What is Sustiva?
Sustiva is a drug that contains the active substance efavirenz. It is available in capsules (yellow and white: 50 mg; white: 100 mg; yellow: 200 mg), in yellow capsules-shaped tablets (600 mg) and in an oral solution (from 30 mg / ml).
What is Sustiva used for?
Sustiva is an antiviral drug, indicated in combination with other antiviral medicines to treat adults and children at least 3 years of age with human type immunodeficiency virus. The dose of Sustiva should be reduced for patients taking voriconazole (for the treatment of fungal infections). Patients taking rifampicin (an antibiotic) may need to take a higher dose of Sustiva.
For more details, see the summary of product characteristics (also included with the EPAR).
How does Sustiva work?
Sustiva contains the active ingredient efavirenz, a non-nucleoside reverse transcriptase inhibitor (NNRTI). It blocks the activity of reverse transcriptase, an enzyme produced by the HIV virus that allows it to infect cells in the body and produce more viruses. By blocking this enzyme, Sustiva, taken in combination with other antiviral drugs, reduces the amount of HIV in the blood, keeping it at a low level. Sustiva does not cure HIV infection or AIDS, but it can
delay the damage to the immune system and the development of infections and diseases associated with AIDS.
How has Sustiva been studied?
Sustiva has been examined in three main studies involving more than 1 100 adults:
- the first study compared Sustiva in combination with lamivudine and zidovudine or indinavir (other antiviral drugs) with the combination of indinavir, lamivudine and zidovudine;
- the second study compared Sustiva in combination with nelfinavir and two other antiviral drugs with the same combination without Sustiva;
- the third study compared the addition of Sustiva or placebo (a dummy treatment) to a treatment regimen based on antiviral drugs including indinavir and two other antiviral drugs, in patients previously treated for HIV infection.
Sustiva has also been studied in 57 children aged between 3 and 16 years, in combination with nelfinavir and other antiviral drugs.
In all the aforementioned studies, the main measure of effectiveness was the number of patients with HIV-1 levels not appreciable in the blood (viral load) after 24 or 48 weeks of treatment.
What benefit has Sustiva shown during the studies?
Studies have shown that therapeutic combinations involving the use of Sustiva are as effective as the comparator medicines:
- the first study showed that, 48 weeks later, 67% of adults treated with Sustiva in combination with zidovudine and lamivudine showed a viral load of less than 400 copies / ml compared to 54% of patients treated with Sustiva and indinavir, and 45% of those treated with indinavir, lamivudine and zidovudine;
- in the second study Sustiva in combination with nelfinavir gave better results than the combination without Sustiva with, respectively, 70% and 30% of patients with viral load less than 500 copies / ml after 48 weeks of treatment;
- the results of the third study show that, after 24 weeks, a higher percentage of patients treated with Sustiva had viral loads below 400 copies / ml compared to patients treated with placebo.
Similar results were found in the study on children.
What is the risk associated with Sustiva?
The most common side effects seen with Sustiva (seen in more than 1 in 10 patients) are skin rashes. Sustiva can also involve symptoms of the nervous system such as dizziness, insomnia, drowsiness, difficulty concentrating and alteration of dream activity, and psychiatric disorders including severe depression, suicidal thoughts, suicide attempts and aggressive behavior, especially in patients with a history of mental illness. Taking Sustiva with food may increase the frequency of side effects. For the full list of all side effects reported with Sustiva, see the Package Leaflet.
Sustiva should not be used in people who may be hypersensitive (allergic) to efavirenz or any of the other substances. It must not be used in patients with severe hepatic impairment or being treated with any of the following drugs:
- astemizole, terfenadine (usually used to treat allergy symptoms - these medicines can be purchased without a prescription);
- dihydroergotamine, ergotamine, ergonovine, methylergonovine (used in the treatment of migraine);
- midazolam, triazolam (used for the treatment of anxiety or sleep disorders);
- pimozide (for the treatment of mental illnesses);
- cisapride (for the treatment of certain stomach disorders);
- bepridil (for the treatment of angina);
- St. John's wort (a herbal preparation used in the treatment of depression).
Finally, precaution should be used in the use of Sustiva in patients who are simultaneously taking other medications. For more details, see the package leaflet.
As with other anti-HIV drugs, patients receiving Sustiva may be at risk of lipodystrophy (changes in the distribution of body fat), osteonecrosis (death of bone tissue) or immune reactivation syndrome (symptoms of infections caused by the reactivation of the immune system ). Patients with liver problems (including hepatitis B or C) may be at high risk of developing liver damage if they are treated with Sustiva.
Why has Sustiva been approved?
The Committee for Medicinal Products for Human Use (CHMP) has determined that the benefits of Sustiva outweigh the risks in the antiviral treatment of adults, adolescents and children 3 years of age or older with HIV in combination with other antiviral medicines. The committee noted that Sustiva has not been sufficiently studied in patients at an advanced stage of the disease (with CD4 cell counts less than 50 cells / mm3) or where treatment with protease inhibitors (another type of antiviral drug) is either concluded without success. The committee also noted that the information currently available is not sufficient to evaluate the efficacy of therapies based on the use of protease inhibitors used after the failure of Sustiva therapy, although there is no evidence to suggest that in these patients protease inhibitors are not effective. The committee recommended the granting of a marketing authorization for Sustiva.
More information on Sustiva
On 28 May 1999 the European Commission issued a marketing authorization for Sustiva, valid throughout the European Union. The marketing authorization holder is Bristol-Myers Squibb Pharma EEIG. The marketing authorization was renewed on May 28, 2004 and May 28, 2009.
For the full EPAR of SUSTIVA, click here.
Last update of this summary: 05-2009.
