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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:May 01, 2014; last reviewed:May 01, 2014)

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Appendix B, Table 4. Characteristics of Integrase Inhibitors
Generic Name (Abbreviation)/ Trade Name Formulations Dosing Recommendationsa
 
Elimination/
Metabolic Pathway
 
Serum
Half-Life
 
Adverse Eventsb
Dolutegravir
(DTG)
Tivicay
50 mg tablet
ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
  • 50 mg once daily
ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Co-Administered 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
  • Elvitegravir
    (EVG) 
    Stribild (only available as a co-formulated product with cobi/TDF/FTC)
    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.
    EVG: CYP3A, UGT1A1/3

    cobi: CYP3A, CYP2D6 (minor)
    ~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.
  • Raltegravir
    (RAL)/
    Isentress
    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
    a For dosage adjustment in hepatic insufficiency, see Appendix, Table 7.
    b Also see Table 14.

    Key to Abbreviations: BID = twice daily; cobi = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; FTC = emtricitabine; FPV/r = ritonavir-boosted fosamprenavir; HBV = hepatitis B virus; HSR = hypersensitivity reaction; INSTI = integrase strand transfer inhibitor; RAL = raltegravir; TDF = tenofovir disoproxil fumerate; TPV/r = ritonavir-boosted tipranavir ; UGT = uridine diphosphate gluconyltransferase

     

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