Azitro

Azitro is a systemic antibacterial drug, is part of a group of macrolide drugs.

[1],

Indications of the azitro

In doses of 100 mg / 5 ml, as well as 200 mg / 5 ml is used to eliminate infectious diseases provoked by susceptible bacteria with azithromycin:

• pathology of ENT organs (otitis media with tonsillitis or bacterial pharyngitis, as well as sinusitis);
• diseases in the respiratory system (non-hospital pneumonia, as well as bacterial-type bronchitis);
• pathologies of an infectious nature on the skin, as well as inside soft tissues (erysipelas, chronic erythema of migratory type (early stage of tick-borne borreliosis), and also secondary type pyodermatosis).

The drug in doses of 200 mg / 5 ml is used to treat STDs (cervicitis or uncomplicated urethritis, caused by the bacterium Chlamydia trachomatis).

[2], [3]

Release form

It is produced in a powder form (16.5 g of substance) in a vial to make 20 ml of a suspension. Inside a single pack 1 bottle, to which is attached a dosage syringe and a special adapter.

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

Pharmacodynamics

Azithromycin is included in the category of macrolides. Is azalide with a wide range of antimicrobial activity. The activity of the substance is due to the inhibition of the binding of microbial proteins by synthesis with the ribosomal 50 S subunit, and in addition to preventing peptide migration (in the absence of effects on the binding of polynucleotides). Basically, the bacteriostatic effect develops.

Resistance to azithromycin can have both an innate and acquired character. Full cross resistance for pneumococci, Staphylococcus aureus (here enter also methicillin-resistant bacteria) enterococci of fecal and β-hemolytic streptococcus type A develops between the following substances: azithromycin with erythromycin, as well as other macrolides and linkomycins.

Sensitivity to azithromycin is possessed by such microbes:

• gram-negative aerobes: Haemophilus parainfluenzae and influenza rod, as well as moraxella catarrhis;
• other bacteria: legionella pneumophila, Chlamydia trachomatis, chlamydophile pneumonia and mycoplasma pneumonia, and also Mycobacterium avium.

Types of bacteria that acquire resistance to the drug individually - Gram-positive aerobes: Streptococcus agalactia, Staphylococcus aureus, Streptococcus pyogenes and Pneumococci.

Bacteria that have inherent resistance to the substance:

• Gram-positive aerobes: methicillin-resistant epidermal and golden staphylococci, and in addition enterococcus fecal;
• Gram-negative aerobes: Klebsiella, E. Coli, as well as Pseudomonas aeruginosa;

Gram-negative anaerobes: a group of bacteroids fragilis.

[7], [8], [9], [10], [11]

Pharmacokinetics

After the use of drugs, the bioavailability of the substance reaches approximately 37%. The peak serum level is observed 2-3 hours after the use of the suspension.

The substance is quickly distributed inside the body fluids and tissues. Perfectly passes inside the tissues and organs of the urinary tract, respiratory ducts and soft tissues with skin. Cumulates inside the cells, as a result of which the index of the drug inside the tissues significantly exceeds the analogous plasma values (up to 50 times). This suggests that the drug has a high affinity in the tissues due to weak synthesis of the substance with the plasma protein.

The indices of the active ingredient inside the target organs (this is the throat with the lungs and the prostate) is higher than the MIC of 90 for pathogen substances with a single 500 mg dosage. A large amount of azithromycin cumulates inside fibroblasts with phagocytes. The latter perform the movement of the medicine to the site of inflammation.

The drug in its bactericidal values continues to persist on the site of inflammation in the period of 5-7 days after the use of the last dosage, which makes it possible to treat with short courses - for 3 or 5 days. The final half-life of the substance is similar to the time of its half-life from the tissues, and is 2-4 days.

About 12% of the drug is excreted unchanged in the urine in the period of 3 days. Large concentrations of unchanged substance are observed in bile. Ten decay products were determined, which are formed by hydroxylation processes, as well as N- and O-demethylation, as well as other metabolic transformations. The disintegration products of azithromycin do not have antimicrobial properties.

[12], [13], [14], [15], [16], [17]

Dosing and administration

The duration of therapy and the size of the doses are prescribed by the doctor. The suspension is taken once a day - 1 hour before meals or 2 hours after it. This is necessary, because the simultaneous use with food violates the absorption of the active substance.

To improve the taste after using the suspension is allowed to drink medicine with any fruit juice. If you miss a dose, you should try to take it as quickly as possible, and all the subsequent ones should be consumed at intervals of 24 hours.

For adults (azithromycin in the proportion of 200 mg / 5 ml):

• treatment of infectious diseases of the respiratory system and ENT organs, as well as soft tissues with skin (eliminates chronic erythema migratory type) - the total dose of the drug is 1500 mg. The medicine is taken 500 mg once a day for a period of 3 days;
• elimination of STDs provoked by the bacterium Chlamydia trachomatis - single use of 1000 mg Azitro;
• treatment of erythema migratory type - the course lasts for 5 days. The size of the total dosage of the drug is 3 g. For 1 day it is required to consume 1 g of drugs, and on subsequent days to take 500 mg of the suspension once a day.

