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Vocabulary flashcards covering key Protease Inhibitor concepts, boosters, dosing considerations, side effects, and drug interactions from the notes.
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Protease inhibitors (PIs)
A class of antiretroviral drugs that inhibit HIV protease, blocking maturation of viral particles and late-stage viral replication.
Atazanavir (ATV)
A protease inhibitor used in HIV therapy; often boosted with cobicistat or ritonavir; brand names Reyataz and Evotaz.
Darunavir (DRV)
A protease inhibitor used in HIV therapy; boosted with ritonavir or cobicistat; brand names Prezista and Prezcobix.
Lopinavir/ritonavir (LPV/r)
Fixed-dose protease inhibitor boosted with ritonavir; brand Kaletra; tablets can be taken with or without food; the oral solution should be taken with food.
Ritonavir (RTV)
A protease inhibitor primarily used as a pharmacokinetic boost for other PIs; potent inhibitor of cytochrome P450; ritonavir is typically taken with food for optimal absorption (Kaletra tablets exception).
Boosters (ritonavir or cobicistat)
Agents that inhibit metabolism of a co-administered PI to raise its blood levels and boost efficacy.
Boosted PI therapy advantages
Higher PI levels may overcome resistance, allow lower doses, and reduce pill burden and dosing frequency.
Take with food (ritonavir)
Ritonavir must be taken with food for optimal absorption.
Kaletra dosing and food
Kaletra tablets can be taken with or without food; Kaletra oral solution should be taken with food.
Liver impairment precautions
All protease inhibitors carry precautions about potential liver impairment or worsening existing liver disease.
Lipodystrophy
Cosmetic fat redistribution syndrome seen with PIs, including changes in fat distribution.
Lipohypertrophy
Central fat accumulation (e.g., dorsal fat pad, larger abdomen, breast growth in women); likely related to the protease inhibitor component.
Lipoatrophy
Peripheral fat wasting (face, buttocks, arms, legs); more likely related to an NRTI used in the regimen.
Fat redistribution with darunavir
Fat redistribution is seen less frequently with darunavir.
Metabolic risks of PIs
PIs may increase risk of diabetes (or worsen existing diabetes), high cholesterol, and possibly heart disease.
Cytochrome P450 interactions
PIs are inhibitors and inducers of the cytochrome P450 system; ritonavir is the most potent inhibitor; interactions can be exploited therapeutically for boosting but require care.
Drug interactions management
A thorough review of potential drug interactions with a pharmacist is recommended before adding new medications.