Peringatan Keamanan

The oral LD50 of colchicine in mice is 5.87 mg/kg.L8189

Acute overdose exceeding 0.5 mg/kg (35 mg for a 70 kg average adult) is usually fatal. Fatalities have been reported with as little as 7 mg.L47591 Colchicine poisoning presents in three sequential and usually overlapping phases. The first stage of acute colchicine toxicity typically occurs within 24 hours of ingestion and includes gastrointestinal symptoms such as abdominal pain, nausea, vomiting, diarrhea, and significant fluid loss, leading to volume depletion. Peripheral leukocytosis may also be seen. The second stage develops 24 to 72 hours after ingestion and is characterized by multi-organ failure. Death is usually a result of respiratory depression and cardiovascular collapse. Recovery may be accompanied by rebound leukocytosis about one week after ingestion.L8138,L47591

No specific antidote is known. Elimination of toxins by gastric lavage followed by activated charcoal should be attempted within 1-2 hours of ingestion. Colchicine is not effectively removed by hemodialysis.L8138,L47591

Colchicine

DB01394

small molecule approved

Deskripsi

Colchicine is an alkaloid drug derived from a plant belonging to the Lily family, known as Colchicum autumnale, or "autumn crocus."A183611 Its use was first approved by the FDA in 1961.L8192 Colchicine is used in the treatment of gout flares and Familial Mediterranean fever,L8138 and prevention of major cardiovascular events.L47591 It has also been investigated in other inflammatory and fibrotic conditions.A183602

Struktur Molekul 2D

Berat 399.443
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After several doses of 0.6 mg twice daily, the average elimination half-life of colchicine ranges from 26.6 to 31.2 hours.[L8138] Another study reported the elimination half-life ranging to be 20 to 40 hours.[A183608]
Volume Distribusi The mean apparent volume of distribution in young and healthy patients is about 5-8 L/kg. It is known to cross the placenta and distribute into the breast milk.[L8138] Colchicine has been found to distribute to various tissues, mainly into the bile, liver, and kidney tissues. Smaller amounts have been detected in the heart, lungs, intestinal tissue, and stomach.[L8192]
Klirens (Clearance) In one pharmacokinetic study involving patients who received a single oral dose of 0.6 mg colchicine, the clearance was 0.0321 ± 0.0091 mL/min in young, healthy adults and 0.0292 ± 0.0071 mL/min in adults between the ages of 60 and 70 years. Patients with end-stage renal impairment showed a 75% lower clearance of colchicine.[L8138] In a pharmacokinetic study of patients with Familial Mediterranean Fever (FMF), the apparent mean clearance was calculated at 0.726 ± 0.110 L/h/kg.[A183953]

Absorpsi

Colchicine is rapidly absorbed after oral administration from the gastrointestinal tract.L8138 The bioavailability of colchicine is about 45%:L8138,L47591 one study suggests that colchicine bioavailability is highly variable, ranging from 24 to 88%.A183608 In healthy adults, the mean Cmax of 2.5 ng/mL (range 1.1 to 4.4 ng/mL) was achieved in one to two hours (range 0.5 to 3 hours) after a single dose administered under fasting conditions.L8138 In a multiple-dose study of colchicine administration at a dose of 1 mg per day, steady-state concentrations were achieved by day 8 following administration.A183608 Administration of colchicine with food does not affect the colchicine absorption rate but decreases the extent of colchicine by approximately 15%.L8138

Metabolisme

Colchicine is metabolized in the liver. It undergoes CYP3A4-mediated demethylation into major metabolites, 2-O-demethylcolchicine and 3-O-demethylcolchicine. It also forms one minor metabolite, 10-O-demethylcolchicine (colchiceine).L8138,L8192 Plasma levels of these metabolites are less than 5% of parent drug.L47591

Rute Eliminasi

In a pharmacokinetic study of healthy research subjects who received 1 mg of oral colchicine, about 40% to 65% of the dose was recovered in the urine in the form of an unchanged drug. Colchicine undergoes enterohepatic recirculation and biliary excretion.A11504,L8138