Since elderly patients may fall into the category of people at risk of cardiac conduction disorder, care should be taken when azithromycin is used, because it can trigger arrhythmia or pirouette tachycardia.

For children:

• treatment of infectious diseases in the respiratory system, ENT organs, as well as soft tissues with skin (excluding only erythema of the migrating type in chronic form) - the total dose of the drug is 30 mg / kg for the period of 3 days of therapy (single daily the dose in this case is 10 mg / kg);
• when eliminating erythema migratory type - the size of the total dosage of the drug is 60 mg / kg during the 5 days of the therapeutic course. The treatment regimen is as follows: on the 1st day, 20 mg / kg of medication is taken, and then on subsequent days it is required to take 10 mg / kg once a day.

It turned out that Azitro effectively operates in the process of eliminating pharyngitis from children of streptococcal type. A daily one-time drug intake of 10 or 20 mg / kg is administered every 3 days. Comparison of these dosages during clinical tests showed that their drug efficacy is quite similar, but still the destruction of bacteria in the case of taking a daily dose of 20 mg / kg was more significant. But often for the prevention of pharyngitis, provoked by streptococcus pyogenic, as well as polyarthritis of the rheumatic type, developing in the form of a secondary pathology, the drug of the first choice is penicillin.

Children weighing 5-15 kg (using azithromycin in the amount of 100 mg / 5 ml). At the specified weight parameters a special scheme of used dosages is required:

• weight 5 kg - the daily dose of the suspension is 2.5 ml (the azithromycin level in this dosage is 50 mg);
• weight 6 kg - the daily dose is 3 ml (azithromycin - 60 mg);
• weight 7 kg - the size of the daily dose is 3.5 ml (azithromycin level - 70 mg);
• weight 8 kg - daily dose is 4 ml (azithromycin - 80 mg);
• weight 9 kg - daily dose is 4.5 ml (azithromycin level - 90 mg);
• weight 10-14 kg - daily dosage is 5 ml (active substance content - 100 mg).

Children weighing more than 15 kg (using azithromycin in a ratio of 200 mg / 5 ml). Taking into account the weight of the child, such dosage schemes are offered:

• weight within 15-24 kg - daily dose is 5 ml (azithromycin - 200 mg);
• weight 25-34 kg - daily dose is 7.5 ml (content of the active ingredient is 300 mg);
• weight within 35-44-kg - the daily dosage is equal to 10 ml (substance content - 400 mg);
• weight ≥45 kg - daily dose is 12.5 ml (azithromycin level - 500 mg).

[26], [27], [28], [29],

Use of the azitro during pregnancy

The drug can pass through the placental barrier, but it does not have a negative effect on the fetus. It should be noted that the carefully controlled appropriate testing of drug use in pregnant women has not been carried out. As a result, it is required to prescribe Azitro pregnant only in cases when the help from him for a woman will be higher than the probability of complications in the fetus.

Azithromycin passes into the mother's milk, because of which it is required to cancel breastfeeding for the period of the treatment course itself, and also 2 more days after its completion.

Contraindications

Among the contraindications:

• the presence of hypersensitivity to the active component or other elements of the drug or other macrolides and ketolid antibiotics;
• disorders in the liver in a severe degree;
• since azithromycin in combination with ergot derivatives is capable of causing ergotism in theory, it is impossible to combine these medicines.

[18], [19], [20], [21]

Side effects of the azitro

Reception of a suspension can cause the development of such side effects:

• reactions of the hematopoietic system: occasionally develops a hemolytic form of anemia, leuko- or thrombocytopenia, as well as eosinophilia. Clinical tests alone noted the occurrence of transient neutropenia with mild severity, but the association between the use of azithromycin and the development of this disorder could not be detected;
• disturbances of the psyche: occasionally there are feelings of anxiety, aggressiveness, nervousness or excitement, and in addition there are hallucinations and delusions develop;
• manifestations of the organs of the National Assembly: in some cases, headaches and vertigo / vertigo arise, and besides paresthesia with convulsions, syncope, dysgeusia, hypoesthesia or asthenia, a feeling of severe fatigue, insomnia or drowsiness. Occasionally parasymia, anosmia, myasthenia gravis or agevia develops;
• violations in the work of the visual organs: occasionally develop a disorder of vision;
• manifestations from the side of the auditory organs: occasionally there is an ear ringing, deafness or hearing disorder. Often, these problems developed during clinical trials with prolonged use of the drug in high doses. In general, such manifestations were curable;
• violations in the work of SSS: occasionally there is tachycardia or arrhythmia (this includes ventricular tachycardia). The prolongation of the QT-interval, the development of pirouette-type arrhythmia, the lowering of the level of blood pressure and ventricular fibrillation were reported separately;
• manifestations of the gastrointestinal tract: often there is discomfort in the abdomen, nausea, diarrhea and vomiting. Less often there is swelling, loose stools, anorexia and gastritis with dyspepsia. Occasionally, the shade of the tongue and teeth changes and constipation develops. Single pancreatitis or pseudomembranous form of colitis was observed;
• reactions of the organs of the hepatobiliary system: occasionally there was intrahepatic cholestasis or hepatitis (also there were data on pathological changes in the values of liver functional tests). Single reported on the development of hepatic dysfunction and hepatitis in a necrotic or fulminant form;
• infectious and invasive processes: rarely there is candidiasis (also its oral form), vaginal pathologies, bacterial and fungal infections, as well as pneumonia, gastroenteritis, runny nose with a pharyngitis and respiratory function disorder;
• cutaneous manifestations: infrequently allergy symptoms occur, including a rash with itching. Occasionally, hives develop, photophobia and Quincke's edema. In addition, there are also erythema multiforme and Stevens-Johnson / Lyell syndromes;
• disorders in the work of the muscular system and bones: sometimes there are pains in the joints;
• reactions from the system of urination: occasionally there is a deficiency of the kidneys of an acute nature, kidney pain, as well as dysuria and tubulointerstitial nephritis;
• disorders of the mammary glands and reproductive organs: sometimes there are bleeding from the uterus, vaginitis and testicular disorders;
• general reactions: sometimes there is anaphylaxis, which includes pain in the sternum and swelling;
• results of laboratory tests: often a decrease in the number of bicarbonates or lymphocytes, and in addition, an increase in the level of eosinophils. Sometimes urea, as well as creatinine with bilirubin inside the plasma and the activity of AST and ALT elements, may increase, and the potassium index may also change. All these violations were reversible;
• intoxication processes and lesions: caused by the complication procedure.

