A popular and reliable modern antibiotic presented in almost any pharmacy is Azithromycin. Instructions for use of the drug indicate that the medication belongs to the category of antimicrobial formulations extensive in their effect. Belongs to the macrolide group. The name was given to the drug by the active component - it is azithromycin, which is part of the class of azalides. The drug in pharmacies is represented by capsules, tablets and suspension. Suitable for the treatment of children and adults.
What is for sale?
Most often, patients visit a pharmacy to buy Azithromycin tablets. Instructions for use and packaging of the drug contain a reference to the amount of active ingredient in a single dose. There are three options for release: 125, 250, 500 mg. 250 mg is an option produced not only by tablets, but also by capsules. Distinctive features are additional components used in the manufacture of the drug. A complete list is necessarily indicated in the instructions for use. Azithromycin may contain substances that are not tolerated by a particular patient, therefore it is important to study the accompanying documentation.
As auxiliary compounds, manufacturers most often use:
- cellulose;
- lactose;
- povidone;
- magnesium stearate;
- aerosil.
Drug dynamics
The manufacturer in the instructions for use of "Azithromycin" indicates that the drug belongs to the class of azalides, that is, medications based on macrolides. The main effect of the application is bacteriostatic. Soon after penetration into the body, the active substance enters into strong bonds with the components of the ribosome, which means that it slows down the translation of the peptide translocase. In the molecule of a pathological microorganism, the processes of formation of protein structures are inhibited, growth and reproduction are prevented, therefore, colonies cannot develop.
The manufacturer also indicates in the instructions for use: "Azithromycin" in a high dose can have a bactericidal effect.
The effectiveness of the drug shows both against pathogens that can invade the cell, after infection with extracellular forms. Activity was identified relative to certain representatives of the following species and groups:
- staphilo-, strepto-, peptrostreptococci;
- chlamydia
- clostridia;
- neysseries;
- legionella;
- hemophilic bacillus;
- moraxella;
- campylobacter;
- bordetella;
- urea, mycoplasmas;
- mycobacteria;
- treponema.
Drug kinetics
According to the instructions for use, Azithromycin (500 mg capsules, tablets, powder for suspension) is based on the active ingredient, which is absorbed into the body at a relatively high rate after oral administration. The substance is lipophilic, shows an increased level of resistance to acids. The bioavailability with a single use in food of 500 mg is estimated at 37%. The indicator is determined by the passage through the liver cells. The highest parameters in the blood of azithromycin are observed at the level of 0.4 mg / l. The time period required to achieve this indicator is from two and a half to three hours.
As follows from the instructions for use of "Azithromycin", 500 mg of the active component at the initial intake is orally distributed in a volume varying about 31.1 l / kg. In tissues, cells of the body, the substance accumulates more actively than in the blood plasma, 10-50 times.
Studies have shown that at any dosage (150, 250, 500 mg), Azithromycin (the manufacturer pays attention to this fact in the instructions for use) is able to penetrate the barriers present in the body. Quite quickly, the active component enters the soft tissues and organs of the respiratory system, reproductive, urinary system, prostate gland, skin integuments. The cumulative effect is observed in environments that are characterized by a low level of acidity. "Azithromycin" is able to cumulate in lysosomes. This effect has found application for the eradication of pathogens that invade cell cavities.
Biological chemistry
In the body, the active component of the drug is carried by macrophages, phagocytes, certain categories of leukocytes. The instructions for use with "Azithromycin" (500 mg capsules and other release options) indicate the ability to penetrate cell membranes. As it was possible to identify during specific studies, in the infected focus, the active compound accumulates in the amount of a quarter, sometimes even a third, exceeding the content in other tissues of the body. Specific indicators are determined by the intensity of the inflammatory process.
If you take tablets, syrup, Azithromycin capsules as a course of food according to the instructions for use (500 mg or other volume as recommended by the doctor), after the last dose is received in the tissues and cells of the body, the active substance is stored in sufficient concentrations to have a bactericidal effect, a few more days: from five to seven.
The level of entry into association with plasma proteins in a particular case is almost impossible to predict. In the instructions for use of Azithromycin capsules, tablets and suspensions, the manufacturer indicates that in some patients the parameter was estimated at only 7%, while in others it reached half of the total dose used. The degree of entry in connection with plasma proteins is inversely proportional to the concentration of the components of the drug in the circulatory system.
