Azithromycin

Azithromycin has a broad range of antibacterial activity.

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Indications Azithromycin

It is used to eliminate the following disorders:

• infections affecting the ENT system and respiratory organs (such as pharyngitis with laryngitis and tonsillitis, as well as sinusitis, otitis media, pneumonia and chronic bronchitis in the acute stage);
• uncomplicated bacterial infections developing in the genitourinary system (caused by the activity of Chlamydia trachomatis – urethritis or cervicitis);
• lesions affecting the skin or soft tissues (infectious dermatitis, erysipelas or impetigo);
• scarlet fever;
• early stage Lyme disease;
• diseases associated with the action of Helicobacter pylori in the duodenum or stomach.

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Release form

The product is produced in capsules or tablets of 0.25 or 0.5 g. Capsules of 0.25 g are produced in 6 pieces inside a blister (in a pack - 1 blister plate); capsules of 0.5 g - in the amount of 3 pieces inside a blister cell (in a box - 1 blister).

In addition, the drug may be in the form of a powder used to make a suspension for oral administration (volumes of 0.1 g/20 ml, 0.5 g/20 ml or 0.2 g/20 ml). It is packaged in plastic bottles with a capacity of 20 g - 1 such bottle per pack together with a measuring cup.

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Pharmacodynamics

Azithromycin is a semi-synthetic antibiotic - it is produced artificially as a derivative of erythromycin. It belongs to the category of azalides with macrolides (the first representative of azalide drugs).

By synthesizing with the 50S ribosome subunit, the drug inhibits the process of protein biosynthesis and slows down microbial growth along with inhibiting their vital activity. At high medicinal concentrations, a bactericidal effect is observed.

The medication actively affects the following microorganisms:

• gram-positive (except for erythromycin-resistant microflora) – epidermal and golden staphylococcus, pneumococcus, pyogenes streptococcus and agalactiae streptococcus, as well as streptococci from categories C, F, and G;
• gram-negative - whooping cough and parapertussis bacilli, influenza bacilli, diplococci from the Neisseria category, legionella and campylobacter, and in addition, microbes from the monotypic subspecies Moraxella catarrhalis and Gardnerella catarrhalis;
• anaerobic microflora (peptococci and peptostreptococci, Clostridia perfringens, and also B. bivius);
• chlamydia (such as Chlamydophila pneumoniae and Chl. trachomatis);
• mycoparasites from the subspecies of mycobacteria;
• mycoplasmas (such as Mycoplasma pneumoniae);
• ureaplasmas (such as ureaplasma urealyticum);
• spirochetes (bacteria that cause the appearance of pale spirochetes or the development of tick-borne borreliosis).

Lipophilene exhibits resistance to acidic environments.

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Pharmacokinetics

When taking a capsule, tablet or suspension, the active element is quickly absorbed from the gastrointestinal tract.

Bioavailability indicators when using 0.5 g of the drug reach 37%, it takes 2-3 hours to reach peak values of the substance. The level of protein synthesis in the plasma is inversely proportional to the drug indicators in the blood and fluctuates in the range of 7-50%. The half-life is 68 hours.

Plasma values of the drug stabilize after 5-7 days of therapy.

The drug easily overcomes hematoparenchymal barriers, penetrates into tissues, through which it moves to the affected area (with the help of phagocytes with polymorphonuclear leukocytes, as well as macrophages), and then, in the presence of microbes, is released inside the infectious focus.

It passes through the plasma walls, making it very effective in treating infections caused by the activity of pathogenic bacteria located inside the cells.

The volume of the element inside cells with tissues is 10-15 times higher than plasma values, and its level inside the site of infection is 24-34% higher than the levels inside healthy tissues.

After the last use of the drug, the level of the substance required to maintain the antibacterial effect remains for another 5-7 days.

Inside the liver, the drug undergoes demethylation and loses its activity. Half of the consumed dose is excreted unchanged in the bile, and another 6% is excreted via the kidneys.

