Cefaclor Stada (Capsules) Instructions for Use

Marketing Authorization Holder

Stada Arzneimittel, AG (Germany)

Manufactured By

Cimex, AG/Ltd. (Switzerland)

ATC Code

J01DC04 (Cefaclor)

Active Substance

Cefaclor (Rec.INN registered by WHO)

Dosage Forms

	Cefaclor Stada	Capsules 500 mg: 10, 20 or 30 pcs.
		Granules for oral suspension 125 mg/5 ml: bottle 100 ml 1 or 2 pcs.
		Granules for oral suspension 250 mg/5 ml: bottle 100 ml 1 pc. in a set with a measuring spoon

Dosage Form, Packaging, and Composition

Excipients: simethicone, corn starch, methylcellulose, sodium dodecyl sulfate, sucrose, xanthan gum, strawberry flavor.

63.5 g – bottles with a volume of 100 ml (1) in a set with a measuring spoon – cardboard packs.
63.5 g – bottles with a volume of 100 ml (2) in a set with a measuring spoon – cardboard packs.

Granules for oral suspension white or white with a yellowish tint, homogeneous, with a strawberry smell; the prepared suspension is white or pale yellowish in color, with a strawberry smell.

Excipients: dimethicone, xanthan gum, corn starch, strawberry flavor, sodium lauryl sulfate, methylcellulose, sucrose.

63.5 g – dark glass bottles with a volume of 100 ml (1) in a set with a measuring spoon – cardboard packs.

Excipients: dimethicone, corn starch, magnesium stearate.

Capsule shell composition gelatin, purified water, titanium dioxide (E171), indigo carmine (E132).

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Second generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

Cephalosporin antibiotic of the II generation.

Like all beta-lactam antibiotics, Cefaclor inhibits the biosynthesis of the cell wall of multiplying bacteria. Its type of action is bactericidal.

Like all first and second generation cephalosporins, Cefaclor is characterized by only intermediate resistance to beta-lactamases, but is resistant to penicillinases.

The following gram-positive and gram-negative microorganisms are considered sensitive to Cefaclor: Staphylococcus spp., Streptococcus pneumoniae, Escherichia coli, Proteus mirabilis, Klebsiella spp, Heamophilus influenzae, including strains resistant to ampicillin, Neisseria gonorrhoeae, including penicillinase-producing strains, Bacteroides spp (except for fragilis), Moraxella catarrhalis, Citrobacter diversus, Propionibacterium, Peptococcus spp, Peptostreptococcus spp.

The following microorganisms are considered resistant to cefaclor: Listeria spp., Bordetella spp., Mycoplasma spp., Chlamydia spp., Enterococcus faecalis, Enterococcus faecium, Pseudomonas spp., Bacteroides fragilis, Campylobacter jejuni, most strains of Enterobacter spp., Morganella morganii, Proteus vulgaris, Providencia spp., Serratia spp., Acinetobacter spp.

Pharmacokinetics

From 75% to 92% of the cefaclor dose is absorbed, mainly from the upper part of the small intestine. After a single dose of cefaclor on an empty stomach at a dose of 250 mg, 500 mg and 1000 mg, C_max in plasma was reached 60 minutes after administration and was about 7, 15 and 26 mg/l, respectively.

In children who received Cefaclor on an empty stomach at a dose of 10 mg/kg and 15 mg/kg, C_max in serum was about 10.8 mg/l and 13.1 mg/l, respectively. After 10 days of administration, Cefaclor did not accumulate in the body.

Although food intake does not affect the degree of absorption (AUC), it reduces the rate of absorption, leading to an increase in the time to reach C_max and a 30% decrease in C_max.

4-6 hours after administration, the active drug is usually not detected in plasma.

Distribution

Cefaclor is distributed in various tissues and physiological fluids. For example, high concentrations are achieved in the prostate gland and in bile. Binding to serum proteins is about 25%. The concentrations of cefaclor in human tissues and fluids at various time intervals after administration are given below.

