21
Elimination/
Metabolic Pathway
Serum
Half-Live Adverse Events Storage
CYP3A4 inhibitor
and substrate
5-6 hours • GI intolerance, nausea, vomiting,
diarrhea
• Pancreatitis
• Asthenia
• Hyperlipidemia (especially
hypertriglyceridemia)
• Serum transaminase elevation
• Hyperglycemia
• Insulin resistance/diabetes
mellitus
• Fat accumulation
• Possible increased bleeding
episodes in patients with
hemophilia
• PR interval prolongation
• QT interval prolongation and
torsades de pointes have been
reported; however, causality
could not be established.
Oral tablet
is stable
at room
temperature.
Oral solution
is stable
at 2°-8° C
(36°-46° F)
until date on
label and is
stable for up
to 2 months
when stored
at room
temperature
(≤25º C or
77º F).
Elimination/
Metabolic Pathway
Serum
Half-Live Adverse Events
b
UGT1A1-mediated
glucuronidation
~14 h ▶ Insomnia
▶ Headache
CYP3A enzyme-
mediated metabolism;
also glucuronidation
by UGT1A1/3
enzymes
12.9 h ▶ Nausea
▶ Diarrhea
▶ See also cobicistat, tenofovir, emtricitabine
UGT1A1-mediated
glucuronidation
~9 h ▶ Nausea
▶ Headache
▶ Diarrhea
▶ Pyrexia
▶ CPK elevation, muscle weakness, myopathy, and
rhabdomyolysis
▶ Rare severe skin and sysemic reactions
CYP3A metabolism
(minor CYP2D6
metabolism)
3.5 hours • Diarrhea
• Inhibition of creatinine excretion resulting in early
increase in serum creatinine (~0.14 mg/dL) and
decrease in eGFR; no effect on actual GFR
• See also elvitegravir, tenofovir, emtricitabine
c
Adverse events can include dizziness, somnolence, insomnia, abnormal dreams, depression,
suicidality, confusion, abnormal thinking, impaired concentration, amnesia, agitation,
depersonalization, hallucinations, and euphoria. Approximately 50% of patients receiving EFV
may experience any of these symptoms. Symptoms usually subside spontaneously aer 2 to 4 weeks
but may necessitate discontinuation of EFV in a small percentage of patients.
d
See full prescribing information.
