Sustiva (efavirenz) is a synthetic non-nucleoside reverse transcriptase inhibitor (NNRTI) drug for the treatment of HIV-1. When used as part of a treatment regimen in combination with other antiretroviral drugs, Sustiva has been shown to significantly reduce HIV viral load, slow damage to the immune system, and reduce the risk of progression to AIDS. Sustiva binds directly to HIV-1 RNA-dependent DNA polymerase reverse transcriptase, disabling its crucial function in viral replication, and offers the advantage of penetration into the cerebrospinal fluid (CSF). This medication also has a once-daily dosing schedule for convenience.
Dosage and administration
Sustiva is indicated for the treatment of HIV-1 infection, and for HIV post-exposure prophylaxis in an occupational setting (off-label), as part of a three-drug combination regimen. It can be used in adults, children, and infants three months and older weighing at least 3.5 kg. However, despite FDA approval for use in infants three months and older, it is generally not recommended for use in children under three years due to concerns with under-dosing related to differences in metabolism of the drug. As a tablet-form medication, Sustiva cannot be scored, crushed, or chewed. The capsules may be opened and sprinkled. Sustiva should be taken on an empty stomach. Dosing and administration instructions are given in the product monograph.
No dosage adjustments are required for Sustiva in patients with mild liver dysfunction, but the drug should not be used in moderate to severe liver impairment. Dosage adjustments are not likely necessary in renal-impaired patients.
Most patients using Sustiva report central nervous system (CNS) side effects often described as feeling ‘stoned.’ Patients should take precautions with driving or other potentially dangerous activities requiring attentiveness. Serious psychiatric effects have also been reported. Other side effects include, but are not limited to:
A complete list of potential side effects is provided in the product monograph.
Current HIV treatment guidelines recommend all HIV-positive patients seek screening for HBV and HCV at the time of diagnosis. Co-infection with HIV and HBV or HCV should be treated with antiretroviral therapy targeting both viruses, and should continue indefinitely to achieve optimal suppression of HIV and prevention of HBV or HCV exacerbation. Regimens and considerations are outlined in the appropriate treatment guidelines.
Pregnancy and lactation
Highly active retroviral combination treatment should be used in all pregnant women, regardless of viral load and CD4 count. Efavirenz may be teratogenic and should be avoided in the first trimester of pregnancy. Women taking Sustiva should use two forms of contraception during treatment and continuing for 12 weeks after. Treatment guidelines and the product monograph outline recommendations for women who are inadvertently exposed to Sustiva while pregnant. Medical professionals should report exposure to Sustiva before or during pregnancy to the Antiretroviral Pregnancy Registry to assist in data collection. Current guidelines should be consulted when treating women in pregnancy. Sustiva is excreted in the breast milk. The CDC recommends all HIV-positive women, treated or untreated, avoid breastfeeding to prevent vertical transmission of the virus.
A complete list of potential drug interactions is provided in the product monograph and should be consulted by prescribers.
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