Azithromycin

Azithromycin has a wide range of antibacterial activity.

[1], [2], [3], [4], [5]

Indications of the azithromycin

It is used to eliminate such disorders:

• infections affecting the ENT system and respiratory organs (such as pharyngitis with laryngitis and tonsillitis, and in addition sinusitis, otitis media, pulmonary inflammation and chronic bronchitis at the stage of exacerbation);
• uncomplicated infections of bacterial origin developing in the genitourinary system (triggered by the activity of Chlamydia trachomatis - urethritis or cervicitis);
• lesions affecting the skin or soft tissue (infectious form of dermatitis, erysipelas or impetigo);
• scarlet fever;
• Lima's disease at the initial stage;
• associated with the action Helicobacter pylori disease in the area of the 12-intestine or stomach.

[6], [7], [8], [9],

Release form

The release occurs in capsules or tablets with a volume of 0.25 or 0.5 g. Capsules with a volume of 0.25 g are produced by 6 pieces inside a blister (in a pack - 1 blister plate); volume 0.5 g - in the number of 3 pieces inside the blister cell (in the box - 1 blister).

In addition, the preparation may take the form of a powder used in the manufacture of a suspension for ingestion (volumes 0.1 g / 20 ml, 0.5 g / 20 ml or 0.2 g / 20 ml). Packed in plastic bottles with a capacity of 20 g - 1 such a vial in a pack together with a measuring cup.

[10], [11],

Pharmacodynamics

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

With the help of synthesis with a subunit of 50S ribosomes, the drug inhibits the process of protein biosynthesis and slows down microbial growth together with the inhibition of their vital activity. At high medicinal concentrations, a bactericidal effect is observed.

The medicament actively influences such microorganisms:

• Gram-positive (in addition to microflora resistant against erythromycin) - epidermal and golden staphylococcus, pneumococcus, streptococcus pyogenic and streptococcus agalactia, and in addition to streptococci from category C, F, and G;
• gram-negative - sticks of pertussis and paracottus, influenza rod, diplococci from the category of Neisseria, Legionella and Campylobacter, and in addition microbes from the monotypic subspecies of moraxella cataralis and Gardnerella catarrhalis;
• microflora of anaerobes (peptococci and peptostreptococcus, clostridium perfringence, and B. Bivius);
• Chlamydia (such as chlamydophile pneumonia and Chl. Trachomatis);
• Mycopaths from subspecies of mycobacteria;
• Mycoplasma (such as Mycoplasma pneumonia);
• ureaplasmas (such as ureaplasma urealiticum);
• spirochetes (bacteria that cause the appearance of pale spirochetes or the development of tick-borne borreliosis).

Lipofilen shows resistance to acidic medium.

[12], [13], [14]

Pharmacokinetics

When using capsules, tablets or suspensions, the active element is rapidly absorbed from the digestive tract.

Bioavailability indicators with the use of 0.5 g of drugs reach 37%, 2-3 hours are required to reach peak values of the substance. The level of protein synthesis inside the plasma is inversely proportional to the indices of the drug inside the blood and varies in the range of 7-50%. The elimination half-life is 68 hours.

Plasma values of drugs 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, and in addition macrophages), and then in the presence of microbes it is released inside the infectious focus.

Passes through the walls of the plasma, which is very effective in the treatment of infections that are caused by the activity of bacteria-pathogens that are inside cells.

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

After the last application of drugs, the indicator of the substance required to maintain the antibacterial effect persists for another 5-7 days.

Inside the liver, the drug undergoes demethylation and loses its activity. Half of the consumed portion is excreted unchanged with bile, and about 6% - with the help of kidneys.

[15], [16], [17], [18]

Dosing and administration

Use the medicine one time per day, 60 minutes before meals or 120 minutes after. The missed portion should be taken as quickly as possible, and the next one should be consumed after 24 hours.

The sizes of portions for adults, as well as children, whose weight is above 45 kg:

• Treatment of pathology of respiratory tract, soft tissues and skin - 0.5 g once a day. The therapy lasts 3 days;
• with the chronic form of erythema migratory nature - in the first day, take 2 tablets LS with a volume of 0.5 g, and during the 2-5th days, take 0.5 g once a day;
• treatment of urethritis or cervicitis of uncomplicated nature - a single use of the 1st g of drugs.

Use of Azithromycin Forte.

To eliminate diseases in the respiratory organs, skin and soft tissues, it is recommended to take 1.5 g of the drug per course (divide the dosage by 3 uses at intervals equal to 24 hours).

To get rid of acne, the drug 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 for 500 mg. Use the 4th pill on the 8th day of the course. Subsequently, portions are applied at intervals of 7 days.

For therapy in tick-borne borreliosis, the patient should take 1 g of drugs on the first day, and then 500 mg on days 2-5. In general, the whole course requires taking 3 g of the substance.

The sizes of children's dosages are determined by their weight. The standard ratio is 10 mg / kg per day. Treatment can occur according to this scheme:

• 3 use in a dose of 10 mg / kg at intervals equal to 24 hours;
• 1 consumption in a dose of 10 mg / kg, as well as 4 applications at a dosage of 5-10 mg / kg.

