Peringatan Keamanan

In rats, the LD50 of fidaxomicin was approximately 200 mg/kg and the no observed adverse effect level (NOAEL) was determined to be 62.5 mg/kg following administration of a single intravenous dose.A190489

There is limited clinical data on acute overdose in humans.L11575

Fidaxomicin

DB08874

small molecule approved

Deskripsi

Fidaxomicin is a novel macrolide antibiotic used in the treatment of diarrhea caused by Clostridioides (formerly Clostridium) difficile in adult and pediatric patients over the age of 6 months.L11575 Fidaxomicin is a naturally-occurring 18-member macrocycle derived from fermentation.A190501 Because fidaxomicin contains an 18-membered lactone ring in its structure, it is referred to as a macrocyclic lactone antibiotic drug.A190492 The antibacterial activity of fidaxomicin is distinct from macrolides and rifamycins, as the bactericidal activity is time-dependent, and not concentration-dependent.A190492 Fidaxomicin was the first macrocyclic lactone antibiotic with activity against C. difficile,A190486 and it displays a narrow spectrum of activity against gram-positive anaerobes.A7445 It mediates its potent bactericidal action on the bacteria by inhibiting the bacterial RNA synthase, thereby disrupting bacterial transcription.A190486 The minimum inhibitory concentration (MIC90) for fidaxomicin is four times less than that of vancomycin, which was the primary drug of choice for C. difficile infection before the approval of fidaxomicin.A190492 Unlike vancomycin, however, fidaxomicin has a negligible effect on normal colonic microflora.A190516

The FDA initially approved fidaxomicin in May 2011 for the treatment of C. difficile-associated diarrhea in adult patients over the age of 18.A190492 Later that year in December, the drug was also approved by the European Medicine Agency.A190492 In June 2012, fidaxomicin was also granted approval by Health Canada.A190486 The approved indication of fidaxomicin was expanded by the FDA in January 2020 to include pediatric patients over the age of 6 months in the treatment population.L11575

Struktur Molekul 2D

Berat 1058.05
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration of a single dose of 200 mg fidaxomicin in healthy adults, the elimination half-life of fidaxomicin was approximately 11.7 ± 4.80 hours.[L11575]
Volume Distribusi Fidaxomicin is mainly confined to the gastrointestinal tract when orally administered.[L11575] There is limited information on the volume of distribution of fidaxomicin.
Klirens (Clearance) There is limited information on the clearance of fidaxomicin.

Absorpsi

Following oral administration of a single dose of 200 mg fidaxomicin in healthy adults, the Cmax of fidaxomicin and its main metabolite OP-1118 were 5.20 ± 2.81 ng/mL and 12.0 ± 6.06, respectively. The median Tmax of fidaxomicin was 2 hours. The systemic absorption of fidaxomicin following oral administration is minimal.L11575 In a food-effect study involving healthy adults in either with a high-fat meal versus under fasting conditions, the Cmax of fidaxomicin and OP-1118 were decreased by 21.5% and 33.4%, respectively; however, this effect is deemed to be clinically insignificant as the therapeutic action of fidaxomicin does not depend on drug concentrations in the systemic circulation.L11575

Metabolisme

Following oral administration, fidaxomicin is transformed to its main and pharmacologically active metabolite, OP-1118, via hydrolysis at the isobutyryl ester. As cytochrome enzymes are not involved in the metabolism of fidaxomicin, it is speculated that this biotransformation is mediated by gastric acid or enzymatic activity of intestinal microsomes.A190492,L11575

Rute Eliminasi

Following oral administration, fidaxomicin is mainly excreted in feces. More than 92% of the dose was recovered in the faces as either the unchanged parent drug or metabolites in one study consisting of healthy adults receiving single doses of 200 mg and 300 mg of fidaxomicin. In another study of healthy adults, approximately 0.59% fo the oral dose (200 mg) administered was recovered in the urine as the main metabolite, OP-1118.L11575

Interaksi Makanan

1 Data
  • 1. Take with or without food. High-fat meal decreases the Cmax of fidaxomicin and its metabolite in a clinically insignificant way.

