17
Elimination
Serum/
Intracellular
Half-Lives Adverse Events
b
• Metabolized by alcohol
dehydrogenase and
glucuronyl transferase
• Renal excretion of
metabolites: 82%
• Dosage adjustment for
ABC is recommended
in patients with hepatic
insufficiency (Table 4).
1.5 hours/12-26
hours
• Hypersensitivity reaction (HSR):
Patients who test positive for
HLA-B*5701 are at highest risk.
HLA screening should be done
before initiation of ABC. Do not
rechallenge after possible HSR.
• Symptoms of HSR may include
fever, rash, nausea, vomiting,
diarrhea, abdominal pain, malaise,
or fatigue or respiratory symptoms
such as sore throat, cough, or
shortness of breath.
• Some cohort studies suggest
increased risk of MI with recent or
current use of ABC, but this risk
has not been observed in all.
• Renal excretion: 86%
• Dosage adjustment
in patients with
renal insufficiency is
recommended (Table 4).
10 hours/
>20 hours
• Minimal toxicity
• Hyperpigmentation/skin
discoloration
• Severe acute exacerbation of
hepatitis may occur in HBV-
coinfected patients who
discontinue FTC.
• Renal excretion: 70%
Dosage adjustment
in patients with
renal insufficiency is
recommended (Table 4).
5-7 hours/18-22
hours
• Minimal toxicity
• Severe acute exacerbation of
hepatitis may occur in HBV-
coinfected patients who
discontinue 3TC.
• Renal excretion - primary
route of elimination
• Dosage adjustment
in patients with
renal insufficiency is
recommended (Table 4).
17 hours/
>60 hours
• Renal insufficiency, Fanconi
syndrome, proximal tubulopathy
• Osteomalacia, decrease in bone
mineral density
• Severe acute exacerbation
of hepatitis may occur in
HBV- coinfected patients who
discontinue TDF.
• Asthenia, headache, diarrhea,
nausea, vomiting, and flatulence