Phthalazol

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

Composition:

Active substance: phthalylsulfathiazole;

1 tablet contains 500 mg of phthalylsulfathiazole;

Excipients: potato starch, talc, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or white with a yellowish tint tablets, with a flat surface, a score line and bevelled edges.

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

ATC code A07AB02.

Pharmacological properties.

Pharmacodynamics.

Phthalazol is a sulfonamide drug. It exerts a bacteriostatic effect. The main mechanism of action is due to inhibition of synthesis of microbial growth factors—folic acid and dihydrofolic acid.

Pharmacokinetics.

Phthalazol is slowly absorbed from the gastrointestinal tract; the majority of the drug remains in the small intestine, where the active (sulfonamide) part of the molecule is gradually released. As a result, high concentrations of sulfonamide are formed in the intestine. The drug is excreted predominantly in feces. A small absorbed amount (5–10% of the dose) is uniformly distributed throughout the body, acetylated in the liver, and excreted in urine.

Clinical characteristics.

Indications.

• Acute dysentery (shigellosis);
• chronic dysentery in the stage of exacerbation;
• colitis, enterocolitis, gastroenteritis;
• prevention of infectious complications during intestinal surgery.

Contraindications.

• Increased individual sensitivity to phthalylsulfathiazole, sulfanilamide drugs and/or other components of the medicinal product;
• Basedow's disease (Graves' disease);
• blood disorders;
• acute hepatitis.

Interaction with other medicinal products and other types of interactions.

If the patient is taking any other medicinal products, it is necessary to consult a physician regarding the possibility of using Phthalazol.

Depending on the nature of the disease, the drug can be used in combination with antibiotics (an enhanced antimicrobial effect is observed). Phthalazol may be prescribed simultaneously with well-absorbed sulfanilamides (sulfadimidine, etazole, etazole-sodium, etc.). It is incompatible with PAS (para-aminosalicylic acid), salicylates, and phenytoin (increased toxic effect of phthalazol), oxacillin (reduced oxacillin activity), nitrofurans (increased risk of anemia and methemoglobinemia), and preparations of male and female sex hormones (suppression of gonadal function), calcium chloride and vitamin K (impaired blood coagulation).

Phthalazol must not be used simultaneously with enteral adsorbents and laxatives.

Myelotoxic medicinal products enhance the manifestations of hematotoxicity of the drug.

Special precautions for use.

Consult a physician before taking the medication!

Use with caution in patients with nephrosis or nephritis.

During Phthalazol therapy, patients should take vitamin B complex (thiamine, riboflavin, nicotinic acid), since suppression of intestinal flora reduces synthesis of these vitamins.

If symptoms of disease do not begin to resolve, or if the patient's condition worsens, or adverse reactions occur, discontinue Phthalazol and consult a physician regarding further use of the medication.

Use during pregnancy or breastfeeding.

Phthalylsulfathiazole crosses the placenta, and animal studies have shown adverse effects on the fetus; therefore, the drug should not be used during pregnancy.

Phthalylsulfathiazole is excreted in breast milk and may cause kernicterus in infants, as well as hemolytic anemia in infants with glucose-6-phosphate dehydrogenase deficiency; therefore, the drug should not be used during breastfeeding.

Ability to affect reaction rate while driving or operating machinery.

The medication does not affect psychomotor reaction speed; it may be used at recommended doses by individuals driving vehicles or operating machinery.

Administration and Dosage

Do not use the medication for longer than the specified period without consulting a physician!

Administer orally to adults and children aged 3 years and older.

Adults and children aged 12 years and older.

For acute dysentery in adults and children aged 12 years and older, the following dosage is recommended:
Days 1–2: 6 g per day (1 g every 4 hours);
Days 3–4: 4 g per day (1 g every 6 hours);
Days 5–6: 3 g per day (1 g every 8 hours).
The total course dose is 25–30 g.

Five to six days after the first course of treatment, a second course should be administered:
Days 1–2: 1 g every 4 hours (every 8 hours at night), total 5 g per day;
Days 3–4: 1 g every 4 hours (do not administer at night), total 4 g per day;
Day 5: 1 g every 4 hours (do not administer at night), total 3 g per day.
The total dose for the second course is 21 g; in mild cases, the dose may be reduced to 18 g.