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Dosing and administration

The medicine should be taken once a day, 60 minutes before meals or 120 minutes after. The missed dose should be taken as quickly as possible, and the next one should be taken after 24 hours.

Portion sizes for adults and children weighing over 45 kg:

• treatment of pathologies of the respiratory tract, soft tissues and skin - 0.5 g once a day. Therapy lasts 3 days;
• for chronic erythema migrans - on the 1st day take 2 tablets of the drug with a volume of 0.5 g, and over the course of the 2nd-5th days take 0.5 g once a day;
• treatment of uncomplicated urethritis or cervicitis – single use of 1 g of the drug.

Use of Azithromycin Forte.

To eliminate diseases in the respiratory system, skin and soft tissues, it is recommended to take 1.5 g of the drug per course (divide the dosage into 3 doses with intervals of 24 hours).

To get rid of acne, the medicine is taken for 3 days at a dosage of 0.5 g / day, and then for the next 9 weeks it is required to use it once a week, 500 mg. The 4th tablet must be taken on the 8th day of the course. In the future, portions are used at intervals of 7 days.

For therapy of tick-borne borreliosis, the patient should take 1 g of the drug on the 1st day, and then 500 mg on days 2-5. In total, 3 g of the substance should be taken for the entire course.

The dosage for children is determined by their weight. The standard ratio is 10 mg/kg per day. Treatment can be done according to the following scheme:

• 3 doses of 10 mg/kg at intervals of 24 hours;
• 1 dose of 10 mg/kg, and 4 doses of 5-10 mg/kg.

At the initial stage of development of tick-borne borreliosis, the size of the first dose for a child is 20 mg/kg, and in the following 4 days the children's drug is used at a dose of 10 mg/kg.

During pulmonary inflammation, the drug must first be administered intravenously (at least 2 days at a rate of 0.5 g/day). After this, the patient is transferred to taking capsules. This therapy lasts 1-1.5 weeks. The size of the medicinal portion is 0.5 g/day.

During diseases in the pelvic area, at the initial stage of therapy, it is also necessary to administer infusions, after which the patient should take capsules of 0.25 g (2 pieces per day for 7 days).

The timing of the transition to taking capsules/tablets is determined taking into account changes in the clinical picture and laboratory data.

To prepare the suspension, 2 g of the substance must be diluted in water (60 ml).

When preparing a solution for injection, 0.5 g of lyophilisate must be dissolved in dilute water (4.8 ml).

If infusions are required, 500 mg of lyophilisate is diluted to a concentration level of 1-2 mg/ml (up to 0.5 or 0.25 l, respectively) using Ringer's solution, sodium chloride solution (0.9%) or dextrose (5%). In the first case, the infusion procedure should last 3 hours, in the second - 1 hour.

Therapeutic regimen for the treatment of ureaplasma.

When eliminating ureaplasmosis, complex therapy should be used.

A few days before starting to use Azithromycin, the patient must be prescribed immunomodulators. The medicine is administered intramuscularly, once a day, with intervals of 1 day. Such injections must be carried out during the entire therapeutic course.

Along with the 2nd use of the immunomodulator, the use of a bactericidal antibiotic begins. After finishing its intake, a transition to Azithromycin should be made. During the first 5 days, the medicine should be taken daily, in a dosage of 1 g - before breakfast (1.5 hours).

At the end of this time period, it is necessary to take a break for 5 days, after which start using the drug again, following the above scheme. After the next 5 days, it is necessary to take another 5-day course of Azithromycin - for the last, 3rd time. The dosage size remains the same everywhere - 1 g.

During the 15-16 day period of therapy using Azithromycin, the patient must also take 2-3 times a day medications that stimulate the binding of their own interferons, as well as antifungal drugs from the polyene category.

After completing a course of antibiotics, it is necessary to undergo restorative treatment, which involves using agents that stabilize the gastrointestinal tract and help restore its microflora. Maintenance therapy should last at least 14 days.

