Peringatan Keamanan

Data on nitazoxanide overdosage is not available FDA label. In studies in rodents and dogs, the oral LD50 was higher than 10,000 mg/kg. One-time oral doses of up to 4000 mg nitazoxanide have been given to healthy adult volunteers without severe adverse effects. Gastric lavage may be appropriate soon after oral administration if overdose occurs. Supportive and symptomatic treatment should also be administered FDA label.

According to previous studies FDA label, less than 1% of the patients age 12 years and older participating in clinical trials with NTZ suffered from the following adverse effects:
Systemic: asthenia, fever, pain, allergic reaction, pelvic pain, back pain, chills, fever, flu-like syndrome.
Central Nervous System: dizziness, somnolence, insomnia, tremor, hypesthesia.
Gastrointestinal System: vomiting, dyspepsia, anorexia, flatulence, constipation, dry mouth, thirst.
Urogenital System: discolored urine, dysuria, amenorrhea, metrorrhagia, kidney pain, edema labia.
Metabolic & Nutrition: increased SGPT.
Hemic & Lymphatic Systems: anemia, leukocytosis.
Skin: rash, pruritus.
Special Senses: eye discoloration, ear ache.
Respiratory System: epistaxis, lung disease, pharyngitis.
Cardiovascular System: tachycardia, syncope, hypertension.
Muscular System: myalgia, leg cramps, spontaneous bone fracture.

Nitazoxanide

DB00507

small molecule approved investigational vet_approved

Deskripsi

Nitazoxanide belongs to the class of drugs known as thiazolides. Nitazoxanide (NTZ) is a broad-spectrum anti-infective drug that markedly modulates the survival, growth, and proliferation of a range of extracellular and intracellular protozoa, helminths, anaerobic and microaerophilic bacteria, in addition to viruses. This drug is effective in the treatment of gastrointestinal infections including Cryptosporidium parvum or Giardia lamblia in healthy subjects. It is generally well tolerated. Nitazoxanide is a first-line, standard treatment for illness caused by C. parvum or G. lamblia infection in healthy (not immunosuppressed) adults and children and may also be considered in the treatment of illnesses caused by other protozoa or helminths A31976. Recently, this drug has been studied as a broad-spectrum antiviral agent due to its ability to inhibit the replication of several RNA and DNA viruses A31977.

Struktur Molekul 2D

Berat 307.282
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 7.3h [L1422]
Volume Distribusi -
Klirens (Clearance) Nitazoxanide is cleared in the urine and feces. The metabolite, tizoxanide, is also found in the urine, plasma, and breastmilk [L1424]. The drug is not found unchanged in the urine [L1424].

Absorpsi

The relative bioavailability of the suspension compared to the tablet was 70%. When administered with food the AUC and Cmax increased by two-fold and 50%, respectively, for the tablet and 45 to 50% and ≤ 10%, respectively, for the oral suspension FDA label.

Metabolisme

The active metabolite of this drug is tizoxanide (desacetyl-nitazoxanide). The initial reaction in the metabolic pathway of Nitazoxanide is hydrolysis to tizoxanide, followed by conjugation, primarily by glucuronidation to tizoxanide glucuronide. The oral suspension bioavailability of this drug is not equivalent to that of the oral tablets. Compared to the to the tablet, the bioavailability of the suspension was 70% FDA label. When administered with food, the AUCt of tizoxanide and tizoxanide glucuronide in plasma is increased to almost two-fold and the maximum concentration is increased by almost 50% compared to when ingested without food FDA label. When the oral suspension was ingested with food, the AUC of tizoxanide and tizoxanide glucuronide increased by approximately 50% and the Cmax increased by less than 10% FDA label.

Rute Eliminasi

Tizoxanide is excreted in the urine, bile and feces, and tizoxanide glucuronide is excreted in urine and bile. Approximately 2/3 of the oral dose of nitazoxanide is excreted in the faeces and 1/3 in the urine FDA label, A31981.

Interaksi Makanan

1 Data
  • 1. Take with food. Food improves oral bioavailability.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Pyruvate synthase por

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17722965
    Anderson VR, Curran MP: Nitazoxanide: a review of its use in the treatment of gastrointestinal infections. Drugs. 2007;67(13):1947-67.
  • PMID: 28748751
    Shakya A, Bhat HR, Ghosh SK: Update on Nitazoxanide: A Multifunctional Chemotherapeutic Agent. Curr Drug Discov Technol. 2017 Jul 27. pii: CDDT-EPUB-85034. doi: 10.2174/1570163814666170727130003.
  • PMID: 25108173
    Rossignol JF: Nitazoxanide: a first-in-class broad-spectrum antiviral agent. Antiviral Res. 2014 Oct;110:94-103. doi: 10.1016/j.antiviral.2014.07.014. Epub 2014 Aug 7.
  • PMID: 16495369
    Balamurugan K, Said HM: Role of reduced folate carrier in intestinal folate uptake. Am J Physiol Cell Physiol. 2006 Jul;291(1):C189-93. doi: 10.1152/ajpcell.00594.2005. Epub 2006 Feb 22.
  • PMID: 10984012
    Broekhuysen J, Stockis A, Lins RL, De Graeve J, Rossignol JF: Nitazoxanide: pharmacokinetics and metabolism in man. Int J Clin Pharmacol Ther. 2000 Aug;38(8):387-94.

Contoh Produk & Brand

Produk: 6 • International brands: 22
Produk
  • Alinia
    Powder, for suspension • 100 mg/5mL • Oral • US • Approved
  • Alinia
    Tablet • 500 mg/1 • Oral • US • Approved
  • Alinia
    Powder, for suspension • 100 mg/5mL • Oral • US • Approved
  • Alinia
    Tablet • 500 mg/1 • Oral • US • Approved
  • N/a
    Tablet • 500 mg/1 • Oral • US • Generic • Approved
  • Nitazoxanide
    Tablet, film coated • 500 mg/1 • Oral • US • Generic • Approved
International Brands
  • Alpex Nizox — Alpex Pharmaceutical
  • ANNITA — Alpex Pharmaceutical
  • Azoxanid — G&R
  • Celectan — Farma
  • Colufase — Roemmers
  • Coluquim — Quilab
  • Daxon — Siegfried
  • Dianide — General Pharma
  • Diar — ACI
  • Famidox — Lafrancol

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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