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Biktarvy 50 mg/200 mg/25 mg film-coated tablets(六)
2019-02-25 14:14:55 来源: 作者: 【 】 浏览:10199次 评论:0
ons.
Co-administration is not recommended.
Oxcarbazepine
Phenobarbital
Phenytoin
(Induction of CYP3A, UGT1A1, and P-gp)
Interaction not studied with any of the components of Biktarvy.
Co-administration of oxcarbazepine, phenobarbital, or phenytoin may decrease bictegravir and tenofovir alafenamide plasma concentrations.
Co-administration is not recommended.
ANTACIDS, SUPPLEMENTS AND BUFFERED MEDICINES
Magnesium/aluminium-containing antacid suspension (20 mL single dose5), Bictegravir
(Chelation with polyvalent cations)
Bictegravir (antacid suspension 2 hours prior, fasted):
AUC: ↓ 52%
Cmax: ↓ 58%
Bictegravir (antacid suspension after 2 hours, fasted):
AUC: ↔
Cmax: ↔
Bictegravir (simultaneous administration, fasted):
AUC: ↓ 79%
Cmax: ↓ 80%
Bictegravir (simultaneous administration with food):
AUC: ↓ 47%
Cmax: ↓ 49%
Biktarvy should not be taken simultaneously with supplements containing magnesium and/or aluminium due to the expected substantial decrease of bictegravir exposure (see section 4.4).
Biktarvy should be administered at least 2 hours before, or with food 2 hours after antacids containing magnesium and/or aluminium.
Ferrous fumarate (324 mg single dose), Bictegravir
(Chelation with polyvalent cations)
Bictegravir (simultaneous administration, fasted):
AUC: ↓ 63%
Cmax: ↓ 71%
Bictegravir (simultaneous administration with food):
AUC: ↔
Cmax: ↓ 25%
Biktarvy should be administered at least 2 hours before iron supplements, or taken together with food.
Calcium carbonate (1200 mg single dose), Bictegravir
(Chelation with polyvalent cations)
Bictegravir (simultaneous administration, fasted):
AUC: ↓ 33%
Cmax: ↓ 42%
Bictegravir (simultaneous administration with food):
AUC:
Cmax:
Biktarvy and calcium-containing supplements can be taken together, without regard to food.
Sucralfate
(Chelation with polyvalent cations)
Interaction not studied with any of the components of Biktarvy.
Co-administration may decrease bictegravir plasma concentrations.
Co-administration not recommended.
ANTIDEPRESSANTS
Sertraline (50 mg single dose), Tenofovir alafenamide6
Tenofovir alafenamide:
AUC:
Cmax:
Sertraline:
AUC:
Cmax:
No interaction is expected with bictegravir and emtricitabine
No dose adjustment is required upon co-administration.
IMMUNOSUPPRESSANTS
Ciclosporin (IV or oral use)
(P-gp inhibition)
Interaction not studied with any of the components of Biktarvy.
Co-administration of ciclosporin (IV or oral use) is expected to increase plasma concentrations of both bictegravir and tenofovir alafenamide.
Co-administration of ciclosporin (IV or oral use) is not recommended. If the combination is needed, clinical and biological monitoring, notably renal function, is recommended.
OPIOIDS
Methadone
Not studied.
(Inhibition of CYP1A2, 2B6, 2D6 by a bictegravir metabolite cannot be excluded).
Caution is recommended.
ORAL ANTI-DIABETICS
Metformin (500 mg twice daily), Bictegravir/Emtricitabine/ Tenofovir alafenamide
(Inhibition of OCT2/MATE1)
Metformin:
AUC: ↑ 39%
Cmin: ↑ 36%
Cmax:
No dose adjustment is required upon co-administration in patients with normal renal function.
In patients with moderate renal impairment, close monitoring should be consider
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