Zosin

Zosin is a drug from the category of macrolide antibiotics.

Indications Zosina

It is used for infections that appear under the influence of bacteria that are sensitive to the drug:

• upper respiratory tract: pharyngitis with sinusitis or tonsillitis with laryngitis;
• lower respiratory tract: bronchitis, acute or chronic, as well as pneumonia;
• otitis media;
• disseminated mycobacterial infections (Mycobacterium intracellulare or Mycobacterium avium);
• lesions of the subcutaneous tissue and epidermis: furunculosis or folliculitis, as well as wounds;
• combination therapy to destroy Helicobacter pylori in individuals with gastrointestinal ulcers;
• toxoplasmosis or leprosy.

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Release form

It is produced in tablet form.

Pharmacodynamics

Clarithromycin exhibits antibacterial activity by inhibiting protein binding and synthesizing with the 50s-subunit of ribosomes of microbes with sensitivity to drugs. The substance demonstrates activity against a wide range of gram-positive and -negative aerobes with anaerobes. The MIC values of clarithromycin are often two times lower than the erythromycin MIC values. The metabolic product of clarithromycin (component 14-hydroxyclarithromycin) also has an antibacterial effect.

The drug has in vitro efficacy against the following bacteria:

• gram-positive microbes: Staphylococcus aureus (strains sensitive to methicillin have been added here), pneumococcus, pyogenic streptococcus with Streptococcus agalactiae and Listeria monocytogenes;
• gram-negative microorganisms: Moraxella catarrhalis, Legionella pneumophila, Haemophilus influenzae with Haemophilus parainfluenzae, as well as gonococci, Helicobacter pylori and whooping cough bacteria;
• mycoplasmas: ureaplasma urealyticum and mycoplasma pneumoniae;
• other bacteria: Chlamydia trachomatis, Hansen's bacillus, Mycobacterium avium, Mycobacterium fortuitum and Mycobacterium kansasi;
• anaerobes: Peptostreptococcus species, individual strains of Bacteroides fragilis, Propionibacterium acnes, Clostridium perfringens and Peptococcus species.

Clarithromycin was not carcinogenic or mutagenic in tests. The Ames test for clarithromycin metabolites was negative.

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Pharmacokinetics

Clarithromycin is rapidly absorbed within the gastrointestinal tract after oral administration. Bioavailability is 55%. Food does not affect the bioavailability of the drug.

The active element with its metabolic product (14-hydroxyclarithromycin) is distributed in a large number of tissues and fluids. The drug undergoes extensive metabolic processes in the liver and is then excreted with bile.

Serum Cmax values develop after 120 minutes. Stable plasma Cmax levels of clarithromycin are recorded after 2-3 days and are approximately 1 mcg/ml after administration of 0.25 g of the substance at 12-hour intervals, and 3-4 mcg/ml after administration of 0.5 g of the drug at 8-hour intervals.

The half-life of the drug is approximately 3-4 hours when using the first of the above methods, and 5-7 hours when using the second. When using 0.25 g of the drug at 12-hour intervals, 14-hydroxyclarithromycin acquires a constant Cmax value of approximately 0.6 mcg/ml and a half-life of approximately 5-6 hours. When using 0.5 g of the drug at 8-12-hour intervals, the Cmax level of 14-hydroxyclarithromycin is approximately 1 mcg/ml, with a half-life of approximately 7-9 hours.

When 0.25 g of clarithromycin is administered at 12-hour intervals, 20% of the dose is excreted in the urine (in an unchanged state), and when 0.5 g of the substance is used at 12-hour intervals, this figure is approximately 30%. Excretion of 14-hydroxyclarithromycin is 10% or 15% (use, respectively, of 0.25 or 0.5 g of the drug at 12-hour intervals).

Clarithromycin is excreted in breast milk.

The half-life is increased in people with renal impairment.

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Dosing and administration

Teenagers aged 12 and over and adults should take the medicine twice a day, in a 0.25 g portion, with a 12-hour interval. It is possible to increase the dosage to 0.5 g twice a day (in severe forms of the disease). The treatment cycle is 7-14 days.

For ulcers affecting the intestine, it is necessary to administer 0.5 g of the drug 3 times a day, in combination with 40 mg of omeprazole (once a day). The cycle lasts 2 weeks.

Children aged 0.5-12 years should be given 7.5 mg/kg of the substance at 12-hour intervals over a 5-10-day course.

People with severe renal insufficiency require dose adjustment. For CC values less than 30 ml/min, the dosage is 0.25 g, 1 time (mild or moderate damage) or 2 times a day (severe stages).

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Use Zosina during pregnancy

It is prohibited to use Zosin during breastfeeding or pregnancy. The only exceptions are situations when the probable benefit from treatment is more expected than the risk of complications.

Contraindications

Contraindicated for use in people with severe intolerance to clarithromycin or other macrolides.

It is prohibited to combine the drug with terfenadine, ergot alkaloids, pimozide or cisapride.

Side effects Zosina

Often the drug is tolerated without complications.

Side effects include headaches, diarrhea, vomiting, stomatitis, abdominal pain and nausea.

Occasionally, signs of allergy are observed, ranging from a mild epidermal rash and urticaria to anaphylaxis. Thrombocytopenia or Stevens-Johnson syndrome may occur. Taste bud dysfunction is also possible.

Transient negative symptoms affecting the central nervous system function may occur, including dizziness, hallucinations, feelings of confusion or anxiety, and insomnia.

There are reports of pseudomembranous colitis developing as a result of using clarithromycin, which can range from mild to life-threatening.

Liver dysfunction, cholestasis (with or without jaundice) or hepatitis may also develop, and laboratory test results may change.

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Overdose

Intoxication leads to the potentiation of negative manifestations.

Gastric lavage and symptomatic procedures should be performed.

Interactions with other drugs

Combined use of the drug with theophylline may lead to an increase in serum levels and potential toxicity of the latter.

The therapeutic properties of warfarin with digoxin can be potentiated when combined with Zosin.

Combination of the drug with zidovudine in adults with HIV may cause a decrease in chronic zidovudine levels.

There is evidence that macrolides can affect the metabolic processes of terfenadine, thereby increasing its plasma levels, which can lead to cardiac arrhythmia. Therefore, caution should be exercised when using the medication together with terfenadine or other non-sedative antihistamines.

Similar effects have been observed when clarithromycin is used in combination with pimozide or cisapride.

Zosin is able to potentiate the activity of carbazepine by slowing down the processes of its elimination.

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Storage conditions

Zosin should be stored in a dry place, out of reach of children. Temperature – standard.

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Shelf life

Zosin is permitted to be used within a 36-month period from the date of release of the pharmaceutical product.

Application for children

No clinical tests have been conducted in infants under six months of age. Older children tolerate the drug without complications.