Last Updated: April 16, 2019; Last Reviewed: April 16, 2019
Dolutegravir (DTG, Tivicay)
|Dolutegravir (DTG, Tivicay)
For additional information see Drugs@FDA: https://www.accessdata.fda.gov/scripts/cder/daf/
|Tablets: 10 mg, 25 mg, and 50 mg
Fixed-Dose Combination Tablets:
- [Juluca] Dolutegravir 50 mg/rilpivirine 25 mg
- [Triumeq] Abacavir 600 mg/dolutegravir 50 mg/lamivudine 300 mg
||Selected Adverse Events
|Neonate and Infant Dose:
Child and Adolescent Dose:
- Dolutegravir is not approved for use in neonates/infants.
Child and Adolescent (Weighing ≥40 kg) and Adult Dose
- No dosing recommendations can be made for children weighing <25 kg.
- The Panel on Antiretroviral Therapy and Medical Management of Children Living with HIV (the Panel) recommends an investigational dose of dolutegravir 50 mg once daily for children and adolescents weighing ≥25 kg who are antiretroviral (ARV)-naive or ARV-experienced (but integrase strand transfer inhibitor [INSTI]-naive) and who are not being treated with uridine diphosphate glucuronyl transferase (UGT) 1A1 or cytochrome P450 3A (CYP3A) inducers.
- The Panel’s recommended dose is based on interim data from ongoing trials that indicate that using the FDA-approved dose of dolutegravir 35 mg in patients weighing ≥30 kg to 40 kg may result in suboptimal trough concentrations (see text). Using a 50-mg dose also avoids the need to administer two tablets with different strengths (i.e., a 10-mg tablet plus a 25-mg tablet). Dolutegravir is not approved by the Food and Drug Administration (FDA) for use in children weighing <30 kg.
|ARV-naive or ARV-experienced/INSTI-naive patients
||Dolutegravir 50 mg once daily
|ARV-naive or ARV-experienced/INSTI-naive patients who are also receiving one of the following potent UGT1A/CYP3A inducers: efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin
||Dolutegravir 50 mg twice daily
|INSTI-experienced patients with any INSTI-associated resistance substitutions or clinically suspected INSTI resistancea
||Dolutegravir 50 mg twice daily
- One tablet once daily with a meal as a complete regimen to replace the current ARV regimen in patients who have been virologically suppressed (HIV RNA <50 copies/mL) on a stable ARV regimen for at least 6 months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Juluca.
- Juluca is not approved for use in children or adolescents. See the Simplification of Treatment section below.
Child and Adolescent (Weighing ≥25 kg) and Adult Dose:
- One tablet once daily
- For use in patients who are ARV-naive or ARV-experienced (but INSTI-naive) and who are not being treated with UGT1A1 or CYP3A inducers
- See the abacavir section for special instructions about testing for abacavir hypersensitivity.
- The FDA-approved dose for pediatric patients weighing >40 kg is one tablet once daily.
- Neuropsychiatric symptoms (i.e., depression and/or suicidal thoughts or actions), especially in patients with a history of psychiatric illness
- Rare cases of hypersensitivity reactions, including rash and drug reaction (or rash) with eosinophilia and systemic symptoms, constitutional symptoms, and organ dysfunction (including liver injury) have been reported.
- Dolutegravir may be taken without regard to meals.
- Dolutegravir should be taken 2 hours before or 6 hours after taking cation-containing antacids or laxatives, sucralfate, oral iron supplements, oral calcium supplements, or buffered medications.
- In patients who have difficulty swallowing tablets whole, 10-mg, 25-mg, and 50-mg tablets may be either split into halves followed by immediate ingestion of both halves of the tablet, or crushed and added to a small amount of semisolid food or liquid, all of which should be consumed immediately.1
- The efficacy of dolutegravir 50 mg twice daily is reduced in patients with certain combinations of INSTI-resistance mutations (see the Resistance section below).
- When using fixed-dose combination (FDC) tablets that contain dolutegravir, see other sections of the Drug Appendix for special instructions and additional information about the individual components of the FDC.
Dolutegravir Dosing in Patients with Hepatic Impairment:
- UGT1A1 and CYP3A substrate. Drugs that induce these enzymes and transporters may decrease plasma concentrations of dolutegravir.
Dolutegravir Dosing in Patients with Renal Impairment:
- No dose adjustment is necessary in patients with mild or moderate hepatic impairment. Due to a lack of data, dolutegravir is not recommended for use in patients with severe hepatic impairment.
- Dolutegravir decreases tubular secretion of creatinine and increases measured serum creatinine, without affecting glomerular filtration.
- No dose adjustment is required in INSTI-naive patients with mild, moderate, or severe renal impairment, or in INSTI-experienced patients with mild or moderate renal impairment.
- Use dolutegravir with caution in INSTI-experienced patients with severe renal impairment (creatinine clearance <30 mL/min), because dolutegravir concentrations will be decreased. The cause of this decrease is unknown.