Peringatan Keamanan

IPN-RAT LD50 580 mg/kg

Chlorpropamide

DB00672

small molecule approved investigational

Deskripsi

Chlorpropamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating ? cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic ? cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Chlorpropamide is not recommended for the treatment of NIDDM as it increases blood pressure and the risk of retinopathy (UKPDS-33). Up to 80% of the single oral dose of chlorpropramide is metabolized, likely in the liver; 80-90% of the dose is excreted in urine as unchanged drug and metabolites. Renal and hepatic dysfunction may increase the risk of hypoglycemia.

Struktur Molekul 2D

Berat 276.74
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 36 hours with interindividual variation ranging from 25-60 hours. Duration of effect persists for at least 24 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Readily absorbed from the GI tract. Peak plasma concentrations occur within 2-4 hours and the onset of action occurs within one hour. The maximal effect of chlorpropamide is seen 3-6 hours following oral administration.

Metabolisme

Up to 80% of dose is metabolized likely through the liver to to 2-hydroxylchlorpropamide (2-OH CPA), p-chlorobenzenesulfonylurea (CBSU), 3-hydroxylchlorpropamide (3-OH CPA), and p-chlorobenzenesulfonamide (CBSA); CBSA may be produced by decomposition in urine. It is unknown whether chlorpropamide metabolites exert hypoglycemic effects.

Rute Eliminasi

80-90% of a single oral dose is excreted in the urine as unchaged drug and metabolites within 96 hours.

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Take before a meal. Take 30 minutes before a meal.
  • 3. Take on an empty stomach. Food decreases the rate of absorption.

Interaksi Obat

1527 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Chlorpropamide.
Carbocisteine The risk or severity of adverse effects can be increased when Chlorpropamide is combined with Carbocisteine.
Chloramphenicol The metabolism of Chlorpropamide can be decreased when combined with Chloramphenicol.
Cimetidine The serum concentration of Chlorpropamide can be increased when it is combined with Cimetidine.
Fluconazole The serum concentration of Chlorpropamide can be increased when it is combined with Fluconazole.
Metreleptin Metreleptin may increase the hypoglycemic activities of Chlorpropamide.
Probenecid The protein binding of Chlorpropamide can be decreased when combined with Probenecid.
Ranitidine The serum concentration of Chlorpropamide can be increased when it is combined with Ranitidine.
Voriconazole The serum concentration of Chlorpropamide can be increased when it is combined with Voriconazole.
Allopurinol The excretion of Chlorpropamide can be decreased when combined with Allopurinol.
Clarithromycin The serum concentration of Chlorpropamide can be increased when it is combined with Clarithromycin.
Ascorbic acid Ascorbic acid may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Citric acid Citric acid may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Ammonium chloride Ammonium chloride may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Methenamine Methenamine may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Dehydroascorbic acid Dehydroascorbic acid may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Sodium phosphate, monobasic Sodium phosphate, monobasic may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Sodium ascorbate Sodium ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Calcium ascorbate Calcium ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Magnesium ascorbate Magnesium ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Zinc ascorbate Zinc ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Niacinamide ascorbate Niacinamide ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Ferrous ascorbate Ferrous ascorbate may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Sodium phosphate, dibasic Sodium phosphate, dibasic may decrease the excretion rate of Chlorpropamide which could result in a higher serum level.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Chlorpropamide.
Rifampin The serum concentration of Chlorpropamide can be decreased when it is combined with Rifampicin.
Moxifloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Epitizide.
Esmolol Esmolol may increase the hypoglycemic activities of Chlorpropamide.
Landiolol Landiolol may increase the hypoglycemic activities of Chlorpropamide.
Ethanol The risk or severity of adverse effects can be increased when Chlorpropamide is combined with Ethanol.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Chlorpropamide.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Chlorpropamide.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Chlorpropamide.
Amineptine Amineptine may decrease the hypoglycemic activities of Chlorpropamide.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Chlorpropamide.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Chlorpropamide.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Chlorpropamide.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Chlorpropamide.
Opipramol Opipramol may decrease the hypoglycemic activities of Chlorpropamide.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Chlorpropamide.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Chlorpropamide.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Chlorpropamide.
Melitracen Melitracen may decrease the hypoglycemic activities of Chlorpropamide.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Chlorpropamide.
Iprindole Iprindole may decrease the hypoglycemic activities of Chlorpropamide.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Chlorpropamide.
Amitriptyline Amitriptyline may decrease the hypoglycemic activities of Chlorpropamide.
Doxepin Doxepin may decrease the hypoglycemic activities of Chlorpropamide.
Imipramine Imipramine may decrease the hypoglycemic activities of Chlorpropamide.
Desipramine Desipramine may decrease the hypoglycemic activities of Chlorpropamide.
Clomipramine Clomipramine may decrease the hypoglycemic activities of Chlorpropamide.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Chlorpropamide.
Clofibrate The risk or severity of hypoglycemia can be increased when Clofibrate is combined with Chlorpropamide.
Fenofibrate The risk or severity of hypoglycemia can be increased when Fenofibrate is combined with Chlorpropamide.

Target Protein

ATP-binding cassette sub-family C member 8 ABCC8
ATP-sensitive inward rectifier potassium channel 10 KCNJ10

Referensi & Sumber

Synthesis reference: McLamore, W.M.; U S . Patent 3,349,124; October 24,1967; assigned to Chas. Pfizer Co., Inc.

Contoh Produk & Brand

Produk: 17 • International brands: 13
Produk
  • Apo Chlorpropamide Tab 100mg
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo Chlorpropamide Tab 250mg
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Chlorpropamide
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Chlorpropamide
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Chlorpropamide
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Chlorpropamide
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Chlorpropamide
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Chlorpropamide
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 17 produk.
International Brands
  • Abemide — Kobayashi Kako
  • Chloronase — Hoechst
  • Dabinese — Pfizer
  • Diabeedol — Sriprasit Dispensary
  • Diabemide — Guidotti
  • Diabezin — Prince
  • Diabitex — Plantex-Ikapharm
  • Dibecon — Pharmasant
  • Glycemin — Siam Bheasach
  • Hypomide — Aspen Pharmacare

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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