Peringatan Keamanan

Two cases of human overdoses with cysteamine are recorded in the literature, according to prescribing information. In one case, vomiting was immediate after the administration of cysteamine, and the patient did not experience other symptoms. A 200 to 250 mg/kg dose was accidentally ingested by a healthy 13-month-old child. Vomiting and dehydration followed. A full recovery was made after hospitalization and the replenishment of fluids.L15646

There is no known antidote for an overdose with cysteamine. In the case of an overdose, provide supportive treatment, especially to the cardiovascular and respiratory systems. Hemodialysis may be useful in some cases due to the fact that cysteamine has poor plasma protein binding.L15646

Cysteamine

DB00847

small molecule approved investigational

Deskripsi

Cystinosis is a rare disease caused by mutations in the CTNS gene that encodes for cystinosin, a protein responsible for transporting cystine out of the cell lysosome. A defect in cystinosin function is followed by cystine accumulation throughout the body, especially the eyes and kidneys.A218721

Several preparations of cysteamine exist for the treatment of cystinosis manifestations, some in capsule form, and others in ophthalmic solution form.L15606,L15616 In particular, cystine deposits on the eye can cause significant discomfort throughout the day and require frequent treatment with eye drops, typically every waking hour.L15611

On August 25th 2020, the first ophthalmic solution for cystinosis requiring only 4 daily treatments was granted FDA approval.L15606 Cysteamine eye drops are a practical and effective option for those affected by ocular cystinosis. Marketed by Recordati Rare Diseases Inc., CYSTADROPS® reduce the burden of multiple frequent medications normally administered to those with cystinosis.L15601

Struktur Molekul 2D

Berat 77.149
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of cysteamine is about 3.7 hours.[A218941]
Volume Distribusi Cysteamine has a volume of distribution of about 129 L, according to one pharmacokinetic study.[A218941] Prescribing information indicates a volume of distribution of 382 L for the delayed-release formulation and 198 L for the immediate-release preparation.[L15616] It is known to cross the blood-brain barrier.[A218946]
Klirens (Clearance) The plasma clearance of cysteamine is about 1.2 - 1.4 L/min.[L15616] One reference mentions a clearance of 89.9 L/h in patients with Cystic Fibrosis.[A218941]

Absorpsi

Orally administered cysteamine is absorbed in the gastrointestinal tract and reaches its maximum plasma concentration in about 1.4 hours, with some variation according to the type of formulation (delayed versus immediate-release).A218941,A218936,L15616 One pharmacokinetic study of adults with Cystic Fibrosis revealed a Cmax of 2.86 mg/L.A218941The maximum plasma concentration after administration of cysteamine eye drops is unknown, however, it is likely to be considerably lower than oral administration.L15606 According to prescribing information, the AUC 0-12 h for the delayed-release oral tablets is 99.26 ± 44.2 ?mol*h/L with a Cmax of 27.70 ± 14.99 ?mol/L.L15616 The AUC 0-12 for the immediate-release tablets is 192.00 ± 75.62 ?mol*h/L with a Cmax of 37.72 ± 12.10 ?mol/L.L15616

Metabolisme

There is limited information in the literature regarding the metabolism of cysteamine. This drug undergoes significant first-pass metabolism.A218946

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Take on an empty stomach. The delayed-release capsules should be taken at least 30 minutes before or 2 hours after a high-fat meal to ensure adequate exposure.
  • 2. Take with or without food. The immediate release preparation can be taken with or without food.