[22], [23], [24], [25]

Overdose

Manifestations of drug overdose: diarrhea, vomiting and nausea, which have a pronounced character, as well as a curable hearing loss.

To treat disorders, gastric lavage is required, as well as therapy aimed at maintaining the patient's health and eliminating signs of disturbance.

[30], [31]

Interactions with other drugs

It is required to combine with caution the azithromycin with other drugs that can prolong the QT-interval (such are ketoconazole with lithium, and in addition quinidine together with terfenadine, as well as cyclophosphamide with the substance haloperidol).

In the process of studying drug interaction with antacids, there was no change in the bioavailability of azithromycin, although the peak level of the substance inside the plasma decreased by 25%. It is required to use azithromycin at least 1 hour before using antacids or 2 hours after.

Combined drug administration with cetirizine (20 mg dose) during 5 days did not cause pharmacokinetic interaction at equilibrium indices, but significantly changed the QT-interval values.

The combination of Azitra with ergot alkaloids or dihydroergotamine can provoke the development of vasoconstrictive action accompanied by perfusion disorders, which results in the defeat of the fingers on the legs and hands. Because of this, it is necessary to avoid such combinations.

In the case of using cimetidine 2 hours before taking azithromycin, the pharmacokinetic parameters of the latter were not found to change.

Individual macrolides are able to affect the metabolism of cyclosporine. Because of this, with the combined use of these funds, it is required to constantly monitor the cyclosporine parameters and to change the applied dose in accordance with them.

Combination of the drug with warfarin may increase the anticoagulant effect, and therefore it is necessary to monitor the indices of PTV during the treatment period.

There is information that macrolides are capable of affecting the intestinal metabolism of digoxin, so that combined use of these medicines requires regular monitoring of digoxin values.

The drug does not affect the pharmacokinetic parameters of theophylline in the case of their combined use. But in this case, the simultaneous administration of theophylline with other macrolides caused an increase in the serum indices of this substance.

The administration of zidovudine once in the amount of 1000 mg in combination with azithromycin (repeated use of 600 or 1200 mg doses) did not affect the pharmacokinetic parameters, as well as the excretion of urinary zidovudine or its glucuronic degradation products. But the use of azithromycin led to an increase in the level of zidovudine phosphorylated type within mononuclear cells in the peripheral blood flow system.

The combined Azithra with rifabutin had no effect on the values of these drugs inside the plasma. People who used these drugs at the same time developed neutropenia, but it should be taken into account that it was not possible to connect the occurrence of this disorder with the use of azithromycin.

Admission together with cisapride is able to prolong the prolongation of the QT-interval, and in addition to increase the arrhythmia of the ventricles or the syndrome of fibrillation. Because of this, it is recommended not to combine these substances.

Combined use with alfentanil or astemizole should be done with caution, because in combination with erythromycin, there was an increase in exposure.

With simultaneous reception with nelfinavir, the equilibrium serum azithromycin values increase. Although it is not recommended to change the dosage of the drug in the case of a combination with nelfinavir, careful monitoring of the development of the negative effects of azithromycin will be justified.

It is required to bear in mind the possibility of developing cross-resistance between azithromycin, as well as other macrolides (eg erythromycin) and clindamycin with lincomycin.

[32], [33], [34]

Storage conditions

Azitro must be kept in a place inaccessible to young children. The temperature conditions for the powder are not more than 30 ° C, but the ready-to-use suspension can be stored at an index of not more than 25 ° C.

[35], [36], [37], [38]

Shelf life

Azitro is suitable for use within 3 years from the date of release of the medicine. At the same time, the finished suspension can be stored for a period of not more than 5 days.

[39], [40], [41]