Azitral

Azitral is a systemic antibacterial drug with the active ingredient azithromycin. It belongs to the macrolide category.

Indications Azitrala

It is used to eliminate infectious diseases caused by bacteria sensitive to the effects of azithromycin:

• diseases in the respiratory tract – alveolitis, interstitial pneumonia, as well as bacterial bronchitis;
• ENT diseases - tonsillitis with sinusitis, and in addition, inflammation of the middle ear and pharyngitis;
• infectious pathologies in the area of soft tissues with skin - erysipelas, secondary pyodermatoses, as well as impetigo and chronic erythema migrans (the initial stage of development of tick-borne borreliosis);
• STDs – cervicitis, as well as uncomplicated urethritis;
• pathologies in the duodenum or stomach caused by the bacterium Helicobacter pylori.

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Release form

It is released in tablet form.

Azitral 250 - 6 tablets in a blister. Inside a separate package there is 1 blister plate, in a box - 10 packages of medicine.

Azitral 500 - there are 3 tablets inside the strip. In a separate pack - 1 plate with tablets, inside the box - 5 packs with medicine.

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Pharmacodynamics

Azithromycin is a member of a new subgroup of macrolides – azalide substances. It is synthesized with the ribosomal (70S) subunit of 50S sensitive bacteria, inhibiting protein binding dependent on RNA. The substance also inhibits the reproduction and growth of microbes, and in high concentrations can have a bactericidal effect.

Azithromycin has a wide spectrum of antimicrobial action. Among the bacteria sensitive to it are:

• gram-positive – pneumococcus, streptococcus pyogenes, streptococcus agalactiae, streptococci types C and F, as well as G, and also S.viridans and Staphylococcus aureus;
• gram-negative – Haemophilus influenzae, H. parainfluenzae, Moraxella catarrhalis, whooping cough, parapertussis, Legionella pneumophila, Ducrey bacillus, Campylobacter jejuni, gonococcus and Gardnerella vaginalis;
• individual anaerobes – Bacteroides bivius, Clostridium perfringens, Peptostreptococcus species, as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum and Borrelia burgdorferi.

The drug does not affect gram-positive bacteria resistant to erythromycin.

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Pharmacokinetics

When taken orally, the substance is rapidly absorbed from the gastrointestinal tract. The bioavailability level is approximately 37% (undergoes first hepatic passage). After oral administration of 500 mg of the drug, the peak plasma level of the substance is reached after 2.5-3 hours, amounting to 0.4 mg/l.

The substance is well distributed within the respiratory system, tissues with organs of the genitourinary system (including the prostate), and also soft tissues and skin. The concentration level of the drug inside cells with tissues exceeds its similar indicators inside the serum (by 10-100 times). Equilibrium plasma values are reached after 5-7 days. Large quantities of the drug accumulate inside phagocytes, moving it to areas of inflammation, as well as infection (there they are gradually released by phagocytosis).

Synthesis with protein is inversely proportional to blood concentration (7-50% of the drug). About 35% of the substance undergoes hepatic metabolism by demethylation processes. In this case, azithromycin loses its activity.

More than 50% of the drug is excreted unchanged in the bile, and approximately 4.5% in the urine, over a period of 72 hours.

The half-life is 14-20 hours (in the interval 8-24 hours after taking the drug), and 41 hours (in the interval 24-72 hours). Food intake significantly affects the pharmacokinetic properties of the drug.

In elderly men (over 65-85 years old), no changes in the pharmacokinetics of the drug are observed, but in elderly women the peak indicator increases by 30-50%.

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Dosing and administration

Azitral should be taken 1 hour before or 2 hours after meals, because when taken with food, absorption of the active component is impaired. Tablets should be taken once a day.

For teenagers weighing over 45 kg and adults:

• to treat infections in the respiratory system, ENT organs, soft tissues and skin (excluding chronic migratory erythema), it is necessary to take 500 mg of the drug over a period of 3 days;
• when eliminating chronic migratory erythema, take the medicine once a day for a period of 5 days: the dose on the 1st day is 1 g, and on the following days - 500 mg;
• To treat STDs, a single dose of 1 g of medication is required;
• when treating ulcerative pathologies of the duodenum or stomach, it is necessary to take 1 g of the drug for 3 days (combination treatment);
• To eliminate acne vulgaris, you need to take 6 g of the drug per course. The following treatment regimen is suggested: take 500 mg once a day during the first 3 days, and during the next 9 weeks, take 500 mg of the drug once a week.

If you miss a dose of the medicine, you should take the missed tablet as soon as possible and then take them at intervals of 24 hours.