Interaksi Obat

44 Data
Magnesium oxide The bioavailability of Cysteamine can be decreased when combined with Magnesium oxide.
Sodium bicarbonate The bioavailability of Cysteamine can be decreased when combined with Sodium bicarbonate.
Aluminum hydroxide The bioavailability of Cysteamine can be decreased when combined with Aluminum hydroxide.
Calcium carbonate The bioavailability of Cysteamine can be decreased when combined with Calcium carbonate.
Magaldrate The bioavailability of Cysteamine can be decreased when combined with Magaldrate.
Magnesium hydroxide The bioavailability of Cysteamine can be decreased when combined with Magnesium hydroxide.
Magnesium trisilicate The bioavailability of Cysteamine can be decreased when combined with Magnesium trisilicate.
Magnesium carbonate The bioavailability of Cysteamine can be decreased when combined with Magnesium carbonate.
Bismuth subnitrate The bioavailability of Cysteamine can be decreased when combined with Bismuth subnitrate.
Magnesium silicate The bioavailability of Cysteamine can be decreased when combined with Magnesium silicate.
Aluminium acetoacetate The bioavailability of Cysteamine can be decreased when combined with Aluminium acetoacetate.
Hydrotalcite The bioavailability of Cysteamine can be decreased when combined with Hydrotalcite.
Magnesium peroxide The bioavailability of Cysteamine can be decreased when combined with Magnesium peroxide.
Almasilate The bioavailability of Cysteamine can be decreased when combined with Almasilate.
Aluminium glycinate The bioavailability of Cysteamine can be decreased when combined with Aluminium glycinate.
Aloglutamol The bioavailability of Cysteamine can be decreased when combined with Aloglutamol.
Calcium silicate The bioavailability of Cysteamine can be decreased when combined with Calcium silicate.
Aluminium phosphate The bioavailability of Cysteamine can be decreased when combined with Aluminium phosphate.
Pantoprazole The bioavailability of Cysteamine can be decreased when combined with Pantoprazole.
Omeprazole The bioavailability of Cysteamine can be decreased when combined with Omeprazole.
Lansoprazole The bioavailability of Cysteamine can be decreased when combined with Lansoprazole.
Esomeprazole The bioavailability of Cysteamine can be decreased when combined with Esomeprazole.
Rabeprazole The bioavailability of Cysteamine can be decreased when combined with Rabeprazole.
Dexlansoprazole The bioavailability of Cysteamine can be decreased when combined with Dexlansoprazole.
Dexrabeprazole The bioavailability of Cysteamine can be decreased when combined with Dexrabeprazole.
Sodium zirconium cyclosilicate The bioavailability of Cysteamine can be decreased when combined with Sodium zirconium cyclosilicate.
Vonoprazan The bioavailability of Cysteamine can be decreased when combined with Vonoprazan.
Olanzapine Olanzapine can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Cimetidine The bioavailability of Cysteamine can be decreased when combined with Cimetidine.
Nizatidine The bioavailability of Cysteamine can be decreased when combined with Nizatidine.
Ranitidine The bioavailability of Cysteamine can be decreased when combined with Ranitidine.
Famotidine The bioavailability of Cysteamine can be decreased when combined with Famotidine.
Methantheline The bioavailability of Cysteamine can be decreased when combined with Methantheline.
Promethazine Promethazine can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Doxepin Doxepin can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Asenapine Asenapine can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Metiamide The bioavailability of Cysteamine can be decreased when combined with Metiamide.
Roxatidine acetate The bioavailability of Cysteamine can be decreased when combined with Roxatidine acetate.
Lafutidine The bioavailability of Cysteamine can be decreased when combined with Lafutidine.
Lavoltidine The bioavailability of Cysteamine can be decreased when combined with Lavoltidine.
Niperotidine The bioavailability of Cysteamine can be decreased when combined with Niperotidine.
Epinastine Epinastine can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Ethanol The risk or severity of adverse effects can be increased when Ethanol is combined with Cysteamine.
Tegoprazan The bioavailability of Cysteamine can be decreased when combined with Tegoprazan.

