Two 200 mg capsules once daily

Brand name: Reyataz

Common name: atazanavir sulfate

Class: HIV protease inhibitor (PI)

Standard dose: Two 200 mg capsules once daily, take with food. Treatment-experienced people should take 300 mg with 100 mg Norvir once daily. 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: $846.92 for 200 mg, 60 capsules

Manufacturer contact: Bristol-Myers Squibb, www.reyataz.com, 1 (800) 272–4878

AIDS Treatment Information Service: 1 (800) HIV–0440 (448–0440)

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), 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 (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 an hour apart from Videx, due to Videx’s buffer. Boost with Norvir (300 mg Reyataz with 100 mg Norvir) when taking in combination with Sustiva. With Fortovase, use six Fortovase capsules with 400 mg Reyataz once-a-day with a high-fat meal (further efficacy and safety information is needed).

Viread decreases the concentration levels of Reyataz. In addition, Reyataz increases Viread concentrations. The reasons for these interactions are not fully understood. Higher Viread concentrations could increase Viread -associated adverse events, including renal disorders. The FDA suggests that patients receiving Reyataz and Viread should be monitored for Viread-associated adverse events. When coadministered with Viread, it is recommended that Reyataz 300 mg is given with Norvir 100 mg and Viread 300 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 (simvastatin) or Mevacor (lovastatin); lipid-lowering alternatives are Lipitor (atorvastatin), Lescol, and Pravachol (pravastatin), but they should be used with caution due to potential for liver toxicity.

Protease inhibitors increase blood levels of Viagra (sidenafil citrate), Cialis (tadalafil) and Levitra (vardenafil). Use with caution. Initially the Viagra dose should be 12.5 mg (1/2 of 25 mg tablet) and increased as needed and tolerated. It’s recommended that people on PIs do not exceed 25 mg of Viagra in a 48-hour period because of potential for serious reaction. Use Cialis at reduced doses of 10 mg every 72 hours and Levitra at reduced doses of no more than 2.5 mg every 72 hours, with increased monitoring for adverse events.

Tips: Not recommended for people with previous PI treatment failure. Unconjugated bilirubin is not associated with either disease or liver toxicity, the usual cause of jaundice. Needs an acidic environment, which you get from taking it with food. Study is underway to see if a Videx dose adjustment is needed. Reyataz, approved in June 2003, is the second-newest protease inhibitor on the market. Reyataz is the only protease inhibitor shown to lead to the 150L mutation in HIV. This indicates a lack of cross-resistance to other protease inhibitors. The manufacturer does not recommend that it be taken with Crixivan because of the increased potential for jaundice.

Doctor
Reyataz is the newest PI, having been approved for use in 2003. Its main advantage is its convenience. Although it can be prescribed as two pills once a day, many practitioners prefer to boost it with Norvir. Recent studies suggest that boosted Reyataz is equal in potency to Kaletra. Boosted or unboosted, Reyataz has minimal impact on lipid levels and is well tolerated. Its major side effect is jaundice, characterized by a yellowing of the eyes and, to a lesser degree, the skin due not to liver disease but to the harmless impairment of bilirubin clearance. The jaundice resolves when Reyataz is stopped; it also may become less marked with the passage of time. Viread can lower Reyataz blood levels; in this setting, Reyataz should be boosted with Norvir.
Activist
Waiting for atazanavir to emerge from the pipeline in 2003, I thought: a potent once daily PI (two puny capsules) with little impact on lipids and no gut disturbance? Bring it on! Oh, wait. Did I say potent? It was approved for use as a single PI in a regimen but it makes some people nervous without a ritonavir boost—especially if it’s not their first regimen or they’ve got a high viral load, or if they want to use it with Viread or efavirenz (which reduce its levels). Atazanavir can raise bilirubin levels for some people, to the point of appearing jaundiced. Turning yellow ain’t cool, for sure, but there doesn’t appear to be any liver injury associated with it and it resolves when you stop the drug. Atazanavir’s big drag: if you have acid reflux, the best atazanavir will let you do is short-acting medications. No proton pump inhibitors allowed.

Nukes | Retrovir / AZT / zidovudine | Videx, Videx EC / ddI / didanosine |
| Hivid / ddC / zalcitabine | Zerit / d4T / stavudine | Epivir / 3TC / lamivudine |
| Ziagen / abacavir sulfate | Combivir (Retrovir, Epivir) |
| Trizivir (Retrovir, Epivir, Ziagen) | Emtriva / emtricitabine / FTC |
| Viread / tenofovir disoproxil fumarate | Epzicom (Epivir, Ziagen) |
| Truvada (Viread, Emtriva) |

Non-Nukes | Rescriptor / delavirdine | Viramune / nevirapine |
| Sustiva / efavirenz |

HIV Protease Inhibitors | Invirase / saquinavir hard-gel | Crixivan / indinavir | Norvir / ritonavir | Viracept / nelfinavir | Fortovase / saquinavir soft-gel |
| Agenerase / amprenavir | Kaletra (lopinavir/ritonavir) |
| Reyataz / atazanavir | Lexiva / fos-amprenavir | tipranavir |

Fusion Inhibitor | Fuzeon / T-20 / enfuvirtide |

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