Interaksi Obat

55 Data
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Fidaxomicin.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Fidaxomicin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Fidaxomicin.
Dicoumarol The risk or severity of bleeding can be increased when Fidaxomicin is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Fidaxomicin is combined with Phenindione.
Coumarin The risk or severity of bleeding can be increased when Fidaxomicin is combined with Coumarin.
Tioclomarol The risk or severity of bleeding can be increased when Fidaxomicin is combined with Tioclomarol.
Warfarin The risk or severity of bleeding can be increased when Fidaxomicin is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Fidaxomicin is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Fidaxomicin is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Fidaxomicin is combined with 4-hydroxycoumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Fidaxomicin is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Fidaxomicin is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Fidaxomicin is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Fidaxomicin is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Fidaxomicin is combined with Diphenadione.
(S)-Warfarin The risk or severity of bleeding can be increased when Fidaxomicin is combined with (S)-Warfarin.
Lactulose The therapeutic efficacy of Lactulose can be decreased when used in combination with Fidaxomicin.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Fidaxomicin.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Fidaxomicin.
Lidocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Quinisocaine.
Cisatracurium Fidaxomicin may increase the neuromuscular blocking activities of Cisatracurium.
Ambroxol The risk or severity of methemoglobinemia can be increased when Fidaxomicin is combined with Ambroxol.
Fecal microbiota The therapeutic efficacy of Fecal microbiota can be decreased when used in combination with Fidaxomicin.

Target Protein

RNA polymerase sigma factor SigA sigA1

Referensi & Sumber

Synthesis reference: Youe-Kong Shue, Chi-Jen Frank Du, Ming-Hsi Chiou, Mei-Chiao Wu, Yuan-Ting Chen, Franklin W. Okumu, Jonathan James Duffield, "Medium for the Production of Tiacumicin B." U.S. Patent US20100028970, issued February 04, 2010.
Artikel (PubMed)
  • PMID: 22752861
    Artsimovitch I, Seddon J, Sears P: Fidaxomicin is an inhibitor of the initiation of bacterial RNA synthesis. Clin Infect Dis. 2012 Aug;55 Suppl 2:S127-31. doi: 10.1093/cid/cis358.
  • PMID: 22610025
    Crawford T, Huesgen E, Danziger L: Fidaxomicin: a novel macrocyclic antibiotic for the treatment of Clostridium difficile infection. Am J Health Syst Pharm. 2012 Jun 1;69(11):933-43. doi: 10.2146/ajhp110371.
  • PMID: 20509714
    Authors unspecified: Fidaxomicin: Difimicin; Lipiarmycin; OPT 80; OPT-80; PAR 101; PAR-101. Drugs R D. 2010;10(1):37-45. doi: 10.2165/11537730-000000000-00000.
  • PMID: 26744587
    Zhanel GG, Walkty AJ, Karlowsky JA: Fidaxomicin: A novel agent for the treatment of Clostridium difficile infection. Can J Infect Dis Med Microbiol. 2015 Nov-Dec;26(6):305-12. doi: 10.1155/2015/934594.
  • PMID: 22752858
    Weiss K, Allgren RL, Sellers S: Safety analysis of fidaxomicin in comparison with oral vancomycin for Clostridium difficile infections. Clin Infect Dis. 2012 Aug;55 Suppl 2:S110-5. doi: 10.1093/cid/cis390.
  • PMID: 26112840
    Vaishnavi C: Fidaxomicin--the new drug for Clostridium difficile infection. Indian J Med Res. 2015 Apr;141(4):398-407. doi: 10.4103/0971-5916.159251.
  • PMID: 22752862
    Louie TJ, Cannon K, Byrne B, Emery J, Ward L, Eyben M, Krulicki W: Fidaxomicin preserves the intestinal microbiome during and after treatment of Clostridium difficile infection (CDI) and reduces both toxin reexpression and recurrence of CDI. Clin Infect Dis. 2012 Aug;55 Suppl 2:S132-42. doi: 10.1093/cid/cis338.
  • PMID: 18268081
    Shue YK, Sears PS, Shangle S, Walsh RB, Lee C, Gorbach SL, Okumu F, Preston RA: Safety, tolerance, and pharmacokinetic studies of OPT-80 in healthy volunteers following single and multiple oral doses. Antimicrob Agents Chemother. 2008 Apr;52(4):1391-5. doi: 10.1128/AAC.01045-07. Epub 2008 Feb 11.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
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    Tablet, film coated • 200 mg/1 • Oral • US • Approved
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    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Dificid
    Tablet • 200 mg • Oral • Canada • Approved
  • Dificlir
    Tablet, film coated • 200 mg • Oral • EU • Approved
  • Dificlir
    Tablet, film coated • 200 mg • Oral • EU • Approved
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    Tablet, film coated • 200 mg • Oral • EU • Approved
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    Tablet, film coated • 200 mg • Oral • EU • Approved
Menampilkan 8 dari 9 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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