Rescriptor

Non-Nucleoside Reverse Transcriptase Inhibitor

Common Name: delavirdine (DLV)

Brand Name: Rescriptor

Class: non-nucleoside analog (also called non-nucleoside reverse transcriptase inhibitor, NNRTI or non-nuke)

Standard dose: Two 200 mg tablets or four 100 mg tablets three times a day (every 8 hours). Only the 100 mg tablets can be dissolved in liquid; however, avoid grapefruit juice. No food restrictions (may be taken with or without food). Take missed dose as soon as possible, but do not double up on your next dose.

AWP: $344.83 / month for 200 mg

Manufacturer contact: Pharmacia and Upjohn Company, a Pfizer company, www.pfizer.com, 1-800-879-3477 (TRY-FIRST)

AIDSInfo:
1 (800) HIV-0440 (448-0440), www.aidsinfo.nih.gov

Potential side effects and toxicity: Most common side effects include headache, nausea, vomiting, diarrhea, fatigue, elevated liver enzymes, and itchy skin or rash. A serious side effect of the NNRTI class is rash, which can be life-threatening. Most rashes occur within the first 1-3 weeks after starting Rescriptor. If you experience blistering, mouth lesions, conjunctivitis (redness or inflammation of eye, which if untreated may result in permanent vision loss), swelling, muscle or joint aches, fever or general malaise (general ill feeling), you may need to stop the medication, so seek medical attention right away. Body fat accumulation or redistribution may occur.

Potential drug interactions: You cannot take Rescriptor with oral Versed (midazolam), Halcion (triazolam), Xanax (alprazolam), Orap (pimozide), ergot alkaloids, used for migraine headaches (Wigraine, Methergine, and Cafergot) in any form, or the herb St. John's wort. Do not use Zocor (simvastatin), Vytorin, or Mevacor (lovastatin) cholesterol (lipid) lowering meds; suggested alternatives are Lipitor (atorvastatin), Lescol (fluvastatin), Crestor (rosuvastatin), and Pravachol (pravastatin, the one with less frequency of problems and interactions according to study data). Liver enzymes should be checked regularly if you are on these cholesterol meds, as they can increase risk for liver toxicity with Rescriptor. Certain amphetamines and antiarrhythmic drugs should not be used with Rescriptor, therefore inform your health care provider if you have a history of heart or blood pressure problems. Potential toxicity when taken with Biaxin (clarithromycin), dapsone, Mycobutin (rifabutin), Procardia or Adalat (nifedipine), Norvasc (amlodipine), Plendil (felodipine), Coumadin (warfarin), and quinidine. Use caution with Tegretol (carbamazepine, an anti-seizure medication, also used to treat peripheral neuropathy), phenobarbital, and Dilantin (phenytoin). Mycobutin and rifampin (used to treat tuberculosis) are drugs that decrease Rescriptor levels. Rescriptor is not recommended with either rifampin or Mycobutin. Rescriptor increases levels of Crixivan, Lexiva, Invirase, Kaletra, Norvir, Reyataz, Viracept, immunosuppressants, birth control pills (ethinyl estradiol), and methadone, so caution is advised if using together. Cialis, Levitra, and Viagra levels are increased by Rescriptor; doses should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours. Also, increased levels of trazodone (Desyrel) can occur with Rescriptor. A lower dose of trazodone is recommended. Increased levels of the inhaled and nasal sprays that contain fluticasone, a steroid for asthma or allergies (found in Advair, Flonase, and Flovent) can occur with Rescriptor and therefore should be used with caution.

Tips: Research demonstrates smaller doses of Rescriptor increase blood levels of some protease inhibitors, making it unique among the NNRTIs. Some people who cannot tolerate Norvir (ritonavir) are successfully using Rescriptor instead to boost their protease inhibitor. Studies of this use, however, have not been published. Antacids (like Tagamet, Zantac, Prilosec, and Tums) and gastric achlorhydria (low stomach acid) decrease absorption of Rescriptor, so take at least one hour apart from these drugs and take with acidic beverages such as orange or cranberry juice to increase stomach acidity. Please see package insert for more complete potential side effects and interactions.

Doctor

Rescriptor (delavirdine) was approved for the treatment of HIV infection in 1997. The dosing regimen of this antiretroviral is a good example of the large number of pills that had to be taken multiple times per day in the past. The original dosing schedule was 4 tablets three times daily (thankfully no dietary restrictions). When the pill size changed, it came down to 2 pills three times per day. In general, this antiretroviral is not used to any great extent in current HAART therapy. Our clinic participated in the first clinical trials with this drug. The most common problems we observed with delavirdine were skin rash and liver function abnormalities. Data is available suggesting delavirdine can be used (like Norvir) to boost levels of other protease inhibitors (mostly indinavir, nelfinavir, saquinavir, and amprenavir), but the drug has to be taken in full dose to be effective. That would be a painful reminder of yesteryear! -- Frank M. Graziano, M.D., Ph.D.

Activist

Rescriptor, the first non-nuke, was quickly overshadowed and superseded by Viramune and Sustiva. It has a myriad of drug-drug interactions from Flonase to Viagra and everything in-between; and comparatively speaking, has a high pill burden (two 200 mg tablets, three times a day). Rescriptor has all but vanished into obscurity. -- Morris Jackson

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