Peringatan Keamanan

Experience with empagliflozin overdose is limited - employ standard symptomatic and supportive measures, as well as gastric decontamination when appropriate. The use of hemodialysis in empagliflozin overdose has not been studied but is unlikely to be of benefit given the drug's relatively high protein-binding.L13688

Empagliflozin

DB09038

small molecule approved

Deskripsi

Empagliflozin is an inhibitor of sodium-glucose co-transporter-2 (SGLT2), the transporters primarily responsible for the reabsorption of glucose in the kidney.A203453 It is used clinically as an adjunct to diet and exercise, often in combination with other drug therapies,L13673,L13679,L11479 for the management of type 2 diabetes mellitus.L13688

The first known inhibitor of SGLTs, phlorizin, was isolated from the bark of apple trees in 1835 and researched extensively into the 20th century, but was ultimately deemed inappropriate for clinical use given its lack of specificity and significant gastrointestinal side effects.A203501 Attempts at overcoming these limitations first saw the development of O-glucoside analogs of phlorizin (e.g. remogliflozin etabonate), but these molecules proved relatively pharmacokinetically unstable. The development of C-glucoside phlorizin analogs remedied the issues observed in the previous generation, and led to the FDA approval of canagliflozin in 2013 and both dapagliflozin and empagliflozin in 2014.A203501 As the most recently approved of the "flozin" drugs, empagliflozin carries the highest selectivity for SGLT2 over SGLT1 (approximately 2700-fold). Empagliflozin was further approved by the EMA in March 2022 and Health Canada in April 2022, making it the first and only approved treatment in Europe and Canada for adults with symptomatic chronic heart failure regardless of ejection fraction.L40783,L13916

Struktur Molekul 2D

Berat 450.91
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The apparent terminal elimination half-life was found to be 12.4 h based on population pharmacokinetic analysis.[L13688]
Volume Distribusi The estimated apparent steady-state volume of distribution is 73.8 L.[L13688]
Klirens (Clearance) Apparent oral clearance was found to be 10.6 L/h based on a population pharmacokinetic analysis.[L13688]

Absorpsi

Following oral administration, peak plasma concentrations are reached in approximately 1.5 hours (Tmax). At steady-state, plasma AUC and Cmax were 1870 nmol·h/L and 259 nmol/L, respectively, following therapy with empagliflozin 10mg daily and 4740 nmol·h/L and 687 nmol/L, respectively, following therapy with empagliflozin 25mg daily.L13688 Administration with food does not significantly affect the absorption of empagliflozin.

Metabolisme

Empagliflozin undergoes minimal metabolism. It is primarily metabolized via glucuronidation by 5'-diphospho-glucuronosyltransferases 2B7, 1A3, 1A8, and 1A9 to yield three glucuronide metabolites: 2-O-, 3-O-, and 6-O-glucuronide.L13688 No metabolite represented more than 10% of total drug-related material.

Rute Eliminasi

After oral administration of radiolabeled empagliflozin approximately 41.2% of the administered dose was found eliminated in feces and 54.4% eliminated in urine. The majority of radioactivity in the feces was due to unchanged parent drug while approximately half of the radioactivity in urine was due to unchanged parent drug.L13688