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Use Azitrala during pregnancy

The use of tablets during pregnancy is permitted only for strict indications, in cases where the probable benefit to the patient is higher than the risk of complications in the fetus.

The active substance penetrates into breast milk, which is why breastfeeding must be discontinued during treatment with Azitral.

Contraindications

Among the contraindications:

• intolerance to the components of the drug, as well as other macrolides;
• disorders of the kidneys or liver, as well as severe electrolyte imbalance (especially in cases of hypomagnesemia or hypokalemia);
• bradycardia, severe heart failure or arrhythmia with pronounced clinical symptoms;
• concomitant use with ergot alkaloid medications;
• intended for children weighing less than 45 kg.

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Side effects Azitrala

Taking the tablets may cause the following side effects:

• reactions of the hematopoietic system: development of thrombocytopenia or transient neutropenia with mild severity;
• manifestations from the nervous system: development of headaches, asthenia, and dizziness/vertigo. In addition, a feeling of drowsiness or insomnia may occur, paresthesia, convulsions or fainting may occur, and olfactory or gustatory perception may be impaired;
• mental disorders: occasionally there are feelings of anxiety, restlessness, aggressiveness, nervousness and hyperactivity;
• reactions of the auditory organs: tinnitus, development of deafness or hearing loss (most of these disorders are curable);
• CVS disorders: development of palpitations, as well as arrhythmia (due to ventricular tachycardia). Occasionally, prolongation of the QT interval, ventricular fibrillation, chest pain and decreased blood pressure are observed;
• reactions of the gastrointestinal tract: diarrhea, nausea, abdominal discomfort, vomiting, dyspepsia, loose stools or constipation, bloating and change in the color of the tongue. Anorexia, gastritis with pancreatitis and, occasionally, pseudomembranous colitis may develop;
• disorders in the hepatobiliary system: hepatitis, intrahepatic cholestasis, and treatable increase in liver transaminase activity are occasionally observed. Liver dysfunction (sometimes leading to death) and necrotic hepatitis develop occasionally;
• skin reactions: the appearance of Quincke's edema, itchy rashes and urticaria, as well as the development of photosensitivity, Lyell's or Stevens-Johnson syndromes, and erythema multiforme;
• disorders of the musculoskeletal system: occurrence of joint pain;
• manifestations from the urinary system: acute renal failure or tubulointerstitial nephritis;
• reactions from the reproductive organs: development of vaginitis;
• Others: the occurrence of anaphylaxis (this includes swelling, which sometimes leads to death) or candidiasis.

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Overdose

In case of overdose, symptoms such as diarrhea, vomiting and severe nausea, as well as transient hearing loss, are observed.

To eliminate the disorders, gastric lavage using a tube is required.

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Interactions with other drugs

It is necessary to pay attention to the combined use of Azitral with such substances as warfarin, digoxin, theophylline with ergotamine and carbamazepine, and also terfenadine and phenytoin with cyclosporine and triazolam. This is necessary because macrolides can enhance the properties of the above drugs.

Azithromycin is not synthesized with enzymes of the hemoprotein 450 system, which differs from most macrolide antibiotics.

Lincomycins reduce the properties of azithromycin, and chloramphenicol with tetracycline, on the contrary, increase them. The drug has no pharmaceutical compatibility with the substance heparin.

The drug should be used with caution in combination with other agents that can prolong the QT interval.

Studies on the effect of antacids on the pharmacokinetic parameters of azithromycin have not shown changes in bioavailability parameters, but a decrease in the peak level of the substance in plasma (by 30%) was observed. In the case of taking cimetidine 2 hours before taking azithromycin, the pharmacokinetics of the latter did not change. Antacids can inhibit the absorption of azithromycin. It is necessary to maintain an interval of at least 2 hours between the use of Azitral and antacid.

Combination of the drug with warfarin or coumarin anticoagulants (oral form) increases the likelihood of bleeding. Therefore, during the therapy, it is necessary to constantly monitor the PTT indicators.

The combination of a single 1000 mg dose of zidovudine and multiple doses of 600 or 1200 mg of azithromycin had no effect on the plasma pharmacokinetics of zidovudine or its (and its glucuronic breakdown products) urinary excretion. However, azithromycin administration increased levels of phosphorylated zidovudine (a drug-active breakdown product) within mononuclear cells in the peripheral circulation.

Taking Azitral with rifabutin does not change the plasma levels of these drugs. However, people who took them together sometimes developed neutropenia. But it should be taken into account that the disorder was caused by the use of rifabutin, and it was not possible to link it to the use of azithromycin.

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Storage conditions

Azitral should be kept in a place inaccessible to small children. Temperature conditions – no more than 25°C.

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Shelf life

Azitral can be used for a period of 3 years from the date of release of the drug.