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Guides Introduction to combination therapy

The most commonly used first line combinations

Drug name and comments Side effects Other notes
Efavirenz (Sustiva/Stocrin)
Efavirenz is recommended as part of a first-line therapy. It is 1 pill, once-daily. Side effects, which can be significant, usually reduce after the first few weeks.
Side effects are sleep disturbance (including nightmares), mood changes (including anxiety and depression), rash, liver toxicity and lipid changes. About 20% people switch to another drug. Efavirenz should not be used during pregnancy or by women trying to conceive a baby.
Nevirapine (Viramune)
Nevirapine is an alternative to efavirenz, but has a slightly higher risk of serious side effects. Nevirapine is started at 1 tablet a day for the first 2 weeks, and then 1 tablet twice-daily.
Main side effects are rash and liver toxicity. These occur in the first 6-8 weeks. Any low level rash should be taken seriously. Serious rash can be fatal. If you still have a rash after the first two weeks do not increase the nevirapinr dose. Your doctor needs to see any rash. Women with a CD4 count over 250 and men with a count over 400 should not start with nevirapine.
Lopinavir/r (Kaletra)
Kaletra is less widely used as a first-line protease inhibitor because it is a twice-daily drug. Kaletra includes ritonavir inside the same pill.
Main side effects are changes in lipids (blood fat) which should be routinely monitored, lipodystrophy (fat accumulation) and diarrhoea. The daily dose of ritonavir in Kaletra is 200 mg daily. Kaletra includes lopinavir and ritonavir in the same pill.
Atazanavir/r (Reyataz)
Atazanavir/r now widely used as first-line treatment, because it is dosed once-daily and generally easy to tolerate. Usually taken with a separate dose of 100 mg ritonavir.
Main side effects are yellowing eyes or skin in 10% of patients. This is not a problem unles total bilirubin levels increase to 60-70 mmol/L. Lipids can increase due to the use of ritonavir. Taken with a separate dose of ritonavir (/r), unless you have high drug levels.
Darunavir/r (Prezista) Approved as a once-daily first-line PI for naive patients. When compared to Kaletra, darunavir had lower rates of nausea, diarrhoea and lipid changes. Taken with a separate dose of ritonavir (/r).
Fosamprenavir/r (Telzir)
In studies fosamprenavir/r had similar results to Kaletra, but is less commonly used.
Side effects, including diarrhoea and lipids are similar to Kaletra. Taken with a separate dose of ritonavir (/r).
Saquinavir/r (Invirase)
Saquinavir/r has shown similar results to Kaletra. There is less comparative data to Kaletra than for fosamprenavir/r.
Side effects, including diarrhoea and lipds are similar to Kaletra. May have a lesser effect on trigliceride levels. Taken with a separate dose of ritonavir (/r).

Each option is used with either Truvada (tenofovir + FTC) or Kivexa (abacavir + 3TC).


July 2010

Decisions relating to your treatment should always be taken in consultation with your doctor. Information in this guide is intended to support those discussions.

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