Pharmacological properties of the drug Macropen
Macrolide antibiotic. Inhibits protein synthesis in microorganisms. Effective against intracellular pathogens (mycoplasma, legionella, chlamydia, Ureaplasma urealyticum ), gram-positive bacteria (streptococci, staphylococci, Corynebacterium diphtheriae, Listeria monocytogenes, Erysepelothrix, Clostridium spp .) and some gram-negative bacteria ( Neisseria spp., Moraxella catarrhalis, Bordetella pertussis , Helicobacter spp., Campylobacter spp., Haemophilus influenzae, Bacteroides spp .). After oral administration, it is quickly and completely absorbed, reaching maximum plasma concentrations 1–2 hours after administration. Higher concentrations of the antibiotic are created in inflamed tissues than in the blood serum; high concentrations of medicamycin are observed in bronchial secretions and skin. It is excreted in the form of metabolites, mainly in bile, and in small quantities in urine.
Indications:
Macropen is used for the treatment of infectious and inflammatory diseases caused by pathogens sensitive to midecamycin:
- infectious diseases of the respiratory, urinary and birth tract caused by chlamydia, mycoplasma, legionella and ureaplasma (Mycoplasma spp., Chlamydia spp., Legionella spp. and Ureaplasma urealyticum);
- infections of the respiratory tract and ENT organs (bronchitis, pneumonia, tonsillitis, otitis, sinusitis), genitourinary organs (including nonspecific urethritis), skin and subcutaneous tissue, in patients for whom penicillin antibiotics are contraindicated (with hypersensitivity to penicillin , benzylpenicillin, etc.);
- enteritis and gastroenteritis caused by Campylobacter (bacteria of the genus Campylobacter);
- diphtheria and whooping cough (treatment and prevention);
- trachoma, brucellosis, Legionnaires' disease, gonorrhea, syphilis, scarlet fever, erysipelas (reserve antibiotic).
Use of the drug Macropen
The suspension is intended for use in children. Dosing recommendations are given in the table below.
Body weight, kg (approximate age) | Suspension dosing |
Up to 30 (10 years) | 22.5 ml (787.5 mg) 2 times a day |
Under 20 (6 years) | 15 ml (525 mg) 2 times a day |
Up to 15 (4 years) | 10 ml (350 mg) 2 times a day |
Up to 10 (1–2 years) | 7.5 ml (262.2 mg) 2 times a day |
Up to 5 (2 months) | 3.75 ml (131.25 mg) 2 times a day |
To prepare the suspension, add 100 ml of boiled water to the contents of the bottle and mix thoroughly. Adults and children aged 10 years and older (body weight from 30 kg) are prescribed a dose of 400 mg 3 times a day. The maximum daily dose for adults is 1600 mg, for children - 30-50 mg/kg, divided into 2 doses. For severe infections, the daily dose is divided into 3 doses. The course of treatment usually lasts 7–10 days, for chlamydial infection - 14 days.
Macropen 400 mg No. 16 Tablets
Trade name: Macropen® International nonproprietary name: Midecamycin Dosage form: Film-coated tablets, 400 mg Composition: One tablet contains the active substance - midecamycin 421.0 mg (in terms of midecamycin content 950 μg/mg), excipients: potassium polakrilin, talc, microcrystalline cellulose, magnesium stearate, film shell: copolymer of basic butylated methacrylate, polyethylene glycol, titanium dioxide E 171, talc. Description: Round, slightly biconvex, white film-coated tablets, with a chamfer and a score on one side. Pharmacotherapeutic group: Antimicrobial drugs for systemic use. Macrolides.
