Peringatan Keamanan

Animal studies in pregnancy have shown no adverse effects on the mother or offspring at normal doses, however these results are not always applicable to humans. There is a voluntary fetal exposure registry FDA label,L6067. Animal studies at 100 times the maximum recommended human dose resulted in an increase in rib malformations. Sitagliptin is excreted in the milk of rats but it is not known if it would also be expressed in human breast milk. Because many drugs are expressed in human breast milk, the risk and benefit of prescribing the medication must be considered. There is currently a lack of safety and effectiveness data in pediatric patients. No differences in safety and efficacy were observed in geriatric patients compared to younger patients, however caution should be used in this population as they are more likely to have reduced renal functionFDA label. Sitagliptin has also been associated with a 34% relative risk increase for all cause infectionA2260. There was no significant difference in patient response across sex, age, race, ethnicity, and BMIA2257.

Sitagliptin

DB01261

small molecule approved investigational

Deskripsi

Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in conjunction with diet and exercise to improve glycemic control in patients with type 2 diabetes mellitusFDA label,A2260,A2255,A2256. The effect of this medication leads to glucose dependent increases in insulin and decreases in glucagon to improve control of blood sugarFDA label,A2255. Sitagliptin was granted FDA approval on October 16, 2006L6061.

Struktur Molekul 2D

Berat 407.3136
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 12.4 hours[FDA label]. Other studies have reported a half life of approximately 11 hours[A2260].
Volume Distribusi 198L[FDA label,A2260].
Klirens (Clearance) 350mL/min[FDA label,A2256].

Absorpsi

Sitagliptin is 87% orally bioavailable and taking it with or without food does not affect its pharmacokineticsFDA label,A2260. Sitagliptin reaches maximum plasma concentration in 2 hoursA2260.

Metabolisme

Sitagliptin is mostly not metabolised, with 79% of the dose excreted in the urine as the unchanged parent compoundFDA label. Minor metabolic pathways are mediated mainly by cytochrome p450(CYP)3A4 and to a lesser extent by CYP2C8FDA label. After 18 hours, 81% of the dose has remained unchanged, while 2% has been N-sulfated to the M1 metabolite, 6% has been oxidatively desaturated and cyclized to the M2 metabolite, <1% glucuronidated at an unknown site to the M3 metabolite, <1% has been carbamoylated and glucuronidated to the M4 metabolite, 6% has been oxidatively saturated and cyclized to the M5 metabolite, and 2% has been hydroxylated at an unknown site to the M6 metaboliteA177649. The M2 metabolite is the cis isomer while the M5 metabolite is the trans isomer of the same metaboliteA177649.

