atazanavir, or ATV atazanavir sulfate
Standard DoseFor most treatment-naïve (first time on HIV therapy) and treatment-experienced individuals, the dose is one 300 mg capsule plus 100 mg Norvir or 150 mg Tybost once daily with food. Must be taken in combination with another antiretroviral(s) which does not contain this drug or medication from the same drug class. See package insert for dosing recommendations during pregnancy, liver or kidney impairment, and with certain drug interactions. Capsules also available in 150 mg and 200 mg. Take Norvir or Tybost at same time as Reyataz. Pediatric dose with 50 mg oral powder available based on body weight for children at least 3 months of age weighing at least 11 pounds (5 kg).
Take missed dose as soon as possible, unless it’s closer to the time of your next dose. Do not double up on your next dose. Swallow capsules whole—do not open or mix with anything. Oral powder may be used by adult patients who cannot swallow the capsules.
See package insert for more complete information on potential side effects and interactions.
AWP300 mg, 30 capsules: $1,739.30/month
Generic atazanavir 300 mg, 30 capsules: $1,652.33/month
Potential Side Effects and Toxicity
Most common side effects may include nausea, ocular icterus (yellowing of the skin or eyes as a result of increased bilirubin levels), jaundice, and rash. The ocular icterus and jaundice were reversible on discontinuation of the drug. Other less common side effects may include kidney stones, gallstones, abnormal heart rhythm, and elevated liver enzymes (more common in people with hepatitis B or C). Capsules do not contain phenylalanine but oral powder does; thus, use with caution in individuals with phenylketonuria (PKU). Kidney laboratory testing should be performed in all patients prior to initiation of Reyataz and continued during treatment. Renal laboratory testing should include serum creatinine, estimated creatinine clearance, and urinalysis with microscopic examination. Rarely, chronic kidney disease has been observed.
Observational cohort studies reported an association between some PIs (including darunavir, found in Prezista and Prezcobix, and lopinavir/ritonavir, brand name Kaletra) and an increased risk of cardiovascular (CV) events; however, this has not been observed with Reyataz (atazanavir, or ATV). Another observational cohort study of predominantly male participants found a lower rate of cardiovascular events in those receiving atazanavir-containing regimens compared with other regimens. Further study is needed.
Potential Drug Interactions
Do not use with alfuzosin, rifampin, irinotecan, ergot derivatives, triazolam, oral midazolam, St. John’s wort, Revatio, or Viramune (nevirapine). Do not use lovastatin, simvastatin, or co-formulations containing them (Advicor and Vytorin) for treatment of high cholesterol. Alternatives for these are atorvastatin, rosuvastatin, pravastatin, pitavastatin, and fluvastatin, but should be used with caution and started at the lowest dose possible; monitor for increased side effects. Of note, Tybost is not interchangeable with Norvir. Proton pump inhibitors (PPIs, like Aciphex, Dexilant, Nexium, Protonix, and Prevacid) and H2-receptor antagonists (H2RAs, like Pepcid, Zantac, and Tagamet) can stop Reyataz from being absorbed. Treatment-experienced people should not take PPIs while on Reyataz. See package insert for antacid dose adjustment. If taking chewable antacids like Rolaids and Tums, take Reyataz with food two hours before or one hour after. Treatment-experienced people should not take Reyataz with Sustiva. Viread decreases the levels of Reyataz and Reyataz/Norvir increases Viread levels; monitor for adverse events. Reyataz can be taken unboosted with Epzicom if absolutely necessary. Bepridil, amiodarone, quinidine, and lidocaine should be used cautiously because of the risk of worsening abnormal heart rhythm. Close monitoring is required when used with warfarin. Calcium channel blockers should be monitored. Use caution when using the antifungals itraconazole or ketoconazole. Voriconazole is not recommended. Reducing dose and frequency of rifabutin to 150 mg every other day or three times a week is recommended. Reyataz + Norvir increases levels of fluticasone (found in Advair, Flonase, and Flovent); monitor for signs of Cushing’s syndrome. An alternative corticosteroid is recommended. Reyataz can be taken with birth control pills that contain no more than 30 mcg of ethinyl estradiol if taking Reyataz without Norvir and at least 35 mcg if taken with Norvir. Use caution with carbamazepine, phenobarbital, and phenytoin. ED drugs should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours. A lower dose of trazodone is recommended. Use with caution with bosentan, salmeterol, and immunosuppressants, and use lower dose of colchicine. Use with Norvir when taking buprenorphine; monitor for sedation. Do not take with Zepatier. Reyataz/Norvir is not recommended with Harvoni if tenofovir DF (TDF, in Truvada) is part of HIV regimen. With Epclusa, monitor for tenofovir toxicities if TDF is part of HIV regimen. 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.
Yellowing of the eyes and skin is a common reason for discontinuation. Reyataz plus Norvir and 2 NRTIs is still recommended as a preferred regimen during pregnancy. Reyataz plus Tybost (Evotaz) is not recommended during pregnancy. Maintaining adequate hydration is important with Reyataz. Reyataz + Norvir + Epzicom is no longer included in the list of “Recommended Initial Regimens in Certain Clinical Situations” because it has disadvantages when compared with other regimens in this category.
Dr. Ross Slotten says:
Reyataz or atazanavir was first approved in 2003 as an alternative PI to Kaletra because of ease of administration and better tolerance. It can be given with or without a booster, although without a booster, there is greater risk of resistance. However, Reyataz was eventually eclipsed by Prezista in part because it causes jaundice in 10 percent of patients. I don’t mean just yellow eyes; I mean quite striking yellow skin like someone with acute hepatitis, although the rise in bilirubin—the cause of the jaundice—is not due to liver impairment. Like its forebear Crixivan (indinavir), it can crystalize in the kidneys and cause kidney stones, another unpleasant adverse effect. Despite a B1 rating by the DHHS expert panel when combined with TDF/FTC, what role boosted atazanavir will have in the future is unclear. It is likely to follow Kaletra to the pharmaceutical graveyard.
Activist Bridgette Picou says:
Reyataz, or atazanavir, is taken with other HIV medications and is a lipid-friendly protease inhibitor. Atazanavir may cause an increase in bilirubin, which can cause your eyes or skin to appear yellow. This a harmless side effect and usually disappears after stopping the medication. Know that you should talk about use of acid reflux medication with your doctor as these may prevent full absorption of Reyataz.