Metabolism and excretion

In solution, Cefaclor is chemically unstable and spontaneously decomposes in physiological fluids, for example, in urine. Therefore, the degree of true metabolic clearance is difficult to estimate. The metabolized drug, if present, constitutes a very small fraction of the degradation products of cefaclor.

Excretion occurs mainly through the kidneys. Within 8 hours after administration, 50-70% of the dose is excreted by the kidneys in the form of a microbiologically active drug and up to 30% of the dose in the form of inactive degradation products.

92% of the dose of radioactively labeled cefaclor is excreted by the kidneys and 4% through the gastrointestinal tract.

The average T_1/2 from plasma is 45 minutes (29-60 minutes). It is dose-dependent, i.e., after a single dose of a higher dose (for example, 500 mg or 1000 mg), the T_1/2 is somewhat longer than after a single dose of lower doses.

The T_1/2 from serum is increased in impaired renal function, but when such patients take cefaclor 3 times/day, the drug does not accumulate in the body. In anuria, the T_1/2 of cefaclor from serum is up to 3.5 hours. Cefaclor is excreted during hemodialysis. Hemodialysis reduces the T_1/2 from serum by 25-30%. The apparent volume of distribution is about 26 L. The renal clearance of cefaclor is in the range of 188-230 ml/min, and the total clearance is 370-455 ml/min.

The results of pharmacokinetic studies in children and adults are practically the same.

Indications

For the treatment of acute and chronic infections of varying severity caused by microorganisms sensitive to cefaclor

• Infections of the upper and lower respiratory tract;
• Infections of the ear, throat and nose, for example, otitis media, sinusitis, tonsillitis and pharyngitis;
• Infections of the kidneys and urinary tract, including gonorrhea;
• Infections of the skin and soft tissues.

ICD codes

Dosage Regimen

Orally. Adults and children over 10 years old – 0.25-0.5 g 3 times/day.

Capsules should be taken with a small amount of water.

For young children, prescribe in the form of a suspension.

Children under 1 month – dose not determined, from 1 month and older – 6.7-13.4 mg/kg every 8 hours or 10-20 mg/kg every 12 hours. The maximum daily dose is 40 mg/kg, but not more than 1 g/day. The average duration of treatment is 7-10 days. The duration of taking the drug should not be shortened.

Preparation of oral suspension.

Add water to the bottle with granules up to the mark and shake thoroughly. After the foam settles, add water up to the mark. The suspension is ready for use.

In the refrigerator (2°-8°C (17.6°F)) the prepared Cefaclor Stada suspension is stored for 14 days.

Before each use, the contents of the bottle should be shaken thoroughly.

The dose is measured with the supplied measuring spoon.

Cefaclor Stada suspension can be taken with meals, this does not affect the absorption of the drug.

1 measuring spoon (5 ml) of Cefaclor Stada suspension 125 mg/5 ml contains 125 mg of cefaclor.

1 measuring spoon (5 ml) of Cefaclor Stada suspension 250 mg/5 ml contains 250 mg of cefaclor.

In kidney diseases, no change in the dose of Cefaclor Stada is required. During hemodialysis, the T_1/2 of the drug from serum is reduced by 25-30%. If regular hemodialysis is necessary, a loading dose of 250 mg to 1 g of cefaclor is recommended before the hemodialysis procedure. Between hemodialysis procedures, the drug is used in the above doses.

Adverse Reactions

Allergic reactions: skin rash, skin itching, genital itching, urticaria, eosinophilia, arthralgia, fever, shortness of breath, angioedema, conjunctivitis, fainting, polymorphic erythema, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), anaphylaxis.

From the nervous system agitation, anxiety, insomnia, dizziness, paresthesia, motor agitation, confusion, hallucinations, asthenia.

From the genitourinary system: vaginitis.

From the urinary system: impaired renal function, interstitial nephritis, dysuria, nocturia.

