糖尿病 (SGLT2I)、預防心血管事件<20201222>、預防腎病變(目前健保未給付)<20210910>

1. Type 2 diabetes mellitus
2. Chronic kidney disease: To reduce the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, and hospitalization for heart failure in adults with chronic kidney disease at risk of progression.<20210910>
3. Heart failure: Risk reduction of cardiovascular mortality, hospitalization for heart failure, and urgent heart failure visit in adults with heart failure.<20230907> #仿單變更2020 #仿單變更2021#仿單變更2023

Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitor

Absorption:
Bioavailability 78%
Distribution:
Protein binding: ~91%
Metabolism:
Primarily mediated by UGT1A9 to an inactive metabolite (dapagliflozin 3-O-glucuronide); CYP-mediated metabolism (minor)
Excretion:
Urine (75%; <2% as parent drug); feces (21%; ~15% as parent drug)
Pharmacodynamics:
1. Duration: Following discontinuation, urinary glucose excretion returns to baseline within ~3 days for the 10 mg dose
2. Half-life elimination: ~12.9 hours
3. Time to peak, plasma: 2 hours

1. History of serious hypersensitivity to dapagliflozin or any component of the formulation
2. Hemodialysis <20210910>

Due to adverse effects on renal development observed in animal studies, the manufacturer does not recommend use of dapagliflozin during the second and third trimesters of pregnancy

It is not known if dapagliflozin is present in breast milk.
Due to the potential for serious adverse reactions in the breastfeeding infant, breastfeeding is not recommended by the manufacturer.

1. Common: Dyslipidemia, hypovolemia, nausea, dysuria, increased urine output, urinary tract infection, increased hematocrit, genitourinary fungal infection, influenza, back pain, limb pain, nasopharyngitis
2. Postmarketing: ketoacidosis

Diabetes mellitus, type 2, treatment:
Initial 5 mg once daily; may increase to 10 mg once daily, taken in the morning, with or without food.

Heart failure with reduced ejection fraction, adjunctive:
10 mg once daily. May be used in persistently symptomatic patients who are already optimized on other therapies. <20201222>

Prevent chronic kidney disease:
10 mg once daily. May be used as a secondary agent in patients with persistently elevated urinary albumin excretion who are receiving other first-line therapies.<20210910>

eGFR >45 mL/minute/1.73 m²: No dosage adjustment necessary.<20201222>

eGFR 25-45 mL/minute/1.73 m²:
1. Hyperglycemia: Use is not recommended
2. Preventing cardiovascular events: Insufficient data
3. Heart failure: No dosage adjustment necessary <20201222>
4. CKD control: No dosage adjustment necessary <20210910>

eGFR <25 mL/minute/1.73 m²:
1. Hyperglycemia: Use is contraindicated
2. The manufacturer's labeling does not recommend initiation of therapy; however, patients previously established on dapagliflozin may continue for preventing eGFR reduction, ESKD, cardiovescular events, heart failure <20210910>

<20240501>

No dosage adjustment necessary; use caution if initiating in severe impairment (has not been studied)

儲存於 30度以下