HIV doctors have guidelines on how to use anti-HIV drugs. The drugs recommended are the most effective and safest drugs available for the treatment of HIV.

The drugs recommended for people starting HIV treatment for the first time generally have few side-effects. It is particularly good to know that they do not cause the more serious side-effects that were caused by some of the older HIV drugs – these drugs are now only used rarely because there are alternatives available, which are safer and often easier to take.

Because so few people now need to stop or change treatment because of side-effects, doctors have estimated that people will probably be able to take the currently available first-choice anti-HIV drugs safely for decades.

New British HIV treatment guidelines were issued in 2008 recommending that HIV treatment should be started when a person’s CD4 cell count is around 350 (earlier guidelines recommended starting treatment with a CD4 cell count of around 200). One of the main reasons why doctors felt able to recommend starting treatment earlier was because there are now anti-HIV drugs available that seem to be safe and only cause mild side-effects.

Remember, if you experience any side-effects, then mention them at your clinic. If a side-effect persists, you don’t have to suffer in silence and it’s nearly always possible to do something about it.

Recommended first HIV treatment combination

If you are starting HIV treatment for the first time the recommended treatment is a combination of drugs that includes:

• Efavirenz (Sustiva). This is a non-nucleoside reverse transcriptase inhibitor (NNRTI)

with either

• Truvada. This is a combination pill containing the nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) FTC (emtricitabine) and tenofovir

or:

• Kivexa. This is a combination pill containing the NRTIs 3TC (lamivudine) and abacavir.

You can find out more about these drugs in the NAM booklet, Anti-HIV drugs. 

Although these drugs are effective and generally safe, they can still cause side-effects. Details of some of the most common are provided below.

Efavirenz is generally a very safe drug and few people need to stop taking it because of side-effects. But it can cause side-effects including problems concentrating, dizziness, sleep disturbances such as insomnia (difficulty sleeping), vivid dreams and nightmares. Mental health problems including depression, anxiety and low mood have also been reported as side-effects of efavirenz.

These side-effects are often most noticeable in the first few weeks after treatment with efavirenz is started and then lessen or even go away completely. However, a small number of people experience longer-term or more serious sleep and mood problems due to treatment with efavirenz and some people need to stop taking the drug because of these.

Make sure you tell your doctor if you experience any of these side-effects.

If you do experience side-effects caused by efavirenz then discuss these with your doctor. There may be a number of options available to you to help reduce these side-effects. One simple step you can take is avoiding taking efavirenz with a high-fat meal as doing this will increase the level of the drug in your body and can increase the side-effects. You could also talk to your doctor about what time you take the dose, as taking it an hour or so before bed means that the drug level should be highest when you are asleep.

If you have a history of mental health problems then efavirenz might not be a good choice and you may wish to talk about other treatment options with your doctor.

You should not take efavirenz if you are thinking of becoming pregnant. There is a theoretical risk that it can cause birth defects. If you become pregnant whilst taking efavirenz, you should contact your clinic for advice.

The drugs in Truvada (FTC and tenofovir) are generally very safe and few people need to stop taking Truvada because of side-effects.

But both FTC and tenofovir can cause diarrhoea and nausea (feeling sick). A small number of people have reported dizziness as a side-effect of tenofovir, and headache and difficulty sleeping have been reported as side-effects of FTC. You can take other medicines, such as anti-diarrhoea pills, anti-sickness (sometimes called anti-nausea pills or anti-emetics), and pain killers to help relieve these side-effects if they develop.

There is a small long-term risk of developing bone problems as a result of treatment with tenofovir. Your doctor should do regular blood tests to check levels of minerals to make sure that you are not at risk of this side-effect.

Kidney problems may also be a side-effect of tenofovir, particularly for people who are taking other medicines that affect the kidneys, or for those who have other risk factors for kidney disease, such as high blood pressure or diabetes. Your doctor should do regular blood tests to check the health of your kidneys.

In rare cases, FTC can cause changes in the colour of the skin, particularly in people of non-white race. You should talk to your doctor if this happens to discuss your treatment options.

The drugs in Kivexa (3TC and abacavir) are generally safe. But abacavir can cause a potentially dangerous allergic reaction. If you are thinking about treatment with abacavir it is very important that you first have a blood test to see if you have a gene linked to this allergic reaction called HLA-B*5701. If your result is positive you should not take abacavir. If it is negative, it is highly unlikely that you will have an allergic reaction but you should still report any fever, rash or headache to your doctor immediately. If you stop taking abacavir because you have had an allergic reaction to the drug you must never take abacavir again as this can be very dangerous, even fatal.

Some (but not all) research has linked abacavir to an increased risk of heart attack, particularly for people who have other risk factors for heart disease. Because of this, abacavir is not recommended for people who have risk factors for heart disease.

Both abacavir and 3TC can cause headache, nausea, vomiting and diarrhoea. These side-effects are usually quite mild and lessen or go away completely after a few weeks of treatment. Your doctor can also give you other medicines to control these side-effects if you need them.

A rarer side-effect of 3TC is hair loss and if you experience this you should talk to your doctor about your treatment options.

Rather than take efavirenz, an alternative option is to base treatment on a type of anti-HIV drug called a boosted protease inhibitor (these protease inhibitors have their anti-HIV effect boosted by taking them with a small dose of a second protease inhibitor called ritonavir).

