Peringatan Keamanan

The oral LD50 of carbocisteine in rats is >15000 mg/kg.L32378 An overdose with carbocisteine is likely to result in gastrointestinal discomfort with nausea and vomiting.L32373

Carbocisteine

DB04339

small molecule approved investigational

Deskripsi

Dyspnea and cough are common symptoms of chronic obstructive pulmonary disease (COPD)A231169 and other respiratory conditions characterized by increased mucus production. Individuals with COPD have a greater risk of pulmonary infection due to the growth and accumulation of viruses and bacteria in thick bronchial mucus. Carbocisteine is a mucolytic drug that alleviates respiratory symptoms and infections by reducing the viscosity of mucus, allowing it to be expelled.L32383

Several licenses for this drug were withdrawn following serious and fatal paradoxical effects after carbocisteine therapy in children; respiratory dress, dyspnea, and cough aggravation were reported by physicians in France and Italy.A230993 Carbocisteine is currently not FDA or Health Canada approved, but is approved for use in Asia, Europe, and South America.

Struktur Molekul 2D

Berat 179.194
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of carbicostine is 1.33 hours.[A230988]
Volume Distribusi Carbocisteine penetrates well into the lung and bronchial secretions.[A230988]
Klirens (Clearance) Clearance information for carbocisteine is not readily available in the literature.

Absorpsi

Carbocisteine is rapidly absorbed in the gastrointestinal tract when taken orally with peak serum concentrations achieved within 1 to 1.7 hours.A230988

Metabolisme

Metabolic pathways for carbocisteine include acetylation, decarboxylation, and sulfoxidation, leading to the formation of pharmacologically inactive carbocisteine derivatives. Significant variability exists in metabolism due to genetic polymorphism in sulfoxidation capacity. Two cytosolic enzymes are responsible for the metabolism of carbocisteine: cysteine dioxygenase and phenylalanine 4-hydroxylase.A231104 Reduced metabolism can cause increased exposure to carbocisteine, explaining variable clinical response between patients who may polymorphisms affecting the enzymes responsible for carbocisteine metabolism.A230988 It is generally accepted that sulfodixation is the main metabolic pathway of carbocisteine, however, one group of researchers found a novel urinary metabolite, S-(carboxymethylthio)-L-cysteine (CMTC). No cysteinyl sulfoxide metabolites were found in the urine of patients taking carbocisteine in this study.A230998

Rute Eliminasi

About 30% to 60% of an orally administered dose is detected unchanged in the urine.A230988

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

18 Data
Glimepiride The risk or severity of adverse effects can be increased when Glimepiride is combined with Carbocisteine.
Acetohexamide The risk or severity of adverse effects can be increased when Acetohexamide is combined with Carbocisteine.
Chlorpropamide The risk or severity of adverse effects can be increased when Chlorpropamide is combined with Carbocisteine.
Tolazamide The risk or severity of adverse effects can be increased when Tolazamide is combined with Carbocisteine.
Glyburide The risk or severity of adverse effects can be increased when Glyburide is combined with Carbocisteine.
Glipizide The risk or severity of adverse effects can be increased when Glipizide is combined with Carbocisteine.
Gliclazide The risk or severity of adverse effects can be increased when Gliclazide is combined with Carbocisteine.
Tolbutamide The risk or severity of adverse effects can be increased when Tolbutamide is combined with Carbocisteine.
Gliquidone The risk or severity of adverse effects can be increased when Gliquidone is combined with Carbocisteine.
Glisoxepide The risk or severity of adverse effects can be increased when Glisoxepide is combined with Carbocisteine.
Glibornuride The risk or severity of adverse effects can be increased when Glibornuride is combined with Carbocisteine.
Carbutamide The risk or severity of adverse effects can be increased when Carbutamide is combined with Carbocisteine.
Metahexamide The risk or severity of adverse effects can be increased when Metahexamide is combined with Carbocisteine.
Griseofulvin The risk or severity of adverse effects can be increased when Griseofulvin is combined with Carbocisteine.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Carbocisteine.
Disulfiram The risk or severity of adverse effects can be increased when Disulfiram is combined with Carbocisteine.
Metronidazole The risk or severity of adverse effects can be increased when Metronidazole is combined with Carbocisteine.
Ketoconazole The risk or severity of adverse effects can be increased when Ketoconazole is combined with Carbocisteine.

