Macrotussin

Macrotussin is a suspension for internal reception, which is used to treat cough and cold.

Indications Macrotussin

Among the indications of infection and inflammation in the airways, provoked by microbes, erythromycin-sensitive substances (in these diseases, cough is also observed):

• acute form of laryngitis;
• bronchitis with tracheitis;
• pneumonia;
• chronic bronchitis in the acute stage;
• chronic obstructive pulmonary pathology in the stage of infectious exacerbation;
• developing as a result of cystic fibrosis infectious complications;
• whooping cough with paracismus and diphtheria (in the latter case also for removal of bacterial carriers);
• purulent form of sinusitis;
• removal of carriers of pertussis.

Release form

Produced in the form of bottles with a volume of 120 or 180 ml. One bottle in a package, complete with a spoon-dispenser.

Pharmacodynamics

The combination medicine, its effect is conditioned by the properties of the constituent components.

Erythromycin is a macrolide antibiotic and acts by inhibiting the process of protein biosynthesis in sensitive microbes. This occurs as a result of the connection with the 50S ribosomal subunits. This process leads to suppression of growth processes and reproduction of pathogenic organisms.

Erythromycin also has bacteriostatic properties. Among the microorganisms, which are affected - streptococci and staphylococci. In addition, strains that produce penicillinase (excluding MRSA strains), diphtheria corynebacterium, listeria monocytogenes, clostridia, legionella, Bordetella spp., Neisseria spp., Influenza rod, moracell katalis, and Campylobacter vegini.

Erythromycin actively affects intracellular pathogens - such as mycoplasma, pale treponema, chlamydia and rickettsia. However, it does not affect gram-negative bacteria (such as Escherichia coli, pseudomonas, shigella, etc.).

Guaifenesin is a substance that encourages expectoration. Improves the secretion of elements of bronchial mucus, having a weak viscosity, and besides it helps depolymerize acidic glycosaminoglycans and increases the activity of ciliated epithelial cilia in the respiratory tract. It reduces the adhesion of sputum, thereby diluting it and facilitating the release of respiratory organs, and in addition reduces the surface tension. In some cases, the drug may cause a mild sedative effect.

Pharmacokinetics

After oral administration, erythromycin stearate unchanged passes through the stomach into the duodenum intestine. The stearic residue in this case protects the erythromycin base from the action of hydrochloric acid on it. Due to hydrolysis of this substance in the duodenum the separate components - erythromycin and octadecanoic acid are formed.

Absorption of erythromycin occurs through the intestine. The bioavailability of the active ingredient in the case of erythromycin stearate is higher than that of erythromycin alone. After consuming 500 mg of medication peak concentration is 2.4 μg / ml, it is reached in 2-4 hours.

The half-life of erythromycin is about 1.9-2.4 hours, in the therapeutic concentration it remains in the body for 6-8 hours. Binding to α1-glycoproteins of blood plasma - 40-90%.

The drug effectively penetrates throughout tissues with organs (but not tissue in the central nervous system). Like other macrolide antibiotics, erythromycin has a high degree of passage into the cells. It should be noted that at the same time, the intracellular accumulation of antibiotic is capable of 4-24 times higher than in plasma.

Part of erythromycin is metabolized in the liver - the mechanism of N-demethylation. Excretion occurs mainly along with bile. Unchanged in the urine is allocated only 2.5-4.5% of the drug. The active substance is able to pass through the placenta, but in the fetal blood plasma its indices are low. It is also excreted through breast milk (the level of its accumulation in milk is 5 times greater than plasma milk).

Guaifenesin is absorbed from the digestive tract after half an hour. It mainly passes into those tissues containing acidic mucopolysaccharides. Once in the body, the substance reaches a peak concentration after 1-2 hours, while maintaining therapeutic parameters for 6 hours.

The half-life of guaifenesin is approximately 1 hour.

Excretion occurs with phlegm. Through the kidneys, unchanged decomposition products are deduced. Guaifenesin is also capable of giving a pink tint to the urine.

Dosing and administration

Suspension with the drug should be shaken carefully before use. Drink the medicine at least half an hour before meals or 2 hours after that. Dosages are prescribed depending on the severity of the course of the disease, as well as the age of the patient. Take Macrotussin four times a day.

In the case of a mild or mild disease, a single dose is:

• children 6-7 years - 10 ml (2 tablespoons);
• children 7-9 years of age - 12.5 ml (2.5 tablespoons);
• children 9+ years and adults - 15 ml (3 tablespoons).

The duration of the treatment course is determined by the doctor (depends on the nature of the pathology, indications and age of the patient). On average, it lasts about 7-10 days.

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Use Macrotussin during pregnancy

Information on the effects of medication on the body of a pregnant woman is not enough, so you can use it during this period only with the appointment of a doctor and under his supervision.

