What is Sustiva (efavirenz)?
Sustiva (efavirenz) is an NNRTI (Non-Nucleoside Reverse Transcriptase Inhibitor) drug that is used to treat HIV-1 in combination with other antiretroviral drugs. Sustiva disables the function in viral replication as it binds to HIV-1 DNA polymerase reverse transcriptase. The drug is offered as a once-daily dose and the advantage of penetration into the cerebrospinal fluid (CSF).
Dosing & Administration
Sustiva is used as part of a three-drug combination regimen to treat HIV-1, and for HIV post-exposure prophylaxis in an occupational setting (off-label). This drug is used in adults, children, and infants weighing at least 3.5 kg. However, although it is approved for use in infants, it is not recommended in children younger than three because of underdosing concerns. This medication is available as a capsule that can be opened or as a hard capsule that cannot be scored, crushed or chewed. This drug should be taken on an empty stomach. Further details about dosing and drug administration are available in the package insert.
Dosage adjustments are not necessary for patients with mild liver dysfunction; however, this drug should not be used in patients with moderate to severe liver impairment. Patients with renal impairment do not need dosage adjustments.
Sustiva is contraindicated in patients with severe liver dysfunction or hypersensitivity to the drug. Patients with a personal or family history of certain heart conditions should also exercise extreme caution using this drug. Details about the types of medications that are contraindicated for use with Sustiva are provided in the package insert.
Sustiva Side Effects
Sustiva is associated with CNS effects often described as feeling high. Patients should be advised to take precautions with driving and other activities requiring attentiveness. Serious psychiatric effects have also been reported. A complete list of potential adverse effects is provided in the product monograph.
Sustiva should be used with caution in patients with cardiac disease as this drug may prolong the QTc.
Patients with moderate or severe liver dysfunction should not use Sustiva due to reports of serious hepatotoxicity, especially in patients with underlying liver disease.
Patients who are HIV positive should also be screened for comorbid HBV and HCV infection. If co-infected, patients should begin an antiretroviral regimen that will target co-infected viruses, regardless of CD4 counts or viral loads. Drug regimens and prescribing considerations are outlined in the current HIV treatment guidelines.
Sustiva is contraindicated with many herbal and drug-to-drug interactions. Further details are listed in the package insert.
Pregnancy & Lactation
During treatment, women using Sustiva should use two forms of contraception as efavirenz may be teratogenic. The drug is transmitted through breast milk, so it is recommended that HIV positive women avoid breastfeeding.
No specific overdose antidote is known, so the drug overdose should be treated with standard supportive care. Sustiva is not significantly dialyzable.
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