Delavirdine

(CC) Image: David E. Volk Delavirdine, a non-nucleoside reverse transcriptase inhibitor for HIV-1.
delavirdine
IUPAC name: see chemistry section Synonyms: SPP Formula: C22H28N6O3S
Uses:	HIV
Properties:	Reverse Transcriptase inhibitor
Hazards:	see drug interactions
Mass (g/mol): CAS #: 456.5611 136817-59-9

Delavirdine (DLV), also called SPP, is an antiviral drug that is a non-nucleoside, reverse transcriptase inhibitor (nNRTI) specific for HIV-1. It binds directly to reverse transcriptase catalytic site and blocks the DNA polymerase activity. HIV-2 RT and eukaryotic (human, for example) DNA polymerases are not effected by this drug. Rashes are the major side effect of delavirdine toxicity, and they should be reported to the attending physician. Rashes typically are resolved in two weeks or less, but patients with severe rash or rash accompanied by fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches should discontinue medication and consult a physician.

Chemistry

Its chemical name is N-[2-[4-[3-(propan-2-ylamino)pyridin-2-yl]piperazine-1-carbonyl]-1H-indol- 5-yl]methanesulfonamide and its chemical formula is C₂₂H₂₈N₆O₃S (Molecular Mass 456.5611).

Drug interactions

The effect of delavirdine is decreased when used with St. John's Wort, antacids, some anticonvulsants such as carbamazepine, fosphenytoin, methylphenobarbital, phenobarbital and phentoin, and with rifampin or rifabutin. Amprenavir and derivatives (Fosamprenavir) decrease delavirdine levels.

Delavirdine increases the effects and toxicity of benzodiazepine when taken with alprazolam, midazolam or triazolam and also the effects of some statins, including atorvastatin, lovastatin and simvastatin. The toxicity of ergot may be a concern when delavirdine is taken with the ergot derivatives dihydroergotamine, dihydroergotoxine, ergonovine, ergotamine, methylergonovine, and methysergide. An increased risk of cardiotoxicity and arrhythmias are noted when delavirdine is taken with astemizole, cisapride or terfenadine. The effects of the antiviral drugs indinavir and ritonavir are increased when taken with delavirdine. Increased toxicity is also noted with quinupristin and saquinavir.

External Links

• Delavirdine - FDA approved drug information (drug label) from DailyMed (U.S. National Library of Medicine).
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