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

805 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Empagliflozin.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Empagliflozin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Empagliflozin is combined with Levodopa.
Risperidone Empagliflozin may increase the hypotensive activities of Risperidone.
Ramipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Ramipril.
Fosinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Fosinopril.
Trandolapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Trandolapril.
Enalapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Enalapril.
Moexipril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Moexipril.
Lisinopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Lisinopril.
Perindopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Perindopril.
Quinapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Quinapril.
Omapatrilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Omapatrilat.
Rescinnamine The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Rescinnamine.
Captopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Captopril.
Cilazapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Cilazapril.
Spirapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Spirapril.
Temocapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Temocapril.
Enalaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Enalaprilat.
Imidapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Imidapril.
Zofenopril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Zofenopril.
Delapril The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Delapril.
Benazeprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Benazeprilat.
Fosinoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Fosinoprilat.
Ramiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Ramiprilat.
Perindoprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Perindoprilat.
Quinaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Quinaprilat.
Trandolaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Trandolaprilat.
Moexiprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Moexiprilat.
Cilazaprilat The risk or severity of renal failure, hypotension, and hyperkalemia can be increased when Empagliflozin is combined with Cilazaprilat.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Empagliflozin.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Empagliflozin.
Nicorandil Nicorandil may increase the hypotensive activities of Empagliflozin.
Moxifloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Empagliflozin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Empagliflozin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Empagliflozin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Empagliflozin can be increased when used in combination with Pipemidic acid.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Empagliflozin.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Empagliflozin.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Empagliflozin.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Empagliflozin.
Amineptine Amineptine may decrease the hypoglycemic activities of Empagliflozin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Empagliflozin.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Empagliflozin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Empagliflozin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Empagliflozin.
Opipramol Opipramol may decrease the hypoglycemic activities of Empagliflozin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Empagliflozin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Empagliflozin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Empagliflozin.
Melitracen Melitracen may decrease the hypoglycemic activities of Empagliflozin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Empagliflozin.
Iprindole Iprindole may decrease the hypoglycemic activities of Empagliflozin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Empagliflozin.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Empagliflozin.
Imipramine Imipramine may decrease the hypoglycemic activities of Empagliflozin.
Doxepin Doxepin may decrease the hypoglycemic activities of Empagliflozin.
Desipramine Desipramine may decrease the hypoglycemic activities of Empagliflozin.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Empagliflozin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Empagliflozin.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Empagliflozin.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Empagliflozin.
Procaine Procaine may increase the orthostatic hypotensive activities of Empagliflozin.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Empagliflozin.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Empagliflozin.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Empagliflozin.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Empagliflozin.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Empagliflozin.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Empagliflozin.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Empagliflozin.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Empagliflozin.

Target Protein

Sodium/glucose cotransporter 2 SLC5A2

Referensi & Sumber

Synthesis reference: Wang XJ, Zhang L, Byrne D, Nummy L, Weber D, Krishnamurthy D, Yee N, Senanayake CH: Efficient synthesis of Empagliflozin, an inhibitor of SGLT-2, utilizing an AlCl3-promoted silane reduction of a beta-glycopyranoside. Org Lett. 2014 Aug 15;16(16):4090-3.
Artikel (PubMed)
  • PMID: 25805666
    Scheen AJ: Pharmacokinetics, Pharmacodynamics and Clinical Use of SGLT2 Inhibitors in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease. Clin Pharmacokinet. 2015 Jul;54(7):691-708. doi: 10.1007/s40262-015-0264-4.
  • PMID: 24716752
    Gangadharan Komala M, Mather A: Empagliflozin for the treatment of Type 2 diabetes. Expert Rev Clin Pharmacol. 2014 May;7(3):271-9. doi: 10.1586/17512433.2014.908703. Epub 2014 Apr 9.
  • PMID: 24746173
    Lamos EM, Younk LM, Davis SN: Empagliflozin, a sodium glucose co-transporter 2 inhibitor, in the treatment of type 1 diabetes. Expert Opin Investig Drugs. 2014 Jun;23(6):875-82. doi: 10.1517/13543784.2014.909407. Epub 2014 Apr 19.
  • PMID: 24766495
    Liakos A, Karagiannis T, Athanasiadou E, Sarigianni M, Mainou M, Papatheodorou K, Bekiari E, Tsapas A: Efficacy and safety of empagliflozin for type 2 diabetes: a systematic review and meta-analysis. Diabetes Obes Metab. 2014 Oct;16(10):984-93. doi: 10.1111/dom.12307. Epub 2014 May 28.
  • PMID: 24722494
    Haring HU, Merker L, Seewaldt-Becker E, Weimer M, Meinicke T, Broedl UC, Woerle HJ: Empagliflozin as add-on to metformin in patients with type 2 diabetes: a 24-week, randomized, double-blind, placebo-controlled trial. Diabetes Care. 2014 Jun;37(6):1650-9. doi: 10.2337/dc13-2105. Epub 2014 Apr 10.
  • PMID: 24991224
    Neumiller JJ: Empagliflozin: a new sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. Drugs Context. 2014 Jun 11;3:212262. doi: 10.7573/dic.212262. eCollection 2014.
  • PMID: 25260362
    Bogdanffy MS, Stachlewitz RF, van Tongeren S, Knight B, Sharp DE, Ku W, Hart SE, Blanchard K: Nonclinical safety of the sodium-glucose cotransporter 2 inhibitor empagliflozin. Int J Toxicol. 2014 Nov-Dec;33(6):436-49. doi: 10.1177/1091581814551648. Epub 2014 Sep 26.
  • PMID: 25296258
    Authors unspecified: Empagliflozin (Jardiance) for diabetes. Med Lett Drugs Ther. 2014 Oct 13;56(1453):99-100.
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