Pharmacological properties:
Pharmacokinetics Absorption. Medicamycin and mediamycin acetate are rapidly and relatively well absorbed and reach maximum serum concentrations of 0.5 mcg/ml to 2.5 mcg/ml and 1.31 mcg/ml to 3.3 mcg/ml, respectively, within 1 to 2 hours. Eating slightly reduces maximum concentrations, especially in children (4 to 16 years). Therefore, it is recommended to take midecamycin before meals. Distribution.Midecamycin penetrates well into tissues, where it reaches more than 100% concentration than in the blood. High concentrations were found in bronchial secretions and in the skin. The volume of distribution of midecamycin acetate is large: 228 - 329 liters in healthy volunteers. 47% of midecamycin and 3 - 29% of metabolites are protein bound. Midecamycin acetate is excreted into breast milk. After a dose of 1200 mg/day, 0.4 mcg/ml - 1.7 mcg/ml midecamycin acetate is detected in breast milk. Metabolism and removal. Midecamycin is primarily metabolized into active metabolites in the liver. It is excreted primarily in bile, and only about 5% in urine. Significant increases in maximum serum concentrations, area under the curve, and half-life may be observed in patients with cirrhosis. Pharmacodynamics Antibacterial action Midecamycin is a broad-spectrum macrolide antibiotic whose activity is similar to that of erythromycin. It is active against gram-positive bacteria (staphylococci, streptococci, pneumococci, Bacillus anthracis, Corynebacterium diphtheriae, and Listeria monocytogenes), against some gram-negative bacteria (Bordetella pertussis, Campylobacter, Moraxella catarrhalis and Neisseria spp.), anaerobes (Clostridium spp. and Bacteroides spp.) and other bacteria such as mycoplasma, ureaplasma, chlamydia and legionella. In vitro bacterial susceptibility to midecamycin acetate (MDM-acetate) and midecamycin (MDM) Average MIC90 (µg/ml) Bacteria MDM-acetate MDM Streptococcus pneumoniae 0.5 0.10 Streptococcus pyogenes 0.67 0.20 Streptococcus viridans 0.28 0.39 Staphylococcus a ureus 1.5 1.5 Listeria monocytogenes 2 1.5 Bordetella pertussis 0.25 0.20 Legionella pneumophila 0.1 0.12 – 1 Moraxella catarrhalis 2 — Helicobacter pylori 0.5 — Propionibacterium acnes 0.12 — Bacteroides fragilis 5.5 3.13 Mycoplasma pneumoniae 0.024 0.0078 Ureaplasma urealyticum 0.34 1. 56 Mycoplasma hominis 2.3 — Gardnerella vaginalis 0.08 — Chlamydia trachomatis 0.06 — Chlamydia pneumoniae 0.5 — Criteria for midecamycin, regarding interpretation, the MICs are the same as for other macrolides, according to NCCLS (National Committee on Clinical Laboratory Standards) standards. Bacteria are defined as sensitive if their MIC90 is ? 2 µg/ml, how resistant if their MIC90? 8 µg/ml. Antimicrobial effectiveness of metabolites Metabolites of midecamycin have a similar antibacterial spectrum as midecamycin, but their effect is somewhat weaker. Results from some animal trials have demonstrated that the efficacy of midecamycin and midecamycin acetate is better in vivo than in vitro. This is partly due to high concentrations of active metabolites in tissues. Mechanism of action. Midecamycin inhibits RNA-dependent protein synthesis at the stage of protein chain elongation. Midecamycin reversibly binds to the 50S subgroup and blocks the transpeptidation and/or translocation reaction. Due to the different structure of ribosomes, communication with the ribosomes of a eukaryotic cell does not occur. This is why the toxicity of macrolides to human cells is low. Like other macrolide antibiotics, midecamycin has a primarily bacteriostatic effect. However, it may also have a bactericidal effect, which depends on the type of bacterium, the drug concentration at the site of action, the size of the inoculum and the reproductive stage of the microorganism. In vitro activity is reduced in acidic conditions. If the pH value in the culture medium of Staphylococcus aureus or Streptococcus pyogenes increases from 7.2 to 8.0, the MIC for midecamycin is two times lower. If the pH drops, the situation is reversed. High intracellular concentrations of macrolides are achieved as a result of their good lipid solubility. This is especially important when treating infections caused by microorganisms with an intracellular development cycle, such as chlamydia, legionella and listeria. Midecamycin has been shown to accumulate in human alveolar macrophages. Macrolides also accumulate in neutrophils. While the ratio between extracellular and