Rescriptor (delavirdine mesylate) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) drug that has been shown to reduce viral load and increase CD4 count in patients with HIV-1 infection when used as part of a combination regimen with other antiretroviral drugs. Rescriptor inhibits HIV-1 activity through direct binding to the reverse transcriptase enzyme, disrupting its catalytic site. Reverse transcriptase is a viral enzyme that synthesizes DNA on an RNA template. Delavirdine has synergistic properties when used with zidovudine, lamivudine, didanosine, zalcitabine, interferon-alpha, and protease inhibitors (PIs). The HIV-2 virus is resistant to NNRTI drugs, so Rescriptor should not be used in these patients.
Dosing and administration
Rescriptor can be used in adults and adolescents 16 years and older. Safety and efficacy in children under 16 years have not been established. The dose is 400mg by mouth three times a day, taken with or without food. It should be taken at least one hour before or after didanosine or any antacid medications. The 100mg tablets may be dissolved in water for patients who cannot swallow the tablets. Instructions for this are given in the product monograph.
Dosing in patients with hepatic dysfunction has not been established. Elevated serum transaminase levels occur in approximately 25% of patients taking delavirdine, but clinically significant hepatotoxicity appears to be rare. Rescriptor is metabolized by the liver, so caution is advised if used in patients with liver disease. Dosing in patients with renal impairment has also not been established.
The most common adverse reaction seen with Rescriptor is skin eruption, and patients should report any rash to their physician. Rash is most commonly seen within one to three weeks of initiating treatment, and usually self-resolves in three to 14 days. Symptomatic treatment usually suffices without discontinuing treatment.
Other side effects include:
- redistribution of body fat
A complete list of described adverse effects is available in the product monograph and should be consulted by prescribers.
In accordance with current guidelines, patients infected with HIV should be screened for comorbid hepatitis B virus (HBV) and hepatitis C virus (HCV) infection. The presence of co-infection requires special attention and guidelines should be followed closely.
A complete list of described drug interactions are available in the product monograph and should be consulted by prescribers.
Pregnancy and lactation
Highly active retroviral combination treatment should be used in all pregnant women, regardless of viral load and CD4 count. Rescriptor should not be used during pregnancy unless other options are unavailable. Clinicians should report exposure to Rescriptor before or during pregnancy to the Antiretroviral Pregnancy Registry to assist in data collection. Current guidelines should be consulted when treating women in pregnancy. It is unknown if Rescriptor is excreted in the breast milk. The CDC recommends that all HIV positive women, treated or untreated, avoid breastfeeding to prevent vertical transmission of the virus.
In the occurrence of an overdose, patients should seek medical attention immediately and call a local poison control centre.
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