Peringatan Keamanan

Age, gender, race, and body weight do not affect dapagliflozin dosing requirementsLabel,A6758. Although age does not affect dosing requirements, safety has not been established in pediatric populations and patients at an especially advanced age may be more susceptible to adverse effectsLabel. Animal studies in pregnancy showed no fetal toxicity in the first trimester but exposure later in pregnancy was associated with renal pelvic dilatation and maternal toxicity at much higher doses than the maximum recommended human doseLabel. Due to this data, dapagliflozin is not recommended in the second and third trimester of pregnancyLabel. Dapagliflozin is excreted in milk from rats, though this may not necessarily be the case in humansLabel. Children under 2 years old who are exposed to dapagliflozin may be at risk of improper kidney developmentLabel. Dapagliflozin is not recommended in patients with a creatinine clearance below 45mL/min and is contraindicated in patients with creatinine clearance below 30mL/minLabel. Dose adjustments are not necessary in patients with hepatic impairment at any stage, although the risk and benefit to the patient must be assessed as there is limited data on dapagliflozin use in this populationLabel.

Dapagliflozin

DB06292

small molecule approved

Deskripsi

Dapagliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor, and it was the first SLGT2 inhibitor to be approved. indicated for managing diabetes mellitus type 2.A261596 When combined with diet and exercise in adults, dapagliflozin helps to improve glycemic control by inhibiting glucose reabsorption in the proximal tubule of the nephron and causing glycosuria.A6757 Dapagliflozin has been investigated either as monotherapy or as an adjunct treatment with insulin or other oral hypoglycemic agents.A261601

Dapagliflozin was originally approved by the FDA on Jan 08, 2014, to improve glycemic control in adults with type 2 diabetes in conjunction with diet and exercise.L48251 It was later approved to reduce the risk of kidney function decline, kidney failure, cardiovascular death, and hospitalization for heart failure in adults with chronic kidney disease in April 2021.L48251

Struktur Molekul 2D

Berat 408.873
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma terminal half-life (t<sub>1/2</sub>) for dapagliflozin is approximately 12.9 hours following a single oral dose of 10 mg.[L48246] In healthy subjects given a single oral dose of 50 mg of dapagliflozin, the mean terminal half-life was 13.8 hours.[A6757]
Volume Distribusi The volume of distribution was estimated to be 118L.[A6758]
Klirens (Clearance) Oral plasma clearance was 4.9 mL/min/kg, and renal clearance was 5.6 mL/min.[A6757]

Absorpsi

Oral dapagliflozin reaches a maximum concentration within 1 hour of administration when patients have been fasting.A6757 Following oral administration of dapagliflozin, the maximum plasma concentration (Cmax) is usually attained within 2 hours under fasting state. The Cmax and AUC values increase dose proportionally with an increase in dapagliflozin dose in the therapeutic dose range. The absolute oral bioavailability of dapagliflozin following the administration of a 10 mg dose is 78%. Administration of dapagliflozin with a high-fat meal decreases its Cmax by up to 50% and prolongs Tmax by approximately 1 hour but does not alter AUC as compared with the fasted state. These changes are not considered to be clinically meaningful and dapagliflozin can be administered with or without food.L48246

Metabolisme

Dapagliflozin is primarily glucuronidated to become the inactive 3-O-glucuronide metabolite(60.7%).A6757,A6758 Dapagliflozin also produces another minor glucuronidated metabolite(5.4%), a de-ethylated metabolite(<5%), and a hydroxylated metabolite(<5%)A6757. Metabolism of dapagliflozin is mediated by cytochrome p-450(CYP)1A1, CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP3A4, uridine diphosphate glucuronyltransferase(UGT)1A9, UGT2B4, and UGT2B7A6758. Glucuronidation to the major metabolite is mediated by UGT1A9.A6758

Rute Eliminasi

Dapagliflozin and related metabolites are primarily eliminated via the renal pathway. Following a single 50 mg dose of 14C-dapagliflozin, 75% and 21% of total radioactivity is excreted in urine and feces, respectively. In urine, less than 2% of the dose is excreted as the parent drug. In feces, approximately 15% of the dose is excreted as the parent drug.L48246

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Binge drinking or drinking alcohol often may predispose patients to ketoacidosis.
  • 2. Take with or without food.

