Peringatan Keamanan

LD50, oral, mouse: >1000 mg/kg

Carglumic acid

DB06775

small molecule approved

Deskripsi

Carglumic acid is a drug used for the treatment of hyperammonemia in patients with a deficiency in N-acetyl glutamate synthase. This rare genetic disorder results in elevated blood levels of ammonia, which can eventually cross the blood–brain barrier and cause neurologic problems, cerebral edema, coma, and death. Carglumic acid was approved by the U.S. Food and Drug Administration (FDA) on 18 March 2010.

Struktur Molekul 2D

Berat 190.154
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Median values for the terminal half-life was 5.6 hours (range 4.3-9.5).
Volume Distribusi The apparent volume of distribution was 2657 L (range: 1616-5797).
Klirens (Clearance) The apparent total clearance was 5.7 L/min (range 3.0-9.7), the renal clearance was 290 mL/min (range 204-445), and the 24-hour urinary excretion was 4.5 % of the dose (range 3.5-7.5).

Absorpsi

30% bioavailability; Cmax, mean, 100 mg/kg dose = 2.6 ?g/mL (range of 1.9 - 4.8) Carglumic acid is not subject to to intracellular degradation.

Metabolisme

A proportion of carglumic acid may be metabolized by the intestinal bacterial flora. The likely end product of carglumic acid metabolism is carbon dioxide, eliminated through the lungs.

Rute Eliminasi

Following administration of a single radiolabeled oral dose of 100 mg/kg of body weight, 9% of the dose was excreted unchanged in the urine and up to 60% of the dose was excreted unchanged in the feces.

Interaksi Makanan

2 Data
  • 1. Take before a meal. Take carglumic acid right before eating.
  • 2. Take with plain water. Carglumic acid tablets are dispersed in water to produce an oral suspension and should not be swallowed whole.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Carbamoyl-phosphate synthase [ammonia], mitochondrial CPS1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12447942
    Elpeleg O, Shaag A, Ben-Shalom E, Schmid T, Bachmann C: N-acetylglutamate synthase deficiency and the treatment of hyperammonemic encephalopathy. Ann Neurol. 2002 Dec;52(6):845-9.
  • PMID: 15480384
    Caldovic L, Morizono H, Daikhin Y, Nissim I, McCarter RJ, Yudkoff M, Tuchman M: Restoration of ureagenesis in N-acetylglutamate synthase deficiency by N-carbamylglutamate. J Pediatr. 2004 Oct;145(4):552-4.
  • PMID: 20410539
    Thompson CA: Carglumic acid approved to treat genetic hyperammonemia. Am J Health Syst Pharm. 2010 May 1;67(9):690. doi: 10.2146/news100031.
  • PMID: 21941437
    Haberle J: Role of carglumic acid in the treatment of acute hyperammonemia due to N-acetylglutamate synthase deficiency. Ther Clin Risk Manag. 2011;7:327-32. doi: 10.2147/TCRM.S12703. Epub 2011 Aug 2.

Contoh Produk & Brand

Produk: 11 • International brands: 0
Produk
  • Carbaglu
    Tablet, for suspension • 200 mg/1 • Oral • US • Approved
  • Carbaglu
    Tablet, for suspension • 200 mg • Oral • Canada • Approved
  • Carbaglu
    Tablet, for suspension • 200 mg • Oral • EU • Approved
  • Carbaglu
    Tablet, for suspension • 200 mg • Oral • EU • Approved
  • Carbaglu
    Tablet, for suspension • 200 mg • Oral • EU • Approved
  • Carglumic Acid
    Tablet, for suspension • 200 mg/1 • Oral • US • Generic • Approved
  • Carglumic Acid
    Tablet, for suspension • 200 mg/1 • Oral • US • Generic • Approved
  • Carglumic acid
    Tablet, for suspension • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 11 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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