Peringatan Keamanan

The reported oral LD50 of clofazimine in rats and mice is 8400 mg/kg and >5000 mg/kg, respectively.L13820

No specific data are available regarding the treatment of clofazimine overdosage.L13802 In cases of overdose consider gastrointestinal decontamination via gastric lavage or induced vomiting. Employ symptomatic and supportive measures as clinically indicated.

Clofazimine

DB00845

small molecule approved investigational

Deskripsi

Clofazimine is a highly lipophilic antimicrobial riminophenazine dye used in combination with other agents, such as dapsone, for the treatment of leprosy. It was originally described in 1957 and was the prototypical riminophenazine dye - a bright-red dye that, in its clinical use, results in long-lasting discoloration of the skin and bodily fluids.A203144 Although it carries in vitro activity against other mycobacterium, such as Mycobacterium tuberculosis, it is generally considered an ineffective treatment in comparison to classic tuberculosis treatments such as rifampicin and isoniazid.A203144

Struktur Molekul 2D

Berat 473.396
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life is approximately 25 days.[L13802]
Volume Distribusi Clofazimine is highly lipophilic and therefore deposits primarily in fatty tissues and cells of the reticuloendothelial system, where it is taken up by macrophages and further distributed throughout the body. Crystalized deposits have been found in the mesenteric lymph nodes, adrenals, subcutaneous fat, liver, bile, gall bladder, spleen, small intestine, muscles, bones, and skin.[L13802]
Klirens (Clearance) -

Absorpsi

Absorption varies from 45 to 62% following oral administration in leprosy patients.L13802 Co-administration of a 200mg dose of clofazimine with food resulted in a Cmax of 0.41 mg/L with a Tmax of 8 h; administered in a fasting state, the corresponding Cmax was 30% lower while the time to Cmax was 12 h.A203213

Metabolisme

Three metabolites have been identified in the urine following repeated oral doses of clofazimine.L13802 It is unclear whether these metabolites are pharmacologically active. Metabolite I may be the result of the hydrolytic dehalogenation of clofazimine and metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation.A203213

Rute Eliminasi

Part of an ingested dose of clofazimine is found in the feces, which may represent excretion in the bile, and a small amount is also eliminated in the sputum, sebum, and sweat.L13802 Excretion of unchanged drug and metabolites in a 24-hour urine collection was negligible.

Interaksi Makanan

1 Data
  • 1. Take with food. Prescribing information for clofazimine recommends its administration with a meal.

Interaksi Obat

744 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Clofazimine.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Clofazimine.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Clofazimine.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Clofazimine.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Clofazimine.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Clofazimine.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Clofazimine.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Clofazimine.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Clofazimine.
Silodosin The excretion of Silodosin can be decreased when combined with Clofazimine.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Clofazimine.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Clofazimine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Clofazimine.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Clofazimine.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Clofazimine.
Porfimer sodium Clofazimine may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Clofazimine may increase the photosensitizing activities of Verteporfin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Clofazimine.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Clofazimine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Clofazimine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Clofazimine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Clofazimine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Clofazimine.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Clofazimine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Clofazimine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Clofazimine.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Clofazimine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Clofazimine.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Clofazimine.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Clofazimine.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Clofazimine.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Clofazimine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Clofazimine.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Clofazimine.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Clofazimine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Clofazimine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Clofazimine.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Clofazimine.
Vincristine The excretion of Vincristine can be decreased when combined with Clofazimine.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Clofazimine.
Leuprolide The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Sulfisoxazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Promazine.
Droperidol The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Clofazimine.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Ciprofloxacin.
Fluorouracil Clofazimine may decrease the excretion rate of Fluorouracil which could result in a higher serum level.
Perflutren The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Atropine.
Efavirenz The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Efavirenz.
Adenosine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Adenosine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Cinoxacin.
Loperamide The excretion of Loperamide can be decreased when combined with Clofazimine.
Granisetron The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Granisetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Papaverine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Flecainide.
Mibefradil The serum concentration of Mibefradil can be increased when it is combined with Clofazimine.
Probucol The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Lofexidine.
Pracinostat The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Nemonoxacin.
Nilvadipine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Antazoline.
Bedaquiline The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Eperisone.
Butriptyline The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Butriptyline.
Lenvatinib Clofazimine may decrease the excretion rate of Lenvatinib which could result in a higher serum level.
Melperone The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Melperone.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Dexchlorpheniramine maleate.
Amifampridine The risk or severity of QTc prolongation can be increased when Clofazimine is combined with Amifampridine.

Target Protein

Peroxisome proliferator-activated receptor gamma PPARG
Potassium voltage-gated channel subfamily A member 3 KCNA3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31371410
    Kumar H, Chattopadhyay S, Das N, Shree S, Patel D, Mohapatra J, Gurjar A, Kushwaha S, Singh AK, Dubey S, Lata K, Kushwaha R, Mohammed R, Dastidar KG, Yadav N, Vishwakarma AL, Gayen JR, Bandyopadhyay S, Chatterjee A, Jain MR, Tripathi AK, Trivedi AK, Chattopadhyay N, Ramachandran R, Sanyal S: Leprosy drug clofazimine activates peroxisome proliferator-activated receptor-gamma and synergizes with imatinib to inhibit chronic myeloid leukemia cells. Haematologica. 2020 Apr;105(4):971-986. doi: 10.3324/haematol.2018.194910. Epub 2019 Aug 1.
  • PMID: 22020137
    Cholo MC, Steel HC, Fourie PB, Germishuizen WA, Anderson R: Clofazimine: current status and future prospects. J Antimicrob Chemother. 2012 Feb;67(2):290-8. doi: 10.1093/jac/dkr444. Epub 2011 Oct 20.
  • PMID: 26682943
    Te Brake LH, Russel FG, van den Heuvel JJ, de Knegt GJ, de Steenwinkel JE, Burger DM, Aarnoutse RE, Koenderink JB: Inhibitory potential of tuberculosis drugs on ATP-binding cassette drug transporters. Tuberculosis (Edinb). 2016 Jan;96:150-7. doi: 10.1016/j.tube.2015.08.004. Epub 2015 Oct 9.
  • PMID: 6120809
    Feng PC, Fenselau CC, Jacobson RR: Metabolism of clofazimine in leprosy patients. Drug Metab Dispos. 1981 Nov-Dec;9(6):521-4.

Contoh Produk & Brand

Produk: 1 • International brands: 5
Produk
  • Lamprene
    Capsule, gelatin coated • 50 mg/1 • Oral • US • Approved
International Brands
  • Clofozine — AstraZeneca
  • Hansepran — Abbott
  • Lamcoin — Pond's Chemical
  • Lampren — Novartis
  • Lamprène — Novartis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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