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16 Cards in this Set

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Know the NRTIs:
- 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.
Resistance to NRTIs AND a.e.?
- from RT mutations.
A.E.: LACTIC ACIDOSIS, HEPATIC STEATOSIS.
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.
Drug-Drug Interactions:
- Stavudine + Zidovudine = intracellular activation.
- Lamivudine + Zalcitabine = interfering with its phosphorylation.
- Ethanol + abacvir = increase conc.
- Didanosin + zalcitabine = increase peripheal neuropathy.
NNRTIs MOA:
- Block RT activity by binding adjacent to the enzyme's binding site -> induces conformational changes.
- metabolized by CYP 450
NNRTIs drug names:
- Nevirapine (Viramune)
- Delavirdine (Rescriptor)
- Efavirenz (Sustiva)
Most common A.E. for all NNRTIS?
RASH.

Nevirapine: Stevens-Johnsons Syndrome and hepatitis.

Efavirenz: HA, dizziness, abnormal dreams, impaired conc., PSYCHIATRIC DISTURBANCES.
- tetrogenic
- increased liver enzymes

Delavirdine: increased liver enzymes.
Protease Inhibitors: (avir)
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.
PI:
- poor oral bioavailability
- all under go metabolism by CYP3A4 and p-glycoprotein
- extensivily binds to plasma protein.
PI Adverse Effects:
Hyperglycemia
Hyperlipidemia
Fat Redistribution
Increased Liver Enzymes
GI nausea, vomiting, Diarrhea.
Atazanavir A.E.:
- PR interval prolongation of ECG.
Ritonavir and Tipranivir combo:
1. fatal and non-fatal intracranial hemorrhage
Ritonavir and tipranivir:
- hepatitis and hepatic decompensation
ritonavir can cause;
- crsytalluria, renal colic, nephrlithiasis.
Fusion inhibitors:
- Enfuviritide (Fuzeon)
binds to gp41
- given in combo with other drugs
- protein binding is high.
-
A.E. of Enfuviritide:
- Local injection site reactions:
- Pneumonia
- Allergic Reaction