |