19
Elimination/
Metabolic Pathway
Serum
Half-Live Adverse Events
• Metabolized by
CYPs 2B6 and 3A4
• CYP3A4 mixed
inducer/inhibitor
(more an inducer
than an inhibitor)
40-55
hours
• Rash
b
• Neuropsychiatric symptoms
c
• Increased transaminase levels
• Hyperlipidemia
• False-positive results with some cannabinoid
and benzodiazepine screening assays reported.
• Teratogenic in non-human primates and
potentially teratogenic in humans
CYP3A4 substrate 50 hours • Rash
b
• Depression, insomnia, headache
• Hepatotoxicity
Elimination/
Metabolic Pathway
Serum
Half-Live Adverse Events Storage
• CYP3A4 inhibitor
and substrate
• Dosage adjustment
in patients
with hepatic
insufficiency is
recommended
(Table 4).
7 hours • Indirect hyperbilirubinemia
• PR interval prolongation: First
degree symptomatic AV block
reported. Use with caution
in patients with underlying
conduction defects or on
concomitant medications that
can cause PR prolongation.
• Cholelithiasis
• Nephrolithiasis
• Renal insufficiency
• Serum transaminase elevations
• Hyperlipidemia (especially with
RTV boosting )
• Skin rash
Room
temperature
(≤25º C or
77º F)
CYP3A4 inhibitor
and substrate
15 hours
(when
combined
with
RTV)
• Skin rash (10%): DRV has a
sulfonamide moiety; Stevens-
Johnson syndrome, toxic
epidermal necrolysis, acute
generalized exanthematous
pustulosis, and erythrema
multiforme have been reported.
• Avoid in patients with severe
sulfonamide allerg y
• Hepatotoxicity
• Diarrhea, nausea
• Headache
• Hyperlipidemia
• Serum transaminase elevation
