Macropen, 175 mg/5 ml 20 g

Pharmacodynamics

Macropen® is macrolide antibiotic that inhibits protein synthesis of bacterial cells, has bacteriostatic effect in low doses, in high doses – bactericidal. It binds irreversibly to 50S subunit of ribosomal membrane of bacteria. It is effective against intracellular microorganisms: Mycoplasma spp., Chlamydia spp., Legionella spp., Ureaplasma urealyticum; Gram-positive bacteria: Streptococcus spp., Staphylococcus spp, Corynebacterium diphtheriae, Listeria monocytogenes, Clostridium spp.; some gram-negative bacteria: Neisseria spp., Moraxella catarrhalis, Bordetella pertussis, Helicobacter spp., Campylobacter spp., Bacteroides spp.

Pharmacokinetics

After oral administration the drug is quickly and completely absorbed from the gastrointestinal tract.

The Cmax of midecamycin and midecamycin acetate in serum is 0.5-2.5 µg/L and 1.31-3.3 µg/L, respectively, is reached 1-2 hours after oral administration.

High concentrations of midecamycin and midecamycin acetate are produced in internal organs (especially in the tissues of the lungs, parotid and submandibular glands) and skin.

The MAC persists for 6 h. T1/2 is approximately 1 h. Protein binding is 47% of midecamycin and 3-29% of metabolites.

The drug is metabolized in the liver to form 2 active metabolites with antimicrobial activity. It is excreted with the bile and to a lesser extent (about 5%) by the kidneys.

In liver cirrhosis, plasma concentrations, AUC and T1/2 are significantly increased.

Indications

respiratory tract infections, including. caused by atypical pathogens (mycoplasmas, legionella, chlamydia and Ureaplasma urealyticum) – tonsillopharyngitis, acute otitis media, sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia;

infections of the urogenital tract caused by atypical pathogens – mycoplasmas, legionella, chlamydia and Ureaplasma urealyticum;

infections of the skin and subcutaneous tissue;

enteritis caused by bacteria of the genus Campylobacter;

Diphtheria and pertussis (treatment and prevention).

Active ingredient

Composition

Active ingredient:

Midecamycin acetate 200 mg;

Associates:

methylparahydroxybenzoate;

propylparahydroxybenzoate;

citric acid;

sodium hydrophosphate anhydrous;

Banana flavoring;

Sunset Yellow FCF dye (E110);

Hypromellose;

silicone defoamer;

sodium saccharinate;

mannitol.

How to take, the dosage

The drug Macropen is taken before meals.

In adults, an average daily dose of 1.2 g (400 mg three times daily) is prescribed.

The maximum daily dose is 1.6 g.

In children Macropen is prescribed depending on body weight, preferably in suspension.

The daily dose is 30-50 mg per kg of weight, 2 times a day.

The course duration is 7-10 days, with chlamydia 14 days.

Interaction

Concomitant administration of ergot alkaloids or carbamazepine with Macropen® decreases their metabolism in the liver and increases serum concentrations. Therefore, caution should be exercised when taking these drugs concomitantly.

There is no effect on the pharmacokinetic parameters of theophylline.

When Macropen® is used concomitantly with cyclosporine or anticoagulants (warfarin) the excretion of the latter is delayed.

Special Instructions

Hepatic enzyme activity should be monitored during long-term therapy, especially in patients with impaired liver function.

As with any other antimicrobials, prolonged treatment may lead to an overgrowth of resistant bacteria. Prolonged diarrhea may indicate the development of pseudomembranous colitis.

Mannitol in Macropen® (oral suspension granules) may cause diarrhea.

Contraindications

– severe hepatic insufficiency;

– children under 3 years of age (for tablets).

With caution:

– pregnancy;

– period of lactation;

– presence of allergic reaction to acetylsalicylic acid.

Side effects

Gastrointestinal disorders: decreased appetite, stomatitis, nausea, vomiting, diarrhea, feeling of heaviness in epigastrium, increased liver transaminases activity, hyperbilirubinemia, jaundice.

In rare cases, severe and prolonged diarrhea may be observed, which may indicate the development of pseudomembranous colitis.

Allergic reactions: skin rash, urticaria, skin itching, eosinophilia, bronchospasm.

Others: weakness.

Overdose

Symptoms (possible): nausea, vomiting.

Treatment: symptomatic.