Treatment regimen for the elimination of chlamydia.

For chlamydia in the lower urogenital system, Azithromycin is most often prescribed - due to the fact that this drug is well tolerated, and in addition, it can be used by adolescents and pregnant women.

When treating the described form of the disease, the drug is taken once in a 1 g dose.

If chlamydia of the upper genitourinary tract is observed, therapy is carried out in short courses, between which it is necessary to maintain long intervals.

The course requires taking the drug three times (the dosage is 1 g). The intervals between doses are 7 days. Thus, the drug should be taken on the 1st, 7th and 14th days.

Using medication to relieve sore throat.

All antibiotics used to treat tonsillitis must be taken in a 10-day course, but Azithromycin is used according to a different scheme - the course of its administration lasts 3-5 days.

Another advantage of the drug is its higher tolerability (better than penicillin antibiotics) - macrolides are considered to have the lowest toxicity.

For adults and children over 45 kg, the serving size is 0.5 g/day. If a dose is missed, it should be taken as soon as remembered, and all subsequent doses should be taken at intervals of 24 hours.

Children over 6 months and up to 12 years of age should take the medicine in the form of a suspension. It is taken once a day. The therapy lasts at least 3 days, and the portion size is selected individually.

Use of drugs for sinusitis.

To treat sinusitis, it is necessary to use the drug according to one of the following regimens:

• On the first day, take 0.5 g of the medicine, and then for another 3 days in the same dosage;
• Take 0.5 g of Azithromycin on the first day, and then take 0.25 g for another 4 days.

Children under 12 years of age should take the suspension. The dosage is selected based on 10 mg/kg of weight. The drug should be taken once a day for 3 days. Sometimes doctors prescribe a slightly modified regimen - taking 10 mg/kg on the first day, and then, over the next 4 days, reducing the portion size to 5 mg/kg. A maximum of 30 mg/kg is allowed per course.

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Use Azithromycin during pregnancy

During breastfeeding or pregnancy, the drug is used only in situations where the likelihood of benefit from therapy for the woman is higher than the possibility of complications for the baby or fetus.

According to some studies (such as those conducted during the Motherisk Program), Azithromycin is considered completely safe for use in pregnant women.

In each of the control groups (women from the 1st used azithromycin; from the 2nd – other antibiotics; from the 3rd – did not use antimicrobial drugs during therapy), the frequency of occurrence of severe developmental abnormalities in the fetus did not have significant differences.

Contraindications

Among the contraindications:

• the presence of intolerance to macrolides;
• severe stages of liver or kidney diseases.

The suspension is prohibited for use in infants weighing less than 5 kg, and tablets and capsules are prohibited for use in children weighing less than 45 kg.

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Side effects Azithromycin

The most commonly reported side effects include vomiting, lymphopenia, abdominal discomfort, visual disturbances, nausea, decreased blood bicarbonate levels, and diarrhea.

Sometimes patients experience: development of oral candidiasis, vaginal forms of infections, eosinophilia, leukopenia, hypoesthesia, vertigo, seizures (it was found that other macrolides can also cause seizures), feelings of drowsiness and syncope. In addition, there is a decrease in the frequency of bowel movements, a disorder of the olfactory and taste receptors (or a complete loss of smell and taste), headaches, anorexia, digestive disorders, gastritis and bloating, as well as increased fatigue. Along with this, the level of bilirubin and creatinine, AST with ALT and urea, and in addition to this, the level of K in the blood may increase. The development of arthralgia, itching, rash or vaginitis is also noted.

Thrombocytopenia, hyperactivity (motor or mental), neutrophilia, a feeling of aggression, anxiety, lethargy or nervousness, and also a hemolytic form of anemia are observed occasionally. Paresthesia, neurosis, asthenia, sleep disorders, constipation, hepatitis (FPP values also change), insomnia and intrahepatic cholestasis also occur. Changes in the color of the tongue, exanthema, Quincke's edema, TEN, tubulointerstitial nephritis, urticaria with acute renal failure, photophobia, erythema multiforme, candidiasis and anaphylactic shock are noted.