Rute Eliminasi

Approximately 79% of sitagliptin is excreted in the urine as the unchanged parent compoundFDA label. 87% of the dose is eliminated in the urine and 13% in the fecesFDA label,A2260.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1553 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Sitagliptin.
Ranolazine The serum concentration of Sitagliptin can be increased when it is combined with Ranolazine.
Mifepristone The serum concentration of Sitagliptin can be increased when it is combined with Mifepristone.
Aspartame The excretion of Sitagliptin can be decreased when combined with Aspartame.
Aminohippuric acid The excretion of Sitagliptin can be decreased when combined with Aminohippuric acid.
Guanidine The excretion of Sitagliptin can be decreased when combined with Guanidine.
Oxytetracycline The excretion of Sitagliptin can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Sitagliptin can be decreased when combined with Leucovorin.
Dinoprostone The excretion of Sitagliptin can be decreased when combined with Dinoprostone.
Famotidine The excretion of Sitagliptin can be decreased when combined with Famotidine.
Minocycline The excretion of Sitagliptin can be decreased when combined with Minocycline.
Mercaptopurine The excretion of Sitagliptin can be decreased when combined with Mercaptopurine.
Novobiocin The excretion of Sitagliptin can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Sitagliptin can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Sitagliptin can be decreased when combined with Melatonin.
Ouabain The excretion of Sitagliptin can be decreased when combined with Ouabain.
Cilastatin The excretion of Sitagliptin can be decreased when combined with Cilastatin.
Tazobactam The excretion of Sitagliptin can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Sitagliptin can be decreased when combined with trans-2-hydroxycinnamic acid.
Cholic Acid The excretion of Sitagliptin can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Sitagliptin can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Sitagliptin can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Sitagliptin can be decreased when combined with Caprylic acid.
Ataluren The excretion of Sitagliptin can be decreased when combined with Ataluren.
Cabotegravir The excretion of Sitagliptin can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Sitagliptin can be decreased when combined with Pradigastat.
Linezolid The excretion of Sitagliptin can be decreased when combined with Linezolid.
Cefotiam The excretion of Sitagliptin can be decreased when combined with Cefotiam.
Cefalotin The excretion of Sitagliptin can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Sitagliptin can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Sitagliptin can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Sitagliptin can be decreased when combined with Piroxicam.
Methotrexate The excretion of Sitagliptin can be decreased when combined with Methotrexate.
Cephalexin The excretion of Sitagliptin can be decreased when combined with Cephalexin.
Diclofenac The excretion of Sitagliptin can be decreased when combined with Diclofenac.
Acyclovir The excretion of Sitagliptin can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Sitagliptin can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Sitagliptin can be decreased when combined with Cefaclor.
Ketoprofen The excretion of Sitagliptin can be decreased when combined with Ketoprofen.
Cefadroxil The excretion of Sitagliptin can be decreased when combined with Cefadroxil.
Cefamandole The excretion of Sitagliptin can be decreased when combined with Cefamandole.
Cefazolin The excretion of Sitagliptin can be decreased when combined with Cefazolin.
Ceftizoxime The excretion of Sitagliptin can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Sitagliptin can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Sitagliptin can be decreased when combined with Ceftibuten.
Cefaloridine The excretion of Sitagliptin can be decreased when combined with Cefaloridine.
Cimetidine The excretion of Sitagliptin can be decreased when combined with Cimetidine.
Ganciclovir The excretion of Sitagliptin can be decreased when combined with Ganciclovir.
Pantoprazole The excretion of Sitagliptin can be decreased when combined with Pantoprazole.
Indomethacin The excretion of Sitagliptin can be decreased when combined with Indomethacin.
Lansoprazole The excretion of Sitagliptin can be decreased when combined with Lansoprazole.
Tetracycline The excretion of Sitagliptin can be decreased when combined with Tetracycline.
Ibuprofen The excretion of Sitagliptin can be decreased when combined with Ibuprofen.
Letermovir The metabolism of Sitagliptin can be decreased when combined with Letermovir.
Esomeprazole The excretion of Sitagliptin can be decreased when combined with Esomeprazole.
Ceftriaxone The excretion of Sitagliptin can be decreased when combined with Ceftriaxone.
Cefoperazone The excretion of Sitagliptin can be decreased when combined with Cefoperazone.
Taurocholic acid The excretion of Sitagliptin can be decreased when combined with Taurocholic acid.
Favipiravir The excretion of Sitagliptin can be decreased when combined with Favipiravir.
Tafamidis The excretion of Sitagliptin can be decreased when combined with Tafamidis.
Valproic acid The excretion of Sitagliptin can be decreased when combined with Valproic acid.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Sitagliptin.
Moxifloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Sitagliptin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Sitagliptin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Sitagliptin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Sitagliptin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Benzthiazide.

Target Protein

Dipeptidyl peptidase 4 DPP4

Referensi & Sumber

Synthesis reference: Nurit Perlman, Marina Etinger, Valerie Niddam-Hildesheim, Mili Abramov, "Preparation of sitagliptin intermediate." U.S. Patent US20090192326, issued July 30, 2009.
Artikel (PubMed)
  • PMID: 16338283
    Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 Dec;78(6):675-88.
  • PMID: 16855072
    Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA: Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 Aug;46(8):876-86.
  • PMID: 18182122
    Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP: Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 Feb;24(2):489-96. doi: 10.1185/030079908X261069 .
  • PMID: 19065993
    Richter B, Bandeira-Echtler E, Bergerhoff K, Lerch C: Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes. Vasc Health Risk Manag. 2008;4(4):753-68.
  • PMID: 17220239
    Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, Ebel D, Larson P, Zeng W, Chen L, Dilzer S, Lasseter K, Gottesdiener K, Wagner JA, Herman GA: Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor 14Csitagliptin in humans. Drug Metab Dispos. 2007 Apr;35(4):533-8. doi: 10.1124/dmd.106.013136. Epub 2007 Jan 12.

Contoh Produk & Brand

Produk: 486 • International brands: 0
Produk
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    Tablet • 25 mg • Oral • Canada • Generic • Approved
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  • Apo-sitagliptin
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Menampilkan 8 dari 486 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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