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Azitrox
Last reviewed: 23.04.2024
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Azitroxy is an antibacterial drug for systemic use. It is a group of lincomycins, macrolides and streptogramins.
Indications of the azitrox
It is used to eliminate a variety of infections that are caused by bacteria sensitive to the action of the substance azithromycin. Among them are:
- infection in the soft layer of tissues and skin: folliculitis, erysipelas, and in addition furunculosis with impetigo and pyoderma, as well as infectious wounds;
- pathologies affecting the organs of the urogenital system: cervicitis (including its bacterial form) and prostatitis. The medicine can be used for bacterial urethritis (this includes gonorrheal form of urethritis and other STDs);
- infection in the respiratory system: bronchitis in acute or chronic form, as well as pneumonia (this includes its atypical form);
- diseases of the ENT organs: tonsillitis with sinusitis, pharyngitis with sinusitis, tonsillitis, otitis media and scarlet fever;
- other infectious pathologies: an early stage in the development of tick-borne borreliosis, as well as combination therapy for ulcerative diseases in the area of the duodenum intestine with the stomach (triggered by the action of the microbe Helicobacter pylori).
Pharmacodynamics
The active substance of the drug is azithromycin, which has a large range of antimicrobial effects. The drug is included in the subgroup of azalides from the category of macrolide antibiotics.
Azithromycin is a semi-synthetic substance containing a 15-membered structure of a macrocyclic type, which is formed by the incorporation of a nitrogen atom into a 14-membered lactone ring scheme. Such a modification removes individual lactone properties, but at the same time contributes to an increase in the acid resistance of the substance (this figure in azithromycin exceeds the analogous value of erythromycin by 300 times).
Azitroxy has a bacteriostatic effect on most microbes, but it can also have a bactericidal effect against individual strains (in the case of using high concentrations of drugs). The effect of the drug occurs in this way: the molecule of the substance reacts with the ribosomal substance 50S, and as a result of this process the latter begins to change. Such a reaction causes suppression of the peptidranslokase and destruction of the protein binding (these processes are required for bacteria for normal reproduction and growth).
Azithromycin is powerful in infections caused by bacteria outside the cells and pathogens that are inside them.
The drug has a large range of antimicrobial activity. For example, the active ingredient has bacteriostatic properties and affects the following strains:
- Gram-positive aerobes (this includes bacteria that produce β-lactamases): streptococcus agalactia, Streptococcus viridans, pneumococcus and streptococcus pyogenic. In addition to this, also streptococci from groups C, G and F, epidermal and golden staphylococci;
- Gram-negative aerobes: Influenza rod, Ducrea's stick, Campylobacter vellum and Haemophilus parainfluenzae, and in addition, Escherichia coli, Gardnerella vaginalis, Legionella pneumophila, Pertussis tick and paracolitus stick, Moraxella cataralis and Gonococcus.
The drug is active in pathologies provoked by individual anaerobes, among which are peptostreptococci, clostridium perfringence and Bacteroides bivius.
Sensitivity to azithromycin is possessed by such microbes as ureaplasma urealiticum, Chlamydia trachomatis, chlamydia pneumonia and mycoplasma pneumonia, and also pale treponema, Borrelia Burgdorfer and listeria monocytogenes.
The following strains are resistant to the effect of the drug: acinetobacter, pseudomonas and microbes from the enterobacteria group.
Azithromycin also has cross-resistance with erythromycin.
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Pharmacokinetics
When taken internally, the bioavailability of the substance is approximately 37%. Peak levels within the serum are observed 2-3 hours after drug use.
After use, azithromycin is distributed throughout the body. Pharmacokinetic tests have demonstrated that the level of matter inside tissues significantly exceeds plasma indices (by 50 times). This indicates that the substance has a high synthesis with tissues.
The synthesis with the plasma protein varies according to the values inside the plasma and can reach a minimum of 12% in the case of 0.5 μg / ml and a maximum of 52% at 0.05 μg / ml within the serum. The distribution volume in the equilibrium value is 31.1 l / kg.
The final half-life of the component from the plasma completely corresponds to its half-life from the tissues in the period of 2-4 days.
About 12% of the substance is excreted unchanged in urine in the period of 3 days. Unchanged azithromycin in very high concentrations is observed in bile. In the same place, 10 of its decay products, obtained by N- processes as well as O-demethylation, are also found, and together with this, during cleavage of the cladinose conjugate and hydroxylation of aglycone and dezosamine rings.
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Dosing and administration
Tablets are taken orally - either 1 hour before meals, or 2 hours after eating. The daily dose is taken for 1 reception. The medicine should be swallowed, washed down with water, it is impossible to chew the pill. Duration of treatment and dose sizes are assigned individually by the attending doctor.
