Makrotussin

General characteristics. Structure:

Main physical and chemical properties: drug after hashing represents suspension of yellow or yellow-orange color with a specific smell;
structure: 5 ml of suspension contain 125 mg of erythromycin of stearate in terms of erythromycin and 75 mg of a guayfenezin; excipients: sodium carboxymethylcellulose, fragrance food fruit, methylparahydroxybenzoate, tartrazine or dye евросерт "Sunset", sodium saccharinate, sugar, the water purified.

Pharmacological properties:

Pharmacodynamics. The combined drug which effect is caused by effects of the components which are its part. Erythromycin belongs to antibiotics from group of macroleads. The mechanism of action is caused by delay of biosynthesis of proteins of microorganisms, sensitive to them, owing to linkng with 50S-subunits of ribosomes that leads to delay of growth and reproduction of bacteria. Erythromycin works bacteriostatically. The range of antibacterial action includes: Streptococcus spp., Staphylococcus spp., including those which develop a penicillinase, except MRSA strains, Corynebacterium diphtheriae, Listeria monocytogenes, Clostridium spp., Bordetella spp., Legionella spp., Neisseria spp., Haemophilus influenzae, Moraxella catarrhalis, S. jejuni. Erythromycin also shows high activity concerning Mycoplasma spp., Treponema pallidum, Chlamydia spp., Rickettsia spp. Erythromycin does not affect gram-negative microorganisms (E.coli, Pseudomonas spp., Shigella spp., etc.). Guayfenezin treats expectorants. Stimulates secretion of components of bronchial slime with low viscosity, depolymerizes acid mucopolysaccharides and increases activity of cilia of a ciliary epithelium of respiratory tracts. Surface intention and adhesive properties of a phlegm reduces that reduces its viscosity and facilitates evacuation from respiratory tracts. Can have weak sedative effect.

Pharmacokinetics. After erythromycin intake stearate passes through a stomach in a duodenum in an invariable look, at the same time the stearin rest protects the erythromycin basis from effect of hydrochloric acid. In an erythromycin duodenum stearate is hydrolyzed with formation of the basis of erythromycin and stearic acid. Erythromycin in intestines is soaked up. System bioavailability of erythromycin when using erythromycin of stearate is higher, than at basis erythromycin use. Peak concentration of erythromycin in blood makes 2,4 mkg/ml after reception of 500 mg, time of achievement of peak concentration makes 2-4 h. The elimination half-life of erythromycin makes 1,9-2,4 h, at the same time therapeutic concentration in blood are kept by 6-8 h. Erythromycin for 40-90% communicates with α1-гликопротеинами a blood plasma. Drug well gets into all bodies and body tissues, except TsNS fabrics. High extent of intracellular penetration is characteristic of an eritroromitsin, as well as of other makrolidny antibiotics, at the same time concentration of an antibiotic in a cell can exceed plasma at 4-24 time. Erythromycin is partially metabolized by a liver by N-demethylation, removed preferential with bile, with urine in not changed look only 2,5-4,5% of drug are removed. Erythromycin gets through a placental barrier, but its concentration in a fruit blood plasma very low, is actively excreted with maternal milk, concentration of an antibiotic in milk can exceed plasma by 5 times. Guayfenezin quickly (in 30 min.) is absorbed from digestive tract. Preferential gets into the fabrics containing acid mucopolysaccharides. After peroral introduction the maximum concentration is reached in 1-2 h, and therapeutic concentration remains during 6 h. The elimination half-life of a guayfenezin makes about 1 h. It is excreted with a phlegm, removed by kidneys in the form of metabolites, and also in not changed look. Guayfenezin can paint urine in pink color.

Indications to use:

The infectious and inflammatory diseases of a respiratory organs caused by microorganisms, sensitive to erythromycin, which are followed by cough - acute laryngitis, tracheitis, bronchitis, pneumonia, an exacerbation of chronic simple bronchitis and an infectious exacerbation of an obstructive disease of lungs, infectious complications at a mucoviscidosis, diphtheria (also for sanitation of bacillicarriers), whooping cough and parawhooping cough; also Makrotussin shown for treatment of purulent sinusitis and for sanitation of carriers of V. of pertussis.