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1144 Data
Carfilzomib The serum concentration of Colchicine can be increased when it is combined with Carfilzomib.
Voclosporin The serum concentration of Colchicine can be increased when it is combined with Voclosporin.
Sildenafil The serum concentration of Colchicine can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Colchicine can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Colchicine can be increased when it is combined with Loxapine.
Toremifene The serum concentration of Colchicine can be increased when it is combined with Toremifene.
Zonisamide The serum concentration of Colchicine can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Colchicine can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Colchicine can be increased when it is combined with Propafenone.
Paliperidone The serum concentration of Colchicine can be increased when it is combined with Paliperidone.
Biricodar The serum concentration of Colchicine can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Colchicine can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Colchicine can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Colchicine can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Colchicine can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Colchicine can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Colchicine can be increased when it is combined with Temsirolimus.
Mirabegron The serum concentration of Colchicine can be increased when it is combined with Mirabegron.
Enzalutamide The serum concentration of Colchicine can be decreased when it is combined with Enzalutamide.
Ponatinib The serum concentration of Colchicine can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Colchicine can be increased when it is combined with Canagliflozin.
Vorapaxar The serum concentration of Colchicine can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Colchicine can be increased when it is combined with Suvorexant.
Daclatasvir The serum concentration of Colchicine can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Colchicine can be increased when it is combined with Niguldipine.
Lumacaftor The serum concentration of Colchicine can be increased when it is combined with Lumacaftor.
Rolapitant The serum concentration of Colchicine can be increased when it is combined with Rolapitant.
Asunaprevir The serum concentration of Colchicine can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Colchicine can be increased when it is combined with Velpatasvir.
Neratinib The serum concentration of Colchicine can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Colchicine can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Colchicine can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Colchicine can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Colchicine can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Colchicine can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Colchicine can be increased when it is combined with Laniquidar.
Pibrentasvir The serum concentration of Colchicine can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Colchicine can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Colchicine can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Colchicine can be increased when it is combined with ONT-093.
Ivosidenib The metabolism of Colchicine can be increased when combined with Ivosidenib.
Ledipasvir The serum concentration of Colchicine can be increased when it is combined with Ledipasvir.
Erdafitinib The serum concentration of Colchicine can be increased when it is combined with Erdafitinib.
Methylene blue The serum concentration of Colchicine can be increased when it is combined with Methylene blue.
Vardenafil The serum concentration of Colchicine can be increased when it is combined with Vardenafil.
Fedratinib The serum concentration of Colchicine can be increased when it is combined with Fedratinib.
Afatinib The serum concentration of Colchicine can be increased when it is combined with Afatinib.
Istradefylline The serum concentration of Colchicine can be increased when it is combined with Istradefylline.
Elagolix The serum concentration of Colchicine can be increased when it is combined with Elagolix.
Arsenic trioxide The serum concentration of Colchicine can be increased when it is combined with Arsenic trioxide.
Lasmiditan The serum concentration of Colchicine can be increased when it is combined with Lasmiditan.
Norgestimate The serum concentration of Colchicine can be increased when it is combined with Norgestimate.
Favipiravir The serum concentration of Colchicine can be increased when it is combined with Favipiravir.
Ixabepilone The serum concentration of Colchicine can be increased when it is combined with Ixabepilone.
Ripretinib The serum concentration of Colchicine can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Colchicine can be increased when it is combined with Pralsetinib.
Lonafarnib The serum concentration of Colchicine can be increased when it is combined with Lonafarnib.
Entrectinib The serum concentration of Colchicine can be increased when it is combined with Entrectinib.
Tepotinib The serum concentration of Colchicine can be increased when it is combined with Tepotinib.
Umbralisib The serum concentration of Colchicine can be increased when it is combined with Umbralisib.
Cyclosporine The serum concentration of Colchicine can be increased when it is combined with Cyclosporine.
Ranolazine The serum concentration of Colchicine can be increased when it is combined with Ranolazine.
Diosmin The serum concentration of Colchicine can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Colchicine can be increased when it is combined with Sapropterin.
Capmatinib The serum concentration of Colchicine can be increased when it is combined with Capmatinib.
Belumosudil The serum concentration of Colchicine can be increased when it is combined with Belumosudil.
Cyanocobalamin The therapeutic efficacy of Cyanocobalamin can be decreased when used in combination with Colchicine.
Choline C 11 The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Colchicine.
Pravastatin Colchicine may increase the myopathic rhabdomyolysis activities of Pravastatin.
Mevastatin Colchicine may increase the myopathic rhabdomyolysis activities of Mevastatin.
Pitavastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Colchicine is combined with Pitavastatin.
Rosuvastatin Colchicine may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
Eliglustat The serum concentration of Colchicine can be increased when it is combined with Eliglustat.
Cilostazol Cilostazol may decrease the excretion rate of Colchicine which could result in a higher serum level.
Clozapine The metabolism of Colchicine can be decreased when combined with Clozapine.
Viloxazine The metabolism of Colchicine can be decreased when combined with Viloxazine.
Aldesleukin The metabolism of Colchicine can be decreased when combined with Aldesleukin.
Octreotide The metabolism of Colchicine can be decreased when combined with Octreotide.
Fluvoxamine The metabolism of Colchicine can be decreased when combined with Fluvoxamine.
Fluconazole The serum concentration of Colchicine can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Colchicine can be increased when it is combined with Erythromycin.
Citalopram The metabolism of Colchicine can be decreased when combined with Citalopram.
Lovastatin Colchicine may increase the myopathic rhabdomyolysis activities of Lovastatin.
Ziprasidone The metabolism of Colchicine can be decreased when combined with Ziprasidone.
Cabergoline The metabolism of Colchicine can be decreased when combined with Cabergoline.
Diethylstilbestrol The metabolism of Colchicine can be decreased when combined with Diethylstilbestrol.
Isradipine The metabolism of Colchicine can be decreased when combined with Isradipine.
Valproic acid The metabolism of Colchicine can be decreased when combined with Valproic acid.
Acetaminophen The metabolism of Colchicine can be decreased when combined with Acetaminophen.
Dihydroergotamine The metabolism of Colchicine can be decreased when combined with Dihydroergotamine.
Methadone The metabolism of Colchicine can be decreased when combined with Methadone.
Terfenadine The metabolism of Colchicine can be decreased when combined with Terfenadine.
Diltiazem The metabolism of Colchicine can be decreased when combined with Diltiazem.
Methylergometrine The metabolism of Colchicine can be decreased when combined with Methylergometrine.
Mefloquine The serum concentration of Colchicine can be increased when it is combined with Mefloquine.
Mirtazapine The metabolism of Colchicine can be decreased when combined with Mirtazapine.
Sorafenib The serum concentration of Colchicine can be increased when it is combined with Sorafenib.
Nitric Oxide The metabolism of Colchicine can be decreased when combined with Nitric Oxide.
Cerivastatin Colchicine may increase the myopathic rhabdomyolysis activities of Cerivastatin.
Teniposide The metabolism of Colchicine can be decreased when combined with Teniposide.

