Azitrox

Azitrox is an antibacterial drug for systemic use. It belongs to the group of lincomycins, macrolides and streptogramins.

Indications Azitroxa

It is used to eliminate various infections caused by bacteria sensitive to the action of the substance azithromycin. Among them:

• infections in the soft tissue layer and skin: folliculitis, erysipelas, as well as furunculosis with impetigo and pyoderma, as well as infected wounds;
• pathologies affecting the urogenital system: cervicitis (including its bacterial form) and prostatitis. The drug can also be used for bacterial urethritis (this includes gonorrheal urethritis and other STIs);
• infections in the respiratory system: bronchitis in acute or chronic form, as well as pneumonia (this includes its atypical form);
• ENT diseases: tonsillitis with sinusitis, pharyngitis with sinusitis, tonsillitis, otitis media and scarlet fever;
• other infectious pathologies: early stage of development of tick-borne borreliosis, as well as combination therapy for ulcerative diseases in the duodenum with stomach (caused by the action of the microbe Helicobacter pylori).

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Release form

The medicine is released in tablets.

Azitrox 250 is available in 3 or 6 tablets per blister. Inside the package is 1 blister plate with tablets.

Azitrox 500 is available in the amount of 3 tablets inside a blister. A separate pack contains 1 blister plate.

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Pharmacodynamics

The active substance of the drug is azithromycin, which has a wide range of antimicrobial action. The drug belongs to the azalide subgroup of the macrolide antibiotics category.

Azithromycin is a semi-synthetic substance containing a 15-membered macrocyclic structure formed by incorporating a nitrogen atom into the 14-membered lactone ring. Such a modification removes individual lactone properties, but at the same time contributes to the strengthening of the acid resistance of the substance (this indicator for azithromycin exceeds the analogous value of erythromycin by 300 times).

Azitrox has a bacteriostatic effect on most microbes, but can also have a bactericidal effect on individual strains (in the case of using high concentrations of the drug). The effect of the drug occurs in the following way: the substance molecule reacts with the ribosomal substance 50S, and as a result of this process, the latter begins to change. Such a reaction causes suppression of peptide translocase and destruction of protein binding (these are the processes required by bacteria for normal reproduction and growth).

Azithromycin is effective against infections caused by both bacteria located outside the cells and pathogens located inside them.

The drug has a wide range of antimicrobial activity. For example, the active component has bacteriostatic properties and affects the following strains:

• Gram-positive aerobes (including bacteria that produce β-lactamases): Streptococcus agalactiae, Streptococcus viridans, pneumococcus and Streptococcus pyogenes. In addition, also streptococci of groups C, G and F, Staphylococcus epidermidis and Staphylococcus aureus;
• Gram-negative aerobes: influenza bacillus, Ducrey bacillus, Campylobacter jejuni and Haemophilus parainfluenzae, as well as Escherichia coli, Gardnerella vaginalis, Legionella pneumophila, whooping cough bacillus and parapertussis bacillus, as well as Moraxella catarrhalis and gonococcus.

The drug is active in pathologies caused by certain anaerobes, including peptostreptococci, clostridium perfringens and Bacteroides bivius.

Microbes such as Ureaplasma urealyticum, Chlamydia trachomatis, Chlamydia pneumoniae and Mycoplasma pneumoniae, as well as Treponema pallidum, Borrelia burgdorferi and Listeria monocytogenes are sensitive to azithromycin.

The following strains are resistant to the action of the drug: Acinetobacter, Pseudomonas and microbes from the Enterobacter group.

Azithromycin also has cross-resistance with the substance erythromycin.

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Pharmacokinetics

When taken orally, the bioavailability of the substance is approximately 37%. The peak level in the serum is observed 2-3 hours after taking the drug.

After use, azithromycin is distributed throughout the body. Pharmacokinetic tests have shown that the level of the substance inside the tissues significantly exceeds the plasma indicators (50 times). This indicates that the substance has a high synthesis with tissues.

Synthesis with plasma protein fluctuates in accordance with the values within the plasma and can reach a minimum of 12% in the case of a value of 0.5 μg/ml and a maximum of 52% in the case of a value of 0.05 μg/ml within the serum. The distribution volume at steady state is 31.1 L/kg.

The final half-life of the component from plasma is completely consistent with its half-life from tissues in the period of 2-4 days.

About 12% of the substance is excreted unchanged in urine over a period of 3 days. Unchanged azithromycin is observed in very high concentrations in bile. There are also 10 of its decay products obtained by N- and O-demethylation processes, and also during the cleavage of the cladinose conjugate and hydroxylation of aglycone and desosamine rings.

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Dosing and administration

The tablets are taken orally - either 1 hour before a meal or 2 hours after. The daily dose is taken in 1 dose. The medicine should be swallowed with water, the tablet should not be chewed. The duration of treatment and the doses are prescribed by the attending physician individually.