The recommended boosted protease inhibitors for people starting treatment for the first time are:

• lopinavir/ritonavir (Kaletra)
• atazanavir (Reyataz) plus ritonavir
• darunavir (Prezista) plus ritonavir
• fosamprenavir (Telzir) plus ritonavir
• saquinavir (Invirase) plus ritonavir.

Side-effects of boosted protease inhibitors

Protease inhibitors seem more likely than efavirenz to cause side-effects. The main side-effect associated with protease inhibitors (with the exception of atazanavir) is stomach problems including diarrhoea, feeling sick (nausea) and being sick (vomiting). As with many other side-effects, these are often worse in the first few weeks of treatment with a protease inhibitor and often lessen or go away over time. You can take medicines to help control diarrhoea and to stop you being sick.

Kaletra, fosamprenavir and saquinavir can cause increases in blood fats. Your doctor will do regular blood tests to measure levels of cholesterol and blood sugars. Changing your diet, exercise and, if needed, treatment with drugs called statins can all lower cholesterol.

Atazanavir can cause a non-dangerous yellowing of the skin and eyes that goes away if treatment with the drug is stopped.

The NNRTI nevirapine (Viramune) is an alternative treatment for people starting treatment for the first time. It is only recommended for certain groups of patients, particularly women who are pregnant or thinking of becoming pregnant, or people who want to avoid taking efavirenz because of its side-effects.

For women who are pregnant, or thinking of becoming pregnant, the NRTI combination pill Combivir (AZT and 3TC) plus nevirapine is an option. This is because there is good evidence that AZT is effective at preventing mother-to-child transmission of HIV.

Side-effects of nevirapine

The main side-effect of nevirapine is rash. To reduce the risk of this, for the first two weeks of treatment the dose of nevirapine is 200mg once daily, after which it is increased to 200mg twice daily. But a small number of people need to change treatment because of the rash the nevirapine can cause, and a very small number of people require hospitalisation because of this. Very rarely people develop a serious skin condition called Stevens Johnson syndrome.

Nevirapine can cause liver problems. Because of this, women should not start treatment with nevirapine if their CD4 cell count is above 250, and men should not start treatment with nevirapine if their CD4 cell count is above 400.

Side-effects of Combivir

Combivir (AZT and 3TC) is not generally recommended for people starting treatment for the first time because AZT can cause fat loss from the face, limbs and buttocks. Changing treatment from AZT to tenofovir can lead to a very slow return in limb fat.

Some drugs are no longer recommended and they are only used in some circumstances. The NRTI d4T (stavudine, Zerit) is not recommended for people who have other anti-HIV drugs available to them. This is because it causes fat loss from the face, limbs and buttocks. It can also cause painful damage to the nerves in the lower limbs, a side-effect that is called peripheral neuropathy.

One of the reasons why the NRTI ddI (didanosine, Videx) is not recommended for first-line HIV treatment is the side-effects it can cause. These include peripheral neuropathy, pancreatitis and a rare, but unpleasant and potentially dangerous, side-effect called lactic acidosis. There is more information on these side-effects later in this booklet.

HIV treatment is meant to make your health better. If you are experiencing treatment side-effects it is a good idea to make sure that your HIV doctor knows about them. It is nearly always possible to do something about side-effects.

In some circumstances you may need or want to change treatment because of side-effects. This is more likely to be an option if you have little or no resistance to anti-HIV drugs and your viral load is undetectable. Then you should be able to stop the drug that is causing your side-effect and switch to an alternative treatment.

Changing treatment can be more complex if you have a detectable viral load or you have HIV that is resistant to some anti-HIV drugs. Your doctor will look at the results of resistance tests and then discuss possible treatment options with you. Having resistance will, however, limit the number of replacement drugs that are available to you.

It also makes good sense to ask about the possible side-effects of the drugs you are considering switching to.

In recent years a number of anti-HIV drugs have become available that provide very important treatment options for people who have taken a lot of HIV treatment in the past, particularly those with drug-resistant virus.

These drugs are particularly effective against HIV because they work against the virus in a slightly different way to the older anti-HIV drugs. These drugs are:

• T-20 (enfuvirtide, Fuzeon)
• maraviroc (Celsentri)
• raltegravir (Isentress)
• etravirine (Intelence).

They are generally safe and only cause mild side-effects. Information so far suggests that few people need to stop taking these drugs because of side-effects.

Nevertheless, you may need to consider the possibility of some side-effects.

Side-effects of T-20

This is the only anti-HIV drug that has to be given by injection. The key side-effects are pain and a hardening of the skin at the site of the injection. These are often called injection-site reactions. If you need to take T-20, you’ll be given information about how to inject it and how to reduce the risk of injection-site reactions developing.

T-20 has some rarer side-effects as well, which your doctor should explain to you before you start treatment with it.

Side-effects of maraviroc

The main side-effect of maraviroc is nausea. If this is a problem, it can be controlled in many people with anti-sickness medicines.

Serious liver side-effects have been reported in a small number of patients. If you are also infected with hepatitis B or hepatitis C or have any other liver problems, then your doctor should monitor you carefully and do blood tests to check the health of your liver.

Side-effects of raltegravir

Feeling dizzy, stomach pains, sweating and pains in the joints have been reported by some people taking raltegravir.

Side-effects of etravirine

Stomach problems including feeling or being sick and diarrhoea can be side-effects of etravirine. Your doctor can give you medicines to control these if they are a problem. Other possible side-effects include high blood pressure and changes in your blood chemistry. You should have regular tests to monitor these as part of your routine HIV care.