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

Appendix B: Drug Characteristics Tables

Characteristics of Integrase Inhibitors

(Last updated:2/12/2013; last reviewed:2/12/2013)

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Appendix B, Table 4. Characteristics of Integrase Inhibitors
Generic Name (Abbreviation)/ Trade Name Formulations Dosing Recommendations
(For dosage adjustment in hepatic insufficiency, see Appendix B, Table 7.)
Serum
Half-Life
 
Route of Metabolism Adverse Events
(Also see Table 13.)
Raltegravir
(RAL)/
Isentress
400 mg tablet

25, 100 mg chewable tablets
400 mg BID With rifampin:
800 mg BID
Take without regard to meals.
~9 hours UGT1A1-mediated glucuronidation
  • Rash, including Stevens-Johnson syndrome, HSR, and toxic epidermal necrolysis
  • Nausea
  • Headache
  • Diarrhea
  • Pyrexia
  • CPK elevation, muscle weakness, and rhabdomyolysis
Elvitegravir
(EVG) Currently only available as a co-formulated product with:

Cobicistat
(COBI)/
TDF/FTC
Stribild
(EVG 150 mg +
COBI 150 mg +
TDF 300 mg + FTC 200 mg) tablet
1 tablet once daily with food Not recommended for patients with baseline CrCl< 70 mL/min. See Appendix B Table 7 for the equation for calculating CrCl. Not recommended for use with other antiretroviral drugs ~13 hours EVG: CYP3A, UGT1A1/3 COBI: CYP3A, CYP2D6 (minor)
  • Nausea
  • Diarrhea
  • New onset or worsening renal impairment
  • Potential decrease in bone mineral density
  • Severe acute exacerbation of hepatitis may occur in HBV-coinfected patients who discontinue FTC and TDF.

Key to Abbreviations: BID = twice daily, COBI = cobicistat, CPK = creatine phosphokinase, CrCl = creatinine clearance, EVG = elvitegravir, FTC = emtricitabine, HSR = hypersensitivity reaction, RAL = raltegravir, TDF = tenofovir, UGT = uridine diphosphate gluconyltransferase