Therapeutic Classification: antiretrovirals
Pharmacologic Classification: integrase strand transfer inhibitors (INSTI)
Absorption: Bioavailability is unknown.
Distribution: Enters CSF.
Protein Binding: >98.9%.
Metabolism/Excretion: Metabolized primarily by the UGT1A1 enzyme system with some metabolism by the CYP3A4 isoenzyme. 53% excreted unchanged in feces. Metabolites are renally excreted; minimal renal elimination of unchanged drug. Poor UGT1A1 metabolizers have ↑ dolutegravir concentrations and an ↑ risk of adverse effects.
Half-Life: 14 hr
Tablets (Tivicay) and tablets for oral suspension (Tivicay PD) are not interchangeable.
- PO (Adults ): Treatment-naive or treatment-experienced INSTI-naive patients or virologically suppressed (HIV RNA <50 copies/mL) patients switching to dolutegravir plus rilpivirine: 50 mg once daily; Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin: 50 mg twice daily; INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance (consider other combinations that do not include metabolic inducers): 50 mg twice daily.
- PO (Children ≥20 kg): Treatment-naive or treatment-experienced INSTI-naive patients: Tivicay PD: 30 mg once daily; Tivicay tablets: 50 mg once daily Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin: Tivicay PD: 25 mg twice daily; Tivicay tablets: 50 mg twice daily.
- PO (Children 14<20 kg): Treatment-naive or treatment-experienced INSTI-naive patients: Tivicay PD (preferred): 25 mg once daily; Tivicay tablets: 40 mg once daily; Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranvir/ritonavir, carbamazepine, or rifampin: Tivicay PD (preferred): 25 mg twice daily; Tivicay tablets: 40 mg twice daily.
- PO (Children 10<14 kg): Treatment-naive or treatment-experienced INSTI-naive patients: Tivicay PD: 20 mg once daily; Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin: Tivicay PD: 20 mg twice daily.
- PO (Children ≥4 wk and 6<10 kg): Treatment-naive or treatment-experienced INSTI-naive patients: Tivicay PD: 15 mg once daily; Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin: Tivicay PD: 15 mg twice daily.
- PO (Children ≥4 wk and 3<6 kg): Treatment-naive or treatment-experienced INSTI-naive patients: Tivicay PD: 5 mg once daily; Treatment-naive or treatment-experienced INSTI-naive patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin: Tivicay PD: 5 mg twice daily.