Cefaclor 500 mg Capsules

Brand name

The drug is presented on the market under the trade name Cefaclor. This name is used to designate the drug in the pharmacy network and medical practice.

International Nonproprietary Name (INN)

The international nonproprietary name of the medicine is cefaclor. It indicates the active component underlying the therapeutic effect.

Form of release

The drug is available in different forms, which allows you to take into account the age of the patient and the peculiarities of treatment:

• Capsules with dosages of 250 mg and 500 mg of the active substance.
• Powder for the preparation of suspension for oral administration with a concentration of 125 mg/5 ml, 250 mg/5 ml or 375 mg/5 ml.
• Prolonged-release tablets (in some countries), 375 mg or 500 mg.

The choice of form depends on the clinical situation and the physician's preference.

Composition

The main active substance is cefaclor, a second-generation antibiotic from the group of cephalosporins. Auxiliary components in capsules include:

• Lactose monohydrate - as an excipient.
• Corn starch - binder.
• Magnesium stearate - lubricating agent.
• Gelatin - for capsule shell.

Sweeteners (sucrose), flavorings (e.g., strawberry), xanthan gum for density are added to the suspension. The composition may vary slightly depending on the manufacturer.

Pharmacologic Properties

Pharmacodynamics

The drug has a bactericidal action, disrupting the synthesis of peptidoglycan in the cell wall of bacteria. This is achieved by inhibiting transpeptidases, which leads to lysis of microorganisms. It is active against Gram-positive bacteria (Streptococcus pyogenes, Staphylococcus aureus, including penicillinase-producing strains) and Gram-negative microorganisms (Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae). Resistance to beta-lactamases is moderate, making it effective in a number of cases where first-generation drugs are powerless.

Action begins rapidly when the therapeutic concentration is reached in the focus of infection.

Pharmacokinetics

Absorption

After oral administration, the active substance is absorbed in the small intestine, reaching peak blood concentrations in 0.5-1 hour. Bioavailability is about 90% when taken on an empty stomach, but decreases by 25-30% when taken with food.

Distribution

The compound is distributed in tissues including lungs, skin, bone, and urinary tract. Binding to plasma proteins is low - about 25%, which contributes to good penetration into foci of inflammation.

Metabolism

Metabolism is minimal, most of the substance remains unchanged. A small proportion is converted into inactive metabolites in the liver.

Excretion

It is excreted mainly by the kidneys (70-80% unchanged) through tubular filtration and tubule secretion. The elimination half-life is about 0.6-1 hour in patients with normal renal function.

Indications for Use

The drug is used for the treatment of infectious diseases caused by sensitive pathogens:

• Infections of the respiratory tract: bronchitis, pneumonia, pneumonia, pharyngitis, sinusitis.
• Infections of the urinary tract: cystitis, pyelitis.
• Infections of the skin and soft tissues: furunculosis, pyoderma.
• Medium otitis media, especially in children.
• Tonsillitis and other infections of the ENT organs.

Prescription requires bacteriologic confirmation in complicated cases.

Contraindications

The use is prohibited in:

• Hypersensitivity to cephalosporins or penicillins.
• Severe allergic reactions to beta-lactam antibiotics in the anamnesis.
• Acute renal failure without dose adjustment.

With caution, use in colitis or blood coagulation disorders.

Method of Administration and Dosage

How to take

Capsules or suspension is taken orally, drinking water (100-150 ml). It is better to take on an empty stomach 1 hour before a meal or 2 hours after for maximum absorption. The suspension is prepared by adding water up to the mark, shake before each administration.

Dosages for adults and children

Dosage depends on the severity of the infection:

• Adults: 250-500 mg every 8 hours, course of 7-10 days.
• Children over 1 month of age: 20-40 mg/kg/day, divided into 3 doses (maximum 1 g/day).

Dose adjustment for certain conditions

In renal insufficiency:

• Creatinine clearance 10-50 mL/min: dose reduction by 25-50%.
• Clearance less than 10 ml/min: the interval between doses is increased up to 12 hours.

Hepatic insufficiency does not require correction.

Side Effects

Unwanted reactions may include:

• Gastrointestinal: diarrhea, nausea, oral candidiasis.
• Allergic: rash, urticaria, rarely - anaphylaxis.
• Hematologic: eosinophilia, neutropenia.
• Nervous: headache, weakness.

Treatment should be discontinued for serious symptoms.

Overdose

Symptoms of overdose

Exceeding the dose is manifested by nausea, vomiting, convulsions, confusion.

First aid measures

In overdose:

• Stop taking it.
• Rinse the stomach (within 1-2 hours).
• Provide hydration and symptomatic support.
• Seek medical attention.

Drug Interactions

Influence on the effects of other drugs

The medication may:

• Amplify the effect of anticoagulants (warfarin).
• Decrease the effectiveness of probenecid (slows excretion).

Compatibility with alcohol and food

Alcohol does not affect directly, but may worsen the condition in infection. Food decreases the rate of absorption.

Special Precautions

Use in pregnancy and breastfeeding

The use in pregnancy is allowed under strict indications (category B). Penetrates into milk, it is recommended to suspend lactation.

Effects on driving and operating machinery

Faintness or dizziness may affect the ability to drive machinery.

Particulars of use in the elderly and children

The elderly require monitoring of renal function. In children the drug is safe from 1 month of age with accurate dosage.