Peringatan Keamanan

The symptoms of acarbose overdose are likely to be consistent with its adverse effect profile and may therefore include significant gastrointestinal (GI) symptoms (flatulence, distension, etc), although an overdose on an empty stomach (i.e. when not co-administered with food) is less likely to result in these GI symptoms.L31628 In the event of an overdose, patients should be instructed to avoid carbohydrate-containing foods for 4-6 hours following administration as these can precipitate the aforementioned GI symptoms.L31628

Acarbose

DB00284

small molecule approved investigational

Deskripsi

Acarbose is a complex oligosaccharide that acts as an inhibitor of several enzymes responsible for the breakdown of complex carbohydrates in the intestines. It inhibits both pancreatic alpha-amylase and membrane-bound alpha-glucosidases - including intestinal glucoamylase, sucrase, maltase, and isomaltase - which are responsible for the metabolism of complex starches and oligo-, tri-, and disaccharides into absorbable simple sugars.L31633,A37868 By inhibiting the activity of these enzymes, acarbose limits the absorption of dietary carbohydrates and the subsequent postprandial increase in blood glucose and insulin levels. Acarbose is therefore used in conjunction with diet, exercise, and other pharmacotherapies for the management of blood sugar levels in patients with type 2 diabetes.L31628,L31633

Acarbose is one of only two approved alpha-glucosidase inhibitors (the other being miglitol), receiving its first FDA approval in 1995 under the brand name Precose (since discontinued).L31668 This class of antidiabetic therapy is not widely used due to their relatively modest impact on A1c, their requirement for thrice-daily dosing, and the potential for significant gastrointestinal adverse effects.L31668

Struktur Molekul 2D

Berat 645.608
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy volunteers, the plasma elimination half-life of acarbose is approximately 2 hours.[L31628]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The oral bioavailability of acarbose is extremely minimal, with less than 1-2% of orally administered parent drug reaching the systemic circulation. Despite this, approximately 35% of the total radioactivity from a radiolabeled and orally administered dose of acarbose reaches the systemic circulation, with peak plasma radioactivity occurring 14-24 hours after dosing - this delay is likely reflective of metabolite absorption rather than absorption of the parent drug. As acarbose is intended to work within the gut, its minimal degree of oral bioavailability is therapeutically desirable.L31628

Metabolisme

Acarbose is extensively metabolized within the gastrointestinal tract, primarily by intestinal bacteria and to a lesser extent by digestive enzymes, into at least 13 identified metabolites. Approximately 1/3 of these metabolites are absorbed into the circulation where they are subsequently renally excreted. The major metabolites appear to be methyl, sulfate, and glucuronide conjugates of 4-methylpyrogallol.L31628 Only one metabolite - resulting from the cleavage of a glucose molecule from acarbose - has been identified as having alpha-glucosidase inhibitory activity.L31628

Rute Eliminasi

Roughly half of an orally administered dose is excreted in the feces within 96 hours of administration.L31633 What little drug material is absorbed into the systemic circulation (approximately 34% of an orally administered dose) is excreted primarily by the kidneys, suggesting renal excretion would be a significant route of elimination if the parent drug was more readily absorbed - this is further supported by data in which approximately 89% of an intravenously administered dose of acarbose was excreted in the urine as active drug (in comparison to <2% following oral administration) within 48 hours.L31633

