Nifuroxide-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NIFUROZID-ZDOROV'YA (NIFUROZIDE-ZDOROVYE)

Composition:

Active substance: nifuroxazide;

5 ml of the preparation contain 200 mg of nifuroxazide;

Excipients: sucrose; carbomer; sodium hydroxide; citric acid; methylparaben (E 218); 96% ethanol; banana flavor containing maltodextrin, dextrin and glycerol triacetate; purified water.

Pharmaceutical form. Oral suspension.

Main physicochemical properties: a yellow, viscous suspension with a fruity odor.

Pharmacotherapeutic group. Antimicrobial agents used in the treatment of intestinal infections. Nifuroxazide. ATC code A07AX03.

Pharmacological Properties

Pharmacodynamics

Nitrofurazone is an antimicrobial agent derived from nitrofuran. Its mechanism of action is not fully understood. The antimicrobial and antiparasitic properties of nitrofurazone may be due to the presence of an amino group. Local activity combined with the absence of penetration into organs and tissues determines the uniqueness of nitrofurazone compared to other nitrofuran derivatives, as this antidiarrheal agent lacks systemic effects. It is effective against gram-positive and gram-negative bacteria: Streptococcus pyogenes, Staphylococcus aureus, E. coli, Salmonellae, Shigellae.

Nitrofurazone demonstrates mutagenic potential.

The carcinogenic potential of nitrofurazone was evaluated in mice (50/sex/group) and rats (52/sex/group) that received nitrofurazone in the diet for 2 years at doses of 0, 200, 600, or 1800 mg/kg/day. Despite its mutagenic properties, carcinogenicity of nitrofurazone was not demonstrated in either mice or rats.

Based on 2-year studies in mice and rats (5400 mg/m² and 10800 mg/m², respectively), using surface area comparisons with 11- and 22-fold coefficients, the maximum human dose is considered to be 1800 mg (493 mg/m² assuming a patient weight of 60 kg).

Pharmacokinetics

After oral administration, the drug is partially absorbed (10–20%) from the gastrointestinal tract and is extensively metabolized, with the main circulating components in the blood being metabolites. Biotransformation of nitrofurazone occurs in the intestine; approximately 20% of the drug is excreted unchanged. Nitrofurazone and its metabolites are excreted in feces. The rate of elimination depends on the amount of drug administered and gastrointestinal motility. Overall, elimination of nitrofurazone is slow—it remains in the gastrointestinal tract for a prolonged period.

At therapeutic doses, nitrofurazone practically does not suppress normal intestinal microflora, does not induce the emergence of resistant microbial forms, and does not lead to the development of cross-resistance of bacteria to other antibacterial agents. Therapeutic effect is achieved within the first hours of treatment.

Clinical characteristics.

Indications. Acute infectious diarrhea.

Contraindications. Hypersensitivity to nitroxoline, other 5-nitrofuran derivatives, or any of the excipients of the drug.

Interaction with other medicinal products and other forms of interaction. Nitroxoline is not recommended to be used concomitantly with adsorbents, alcohol-containing products, drugs that may cause disulfiram-like reactions, and drugs that suppress the central nervous system.

Special precautions for use

Treatment with nifuroxazide does not exclude the need for dietary management and rehydration. If necessary, concomitant rehydration therapy should be applied according to the patient's age, clinical condition, and severity of diarrhea.

Rehydration should be the main component in the treatment of acute diarrhea in children. Children should be given frequent small amounts of fluids (every 15 minutes).

Prevention or treatment of dehydration should be performed using oral or intravenous rehydration solutions. If oral rehydration is indicated, rehydration solutions specifically designed for this purpose should be used, following the manufacturer's instructions for dilution and administration. The required volume of oral rehydration solution depends on the degree of body weight loss. Intravenous rehydration is necessary in cases of severe diarrhea, intense vomiting, or refusal to eat.

If intravenous rehydration is not required, fluid loss should be compensated by drinking large amounts of fluids containing salt and sugar (based on an average daily requirement of 2 liters of water).

Dietary recommendations during diarrhea should be observed: avoid consumption of fresh vegetables and fruits, spicy foods, frozen foods, and beverages. Rice-based foods are recommended. The decision on consumption of dairy products should be made on a case-by-case basis.

If diarrhea is accompanied by clinical signs indicating severe disease (worsening general condition, fever, signs of intoxication), nifuroxazide should be administered together with systemic antibacterial agents used for the treatment of intestinal infections, as the drug is not absorbed from the gastrointestinal tract and does not enter systemic circulation. The drug should not be used as monotherapy for intestinal infections complicated by sepsis.

Alcohol consumption is strictly prohibited during treatment due to the risk of a disulfiram-like reaction, which may manifest as worsening diarrhea, vomiting, abdominal pain, facial flushing and warmth in the upper body, hyperemia, tinnitus, breathing difficulties, and tachycardia.

The medicinal product contains methylparaben (E 218), which may cause allergic reactions (possibly delayed).

The medicinal product contains a small amount of ethanol (alcohol), less than 100 mg per dose.

The product may be harmful to teeth.

The product contains sucrose; therefore, if the patient has a known intolerance to certain sugars, consultation with a physician is recommended before taking this medicinal product.

Use during pregnancy or breastfeeding

Pregnancy. Data on the use of nifuroxazide in pregnant women are limited. Animal studies on reproductive toxicity are insufficient. Nifuroxazide has shown mutagenic potential. Therefore, this medicinal product is not recommended during pregnancy and should not be administered to women of childbearing potential who are not using effective contraception.

Breastfeeding. It is unknown whether nifuroxazide or its metabolites are excreted in human breast milk. Since nifuroxazide has low bioavailability (gastrointestinal absorption of approximately 10–20% of the administered dose), its concentration in breast milk is likely to be low. However, an effect on the gastrointestinal microbiome of breastfed infants cannot be excluded. Due to the lack of clinical experience with nifuroxazide-containing medicinal products during breastfeeding, their use is not recommended.

Fertility. There is insufficient data from animal studies on the effect of nifuroxazide on fertility.

Ability to influence reaction speed when driving or operating machinery. No effect.

Method of Administration and Dosage

Take orally, regardless of food intake. Shake the suspension well before use. The maximum daily dose of nitrofurazone is 800 mg.

Children aged 2 years and older: 5 ml of suspension three times daily.

Adults: 5 ml of suspension four times daily.

Duration of treatment should not exceed 7 days.

Children. Do not administer to children under 2 years of age.

Overdose. Cases of overdose have not been reported.

In case of exceeding the therapeutic dose, gastric lavage and symptomatic treatment are recommended.

Side effects.

Possible temporary abdominal pain, nausea, vomiting, and worsening of diarrhea. Allergic reactions may occur, including itching, skin rashes, urticaria, Quincke's edema (angioedema), and anaphylactic shock. If an allergic reaction occurs, the drug must be discontinued. Afterwards, the patient must avoid taking nifuroxazide and other nitrofuran derivatives.

Shelf life. 3 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children. The shelf life of the medication after opening the bottle is 28 days.

Packaging. 50 mL, 100 mL in polymer bottles or 100 mL in glass bottles, with a measuring spoon in a carton box.

Prescription status. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Location of manufacturer and address of business activity. 22, Shevchenka Street, Kharkiv, Kharkiv Region, 61013, Ukraine.