Appendix D: First Combinations

A Practical Guide to HIV Drug Treatment for People Living with HIV

Appendix D: First Combinations

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Table 1: Possible antiretroviral drug combinations for people starting treatment
Table 2: Potential advantages and disadvantages of some
antiretroviral drug combinations

Table 1 below outlines possible drug combinations for people starting HIV drug treatment for the first time. The combinations listed here are those recommended by many major treatment guidelines at the time this guide was published.

Table 2 lists a few of the advantages and disadvantages of the drugs in Table 1. You can use the information in these tables as a starting point for discussing treatment options with your doctor. When looking at the options, remember that these are only guidelines and that another combination, perhaps not listed here, may be the right one for you.

The cost of some of these drugs may not be covered by provincial or territorial prescription drug plans. Your doctor and pharmacist can give you more information.

Table 1: Possible antiretroviral drug combinations for people starting treatment
2 nukes	+ a 3rd drug		such as
Truvada (tenofovir + FTC) OR Kivexa (abacavir + 3TC)	a non-nuke		efavirenz (Sustiva)
	OR
	a boosted PI		atazanavir (Reyataz), darunavir (Prezista), fosamprenavir (Telzir) or saquinavir (Invirase), boosted by ritonavir (Norvir)
			OR
			lopinavir-ritonavir (Kaletra)
	OR
	an integrase inhibitor		raltegravir (Isentress)

Table 2: Potential advantages and disadvantages of some antiretroviral drug combinations
Two nukes (nucleoside reverse transcriptase inhibitors or NRTIs) combined in one pill …
Drug		Potential advantages		Potential disadvantages
Kivexa (abacavir + 3TC)		Has been used for many years and both drugs penetrate well into the brain.		Abacavir can cause a hypersensitivity reaction in some people (a blood test can be done before you start taking the medication to see if you’re at risk). There have been recent questions about whether abacavir is associated with an increased risk of heart attacks, particularly among people who are already at increased risk (for example, older people, smokers or people with high blood pressure).
Truvada (tenofovir + FTC)		Also available in combination with efavirenz (Sustiva) as Atripla, which is one pill taken once a day.		There are concerns about the possible effect on kidney function and about weakening of the bones when tenofovir is used for many years.
Other nukes		Other nukes include the individual components of Kivexa and Truvada (for example, abacavir (Ziagen), lamivudine (3TC) and tenofovir (Viread)). Others include AZT (zidovudine, Retrovir), ddI (didanosine, Videx EC) and d4T (stavudine, Zerit). These are chosen mainly for people who have viruses with resistance to some of the primary drugs and need specific drugs based on testing of their virus. In Canada, FTC (emtricitabine) is only available co‑formulated with tenofovir, as Truvada.
… plus one non-nuke (non-nucleoside reverse transcriptase inhibitor or NNRTI) …
Efavirenz (Sustiva)		Available in combination with tenofovir and FTC as Atripla, which is one pill taken once a day.		May cause vivid dreams and other sleep or mental disturbances. May increase cholesterol levels, but studies have not found any increased risk of heart disease. Women who are or might become pregnant should not take efavirenz.
Other non-nukes		Nevirapine (Viramune) is a “first-generation” non-nuke that cannot be started in men whose CD4 count is higher than 400 cells or in women whose CD4 count is higher than 250 cells. It penetrates well into the brain and may increase levels of good cholesterol and reduce triglycerides. However, it may cause an allergic reaction (rarely fatal) for which there is no test to determine risk in advance. Etravirine (Intelence) is a “second-generation” non-nuke that is usually only taken by people who are resistant to efavirenz or nevirapine.
… OR a protease inhibitor …
Atazanavir (Reyataz)		Doesn’t cause an increase in cholesterol (if used without ritonavir).		May cause jaundice (yellow eyes or skin), which is either mild or reversible (goes away if the medication is stopped). NEVER stop taking a medication before discussing it with your doctor, as you will need a replacement drug. Atazanavir is almost always boosted by ritonavir if it is taken with tenofovir (also a component of Truvada).
Darunavir (Prezista)		Effective in many people with resistance to older PIs, especially when combined with other effective drugs.		May (rarely) cause liver toxicity; should not be used by people with severe liver damage. Because it remains effective even when other PIs fail, darunavir is often saved for second or later treatment combinations.
Lopinavir-ritonavir (Kaletra)		Preferred treatment for pregnant women.		Can increase levels of cholesterol, triglycerides (another type of fat) and sugar in the bloodstream.
Boosting with ritonavir (Norvir)		Increases drug levels of other PIs and keeps the medication in the bloodstream longer.		Greater likelihood of side effects. An extra pill to take. Ritonavir may cause mild diarrhea and a small increase in cholesterol. Ritonavir can interact with many medications.
Other PIs		Most other PIs (including nelfinavir (Viracept), saquinavir (Invirase), indinavir (Crixivan), fosamprenavir (Telzir) and tipranavir (Aptivus)) will cause some increase in cholesterol and sometimes liver enzymes. Most are used for individuals who cannot, for some reason, use Kaletra, (boosted) atazanavir or darunavir.
…OR an integrase inhibitor
Raltegravir (Isentress)		Many people experience fewer short-term side effects with raltegravir than with other antiretrovirals.			Because raltegravir is a relatively new drug, its long-term effects are unknown.

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