Target Protein

Kelch-like ECH-associated protein 1 KEAP1
Nuclear factor erythroid 2-related factor 2 NFE2L2
PI-PLC X domain-containing protein 3 PLCXD3
Lactosylceramide alpha-2,3-sialyltransferase ST3GAL5

Referensi & Sumber

Synthesis reference: Maierhofer, A. and Wagner, H.: US. Patent 4,129,593; December 12,1978: assigned to Deutsche Gold- und Silber-Scheideanstalt vormals Roessler (Germany).
Artikel (PubMed)
  • PMID: 28786969
    Alibasic E, Skopljak A, Cengic A, Krstovic G, Trifunovic N, Catic T, Kapo B, Mehic M, Hadzimuratovic A: Efficacy of carbocisteine in the treatment of chronic obstructive pulmonary disease and impact on the quality of life. Med Glas (Zenica). 2017 Aug 1;14(2):182-188. doi: 10.17392/906-17.
  • PMID: 19281081
    Hooper C, Calvert J: The role for S-carboxymethylcysteine (carbocisteine) in the management of chronic obstructive pulmonary disease. Int J Chron Obstruct Pulmon Dis. 2008;3(4):659-69.
  • PMID: 21818391
    Mallet P, Mourdi N, Dubus JC, Bavoux F, Boyer-Gervoise MJ, Jean-Pastor MJ, Chalumeau M: Respiratory paradoxical adverse drug reactions associated with acetylcysteine and carbocysteine systemic use in paediatric patients: a national survey. PLoS One. 2011;6(7):e22792. doi: 10.1371/journal.pone.0022792. Epub 2011 Jul 27.
  • PMID: 8287066
    Gregory WL, James OF, Turner I, Meese CO, Idle JR: Re-evaluation of the metabolism of carbocisteine in a British white population. Pharmacogenetics. 1993 Oct;3(5):270-4. doi: 10.1097/00008571-199310000-00007.
  • PMID: 19664007
    Yoshida M, Nakayama K, Yasuda H, Kubo H, Kuwano K, Arai H, Yamaya M: Carbocisteine inhibits oxidant-induced apoptosis in cultured human airway epithelial cells. Respirology. 2009 Sep;14(7):1027-34. doi: 10.1111/j.1440-1843.2009.01594.x. Epub 2009 Aug 2.
  • PMID: 1673403
    Hofmann U, Eichelbaum M, Seefried S, Meese CO: Identification of thiodiglycolic acid, thiodiglycolic acid sulfoxide, and (3-carboxymethylthio)lactic acid as major human biotransformation products of S-carboxymethyl-L-cysteine. Drug Metab Dispos. 1991 Jan-Feb;19(1):222-6.
  • PMID: -
    Prasanta Raghab Mohapatra, Deepak Aggarwal: Carbocisteine for acute exacerbations of COPD . 2008 Nov 8;372(9650):1630-1631.
  • PMID: 20956181
    Balsamo R, Lanata L, Egan CG: Mucoactive drugs. Eur Respir Rev. 2010 Jun;19(116):127-33. doi: 10.1183/09059180.00003510.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 0 • International brands: 7
International Brands
  • Actithiol — Almirall
  • Lisomucil — Sanofi-Aventis
  • Muciclar — Pfizer
  • Mucodyne — Sanofi-Aventis
  • Mucolex — General Pharma
  • Rhinathiol — Sanofi-Aventis
  • Transbronchin — Meda

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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