Alinia

Agents for Amoebiasis and Other Protozoal Diseases

Nitazoxanide is administered orally. Give with food.

Shake well prior to each administration.
Measure dosage with calibrated spoon, cup, or oral syringe.
Diabetic patients and caregivers should be aware that the oral suspension contains 1.48 g of sucrose per 5 ml.
 
Reconstitution
Review the reconstitution instructions for the particular product and package size, as the amount of water required for reconstitution varies from manufacturer to manufacturer.
Prior to reconstitution, tap the bottle several times to loosen the powder.
Add approximately half of the total amount of water as listed and shake vigorously to suspend the powder. Add the remainder of the water and again shake vigorously. After reconstitution, the oral suspension contains nitazoxanide 100 mg/5 ml.
Storage: Store reconstituted suspension at controlled room temperature. Discard any unused portion after 7 days.

bone fractures / Delayed / 0-1.0

constipation / Delayed / 0-1.0
dysuria / Early / 0-1.0
elevated hepatic enzymes / Delayed / 0-1.0
anemia / Delayed / 0-1.0
hypertension / Early / 0-1.0
sinus tachycardia / Rapid / 0-1.0

abdominal pain / Early / 6.6-7.8
diarrhea / Early / 2.1-4.2
headache / Early / 1.1-3.1
nausea / Early / 0-3.0
vomiting / Early / 0-1.1
anorexia / Delayed / 0-1.0
dyspepsia / Early / 0-1.0
appetite stimulation / Delayed / 0-1.0
xerostomia / Early / 0-1.0
flatulence / Early / 0-1.0
insomnia / Early / 0-1.0
hypoesthesia / Delayed / 0-1.0
dizziness / Early / 0-1.0
tremor / Early / 0-1.0
drowsiness / Early / 0-1.0
pelvic pain / Delayed / 0-1.0
back pain / Delayed / 0-1.0
infection / Delayed / 0-1.0
influenza / Delayed / 0-1.0
fever / Early / 0-1.0
malaise / Early / 0-1.0
asthenia / Delayed / 0-1.0
amenorrhea / Delayed / 0-1.0
urine discoloration / Early / 0-1.0
pruritus / Rapid / 0-1.0
diaphoresis / Early / 0-1.0
rash / Early / 0-1.0
otalgia / Early / 0-1.0
iridal discoloration / Delayed / 0-1.0
epistaxis / Delayed / 0-1.0
pharyngitis / Delayed / 0-1.0
rhinitis / Early / 0-1.0
leukocytosis / Delayed / 0-1.0
syncope / Early / 0-1.0
myalgia / Early / 0-1.0
muscle cramps / Delayed / 0-1.0
gastroesophageal reflux / Delayed / Incidence not known
urticaria / Rapid / Incidence not known

Alinia

Rx

Oral synthetic antiprotozoal agent
Used for the treatment of cryptosporidiosis and giardiasis
Also used off-label for C. difficile-associated diarrhea

500 mg PO every 12 hours 3 days.

500 mg PO every 12 hours for 3 days.

200 mg PO every 12 hours for 3 days.

100 mg PO every 12 hours for 3 days.

500 mg PO every 12 hours for 3 days.

500 mg PO every 12 hours for 3 days.

200 mg PO every 12 hours for 3 days.

100 mg PO every 12 hours for 3 days.

500 mg PO every 12 hours for 3 days.

500 mg PO every 12 hours for 3 days.

200 mg PO every 12 hours for 3 days.

100 mg PO every 12 hours for 3 days.

500 to 1,000 mg PO every 12 hours for at least 14 days. Give in combination with optimized antiretroviral therapy, symptomatic treatment, rehydration, and electrolyte replacement.

500 to 1,000 mg PO every 12 hours for at least 14 days. Give in combination with optimized antiretroviral therapy, symptomatic treatment, rehydration, and electrolyte replacement.

500 mg PO every 12 hours for 3 to 14 days.

200 mg PO every 12 hours for 3 to 14 days.

100 mg PO every 12 hours for 3 to 14 days.

500 mg PO every 12 hours for 3 days as an alternative.

500 mg PO every 12 hours for 3 days as an alternative.

200 mg PO every 12 hours for 3 days as an alternative.

100 mg PO every 12 hours for 3 days as an alternative.

500 mg PO every 12 hours for 3 days as an alternative followed by long-term suppressive therapy.

500 mg PO every 12 hours for 3 days as an alternative followed by long-term suppressive therapy.

200 mg PO every 12 hours for 3 days as an alternative followed by long-term suppressive therapy.

100 mg PO every 12 hours for 3 days as an alternative followed by long-term suppressive therapy.

1,000 mg PO every 12 hours as an alternative; however, effects may be minimal for persons with a low CD4 count.

1,000 mg PO every 12 hours as an alternative; however, effects may be minimal for patients with a low CD4 count.

200 mg PO every 12 hours for 3 days. In clinical trials in pediatric subjects (n = 163), treatment with nitazoxanide significantly reduced time to resolution of symptoms/diarrhea and duration of hospitalization compared with control treatments.

100 mg PO every 12 hours for 3 days. In clinical trials in pediatric subjects (n = 163), treatment with nitazoxanide significantly reduced time to resolution of symptoms/diarrhea and duration of hospitalization compared with control treatments.

7.5 mg/kg/dose PO every 12 hours for 3 days. In clinical trials in pediatric subjects (n = 163), treatment with nitazoxanide significantly reduced time to resolution of symptoms/diarrhea and duration of hospitalization compared with control treatments.

500 mg PO twice daily for 10 days as an alternative for the treatment of the primary episode of C. difficile infection.

500 mg PO twice daily in combination with levofloxacin, doxycycline, and a proton pump inhibitor (PPI) for 7 to 10 days.

