Delavirdine: Difference between revisions

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{{drugbox
__NOTOC__
| IUPAC_name = ''N''-[2-[4-[3-(1-methylethylamino) pyridin-2-yl] piperazin-1-yl] carbonyl-1''H''-indol-5-yl] methanesulfonamide
{{Delavirdine}}
| image = Delavirdine.svg
{{CMG}}; {{AE}} {{AZ}}
| CAS_number = 136817-59-9
| ATC_prefix = J05
| ATC_suffix = AG02
| ATC_supplemental =
| PubChem = 5625
| DrugBank = APRD00149
| C=22 | H=28 | N=6 | O=3 | S=1
| molecular_weight = 456.562 g/mol
| bioavailability = 85%
| protein_bound = 98%
| metabolism = [[Liver|Hepatic]] ([[CYP3A4]]- and [[CYP2D6]]-mediated)
| elimination_half-life = 5.8 hours
| excretion = [[Kidney|Renal]] (51%) and fecal (44%)
| pregnancy_AU = B3
| pregnancy_US = C
| legal_US = Rx-only
| routes_of_administration = Oral
}}
'''Delavirdine''' ('''DLV''') (brand name '''Rescriptor®''') is a non-nucleoside [[reverse transcriptase inhibitor]] (NNRTI) marketed by [[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. [[Food and Drug Administration]] in 1997, its efficacy is lower than other NNRTIs, especially [[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.<ref name="dhhs"> DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download from [http://www.aidsinfo.nih.gov/Guidelines/GuidelineDetail.aspx?MenuItem=Guidelines&Search=Off&GuidelineID=7&ClassID=1 AIDSInfo])</ref>
==Overview==
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 [[cytochrome P450]] isozyme [[CYP3A4]], and interacts with many medications. It should not be administered with a wide range of drugs, including [[amprenavir]], [[fosamprenavir]], [[simvastatin]], [[lovastatin]], [[rifampin]], [[rifabutin]], [[rifapentine]], [[St John's wort]], [[astemizole]], [[midazolam]], [[triazolam]], [[ergot]] medications, and several medications for [[acid reflux]].<ref name="dhhs" />


The most common adverse event is moderate to severe [[rash]], which occurs in up to 20% of patients.<ref>[http://www.pfizer.com/pfizer/download/uspi_rescriptor.pdf RESCRIPTOR® brand of delavirdine mesylate tablets. Product information.]</ref> Other common adverse events include [[fatigue (physical)|fatigue]], [[headache]] and [[nausea]]. Liver toxicity has also been reported.
==Category==
Antiretroviral drug
==References==
 
{{reflist|2}}
==US Brand Names==
 
==FDA Package Insert==
'''  [[Delavirdine description|Description]]'''
'''| [[Delavirdine clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Delavirdine microbiology|Microbiology]]'''
'''| [[Delavirdine indications and usage|Indications and Usage]]'''
'''| [[Delavirdine contraindications|Contraindications]]'''
'''| [[Delavirdine warnings and precautions|Warnings and Precautions]]'''
'''| [[Delavirdine adverse reactions|Adverse Reactions]]'''
'''| [[Delavirdine overdosage|Overdosage]]'''
'''| [[Delavirdine clinical studies|Clinical Studies]]'''
'''| [[Delavirdine dosage and administration|Dosage and Administration]]'''
'''| [[Delavirdine compatibility reconstitution and stability|Compatibility, Reconstitution, and Stability]]'''
'''| [[Delavirdine directions for use|Directions For Use]]'''
'''| [[Delavirdine how supplied|How Supplied]]'''
'''| [[Delavirdine labels and packages|Labels and Packages]]'''


{{HIVpharm}}
==Mechanism of Action==


[[Category:Non-nucleoside reverse transcriptase inhibitors]]
==References==
{{Reflist|2}}


[[fr:Delavirdine]]
[[Category:Antibiotics]]
{{WikiDoc Sources}}
[[Category:Wikinfect]]

Revision as of 05:00, 1 January 2014

Delavirdine
RESCRIPTOR® FDA Package Insert
Description
Clinical Pharmacology
Microbiology
Indications and Usage
Contraindications
Warnings and Precautions
Adverse Reactions
Overdosage
Clinical Studies
Dosage and Administration
How Supplied
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]

Overview

Category

Antiretroviral drug

US Brand Names

FDA Package Insert

Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | Compatibility, Reconstitution, and Stability | Directions For Use | How Supplied | Labels and Packages

Mechanism of Action

References

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