藥劑部參考美國 Johns Hopkins 大學研究團隊所建立的 NxP (Nephrotoxic Potential) 專家共識分級清單，本品具「顯著以上腎毒性風險」，被認定具中度至高度腎損傷潛勢，特別是同時合併其他腎毒性藥物、脫水、高齡或既有腎功能異常的患者族群，應更加注意。

#最小單位貼紙

抗病毒藥品
1. Treatment of HIV-1 infection (as a complete regimen) in adults and pediatric patients ≥25 kg as initial therapy
2. To replace a stable antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) with no history of treatment failure and no known substitutions associated with resistance to the individual components

Bictegravi: Antiretroviral, Integrase Inhibitor
Inhibits HIV integrase by binding to the integrase-active site and blocking the strand transfer step of DNA integration
Emtricitabine: Antiretroviral, Nucleoside Reverse Transcriptase Inhibitor
Interfere with HIV viral RNA-dependent DNA polymerase activities resulting in inhibition of viral replication
Tenofovir: Antiretroviral, Nucleotide Reverse Transcriptase Inhibitor
Interfere with HIV viral RNA-dependent DNA polymerase activities resulting in inhibition of viral replication

Protein binding:
Bictegravir: >99%; Emtricitabine <4%; Tenofovir alafenamide ~80%
Metabolism:
1. Bictegravir: By CYP3A enzymes and hepatic glucuronidation mediated by UGT1A1
2. Emtricitabine: Not significantly metabolized
3. Tenofovir alafenamide: Converted intracellulary by hydrolysis (non-CYP enzymes) to tenofovir then phosphorylated by cellular kinases to the active moiety, tenofovir diphosphate; minimal extent by CYP3A
Half-life elimination:
Bictegravir: 17.3 hours; Emtricitabine: 10.4 hours; Tenofovir alafenamide: 0.51 hours (active metabolite, tenofovir diphosphate: 150 to 180 hours)
Time to peak:
Bictegravir: 2 to 4 hours; Emtricitabine: 1.5 to 2 hours; Tenofovir alafenamide: 0.5 to 2 hours
Excretion:
1. Bictegravir: Feces (60.3%), urine (35%)
2. Emtricitabine: Feces (13.7%), urine (70%)
3. Tenofovir alafenamide: Feces (31.7%), urine (<1%)

Coadministration with dofetilide, rifampin

Data are insufficient to recommend this combination for pregnant females living with HIV

Emtricitabine is present in breast milk; excretion of bictegravir and tenofovir alafenamide are unknown.

1. Hepatic: Increased serum bilirubin, AST, ALT
2. Cardiovascular: Increased serum creatine kinase
3. Central nervous system: Headache, abnormal dreams, fatigue, dizziness, insomnia, depression
4. Dermatologic: Skin rash
5. Endocrine & metabolic: Increased LDL cholesterol
6. Gastrointestinal: Diarrhea, nausea, increased serum amylase, abdominal pain, flatulence, vomit
7. Hematologic & oncologic: Decreased neutrophils
8. Postmarketing: Angioedema, suicidal ideation, urticaria

One tablet once daily

Pediatric patients weighing ≥25 kg (In clinical trials, the youngest patients were 6 years of age): One tablet once daily

Additional Pediatric Considerations:
1. Emtricitabine-associated hyperpigmentation may occur at a higher frequency in pediatric patients compared to adults.
2. Bictegravir may increase SCr via inhibition of tubular secretion; it does not affect glomerular filtration.

1. CrCl <30 mL/minute: Not recommended
2. CrCl ≥30 mL/minute: No dosage adjustment necessary

1. Mild to moderate impairment (Child-Pugh class C): Not recommended (has not been studied)
2. Severe impairment (Child-Pugh class A, B): No dosage adjustments necessary