nitazoxanide (Rx)

1-10%

Headache (1%)

Abdominal pain (8%)

Diarrhea (2%)

Nausea (3%)

Chromaturia (2%)

Vomiting (1%)

<1%

Increased ALT

Anorexia

Appetite increased

Creatinine increased

Diaphoresis

Dizziness

Eye discoloration (pale yellow)

Fever

Flatulence

Infection

Malaise

Pruritus

Thinitis

Salivary glands enlarged

Urine discoloration

Postmarketing Reports

Gastrointestinal disorders: diarrhea, gastroesophageal reflux disease

Nervous System disorders: dizziness

Respiratory, thoracic and mediastinal disorders: dyspnea

Skin and subcutaneous tissue disorders: rash, urticarial

Contraindications

Hypersensitivity

Cautions

Safety and efficacy not established in HIV+ or immunodeficient patients

Effects in hepatic/renal impairment unknown; use caution

Safety and efficacy of suspension in children <1 year not established

Safety and efficacy of tablets in children <12 years not established

Drug interaction overview

• Tizoxanide (active metabolite of nitazoxanide) is highly bound to plasma protein (>99.9%)
• Monitor for adverse reactions if nitazoxanide is coadministered with other highly protein-bound drugs with narrow therapeutic indices, as competition for binding sites may occur (eg, warfarin)
• The prescribing information recommends avoiding concurrent warfarin use

Pregnancy: No data with pregnant women to inform of drug-associated risk; No teratogenicity or fetotoxicity observed in animal reproduction studies with administration of nitazoxanide to pregnant rats and rabbits during organogenesis at exposures 30 and 2 times, respectively, the exposure at maximum recommended human dose of 500 mg twice daily based on body surface area (BSA)

Lactation: Development and health benefits of breastfeeding should be considered along with the mother’s clinical need and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Inhibits growth of sporozoites and oocysts of Cryptosporidium and trophozoites of Giardia

Interferes with pyruvate:ferredoxin oxidoreductase (PFOR), essential to anaerobic energy metabolism

Pharmacokinetics

Protein Bound: >99.9%

Metabolism: hydrolysis & glucuronidation

Metabolites: Tizoxanide, tizoxanide glucuronide (100% conversion)

Excretion: Urine, bile, feces

Peak PlasmaTime: 1-4 hr

Peak plasma concentration: 3 mcg/mL

AUC: 12-19 mcg.hr/mL

Oral Administration

Take with food