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Prezista and Prezcobix

darunavir DRV Protease inhibitor;800 mg darunavir, 150 mg cobicistat DRV (PI), COBI (PK booster)
HHS recommended as a component of initial regimen in certain clinical situations
Standard Dose
Prezista: Two different doses available. One 800 mg tablet + 100 mg Norvir or 150 mg Tybost once daily with food for treatment-naïve people (people taking HIV therapy for the first time) and treatment-experienced adults without Prezista-related resistance. 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 flavored) available for children age 3 and older and for adults who can’t swallow pills. One 600 mg tablet + 100 mg Norvir twice daily with food for pregnant individuals and for people who have at least one Prezista-related resistance mutation. Prezista should always be taken with Norvir or Tybost. Suspension needs to be taken with Norvir or Tybost, with food. Suspension should be shaken before each use and stored at room temperature. Do not refrigerate.

Prezcobix: One tablet once daily with food, for people with no darunavir-associated drug resistance, including both treatment-experienced and treatment-naïve individuals. For adults and children weighing at least 88 pounds (40 kg). Prezcobix is only available for people taking darunavir once daily, not individuals who require darunavir twice daily. It is not recommended to co-administer Prezcobix with tenofovir disoproxil fumarate with creatinine clearance (CrCl) less than 70 mL/min.

Must also be taken in combination with another antiretroviral(s) from a different drug class. Do not use either drug in people with severe liver impairment. Take missed dose as soon as possible, as long as it is at least 12 hours before your next dose. Do not double up on your next dose.
  • Generic and brand name available for 600 mg and 800 mg oral tablets. Brand available only for 75 mg and 150 mg oral tablets and 100 mg/mL oral suspension.
  • For people who took Apretude (CAB-LA) for PrEP, HHS recommended as a component for rapid ART for someone newly diagnosed or entering care with minimal or no labs available.
  • See package insert for more complete information on potential side effects and interactions. 
Manufacturer
Janssen Therapeutics
prezista.com
(800) JANSSEN (526-7736)
AWP
Prezista AWP
600 mg, 60 tablets: $2,514.35/month
800 mg, 30 tablets: $2,514.35/month

Prezcobix AWP
$2,873.84/month
Activist Comments

JUAN MICHAEL PORTER II:

Prezista (darunavir) is an incredibly potent protease inhibitor that works well for treatment experienced and naïve people, so long as they don’t have prior drug resistance. Prezcobix is darunavir boosted with cobicistat. People I know who’ve used either drug have switched treatment for various reasons, though none of them had any complaints. Though viable, there are better options available.

Doctor Comments

JO-ANN JOSE, MD, MPH:

Darunavir has an important role in treatment management for people with significant virus mutations, especially integrase mutations. Prezcobix cannot be used in pregnancy because of the booster. 

Potential Drug Interactions

Many drug interactions are possible due to the need for cobicistat or ritonavir; see package insert. Tybost is not interchangeable with Norvir. Do not take with alfuzosin, dronedarone, ergot derivatives, ivabradine, lomitapide, lurasidone, naloxegol, pimozide, triazolam, oral midazolam, ranolazine, rifampin, Revatio, St. John’s wort or Zepatier. Do not use lovastatin or simvastatin, or co-formulations. Alternatives are atorvastatin and rosuvastatin (dose of either should not exceed 20 mg per day). If also taking Selzentry, Selzentry dose should be 150 mg twice a day. Not recommended with avanafil, rifapentine, rivaroxaban or salmeterol. Erectile dysfunction drugs should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours or 25 mg Viagra per 48 hours. Titration or decreased dose may be needed for buspirone, diazepam, estazolam and zolpidem. Therapeutic drug monitoring is recommended for amiodarone, bepridil, disopyramide, flecainamide, systemic lidocaine, mexiletine, propafenone and quinidine. Take lower dose of colchicine, but do not use colchicine if there is renal (kidney) or hepatic (liver) impairment. 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: Not recommended with everolimus, or ticagrelor, or with irinotecan. Monitoring of clonazepam, phenytoin and phenobarbital is recommended. Tramadol dose decrease may be needed. Monitor therapeutic effects and adverse reactions with use of some analgesics, such as fentanyl and oxycodone. Reducing dose of rifabutin is recommended. Pitavastatin may be used with no dose adjustment, but pravastatin should be used with caution and started at the lowest dose possible. Monitor for increased side effects from these medications. Reduce clarithromycin dose by 50–75% in kidney impairment. Isavuconazole, posaconazole, ketoconazole and itraconazole should be used with caution (maximum dose is 200 mg per day for ketoconazole and itraconazole). Voriconazole should not be used unless the benefits outweigh the risks. Effectiveness of oral contraceptives may be decreased. Increases the exposure of nasal and inhaled fluticasone 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 corticosteroids may be considered. Monitoring is recommended for co-administration with drospirenone or colchicine. Monitoring is recommended with buprenorphine, buprenorphine/naloxone and methadone.

Prezcobix: Do not take with carbamazepine, dexamethasone, phenytoin or phenobarbital or with colchicine (in people with kidney or liver impairment). Not recommended to be taken with betamethasone, budesonide, ciclesonide, everolimus, fluticasone, Mavyret, methylprednisolone, mometasone, rifapentine, salmeterol, ticagrelor, triamcinolone or voriconazole. Monitor for lack of virologic response when eslicarbazepine or oxcarbazepine is needed. Initiation or dose adjustments of insulin or oral hypoglycemic medications may be required for some individuals. Start metformin at lowest dose and titrate based on tolerability and clinical effect. Apixaban dose may need to be adjusted.

Potential Side Effects and Toxicity

Darunavir should be used with caution by people with known severe sulfonamide allergy. Side effects may include diarrhea, nausea, headache, rash, vomiting and abdominal pain. While very rare, severe rash can be accompanied by fever and/or elevations of liver enzymes, and can be life-threatening. Seek immediate medical attention. IRIS (immune reconstitution inflammatory syndrome) may occur as the immune system regains strength. Report symptoms of illness to a health care provider. Protease inhibitors can cause increased risk for bleeding in hemophiliacs. Measure liver function before starting darunavir and then monitor. No dose adjustment necessary for darunavir with mild to moderate liver disease.

More Information

Darunavir is found in the single-tablet regimen Symtuza. A darunavir regimen is the preferred, and only, recommended initial treatment in people with acute or recent HIV infection who have a history of using Apretude for PrEP, taken with Descovy or Truvada. Cobicistat should not be used in pregnancy; the ritonavir booster should be used. Pregnant individuals can voluntarily enroll in the Antiretroviral Pregnancy Registry through their provider; GO TO apregistry.com.