Peringatan Keamanan

Common adverse reactions (reported in ?4% of patients treated with alogliptin 25 mg and more frequently than in patients who received placebo) are: nasopharyngitis, headache, and upper respiratory tract infection.

Alogliptin

DB06203

small molecule approved

Deskripsi

Alogliptin is a selective, orally-bioavailable inhibitor of enzymatic activity of dipeptidyl peptidase-4 (DPP-4). Chemically, alogliptin is prepared as a benzoate salt and exists predominantly as the R-enantiomer (>99%). It undergoes little or no chiral conversion in vivo to the (S)-enantiomer. FDA approved January 25, 2013.

Struktur Molekul 2D

Berat 339.3916
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half-life = 21 hours
Volume Distribusi Following a single, 12.5 mg intravenous infusion of alogliptin to healthy subjects, the volume of distribution during the terminal phase was 417 L, indicating that the drug is well distributed into tissues.
Klirens (Clearance) Renal clearance = 9.6 L/h (this value indicates some active renal tubular secretion); Systemic clearance = 14.0 L/h.

Absorpsi

The pharmacokinetics of NESINA was also shown to be similar in healthy subjects and in patients with type 2 diabetes. When single, oral doses up to 800 mg in healthy subjects and type 2 diabetes patients are given, the peak plasma alogliptin concentration (median Tmax) occurred 1 to 2 hours after dosing. Accumulation of aloglipin is minimal. The absolute bioavailability of NESINA is approximately 100%. Food does not affect the absorption of alogliptin.

Metabolisme

Alogliptin does not undergo extensive metabolism. Two minor metabolites that were detected are N-demethylated alogliptin (<1% of parent compound) and N-acetylated alogliptin (<6% of parent compound). The N-demethylated metabolite is active and an inhibitor of DPP-4. The N-acetylated metabolite is inactive. Cytochrome enzymes that are involved with the metabolism of alogliptin are CYP2D6 and CYP3A4 but the extent to which this occurs is minimal. Approximately 10-20% of the dose is hepatically metabolized by cytochrome enzymes.

Rute Eliminasi

Renal excretion (76%) and feces (13%). 60% to 71% of the dose is excreted as unchanged drug in the urine.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1460 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Alogliptin.
Mirabegron The serum concentration of Alogliptin can be increased when it is combined with Mirabegron.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Alogliptin.
Moxifloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Alogliptin can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Alogliptin can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Alogliptin can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Alogliptin can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Alogliptin can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Epitizide.
Amineptine Amineptine may decrease the hypoglycemic activities of Alogliptin.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Alogliptin.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Alogliptin.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Alogliptin.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Alogliptin.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Alogliptin.
Melitracen Melitracen may decrease the hypoglycemic activities of Alogliptin.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Alogliptin.
Iprindole Iprindole may decrease the hypoglycemic activities of Alogliptin.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Alogliptin.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Alogliptin.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Alogliptin.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Alogliptin.
Opipramol Opipramol may decrease the hypoglycemic activities of Alogliptin.
Doxepin Doxepin may decrease the hypoglycemic activities of Alogliptin.
Glimepiride Alogliptin may increase the hypoglycemic activities of Glimepiride.
Acetohexamide Alogliptin may increase the hypoglycemic activities of Acetohexamide.
Chlorpropamide Alogliptin may increase the hypoglycemic activities of Chlorpropamide.
Tolazamide Alogliptin may increase the hypoglycemic activities of Tolazamide.
Glyburide Alogliptin may increase the hypoglycemic activities of Glyburide.
Glipizide Alogliptin may increase the hypoglycemic activities of Glipizide.
Gliclazide Alogliptin may increase the hypoglycemic activities of Gliclazide.
Tolbutamide Alogliptin may increase the hypoglycemic activities of Tolbutamide.
Gliquidone Alogliptin may increase the hypoglycemic activities of Gliquidone.
Glisoxepide Alogliptin may increase the hypoglycemic activities of Glisoxepide.
Glibornuride Alogliptin may increase the hypoglycemic activities of Glibornuride.
Carbutamide Alogliptin may increase the hypoglycemic activities of Carbutamide.
Metahexamide Alogliptin may increase the hypoglycemic activities of Metahexamide.
Dapagliflozin Dapagliflozin may increase the hypoglycemic activities of Alogliptin.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Alogliptin.
Leuprolide The therapeutic efficacy of Alogliptin can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Goserelin.
Ziprasidone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Alogliptin can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Alogliptin can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Alogliptin can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Alogliptin can be decreased when used in combination with Megestrol acetate.
Levonorgestrel The therapeutic efficacy of Alogliptin can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Progesterone.
Piperazine The therapeutic efficacy of Alogliptin can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate The therapeutic efficacy of Alogliptin can be decreased when used in combination with Medroxyprogesterone acetate.
Niacin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Niacin.
Epinephrine The therapeutic efficacy of Alogliptin can be decreased when used in combination with Epinephrine.
Norethisterone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Norethisterone.
Risperidone The therapeutic efficacy of Alogliptin can be decreased when used in combination with Risperidone.
Pentamidine The therapeutic efficacy of Alogliptin can be decreased when used in combination with Pentamidine.
Ethynodiol diacetate The therapeutic efficacy of Alogliptin can be decreased when used in combination with Ethynodiol diacetate.
Pseudoephedrine The therapeutic efficacy of Alogliptin can be decreased when used in combination with Pseudoephedrine.
Etacrynic acid The therapeutic efficacy of Alogliptin can be decreased when used in combination with Etacrynic acid.
Norgestimate The therapeutic efficacy of Alogliptin can be decreased when used in combination with Norgestimate.

Target Protein

Dipeptidyl peptidase 4 DPP4

Referensi & Sumber

Synthesis reference: Kenji Nakamura, Kenichiro Kiyoshima, Junya Nomura, "SOLID PREPARATION COMPRISING ALOGLIPTIN AND PIOGLITAZONE." U.S. Patent US20100092551, issued April 15, 2010.
Artikel (PubMed)
  • PMID: 18405789
    Christopher R, Covington P, Davenport M, Fleck P, Mekki QA, Wann ER, Karim A: Pharmacokinetics, pharmacodynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4 inhibitor alogliptin in healthy male subjects. Clin Ther. 2008 Mar;30(3):513-27. doi: 10.1016/j.clinthera.2008.03.005.
  • PMID: 18405788
    Covington P, Christopher R, Davenport M, Fleck P, Mekki QA, Wann ER, Karim A: Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes. Clin Ther. 2008 Mar;30(3):499-512. doi: 10.1016/j.clinthera.2008.03.004.
  • PMID: 22686547
    Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000.

Contoh Produk & Brand

Produk: 131 • International brands: 0
Produk
  • Alogliptin
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 6.25 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 12.5 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 12.5 mg/1 • Oral • US • Generic • Approved
  • Alogliptin
    Tablet, film coated • 25 mg/1 • Oral • US • Generic • Approved
  • Alogliptin and Metformin Hydrochloride
    Tablet, film coated • - • Oral • US • Generic • Approved
Menampilkan 8 dari 131 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul