| DELAVIRDINE MESYLATe
Classifications: antiviral; nonnucleoside reverse transcriptase inhibitor (nnrti); Therapeutic: antiviral; nnrti
Pregnancy Category: C
100 mg tablets
Nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 binds directly to reverse transcriptase (RT) and disrupts
RNA- and DNA-dependent DNA polymerase activities.
It prevents replication of the HIV-1 virus. HIV-2 RT and human DNA polymerases such as polymerases alpha, gamma, and delta
are NOT inhibited by delavirdine. Resistant strains appear rapidly.
Treatment of HIV infection in combination with other antiretroviral agents.
Hypersensitivity to delavirdine; pregnancy (category C); lactation.
Impaired liver function; achlorhydria.
Route & Dosage
Adult: PO 400 mg t.i.d.
Child (≤16 y): PO 400 mg t.i.d.
- Disperse in water by adding a single dose to at least 3 oz of water, let stand for a few minutes, then stir to create a
uniform suspension just prior to administration.
- Give drug to patients with achlorhydria with an acid beverage such as orange or cranberry juice.
- Store at 20°25° C (68°77° F) and protect from high humidity in a tightly closed container.
Adverse Effects (≥1%)Body as a Whole:
, allergic reaction, chills, edema, arthralgia
Abnormal coordination, agitation, amnesia, anxiety, confusion, dizziness. CV:
Chest pain, bradycardia, palpitations, postural hypotension, tachycardia. GI:
Nausea, vomiting, diarrhea
, increased LFTs, abdominal cramps, anorexia, aphthous stomatitis
. Hematologic: Neutropenia. Respiratory: Bronchitis
, cough, dyspnea
. Skin: Rash,
, h2-receptor antagonists
decrease absorption; didanosine
should be taken 1 h apart to avoid decreased delavirdine levels; clarithromycin, fluoxetine, ketoconazole
may increase delavirdine levels; carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin
may decrease delavirdine levels; delavirdine may increase levels of clarithromycin, indinavir, saquinavir, dapsone, rifabutin, alprazolam, midazolam, triazolam, dihydropyridine
, calcium channel blockers
(e.g., nifedipine, nicardipine,
etc.), quinidine, warfarin.
Use with hmg-coa reductase inhibitors
may increase the risk of rhabdomyolysis. Use with pimozide
may cause cardiac arrhythmias. Use with trazodone
may increase trazodone
levels. Use with inhaled fluticasone
may increase fluticasone
levels. Use with hypnotics
, alprazolam, midazolam, triazolam
can cause respiratory depression
. Herbal: St. John's wort
may decrease antiretroviral activity.
Rapidly from GI tract, 80% reaches systemic circulation. Peak:
1 h. Distribution:
98% protein bound. Metabolism:
In the liver by CYP3A4. Elimination:
Half in urine, 44% in feces. Half-Life:
Assessment & Drug Effects
- Therapeutic effectiveness: Indicated by decreased viral load.
- Monitor for and immediately report appearance of a rash, generally within 13 wk of starting therapy; rash is usually
diffuse, maculopapular, erythematous, and pruritic.
Patient & Family Education
- Take this drug exactly as prescribed. Missed doses increase risk of drug resistance.
- Do not take antacids and delavirdine at the same time; separate by at least 1 h.
- Report all prescription and nonprescription drugs used to physician because of multiple drug interactions.
- Discontinue medication and notify physician if rash is accompanied by any of the following: Fever, blistering, oral lesions,
conjunctivitis, swelling, muscle or joint pain.