Nifuroxazide-sperco

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NIFUROXAZIDE-SPERCO (NIFUROXAZ-ID-SPERCO)

Composition:

Active substance: nifuroxazide;

1 capsule contains 200 mg of nifuroxazide;

Excipients: sucrose, anhydrous lactose, maize starch, talc, magnesium stearate.

The capsule shell contains: gelatin, titanium dioxide (E 171), quinoline yellow (E 104), yellow sunset FCF (E 110).

Pharmaceutical form. Capsules.

Main physicochemical properties: hard gelatin capsules with yellow body and cap. The contents of the capsules are yellow powder, granules, or pellets. The presence of white specks is acceptable.

Pharmacotherapeutic group. Antimicrobial agents used in intestinal infections. Nifuroxazide.

ATC code A07AX03.

Pharmacological Properties

Pharmacodynamics

Nifuroxazide is an intestinal antiseptic, a derivative of 5-nitrofuran, active against most causative agents of intestinal infections (including mutant strains resistant to other antimicrobial agents): Gram-positive (family Staphylococcus) and Gram-negative (family Enterobacteriaceae: Escherichia, Citrobacter, Enterobacter, Klebsiella, Salmonella, Shigella, Proteus, Yersinia), as well as Vibrio cholerae. It is inactive against bacteria of the genus Pseudomonas and the genus Proteus (species Proteus inconstans), and also against strains of the subgroup A of the species Providencia alcalifaciens. It is presumed that the drug inhibits dehydrogenase activity and disrupts protein synthesis in pathogenic bacteria. At standard therapeutic doses, it exhibits bacteriostatic activity, while at higher doses, it acts bactericidally. The effect appears within the first hours of treatment. At therapeutic doses, it practically does not disturb the balance of intestinal microflora; it does not induce the development of resistant strains of pathogenic microorganisms or cross-resistance of bacteria to other antimicrobial agents, allowing, if necessary, its use in combination therapy with systemic drugs for generalized infections. In viral intestinal infections, it prevents the development of bacterial superinfection.

Pharmacokinetics

After oral administration, the drug is partially absorbed (10–20%) from the gastrointestinal tract and extensively metabolized. The majority of the active substance circulates in the blood in the form of metabolites. It is excreted from the body predominantly in feces.

Preclinical Safety Data

Nifuroxazide shows a potential mutagenic effect.

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

The doses administered to mice and rats (5400 mg/m² and 10,800 mg/m², respectively) exceeded the maximum human dose of 1800 mg (493 mg/m² for a 60 kg patient) by 11 and 22 times, respectively, when adjusted to body surface area.

Clinical characteristics.

Indications.

Acute infectious diarrhea.

Contraindications.

Hypersensitivity to any component of the drug, including other 5-nitrofuran derivatives. Children under 7 years of age (for children under 7 years of age, Nifuroxazide-Sperko is administered in the form of a suspension).

Interaction with other medicinal products and other forms of interaction.

Alcoholic beverages and medicinal products containing alcohol should not be consumed during treatment with nifuroxazide due to the possibility of developing a disulfiram-like reaction, which manifests as worsening of diarrhea, vomiting, abdominal pain, sensation of warmth, skin hyperemia, tinnitus, dyspnea, tachycardia, and feeling of fear. Concomitant administration of other oral medicinal products should be avoided due to the strong adsorptive properties of nifuroxazide.

Special precautions for use

Treatment with nitroxoline does not exclude dietary regimen and rehydration. If diarrhea persists after 3 days of treatment, dosage should be reviewed and a decision on rehydration therapy should be made. When necessary, concomitant rehydration therapy should be administered depending on the patient's age, condition, and severity of diarrhea.

In cases where oral or intravenous rehydration is indicated, instructions for dilution and use of the designated solutions must be strictly followed. If such 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 fresh vegetables and fruits, spicy food, frozen products and beverages. Rice is recommended. The decision on consumption of dairy products should be made on an individual basis.

If diarrhea is accompanied by clinical signs indicating severe disease (worsening of general condition, fever, symptoms of intoxication), Nitroxoline-Sperko should be prescribed together with systemic antibacterial agents used for 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.

Nitroxoline-Sperko contains sucrose, which should be taken into account when prescribing the drug to patients with diabetes mellitus.

This medicinal product contains sucrose and lactose. If you have been diagnosed with intolerance to certain sugars, consult your doctor before taking this medicinal product. The drug is not recommended for patients with hereditary fructose or sucrose intolerance.

The capsule coating contains Sunset Yellow FCF (E 110), which may cause allergic reactions.

Alcohol consumption during treatment is strictly prohibited due to the risk of disulfiram-like reaction (see section "Interaction with other medicinal products and other forms of interaction").

Use during pregnancy or breastfeeding

Pregnancy. Clinical data on the use of nitroxoline in pregnant women are limited. Animal studies on reproductive toxicity are insufficient. Nitroxoline has a potential mutagenic effect. Therefore, nitroxoline is not recommended during pregnancy and should not be prescribed to women of childbearing potential who are not using effective contraception.

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

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

Ability to affect reaction rate when driving or operating machinery

Nitroxoline-Sperko does not affect psychomotor reaction speed.

Dosage and Administration.

For adults and children aged 7 years and older, the recommended dose is 1 capsule 4 times daily, regardless of food intake. Maximum daily dose – 800 mg. Treatment duration should not exceed 7 days.

Children.

Nifuroxazide-Sperko in capsule form is indicated for children aged 7 years and older.

For treatment of children under 7 years of age, Nifuroxazide-Sperko in suspension form should be used.

Overdose.

Cases of overdose have not been reported. In case of overdose, gastric lavage and symptomatic treatment are recommended.

Adverse reactions.

The drug is well tolerated; occasionally, temporary abdominal pain, nausea, vomiting, or exacerbation of diarrhea may occur. In case of mild gastrointestinal symptoms, there is no need for specific therapy or discontinuation of nitroxoline, as such symptoms resolve spontaneously.

In patients hypersensitive to nitrofuran derivatives, granulocytopenia and allergic reactions, usually of the skin type (rash, pruritus, urticaria, pustular eruptions), may occur. In isolated cases, as with other nitrofuran derivatives, dyspnea and severe hypersensitivity reactions, including angioneurotic edema and anaphylactic shock, may develop.

If severe adverse reactions occur, the drug must be discontinued and symptomatic therapy initiated. Subsequently, the patient should avoid taking nitroxoline and other nitrofuran derivatives.

Reporting suspected adverse reactions.

Reporting suspected adverse reactions after drug registration is highly important. It allows continuous monitoring of the benefit-risk balance of the drug. Healthcare professionals and patients or their legal representatives are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua

Shelf life.

3 years.

Do not use the drug after the expiry date stated on the packaging.

Storage conditions.

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

12 capsules in a plastic container, in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

Ukrainian-Spanish joint enterprise "Sperco Ukraine".

Manufacturer's address and location of business activity.

25, 600-richchia Street, Vinnytsia, 21027, Ukraine.

Tel.: + 38 (0432) 52-30-36. E-mail: [email protected]

www.sperco.com.ua