From the digestive system: decreased appetite, dyspepsia (diarrhea, nausea, vomiting, constipation), pseudomembranous enterocolitis, abdominal pain, hepatitis, cholestatic jaundice.

From the hematopoietic organs hypoplastic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, hemolytic anemia, bleeding.

From the cardiovascular system increased blood pressure.

Laboratory parameters hyperazotemia, increased urea concentration, hypercreatininemia, increased activity of liver transaminases, hyperbilirubinemia.

Other candidomycosis, superinfection, increased sweating.

Contraindications

• Children under 3 years of age (capsules);
• Hypersensitivity (including to other beta-lactam antibiotics).

With caution severe allergic diseases, history of bronchial asthma; chronic renal failure, leukopenia, hemorrhagic syndrome; acute gastrointestinal diseases accompanied by vomiting and diarrhea; diabetes mellitus (presence of sucrose); hereditary fructose intolerance, glucose-galactose malabsorption, sucrase-isomaltase deficiency (granules for oral suspension 125 mg/-250 mg); pregnancy, lactation period.

Use in Pregnancy and Lactation

Use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

Cefaclor is excreted in breast milk, so if it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Use in Renal Impairment

With caution chronic renal failure.

In kidney diseases, no change in the dose of Cefaclor Stada is required. During hemodialysis, the T_1/2 of the drug from serum is reduced by 25-30%. If regular hemodialysis is necessary, a loading dose of 250 mg to 1 g of cefaclor is recommended before the hemodialysis procedure. Between hemodialysis procedures, the drug is used in the above doses.

Pediatric Use

Capsules are contraindicated in children under 3 years of age.

For young children, prescribe in the form of a suspension.

Children under 1 month – dose not determined, from 1 month and older – 6.7-13.4 mg/kg every 8 hours or 10-20 mg/kg every 12 hours. The maximum daily dose is 40 mg/kg, but not more than 1 g/day. The average duration of treatment is 7-10 days. The duration of taking the drug should not be shortened.

Special Precautions

If a dose is missed, the drug should be taken as soon as possible. If several doses are missed, a doctor should be consulted to identify possible deterioration of the patient’s condition as early as possible.

The drug should not be discontinued prematurely, as a relapse of the disease is possible.

During treatment, a false-positive direct Coombs test and a false-positive urine test for glucose are possible.

If hypersensitivity reactions occur, the drug should be discontinued and appropriate emergency measures should be taken, such as intravenous administration of norepinephrine, antihistamines or corticosteroids.

Overdose

Symptoms nausea, vomiting, diarrhea

Treatment: activated charcoal, ensuring necessary ventilation and perfusion, monitoring and maintaining blood gases and serum electrolytes at the required level. Hemodialysis is not effective.

Drug Interactions

Enhances the effect of indirect anticoagulants

Enhances (mutually) the nephrotoxicity of aminoglycosides, polymyxins, phenylbutazone.

The antibacterial effect is enhanced by aminoglycosides, metronidazole, polymyxins, rifampicin, and weakened by chloramphenicol, tetracyclines.

Antacids containing magnesium or aluminum hydroxide slow down the rate of absorption of the drug.

Histamine H₂-receptor blockers (cimetidine, ranitidine, nizatidine, roxatidine, famotidine) do not affect the rate and extent of absorption.

Tubular secretion blockers delay the excretion of cefaclor by the kidneys.

Storage Conditions

List B.

Capsules 0.5 g should be stored in a dry, light-protected place, at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Granules for the preparation of an oral suspension 125 mg/5 ml should be stored in a dry place, protected from light, at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Granules for the preparation of an oral suspension 250 mg/5 ml should be stored at a temperature not exceeding 25°C (77°F). The prepared suspension should be stored in a refrigerator for 14 days.

Keep out of reach of children.

Shelf Life

Shelf life: capsules – 3 years, granules – 3 years

The drug must not be used after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.