Page 236 - HIV/AIDS Guidelines

Appendix B, Table 4. Characteristics of Integrase Inhibitor (Last updated March 27, 2012; last
reviewed March 27, 2012)

Dosing Recommendations
Generic Name Route of
Serum/
(abbreviation)/ Formulations (For dosage adjustment in Half-life Metabolism Adverse Events
hepatic insufficiency, see
Trade Name (Also see Table 13)
Appendix B, Table 7.)
Raltegravir (RAL)/ • 400-mg tablet 400 mg BID ~9 hrs UGT1A1- • Rash, including Stevens-Johnson
Isentress mediated syndrome, HSR, and toxic epidermal
• 25-, 100-mg With rifampin: glucuronidation necrolysis
chewable tablets 800 mg BID
• Nausea
Take without regard to meals.
• Headache
• Diarrhea
• Pyrexia
• CPK elevation, muscle weakness,
and rhabdomyolysis

Key to Abbreviations: BID = twice daily, CPK = creatine phosphokinase, HSR = hypersensitivity reaction, RAL = raltegravir, UGT = uridine diphosphate
gluconyltransferase

Appendix B, Table 5. Characteristics of Fusion Inhibitor (Last updated January 29, 2008; last
reviewed March 27, 2012)

Generic Name Dosing Serum/ Adverse Events
(abbreviation)/ Formulations Recommendation Half-life Elimination Storage (Also see Table 13)
Trade Name
Enfuvirtide (T20)/ • Injectable— 90 mg (1mL) 3.8 hrs Expected to Store at room • Local injection site reactions
Fuzeon supplied as subcutaneously BID undergo catabolism temperature (up (pain, erythema, induration,
lyophilized to its constituent to 25ºC or 77ºF). nodules and cysts, pruritus,
powder amino acids, with ecchymosis) in almost 100% of
Reconstituted
subsequent patients
• Each vial contains solution should
recycling of the
108 mg of T20; be refrigerated at • Increased incidence of bacterial
amino acids in the
reconstitute with 2ºC–8ºC (36ºF– pneumonia
body pool
1.1mL of sterile 46Fº) and used
• HSR (<1% of patients):
water for injection within 24 hours.
Symptoms may include rash,
for delivery of
fever, nausea, vomiting, chills,
approximately 90
rigors, hypotension, or elevated
mg/1 mL.
serum transaminases.
Rechallenge is not
recommended.
Key to Abbreviations: BID = twice daily, HSR = hypersensitivity reaction, T20 = enfuvirtide

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents O-11

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