Peringatan Keamanan

There is limited information in the literature regarding overdose with nifurtimox. Some symptoms of nifurtimox toxicity may include weight loss, anorexia, nausea, vomiting, vertigo, headache, nervous excitation, insomnia, convulsions, drowsiness, arthralgias, myalgias, disorientation, abdominal pain, mucosal edema, and skin manifestations. These symptoms are adverse effects of nifurtimox and are likely to be exaggerated with increased exposure.A217891

Nifurtimox

DB11820

small molecule approved investigational

Deskripsi

Chagas disease, caused by a parasite known as Trypanosoma cruzi (T.cruzi), is a vector-transmitted disease affecting animals and humans in the Americas. It is commonly known as American Trypanosomiasis.L15366

The CDC estimates that approximately 8 million people in Central America, South America, and Mexico are infected with T. cruzi, without symptoms. If Chagas disease is left untreated, life-threatening sequelae may result.L15366

Nifurtimox, developed by Bayer, is a nitrofuran antiprotozoal drug used in the treatment of Chagas disease. On August 6 2020, accelerated FDA approval was granted for its use in pediatric patients in response to promising results from phase III clinical trials. Continued approval will be contingent upon confirmatory data.L15361 A convenient feature of Bayer's formulation is the ability to divide the scored tablets manually without the need for pill-cutting devices.L15361

Struktur Molekul 2D

Berat 287.29
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of nifurtimox ranges from 2.4–3.6 hours.[L15361] A pharmacokinetic study of healthy volunteers and patients with renal failure revealed respective mean half-lives of 2.95 h and 3.95 h.[A217936]
Volume Distribusi Nifurtimox crosses the blood-brain barrier and the placenta.[A216931,L15361]
Klirens (Clearance) One pharmacokinetic study of nifurtimox revealed a clearance of 193.4 l?h<sup>-1</sup>. In patients without renal failure; clearance was 99.7 l?h<sup>-1</sup>.[A217936]

Absorpsi

The average AUC of nifurtimox is estimated between 1676-2670 ?g?h/L.L15361 One pharmacokinetic study of healthy volunteers revealed an AUC of 5430 ng?ml-1?h.A217936 Cmax ranges between 425-568 ?g/L (26–50%) after a single dose of 20 mg with food in adults. Tmax is 4 hours, ranging from 2 to 8 hours post-dose in the fed state.A217936,L15361 In a pharmacokinetic study of healthy volunteers, serum concentration was low, likely due to the first-pass effect.A216926

Metabolisme

Nifurtimox is largely metabolized via nitroreductase enzymes. Two major inactive metabolites have been identified: M-4 and M-6. The M-4 metabolite is a cysteine conjugate of nifurtimox, while M-6 is likely formed by hydrolytic cleavage of the hydrazone moiety of nifurtimox. Other minor metabolites have also been identified in human plasma.A217986,L15361

Rute Eliminasi

In the fed state, 44% of the dose was mainly recovered in the urine as metabolites. Fecal and biliary excretion of nifurtimox have not been studied.L15361

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol use during nifurtimox treatment may increase undesirable adverse effects.
  • 2. Take with food.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Nitroreductases
Glyceraldehyde-3-phosphate dehydrogenase, glycosomal

Referensi & Sumber

Synthesis reference: Danong Chen, Glenn Rice. 2013. Novel formulations of nitrofurans including nifurtimox with enhanced activity with lower toxicity.US20150140089A1
Artikel (PubMed)
  • PMID: 2807618
    Paulos C, Paredes J, Vasquez I, Thambo S, Arancibia A, Gonzalez-Martin G: Pharmacokinetics of a nitrofuran compound, nifurtimox, in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1989 Sep;27(9):454-7.
  • PMID: 21057057
    Jeganathan S, Sanderson L, Dogruel M, Rodgers J, Croft S, Thomas SA: The distribution of nifurtimox across the healthy and trypanosome-infected murine blood-brain and blood-cerebrospinal fluid barriers. J Pharmacol Exp Ther. 2011 Feb;336(2):506-15. doi: 10.1124/jpet.110.172981. Epub 2010 Nov 5.
  • PMID: 27432838
    Forsyth CJ, Hernandez S, Olmedo W, Abuhamidah A, Traina MI, Sanchez DR, Soverow J, Meymandi SK: Safety Profile of Nifurtimox for Treatment of Chagas Disease in the United States. Clin Infect Dis. 2016 Oct 15;63(8):1056-1062. doi: 10.1093/cid/ciw477. Epub 2016 Jul 17.
  • PMID: 20178775
    Boiani M, Piacenza L, Hernandez P, Boiani L, Cerecetto H, Gonzalez M, Denicola A: Mode of action of nifurtimox and N-oxide-containing heterocycles against Trypanosoma cruzi: is oxidative stress involved? Biochem Pharmacol. 2010 Jun 15;79(12):1736-45. doi: 10.1016/j.bcp.2010.02.009. Epub 2010 Feb 21.
  • PMID: 21861617
    Cerecetto H, Gonzalez M: Antiparasitic prodrug nifurtimox: revisiting its activation mechanism. Future Microbiol. 2011 Aug;6(8):847-50. doi: 10.2217/fmb.11.74.
  • PMID: -
    Belinda S. Hall, Shane R. Wilkinson: Activation of Benznidazole by Trypanosomal Type I Nitroreductases Results in Glyoxal Formation Antimicrobial agents and chemotherapy.
  • PMID: 3151755
    Castro JA, Diaz de Toranzo EG: Toxic effects of nifurtimox and benznidazole, two drugs used against American trypanosomiasis (Chagas' disease). Biomed Environ Sci. 1988 Jun;1(1):19-33.
  • PMID: 1623911
    Gonzalez-Martin G, Thambo S, Paulos C, Vasquez I, Paredes J: The pharmacokinetics of nifurtimox in chronic renal failure. Eur J Clin Pharmacol. 1992;42(6):671-3. doi: 10.1007/BF00265935.
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Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Lampit
    Tablet, film coated • 30 mg/1 • Oral • US • Approved
  • Lampit
    Tablet, film coated • 120 mg/1 • Oral • US • Approved
International Brands
  • Lampit — Bayer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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