Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection

The information in the brief version is excerpted directly from the full-text guidelines. The brief version is a compilation of the tables and boxed recommendations.

  •   Table of Contents

Download Guidelines

Integrase Inhibitors

Dolutegravir

Last Updated: May 22, 2018; Last Reviewed: May 22, 2018

Dolutegravir (DTG, Tivicay)
Dolutegravir (DTG, Tivicay)
For additional information see Drugs@FDA: https://www.accessdata.fda.gov/scripts/cder/daf/
Formulations
Tablets: 10 mg, 25 mg, and 50 mg

Fixed-Dose Combination Tablets:
  • [Triumeq] Abacavir 600 mg plus dolutegravir 50 mg plus lamivudine 300 mg
  • [Juluca] Dolutegravir 50 mg plus rilpivirine 25 mg
Dosing Recommendations Selected Adverse Events
Neonate and Infant Dose:
  • Not approved for use in neonates/infants
Pediatric Dose (Weighing <30 kg):
  • Not approved for children weighing <30 kg
  • Clinical trials in children with HIV weighing <30 kg are under way (see text).
Pediatric Dose (Weighing ≥30 kg to <40 kg)
Body Weight Dosea
(mg/day)
Dosing
Frequency
Tablet Size
(mg)
30 kg to <40 kg 35 Once daily One 10-mg tablet plus one 25-mg tablet
a These doses are for children who are treatment-naive or treatment-experienced (but integrase strand transfer inhibitor [INSTI]-naive) and who are not being treated with UGT1A1/CYP3A inducers.


Note: Dolutegravir 10-mg and 25-mg tablets may be available in retail pharmacies. If dolutegravir 10-mg or 25-mg tablets must be ordered, have the pharmacy contact their drug wholesaler and tell the drug wholesaler to order directly from the GlaxoSmithKline (GSK) distribution center. The GSK distribution center will ship the formulation directly to the pharmacy.


Child and Adolescent (Weighing ≥40 kg) and Adult Dose
Population Recommended Dose
Treatment-naive or treatment-experienced/INSTI-naive 50 mg once daily
Treatment-naive or treatment-experienced/INSTI-naive when co-administered with the following potent UGT1A/CYP3A inducers: efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin 50 mg twice daily
INSTI-experienced with any INSTI-associated resistance substitutions or clinically suspected INSTI resistancea 50 mg twice daily
a Combinations that do not include metabolic inducers should be considered where possible.


[Triumeq] Abacavir plus Dolutegravir plus Lamivudine
Pediatric (Weighing ≥40 kg) and Adult Dose:
  • 1 tablet once daily
  • For use in patients who are antiretroviral (ARV) treatment-naive or treatment-experienced (but INSTI-naive) and not being treated with UGT1A1/CYP3A inducers
  • See Abacavir section for special instructions about testing for abacavir hypersensitivity.
[Juluca] Dolutegravir plus Rilpivirine
Adult Dose:
  • 1 tablet once daily with a meal as a complete regimen to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable ARV regimen for ≥6 months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Juluca.
  • Not approved for children or adolescents. See Simplification of Treatment section below.
  • Insomnia
  • Headache
  • Neuropsychiatric symptoms (i.e., depression and/or suicidal thoughts or actions) especially in patients with a history of psychiatric illness
  • Hypersensitivity reactions, including rash, constitutional symptoms, and organ dysfunction (including liver injury) have been reported rarely.
Special Instructions
  • May be taken without regard to meals
  • 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-, 25-, 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 semi-solid food or liquid, all of which should be consumed immediately.1
  • The efficacy of 50-mg dolutegravir twice daily is reduced in patients with certain combinations of INSTI-resistance mutations (see Resistance section below).
  • When using fixed-dose combination (FDC) tablets, see other sections of the Drug Appendix for special instructions and additional information about the individual components of the FDC.
Metabolism/Elimination
  • UGT1A1 and cytochrome P450 (CYP) 3A substrate. Drugs that induce these enzymes and transporters may decrease plasma concentrations of dolutegravir.
Dolutegravir Dosing in Patients with Hepatic Impairment:
  • No dose adjustment is necessary in patients with mild or moderate hepatic impairment. Because of lack of data, dolutegravir is not recommended in patients with severe hepatic impairment.
  • Dolutegravir decreases tubular secretion of creatinine and slightly increases measured serum creatinine, but does not affect glomerular filtration.
Dolutegravir Dosing in Patients with Renal Impairment:
  • 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).

Download Guidelines