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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.)
Route of Metabolism Adverse Events
(Also see Table 13.)
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
(EVG) Currently only available as a co-formulated product with:

(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