Interaksi Obat

801 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Dapagliflozin.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Dapagliflozin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Dapagliflozin is combined with Levodopa.
Risperidone Dapagliflozin may increase the hypotensive activities of Risperidone.
Deferasirox The metabolism of Dapagliflozin can be decreased when combined with Deferasirox.
Trandolaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Trandolaprilat.
Moexiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Moexiprilat.
Ramipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Ramipril.
Fosinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Fosinopril.
Trandolapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Trandolapril.
Moexipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Moexipril.
Lisinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Lisinopril.
Perindopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Perindopril.
Quinapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Quinapril.
Omapatrilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Omapatrilat.
Rescinnamine The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Rescinnamine.
Spirapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Spirapril.
Temocapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Temocapril.
Enalaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Enalaprilat.
Imidapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Imidapril.
Zofenopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Zofenopril.
Delapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Delapril.
Benazeprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Benazeprilat.
Fosinoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Fosinoprilat.
Ramiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Ramiprilat.
Perindoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Perindoprilat.
Quinaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Quinaprilat.
Enalapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Enalapril.
Captopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Captopril.
Cilazapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Cilazapril.
Cilazaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Dapagliflozin is combined with Cilazaprilat.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Dapagliflozin.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Dapagliflozin.
Nicorandil Nicorandil may increase the hypotensive activities of Dapagliflozin.
Moxifloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Grepafloxacin.
Pefloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Pefloxacin.
Trovafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Fleroxacin.
Garenoxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Epitizide.
Cyproterone acetate The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Cyproterone acetate.
Amineptine Amineptine may decrease the hypoglycemic activities of Dapagliflozin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Dapagliflozin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Dapagliflozin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Dapagliflozin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Dapagliflozin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Dapagliflozin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Dapagliflozin.
Melitracen Melitracen may decrease the hypoglycemic activities of Dapagliflozin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Dapagliflozin.
Iprindole Iprindole may decrease the hypoglycemic activities of Dapagliflozin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Dapagliflozin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Dapagliflozin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Dapagliflozin.
Opipramol Opipramol may decrease the hypoglycemic activities of Dapagliflozin.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Dapagliflozin.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Dapagliflozin.
Procaine Procaine may increase the orthostatic hypotensive activities of Dapagliflozin.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Dapagliflozin.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Dapagliflozin.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Dapagliflozin.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Dapagliflozin.

Target Protein

Sodium/glucose cotransporter 2 SLC5A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19996149
    Obermeier M, Yao M, Khanna A, Koplowitz B, Zhu M, Li W, Komoroski B, Kasichayanula S, Discenza L, Washburn W, Meng W, Ellsworth BA, Whaley JM, Humphreys WG: In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010 Mar;38(3):405-14. doi: 10.1124/dmd.109.029165. Epub 2009 Dec 8.
  • PMID: 24105299
    Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW: Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3.
  • PMID: 31773634
    Paik J, Blair HA: Correction to: Dapagliflozin: A Review in Type 1 Diabetes. Drugs. 2019 Dec;79(18):2011. doi: 10.1007/s40265-019-01238-2.
  • PMID: 25436106
    Anderson SL: Dapagliflozin efficacy and safety: a perspective review. Ther Adv Drug Saf. 2014 Dec;5(6):242-54. doi: 10.1177/2042098614551938.

Contoh Produk & Brand

Produk: 139 • International brands: 0
Produk
  • Accel-dapagliflozin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Accel-dapagliflozin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-dapagliflozin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ag-dapagliflozin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-dapagliflozin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-dapagliflozin
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-dapagliflozin-metformin
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-dapagliflozin-metformin
    Tablet • - • Oral • Canada • Generic • Approved
Menampilkan 8 dari 139 produk.

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