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Lesson Which Are The Easiest Drug Combinations? (A Look At Fewer Pills and Once-A-Day Dosing)
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Simplifying Protease Inhibitors

Protease Inhibitor Doses Approved by the FDA Simplification Tip Looking Ahead
Aptivus
(tipranavir)
Aptivus
Two 250mg capsules, twice a day. Must be taken with two 100mg capsules of Norvir, also twice a day (a total of four Aptivus capsules and four Norvir capsules a day). Aptivus/Norvir should be taken with food. Aptivus/Norvir should be taken using the approved dosing schedule. Strategies to simplify Aptivus/Norvir treatment, such as fewer pills or once-daily dosing, have not been studied or evaluated. At the present time, it's not clear if Aptivus/Norvir therapy can be made any easier to take.
Crixivan
(indinavir)
Crixivan
Two 400mg capsules, every eight hours (a total of 6 capsules a day). Must be taken on an empty stomach (no food 2 hours before or 1 hour after dosing), or with a light, low-fat snack. Combine Crixivan with Norvir. Norvir boosts Crixivan levels in the bloodstream. This allows Crixivan to be taken fewer times a day, either with or without food. The usual combined dose is two 400mg Crixivan capsules with either one or two 100mg Norvir capsules, both taken at the same time twice a day. Researchers are now looking at the possibility of combining Crixivan with Norvir for once-daily dosing. However, this is not yet a recommended option.
Invirase
(saquinavir)
Invirase

Invirase must be used in combination with Norvir. The approved dose is two 500mg Invirase tablets plus one 100mg Norvir capsule, twice a day (a total of 6 pills a day). Invirase and Norvir should be taken with food.

For several years, Invirase was only available in 200mg capsules. The drug is now available in 500mg tablets. Instead of taking five Invirase capsule plus one Norvir capsule twice a day, the number of pills has been reduce to two Invirase tablets plus one Norvir capsule twice a day.

The manufacturer is looking at the possibility of only having to take Invirase once a day. However, until this once-daily dose has been studied and approved by the U.S. Food and Drug Administration, it should be considered highly experimental.

Kaletra tablets
(lopinavir + ritonavir)
Kaletra

Two tablets, twice a day, or four tablets, once a day (a total of 4 pills a day). Each tablet contains 200mg lopinavir plus 50mg ritonavir.

For HIV-positive people starting anti-HIV treatment for the first time, Kaletra can be taken either once a day or twice a day. For HIV-positive people who have been on other anti-HIV treatments in the past, Kaletra should only be taken using the twice-daily dosing schedule. Please review the Kaletra lesson for specific dosing recommendations, especially if Kaletra is being combined with Sustiva, Viramune, Lexiva, or Viracept.

Researchers have been experimenting with Kaletra monotherapy (Kaletra used without other medications) for the treatment of HIV. Clinical trials reported to date suggest that Kaletra monotherapy has a durable and prolonged treatment effect, but it may be more likely to fail than complete Kaletra-based regimens. Until additional studies have been completed and experts have confidence in the study results, Kaletra monotherapy should be considered highly experimental.
Lexiva
(fosamprenavir)
Lexiva
Two 700mg tablets, twice a day (a total of 4 pills a day), or two 700mg tablets plus two 100mg Norvir capsules, once a day (a total of 4 pills a day), or one 700mg tablet plus one 100mg Norvir capsule twice a day (a total of 4 pills a day). This last dosing option should be used for patients who have tried and failed other protease inhibitors in the past. Lexiva can be taken once a day if it is used in combination with low-dose Norvir. The once-daily dose is two 700mg Lexiva tablets plus two 100mg Norvir capsules. At four pills once a day or two pills twice a day, it's not likely that Lexiva can be made easier to take. However, the manufacturer is currently studying the possibility of using a lower dose of Novir (one 100mg capsule instead of two 200mg capsules) for use in combination with once-daily Lexiva.
Norvir
(ritonavir)
Norvir
Six 100mg capsules, twice a day (a total of 12 pills a day). Very few people use the approved dose of Norvir. This is because it can cause many short- and long-term side effects. Instead, lower doses of Norvir are used to boost blood levels of other protease inhibitors, which can sometimes make a drug combination easier to take. Norvir continues to be studied in combination with other protease inhibitors (PIs), including PIs in development, in an effort to make them more effective and to simplify their dosing schedules. Researchers are also experimenting with Norvir alternatives that can be used to boost blood levels of PIs, without the side effects (and added cost) of Norvir.
Prezista
(darunavir)
Prezista
Two 300mg tablets, twice a day. Must be taken with one 100mg capsule of Norvir, also twice a day (a total of four Prezista capsules and two Norvir capsules a day). Prezista/Norvir should be taken with a light snack or complete meal. Prezista/Norvir should be taken using the approved dosing schedule. Strategies to simplify Prezista/Norvir treatment, such as fewer pills or once-daily dosing, have not been studied or evaluated. Prezista/Norvir at the current dosing recommendation is approved for HIV-positive people who have used other anti-HIV medications, including protease inhibitors, in the past. Once-daily Prezista plus Norvir is being tested in HIV-positive people starting treatment for the first time. This strategy has not yet been reviewed by the FDA.
Reyataz
(atazanavir)
Reyataz 200mg  Reyataz 300mg
Two 200mg capsules, once a day (a total of two pills a day).

If Reyataz is taken with Norvir, the approved dose is one 300mg Reyataz capsule plus one 100mg Norvir capsule, once a day.

Reyataz is the first protease inhibitor approved by the U.S. Food and Drug Administration that only needs to be taken once a day. Reyataz can be combined with other once-daily drugs to allow for a complete once-a-day regimen. At two capsules, once a day, it's not likely that Reyataz can be made any easier to take.
Viracept
(nelfinavir)
Viracept
Two 625mg tablets, twice a day (a total of 4 pills a day), or five 250mg tablets, twice a day, or three 250mg tablets, three times a day (a total of 9-10 pills a day).

Some healthcare providers recommend combining Viracept with Norvir. Norvir boosts Viracept levels in the bloodstream. However, this is done more for potency reasons than for simplification. The correct doses of either Norvir or Viracept, if they are combined, have not yet been determined.

The 625mg Viracept tablet was developed to replace the 250mg tablets that have been used for several years. Using the 250mg tablets, people needed to take five tablets twice a day. Now that the 625mg tablets are available, people will only need to take two Viracept tablets twice a day. It might also be possible to combine Viracept and Norvir to allow for once-daily dosing. However, this has not yet been studied by researchers and is not yet recommended.


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Last Revised: August 17, 2007

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