Target Protein

Tubulin beta chain TUBB

Referensi & Sumber

Synthesis reference: Christian Wehrey, "Colchicine derivatives, process for preparing them, products obtained therefrom and use thereof." U.S. Patent US20040138182, issued July 15, 2004.
Artikel (PubMed)
  • PMID: 26228647
    Leung YY, Yao Hui LL, Kraus VB: Colchicine--Update on mechanisms of action and therapeutic uses. Semin Arthritis Rheum. 2015 Dec;45(3):341-50. doi: 10.1016/j.semarthrit.2015.06.013. Epub 2015 Jun 26.
  • PMID: 25151572
    Dalbeth N, Lauterio TJ, Wolfe HR: Mechanism of action of colchicine in the treatment of gout. Clin Ther. 2014 Oct 1;36(10):1465-79. doi: 10.1016/j.clinthera.2014.07.017. Epub 2014 Aug 21.
  • PMID: 8525161
    Chappey O, Scherrmann JM: Colchicine: recent data on pharmacokinetics and clinical pharmacology. Rev Med Interne. 1995;16(10):782-9.
  • PMID: 29359661
    Angelidis C, Kotsialou Z, Kossyvakis C, Vrettou AR, Zacharoulis A, Kolokathis F, Kekeris V, Giannopoulos G: Colchicine Pharmacokinetics and Mechanism of Action. Curr Pharm Des. 2018;24(6):659-663. doi: 10.2174/1381612824666180123110042.
  • PMID: 27729672
    Campbell KB, Cicci TA, Vora AK, Burgess LD: Beyond Gout: Colchicine Use in the Cardiovascular Patient. Hosp Pharm. 2015 Nov;50(10):859-867. doi: 10.1310/hpj5010-859. Epub 2015 Nov 19.
  • PMID: 24790727
    Saleh Z, Arayssi T: Update on the therapy of Behcet disease. Ther Adv Chronic Dis. 2014 May;5(3):112-34. doi: 10.1177/2040622314523062.
  • PMID: 20586571
    Finkelstein Y, Aks SE, Hutson JR, Juurlink DN, Nguyen P, Dubnov-Raz G, Pollak U, Koren G, Bentur Y: Colchicine poisoning: the dark side of an ancient drug. Clin Toxicol (Phila). 2010 Jun;48(5):407-14. doi: 10.3109/15563650.2010.495348.
  • PMID: 8035398
    Ben-Chetrit E, Scherrmann JM, Zylber-Katz E, Levy M: Colchicine disposition in patients with familial Mediterranean fever with renal impairment. J Rheumatol. 1994 Apr;21(4):710-3.

Contoh Produk & Brand

Produk: 87 • International brands: 0
Produk
  • Colchicine
    Tablet • 0.6 mg/1 • Oral • US
  • Colchicine
    Tablet • 0.6 mg/1 • Oral • US
  • Colchicine
    Tablet • 0.6 mg/1 • Oral • US
  • Colchicine
    Tablet • 0.6 mg/1 • Oral • US
  • Colchicine
    Tablet, film coated • 0.6 mg/1 • Oral • US • Generic • Approved
  • Colchicine
    Capsule • 0.6 mg/1 • Oral • US • Approved
  • Colchicine
    Tablet, film coated • 0.6 mg/1 • Oral • US • Generic • Approved
  • Colchicine
    Tablet, film coated • 0.6 mg/1 • Oral • US • Generic • Approved
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