Maximum doses for adults: single dose – 2 g, daily dose – 7 g.

For treatment of other diseases, adults should receive 1–2 g every 4–6 hours during the first 2–3 days, and then 0.5–1 g every 4–6 hours for the following 2–3 days.

Children aged 3 to 12 years.

For acute dysentery:
Children aged 3 to 7 years: 500 mg per dose, 4 times daily;
Children aged 7 to 12 years: 500–750 mg per dose, 4 times daily.
Treatment duration: up to 7 days.

For treatment of other diseases: on the first day, administer 100 mg/kg body weight per day, divided into equal doses every 4 hours, with a pause at night. In subsequent days, administer 250–500 mg every 6–8 hours. Treatment duration: up to 7 days.

If a child cannot swallow the tablet, it should be crushed and dissolved in a small amount of cooled boiled water.

If the patient is taking any other medications, it is essential to consult a physician regarding the possibility of using this drug.

Children

Administer to children from the age of 3 years.

Overdose

Symptoms: macrocytosis and pancytopenia may occur due to folic acid deficiency. This can be prevented by administering folic acid or calcium folinate. Increased incidence of adverse reactions.

Treatment: discontinue the medication, symptomatic therapy.

Adverse reactions.

If any adverse events occur, consult a physician immediately!

Systemic side effects typical of sulfonamides occur rarely due to the low absorption of the active substance.

Possible adverse reactions:

Immune system disorders: hypersensitivity reactions, including allergic reactions such as fever, rash, and itching;

Blood and lymphatic system disorders: agranulocytosis, aplastic anemia;

Other: vitamin B complex deficiency (thiamine, riboflavin, nicotinic acid) due to suppression of intestinal microflora.

Shelf life. 5 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging. 10 tablets in a blister; 10 tablets in a blister, 1 blister per carton.

Prescription status. Over-the-counter (without prescription).

Manufacturer. JSC "Kyivmedpreparat".

Manufacturer's address and place of business.

139 Saksahanskoho St., Kyiv, 01032, Ukraine.

INSTRUCTION

for medical use of the medicinal product

PHTHALAZOL

(PHTHALAZOL)

Composition:

Active substance: phthalylsulfathiazole;

1 tablet contains phthalylsulfathiazole 500 mg;

Excipients: potato starch, talc, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or off-white tablets with flat surface, a score line and beveled edges.

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

ATC code A07AB02.

Pharmacological properties.

Pharmacodynamics.

Phthalazol is a sulfonamide agent. It exerts a bacteriostatic effect. The main mechanism of action is due to inhibition of microbial synthesis of growth factors—folic acid and dihydrofolic acid.

Pharmacokinetics.

Phthalazol is slowly absorbed from the gastrointestinal tract; the majority of the drug remains in the small intestine, where the active (sulfonamide) part of the molecule is gradually cleaved. This results in high concentrations of sulfonamides in the intestine. The drug is primarily excreted in feces. A small amount (5–10% of the dose) is absorbed, evenly distributed throughout the body, acetylated in the liver, and excreted in urine.

Clinical characteristics.

Indications.

• Acute dysentery (shigellosis);
• chronic dysentery in exacerbation phase;
• colitis, enterocolitis, gastroenteritis;
• prevention of infectious complications during intestinal surgery.

Contraindications.

• Hypersensitivity to phthalylsulfathiazole, sulfonamide drugs, and/or any component of the medicinal product;
• Basedow's disease (Graves' disease);
• blood disorders;
• acute hepatitis.

Interaction with other medicinal products and other forms of interaction.

If the patient is taking any other medicinal products, a physician must be consulted regarding the possibility of using Phthalazol.

Depending on the nature of the disease, the drug may be used in combination with antibiotics (resulting in enhanced antimicrobial effect). It is advisable to co-administer sulfonamides with good systemic absorption (e.g., sulfadimidine, etazol, etazol sodium, etc.). Phthalazol is incompatible with PAS (para-aminosalicylic acid), salicylates, diphenine (phenytoin) (increased toxicity of phthalazol), oxacillin (reduced oxacillin activity), nitrofurans (increased risk of anemia and methemoglobinemia), and sex hormones (suppression of gonadal function), calcium chloride, and vitamin K (reduced blood coagulability).

