Potential side effects and toxicity: Most common include: dizziness and lightheadedness. Elevated levels of unconjugated bilirubin (produced by the liver) was reported in clinical trials in some individuals taking Reyataz. This may result in cases of jaundice (yellowing of the skin or eyes, darkening of the urine, or itching skin), reported in 7–9% of individuals taking Reyataz. However, no evidence of hepatoxicity (liver problems) was reported. These symptoms usually go away after about two weeks or after you stop taking Reyataz, and seldom return on re-initiation.
All other protease inhibitors are associated with increased levels of cholesterol and triglycerides, except possibly unboosted Reyataz and these increased levels may be associated with heart disease. However, if Reyataz is boosted with Norvir these same changes in cholesterol and triglycerides may occur. Other possible side effects as seen in other PIs 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), onset of new cases or worsening of diabetes (see your doctor promptly) and increased bleeding in hemophiliacs.
Potential drug interactions: Do not take with proton pump inhibitors (PPIs—long-acting medicine for acid reflux): Prilosec-OTC, Prevacid, Aciphex or Nexium. May be taken 12 hours apart from short-acting acid reflux medications (H2 inhibitors or blockers) like Zantac and Axid. Antacids like Mylanta must be taken at least two hours apart from Reyataz. 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, due to food restrictions (unless taking Videx-EC with Viread). Boost with Norvir (300 mg Reyataz with 100 mg Norvir) when taking in combination with Sustiva. Viread decreases the concentration levels of Reyataz. In addition, Reyataz increases Viread concentrations. Higher Viread concentrations could increase Viread-associated adverse events, including renal disorders. The FDA suggests those receiving Reyataz and Viread should be monitored for Viread-associated adverse events. When co-administered with Viread, it is recommended that Reyataz 300 mg is given with Norvir 100 mg (all as a single daily dose with food). Reyataz without Norvir should not be taken with Viread. Do not take with Tambocor, Rythmol, Versed, Halcion, Hismanol, Seldane, rifampin, ergot derivatives (such as Cafergot, Wigraine and Methergine, D.H.E. 45, in any form—serious interactions seen with dilation during gynecological exams), garlic supplements, and the herb St. John’s wort. Reduce dose and frequency of rifabutin to 150 mg once a day. Do not use Zocor or Mevacor; lipid-lowering alternatives are Lipitor, Lescol, and Pravachol, but they should be used with caution due to potential for liver toxicity.
Tips: Not recommended for people with previous PI treatment failure. Needs an acidic environment, so take it with food. Reyataz is the only PI leading to the 150L mutation, indicating a lack of cross-resistance to other PIs. Avoid Crixivan because of the increased potential for jaundice.
Doctor
Atazanavir was the first protease inhibitor to be approved as a once-daily agent. The convenience of fewer pills once a day gave it a distinct advantage over prior PIs. In recent studies, boosting it with a small dose of ritonavir has shown it to be as potent in viral suppression and immune reconstitution as Kaletra. The durability and resistance data are less clear, only because the drug has not been available in clinical study as long as Kaletra. Another advantage Reyataz has over other PIs is its side effect profile. It tends to cause less GI distress (many people believe the booster dose of ritonavir causes most of the problems). It is touted as being “lipid neutral,” meaning that unlike other PIs, it doesn’t raise triglycerides or total cholesterol. The main side effect is jaundice (yellowing of the skin or eyes) which occurs in less than 10% of people who take it. This does not require discontinuation of the drug, and usually will resolve if the drug is stopped. An important addition to the label now warns this drug cannot be used at the same time as proton pump inhibitors, and should be used with caution with H-2 blockers. Reyataz requires an acidic environment in the stomach for absorption and proton pump inhibitors and H-2 blockers work by reducing acid production in the stomach.—Chad J. Zawitz, MD
Activist
The new darling in the PI class. It is taken once a day, does not have food restrictions and has little effect on lipids. If you are taking antacids or PPIs, you need to talk to your doctor, since many of them are contraindicated with Reyataz. Also, many people have increases in bilirubin that may make them jaundiced. As an activist, I have been concerned about how BMS priced this expensive PI and how they have marketed this drug by implying it does not cause lipodystrophy. The price is the highest for a protease inhibitor and set the tone for all drugs approved later, so it was a terrible hit to publicly funded programs. Also, there is not a single study that proves that Reyataz does not cause lipodystrophy. Actually, Reyataz showed the same high incidence of lipodystrophy as Viracept (a well-known PI that can cause lipo). Just because this drug may not have the negative lipid effects caused by most PIs, it does not mean that it may not cause fat accumulation. If it was that easy, lipid lowering drugs could prevent or reverse lipo, and they have not shown to do that! I would love to see lipo data on Reyataz/Norvir + Truvada, a popular once a day combo that doctors prescribe hoping that it does not cause body changes. Reyataz is here to stay and growing stronger as more comparison data against Kaletra are generated.—Nelson Vergel
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