intracellular concentrations ranges from 1 to 10 for erythromycin, it is over 10 for newer macrolides, including midecamycin. The accumulation of neutrophils at the site of infection may further increase the concentration of macrolides in infected tissues. In vitro studies have shown that midecamycin also affects immune functions. Thus, increased chemotaxis has been established in comparison with erythromycin. Medicamycin appears to stimulate natural killer cell activity in vivo. All of these studies indicate that midecamycin affects the immune system, which may be important for the in vivo antibiotic action of midecamycin. Sustainability. Resistance to macrolides develops due to the following reasons: reduced permeability of the outer cell membrane (Enterobacter), drug inactivation (S. aureus, E. coli) and, most importantly, an altered site of action. From a geographic perspective, the prevalence of bacterial resistance to macrolides is highly variable. Resistance of methicillin-susceptible S. aureus ranges from 1% to 50%, while most methicillin-resistant S. aureus strains are also macrolide resistant. Resistance of pneumococci is mostly below 5%, but in some parts of the world it is over 50% (Japan). Resistance of Streptococcus pyogenes to macrolides ranges from 1% to 40% in Europe. Resistance develops very rarely in Mycoplasmas, Legionella and C. diphteriae. Indications for use: - infections of the respiratory tract and genitourinary tract caused by mycoplasmas, legionella, chlamydia and Ureaplasma urealyticum; - infections of the respiratory tract, skin and subcutaneous tissue and all other infections caused by bacteria sensitive to midecamycin and penicillin in patients with hypersensitivity to penicillin; — enteritis caused by bacteria of the genus Campylobacter; - treatment and prevention of diphtheria and whooping cough. Directions for use and dosage: Macropen should be taken before meals. Adults and children weighing more than 30 kg: one 400 mg tablet 3 times a day. The maximum daily dose of midecamycin for adults is 1600 mg. The duration of treatment is usually from 7 to 14 days. Chlamydial infections are treated for 14 days. Side effects: During treatment with Macropen, mild gastrointestinal disturbances (decreased appetite, stomatitis, nausea, vomiting and diarrhea) may occur. In rare cases, severe and prolonged diarrhea may occur, which may indicate the development of pseudomembranous colitis. Allergic reactions (skin rash, urticaria, itching, eosinophilia), increased transaminase activity and jaundice are also possible. Contraindications: - hypersensitivity to the active substance or auxiliary components of the drug - severe liver failure - children under 6 years of age. Drug interactions: Macrolides are known to interact with other medications. Macrolide antibiotics affect liver metabolism by inactivating cytochrome P450. Unlike erythromycin, midecamycin and midecamycin acetate do not bind to microsomal oxidases of liver cells and do not produce stable complexes with cytochrome P450. As a result, they do not affect the pharmacokinetics of theophylline. Midecamycin may increase serum levels of cyclosporine (two-fold) and prolong the elimination half-life and AUC (area under the curve) of carbamazepine. Caution is advised in patients taking carbamazepine or cyclosporine concomitantly and serum levels should be monitored whenever possible. Concomitant use of midecamycin and ergot alkaloids may cause decreased hepatic metabolism and increased serum concentrations of ergot alkaloids. Caution should be used when using warfarin concomitantly because midecamycin may slow its elimination, increasing the risk of hemorrhage. Special instructions: During long-term therapy, the activity of liver enzymes should be monitored, especially in patients with impaired liver function. As with any antimicrobial drug, long-term treatment may result in overgrowth of resistant bacteria. Prolonged diarrhea may indicate the development of pseudomembranous colitis. Pregnancy and lactation 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, as the drug is excreted into breast milk. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms. The effect of Macropen on psychophysiological reactions and the ability to drive a car and other mechanisms has not been reported. Overdose: Symptoms: When taking excess doses, nausea and vomiting may occur. Treatment: Symptomatic. Release form: Film-coated tablets, 400 mg.