Phthalazol must not be used simultaneously with enterosorbents or laxatives.

Myelotoxic medicinal products enhance the hematotoxic effects of phthalazol.

Special precautions.

Consult a physician before taking this medicinal product!

Use with caution in patients with nephrosis or nephritis.

During treatment with Phthalazol, patients should take vitamin B complex (thiamine, riboflavin, nicotinic acid), as suppression of intestinal flora reduces synthesis of these vitamins.

If symptoms of disease do not improve or worsen, or if adverse reactions occur, discontinue Phthalazol and consult a physician regarding further treatment.

Use during pregnancy or breastfeeding.

Phthalylsulfathiazole crosses the placenta, and animal studies have shown adverse effects on the fetus; therefore, the drug is contraindicated during pregnancy.

Phthalylsulfathiazole is excreted in breast milk and may cause nuclear jaundice in infants and hemolytic anemia in children with glucose-6-phosphate dehydrogenase deficiency; therefore, the drug should not be used during breastfeeding.

Effect on ability to drive or operate machinery. The medicinal product does not affect psychomotor reaction speed and may be used at recommended doses by individuals driving vehicles or operating machinery.

Dosage and administration.

Do not use the drug longer than indicated without consulting a physician!

Administer orally to adults and children aged 3 years and older.

Adults and children aged 12 years and older.

For acute dysentery, adults and children aged 12 years and older should receive: Days 1–2: 6 g daily (1 g every 4 hours); Days 3–4: 4 g daily (1 g every 6 hours); Days 5–6: 3 g daily (1 g every 8 hours). Total course dose: 25–30 g.

Five to six days after the first course, a second course should be administered: Days 1–2: 1 g every 4 hours (8-hour interval at night), total 5 g daily; Days 3–4: 1 g every 4 hours (no nighttime dose), total 4 g daily; Day 5: 1 g every 4 hours (no nighttime dose), total 3 g daily. Total dose for second course: 21 g; in mild cases, the dose may be reduced to 18 g.

Maximum doses for adults: single dose – 2 g, daily dose – 7 g.

For treatment of other conditions, adults should receive 1–2 g every 4–6 hours during the first 2–3 days, followed by 0.5–1 g every 6–8 hours for the next 2–3 days.

Children aged 3 to 12 years.

For acute dysentery: children aged 3 to 7 years – 500 mg four times daily; children aged 7 to 12 years – 500–750 mg four times daily. Treatment course: up to 7 days.

For treatment of other conditions: on Day 1, administer 100 mg/kg/day in equal doses every 4 hours, with a nighttime break. In subsequent days, administer 250–500 mg every 6–8 hours. Treatment course: up to 7 days.

If a child cannot swallow the tablet, it should be crushed and dissolved in a small amount of cooled boiled water.

If the patient is taking any other medicinal products, consult a physician regarding the possibility of using this drug.

Children.

For use in children aged 3 years and older.

Overdose.

Symptoms: macrocytosis and pancytopenia may occur due to folic acid deficiency. These can be prevented by administering folic acid or calcium folinate. Increased incidence of adverse reactions.

Treatment: discontinue the drug and provide symptomatic therapy.

Adverse reactions.

In case of any adverse events, consult a physician immediately!

Systemic side effects typical of sulfonamides occur rarely due to low absorption of the active substance.

Possible adverse reactions:

Immune system disorders: hypersensitivity reactions, including allergic reactions such as fever, rash, and itching;

Blood and lymphatic system disorders: agranulocytosis, aplastic anemia;

Other: vitamin B complex deficiency (thiamine, riboflavin, nicotinic acid) due to suppression of intestinal microflora.

Shelf life. 5 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging. 10 tablets in a blister; 10 tablets in a blister, 1 blister per carton.

Prescription status. Over-the-counter (without prescription).

Manufacturer. JSC "Kyivmedpreparat".

Manufacturer's address and place of business.

139 Saksahanskoho St., Kyiv, 01032, Ukraine.