Macrotussin

Macrotussin is a suspension for internal use, which is used to treat coughs and colds.

Indications Macrotussin

Indications include infections and inflammations in the respiratory tract caused by microbes sensitive to the substance erythromycin (cough is also observed in these diseases):

• acute laryngitis;
• bronchitis with tracheitis;
• pneumonia;
• chronic bronchitis in the acute stage;
• chronic obstructive pulmonary disease in the stage of infectious exacerbation;
• infectious complications developing as a result of cystic fibrosis;
• whooping cough with parapertussis and diphtheria (in the latter case also to remove carriers of bacteria);
• purulent form of sinusitis;
• removal of carriers of the whooping cough bacillus.

Release form

Available in 120 or 180 ml bottles. One bottle per package, complete with a dosing spoon.

Pharmacodynamics

The drug is a combination drug, its effect is determined by the properties of its constituent components.

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

Erythromycin also has bacteriostatic properties. Among the microorganisms that are affected are streptococci and staphylococci. In addition, there are also strains that produce penicillinase (excluding MRSA strains), diphtheria corynebacterium, listeria monocytogenes, clostridia, legionella, Bordetella spp., Neisseria spp., influenza bacillus, moraxella catarrhalis, and campylobacter jeuni.

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

Guaifenesin is a substance that promotes expectoration. It improves the process of secretion of bronchial mucus elements that have low viscosity, and in addition, it helps to depolymerize acidic glycosaminoglycans and increases the activity of ciliated epithelial cilia in the respiratory organs. It weakens the adhesion of sputum, thereby liquefying it and facilitating the process of exiting the respiratory organs, and in addition, it reduces surface tension. In some cases, the drug can cause a weak sedative effect.

Pharmacokinetics

After oral administration, erythromycin stearate passes unchanged through the stomach into the duodenum. The stearic residue in this case protects the erythromycin base from the effects of hydrochloric acid. As a result of hydrolysis of this substance in the duodenum, separate components are formed - erythromycin and octadecanoic acid.

Erythromycin is absorbed through the intestines. The bioavailability of the active component in the case of erythromycin stearate exceeds similar indicators when using just erythromycin. After taking 500 mg of the drug, the peak concentration is 2.4 mcg / ml, it is achieved in 2-4 hours.

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

The drug effectively penetrates everywhere into tissues with organs (but not tissues in the central nervous system). Like other macrolide antibiotics, erythromycin has a high degree of penetration into cells. It should be noted that the intracellular accumulation of the antibiotic can exceed the similar indicator in plasma by 4-24 times.

Part of erythromycin undergoes metabolism in the liver - the N-demethylation mechanism. Excretion occurs mainly with bile. Only 2.5-4.5% of the drug is excreted unchanged in the urine. The active substance is able to pass through the placenta, but its levels in the fetal blood plasma are low. It is also excreted through breast milk (its accumulation level in milk can be 5 times higher than in plasma).

Guaifenesin is absorbed from the gastrointestinal tract after half an hour. It mainly passes into those tissues that contain acidic mucopolysaccharides. Once in the body, the substance reaches peak concentration after 1-2 hours, maintaining therapeutic indicators for 6 hours.

The half-life of guaifenesin is approximately 1 hour.

Excretion occurs with sputum. Unchanged decay products are excreted through the kidneys. Guaifenesin can also give urine a pink tint.

Dosing and administration

The suspension with the medicine must be shaken thoroughly before use. The medicine must be taken at least half an hour before meals or 2 hours after. Dosages are prescribed depending on the severity of the disease, as well as the age of the patient. Macrotussin should be taken four times a day.

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

• children 6-7 years old – 10 ml (2 spoons);
• children 7-9 years old – 12.5 ml (2.5 spoons);
• children 9+ years old and adults – 15 ml (3 spoons).

The duration of the treatment course is determined by the doctor (depending 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

There is insufficient information about the effect of the drug on the body of a pregnant woman, so it can only be used during this period with a doctor’s prescription and under his supervision.

If you need to take Macrotussin during lactation, you should stop breastfeeding during the course of treatment.

Contraindications

Among the contraindications:

• individual intolerance to erythromycin and other macrolides, as well as any other components of the drug;
• children under 6 years of age;
• QT (congenital or acquired) on ECG;
• severe liver failure.

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

Side effects Macrotussin

Side effects are rare, mostly in case of overdose. Symptoms include diarrhea, vomiting with nausea, abdominal pain, pancreatitis, as well as anorexia, pseudomembranous colitis, liver dysfunction (hepatocellular or cholestatic hepatitis, as well as cholestatic jaundice), parenchymatous nephritis, and agranulocytosis.

Tinnitus and hearing loss may also occur; these symptoms disappear after discontinuing the drug.

As a result of using Macrotussin, the heart rate may increase, the QT interval may lengthen. In some cases, ventricular arrhythmia may occur (sometimes arrhythmia of the torsades de pointes type), coughing may increase, a feeling of general weakness, confusion, nightmares, hallucinations and dizziness may develop.

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

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

Rarely, severe intolerance reactions may develop when using Macrotussin, including Quincke's edema, anaphylaxis, and swelling of the soft tissues on the face. These symptoms require glucocorticoids, adrenaline, fluid infusion, and ensuring air flow through the respiratory system.

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Interactions with other drugs

Since erythromycin is mainly metabolized in the liver with the participation of the hemoprotein P450 system, it can interact with some drugs. The nature of its effect is as follows: an increase in the indicators of rifabutin, phenytoin, tacrolimus, and in addition methylprednisolone, hexobarbital, alfentanil, caffeine, zopiclone, aminophylline, as well as valproic acid and theophylline in the blood plasma. As a result, their toxicity also increases, so it is necessary to reduce the dosage of these substances and monitor their level in the blood serum.

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

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

When combined with carbamazepine, its rate of metabolism in the liver decreases. If it is necessary to use these drugs simultaneously, a 50% reduction in the dosage of carbamazepine may be required.

Concomitant use with quinidine, as well as cisapride and procainamide, also increases serum levels of these substances, which may result in ventricular tachycardia or prolongation of the QT interval.

Due to increased blood concentrations of terfenadine and astemizole in combination with Macrotussin, severe cardiac arrhythmias may occur.

Due to increased levels of GABA-CoA reductase inhibitors (such as lovastatin or simvastatin), rhabdomyolysis may develop (mainly after completion of treatment with erythromycin).

Since the drug increases the strength of the effect of sidenafil on the body, a reduction in the dosage of the latter is required.

Combination with chloramphenicol (antagonism occurs), drugs that increase stomach acidity, and acidic drinks is prohibited, because they reduce the activity of erythromycin. In case of combination with OC, the risk of hepatotoxicity increases.

Combination with calcium antagonists (such as verapamil or felodipine) reduces the rate of their excretion and increases the effectiveness of these drugs. As a result of their combination with erythromycin, bradyarrhythmia, hypotension or lactic acidosis may develop.

Concomitant use with sulfonamide drugs, tetracyclines, and streptomycin increases the effectiveness of Macrotussin.

Laboratory studies have shown that there is antagonism between erythromycin, as well as clindamycin and lincomycin, and therefore these drugs should not be combined.

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

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Storage conditions

The medicine should be kept in standard conditions, in a place closed to children. Temperature conditions – maximum 25°C.

Shelf life

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