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delavirdine (Rescriptor)
Tradename: Rescriptor.
Indication: treatment of HIV infection
Dosage: 400 mg PO TID, with or without food
Pharmacokinetics:
1) well absorbed following oral administration
2) 98% bound to plasma proteins, primarily albumin
3) metabolized in the liver by cyt P450 3A4
4) 51% excreted in the urine, 5% unchanged
5) 1/2life 5.8 hours
Adverse effects: rash & headache
Drug interactions:
1) any drug that inhibits cyt P450 3A4 may increase levels of delavirdine
2) any drug that induces cyt P450 3A4 may diminish levels of delavirdine
3) delavirdine inhibits cyt P450 3A4, thus inhibits its own metabolism & metabolism of other cyt P450 3A4 substrates
4) not recommended for concurrent use with:
a) terfenadine
b) astemizole
c) alprazolam
d) midazolam
e) cisapride
f) rifabutin
g) rifampin
h) triazolam
i) ergot derivatives
j) amphetamines
k) nifedipine
l) anticonvulsants
5) delavirdine increases serum levels of:
a) clarithromycin
b) dapsone
c) quinidine
d) warfarin
e) indinavir
f) saquinavir
6) separate administration of antacids & delavirdine by > 1 hour
Laboratory:
- delavirdine in serum/plasma
Mechanism of action:
1) non-nucleoside reverse transcriptase inhibitor
2) binds directly to reverse transcriptase
3) blocks RNA-dependent & DNA-dependent DNA polymerase
4) emergence of resistance is a problem
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
General
non-nucleoside reverse transcriptase inhibitor (NNRTI)
Properties
MISC-INFO: elimination route KIDNEY
LIVER
1/2life 5.8 HOURS
protein-binding 98%
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
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#: 220233
(subscription needed) http://www.prescribersletter.com