Target Protein

Somatostatin SST
Cystine
Neuropeptide Y receptor type 2 NPY2R

Referensi & Sumber

Synthesis reference: Tethuharu Okazaki, Takeo Komukai, Saburo Uchikuga, "Process for preparing cysteamine-S-substituted compounds and derivatives thereof." U.S. Patent US4371472, issued September, 1969.
Artikel (PubMed)
  • PMID: 19775699
    Dohil R, Fidler M, Gangoiti JA, Kaskel F, Schneider JA, Barshop BA: Twice-daily cysteamine bitartrate therapy for children with cystinosis. J Pediatr. 2010 Jan;156(1):71-75.e1-3. doi: 10.1016/j.jpeds.2009.07.016. Epub .
  • PMID: 27102039
    Elmonem MA, Veys KR, Soliman NA, van Dyck M, van den Heuvel LP, Levtchenko E: Cystinosis: a review. Orphanet J Rare Dis. 2016 Apr 22;11:47. doi: 10.1186/s13023-016-0426-y.
  • PMID: 23416144
    Besouw M, Masereeuw R, van den Heuvel L, Levtchenko E: Cysteamine: an old drug with new potential. Drug Discov Today. 2013 Aug;18(15-16):785-92. doi: 10.1016/j.drudis.2013.02.003. Epub 2013 Feb 14.
  • PMID: 22205430
    Cherqui S: Cysteamine therapy: a treatment for cystinosis, not a cure. Kidney Int. 2012 Jan;81(2):127-9. doi: 10.1038/ki.2011.301.
  • PMID: 20716238
    Gangoiti JA, Fidler M, Cabrera BL, Schneider JA, Barshop BA, Dohil R: Pharmacokinetics of enteric-coated cysteamine bitartrate in healthy adults: a pilot study. Br J Clin Pharmacol. 2010 Sep;70(3):376-82. doi: 10.1111/j.1365-2125.2010.03721.x.
  • PMID: 27153825
    Devereux G, Steele S, Griffiths K, Devlin E, Fraser-Pitt D, Cotton S, Norrie J, Chrystyn H, O'Neil D: An Open-Label Investigation of the Pharmacokinetics and Tolerability of Oral Cysteamine in Adults with Cystic Fibrosis. Clin Drug Investig. 2016 Aug;36(8):605-12. doi: 10.1007/s40261-016-0405-z.
  • PMID: 22554716
    Langman CB, Greenbaum LA, Sarwal M, Grimm P, Niaudet P, Deschenes G, Cornelissen E, Morin D, Cochat P, Matossian D, Gaillard S, Bagger MJ, Rioux P: A randomized controlled crossover trial with delayed-release cysteamine bitartrate in nephropathic cystinosis: effectiveness on white blood cell cystine levels and comparison of safety. Clin J Am Soc Nephrol. 2012 Jul;7(7):1112-20. doi: 10.2215/CJN.12321211. Epub 2012 May 3.
  • PMID: 23113697
    Dohil R, Cabrera BL, Gangoiti JA, Barshop BA, Rioux P: Pharmacokinetics of cysteamine bitartrate following intraduodenal delivery. Fundam Clin Pharmacol. 2014 Apr;28(2):136-43. doi: 10.1111/fcp.12009. Epub 2012 Oct 31.

Contoh Produk & Brand

Produk: 23 • International brands: 3
Produk
  • Cystadrops
    Solution • 3.5 mg/1mL • Ophthalmic • US • Approved
  • Cystadrops
    Solution • 0.37 % w/w • Ophthalmic • Canada • Approved
  • Cystadrops
    Solution / drops • 3.8 mg/ml • Ophthalmic • EU • Approved
  • Cystadrops
    Solution / drops • 3.8 mg/ml • Ophthalmic • EU • Approved
  • Cystagon
    Capsule • 50 mg/1 • Oral • US • Approved
  • Cystagon
    Capsule • 150 mg/1 • Oral • US • Approved
  • Cystagon
    Capsule • 50 mg • Oral • EU • Approved
  • Cystagon
    Capsule • 50 mg • Oral • EU • Approved
Menampilkan 8 dari 23 produk.
International Brands
  • Cystagon
  • Cystaran
  • Procysbi

Sekuens Gen/Protein (FASTA)

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