Non-Nucleoside Reverse Transcriptase Inhibitors: Delavirdine
Contents Introduction Information card Pharmacokinetics Dosing Side effects Drug interactions

Introduction

The information represented on this drug does not necessarily correspond with the information that can be found in the Belgian scientific leaflet.
In April of 1997, the FDA approved delavirdine for use in the treatment of HIV infection. Delavirdine belongs to the bis(heteroaryl)piperazines chemical class, and is chemically very different from nevirapine. (106)

Abbreviation(s):  Generic name: Brand name: DLV delavirdine Rescriptor®		USA (FDA) Adult approval date: Pediatric approval date: April 4, 1997 No pediatric labeling
Pharmaceutical co.: Pharmacia & Upjohn		Belgium: Not yet commercialized

Pharmacokinetics

Delavirdine may be taken fasting or with meals. The drug has a relatively short half-life (approximately 6 hours in plasma). Although delavirdine crosses the blood-brain barrier, cerebral spinal fluid levels are likely to be low. Antacids appear to decrease delavirdine absorption. Therefore, patients should be encouraged to separate delavirdine and antacid dosing by at least 1 hour.(106)

Dosing

The recommended dose is 400 mg three times daily. (106)

Side effects

Rash is the most frequent adverse event associated with delavirdine. The typical skin rash associated with delavirdine is a diffuse, erythematous maculopapular skin eruption. Although pruritis is common, urticaria (hives) is rare. If the rash is mild, most patients can be successfully treated without drug interruption.In rare cases, delavirdine-associated rash may be severe or potentially life threatening. Systemic systems, mucosal involvement, facial swelling, ulcerations, purpura, and desquamation are all worrisome signs. In these cases, delavirdine should be discontinued permanently.(106)
Other events include mild to moderate headache, nausea, diarrhea, and fatigue. Delavirdine use is also associated with increases in liver transaminases. Rare cases of anemia and neutropenia have been reported. (106)

Drug interactions

Delavirdine is metabolized by the cytochrome P450 CYP3A. Because delavirdine also inhibits P450 CYP3A, the drug may affect the metabolism of other medications. In particular, delavirdine may increase serum concentrations of certain anti-arrhythmics, terfenadine, astemizole, and cisapride, leading to potential cardiac arrhythmias. Delavirdine should not be used with these drugs. Delavirdine will likely increase plasma concentrations of sedative hypnotics (alprazolam, midazolam, triazolam), clarithromycin, ergot derivatives, calcium channel blockers, and warfarin. Caution is required when using delavirdine with any of these agents. Rifampin and rifabutin reduce serum concentrations of delavirdine; concurrent therapy should be avoided if possible. Phenytoin, carbamazepine, and phenobarbital may also decrease delavirdine serum concentrations. Antacid can decrease delavirdine absorption. Therefore, the dosing of delavirdine and antacid should be separated by at least 1 hour. (106,114)
 

Interactions with other antiretroviral agents

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