†Indicates off-label use

Nitazoxanide has not been studied in patients with hepatic impairment.

Nitazoxanide has not been studied in patients with renal impairment.

Acetaminophen; Aspirin, ASA; Caffeine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Acetaminophen; Aspirin: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Acetaminophen; Aspirin; Diphenhydramine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aminosalicylate sodium, Aminosalicylic acid: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Butalbital; Caffeine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Caffeine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Caffeine; Orphenadrine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Carisoprodol: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Carisoprodol; Codeine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Citric Acid; Sodium Bicarbonate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Dipyridamole: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Omeprazole: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Aspirin, ASA; Oxycodone: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Bismuth Subsalicylate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Bismuth Subsalicylate; Metronidazole; Tetracycline: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Butalbital; Aspirin; Caffeine; Codeine: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Choline Salicylate; Magnesium Salicylate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Fosphenytoin: (Moderate) No interactions with other drugs have been reported by patients using nitazoxanide. The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins (> 99%). No studies have been performed to determine if there are interactions with other drugs that exhibit high protein binding (e.g., hydantoins like phenytoin or fosphenytoin). Therefore, caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Magnesium Salicylate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Methenamine; Sodium Salicylate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Phenytoin: (Moderate) No interactions with other drugs have been reported by patients using nitazoxanide. The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins (> 99%). No studies have been performed to determine if there are interactions with other drugs that exhibit high protein binding (e.g., hydantoins like phenytoin or fosphenytoin). Therefore, caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Salicylates: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Salsalate: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Sulfonylureas: (Moderate) The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins. Caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur.
Warfarin: (Moderate) No interactions with other drugs have been reported by patients using nitazoxanide. The active metabolite of nitazoxanide, tizoxanide, is highly bound to plasma proteins (> 99%). The manufacturer has reported that nitazoxanide does not affect the pharmacokinetics or anticoagulant effects of warfarin in healthy volunteers. No studies have been performed to determine if there are interactions with other drugs that exhibit high protein binding (e.g., hydantoins like phenytoin or fosphenytoin, the sulfonylureas, or salicylates). Therefore, caution should be exercised when administering nitazoxanide concurrently with other highly plasma protein-bound drugs with narrow therapeutic indices because competition for binding sites may occur. No other clinical studies have been conducted to specifically exclude the possibility of interactions between nitazoxanide and other medicinal products which are not highly-protein bound.

Alinia Oral Pwd F/Recon: 5mL, 100mg
Alinia/Nitazoxanide Oral Tab: 500mg

1,000 mg/day PO per FDA-approved labeling; however, doses up to 2,000 mg/day PO have been used off-label.

1,000 mg/day PO per FDA-approved labeling; however, doses up to 2,000 mg/day PO have been used off-label.

1,000 mg/day PO per FDA-approved labeling; however, doses up to 2,000 mg/day PO have been used off-label.

12 years: 1,000 mg/day PO.
4 to 11 years: 400 mg/day PO.
1 to 3 years: 200 mg/day PO.

Safety and efficacy have not been established; however, doses up to 15 mg/kg/day PO have been used off-label.

Safety and efficacy have not been established.

Mechanism of Action: Nitazoxanide exhibits antiprotozoal activity. Nitazoxanide and its metabolite, tizoxanide, are active in vitro in inhibiting the growth of sporozoites and oocysts of Cryptosporidium parvum and the trophozoites of Giardia lamblia. The exact mechanism of action of nitazoxanide is unknown. It is believed that the antiprotozoal effects of nitazoxanide are due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic energy metabolism. Studies of Giardia lamblia have shown that the PFOR enzyme from this organism directly reduces nitazoxanide by transfer of electrons in the absence of ferredoxin. The DNA-derived PFOR protein sequence of Cryptosporidium parvum appears to be similar to that of Giardia lamblia. It is suggested that interference with the PFOR enzyme-dependent electron transfer reaction may not be the only pathway by which nitazoxanide exhibits antiprotozoal activity. Nitazoxanide has also exhibited activity against other protozoa such as Giardia duodenalis, G. intestinalis and Entamoeba histolytica. Nitazoxanide also has some antiviral activity; it is being studied for rotavirus infection and chronic hepatitis B and C infections.Resistance mechanisms to nitazoxanide by Cryptosporidium parvum, Giardia lamblia or other protozoa have not been examined.

Nitazoxanide is administered orally as a suspension. The pharmacokinetic parameters of nitazoxanide listed are from studies performed in the pediatric population from 12 months to 11 years of age. The parent drug nitazoxanide is not detected in plasma. Once in the systemic circulation, the active metabolite, tizoxanide, is > 99% bound to plasma proteins. Tizoxanide is excreted in the urine, bile, and feces, and tizoxanide glucuronide is excreted in urine and bile.

Following oral administration of a single dose of nitazoxanide with food, the drug is rapidly hydrolyzed to the active metabolite, tizoxanide (desacetyl-nitazoxanide) which then undergoes conjugation primarily to tizoxanide glucuronide. Maximum plasma concentrations (Cmax) of tizoxanide and tizoxanide glucuronide occur within 1—4 hours (Tmax). No studies have been performed to determine if administration of the drug in the fasted state affects the pharmacokinetics of tizoxanide and tizoxanide glucuronide compared to administration with food.

There are no data with nitazoxanide in human pregnancy to inform a drug-associated risk. Animal reproductive studies performed in rats and rabbits at doses up to 2 and 30 times the recommended daily human dose demonstrated no evidence of teratogenicity or fetotoxicity due to nitazoxanide.

There is no information about the presence of nitazoxanide in human milk, the effects on the breast-fed infant, or the effects on milk production. The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for nitazoxanide and any potential adverse effects on the breast-fed infant from nitazoxanide or the mother's underlying condition.