Nifuroxazide-sperko

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NIFUROXAZIDE-SPERCO

Composition:

Active ingredient: nifuroxazide;

5 ml of suspension contains nifuroxazide 200 mg;

Excipients: methylparaben (methyl p-hydroxybenzoate) (E 218), sucrose, carbomer, citric acid monohydrate, simethicone emulsion, banana flavoring (contains propylene glycol), sodium hydroxide, purified water.

Pharmaceutical form. Oral suspension.

Main physicochemical properties: yellow-colored suspension with banana odor. May sediment slightly upon storage, but returns to a homogeneous state after shaking.

Pharmacotherapeutic group. Antidiarrheal agents, drugs used in the treatment of infectious and inflammatory intestinal diseases. Antimicrobial agents for treatment of intestinal infections. Nifuroxazide.

ATC Code A07AX03.

Pharmacological Properties

Pharmacodynamics

Nifuroxazide is an antimicrobial agent derived from 5-nitrofuran. The exact mechanism of action of the drug has not been fully elucidated; however, the antimicrobial and antiparasitic properties of nifuroxazide are possibly due to the presence of an amino group. The local activity and lack of penetration into the body's organs and tissues determine the uniqueness of nifuroxazide compared to other nitrofuran derivatives, since this antidiarrheal agent lacks systemic effects. Nifuroxazide is effective against Gram-positive and Gram-negative bacteria: Streptococcus spp., Staphylococcus spp., E. coli, Salmonella spp., Shigella spp.

Pharmacokinetics

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

Preclinical Safety Data

Nifuroxazide demonstrates 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), which received nifuroxazide in feed 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 for body surface area.

Clinical characteristics.

Indications.

Acute infectious diarrhea.

Contraindications.

Hypersensitivity to nifuroxazide, to other 5-nitrofuran derivatives, or to 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 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 of treatment for acute diarrhea in children. Children should be given frequent drinks (every 15 minutes). Prevention or treatment of dehydration should be carried out using oral or intravenous solutions. If oral rehydration is indicated, it is recommended to use rehydration solutions specifically designed for this purpose, according to the instructions for dilution and administration. The required volume of oral rehydration solutions depends on the degree of body weight loss. In cases of severe diarrhea, intense vomiting, or refusal to eat, intravenous rehydration is required. If intravenous rehydration is not necessary, fluid losses 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 followed: avoid consumption of fresh vegetables and fruits, spicy food, frozen products, and beverages. Rice should be preferred. The decision on consumption of dairy products should be made on a case-by-case basis. If diarrhea is accompanied by clinical symptoms indicating severe disease (worsening general condition, fever, signs of intoxication), nifuroxazide should be administered together with systemic-acting antibacterial agents used for the treatment of intestinal infections, since the drug is not absorbed from the gastrointestinal tract and does not enter systemic circulation. The drug should not be used as monotherapy for the treatment of intestinal infections complicated by sepsis.

Nifuroxazide contains sugar, which should be taken into account when prescribing the drug to patients with diabetes mellitus. The drug is not recommended for patients with hereditary disorders of sucrose or fructose intolerance.

The drug contains methylparaben (E 218), which may cause allergic reactions.

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, sensation of warmth in the face and upper part of the body, facial flushing, tinnitus, breathing difficulties, tachycardia.

Use during pregnancy or breastfeeding

Pregnancy. Data on the use of nifuroxazide for treatment in pregnant women are limited. Data from animal studies on reproductive toxicity are insufficient. Nifuroxazide has shown potential mutagenic activity. Therefore, nifuroxazide is not recommended during pregnancy and should not be prescribed to women of reproductive age who are not using effective contraception.

Lactation. It is unknown whether nifuroxazide or its metabolites are excreted in breast milk. Since nifuroxazide has low bioavailability (approximately 10–20% of the dose is absorbed from the gastrointestinal tract), its concentration in 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 information from animal studies regarding the effect of nifuroxazide on fertility.

Ability to affect reaction speed while driving or operating machinery

Does not affect.

Dosage and Administration.

Nifuroxazide should be taken orally, regardless of food intake, at regular intervals. Shake the suspension well before use. For dosing, use the measuring spoon (capacity 5 ml) provided in the package, graduated in 2.5 ml increments.

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

Adults: 5 ml of suspension four times daily.

Maximum daily dose of nifuroxazide is 800 mg. The duration of treatment should not exceed 7 days.

Children.

Do not use in children under 2 years of age.

Overdose.

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

Adverse reactions.

Possible occurrence of temporary abdominal pain, nausea, vomiting, and exacerbation of diarrhea.

Allergic reactions are also possible, including itching, skin rashes, urticaria, Quincke's edema (angioedema), and anaphylactic shock. The occurrence of allergic reactions requires discontinuation of the drug and contraindicates future use of nifuroxazide and other nitrofuran derivatives.

Cases involving the hematopoietic and lymphatic systems have included one reported case of granulocytopenia.

Reporting suspected adverse reactions.

Reporting of suspected adverse reactions after drug registration is highly important. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua

Shelf life.

3 years. Do not use the medicinal product 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.

100 ml in a dark brown container, with a dosing spoon, packed in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

Ukrainian-Spanish joint venture "Sperco Ukraine".

Manufacturer's address and location of business operations.

25, 600-Richchia St., Vinnytsia, Ukraine, 21027.

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

www.sperco.com.ua