Adult dosage sizes:

• to eliminate infections in the respiratory and ENT organs: it is necessary to take 500 mg of the medicine once a day for 3 days;
• elimination of infectious pathologies inside soft tissues and on the skin: the initial dosage is a single dose of 1000 mg, and then, from the 2nd day of the course, the dose is reduced to 500 mg (single dose per day). The duration of such therapy is 5 days (for the entire course, it is necessary to take 3 g of the drug);
• infections in the urogenital system: a single dose of 1000 mg of the drug;
• at stage 1 of tick-borne borreliosis: the initial daily dosage is 1000 mg (single dose), and then throughout the entire course it is required to take 500 mg of Azitrox once a day. In total, the course is 5 days (during this time it is required to take a total of 3 g of the medicine);
• in combination therapy to eliminate ulcers in the duodenum or stomach (associated with the microbe Helicobacter pylori): a single dose of 1000 mg of the drug per day for a period of 3 days.

Dosage size for children over 12 years old: they are calculated taking into account the patient's weight. Basically, the daily dosage is 10 mg / kg per 1 dose. The duration of treatment is 3 days.

The following scheme can also be used for therapy: on the first day, 10 mg/kg of the drug should be taken, and then, over a period of 4 days, 5 mg/kg should be taken once a day. At the same time, regardless of the scheme used, the total dose for the course should not exceed 30 mg/kg.

When treating early stage tick-borne borreliosis, children are prescribed an initial dosage of 20 mg/kg (once a day), and from the 2nd day it is reduced to 10 mg/kg. The duration of therapy is 5 days (the total dose for the entire course of treatment can be a maximum of 60 mg/kg).

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Use Azitroxa during pregnancy

Azitrox can be used by pregnant women only in cases where the probable benefit to the woman exceeds the possibility of various complications in the fetus. Only the attending physician can prescribe the drug.

The active component of the drug can penetrate into breast milk, which is why, if the drug is used during lactation, it is necessary to stop breastfeeding for the duration of the treatment course.

Contraindications

Main contraindications:

• the presence of intolerance to the elements of the drug, as well as other drugs from the macrolide category;
• disorders of the kidneys or liver (this includes kidney/liver failure);
• children under 12 years of age.

Caution is required when used in people with a history of arrhythmia.

The drug should not be prescribed in combination with ergot derivatives, because such a combination could, in theory, provoke the development of ergotism.

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Side effects Azitroxa

The use of tablets may cause the development of the following side effects:

• reactions from the cardiovascular system: development of cardialgia or tachycardia;
• manifestations from the PNC and CNS: the appearance of dizziness, headaches, a feeling of severe fatigue and anxiety, as well as a disorder of balance and problems with the sleep-wake cycle;
• gastrointestinal and hepatobiliary disorders: vomiting, abdominal pain, nausea, bowel disorders, epigastric pain and bloating. In addition, bile outflow disorders, jaundice, loss of appetite and increased activity of liver enzymes may be observed. In some patients (with prolonged use of tablets), candidomycosis developed in the oral mucosa;
• manifestations of allergies: the appearance of itching and rashes, the development of photosensitivity, urticaria, Quincke's edema and allergic conjunctivitis;
• Others: Some individuals sometimes developed thrush and nephritis.

Overdose

Clinical testing of the effects of azithromycin on the body has shown that adverse reactions resulting from overdose are similar to those that occur with standard therapeutic doses. These include treatable hearing loss, as well as nausea, diarrhea, and vomiting.

To eliminate the disorders, it is necessary to take activated charcoal, as well as perform general supportive and symptomatic treatment procedures.

Interactions with other drugs

As a result of combining Azitrox with antacids containing magnesium or aluminum hydroxide, as well as with food and ethanol, the level of absorption of azithromycin decreases.

When combining the drug with warfarin, no changes in the PT indices were observed, but in any case, it is necessary to combine these drugs with caution, because drugs from the macrolide category can potentiate the anticoagulant properties of warfarin.

Taking the drug in combination with digoxin increases its levels in the blood.

Combining the drug with the substances dihydroergotamine and ergotamine leads to an increase in their toxic properties.

Due to the oxidation processes of microsomes inside the liver, the toxic properties of azithromycin are enhanced, and the level of individual drugs inside the plasma increases. Among them are: terfenadine with cyclosporine and bromocriptine, as well as valproic acid, carbamazepine with theophylline, disopyramide and ergot alkaloids with hexobarbital and phenytoin.

When combined with azithromycin, an increase in the plasma level of some drugs is observed: methylprednisolone with triazolam, as well as felodipine, cycloserine and indirect anticoagulants. As a result, it is necessary to monitor the indicators of these drugs in the blood during combined treatment, and also adjust the dosages accordingly.

Lincomycins in combination with azithromycin weaken the medicinal properties of the latter.

The medicinal effect of azithromycin is potentiated when combined with the substances chloramphenicol and tetracycline.

The use of azithromycin by individuals taking oral antidiabetic drugs may cause hypoglycemic crisis.

The active substance of the drug is incompatible with heparin.

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Storage conditions

Azitrox should be kept in a place where moisture and sunlight do not penetrate, and inaccessible to children. Temperature limits are 15-25 ^o C.

Shelf life

Azitrox is permitted to be used for a period of 3 years from the date of manufacture of the tablets.