19
Table 5C. Characteristics of Protease Inhibitors (PIs) (cont'd)
Drug Formulation Dosing Recommendations Elimination
Serum
Half-life Storage Adverse Events
Tipranavir (TPV)
Aptivus
®
250 mg capsules or
100 mg/mL oral solution
(TPV 500 mg + RTV 200 mg )
orally bid
▶ Unboosted TPV is NOT
recommended
▶ TPV taken with RTV tablets:
Take with meals
▶ TPV taken with RTV capsules
or solution: Take without
regard to meals
Cytochrome
P450 3A4
inducer and
substrate
Net effect
when
combined
with RTV
(CYP
3A4, 2D6
inhibitor)
6 h aer
single
dose of
TPV/r
Refrigerate
capsules
Capsules can
be stored
at room
temperature
(25
º
C or
77
º
F) for up
to 60 days
Oral solution
should not be
refrigerated
or frozen and
should be
used within
60 days aer
opening the
bottle
▶ Hepatotoxicity—clinical hepatitis (including
hepatic decompensation and hepatitis-
associated fatalities) has been reported;
monitor closely, especially in pts with
underlying liver disease
▶ Skin rash—TPV has a sulfonamide
moiety; use with caution in pts with
known sulfonamide allerg y
▶ Rare cases of fatal and nonfatal intracranial
hemorrhages have been reported; most pts
had underlying comorbidity, such as brain
lesion, head trauma, recent neurosurgery,
coagulopathy, hypertension, or alcoholism,
or were on medication with increased risk
of bleeding
▶ Hyperlipidemia (especially
hypertriglyceridemia)
▶ Hyperglycemia
▶ Fat maldistribution
▶ Possible increased bleeding episodes in pts
with hemophilia
Table 5D. Characteristics of Integrase Strand Transfer
Inhibitors (INSTIs)
Drug Formulation Dosing Recommendations Route of Metabolism Serum Half-life Adverse Events
Dolutegravir
(DTG)
Tivicay
®
50 mg tablets Adults: 50 mg once daily
a
Children and Adolescents:
≥12 years and ≥40 kg:
50 mg once daily
a
UGT1A1-mediated
glucuronidation
~14 h ▶ Insomnia
▶ Headache
Elvitegravir (EVG)
Available only as
FTC/TDF/
EVG/COBI
Stribild
®
Tablets: FTC 200 mg +
TDF 300 mg +
EVG 150 mg +
COBI 150 mg
Adults: One tablet once daily
with food
CYP3A enzyme-
mediated metabolism;
also glucuronidation
by UGT1A1/3
enzymes
12.9 h ▶ Nausea
▶ Diarrhea
▶ See also cobicistat, tenofovir,
emtricitabine
Raltegravir (RAL)
Isentress
®
400 mg tablets
Chewable tablets 100 mg
scored and 25 mg
Adults: 400 mg bid
With rifampin: 800 mg bid
Children and Adolescents:
≥12 years: 400 mg bid
6–11 years:
≥25 kg: One 400 mg bid or
chewable tablets
(weight based
a
;
max, 300 mg bid)
<25 kg: Chewable tablets:
weight based
a
Max: 300 mg bid
2 to <6 years:
If ≥10 kg: Chewable tablets:
weight based
a
Max: 300 mg bid
▶ Take without regard to meals
UGT1A1-mediated
glucuronidation
~9 h ▶ Nausea
▶ Headache
▶ Diarrhea
▶ Pyrexia
▶ CPK elevation, muscle weakness,
myopathy, and rhabdomyolysis
▶ Rare severe skin and sysemic reactions
a
See full prescribing information.
