抗病毒藥品 Treatment of HIV-1 infection in adult and pediatric patients weighing ≥40 kg
藥理
Dolutegravir: Integrase Inhibitor (Anti-HIV)
Bind to the integrase active site and block the strand transfer step of retroviral DNA integration. Abacavir: Nucleosid Reverse Transcriptase Inhibitor (Anti-HIV)
Abacavir --converted->Carbovir triphosphate (CBV-TP, active metabolite, an analogue of dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase both by competing with the natural substrate dGTP and by its incorporation into viral DNA. Lamivudine: Nucleosid Reverse Transcriptase Inhibitor (Anti-HIV)
Lamivudine --phosphorylated-> Lamivudine triphosphate (3TC-TP, active 5′-triphosphate metabolite). The principal mode of action of 3TC-TP is inhibition of reverse transcriptase via DNA chain termination after incorporation of the nucleotide analogue.
藥動學
Show no difference in values when compared to dolutegravir as a single agent given with abacavir and lamivudine as a combination product.
禁忌症
1. Hypersensitivity to abacavir, dolutegravir, lamivudine, or any component of the formulation
2. Patients with HLA-B*5701 allele
3. Concomitant dofetilide
4. Moderate or severe hepatic impairment
5. Known or clinically suspected integrase strand transfer inhibitor resistance because the dose of dolutegravir is insufficient in these subpopulations.
懷孕分類
1. Pregnant female: An alternative regimen for whom are antiretroviral-naive, have had antiretroviral therapy (ART) in the past but are restarting, or require a new ART regimen
2. Become pregnant while taking: may continue if viral suppression is effective and the regimen is well tolerated
哺乳分類
Abacavir, dolutegravir, and lamivudine are present in breast milk
Dosage:
One tablet once daily Administration:
1. If patient is on concomitant therapy with efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, or rifampin, an additional daily single-component dolutegravir tablet should be administered 12 hours after Triumeq.
2. Administer 2 hours before or 6 hours after cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications.
3. Alternatively, may be administered with supplements containing calcium or iron at the same time if administered together with food.
小兒調整劑量
1. Weighing <40 kg: Not recommended; product is a fixed-dose combination
2. Weighing ≥40 kg: One tablet once daily
腎功能調整劑量
1. CrCl <50 mL/minute: Not recommended
2. CrCl ≥50 mL/minute: No dosage adjustment necessary
肝功能調整劑量
1. Child-Pugh class B, C: Contraindicated
2. Child-Pugh class A: Not recommended