#最小單位貼紙

抗病毒藥品 Treatment of HIV-1 infection in adults virologically suppressed on a stable antiretroviral regimen for ≥6 months with no history of treatment failure and no known resistance to the individual components

1. Dolutegravir: Antiretroviral, Integrase Inhibitor
inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration
2. Rilpivirine: Antiretroviral, Non-nucleoside Reverse Transcriptase Inhibitor
binds to reverse transcriptase and blocks the RNA-dependent and DNA-dependent polymerase activities, including HIV-1 replication

Dolutegravir:
Distribution:
1. Vd/F ~17.4 L
2. Protein binding: ≥98.9%
Metabolism:
Primarily metabolized via UGT1A1 with some contribution from CYP3A
Excretion:
Feces (53% as unchanged drug); urine (31% as metabolites, <1% as unchanged drug)
Pharmacodynamics:
1. Half-life elimination: ~14 hours
2. Time to peak: 2-3 hours

Rilpivirine:
Absorption:
Increased 40% with a meal (normal-to-high calorie)
Distribution:
Protein binding: 99.7% (primarily albumin)
Metabolism:
Hepatic, primarily by CYP3A4
Excretion:
Feces (85%, ~25% as unchanged drug); urine (~6%; <1% as unchanged drug)
Pharmacodynamics:
1. Half-life elimination: ~50 hours
2. Time to peak: 4-5 hours

1. Hypersensitivity to dolutegravir, rilpivirine, or any component of the formulation
2. Concurrent use with dofetilide, carbamazepine, systemic dexamethasone (>1 dose), oxcarbazepine, phenobarbital, phenytoin, proton pump inhibitors (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), rifampin, rifapentine, and/or St John's wort

1. Pregnant patients: Do not recommend use of the fixed-dose 2-drug combination who are (1) antiretroviral-naive (2) who have had antiretroviral therapy (ART) in the past but are restarting (3) who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen)
2. Become pregnant while treatment: the regimen should be changed or additional agents added (2-drug regimens are not recommended during pregnancy)

Dolutegravir: present in breast milk
Rilpivirine: not known if it is present in breast milk

Common:
Hyperglycemia, diarrhea, increased serum lipase, increased serum ALT or bilirubin, headache, decreased bone mineral density, increased CPK in blood specimen
Post-marketing:
Increased serum creatinine

One tablet once daily
Note: Prior to switching to Juluca, patients must be virologically suppressed on a stable antiretroviral regimen for ≥6 months with no history of treatment failure and no known resistance to dolutegravir or rilpivirine.

CrCl ≥30 mL/minute:
No dosage adjustment necessary
CrCl <30 mL/minute:
1. There are no dosage adjustments provided in the manufacturer's labeling; use with caution and increased monitoring for adverse effects.
2. Dolutegravir concentrations may be decreased, resulting in loss of therapeutic effect and development of resistance.
ESRD, hemodialysis:
There are no dosage adjustments provided (has not been studied)

1. Mild-to-moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.
2. Severe impairment (Child-Pugh class C): There are no dosage adjustments provided (has not been studied). According to the Tivicay product labeling, use of dolutegravir is not recommended.