atazanavir sulfate (ATV)
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) 272–4878
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 7–9% of individuals taking Reyataz. However, no evidence of liver problems was reported. These symptoms may go away after about two weeks or after you stop taking Reyataz. Other side effects include rash, kidney stones, and elevated liver function tests, a sign of liver damage; this may be more common in people with hepatitis B or C.
As seen with other protease inhibitors, there can be increased levels of cholesterol and triglycerides (except possibly unboosted Reyataz) 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 a day if treatment-experienced or 40 mg 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 400 mg Reyataz /100 mg Norvir. 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), Versed, 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). Boost with Norvir (100 mg) when taking in combination 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 receiving Reyataz and Viread should be monitored for Viread-associated adverse events. The heart medications Tambocor, Rythmol, 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. Use caution when using itraconazole or ketoconazole. Vfend is not recommended. Reduce dose and frequency of rifabutin to 150 mg once a day.
Cialis, Levitra, and Viagra levels are increased; doses should not exceed 10 mg Cialis per 72 hours, 2.5 mg Levitra per 24 hours, or 25 mg Viagra per 48 hours. Medications used for seizures such as carbamazepine, Dilantin (phenytoin), or phenobarbital may decrease Reyataz levels and alternate seizure medications should be used. The blood pressure medications called calcium channel blockers should be monitored for side effects because Reyataz may increase levels of these medications. Also increased levels of trazodone can occur with Reyataz. A lower dose of trazodone is recommended.
Tips: Reyataz/Norvir is now one of the three protease inhibitors recommended by the U.S. HIV treatment guidelines for people on antiviral therapy for the first time. May be an option for patients with cholesterol problems. Needs an acidic environment, so take it with food. Please see package insert for more complete potential side effects and interactions.
Atazanavir is now the easiest and best tolerated of the PIs. Whether it’s given boosted or unboosted, the dose is just two pills per day. It’s easy on the tummy and doesn’t raise lipids or cause insulin resistance as much as some other PIs do. Its biggest drawback is that it needs stomach acid to get absorbed, which is a problem if you’re taking medications that lower stomach acid to treat heartburn, ulcers, or reflux. If you’re taking Reyataz with a proton pump inhibitor (Prilosec, Nexium, Protonix, Prevacid and Aciphex), antacids or H2 blockers (Tagamet, Zantac, Pepcid, etc.), you have to separate the doses carefully. The other problem is jaundice—a small fraction of people who take Reyataz will develop yellow eyes or skin. This is a completely harmless side effect, but it’s probably not the “look” you were going for. When that happens, it usually requires a switch to a different drug. There have been recent reports of kidney stones with Reyataz, though this is far less common than with Crixivan.—Joel Gallant, M.D.
Reyataz offers some advantages over earlier drugs. It is not completely cross resistant with other drugs of this class, meaning it can work despite the presence of some resistance mutations. Perhaps more importantly, it was the first protease inhibitor that seems to cause less disturbance of cholesterol processing by the body. It can, however, cause a type of liver problem that results in jaundice (yellowing of the skin or eyes), though this is seen in less than 10% of users. The problem corrects itself quickly when a person is taken off the drug. —Martin Delaney