Ilosone 500 mg Tablets

Brand name

The drug is known under the trade name Ilosone. This name is registered in pharmaceutical registries and is used to identify the drug in pharmacies, medical institutions and among health care professionals. Ilosone is recognized for its effectiveness in the treatment of bacterial infections requiring targeted antibacterial action. The name was chosen by the manufacturers to indicate its affiliation with a specific group of antibiotics, emphasizing its importance and unique properties in medical practice.

International Nonproprietary Name (INN)

The international nonproprietary name of this medicine is erythromycin. This term is accepted by the international community to designate the active substance that provides the therapeutic effect. Erythromycin belongs to the class of macrolide antibiotics, known for their ability to inhibit the growth of a wide range of bacteria. The name is standardized by the World Health Organization, which ensures uniformity in the prescription and production of this drug in different countries and regions.

Form of release

The drug is presented in several forms, which makes it convenient for use depending on the age of the patient and the nature of the infectious process. The main options include:

• Film-coated tablets with dosages of 250 mg and 500 mg of the active ingredient, intended for oral administration by adults and older children.
• Capsules with a dosage of 250 mg, providing an alternative for convenient use.
• Powder for preparation of suspension for oral administration with a concentration of 125 mg/5 ml and 250 mg/5 ml after dilution, often used in pediatrics.
• Ointment for external application (2% concentration) for the treatment of skin infections.

Each form is designed with specific treatment in mind: tablets and capsules are suitable for systemic infections, suspension is convenient for children, and ointment is effective for localized lesions. The choice of form is determined by the doctor based on the diagnosis.

Composition

The main active ingredient is erythromycin, an antibiotic from the group of macrolides. Auxiliary components depend on the form of release. In tablets, the following are used:

• Microcrystalline cellulose - filler for uniform distribution of the active substance.
• Corn starch - a binder for the formation of the mass.
• Magnesium stearate - lubricating agent for ease of manufacture.
• Povidone - solvent to improve structure.
• Hypromellose and titanium dioxide film shell - for protection and ease of administration.

The capsules add lactose monohydrate and gelatin for the shell. The suspension contains sucrose to improve taste, flavorings (e.g., cherry) and xanthan gum as a thickener. The ointment includes petroleum jelly and paraffin as a base. The composition is balanced to ensure stability and bioavailability.

Pharmacologic Properties

Pharmacodynamics

Ilosone has bacteriostatic action, inhibiting protein synthesis in bacterial cells. It binds to 50S-subunit of ribosomes, preventing the process of translation and formation of peptide chains, which stops the growth and multiplication of microorganisms. In high concentrations, the drug can exhibit a bactericidal effect against particularly sensitive strains. The drug is active against Gram-positive bacteria (Streptococcus pneumoniae, Staphylococcus aureus, Streptococcus pyogenes), some Gram-negative pathogens (Haemophilus influenzae, Neisseria gonorrhoeae) and atypical pathogens (Mycoplasma pneumoniae, Chlamydia trachomatis, Legionella pneumophila).

The mechanism of action makes the medication valuable in infections requiring a mild but sustained antibacterial effect. Ilosone is particularly useful in the treatment of atypical infections and as an alternative in the case of penicillin allergy.

Pharmacokinetics

Absorption

After oral administration, the active ingredient is absorbed in the gastrointestinal tract, predominantly in the small intestine, reaching maximum plasma concentrations after 2-4 hours. Bioavailability varies from 30 to 65% depending on the form of release and food intake. For optimal absorption, it is recommended to take the drug on an empty stomach, as food, especially fatty food, reduces absorption.

Distribution

The component is well distributed in the body, penetrating into the lungs, liver, skin, mucous membranes and soft tissues. Binding to plasma proteins is 70-80%, which provides a stable presence in the blood. Concentrations in tissues often exceed plasma concentrations, which enhances the effect in respiratory and skin infections.

Metabolism

Metabolism occurs in the liver with the participation of cytochrome P450 (CYP3A4) enzymes, forming inactive metabolites. About 80% of the dose is metabolized, which reduces the burden on the kidneys.

Excretion

Excretion is predominantly with bile (60-70%) and partially through the kidneys (10-15% unchanged). The elimination half-life is 1.5-2 hours, but may increase in case of hepatic dysfunction. Prolonged excretion through bile provides a sustained effect.

Indications for Use

Ilosone is indicated for the treatment of infections caused by sensitive microorganisms:

• Infections of the upper respiratory tract: pharyngitis, tonsillitis, sinusitis.
• Lower respiratory tract infections: bronchitis, pneumonia.
• Infections of the skin and soft tissues: furunculosis, impetigo, rye.
• Infections caused by atypical bacteria: mycoplasma pneumonia, chlamydia infections.
• Middle otitis media and genital tract infections (gonorrhea, syphilis with penicillin allergy).

Ointment is used for bacterial lesions of the skin and eyes (conjunctivitis). Appointment requires confirmation of the sensitivity of the pathogen.

Contraindications

The use of Ilosone is prohibited when:

• Hypersensitivity to macrolides.
• Severe hepatic insufficiency.
• Simultaneous administration with cisapride or pimozide (risk of arrhythmias).
• Prolongation of the QT interval in the history.

Caution is used in myasthenia gravis and electrolyte disorders.

Method of Administration and Dosage

How to take

Tablets and capsules are taken orally, drinking water (150-200 ml), 1 hour before a meal or 2 hours after for maximum absorption. Suspension is prepared by adding water to the mark, shake before use. The ointment is applied in a thin layer to the affected areas of the skin or conjunctiva 2-3 times a day.

Dosages for adults and children

Dosage depends on the infection:

• Adults: 250-500 mg every 6 hours, course 7-14 days.
• Children older than 1 month: 30-50 mg/kg/day, divided into 4 doses, course 7-10 days.
• Ointment: 2-3 times a day, course 5-7 days.

Dose adjustment for certain conditions

With hepatic insufficiency:

• Mild/moderate: 250 mg every 8 hours.
• Severe: use is contraindicated.

No correction is required in renal insufficiency.

Side Effects

Unwanted reactions include:

• Gastrointestinal: nausea, diarrhea, abdominal pain
• Nervous: dizziness, headache.
• Skin: rash, pruritus, rarely urticaria.
• hepatic: increase in transaminases, jaundice.
• Cardiac: QT prolongation (rare).

Discontinue if symptoms are severe.

Overdose

Symptoms of overdose

Overdose of Ilosone causes nausea, vomiting, arrhythmias, hearing loss.

First aid measures

In overdose:

• Stop taking it.
• Rinse the stomach (within 1-2 hours).
• Supply symptomatic therapy (ECG monitoring).
• Refer to a doctor.

Drug Interactions

Influence on the effects of other drugs

The medication affects:

• Theophylline: increase in blood concentrations.
• Barfarin: increase in anticoagulant effect.
• Carbamazepine: increase in toxicity.

Compatibility with alcohol and food

Alcohol increases toxicity to the liver and is avoided. Food decreases absorption.

Special Precautions

Use in pregnancy and breastfeeding

Ilosone is tolerated in pregnancy for strict indications (category B). Penetrates into milk, lactation is suspended.

Effects on driving and driving mechanisms

Dizziness may make driving difficult.

Particulars of use in the elderly and children

The elderly require control of liver function. In children the drug is safe from 1 month of age with proper dosage.