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PROTEASE INHIBITORS

REYATAZ

(Atazanavir sulfate)

Manufacturer: Bristol-Myers Squibb

Standard dose of Reyataz is two 200 mg capsules taken with food once-a-day or one 300 mg capsule and one 100 mg Norvir capsule, once-a-day.

Evaluation: Reyataz was approved by the FDA in 2003. It is an “azapeptide” protease inhibitor. The dosing—just two capsules taken with food once-a-day—is very convenient. Reyataz doesn’t seem to raise your cholesterol and triglyceride levels the way most other protease inhibitors do. In fact, one study suggests that Reyataz may actually increase your HDL (good) cholesterol, which helps protect you from heart disease. And it is effective. In a head-to-head comparison with Viracept (nelfinavir), Reyataz was clearly better. Reyataz boosted with Norvir (ritonavir) is listed as a “preferred” drug in the current DHHS guidelines.



PREZISTA

(Darunavir)

Manufacturer: Tibotec

The approved dose of Prezista for people just starting treatment is two 400 mg tablets plus one 100 mg Norvir capsule once-a-day. For treatment-experienced patients, it is one 600 mg tablet and one 100 mg Norvir capsule twice-a-day.

Evaluation: Prezista is rapidly gaining in popularity. Prezista boosted by Norvir (ritonavir) is listed as a “preferred” drug in the latest DHHS guidelines. Prezista was approved by the FDA in June, 2006.




LEXIVA

(Fosamprenavir)

Manufacturer: GlaxoSmithKline

The standard dose of Lexiva is two 700 mg pills twice-a-day; two 700 mg tablets with two 100 mg capsules of Norvir once daily; or one 700 mg tablet with one 100 mg capsule of Norvir twice daily. You can take it with or without food.

Evaluation: Lexiva was approved by the FDA in 2003. It is a “prodrug” of Agenerase (amprenavir), a protease inhibitor that was approved by the FDA in 1999. Basically, Lexiva turns into Agenerase in your body. The big advantage is in the dosing. The standard dose of Agenerase was 16 huge pills a day, which was just too many. Lexiva’s dosing is far more convenient and it causes fewer side effects. Because Lexiva is so much better, the manufacturer has taken Agenerase off the market.



KALETRA

(Lopinavir/Ritonavir)

Manufacturer: Abbott Laboratories

Comes in tablets containing 200 mg lopinavir and 50 mg ritonavir. Recom­mended dose is four Kaletra tablets a day.

Evaluation: In clinical trials, Kaletra performed well both as initial therapy and as a “salvage” therapy—meaning it worked well for patients who had developed resistance to other HIV drugs. Kaletra has proved to be an extremely durable drug—it works for a long time. Kaletra is now listed as an “alternative” drug, rather than “preferred”—except for pregnant women, where twice daily Kaletra plus Combivir (lamivudine/zidovudine) remains a “preferred” regimen.



NORVIR

(Ritonavir)

Manufacturer: Abbott Laboratories

Comes in 100 mg capsules and 600 mg/7.5 mL oral solution. Recommended dose is 600 mg (6 capsules) every 12 hours.

Evaluation: Although Norvir is still approved for use as a protease inhibitor, hardly anybody uses it that way anymore—twelve pills a day is just too much, it’s hard to tolerate and it interacts with a lot of other drugs.

However, Norvir still has a use! Low doses of Norvir (usually one 100 mg capsule twice a day—sometimes more), when taken with other protease inhibitors boosts the levels of those other PIs in your blood and keeps them active in your blood longer. In some cases, you may be able to lower the amount of the “main” protease inhibitor you’re taking when you take Norvir with it. Prescribing Norvir for its “boosting” effect with other protease inhibitors has become standard practice.



INVIRASE

(Saquinavir)

Manufacturer: Hoffman-La Roche

Invirase is the hard gel version of Fortovase. The standard dose is 1,000 mg (two 500 mg capsules) twice daily, combined with 100 mg of Norvir twice daily. Should be taken with food.

Evaluation: The manufacturer recently introduced a 500 mg tablet, which reduced the pill burden from five capsules to two 500 mg tablets plus one 100 mg capsule of Norvir taken together twice a day. It is recommended as an “alternative” PI in the latest DHHS guidelines.



VIRACEPT

(Nelfinavir)

Manufacturer: Agouron

The standard dose of Viracept is five 250 mg pills twice a day or two 625 mg pills twice a day. Food increases the levels of Viracept in your blood, so take it with a meal or a snack. It can be stored at room temperature.

Evaluation: Viracept was approved by the FDA in 1997. A new formulation of Viracept approved by the FDA in 2004 reduced the dose to only two 625 mg pills twice a day, compared to the original dose of five 250 mg pills twice a day—a big improvement.

However, Viracept is not a popular drug. It is infamous for causing diarrhea, and it is not as strong, effective or long-lasting as some of the other drugs in the protease inhibitor class. In the latest DHHS guidelines, Viracept is listed as “no longer recommended.”



CRIXIVAN

(Indinavir)

Manufacturer: Merck

Comes in 200, 333, and 400 mg capsules. Recommend­ed dose is 800 mg (two 400 mg capsules) every 8 hours or two 400 mg Crixivan capsules with either one or two 100 mg Norvir (ritonavir) capsules twice-a-day. Crixivan should be taken on an empty stomach or with a light meal. It can be stored at room temperature.

Evaluation: Crixivan is an old drug that is rarely used anymore. The standard dose of every-eight-hours on an empty stomach is very awkward. Doctors can prescribe Crixivan along with a small dose of Norvir. The Norvir boosts the levels of Crixivan in your blood and makes it possible to take it twice a day instead of every eight hours. It also eliminates the need to take Crixivan on an empty stomach. One of the side effects of Crixivan is kidney stones, which are nothing to laugh at. The manufacturer recommends drinking at least six glasses of water every day to reduce the risk of kidney stones, but people get them anyway. Hardly anyone takes Crixivan these days. It is no longer recommended in the DHHS guidelines as a part of initial therapy.



APTIVUS

(Tipranavir)

Manufacturer: Boehringer Ingelheim

The standard dose of Aptivus is 500 mg (two 250 mg capsules, twice-a-day), plus 200 mg twice daily of Norvir. It should be taken with food.

Evaluation: Aptivus was approved by the FDA in June, 2005. It is recommended as a “salvage” therapy for people who have tried and failed other HIV regimens. It is always used with a Norvir booster. It seems to work best when combined with Fuzeon. It is not recommended for patients who are new to HIV treatment or using a protease inhibitor for the first time. Because of the risk of liver damage, your doctor should give you a liver function test before starting Aptivus and periodically during treatment.



FORTOVASE

(Saquinavir)

Fortovase is no longer marketed in the United States. It has been replaced by Invirase.



AGENERASE

(Amprenavir)

Agenerase has been taken off the market—it has been replaced by Lexiva.




Combination Drugs

Protease Inhibitors

Nucleoside Reverse Transcriptase Inhibitors

Non-Nucleoside Reverse Transcriptase Inhibitors

Fusion Inhibitor

Entry Inhibitor

Integrase Inhibitor



Copyright 2010, Positive Health Publications, Inc.

This magazine is intended to enhance your relationship with your doctor - not replace it! Medical treatments and products should always be discussed with a licensed physician who has experience treating HIV and AIDS!