Макропен®

General characteristics. Structure:

Active ingredient: 200 mg of a midekamitsin acetate (that corresponds to 175 mg of a midekamitsin of acetate in 5 ml of a supenziya).

Excipients: methylparahydroxybenzoate, пропилпарагидроксибензоат, citric acid, sodium hydrophosphate, anhydrous, fragrance banana, powder, dye sunset yellow FCF, E110, gipromelloz, defoaming agent silicone, sodium saccharinate, Mannitolum.

Antibiotic of a broad spectrum of activity of group of macroleads to which sensitivity is shown by many causative agents of infections, including intracellular. It is applied at treatment of many infectious and inflammatory diseases. In the form of suspensions it is applied to children.

Pharmacological properties:

Pharmacodynamics. Macrofoams - the makrolidny antibiotic inhibiting protein synthesis of bacterial cells possesses bacteriostatic action in low doses, in big - bactericidal. Reversibly communicates with 50S in subunit of a ribosomalny membrane of bacteria.

It is effective concerning intracellular microorganisms: Mycoplasma spp., Chlamydia spp., Legionella spp., Ureaplasma urealyticum; gram-positive bacteria: Streptococcus spp., Staphylococcus spp., Corynebacterium diphtheriae, Listeria monocytogenes, Clostridium spp. and some gram-negative bacteria: Neisseria spp., Moraxella catarrhalis, Bordetella pertussis, Helicobacter spp., Campylobacter spp., Bacteroides spp.

Pharmacokinetics. After intake drug is quickly and rather fully absorbed from the digestive tract (DT).

The maximum concentration of a midekamitsin and midekamitsin of acetate in serum make 0,5-2,5 mkg/l and 1,31-3,3 mkg/l respectively and are reached in 1-2 hours after intake.

High concentration of a midekamitsin and midekamitsin of acetate are created in internals (especially in tissues of lungs, parotid and submaxillary glands) and skin. The Minimum Overwhelming Concentration (MOC) remains during 6 h. The elimination half-life makes about 1 hour. Communication with proteins - 47% of a midekamitsin and 3-29% of metabolites.

Drug is metabolized in a liver with formation of 2 active metabolites having antimicrobic activity. It is removed with bile and to a lesser extent (about 5%) kidneys.

At cirrhosis: significantly plasma concentration, the area under a curve "concentration time" and an elimination half-life increase.

Indications to use:

In the form of suspension it is applied to children. The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

1.infektsii respiratory tracts, including caused by atypical activators (mycoplasmas, legionella, chlamydias and Ureaplasma urealyticum): tonzillofaringit, acute average otitis, sinusitis, an exacerbation of chronic bronchitis, community-acquired pneumonia;
2.infektsii an urinogenital path, caused by activators: mycoplasmas, legionella, chlamydias and Ureaplasma urealyticum;
3.infektsii skin and hypodermic cellulose;
4.dlya treatments of the enterit caused by sort Campylobacter bacteria;
5.lecheniye and prevention of diphtheria and whooping cough.

Route of administration and doses:

The scheme of purpose of suspension for children (a daily dose of 50 mg/kg of body weight at 2-hkratny reception):

Children	Suspension of 175 mg / 5 ml
to 30 kg (~ 10 years)	22,5 ml (787,5 mg) x 2
to 20 kg (~ 6 years)	15 ml (525 mg) x 2
to 15 kg (~ 4 years)	10 ml (350 mg) x 2
to 10 kg (~ 1 - 2 years)	7,5 ml (262,5 mg) x 2
to 5 kg (~ 2 months)	3,75 ml (131,25 mg) x 2

Treatment duration usually makes from 7 to 14 days. Chlamydial infections are treated 14 days.

For the purpose of prevention of diphtheria: мидекамицин it is recommended in the dose of 50 mg/kg/days divided into two receptions within 7 days. The control bacteriological research after the end of therapy is recommended. For the purpose of prevention of whooping cough мидекамицин it is recommended in a dose of 50 mg/kg/days within 7-14 days in the first 14 days from the contact moment.

Suspension preparation: add 100 ml of water (boiled or distilled) to contents of a bottle and well stir up.

Before the use always to shake up!

Features of use:

At long therapy activity of liver enzymes, especially at patients with the broken function of a liver has to be controlled.

As well as when using any other germicides, prolonged treatment can lead to the excess growth of steady bacteria. Long diarrhea can indicate development of pseudomembranous colitis.

Mannitolum which is contained in Makropena (granules for preparation of suspension for intake) can be the cause of diarrhea.

In the presence of allergic reaction to acetylsalicylic acid, PO azoic dye E (dye a sunset yellow, EPO) can cause allergic reaction, up to a bronchospasm.

Use of drug during pregnancy is shown only when the potential advantage for mother exceeds risk for a fruit. Nursing mothers have to stop breastfeeding during treatment by Makropen as drug is excreted in breast milk.

It was not reported about Makropen's influence on psychophysiological reactions and ability to driving and other mechanisms.

Side effects:

From digestive tract: a loss of appetite, stomatitis, nausea, vomiting and diarrhea, heavy feeling in epigastriums, increase in activity of "hepatic" transaminases and a hyperbilirubinemia, jaundice.

In rare instances heavy and long diarrhea can be observed that can indicate development of pseudomembranous colitis.

Allergic reactions:  skin rash,  small tortoiseshell,  skin  itch,  eosinophilia, bronchospasm.

Other: weakness.

Interaction with other medicines:

At a concomitant use of alkaloids of an ergot or carbamazepine with Makropen their metabolism in a liver decreases and serumal concentration increases. Therefore at a concomitant use of these drugs it is necessary to be careful.

Does not exert impact on pharmacokinetic parameters of theophylline.

At simultaneous use of Makropen with cyclosporine or anticoagulants (warfarin) removal of the last is slowed down.

Contraindications:

• Hypersensitivity to a midekamitsinu/midekamitsin to acetate and any other components of drug;

• heavy liver failure.

With an otsrozhnost appoint during pregnancy and a lactation.

Overdose:

There are no messages on the cases of serious overdose caused by Makropen. Symptoms are possible: nausea, vomiting.

Treatment: symptomatic.

Storage conditions:

To store granules for preparation of suspension at a temperature not above 25 °C. The prepared suspension is suitable within 14 days in the refrigerator or 7 days at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Granules for preparation of suspension for intake, 175 mg / 5 ml. 20 g of granules in a bottle of dark glass (type Sh) with an aluminum cover with control of the first opening. On 1 bottle complete with the dosing spoon from polypropylene in a pack cardboard together with the application instruction.