delavirdine (Rescriptor)
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Introduction
Tradename: Rescriptor.
Indications
treatment of HIV infection
Dosage
400 mg PO TID, with or without food
Pharmacokinetics
- well absorbed following oral administration
- 98% bound to plasma proteins, primarily albumin
- metabolized in the liver by cyt P450 3A4
- 51% excreted in the urine, 5% unchanged
- 1/2life 5.8 hours
elimination via kidney
elimination via liver
1/2life = 5.8 hours
protein binding = 98 %
Adverse effects
- drug adverse effects of antiretroviral agents
- drug adverse effects of non-nucleoside reverse transcriptase inhibitors (NNRTI)
Drug interactions
- any drug that inhibits cyt P450 3A4 may increase levels of delavirdine
- any drug that induces cyt P450 3A4 may diminish levels of delavirdine
- delavirdine inhibits cyt P450 3A4, thus inhibits its own metabolism & metabolism of other cyt P450 3A4 substrates
- not recommended for concurrent use with:
- delavirdine increases serum levels of:
- separate administration of antacids & delavirdine by > 1 hour
Laboratory
Mechanism of action
- non-nucleoside reverse transcriptase inhibitor
- binds directly to reverse transcriptase
- blocks RNA-dependent & DNA-dependent DNA polymerase
- emergence of resistance is a problem
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, 15, American College of Physicians, Philadelphia 1998, 2009
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com