Treatment Information 
Fact Sheet:  Rescriptor (delavirdine mesylate)

Delavirdine (Rescriptor) received accelerated approval from the FDA (Food and Drug Administration) for use in combination with other antiretroviral therapies for the treatment of HIV when therapy is warranted. Results from the various studies suggest that delavirdine must be used in combination with other anti-HIV drugs. However, the role of delavirdine and how it can be optimally used as a treatment for HIV is still not known.

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRTIs use a different mechanism to stop HIV from replicating compared to the nucleoside analogue reverse transcriptase inhibitor (NARTI) drugs such as AZT, ddI, ddC, d4T and 3TC. Both target the reverse transcriptase enzyme which is essential for HIV to reproduce. The FDA has approved one other NNRTI, nevirapine (Viramune), and others are in clinical studies including efavirenz.

Pregnant Women and Children
Delavirdine has not been studied in pregnant women. A study is planned to look at whether delavirdine can prevent or reduce the risk of transmission of HIV from mother to child.

Delavirdine has not been studied in children. Several studies are planned to determine the appropriate dosing for children.

Delavirdine has not been formally studied in pregnant women. However, in animal studies, the drug caused serious side effects to the mother and the fetus, including cancer and developmental problems. It is not known if the same would be true in humans. Delavirdine should be used during pregnancy only if the potential benefits justify the risks involved.

HIV and the Brain
Because HIV can infect brain cells, it's important to consider a drug's ability to reach the brain when putting together an anti-HIV regimen. It's probably wise to include at least one drug that has been shown to cross the blood-brain barrier to some useful degree as part of your regimen. These include AZT (zidovudine, Retrovir), d4T (stavudine, Zerit), abacavir (Ziagen), nevirapine (Viramune), amprenavir (Agenerase) and to a lesser degree indinavir (Crixivan) and 3TC (lamivudine, Epivir). Efavirenz (Sustiva) has not been shown to cross the barrier to a significant degree, but some experts speculate that it might have some useful effect in impacting HIV in the spinal fluid.

What About Side Effects?
The most common side effects these studies report include rash (18%), nausea (6.8%), headache (5.6%), fatigue (3.7%), diarrhea (4.2%) and increased liver function tests (5.8%). The rash primarily affects the upper body and is less intense on the rest of the body. The rash can occur within 1-three weeks of starting delavirdine and lasts for about two weeks. The effects of the rash can be diminished with use of antihistamines or topical corticosteroids. If the rash becomes severe, contact your physician immediately.

How to Use It?

Dosing
The recommended dose of delavirdine is 400mg (four 100mg tablets) three times a day for a total dose of 1,200mg daily. Delavirdine can be taken on an empty stomach or with food. Delavirdine can also be dispersed in water and drunk immediately. However, it is important that the complete dose is taken.

Delavirdine should always be used as part of a three- or four-drug combination that includes nucleoside analogue drugs and/or protease inhibitors. These "companion" drugs are critically needed to enhance its antiviral activity and the duration of the treatment effect.

Drug Interactions
There are a number of drug interactions between delavirdine and other commonly used therapies (for a complete list of drug interactions, call the Project Inform National HIV/AIDS Treatment Hotline). Delavirdine should NOT BE USED with alprazolam (Xanax), astemizole (Hismanal), cisapride (Propulsid), midazolam (Versed), Rifampin (Rifadin, Rifater), terfenadine (Seldane) and triazolam (Halcion) as their use in combination with delavirdine may lead to serious and/or life-threatening side effects. 

A recent study shows that garlic supplements decrease saquinavir levels by half and probably greatly lower the levels of protease inhibitors and NNRTIs, like delavirdine. People who use herbal or natural therapies should always discuss possible interactions with their doctors or pharmacists.

Another recent study shows that garlic supplements decrease saquinavir levels by half and probably greatly lower the levels of protease inhibitors and NNRTIs, like delavirdine. People who use herbal or natural therapies should always discuss possible interactions with their doctors or pharmacists.

Food Interactions
Delavirdine may be taken with or without food.

How To Get It?
Delavirdine is available by prescription through hospitals and pharmacies.

This information was provided by the Community AIDS Treatment Information Exchange (CATIE). For more information, contact CATIE at 1-800-263-1638.

Updated July 13, 2004

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