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Brand Name: Reyataz

Common Name: atazanavir sulfate (ATV)

Class: HIV protease inhibitor

Standard Dose: One 300 mg capsule plus 100 mg Norvir, once daily 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: $857.20 / month 150 mg, 200 mg, or 300 mg capsules

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

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 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.

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 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), changes in heart rhythm, 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 with stomach acid reducing drugs such as Zantac, Pepcid, or Axid if you take the Reyataz (without Norvir) at least two hours before and at least 10 hours after the acid reducing drugs. If taking Reyataz with Norvir and are new to HIV treatment, you do not need to separate the dose of acid reducing drugs from Reyataz/Norvir. If treatment-experienced, then separating as mentioned above must be done. Reyataz should be taken two hours before or one hour after antacids (Rolaids, Tums, and Mylanta). 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 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). The heart medications Tambocor, Rythmol, Cordarone, quinidine, and lidocaine should be used cautiously. Monitoring may be required when 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.Caution must be exercised when using Sporonox or ketoconazole. Vfend is not recommended.

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.

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 Tegretol, Dilantin, or phenobarbital may decrease Reyataz levels and alternate seizure medications should be used. The blood pressure medications called calcium channel blockers, such as Norvasc, Procardia, and others, should be monitored for side effects because Reyataz may increase levels of these blood pressure medications. Also increased levels of Desyrel (trazodone) can occur with Reyataz which may lead to nausea, dizziness, low blood pressure or loss of consciousness. A lower dose of Desyrel 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.

Doctor
Atazanavir (ATV) is now a recommended first-line PI when dosed with ritonavir. It is a generally well tolerated, once a day, simple (2 pills=300 mg atazanavir plus 100 mg ritonavir) PI. The availability of the 300 mg formulation will further reduce the pill count. The data regarding use of non-boosted atazanvir (400 mg/day) is less impressive. Boosted atazanavir must be used when co-administered with efavirenz or tenofovir. Most patients experience an increase in indirect bilirubin levels and for around 5% the increase is severe enough to warrant consideration of switching to an alternative drug. Lipid effects have been minimal even when used with ritonavir boosting. Absorption is dependent on stomach acidity so concurrent dosing with antacids or proton pump inhibitors can significantly decrease plasma levels of atazanavir and decrease efficacy. There is concern about dosing with H2 blockers for the same reason but limited experience suggest that spacing out the dosing often allows for concomitant use of both drugs. It has been included in double-boosted PI regimens with Kaletra or Invirase but more data is needed to better define the role of that strategy.—Keith Henry, MD
Activist

Atazanavir (still makes me think of the cartoon character when I hear it) was the first PI to be approved as a once-a-day drug. Boosted with Norvir, Reyataz can be a powerful part of an HIV regimen. It has a better lipid profile than some other PIs but it has another unfortunate side effect that is sometimes more troubling called hyperbilirubinemia. This can cause jaundice (yellowing of the skin or eyes) which occurs in less than 10% of people who take it, but is no less annoying if you are one of those persons. It is most of the time just a cosmetic side effect and resolves upon discontinuation of the drug. Again, this is one of those “you won’t know until you try it” side effects. Another important thing about this drug is its interaction with some stomach acid reducers. If you take this drug it is crucial to read the product label to see if anything you are thinking about (or currently taking) may affect the efficacy of this drug. But overall, if you don’t get the yellowing problem with this drug, and you don’t need to be on certain medications that could interfere with the drug levels of Reyataz, most people do really well.—Cathy Olufs

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