Prezista

Prezista contains a sulfa component and should be used with caution in patients with severe sulfa allergies. Most common side effects may include diarrhea, nausea, headache, rash, vomiting, and abdominal pain. Measure liver function before starting and then monitor, with perhaps closer monitoring for those with underlying liver problems, especially during the first several months. No dose adjustment necessary with mild to moderate liver disease, but Prezista + Norvir is not recommended for those with severe liver impairment. While very rare, severe rash (in 0.4% of those taking it), accompanied in some cases by fever and/or elevations of AST/ALT (liver enzymes), can be life-threatening. Seek medical attention immediately. When used with Tybost a small increase in serum creatinine (SCr) may be seen which does not translate to a decrease in kidney function. Observational cohort studies reported an association between some PIs (including darunavir) and an increased risk of cardiovascular (CV) events. Although some older PIs have been associated with liver toxicity, lactic acidosis, diabetes, or fat redistribution, these conditions are only rarely, or never, observed with darunavir. IRIS (immune reconstitution inflammatory syndrome) may occur as the immune system regains strength; signs and symptoms from previous infections may occur soon after HIV treatment is initiated. Report symptoms of illness, such as shingles or TB, to a health care provider. Protease inhibitors can cause increased risk for bleeding in hemophiliacs.

Prezista contains a sulfa component and should be used with caution in patients with severe sulfa allergies. Most common side effects may include diarrhea, nausea, headache, rash, vomiting, and abdominal pain. Measure liver function before starting and then monitor, with perhaps closer monitoring for those with underlying liver problems, especially during the first several months. No dose adjustment necessary with mild to moderate liver disease, but Prezista + Norvir is not recommended for those with severe liver impairment. While very rare, severe rash (in 0.4% of those taking it), accompanied in some cases by fever and/or elevations of AST/ALT (liver enzymes), can be life-threatening. Seek medical attention immediately. When used with Tybost a small increase in serum creatinine (SCr) may be seen which does not translate to a decrease in kidney function. Observational cohort studies reported an association between some PIs (including darunavir) and an increased risk of cardiovascular (CV) events. Although some older PIs have been associated with liver toxicity, lactic acidosis, diabetes, or fat redistribution, these conditions are only rarely, or never, seen with darunavir. IRIS (immune reconstitution inflammatory syndrome) may occur as the immune system regains strength; signs and symptoms from previous infections may occur soon after HIV treatment is initiated. Report symptoms of illness, such as shingles or TB, to a health care provider. Protease inhibitors can cause increased bleeding in hemophiliacs.

Drug interactions of Prezista + Norvir may be different than those for Prezista + Tybost. Of note, Tybost is not interchangeable with Norvir. Do not take with alfuzosin, cisapride, colchicine (in patients with kidney or liver impairment), dronedarone, ivabradine, lomitapide, lurasidone, naloxegol, ranolazine, pimozide, ergot derivatives, triazolam, oral midazolam, rifampin, Revatio, Xarelto, or St. John’s wort. Not recommended to be taken with everolimus and ticagrelor. Tramadol dose decrease may be needed. Monitor therapeutic effects and adverse reactions with use of some analgesics, such as fentanyl and oxycodone. Monitoring of clonazepam is recommended. Reduced dose of rifabutin is recommended. Do not use lovastatin or simvastatin, or co-formulations containing these drugs (Advicor and Vytorin). Cholesterol-lowering alternatives are rosuvastatin, atorvastatin (should not exceed 20 mg per day), pitavastatin, and pravastatin, but should be used with caution and started at the lowest dose possible. Monitor for increased side effects from these medications. Reduce clarithromycin dose by 50 to 70% in kidney impairment. The antifungal drugs itraconazole or ketoconazole should be used with caution (maximum dose is 200 mg per day for either). Voriconazole should not be used unless the benefits outweigh the risks. Prezista increases levels of nasal and inhaled fluticasone (found in Advair, Flonase, Breo Ellipta, Arnuity Ellipta, and Flovent) and budesonide, as well as systemic corticosteroids ciclesonide, betamethasone, dexamethasone, methylprednisolone, mometasone, and triamcinolone. Use alternative corticosteroid and monitor for signs of Cushing’s syndrome. Beclomethasone, prednisolone, and prednisone as alternative corticosteriods may be considered, particularly for long-term use. Effectiveness of oral contraceptives may be decreased; consider using alternative methods of contraception. Monitoring is recommended with methadone. Titration or decreased dose may be needed for buspirone, diazepam, estazolam, and zolpidem. Therapeutic drug monitoring is recommended for antiarrhythmics amiodarone, bepridil, disopyramide, flecainamide, systemic lidocaine, mexiletine, propafenome, and quinidine. Tell your provider or pharmacist about all medications, herbals, and supplements you are taking or thinking of taking, prescribed or not, as there are many other drug interactions not listed here.

Prezista, which is found in the single-tablet regimen Symtuza (see that page), is recommended as part of an initial regimen “in certain clinical situations” in DHHS guidelines. DHHS wrote this is “in part because of greater tolerability” with the integrase inhibitor medications compared to Prezista + Norvir or Prezcobix. There is growing evidence that a protease inhibitor-based regimen, boosted by ritonavir plus Epivir (lamivudine), can maintain viral suppression in patients who initiated triple-drug therapy, who achieved sustained viral suppression for at least 1 year, and who have no evidence of, or risk of resistance to, either darunavir or lamivudine. Use of Prezista with Norvir and Epivir may be a reasonable option when the continued use of TDF, TAF, or ABC is contraindicated or not desirable. Additionally, another ART switch strategy with some supporting evidence in patients with viral suppression in the DHHS guidelines is to switch patients to a boosted protease inhibitor + integrase inhibitor. In two small observational studies, patients were switched from their current ART regimens to Prezista + Norvir + Tivicay, and viral suppression was maintained in over 97% of participants. For patients on a complicated salvage regimen with current viral suppression and a history of treatment failure, there is evidence to support simplifying the regimen to a combination of Genvoya + Prezista. Prezista + Norvir is a preferred component in the DHHS perinatal guidelines for use in pregnancy. Prezista + Tybost is also found in the fixed-dose tablet Prezcobix.

Dr. Ross Slotten says:

First approved in 2006, Prezista has become the preferred PI because of its relative lower side effect profile, although GI symptoms like diarrhea remain a problem for that class of medications. Prezista has replaced Kaletra as the preferred PI. In treatment-naïve individuals, its 800 mg formulation can be taken once daily. For those individuals with underlying resistance to other PIs, Prezista should be taken twice daily in its 600 mg formulation in combination with other medications.

Activist Bridgette Picou says:

Prezista is considered a lipid-friendly drug. The action of certain medications may be increased or decreased because the metabolism of the booster component of a Prezista-based regimen takes place in the liver. Talk to your provider about all medications you take. Side effects can include nausea, diarrhea, and rash.