Interaksi Makanan

1 Data
  • 1. Take with food. Each dose should be taken with the first bite of a main meal.

Interaksi Obat

609 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Acarbose.
Digoxin The serum concentration of Digoxin can be decreased when it is combined with Acarbose.
Metildigoxin The serum concentration of Metildigoxin can be decreased when it is combined with Acarbose.
Acetyldigoxin The serum concentration of Acetyldigoxin can be decreased when it is combined with Acarbose.
Neomycin The metabolism of Acarbose can be decreased when combined with Neomycin.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Acarbose.
Moxifloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Acarbose can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Acarbose can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Acarbose can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Acarbose can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Acarbose can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Acarbose can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Acarbose can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Acarbose can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Acarbose can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Acarbose can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Acarbose can be decreased when used in combination with Epitizide.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Acarbose.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Acarbose.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Acarbose.
Trimipramine Trimipramine may decrease the hypoglycemic activities of Acarbose.
Amineptine Amineptine may decrease the hypoglycemic activities of Acarbose.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Acarbose.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Acarbose.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Acarbose.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Acarbose.
Opipramol Opipramol may decrease the hypoglycemic activities of Acarbose.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Acarbose.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Acarbose.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Acarbose.
Melitracen Melitracen may decrease the hypoglycemic activities of Acarbose.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Acarbose.
Iprindole Iprindole may decrease the hypoglycemic activities of Acarbose.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Acarbose.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Acarbose.
Imipramine Imipramine may decrease the hypoglycemic activities of Acarbose.
Doxepin Doxepin may decrease the hypoglycemic activities of Acarbose.
Desipramine Desipramine may decrease the hypoglycemic activities of Acarbose.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Acarbose.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Acarbose.
Dapagliflozin Dapagliflozin may increase the hypoglycemic activities of Acarbose.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Acarbose.
Leuprolide The therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.
Nelfinavir The therapeutic efficacy of Acarbose can be decreased when used in combination with Nelfinavir.
Indinavir The therapeutic efficacy of Acarbose can be decreased when used in combination with Indinavir.
Ziprasidone The therapeutic efficacy of Acarbose can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Acarbose can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Acarbose can be decreased when used in combination with Desogestrel.
Olanzapine The therapeutic efficacy of Acarbose can be decreased when used in combination with Olanzapine.
Megestrol acetate The therapeutic efficacy of Acarbose can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Acarbose can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Acarbose can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Acarbose can be decreased when used in combination with Progesterone.
Chlorpromazine The therapeutic efficacy of Acarbose can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Acarbose can be decreased when used in combination with Haloperidol.
Ritonavir The therapeutic efficacy of Acarbose can be decreased when used in combination with Ritonavir.
Piperazine The therapeutic efficacy of Acarbose can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate The therapeutic efficacy of Acarbose can be decreased when used in combination with Medroxyprogesterone acetate.
Niacin The therapeutic efficacy of Acarbose can be decreased when used in combination with Niacin.
Epinephrine The therapeutic efficacy of Acarbose can be decreased when used in combination with Epinephrine.
Norethisterone The therapeutic efficacy of Acarbose can be decreased when used in combination with Norethisterone.
Risperidone The therapeutic efficacy of Acarbose can be decreased when used in combination with Risperidone.
Pentamidine The therapeutic efficacy of Acarbose can be decreased when used in combination with Pentamidine.

Target Protein

Maltase-glucoamylase MGAM
Sucrase-isomaltase, intestinal SI
Pancreatic alpha-amylase AMY2A
Lysosomal alpha-glucosidase GAA

Referensi & Sumber

Synthesis reference: Anneliese Crueger, Wolfgang Piepersberg, Jurgen Distler, Ansgar Stratmann, "Acarbose biosynthesis genes from actinoplanes sp., process for the isolation thereof and the use thereof." U.S. Patent US5753501, issued December, 1977.
Artikel (PubMed)
  • PMID: 3286212
    Clissold SP, Edwards C: Acarbose. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs. 1988 Mar;35(3):214-43.
  • PMID: 29630266
    McIver LA, Tripp J: Acarbose .
  • PMID: 9429368
    Everett JA: Use of oral antidiabetic agents during breastfeeding. J Hum Lact. 1997 Dec;13(4):319-21. doi: 10.1177/089033449701300418.
  • PMID: 8893066
    Martin AE, Montgomery PA: Acarbose: an alpha-glucosidase inhibitor. Am J Health Syst Pharm. 1996 Oct 1;53(19):2277-90; quiz 2336-7. doi: 10.1093/ajhp/53.19.2277.
  • PMID: 26246763
    White JR Jr: A Brief History of the Development of Diabetes Medications. Diabetes Spectr. 2014 May;27(2):82-6. doi: 10.2337/diaspect.27.2.82.

Contoh Produk & Brand

Produk: 74 • International brands: 3
Produk
  • Acarbose
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Acarbose
    Tablet • 50 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 74 produk.
International Brands
  • Glucobay
  • Prandase — Bayer AG
  • Precose

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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