Appendix B: Drug Characteristics Tables

Characteristics of Integrase Inhibitors

Appendix B, Table 6. Characteristics of Integrase Strand Transfer Inhibitors
Generic Name
(Abbreviation)
Trade Name
Formulations Dosing Recommendationsa Elimination/
Metabolic Pathways
Serum Half-Life Adverse Eventsb
Bictegravir
(BIC)
BIC is only available as a component of the STR Biktarvy (BIC/TAF/FTC).c Biktarvy:
  • One tablet PO once daily
CYP3A4 substrate

UGT1A1-mediated glucuronidation
~17 hours Diarrhea

Nausea

Headache

Weight gain
Dolutegravir
(DTG)
Tivicay
Tivicay:
  • 50 mg tablet
STRs that Contain DTG:c
  • Dovato (DTG/3TC)
  • Juluca (DTG/RPV)
  • Triumeq (DTG/ABC/3TC)
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
  • DTG 50 mg PO once daily
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin:
  • DTG 50 mg PO twice daily
INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance:
  • DTG 50 mg PO twice daily
See Appendix B, Table 1 for dosing information for STRs that contain DTG.
UGT1A1-mediated glucuronidation

Minor substrate of CYP3A4
~14 hours Insomnia

Headache

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)

Weight gain

Hepatotoxicity

There is a potential increased risk of NTDs in infants born to individuals who received DTG around the time of conception (see Table 6b for more information).

HSRs, including rash, constitutional symptoms, and organ dysfunction (including liver injury), have been reported.
Elvitegravir
(EVG)
             
EVG is only available as a component of an STR tablet that also contains COBI, FTC, and either TDF or TAF.

STRs that Contain EVG:c
  • Genvoya (EVG/c/TAF/FTC)
  • Stribild (EVG/c/TDF/FTC)
Genvoya:
  • One tablet PO once daily with food
  • See Appendix B, Table 10 for recommendations on dosing in persons with renal insufficiency.
Stribild:
  • One tablet PO once daily with food
  • Not recommended for patients with baseline CrCl <70 mL/min (see Appendix B, Table 10 for the CrCl calculation equation).
EVG:
  • CYP3A and UGT1A1/3 substrate
COBI:
  • CYP3A inhibitor and substrate
  • CYP2D6 inhibitor
EVG/c: ~13 hours Nausea

Diarrhea

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)
Raltegravir
(RAL)
Isentress
Isentress HD
Isentress:
  • 400 mg tablet
  • 25 and 100 mg chewable tablets
  • 100 mg single-use packet for oral suspension
Isentress HD:
  • 600 mg tablet
Isentress
In ARV-Naive Patients or ARV-Experienced Patients:
  • 400 mg PO twice daily
With Rifampin:
  • 800 mg twice daily
Isentress HD
In ARV-Naive or ARV-Experienced Patients with Virologic Suppression on a Regimen containing RAL 400 mg Twice Daily:
  • 1,200 mg (two 600-mg tablets) PO once daily
With Rifampin:
  • Not recommended
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

Weight gain

Insomnia

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)
a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 10. When no food restriction is listed, the ARV drug can be taken with or without food.

b Also see Table 17.

c See Appendix B, Table 1 for information about these formulations.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; INSTI = integrase strand transfer inhibitor; NTD = neural tube defect; PO = orally; RAL = raltegravir; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TPV/r = tipranavir/ritonavir; UGT = uridine diphosphate glucuronyl transferase

Appendix B: Drug Characteristics Tables

Characteristics of Integrase Inhibitors

Appendix B, Table 6. Characteristics of Integrase Strand Transfer Inhibitors
Generic Name
(Abbreviation)
Trade Name
Formulations Dosing Recommendationsa Elimination/
Metabolic Pathways
Serum Half-Life Adverse Eventsb
Bictegravir
(BIC)
BIC is only available as a component of the STR Biktarvy (BIC/TAF/FTC).c Biktarvy:
  • One tablet PO once daily
CYP3A4 substrate

