Peringatan Keamanan

Intravenous LD50 in rats is 125mg/kg. In dogs it is >200mg/kg. No cases of overdosage have been reported. Repeated daily doses up to 8 mg/kg (maximum total dose of 896 mg) in adult patients have been administered in clinical trials with no reported dose-limiting toxicity. The minimum lethal dose is 125 mg/kg in rats, equivalent to 8.1 times the recommended human clinical dose for esophageal candidiasis based on body surface area comparisons.

Micafungin

DB01141

small molecule approved investigational

Deskripsi

Micafungin is an antifungal drug. It belongs to the antifungal class of compounds known as echinocandins and exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall.

Struktur Molekul 2D

Berat 1270.274
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 14-17 hours
Volume Distribusi * 0.39 ± 0.11 L/kg [adult patients with esophageal candidiasis]
Klirens (Clearance) * 0.359 +/- 0.179 mL/min/kg [Adult Patients with IC with 100 mg] * 0.321 +/- 0.098 mL/min/kg [HIV- Positive Patients with EC with 50 mg] * 0.327 +/- 0.093 mL/min/kg [HIV- Positive Patients with EC with 100 mg] * 0.340 +/- 0.092 mL/min/kg [HIV- Positive Patients with EC with 150 mg] * 0.214 +/- 0.031 mL/min/kg [hematopoietic stem cell transplant recipients 3 mg/kg] * 0.204 +/- 0.036 mL/min/kg [hematopoietic stem cell transplant recipients 4 mg/kg] * 0.224 +/- 0.064 mL/min/kg [hematopoietic stem cell transplant recipients 6 mg/kg] * 0.223 +/- 0.081 mL/min/kg [hematopoietic stem cell transplant recipients 8 mg/kg]

Absorpsi

Not absorbed orally

Metabolisme

Micafungin is metabolized to M-1 (catechol form) by arylsulfatase, with further metabolism to M-2 (methoxy form) by catechol-O-methyltransferase. M-5 is formed by hydroxylation at the side chain (w-1 position) of micafungin catalyzed by cytochrome P450 (CYP) isozymes. Even though micafungin is a substrate for and a weak inhibitor of CYP3A in vitro, hydroxylation by CYP3A is not a major pathway for micafungin metabolism in vivo.

Rute Eliminasi

Fecal excretion is the major route of elimination (total radioactivity at 28 days was 71% of the administered dose).

Interaksi Obat

22 Data
Tolcapone The metabolism of Micafungin can be decreased when combined with Tolcapone.
Entacapone The metabolism of Micafungin can be decreased when combined with Entacapone.
Testosterone propionate The metabolism of Micafungin can be decreased when combined with Testosterone propionate.
3,5-Dinitrocatechol The metabolism of Micafungin can be decreased when combined with 3,5-Dinitrocatechol.
Quercetin The metabolism of Micafungin can be decreased when combined with Quercetin.
Sirolimus The metabolism of Sirolimus can be decreased when combined with Micafungin.
Temsirolimus The metabolism of Temsirolimus can be decreased when combined with Micafungin.
Dicoumarol The therapeutic efficacy of Dicoumarol can be increased when used in combination with Micafungin.
Phenindione The therapeutic efficacy of Phenindione can be increased when used in combination with Micafungin.
Warfarin The therapeutic efficacy of Warfarin can be increased when used in combination with Micafungin.
Phenprocoumon The therapeutic efficacy of Phenprocoumon can be increased when used in combination with Micafungin.
Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Micafungin.
4-hydroxycoumarin The therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Micafungin.
Coumarin The therapeutic efficacy of Coumarin can be increased when used in combination with Micafungin.
(R)-warfarin The therapeutic efficacy of (R)-warfarin can be increased when used in combination with Micafungin.
Ethyl biscoumacetate The therapeutic efficacy of Ethyl biscoumacetate can be increased when used in combination with Micafungin.
Fluindione The therapeutic efficacy of Fluindione can be increased when used in combination with Micafungin.
Clorindione The therapeutic efficacy of Clorindione can be increased when used in combination with Micafungin.
Diphenadione The therapeutic efficacy of Diphenadione can be increased when used in combination with Micafungin.
Tioclomarol The therapeutic efficacy of Tioclomarol can be increased when used in combination with Micafungin.
(S)-Warfarin The therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Micafungin.
Opicapone The metabolism of Micafungin can be decreased when combined with Opicapone.

Target Protein

1,3-beta-glucan synthase component FKS1 fksA
1,3-beta-glucan synthase component GSC2 GSC2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20606829
    Grover ND: Echinocandins: A ray of hope in antifungal drug therapy. Indian J Pharmacol. 2010 Feb;42(1):9-11. doi: 10.4103/0253-7613.62396.
  • PMID: 20054447
    Bormann AM, Morrison VA: Review of the pharmacology and clinical studies of micafungin. Drug Des Devel Ther. 2009 Dec 29;3:295-302.
  • PMID: 17661660
    Vehreschild JJ, Cornely OA: Micafungin sodium, the second of the echinocandin class of antifungals: theory and practice. Future Microbiol. 2006 Aug;1(2):161-70.
  • PMID: 15882123
    Groll AH, Stergiopoulou T, Roilides E, Walsh TJ: Micafungin: pharmacology, experimental therapeutics and clinical applications. Expert Opin Investig Drugs. 2005 Apr;14(4):489-509.
  • PMID: 16575738
    Chandrasekar PH, Sobel JD: Micafungin: a new echinocandin. Clin Infect Dis. 2006 Apr 15;42(8):1171-8. Epub 2006 Mar 14.
  • PMID: 17516879
    Wiederhold NP, Lewis JS 2nd: The echinocandin micafungin: a review of the pharmacology, spectrum of activity, clinical efficacy and safety. Expert Opin Pharmacother. 2007 Jun;8(8):1155-66.
  • PMID: 17504145
    Ikeda F, Tanaka S, Ohki H, Matsumoto S, Maki K, Katashima M, Barrett D, Aoki Y: Role of micafungin in the antifungal armamentarium. Curr Med Chem. 2007;14(11):1263-75.
  • PMID: 19724014
    Sucher AJ, Chahine EB, Balcer HE: Echinocandins: the newest class of antifungals. Ann Pharmacother. 2009 Oct;43(10):1647-57. doi: 10.1345/aph.1M237. Epub 2009 Sep 1.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 38 • International brands: 0
Produk
  • Micafungin
    Injection, powder, lyophilized, for solution • 50 mg/1 • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 100 mg/1 • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 10 mg/1mL • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 20 mg/1mL • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 10 mg/1mL • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 20 mg/1mL • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 50 mg/5mL • Intravenous • US • Generic • Approved
  • Micafungin
    Injection, powder, lyophilized, for solution • 100 mg/5mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 38 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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