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Protease Inhibitors
Antiretroviral
| Question | Answer |
|---|---|
| protease inhibitors (PI) | inhibit HIV enzymes for maturation of HIV to a fully functional virus = produce immature nonfunctional, non infectious virus; no activation, affected by food, short half live, high PRO binding, inhibit CYP3A4(high drug-drug interactions) |
| Protease | responsible for cleaving immature budding particles to produce final structural proteins of the mature virion core |
| Protease mutations | broad resistance to substitutions at the 10, 46, 54, 82, 84, and 90 codons |
| Protease adverse events | dyslipidemia, lipodystropy, hyperglycemia, dorsocervical fat enlargement(buffalo hump), central obesity,peripheral/facial wasting, breast enlargement,cushing appearance, GI effects |
| Can lead to redistribution and accumulation of body fat | protease inhibitors |
| Cushing appearance | protease inhibitors |
| Protease inhibitors | atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir |
| Ritonavir | PI, boosting effect,metabolize in liver, inhibit CYP3A4(high drug-drug interactions), 3-5 hrs,NVD, paresthesias, HA, altered taste, abdpain,increase creatine kinase, long QT/PR |
| Atazanavir | PI, need light meal to increase PO absorption, need acidic medium for absorption, excretion:liver(biliary), NVD, abdpain,HA,skin rash, peripheral neuropathy, nephrolithiasis, DO NOT CAUSE FAT REDISTRIBUTION(RITONAVIR), long PR/QT/AV block, avoid with PPI |
| Darunavir | PI, must be co-administered with Ritonavir (booster), NVD,HA,rash,dyslipidemia,hepatotoxcitiy, severe hepatitis, increase amylase/lipase, caution w/pts w/sulfonamide allergy r/t contains sulfa component, inhibit CYP3A4 |
| Fosamprenavir prodrug of amprenavir | PI, take w/food or not(no fatty foods), administer in combo w/low dose ritonavir, long halflife,metabolize in liver by CYP3A4, HA,NVD,rash,depression,perioral paresthesias, inducer/inhibitor of CYP3A4,contains sulfa,vitamin E,propylene glycol(use caution) |
| Indinavir | PI,acidic,take on empty stomach or w/small lowfat/PRO meal,excreted fecal,indirect hyperbilirubinemia/nephrolithiasis, insulin resistance,thrombocytopenia,NVD,insomnia,dry throat,dry skin, consume 48oz of water daily to maintain hydration, inhibit CYP3A4 |
| Lopinavir | PI, used combo w/ritonavir, take w/ food, highly PRO bound, half-life 5-6hrs, metabolize by CYP34(inhibited by ritonavir), NVD,abdpain,asthenia,increase TG/cholesterol |
| Nelfinavir | PI, high absorption, metabolism CYP3A, excreted feces, highly PRO-bound, half-life 3.5-5hrs,diarrhea/flatulence, inhibit CYP3A, good for PG women |
| Saquinavir | PI, take 2 hrs after fatty meal, half-life 2 hrs, protein-bound, excreted in feces, NVD, abd pain, dyspepsia, rhinitis,long QT/PR, first pass metabolism by CYP3A4, check LFT |
| Tipranavir | PI, new, combo w/ritonavir, poor absorption, but increase w/fatty meal, metabolize by liver, contains sulfa, NVD, abdpain, rash, liver toxicity, intracranial hemorrhage, depression, increase amylase, decrease WBC, inhibit and induce CYP3A4 |
Created by:
cburrows
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