UGT1A1-mediated glucuronidation
~17 hours Diarrhea

Nausea

Headache

Weight gain
Dolutegravir
(DTG)
Tivicay
Tivicay:
  • 50 mg tablet
STRs that Contain DTG:c
  • Dovato (DTG/3TC)
  • Juluca (DTG/RPV)
  • Triumeq (DTG/ABC/3TC)
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
  • DTG 50 mg PO once daily
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients when Coadministered with EFV, FPV/r, TPV/r, or Rifampin:
  • DTG 50 mg PO twice daily
INSTI-Experienced Patients with Certain INSTI Mutations (See Product Label) or with Clinically Suspected INSTI Resistance:
  • DTG 50 mg PO twice daily
See Appendix B, Table 1 for dosing information for STRs that contain DTG.
UGT1A1-mediated glucuronidation

Minor substrate of CYP3A4
~14 hours Insomnia

Headache

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)

Weight gain

Hepatotoxicity

There is a potential increased risk of NTDs in infants born to individuals who received DTG around the time of conception (see Table 6b for more information).

HSRs, including rash, constitutional symptoms, and organ dysfunction (including liver injury), have been reported.
Elvitegravir
(EVG)
             
EVG is only available as a component of an STR tablet that also contains COBI, FTC, and either TDF or TAF.

STRs that Contain EVG:c
  • Genvoya (EVG/c/TAF/FTC)
  • Stribild (EVG/c/TDF/FTC)
Genvoya:
  • One tablet PO once daily with food
  • See Appendix B, Table 10 for recommendations on dosing in persons with renal insufficiency.
Stribild:
  • One tablet PO once daily with food
  • Not recommended for patients with baseline CrCl <70 mL/min (see Appendix B, Table 10 for the CrCl calculation equation).
EVG:
  • CYP3A and UGT1A1/3 substrate
COBI:
  • CYP3A inhibitor and substrate
  • CYP2D6 inhibitor
EVG/c: ~13 hours Nausea

Diarrhea

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)
Raltegravir
(RAL)
Isentress
Isentress HD
Isentress:
  • 400 mg tablet
  • 25 and 100 mg chewable tablets
  • 100 mg single-use packet for oral suspension
Isentress HD:
  • 600 mg tablet
Isentress
In ARV-Naive Patients or ARV-Experienced Patients:
  • 400 mg PO twice daily
With Rifampin:
  • 800 mg twice daily
Isentress HD
In ARV-Naive or ARV-Experienced Patients with Virologic Suppression on a Regimen containing RAL 400 mg Twice Daily:
  • 1,200 mg (two 600-mg tablets) PO once daily
With Rifampin:
  • Not recommended
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

Weight gain

Insomnia

Depression and suicidal ideation (rare; usually occurs in patients with pre-existing psychiatric conditions)
a For dose adjustments in patients with hepatic insufficiency, see Appendix B, Table 10. When no food restriction is listed, the ARV drug can be taken with or without food.

b Also see Table 17.

c See Appendix B, Table 1 for information about these formulations.

Key: 3TC = lamivudine; ABC = abacavir; ARV = antiretroviral; BIC = bictegravir; COBI = cobicistat; CPK = creatine phosphokinase; CrCl = creatinine clearance; CYP = cytochrome P; DTG = dolutegravir; EFV = efavirenz; EVG = elvitegravir; EVG/c = elvitegravir/cobicistat; FDC = fixed-dose combination; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; HSR = hypersensitivity reaction; INSTI = integrase strand transfer inhibitor; NTD = neural tube defect; PO = orally; RAL = raltegravir; RPV = rilpivirine; STR = single-tablet regimen; TAF = tenofovir alafenamide; TDF = tenofovir disoproxil fumarate; TPV/r = tipranavir/ritonavir; UGT = uridine diphosphate glucuronyl transferase
Updated
Reviewed
Dec. 18, 2019

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