Route of administration and doses:

Before each use Makrotussin's suspension needs to be shaken up. Drug needs to be used not earlier than in 30 min. prior to meal or in 2 h after meal. The dose of drug is established individually taking into account age and weight of a condition of the patient. Makrotussin accept 4 times a day. Drug is dosed by means of the measured spoon enclosed in packaging. At easy and moderately severe disease the single dose makes:

Age, years	Dose of drug, ml	Route of administration
2-3	7,5	1,5 measured spoons
4-6	10	2 measured spoons
7-8	12,5	2,5 measured spoons
9 is also more senior, adults	15	3 measured spoons

Features of use:

It is not necessary to exceed the recommended drug doses. Owing to the high content of sucrose drug should be used with care to the persons suffering from a diabetes mellitus. It is not recommended to wash down suspension with milk and dairy products, and also fruit juice or acid drinks. Drug with care is appointed to persons with an abnormal liver function.

Use at pregnancy and during feeding by a breast. Drug is appointed to pregnant women only when the expected advantage for mother exceeds potential risk for a fruit. At the use of drug in the period of a lactation, it is necessary to stop feeding by a breast for all term of treatment by Makrotussin.

Influence on ability to drive the car and to work with mechanisms. In therapeutic doses drug does not influence ability to manage vehicles and to work with mechanisms that move.

Side effects:

In rare instances, as a rule, at exceeding of the recommended doses, nausea, vomiting, an abdominal pain, a diarrhea, an abnormal liver function in the form of increase in level of serumal transaminases can be noted. At patients with hypersensitivity to makrolidny antibiotics or a guayfenezin development of allergic reactions is possible. In isolated cases at Makrotussin's use, as well as other macroleads, development of heavy reactions of hypersensitivity, including a Quincke's disease and acute anaphylaxis is possible. In this case it is necessary to appoint adrenaline and glucocorticoids, intravenous infusion of liquid, to provide passability of respiratory tracts.

Interaction with other medicines:

Makrotussin it is not necessary to apply along with imatinibiny, colchicine, GMG-KOA-reduktazy inhibitors (statines), cyclosporine derivative of ergotamine because of delay of hepatic metabolism of the above-stated medicines that leads to sharp increase in their plasma concentration and toxic action. Also it is not necessary to apply Makrotussin along with the anti-arrhythmic drugs IA and III of a class, terfenadiny, astemizoly, tsizapridy, Pimozidum, ftorkhinolovy antibacterial drugs because of strengthening of prolongation of an interval of QT on an ECG that can lead to gastric tachycardia of torsades de pointes and death. It is impossible to combine treatment by Makrotussin with inhibitors of the return serotonin reuptake (пароксетин, fluoxetine, sertraline) owing to substantial increase of plasma concentration of the last that can lead to development of a serotoninovy syndrome. With care appoint Makrotussin the patient accepting foxglove glycosides, peroral anticoagulants, carbamazepine, буспирон, clozapine, Valproatums, benzodiazepine derivatives, mifepristone, феллодепин, исрадипин, никардипин, xanthine derivatives including theophylline, and also sildenafit because of increase in plasma concentration of the last. If such combinations are necessary, then reduce a dose of medicine, and carry out treatment, controlling plasma concentration. Existence of antagonism between erythromycin, lincomycin and clindamycin therefore these drugs should not be used at the same time is in vitro shown. The drug filler, tartrazine, can cause allergic reactions in persons with intolerance of acetylsalicylic acid.

Contraindications:

Hypersensitivity to erythromycin, a guayfenezin and other components of drug, age up to 2 years, the inborn and acquired syndromes of the prolonged QT interval on an ECG.

Overdose:

Development of nausea, vomiting, diarrhea which are eliminated after drug withdrawal, and also tranzitorny decrease in hearing, disturbance of a cordial rhythm is possible. There is no specific antidote, a symptomatic treatment. Erythromycin is not removed from an organism at a hemodialysis or peritoneal dialysis.

Storage conditions:

To store at a temperature from +15 °C to +25 °C. To store in the place, unavailable to children. A period of validity — 2 years. The deadline of the validity is specified on packaging after words: "To use to..."

Issue conditions:

According to the recipe

Packaging:

Bottles on 120 ml and 180 ml.