Packaging: 8 tablets in a blister pack made of polyvinyl chloride and polyvinyl dichloride film and printed aluminum foil. 2 contour packages in a cardboard box along with instructions for use. Storage conditions: Store in a place protected from moisture, at a temperature not exceeding 25 0C. Keep out of the reach of children! Shelf life: 3 years. Do not use after expiration date. Conditions for dispensing from pharmacies: By prescription
Special instructions for the use of the drug Macropen
During long-term treatment, liver enzyme activity should be monitored, especially in patients with impaired liver function. Long-term use of the drug can lead to the development of superinfection. Persistent diarrhea may be a manifestation of pseudomembranous colitis. No negative effects on the fetus have been identified, however, the use of the drug during pregnancy is indicated only if the expected therapeutic effect for the expectant mother exceeds the potential risk to the fetus. Since the drug is excreted in breast milk, breastfeeding should be discontinued during treatment.
Interaction
When using the drug with carbamazepine , its transformation in the liver decreases and, accordingly, the concentration in the serum increases, which increases the risk of the toxic effects of the latter: urinary retention, ataxia, convulsions .
When using Macropen with warfarin , the risk of bleeding increases, with cyclosporine - the risk of nephrotoxicity, with ergometrine and ergotamine - peripheral vascular spasm ( ischemia and possible gangrene of the extremities).
Reviews about Macropen
Reviews about Macropen are in most cases positive . Most of them are about the use of the drug for sinusitis. High efficiency is noted - in many cases, with timely administration of the drug, the patient's condition quickly improves, and puncture can be dispensed with. Duration of treatment is from 7 to 14 days. It is important to complete the course of treatment, otherwise the “hidden” infection may become chronic.
A large number of reviews about the use of the suspension for children. Parents are satisfied with the results of the treatment: it quickly and effectively helps with coughs, especially prolonged ones. Since the treatment lasted up to 10 days, the child was given probiotics ( Linex , Bactisubtil ) in parallel. Some noted the appearance of adverse reactions in children: nausea, lethargy, vomiting. In such cases, Macropen was canceled. In any case, there is no point in drawing conclusions that the drug is not effective. It depends on the individual characteristics of the organism.
Macropen price, where to buy
This drug can be found in any pharmacy. By purchasing Macropen tablets, the price of which in Moscow pharmacies varies and ranges from 268 to 376 rubles. for 16 capsules, you can make a request on the Internet and choose a more acceptable option. The price of Macropen suspension is from 270 rubles. up to 306 rub.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Macropen granules for Prig Susp.
for internal approx. 175 mg/5 ml 115 ml JSC KRKA, d.d., Novo mesto 542 rub. order - Macropen tablets p.p.o. 400 mg 16 pcs. Merck KGaA and Co. Werk Spittal / KRKA SA, d.d.
RUR 454 order
Pharmacy Dialogue
- Macropen (tab. 400 mg No. 16)KPKA
RUB 445 order
- Macropen (susp. 175 mg/5 ml 115 ml)KPKA
530 rub. order
- Macropen (tab. 400 mg No. 16)KPKA
435 rub. order
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Pharmacy24
- Macropen 175 mg/5 ml 115 ml granules
96 UAH. order - Macropen 400 mg No. 16 tablets KRKA, d.d., Novo Mesto, Slovenia/Merck KGaA i Co., Werk Spital, Austria
106 UAH order
PaniPharmacy
- Macropen tablets Macropen tablets. p/o 400 mg No. 16 Slovenia, KRKA dd Novo Mesto
116 UAH order
- Macropen liquid Macropen granules for suspension 175 mg/5 ml 115 ml Slovenia, KRKA dd Novo Mesto
120 UAH order
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