ISENTRESS HD (raltegravir) is an Integrase Strand Transfer Inhibitor (INSTI) drug indicated for the treatment of HIV-1 infection as part of a combination regimen with other antiretrovirals. Raltegravir inhibits the action of the HIV replication enzyme integrase, thereby disrupting the completion of infectious virions.
Dosing & Administration
ISENTRESS HD dosing is based on whether or not the patient is treatment-naïve, and is based on weight for children, infants, and neonates. Dosing guidelines are given in the product monograph. ISENTRESS HD is available as a film-coated tablet, which should not be scored, chewed or crushed. However, a chewable tablet and a powder for oral suspensions are available in the ISENTRESS (non-HD) formulation.
ISENTRESS HD is indicated for the treatment of HIV infection, and off-label for HIV post-exposure prophylaxis following occupational or non-occupational exposure, including sexual assault. ISENTRESS (non-HD formulation) is also indicated off-label for perinatal HIV prophylaxis in neonates at high risk for HIV infection.
ISENTRESS HD can be used without dosage adjustment in patients with mild or moderate hepatic impairment, but must be used with caution or not at all in patients with severe hepatic impairment. No dose adjustments are necessary in patients with renal impairment.
ISENTRESS HD is contraindicated in patients with hypersensitivity to the drug.
ISENTRESS HD is associated with osteonecrosis, immune reactivation syndrome, myopathy and rhabdomyolysis, and rash. A complete list of potential adverse effects is provided in the product monograph.
ISENTRESS HD has been associated with depression and suicidal ideation and behaviors and should be used with caution in people with underlying psychiatric concerns.
Serious, even fatal rashes and organ dysfunction related to hypersensitivity reactions have been reported in patients taking ISENTRESS HD.
All patients who test positive for HIV infection should be screened for comorbid HBV and Hepatitis C virus (HCV) infection. Co-infected patients should be started on an antiretroviral regimen targeting co-infected viruses, regardless of CD4 counts or viral loads. Current HIV treatment guidelines outline drug regimens and prescribing considerations.
ISENTRESS HD is associated with a large number of drug-drug and herbal interactions and cautions. These are listed in the product monograph.
Pregnancy & Lactation
Highly active retroviral combination treatment should be used in all pregnant women, regardless of viral load and CD4 count. There is insufficient data to determine whether ISENTRESS HD causes birth defects. Current guidelines should be consulted when treating pregnant women. Excretion of ISENTRESS HD in breast milk is unknown. The CDC recommends that all HIV positive women, treated or untreated, avoid breastfeeding to prevent vertical transmission of the virus.
ISENTRESS HD overdose should be treated with standard supportive care and monitoring. It is unknown if raltegravir is dialyzable.
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