Chest pain and ventricular tachycardia may appear occasionally, and in addition, the heart rate may increase. It has been found that the same symptoms can be provoked by other macrolides. In addition, there is data on prolongation of QT interval values and a decrease in blood pressure.

Reactions such as liver dysfunction, anxiety, myasthenia gravis, or necrotic or fulminant hepatitis may also be expected.

Macrolides may occasionally cause hearing loss. In some patients, hearing impairment, tinnitus, or complete deafness have occurred.

Mostly, such cases were registered at the stage of research, in which the drug was used in large doses for a long time. The reports show that the above disorders are curable.

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Overdose

In case of intoxication, vomiting, bowel disturbances, nausea, and transient hearing loss are observed.

Symptomatic measures are taken to eliminate disorders.

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Interactions with other drugs

The absorption of the drug is reduced when combined with ethyl alcohol, food, and antacids containing Al3+ or Mg2+.

When macrolides are combined with warfarin, the anticoagulant effect may be potentiated, which is why people who use this combination (although tests have not shown changes in PT levels when taking these drugs in standard doses) need to carefully monitor these values.

Azithromycin does not interact with theophylline, carbamazepine, triazolam, terfenadine, and digoxin, which distinguishes it from other macrolides.

The combination of terfenadine and various antibiotics leads to prolongation of QT interval values, as well as to the development of arrhythmia. Therefore, azithromycin should be used with caution in individuals who use terfenadine.

Macrolides increase the values inside the plasma, and also enhance the toxic properties and inhibit the excretion of such substances as cycloserine, methylprednisolone with felodipine, as well as drugs that are oxidized with the participation of microsomes, and indirect coagulants. But when using azithromycin (and other azalides), such an interaction was not noted.

The drug's effectiveness is enhanced when used simultaneously with tetracycline or chloramphenicol. When combined with lincosamides, the drug's effect is weakened.

Drug incompatibility with heparin is noted.

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Storage conditions

Azithromycin (in any form of release) must be kept in a dark and dry place with a temperature of 15-25˚C. At the same time, the finished suspension of the drug must be kept at a temperature of 2-8˚C.

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Shelf life

Azithromycin in capsules and powder can be used for 2 years from the date of release of the drug. Tablets have a shelf life of 3 years, and the finished suspension can be stored for no more than 3 days.

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Reviews

Azithromycin, when used to treat tonsillitis, frontal sinusitis, chlamydia, as well as sinusitis and other pathologies caused by the action of bacteria sensitive to the drug, receives mostly good reviews.

The drug has a powerful effect in the treatment of bacterial infections, and is also tolerated by patients without complications. Side effects associated with the drug are rare and disappear completely after completion of therapy.

Doctors also speak positively about the drug. Among the main advantages of the drug, in their opinion:

• the presence of immunomodulatory and anti-inflammatory properties;
• powerful effect on relatively probable microbes causing infections developing within the respiratory system;
• forming high values of the substance inside the tissues, demonstrates bactericidal action against Haemophilus influenzae, Moraxella cartalais, Helicobacter pylori, gonococcus, pneumococcus, Streptococcus pyogenes, Campylobacter, Streptococcus agalactiae, Bordet-Gengou bacteria and Corynebacterium diphtheriae;
• effectively affects atypical pathogenic microbes that reproduce intracellularly (including chlamydia and mycoplasma);
• approved for use in pregnant women;
• has a medicinal form that can be prescribed to children.

Since Azithromycin has a post-antibiotic effect, it can be taken in short courses. At the same time, the effect of the drug allows increasing sensitivity to the impact of immune factors even in bacteria resistant to it.

The basis of macrolides, the element erythromycin, decomposes in the acidic environment of the stomach and also has a strong effect on intestinal motility. In turn, Azithromycin is not affected by the acidic environment of the stomach and acts less actively in relation to intestinal function.