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

During pulmonary inflammation, it is first required to administer the drug intravenously (at least 2 days at a dose of 0.5 g / day). After this, the patient is transferred to the use of capsules. This therapy lasts 1-1.5 weeks. The size of the medicinal portion is 0.5 g / day.

During illnesses in the pelvic area at the initial stage of therapy, it is also necessary to introduce infusions, after which the patient should take capsules with a volume of 0.25 g (2 pcs per day for 7 days).

The terms for switching to capsules / tablets are determined taking into account changes in the clinical picture and laboratory data.

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

When making a solution for injection, it is necessary to dissolve 0.5 g of lyophilizate in d / and water (4.8 ml).

If it is necessary to administer infusions, 500 mg of lyophilizate is diluted to a concentration of 1-2 mg / ml (up to 0.5 or 0.25 L, respectively), with Ringer's solution, 0.9% solution of sodium chloride or dextrose (5%). In the 1st case the procedure of infusion should last 3 hours, in the second - 1 hour.

Therapeutic regimen in the treatment of ureaplasma.

When eliminating ureaplasmosis, complex therapy should be used.

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

Together with the second application of the immunomodulator, the use of an antibiotic of a bactericidal nature begins. At the end of his admission should make a transition to Azithromycin. During the first 5 days, the drug should be consumed daily, at a dosage of 1 g - before breakfast (1.5 hours).

At the end of this time interval, you need to take a break for 5 days, then again start using the drug, guided by the above scheme. After the next 5 days, another 5-day course of Azithromycin should be done - the last, the third, the time. The size of dosages everywhere remains the same - to 1 g.

During the period of 15-16 days, while therapy with Azithromycin lasts, the patient should also take 2-3 times a day of medication, stimulating the binding of their own interferons, and in addition antimycotics from the category of polyenes.

After the course of taking antibiotics, it is required to undergo restorative treatment, which uses drugs that stabilize the digestive tract and help restore its microflora. Supportive therapy should last at least 14 days.

Treatment regimen for the elimination of chlamydia.

With chlamydia in the lower part of the urogenital system, Azithromycin is most often prescribed - because this medicine is well tolerated, and in addition it can be used by adolescents and pregnant women.

In the treatment of the described form of the disease, the drug is consumed once in a portion of 1 g.

If clamidiosis of the upper part of the genito-urinary tract is observed, therapy is carried out with short courses, between which it is necessary to withstand long gaps.

The course requires three times to take the drug (dosage size is 1 g). Intervals between uses - 7 days. Thus, drugs must be taken on the 1st, 7th and 14th days.

Use of medication to eliminate sore throat.

All antibiotics, which are used in the treatment of angina, must be taken with a 10-day course, but Azithromycin is used according to a different scheme - the course of its reception lasts 3-5 days.

Another plus of the drug is its higher tolerability (better than penicillin antibiotics) - it is believed that macrolides have the lowest toxicity.

For adults, as well as children weighing more than 45 kg, the serving size is 0.5 g / day. When a dose is missed, it is necessary to take it immediately, as it will be remembered, and all subsequent procedures should take place at intervals of 24 hours.

Children older than 6 months and up to 12 years of age should use medication in the form of a suspension. Reception is carried out once a day. The therapy lasts at least 3 days, and the size of the portion is selected individually.

Application of drugs for sinusitis.

To treat sinusitis, you need to take the drug according to one of the following modes:

• in the first day, take 0.5 g of the drug, and then for another 3 days in the same dosage;
• reception in the first day of 0.5 g of Azithromycin, and then another 4 days to use in a dosage of 0.25 g.

Children younger than 12 years of age must take a suspension. Dosage is selected from the calculation of 10 mg / kg body weight. Use the drug once a day, for 3 days. Sometimes doctors prescribe a slightly changed regimen - taking 10 mg / kg on the first day, and then, in the next 4 days, reduce the portion size to 5 mg / kg. For the course, a maximum of 30 mg / kg is allowed.

[24], [25], [26],

Use of the azithromycin during pregnancy

When breastfeeding or pregnancy, the drug is used only in situations where the likelihood of the benefits of therapy for a woman is higher than the possibility of complications in the infant or fetus.

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

In each of the control groups (women from the first used azithromycin, of the second - other antibiotics, of the third - did not use for the treatment of antimicrobial drugs), the frequency of appearance of severe anomalies in the development of the fetus did not differ significantly.

Contraindications

Among the contraindications:

• the presence of intolerance against macrolides;
• severe stages of hepatic or renal diseases.

Suspension is forbidden to appoint infants, whose weight is less than 5 kg, and tablets with capsules - children, whose weight is less than 45 kg.

[19], [20], [21]

Side effects of the azithromycin

The most common side effects are vomiting, lymphocytopenia, abdominal discomfort, visual disturbances, nausea, a decrease in the level of blood bicarbonates, and diarrhea.

