Macropen, 400 mg 16 pcs

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, incl. caused by atypical pathogens (mycoplasma, legionella, chlamydia and Ureaplasma urealyticum) – tonsillopharyngitis, acute otitis media, sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia;
genitourinary tract infections 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 whooping cough (treatment and prevention).

Pharmacological effect

Pharmacological action – antibacterial.

Pharmacodynamics

Macropen® is a macrolide antibiotic that inhibits the synthesis of proteins in bacterial cells; it has a bacteriostatic effect in small doses and a bactericidal effect in large doses. Reversibly binds to the 50S subunit of the bacterial ribosomal membrane. 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 fairly 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, achieved 1–2 hours after oral administration.

High concentrations of midecamycin and midecamycin acetate are created in internal organs (especially in lung tissue, parotid and submandibular glands) and skin.

The MIC is maintained for 6 hours. T1/2 is approximately 1 hour. 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 in the bile and to a lesser extent (about 5%) by the kidneys.

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

Special instructions

During long-term therapy, the activity of liver enzymes should be monitored, especially in patients with impaired liver function.

As with any other antimicrobial drug, long-term treatment may lead to overgrowth of resistant bacteria.

Prolonged diarrhea may indicate the development of pseudomembranous colitis.

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

Active ingredient

Midecamycin

Composition

1 Film-coated tablet:

Active ingredient:

midecamycin – 421 mg (corresponds to 400 mg of midecamycin with an activity of 1000 μg/mg);

Excipients: potassium polacriline; magnesium stearate; talc; MCC

Film shell: methacrylic acid copolymer; macrogol; titanium dioxide; talc.

Pregnancy

The use of the drug during pregnancy is indicated only in cases where the potential benefit to the mother outweighs the risk to the fetus.

Nursing mothers should stop breastfeeding during treatment with Macropen®, because the drug is excreted into breast milk.

Contraindications

hypersensitivity to midecamycin/midecamycin acetate and any other components of the drug;
severe liver failure;
children under 3 years of age (for tablets).

With caution: pregnancy; lactation period; the presence of an allergic reaction to acetylsalicylic acid.

Side Effects

From the gastrointestinal tract: decreased appetite, stomatitis, nausea, vomiting, diarrhea, feeling of heaviness in the epigastrium, increased activity of liver transaminases, hyperbilirubinemia, jaundice.

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

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

Other: weakness.

Interaction

When ergot alkaloids or carbamazepine are taken simultaneously with Macropen®, their metabolism in the liver decreases and serum concentration increases. Therefore, caution should be used when taking these drugs together.

Does not affect the pharmacokinetic parameters of theophylline.

When using Macropen® simultaneously with cyclosporine or anticoagulants (warfarin), the elimination of the latter slows down.

Overdose

Symptoms (possible): nausea, vomiting.

Treatment: symptomatic.

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

3 years

Manufacturer

KRKA dd Novo Mesto, Slovenia