Adult Dosage Dimensions:
- to eliminate infections in the respiratory and ENT organs: it is required to take 500 mg of the drug once a day during the 3-day period;
- 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 (one-time reception per day). The duration of such therapy is 5 days (for the entire course you need to take 3 g of medicine);
- infection in the area of the urogenital system: a one-time intake of 1000 mg of the drug;
- at the first stage of tick-borne borreliosis: the initial daily dosage is 1000 mg (single dose), and then throughout the entire course of taking 500 mg of Azitrox once a day. In general, the course is 5 days (during this time it is required in general to take 3 g of medicine);
- with combined therapy to eliminate ulcers in the area of the duodenum gut or stomach (associated with the microbe Helicobacter pylori): a single dose per day 1000 mg of medication in a period of 3 days.
Dosage for children over 12 years of age: they are calculated taking into account the weight of the patient. In general, the daily dosage is 10 mg / kg for 1 dose. The duration of treatment in this case is 3 days.
In therapy, the following regimen can also be used: on the first day, 10 mg / kg of the drug is required, and then, for 4 days, 5 mg / kg once a day. In this case, regardless of the scheme used, the total dose for the course should not exceed 30 mg / kg.
When treating the early stage of tick-borne borreliosis, children are given an initial dosage of 20 mg / kg (once per day), and from day 2 reduce it 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).
Use of the azitrox during pregnancy
Azitroxy can be used by pregnant women only in cases when the probable benefit for a woman exceeds the possibility of the fetus having various complications. Prescribe a medicine can only be a doctor in charge.
The active component of the drug can penetrate into the mother's milk, because of which, in the case of using the drug during lactation, it is required for the period of the medical course to refuse from breast-feeding.
Contraindications
The main contraindications:
- the presence of intolerance relative to the elements of the drug, as well as other drugs from the category of macrolides;
- disorders in the work of the kidney or liver (this includes kidney / liver failure);
- children under 12 years of age.
Caution is required when using in people with arrhythmia.
The medicine can not be prescribed in conjunction with ergot derivatives, because such a combination in theory can provoke the development of ergotism.
Side effects of the azitrox
The use of tablets can cause the development of the following side effects:
- reactions from the CCC: development of cardialgia or tachycardia;
- manifestations from the PSC and CNS: the appearance of dizziness, headaches, a feeling of severe fatigue and anxiety, and in addition, a balance disorder and problems with wakefulness and sleep;
- disorders in the GI and hepatobiliary system: vomiting, abdominal pain, nausea, stool disorders, epigastric pains and bloating. In addition, there may be a disorder in the processes of bile flow, jaundice, loss of appetite and an increase in the activity of liver enzymes. Individual patients (with prolonged taking of tablets) developed candidomycosis in the oral mucosa;
- manifestations of allergy: the appearance of itching and rashes, the development of photosensitivity, urticaria, Quincke edema and allergic form of conjunctivitis;
- others: some individuals sometimes developed thrush and jade.
Overdose
In clinical trials of the effects of azithromycin on the body, it was found that the negative reactions that occur as a result of an overdose are similar to side effects that develop when standard dosage forms are taken. Among them: a treatable loss of hearing, as well as nausea, diarrhea and vomiting.
To eliminate the disorders, it is necessary to take activated charcoal, and also to perform general supportive and symptomatic medical procedures.
Interactions with other drugs
As a result of the combination of Azitrox with antacids, which contain magnesium or aluminum hydroxide, and in addition to food and ethanol, the level of absorption of azithromycin decreases.
When combining the drug with warfarin, there were no changes in PTV values, but in any case, it is necessary to combine these drugs with care, because agents from the macrolide category are able to potentiate the anticoagulant properties of warfarin.
Combined medication with digoxin raises blood levels.
Combination of the drug with dihydroergotamine and ergotamine leads to an increase in their toxic properties.
Due to the processes of oxidation of microsomes inside the liver, the toxic properties of azithromycin are enhanced, and the index of individual drugs within the plasma is also increased. Among them: terfenadine with cyclosporine and bromocriptine, and in addition valproic acid, carbamazepine with theophylline, disopyramide and ergot alkaloids with hexobarbital and phenytoin.
When combined with azithromycin, an increase in the plasma level of certain drugs is observed: methylprednisolone with triazolam, and in addition felodipine, cycloserine and indirect anticoagulants. As a consequence, it is required to monitor the indices of these drugs in the blood with combined treatment, and also to adjust the dosages in accordance with them.
Linkomycins in combination with azithromycin weaken the medicinal properties of the latter.
The medicinal effect of azithromycin is potentiated by the combination with substances chloramphenicol and tetracycline.
The use of azithromycin by persons using oral antidiabetic drugs may cause a hypoglycemic crisis.
The active substance of the drug has an incompatibility with heparin.
Storage conditions
Azitroxy is required to contain in a place where moisture and sunlight do not penetrate, and also inaccessible children. Temperature limits - 15-25 about C.
Shelf life
Azitroxy is allowed to be used during the 3 years since the manufacture of tablets.
Attention!
To simplify the perception of information, this instruction for use of the drug "Azitrox" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.