Zosin

Zosin is a medicine from the category of macrolide antibiotics.

Indications Zosin

It is used for infections that occur under the influence of bacteria that are sensitive to the medication:

• upper respiratory duct: pharyngitis with sinusitis or tonsillitis with laryngitis;
• the lower part of the respiratory ducts: bronchitis, occurring in acute or chronic form, as well as pneumonia;
• otitis media ;
• mycobacteria caused by disseminated infections (Mycobacterium intracellulare or Mycobacterium avium);
• lesions of the subcutaneous tissue and the epidermis: furunculosis or folliculitis, as well as wounds;
• combined treatment to destroy Helicobacter pylori in individuals with ulcers in the gastrointestinal tract;
• toxoplasmosis or leprosy.

[1],

Release form

The release is made in tablet form.

Pharmacodynamics

Clarithromycin exhibits antibacterial activity by suppressing protein binding and synthesized from microbial 50s subunit of ribosomes with sensitivity to drugs. The substance shows activity against a large range of gram-positive and negative aerobes with anaerobes. The MIC values of clarithromycin are often twice as low as those of the erythromycin BMD. The metabolic product clarithromycin (component 14-hydroxycarythromycin) also has an antibacterial effect.

The drug is effective in vitro with respect to such bacteria:

• Gram-positive microbes: Staphylococcus aureus (strains with sensitivity to methicillin are added here), pneumococcus, pyogenic streptococcus with streptococcus agalactia and listeria monocytogenes;
• Gram-negative microorganisms: Moraxella catarallis, Legionella pneumophilus, Haemophilus bacilli with Haemophilus parainfluenzae, and also gonococci, Helicobacter pylori and pertussis bacilli;
• mycoplasmas: ureaplasma urealiticum and mycoplasma pneumonia;
• other bacteria: Chlamydia trachomatis, Hansen's rods, Mycobacterium avium, mycobacterium fortuitum and kansasi mycobacterium;
• anaerobes: Peptostreptococcus species, individual strains of bacteroids Fragilis, Acne propionibacteria, Clostridium perfringens and Peptococcus species.

Clarithromycin did not cause a carcinogenic or mutagenic effect during testing. The Ames test result for clarithromycin metabolism was negative.

[2], [3]

Pharmacokinetics

Clarithromycin is absorbed at high speed inside the gastrointestinal tract after oral administration. Bioavailability figures are 55%. Food does not affect the level of bioavailability of the drug.

The active element with its metabolic product (14-hydroxyclaritromycin) is distributed within a large amount of tissue and fluids. The drug undergoes extensive metabolic processes inside the liver, and then excreted in the bile.

Serum Cmax values develop after 120 minutes. The stable plasma level of Cmax of clarithromycin is recorded after 2-3 days and equals approximately 1 μg / ml after applying 0.25 g of the substance at 12-hour intervals, as well as 3-4 μg / ml after administration of 0.5 g of drug with 8-hour intervals.

The half-life of the drug is approximately 3-4 hours in the case of using the first of these methods, as well as 5-7 hours if the second is used. When used, 0.25 g of the drug at 12-hour intervals, 14-hydroxylarithromycin acquires a constant Cmax of approximately 0.6 μg / ml and a half-life of approximately 5-6 hours. When using 0.5 g of drug at 8-12 hour intervals, the Cmax 14-hydroxylaritromycin level is about 1 μg / ml, with a half-life of approximately 7-9 hours.

With the introduction of 0.25 g of clarithromycin at 12-hour intervals, 20% of the portion is excreted in the urine (in an unchanged state), and when using 0.5 g of the substance at 12-hour intervals, this figure is approximately 30%. Excretion in 14-hydroxylaritromycin is 10% or 15% (use, respectively, 0.25 or 0.5 g of the drug at 12-hour intervals).

Clarithromycin is excreted in mother's milk.

The duration of the half-life increases in people with kidney failure.

[4], [5], [6], [7]

Dosing and administration

Teenagers from 12 years old and adults need to use the medicine 2 times a day, in a serving of 0.25 g, with a 12-hour interval. It is possible to increase the dosage to 0.5 g 2 times a day (in severe forms of the disease). The treatment cycle is 7-14 days.

For ulcers affecting the intestines, it is required to inject 0.5 g of drug 3 times a day, in combination with 40 mg of omeprazole (1 time per day). The cycle lasts 2 weeks.

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

People with kidney insufficiency in a severe degree need to adjust the portion. With KK values less than 30 ml / min, the dosage is 0.25 g, 1 time (mild or moderate lesions) or 2 times a day (severe stages).

[9]

Use Zosin during pregnancy

It is forbidden to use Zosin during breastfeeding or pregnancy. The only exceptions are situations where the likely benefits of treatment are more expected than the risk of complications.

Contraindications

It is contraindicated to appoint people with strong intolerance regarding clarithromycin or other macrolides.

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

Side effects Zosin

Often, the drug is tolerated without the appearance of complications.

Among the side effects are headaches, diarrhea, vomiting, stomatitis, pain in the abdominal area and nausea.

Occasionally, signs of allergy are observed, starting with a mild epidermal rash and urticaria, and ending with anaphylaxis. Thrombocytopenia or Stevens-Johnson syndrome may occur. It is also possible disorder of the taste receptors.

Transient negative symptoms affecting the function of the central nervous system can occur - dizziness, hallucinations, a sense of clouding of consciousness or anxiety, and also insomnia.

There are reports of the development of the pseudomembranous form of colitis due to the use of clarithromycin - it can have both a weak expression and be life-threatening.

It is also possible the development of hepatic dysfunction, cholestasis (accompanied by jaundice or not) or hepatitis and a change in the testimony of laboratory tests.

[8]

Overdose

Intoxication leads to a potentiation of negative manifestations.

Gastric lavage and symptomatic procedures should be performed.

Interactions with other drugs

The combined use of the drug with theophylline can lead to an increase in serum indicators and the potential toxicity of the latter.

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

The combination of medication with zidovudine in adults with HIV may cause a decrease in persistent zidovudine levels.

There is evidence indicating that macrolides can affect the metabolism of terfenadine, thereby increasing its plasma parameters, which can cause cardiac arrhythmias. Therefore, when using the drug together with terfenadine or other non-sedative-type antihistamine drugs, caution should be exercised.

Similar effects were observed when using clarithromycin in combination with pimozide or cisapride.

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

[10], [11]

Storage conditions

Zosin must be kept in a dry place closed to children. Temperature is standard.

[12]

Shelf life

Zosin is allowed to apply within a 36-month term from the moment a pharmaceutical product is released.

Application for children

No clinical tests have been performed on infants who have not reached half a year of age. Older children tolerate the drug without complications.