Updated
Reviewed
Dec. 18, 2019
Appendix B: Drug Characteristics Tables
Characteristics of Integrase 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:
|
CYP3A4 substrate UGT1A1-mediated glucuronidation |
~17 hours | Diarrhea Nausea Headache Weight gain |
Dolutegravir (DTG) Tivicay |
Tivicay:
|
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
|
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:
|
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:
|
Isentress In ARV-Naive Patients or ARV-Experienced Patients:
In ARV-Naive or ARV-Experienced Patients with Virologic Suppression on a Regimen containing RAL 400 mg Twice Daily:
|
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
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:
|
CYP3A4 substrate UGT1A1-mediated glucuronidation |
~17 hours | Diarrhea Nausea Headache Weight gain |
Dolutegravir (DTG) Tivicay |
Tivicay:
|
In ARV-Naive or ARV-Experienced, INSTI-Naive Patients:
|
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:
|
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:
|
Isentress In ARV-Naive Patients or ARV-Experienced Patients:
In ARV-Naive or ARV-Experienced Patients with Virologic Suppression on a Regimen containing RAL 400 mg Twice Daily:
|
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 |
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