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Table of Contents

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: April 8, 2015; last reviewed: April 8, 2015)

Appendix B, Table 4. Characteristics of Integrase Inhibitors
Generic Name
Trade Name
Formulations Dosing Recommendationsa Elimination/
Metabolic Pathways
Serum Half-Life Adverse Eventsb

Also available as a component of fixed-dose combination.
  • 50 mg tablet
ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
  • 50 mg once daily
ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin
  • 50 mg BID
INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance:
  • 50 mg BID
Take without regard to meals
UGT1A1 mediated glucuronidation

Minor contribution from CYP3A4
~14 hours 
  • HSRs including rash, constitutional symptoms, and organ dysfunction (including liver injury) have been reported.
  • Insomnia
  • Headache
  • (DTG 50 mg plus 3TC 300 mg plus ABC 600 mg) tablet
  • Take 1 tablet daily without regard to meals.

Also available as a component of fixed-dose combination.
85 and 150 mg tablets
With Once Daily ATV/r or Twice Daily LPV/r:
  • 85 mg once daily with food
With Twice Daily DRV/r, FPV/r, or TPV/r:
  • 150 mg once daily with food
Unboosted EVG is not recommended.
CYP3A, UGT1A1/3 substrate
~9 hours
  • Nausea
  • Diarrhea
  • (EVG 150 mg plus COBI 150 mg plus FTC 200 mg plus TDF 300 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.
EVG: As above

COBI: CYP3A, CYP2D6 (minor); CYP3A inhibitor
~13 hours 
  • 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.
  • 400 mg tablet
  • 25 and 100 mg chewable tablets
  • 100 mg single packet for oral suspension
400 mg BID

With Rifampin:
  • 800 mg BID
Take without regard to meals.
UGT1A1-mediated glucuronidation ~9 hours
  • Rash, including Stevens-Johnson syndrome, HSR, and toxic epidermal necrolysis
  • Nausea
  • Headache
  • Diarrhea
  • Pyrexia
  • CPK elevation, muscle weakness, and rhabdomyolysis
  • Insomnia
a For dosage adjustment in hepatic insufficiency, see Appendix B, Table 7.

b Also see Table 14.

Key to Abbreviations: 3TC = lamivudine; ABC = abacavir; ARV  = antiretroviral; ATV/r = atazanavir/ritonavir; BID = twice daily; c, COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HBV = hepatitis B virus; HSR = hypersensitivity reaction; INSTI = integrase strand transfer inhibitor; LPV/r = lopinavir/ritonavir; RAL = raltegravir; TDF = tenofovir disoproxil fumerate; TPV/r = tipranavir/ritonavir; UGT = uridine diphosphate gluconyltransferase

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