Reyataz
Protease Inhibitor
Common Name: atazanavir sulfate (ATV)
Brand Name: Reyataz
Class: HIV protease inhibitor (PI)
Standard dose: One 300 mg capsule plus 100 mg Norvir, once daily (this dose must be used if taking Viread or Truvada), or two 200 mg capsules, once daily; take with food. Also available in 100 mg and 150 mg capsules. Take missed dose as soon as possible, but do not double up on your next dose.
AWP: $927.14 / month 150 mg, 200 mg, or 300 mg capsules
Manufacturer contact: Bristol-Myers Squibb,
www.reyataz.com, 1 (800) 321-1335
AIDSInfo:
1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
Potential side effects and toxicity: Dizziness and lightheadedness. Elevated levels of unconjugated bilirubin (produced by the liver) were reported in studies. This may result in cases of jaundice (yellowing of the skin or eyes), reported in 4-9% of individuals taking Reyataz. However, no evidence of liver problems was reported. Nevertheless, report jaundice to your health care provider right away. Other side effects may include rash, kidney stones, and elevated liver function enzymes, a sign of liver damage; this may be more common in people with hepatitis B or C.
As seen with other protease inhibitors (except unboosted Reyataz), there can be increased levels of cholesterol and triglycerides which may be associated with an increased risk of heart disease. However, if Reyataz is boosted with Norvir these same changes in cholesterol and triglycerides may occur. Other possible side effects seen with protease inhibitors are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts and sometimes the upper back), changes in heart rhythm, onset of new cases or worsening of diabetes (see your doctor promptly), and increased bleeding in hemophiliacs. Immune Reconstitution Inflammatory Syndrome (IRIS) may occur as the immune system regains strength; report symptoms of illness, such as shingles and TB, to health care provider.
Potential drug interactions: Treatment-experienced people cannot take with proton pump inhibitors (PPIs—long-acting medicine for acid reflux). Treatment-naïve people can take no more than 20 mg a day of the PPI Prilosec-OTC (or the equivalent thereof) 12 hours before their Reyataz/Norvir. Pepcid may be taken (no more than 20 mg twice a day if treatment-experienced or 40 mg twice a day if treatment-naïve, or equivalent doses) at the same time as Reyataz/Norvir (before the antacid has started to work) or at least 10 hours later. If taking with Viread or Truvada and Pepcid, you must take them with the 400 mg Reyataz/100 mg Norvir dose for treatment-experienced people. When taking Reyataz without Norvir, dose can be taken at least two hours before and at least 10 hours after Pepcid, Zantac, or Axid. Reyataz should be taken two hours before or one hour after antacids (Rolaids, Tums, and Mylanta). Do not take with rifampin, Camptosar (irinotecan), oral Versed (midazolam), Halcion, ergot derivatives (such as Cafergot, Wigraine, Methergine, and D.H.E. 45), pimozide, Crixivan, or St. John’s wort. Do not use simvastatin, Vytorin, or lovastatin; lipid-lowering alternatives are Lipitor, Lescol, and pravastatin, but they should be used with caution due to potential for liver toxicity.
Must be taken two hours apart from Videx, due to Videx’s buffer, and must take Videx EC an hour before or two hours after Reyataz (unless taking Videx EC with Viread). Treatment-naïve people should take 400 mg Reyataz and boost with Norvir (100 mg) when taking in combination with Sustiva. HIV treatment-experienced people should not use Reyataz with Sustiva. Viread decreases the concentration levels of Reyataz. In addition, Reyataz increases Viread concentrations, which could increase Viread-associated adverse events, including kidney disorders. The FDA suggests those taking Reyataz and Viread should be monitored for Viread-associated adverse events. The heart medications bepridil, Cordarone, quinidine, and lidocaine should be used cautiously. Monitoring may be required when used with Coumadin or immunosuppressants. Increased levels of the inhaled and nasal sprays with fluticasone (found in Advair, Flonase, and Flovent) can occur and should be used with caution. Effectiveness of birth control pills may decrease, consider the use of alternative or additional contraception. Oral contraception should contain no more than 30 mcg of ethinyl estradiol if taking Reyataz without Norvir and and at least 30 mcg if taken with Norvir. Use caution when using itraconazole or ketoconazole. Vfend is not recommended. Reduced dose and frequency of rifabutin to 150 mg every other day or three times once a week is recommended.
Cialis, Levitra, and Viagra levels are increased; doses should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours. Calcium channel blockers should be monitored. A lower dose of trazodone is recommended.
Tips: Boosted Reyataz is one of the four protease inhibitors recommended by the U.S. HIV treatment guidelines for people on antiviral therapy for the first time, and probably the most popular of the four. Needs an acidic environment, so take it with food. Please see package insert for more complete potential side effects and interactions.
Doctor
Reyataz (atazanavir) was approved (two 200 mg capsules once daily) for use in combination with other antiretroviral drugs in the treatment of HIV infection in 2003. Atazanavir was the first protease inhibitor to be approved for once-daily dosing. This was a “wow” moment—a protease inhibitor taken once daily. All those pioneer patients who suffered (some lost their lives) through endless pill numbers and multiple dosing schedules smiled. Atazanavir is generally boosted with low dose ritonavir, although I do use unboosted atazanavir with Epzicom in a few of my patients. The HAART regimen of atazanavir/Truvada/ritonavir (three pills once daily) is frequently used in our clinic. Atazanavir is a well tolerated antiretroviral medication, but there are two issues of concern—yellow discoloration of the skin and eyes and the potential for elevated bilirubin levels in blood. Both are benign problems. Those individuals who do get the skin changes, however, don’t appreciate the yellow hue (the most common reason for stopping atazanavir). I am usually not that concerned about an elevated bilirubin in the blood, but it can cause confusion for health care workers if gallbladder disease is an issue or the patient has hepatitis C. We have seen one patient in our clinic with an atazanavir kidney stone. Elevated lipid levels (as seen with other PIs) are not a common issue with atazanavir usage, and most prefer this drug if lipids are a problem. Atazanavir has been a huge step forward in HAART therapy and many patients have taken advantage of it. —Frank M. Graziano, M.D., Ph.D.
Activist
Reyataz, when boosted with Norvir, is the only once-a-day “preferred” DHHS guidelines PI-based treatment option. Unlike most other PIs, Reyataz doesn’t seem to raise cholesterol and triglyceride levels, and a study has shown that it may even increase “good” cholesterol (HDL), thus offering protection against heart disease. On the down side, it can cause hyperbilirubinemia, a fancy word for jaundice, or yellowing of the skin or eyes. Jaundice is benign, it just ain’t pretty; fortunately, it only affects a relatively small percentage of people and goes away when the drug is no longer taken. —Morris Jackson
