Delavirdine



Delavirdine
Systematic (IUPAC) name
N-[2-[4-[3-(1-methylethylamino) pyridin-2-yl] piperazin-1-yl] carbonyl-1H-indol-5-yl] methanesulfonamide
Identifiers
CAS number 136817-59-9
ATC code J05AG02
PubChem 5625
DrugBank APRD00149
Chemical data
S 
Mol. mass 456.562 g/mol
Pharmacokinetic data
Bioavailability 85%
Protein binding 98%
CYP2D6-mediated)
Half life 5.8 hours
Excretion Renal (51%) and fecal (44%)
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US)

Legal status

℞-only(US)

Routes Oral

Delavirdine (DLV) (brand name Rescriptor®) is a non-nucleoside Pfizer. It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. It is presented as the mesylate. The recommended dosage is 400 mg, three times a day.

Although delavirdine was approved by the U.S. efavirenz, and it also has an inconvenient schedule. These factors have led the U.S. DHHS not to recommend its use as part of initial therapy.[1] The risk of cross-resistance across the NNRTI class, as well as its complex set of drug interactions, make the place of delavirdine in second-line and salvage therapy unclear, and it is currently rarely used.

Like ritonavir, delavirdine is an inhibitor of ergot medications, and several medications for acid reflux.[1]

The most common adverse event is moderate to severe rash, which occurs in up to 20% of patients.[2] Other common adverse events include fatigue, headache and nausea. Liver toxicity has also been reported.

References

  1. ^ a b DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download from AIDSInfo)
  2. ^ RESCRIPTOR® brand of delavirdine mesylate tablets. Product information.
v • d • e
Antivirals used against HIV (first-line agent.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Delavirdine". A list of authors is available in Wikipedia.