Standard DoseOne 800 mg tablet with 100 mg Norvir or 150 mg Tybost once daily with food for treatment-naïve people (those taking HIV therapy for the first time) and treatment-experienced adults without Prezista-related resistance. One 600 mg tablet with 100 mg Norvir twice daily with food for pregnant women and those who have at least one Prezista-related resistance mutation. Prezista should always be taken with Norvir or Tybost. Must also be taken in combination with another antiretroviral(s) which does not contain this medication or medication from the same drug class.
For adults and children 3 years of age and older weighing at least 22 pounds (10 kg).
Prezista for children is dosed based on weight. There are 75 mg and 150 mg tablets as well as an oral suspension (100 mg/mL) (strawberry cream flavor) available for children three and older and adults who can’t swallow pills.
Suspension needs to be taken with Norvir or Tybost, with food.
Take missed dose as soon as possible, unless it is closer to the time of your next dose. Do not double up on your next dose.
(800) JANSSEN (526-7736)
AWP800 mg tablets: $2,027.65/month
Potential Side Effects and Toxicity
• See package insert for more complete information on potential side effects and interactions.
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.
Potential Drug Interactions
Drug interactions of Prezista + Norvir may be different than those for Prezista + Tybost. Do not take with alfuzosin, dronedarone, colchicine (in patients with kidney or liver impairment), lomitapide, lurasidone, ranolazine, pimozide, ergot derivatives, triazolam, oral midazolam, rifampin, Revatio, Xarelto, or St. John’s wort. 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 now found in the recently approved 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 is also found in the fixed-dose tablet Prezcobix.
Dr. David Hardy says:
Approved in 2006, it is still the “newest” protease inhibitor (this tells you something about recent progress in this class of medications). It must always be given with a booster, Norvir (ritonavir) or Tybost (cobicistat), to be effective. It is approved to be given as a part of a first-time ART regimen dosed once-daily (800 mg tablet + booster) with two NRTIs or dosed twice-daily (600 mg tablet + booster) for PLWH whose HIV has some resistance to protease inhibitors. Its major side effects are nausea, queasiness, diarrhea, and rash. It is the first and only protease inhibitor that is now approved as part of an STR (see Symtuza).
Activist Moisés Agosto-Rosario says:
Darunavir is lipid-friendly and less likely to cause metabolic complications. If prescribed with Truvada, it is important to monitor kidney function and bone density. As with the other protease inhibitors, darunavir is metabolized by the liver; many drug-drug interactions can occur either increasing or decreasing drug levels, causing serious problems. Your doctor must be aware of all the medications you take even if they are over-the-counter or supplements.