糖尿病 (SGLT2I / Metformin) Type 2 diabetes mellitus

Antidiabetic

Absorption: 1. Tmax: Dapagliflozin 0.9-1.03 hours; Metformin 3.52-3.66 hours
2. Bioavailability: Dapagliflozin 78%
3. Effects of food: Not clinically relevant
Distribution: 1. Protein Binding: Dapagliflozin 91%; Metformin negligible
2. Vd: Metformin 654 L
Metabolism:
1. Dapagliflozin, Hepatic: extensive via UGT1A9 (into Dapagliflozin, 3-O-glucuronide [inactive, major]), Weak P-glycoprotein substrate and OAT3 substrate
2. Metformin: no metabolites identified in humans
Excretion:
1. Dapagliflozin: Fecal 21%, Renal 75%
2. Metformin: Renal 90% within 24 hours
Elimination Half Life: 1. Dapagliflozin: 8 to 12.9 hours
2. Metformin: 6.2 to 16.2 hours (plasma), 17.6 hours (blood)

1. Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma
2. Dialysis; End stage renal disease
3. Serious hypersensitivity to dapagliflozin or metformin hydrochloride
4. Moderate or severe renal impairment (eGFR below 60 mL/min/1.73 m²)

C

Infant risk cannot be ruled out

Serious:
Hypotension(Dapagliflozin can cause a decrease in blood volume, which can sometimes lead to symptomatic hypotension) <20240419>, Urticaria, Diabetic ketoacidosis, Lactic acidosis, Raised low density lipoprotein cholesterol, Hypersensitivity reaction, Bladder cancer, Injury of kidney, Pyelonephritis, Renal impairment, Sepsis due to urinary tract infection, Necrotizing fasciitis, Perineum, Angioedema
Common:
Serum vitamin B12 low, Diarrhea, Headache, Urinary tract infectious disease, Genital infection, Mycotic, Nasopharyngitis

Initial:
Individualize based on current regimen; administer orally once daily in morning with food
Adjustment:
Titrate gradually as needed; MAX dose, dapagliflozin 10 mg/metformin 2000 mg per day

Safety and efficacy not established in patients younger than 18 years

1. eGFR 45 mL/minute/1.73 m2: No dosage adjustment necessary
2. eGFR 30-45 mL/minute/1.73 m2: The manufacturer does not recommend use. However, both dapagliflozin and metformin may be considered for use in select patients with eGFR 30 mL/minute/1.73 m2; refer to individual agents.
3. eGFR <30 mL/minute/1.73 m2, Hemodialysis: Use is contraindicated.

Hepatic impairment: Avoid use

store under 30 degree C