Sometimes the patients are noted: the development of oral candidiasis, vaginal forms of infections, eosinophilia, leukopenia, hypesthesia, vertigo, seizures (it was found that other macrolides can also cause seizures), drowsiness and syncope. In addition, there is a decrease in the frequency of intestinal emptying, a breakdown in the function of olfactory and taste buds (or complete loss of odor and taste), headaches, anorexia, digestive disorders, gastritis and bloating, and increased fatigue. Along with this, the level of bilirubin and creatinine, AsAt with AlAT and urea, and in addition to this level of K inside the blood can increase. There is also a development of arthralgia, itching, rash or vaginitis.

Occasionally, there is thrombocytopenia, hyperactivity (having a motor or mental character), neutrophilia, a feeling of aggressiveness, anxiety, lethargy or nervousness, as well as a hemolytic form of anemia. Also there are paresthesia, neurosis, asthenia, sleep disorders, constipation, hepatitis (also change the values of PFR), insomnia and intrahepatic cholestasis. There is a change in the shade of the tongue, exanthema, Quincke edema, TEN, tubulointerstitial nephritis, urticaria with OPN, photophobia, erythema multiforme, candidiasis and anaphylactic shock.

Single pain can appear in the sternum and ventricular tachycardia, and in addition to intensify the rhythm of the heartbeat. It was revealed that the same signs can be provoked by the action of other macrolides. In addition, there is evidence of prolongation of QT-interval values and a decrease in blood pressure.

One can also expect the appearance of such reactions as functional insufficiency of the liver, a feeling of excitement, myasthenia gravis or hepatitis of a necrotic or fulminant character.

Occasionally, macrolides may cause hearing loss. In some patients, hearing disorder occurred, there was an ear ring or complete deafness developed.

Basically, such cases were recorded at the research stage, in which the drug was used in large portions for a long time. The reports demonstrate that the above violations are curable.

[22], [23]

Overdose

In intoxication, vomiting, stools, nausea, and a transient loss of hearing are noted.

Symptomatic measures are taken to eliminate the disorders.

[27], [28]

Interactions with other drugs

Absorption of drugs is reduced when combined with ethyl alcohol, food, as well as antacid agents containing Al3 + or Mg2 +.

When combining macrolides with warfarin, potentiation of anticoagulant effects is possible, which means that people who use this combination (although the tests did not show changes in the level of PTV when taking these drugs in standard portions), it is necessary to closely monitor these values.

Azithromycin has no interaction with theophylline, carbamazepine, triazolam, terfenadine, and digoxin, which differs from other macrolides.

The combination of terfenadine and various antibiotics leads to the prolongation of QT-interval values, and in addition to the development of arrhythmia. Therefore, caution should be applied to azithromycin in persons who use terfenadine.

Macrolides increase the values inside the plasma, and in addition increase toxic properties and inhibit the excretion of substances such as cycloserine, methylprednisolone with felodipine, as well as drugs that oxidize with microsomes, and indirect coagulants. But with the use of azithromycin (and at the same time other azalides), such an interaction was not noted.

An increase in the effectiveness of the drug is observed with simultaneous use with tetracycline or chloramphenicol. When combined with lincosamides, the effect of LS on the contrary is weakened.

Drug incompatibility of the drug with heparin is noted.

[29], [30], [31], [32]

Storage conditions

Azithromycin (in any form of release) is required to be kept in a dark and dry place with a temperature in the range of 15-25 ° C. At the same time, the finished suspension of the preparation should be kept at a temperature of 2-8 ° C.

[33], [34], [35], [36]

Shelf life

Azithromycin in capsules and powder can be used for 2 years since the release of the drug. Tablets have a shelf life of 3 years, and the finished suspension is allowed to store no more than 3 days.

[37], [38],

Reviews

Azithromycin in the treatment of angina, frontal sinusitis, chlamydia, as well as sinusitis and other pathologies caused by the action of bacteria sensitive to drugs, gets mostly good reviews.

The drug has a powerful effect in the treatment of infections of bacterial origin, and at the same time, without complications, it is tolerated by patients. The drug-related side effects are rare and completely go away after completion of therapy.

Physicians also speak about the medicine positively. Among the main advantages of drugs, in their opinion:

• presence of immunomodulating and anti-inflammatory properties;
• powerful impact of relatively likely microbes-pathogens of infections developing within the respiratory system;
• forming high values of the substance inside the tissues, demonstrates bactericidal action against the hemophilic rod, Morakselly kartralis, Helicobacter pylori, Gonococcus, Pneumococcus, Streptococcus pyogenes, Campylobacter, Streptococcus agalactia, Borde-Gangu bacteria and diphtheria corynebacterium;
• effectively influences atypical microbes-pathogens, multiplying intracellularly (among such chlamydia with mycoplasmas);
• is permitted for use in pregnant women;
• has a medicamentous form that can be prescribed to children.

Since Azithromycin has a postantibiotic effect, it can be taken as short-term courses. At the same time, the influence of the drug makes it possible to increase the sensitivity with respect to the influence of immune factors, even in bacteria resistant to it.

The basis of macrolides, the element erythromycin, decomposes inside the acidic gastric environment, and also has a strong effect on intestinal motility. In turn, Azithromycin is not affected by the acidic environment of the stomach and less active against the intestinal function.