Nifurozid-zdorovya

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NIFUROZID-ZDOROVIYA

Composition:

Active substance: nifuroxazide;

1 capsule contains 100 mg or 200 mg of nifuroxazide;

Excipients: maize starch, microcrystalline cellulose, sucrose, magnesium stearate;

Capsule shell of 100 mg capsule contains: quinoline yellow (E 104), erythrosine (E 127), titanium dioxide (E 171), gelatin;

Capsule shell of 200 mg capsule contains: titanium dioxide (E 171), iron oxide red (E 172), iron oxide yellow (E 172), gelatin.

Dosage form. Capsules.

Main physicochemical characteristics: hard gelatin capsules (100 mg capsules – yellow in color; 200 mg capsules – caramel-colored). The capsule contents are a mixture containing yellow granules and powder. The presence of particle agglomerates is acceptable. A manufacturer's trademark may be printed on the capsule.

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

Pharmacological Properties

Pharmacodynamics

Nitrofurazone is an antimicrobial agent belonging to the nitrofuran derivatives. Its mechanism of action is not fully understood. The antimicrobial and antiparasitic properties of nitrofurazone are possibly due to the presence of an amino group. Its local activity and lack of penetration into the body's organs and tissues determine the uniqueness of nitrofurazone compared to other nitrofuran derivatives, since this antidiarrheal agent lacks systemic effects. It is effective against both 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 their 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 dose for humans is 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 extensively metabolized, with the main circulating components 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 nifuroxazide, other 5-nitrofuran derivatives, or any component of the drug.

Interaction with other medicinal products and other forms of interaction. Nifuroxazide should not be used concomitantly with adsorbents, alcohol-containing preparations, drugs that may cause disulfiram-like reactions, and drugs that depress the central nervous system.

Special precautions for use

Treatment with nifuroxazide does not exclude the need for dietary management and rehydration. If diarrhea persists after 3 days of treatment, the dosage should be reviewed and a decision on rehydration therapy should be made. When necessary, concomitant rehydration therapy should be administered according to the patient's age, clinical condition, and severity of diarrhea.

In cases where oral or intravenous rehydration is indicated, the instructions for dilution and administration of the prescribed solutions must be strictly followed. If such rehydration is not required, fluid losses should be compensated by drinking large amounts of fluids containing salt and sugar (bearing in mind that the average daily requirement is 2 liters of water).

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

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

Alcohol consumption is strictly prohibited during treatment due to the risk of developing 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.

If a patient has known intolerance to certain sugars, medical advice should be sought before taking this medication.

Use during pregnancy or breastfeeding

Pregnancy. Data on the use of nifuroxazide in pregnant women are limited. Reproductive toxicity studies in animals 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 dose), the amount excreted in milk is likely to be low. However, effects on the gut microbiome of breastfed infants cannot be ruled out. 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 affect reaction speed when driving or operating machinery.
Nifuroxazide-Health does not affect the patient's reaction speed when driving or operating machinery.

Dosage and Administration.

Take orally, independent of food intake.

Adults and children aged 15 years and older: 200 mg (2 capsules of 100 mg or 1 capsule of 200 mg) 4 times daily. Maximum daily dose of nifuroxazide — 800 mg.

Children aged 6 years and older: 2 capsules of 100 mg 3–4 times daily. Daily dose of nifuroxazide — 600–800 mg.

Duration of treatment — no more than 7 days.

Children. Nifurozid-Zdorov'ya 100 mg is indicated for children aged 6 years and older.

For treatment of children under 6 years of age, prescribe Nifurozid-Zdorov'ya suspension.

Nifurozid-Zdorov'ya 200 mg is indicated for children aged 15 years and older.

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 transient abdominal pain, nausea, vomiting, and worsening of diarrhea. Allergic reactions are possible, including itching, skin rash, urticaria, Quincke's edema (angioedema), and anaphylactic shock. If an allergic reaction occurs, the drug must be discontinued. The patient should thereafter avoid taking nifuroxazide and other nitrofuran derivatives.

Shelf life. 2 years — for the 100 mg dosage form; 3 years — for the 200 mg dosage form.

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

Keep out of reach of children.

Packaging. Capsules: 10 pcs (10×1), 20 pcs (10×2) in blisters, in a cardboard box.

Prescription status. Prescription only.

Manufacturer: LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and place of business activity: Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, building 22.