Stopdiar

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT STOPDIAR (STOPDIAR)

Composition:

Active substance: nifuroxazide;

1 hard capsule contains 200 mg of nifuroxazide;

Excipients: corn starch, pregelatinized starch, sucrose, magnesium stearate;

Hard capsule shell: gelatin, titanium dioxide (E 171), yellow iron oxide (E 172).

Pharmaceutical form. Hard capsules.

Main physicochemical characteristics: hard gelatin capsules, cylindrical, yellow in color. The granular content inside the capsule is yellow.

Pharmacotherapeutic group.

Antidiarrheal agents; drugs used in the treatment of infectious and inflammatory intestinal diseases. Antimicrobial agents used in intestinal infections.

ATC code A07AX03.

Pharmacological properties

Pharmacodynamics

Nitrofurazone 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. Nitrofurazone is not active against Proteus vulgaris, Proteus mirabilis, and Pseudomonas aeruginosa.

It is presumed that nitrofurazone inhibits dehydrogenase activity and disrupts protein synthesis in pathogenic bacteria.

At therapeutic doses, it practically does not disturb the balance of the normal bacterial flora of the large intestine, does not induce the development of resistant strains of pathogenic microorganisms, and does not cause cross-resistance to other antimicrobial agents. The efficacy of the drug is independent of the pH within the intestinal lumen.

Pharmacokinetics

After oral administration, the drug is partially absorbed (10–20%) from the gastrointestinal tract and extensively metabolized, with circulating components in the blood being primarily metabolites.

Preclinical safety data

Nitrofurazone exhibits mutagenic potential.

The carcinogenic potential of nitrofurazone was evaluated in mice (50 animals of each sex per group) and rats (52 animals of each sex per group), which 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.

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 normalized to body surface area.

Clinical characteristics.

Indications.

Acute infectious diarrhea.

Contraindications.

• Hypersensitivity to nifuroxazide and to other nitrofuran derivatives or to any of the excipients.
• Children under 7 years of age.

Interaction with other medicinal products and other forms of interaction.

• Concomitant administration of other oral medicinal products should be avoided due to the strong adsorptive properties of nifuroxazide.
• Simultaneous use of nifuroxazide with adsorbents, alcohol-containing products, agents that may cause disulfiram-like reactions, and agents that depress the central nervous system is not recommended.
• Consumption of alcoholic beverages during treatment with nifuroxazide is strictly prohibited due to the risk of developing a disulfiram-like reaction, characterized by exacerbation of diarrhea, vomiting, abdominal pain, sensation of warmth in the face and upper part of the body, hyperemia, tinnitus, dyspnea, and tachycardia.

Special precautions for use

• Nitrofurazone should not be used for more than 7 days. There are no indications for prolonged therapy. If diarrhea persists for more than 3 days after initiation of treatment, further diagnostic evaluation is required to determine the underlying cause of symptoms. Antibiotic therapy may become necessary.
• In cases of severe invasive diarrhea with clinical signs of general weakness, fever, and symptoms of intoxication, systemic-acting antibiotics should be considered, since nitrofurazone is not absorbed from the gastrointestinal tract.
• In the event of hypersensitivity reactions (dyspnea, facial swelling, swelling of lips, tongue, skin rash, pruritus), nitrofurazone should be discontinued immediately.
• During treatment of diarrhea, continuous additional oral rehydration is necessary to compensate for fluid loss caused by diarrhea. It is recommended to consume large amounts of fluids containing salt and sugar (based on an average daily requirement of 2 liters of water for an adult). In cases of severe or prolonged diarrhea, intense vomiting, or anorexia, intravenous rehydration should be administered depending on the patient's age and clinical condition. When performing oral or intravenous rehydration, instructions for dilution and use of the designated rehydration solutions must be strictly followed.
• Consumption of alcohol during nitrofurazone treatment is strictly prohibited 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 body, hyperemia, tinnitus, dyspnea, and tachycardia.
• Food intake is recommended; however, during diarrhea, dietary recommendations should be followed: avoid fresh vegetables and fruits, spicy foods, frozen products, and cold beverages. Baked meat and rice are recommended.
• Stopdiar contains sucrose. Patients with diagnosed intolerance to certain sugars should consult a physician before taking this medicinal product. Patients with rare hereditary forms of fructose intolerance, glucose-galactose malabsorption syndrome, or sucrase-isomaltase deficiency should not take this medicinal product.

Stopdiar contains 0.072 g of sucrose per dose. Use with caution in patients with diabetes mellitus.

Use during pregnancy or breastfeeding

Pregnancy

Clinical data on the use of nitrofurazone in pregnant women are limited. Animal studies on reproductive toxicity are insufficient. Nitrofurazone has shown mutagenic potential. Therefore, nitrofurazone is not recommended during pregnancy and should not be administered to women of childbearing potential who are not using effective contraception.

Lactation

It is unknown whether nitrofurazone or its metabolites are excreted in breast milk. Since nitrofurazone has low bioavailability (gastrointestinal absorption of approximately 10–20% of the administered dose), its concentration 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 nitrofurazone-containing medicinal products during breastfeeding, their use is not recommended.

Fertility

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

Ability to influence reaction speed when driving or operating machinery

Nitrofurazone does not affect the ability to drive or operate machinery.

Dosage and Administration.

The drug should be taken orally, swallowed with a small amount of water, regardless of food intake. The duration of treatment should not exceed 7 days.

Adults: 1 capsule four times daily (every 6 hours).

Children aged 7 years and older: 1 capsule three or four times daily (every 6–8 hours).

Children.

The drug can be used in children aged 7 years and older.

Overdose.

Specific information regarding symptoms of nifuroxazide overdose is not available.

One case of nifuroxazide overdose has been reported in a two-year-old child who received an unknown quantity of the oral suspension formulation. The child experienced somnolence and diarrhea, which subsequently resolved. In case of suspected nifuroxazide overdose, careful observation of the patient is recommended, along with symptomatic and supportive treatment.

Side effects

Immune system disorders

Frequency unknown: allergic reactions such as urticaria, pruritus, angioedema, anaphylactic shock. If an allergic reaction occurs, the drug must be discontinued. The patient should subsequently avoid intake of rifamox and other nitrofuran derivatives.

Blood and lymphatic system disorders

One case of granulocytopenia has been reported.

Gastrointestinal disorders

Individual cases of hypersensitivity to nifuroxazide may manifest as abdominal pain, nausea, vomiting, and worsening of diarrhea.

In case of mild symptoms, no specific treatment or discontinuation of nifuroxazide is required. However, if symptoms are severe, administration of this medicinal product should be discontinued. In such cases, subsequent use of nitrofuran derivatives should be avoided.

Skin and subcutaneous tissue disorders

Rare (from > 1/10,000 to < 1/1,000): skin reactions in the form of rash. One case of pustular eruption in an elderly patient has been reported. One case of nodular pruritus associated with contact allergy to nifuroxazide has been reported.

Shelf life

3 years.

Storage conditions

No special storage conditions are required for this medicinal product.

Keep out of reach and sight of children.

Packaging

12 hard capsules in a blister. 1 blister in a cardboard package.

Prescription status

Prescription only.

Manufacturer

Gedeon Richter Ltd., Poland.

Address of the manufacturer and location of its operations

5, ks. J. Poniatowskiego St., 05-825 Grójec, Poland.

Marketing authorization holder

Gedeon Richter Plc., Hungary.

Address of the marketing authorization holder

19-21 Demrédi St., H-1103 Budapest, Hungary.