If you want to take Macrotussin during the lactation period, you should stop breastfeeding for the duration of the procedure.

Contraindications

Among the contraindications:

• individual intolerance to erythromycin and other macrolides, as well as any other elements of the drug;
• children under the age of 6;
• SUIQT (congenital or acquired) on the ECG;
• hepatic failure in severe form.

It is also forbidden to take in combination with such substances as pimozide, astemizole, and also terfenadine, and in addition ergotamine and cisapride with dihydroergotamine.

Side effects Macrotussin

Adverse reactions are observed occasionally, mainly in the case of an overdose. Symptoms include diarrhea, vomiting with nausea, abdominal pain, pancreatitis, as well as anorexia, a pseudomembranous form of colitis, a disorder in the liver (hepatocellular or cholestatic form of hepatitis, as well as a cholestatic form of jaundice), a parenchymal jade and agranulocytosis.

Tinnitus and hearing loss may also occur - these manifestations occur after the drug is withdrawn.

Due to the use of Macrotussin, the heart rate may increase, and the QT interval may lengthen. In some cases, ventricular arrhythmias occur (sometimes an arrhythmia in the form of pirouette tachycardia), cough increases, a feeling of general weakness, confusion develops, nightmares, hallucinations and dizziness occur.

The course of myasthenia gravis may also worsen. Among the reactions due to the chemotherapeutic effect: superinfection, which is provoked by resistant to LS or fungi bacteria.

In patients with intolerance to guaifenesin or macrolide antibiotics, allergies may develop-rashes, itching, urticaria, malignant exudative or polyformiform erythema, Lyell's syndrome, and anaphylaxis.

Occasionally, with the use of Macrotussin, severe reactions of intolerance can develop - among them Quincke's edema, anaphylaxis, and also the swelling of soft tissues on the face. With these symptoms, it is required to take glucocorticoids, as well as adrenaline, to introduce fluid infusion and to ensure air permeability through the respiratory organs.

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Interactions with other drugs

Since erythromycin is mainly metabolized in the liver with the help of the P450 hemoprotein system, it is able to interact with certain medications. The nature of its effects is as follows: an increase in the rifabutin, phenytoin, tacrolimus, and in addition methylprednisolone, hexobarbital, alfentanil, caffeine, zopiclone, aminophylline, and valproic acid and theophylline in the blood plasma. As a consequence, their toxicity also increases, so you need to lower the dosage of these substances and monitor their level in the blood serum.

It is forbidden to combine Macrotussin with OCS inhibitors (such as fluoxetine and paroxetine with sertraline), since the concentration of the latter in the plasma is significantly increased, as a result of which serotonin intoxication may develop.

When combined with digoxin, the absorption of the latter increases and its concentration in the blood serum increases. The combination with cyclosporine also provokes an increase in its concentration, which increases the nephrotoxicity of the substance.

In the case of a compound with carbamazepine, the rate of its metabolism in the liver decreases. If you need to take these drugs at the same time, you may need a 50% reduction in the dosage of carbamazepine.

The compound with quinidine as well as cisapride and procainamide also increases the levels of these substances in the blood serum, resulting in the development of ventricular tachycardia or the prolongation of the QT interval.

Due to increased concentrations in the blood of terfenadine and astemizole in combination with Macrotussin, severe heart rhythm disorders can occur.

Due to an increase in the indices of agents slowing GABA-KoA-reductase (such as lovastatin or simvastatin), rhabdomyolysis may develop (mainly after the completion of treatment with erythromycin).

Since the medicine increases the strength of the effect on the body of syyafil, a lower dosage of the latter is required.

It is forbidden to combine chloramphenicol (antagonism), drugs that increase the acidity of the stomach, and acidic drinks, because they reduce the activity of erythromycin. In the case of combination with OK, the risk of hepatotoxicity increases.

The compound with calcium antagonists (such as verapamil or felodipine) reduces the rate of their elimination, and also increases the effectiveness of these drugs. Due to their combination with erythromycin, bradyarrhythmia, hypotension or lactic acidosis may develop.

Simultaneous reception with sulfanilamide drugs, tetracyclines, and streptomycin enhances the effectiveness of Macrotussin.

Laboratory studies have shown that there is antagonism between erythromycin, as well as clindamycin and lincomycin, which is why it is forbidden to combine these medicines.

Patients with intolerance to aspirin may develop an allergy to the drug, since its filler is tartrazine.

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Storage conditions

It is necessary to keep the medicine under standard conditions, in a place that is closed from children. The temperature conditions are a maximum of 25 ° C.

Shelf life

Macrotussin is allowed to be used for 2 years from the date of manufacture of the medicine.