Once in the liver cells, azithromycin enters into chemical reactions, as a result of which products are formed that do not have a pharmacological effect on the patient's body. Plasma clearance, as indicated in the instructions for use of "Azithromycin" in capsules, tablets, powder, is estimated at 630 ml / min. The withdrawal from the circulatory system occurs in two stages:
- 14-20 hours in the range of 8-24 hours after using the medication for food;
- 41 hours - in the interval 24-72 hours after administration.
Elimination of about half of the substance received in the body is carried out through the bile ducts; the agent leaves the body without transforming. About 6% are excreted in urine.
In the instructions for use of "Azithromycin" (500 mg and other dosage options), the manufacturer indicates a strong influence on the kinetics of the drug from food. If you use the substance during the meal, the highest concentration indicators are more than halved. In old age, mainly in men, the pharmacological kinetics remains the same as in younger patients. In women, usually the highest concentration indicators increase by a third, and sometimes by half relative to the characteristic middle-aged patients, youth.
When will it help?
The instructions for the use of "Azithromycin" (500 mg, 125 and 250 mg) indicate the following diagnoses in which the drug shows pronounced effectiveness:
- Lyme disease (initial stage);
- cervicitis;
- tonsillitis;
- urethritis;
- erysipelas;
- dermatosis;
- bronchitis;
- pulmonary inflammation;
- impetigo;
- angina;
- otitis;
- sinusitis.
Before taking, it is reasonable to conduct a test to establish the sensitivity of pathological microorganisms to azithromycin. Efficiency (this particular attention is paid to the instructions for use of "Azithromycin" - 250, 125 and 500 mg capsules, tablets, suspensions) is expressed only if the disease is caused by strains sensitive to the antimicrobial drug.
Limitations
The manufacturer indicates that Azithromycin is not intended for use by persons suffering from hypersensitivity to drugs from the macrolide category.
Particular attention should be paid to patients who have established insufficient functioning of the kidneys, liver. Such health problems are not absolute contraindications, but improper use can provoke adverse reactions.
Rules and Scopes
The choice of dosage, format must be subordinated:
- diagnosis;
- the sensitivity of pathological life forms to antibiotics;
- individual characteristics of the patient (weight, age).
As a rule, the doctor sends to the tests, allowing to establish the specifics of pathological microflora. Based on the information received, the doctor prescribes the drug, prescribes a prescription for it (the drug is not dispensed from pharmacies in any form without it, as indicated in the instructions for use). Adults "Azithromycin" is often recommended in the form of tablets, capsules. The manufacturer advises using this form of medicine one hour before the meal or 120 minutes after it. "Azithromycin" is used once a day.
If infection of the skin, soft tissues, organs of the respiratory system is established, for adult patients the optimal format of the course:
- 0.5 g on the first day;
- 0.25 g for another 2-5 days.
Less often, the doctor recommends (for the possibility of such a course is indicated in the instructions for use) for adults "Azithromycin" 500 mg three days in a row.
How is borreliosis treated initially? According to the instructions for use, "Azithromycin": 250 mg (four capsules) or 500 mg (two capsules) on the first day, then the dosage is halved.
When compiling an admission scheme for minors, it is necessary to focus not only on age, but also on body weight. The optimal format is a suspension for children. The instructions for use of "Azithromycin" indicate that with a weight of more than 10 kg on the first day, the drug is used in an amount of 10 mg per kilogram of weight, then the dosage is reduced by half and maintained at this level until the program is completed. An alternative is a three-day course, each day the dose is calculated as 10 mg per kilogram of weight.
Features of use
The manufacturer draws attention to the fact that when skipping a dose, it is necessary to replenish this amount as soon as possible. The next dose should be a day after the use of the missed amount.
As tests have shown - and this is recorded in the instructions for use - Azithromycin (250 mg, 500, 125 mg) is characterized by increased resistance to acid influence. The tool is quickly and effectively absorbed when passing through the gastrointestinal tract, penetrates the skin, other organs and tissues.
Increasing the concentration of azithromycin in the inflammatory focus allows to achieve a bactericidal effect, the duration of which is up to a week after the last dose is ingested. Therefore, you can use the tool for a very short course, following the instructions for use. Reviews on "Azithromycin" contain information on the effectiveness of the composition, even if it takes only three days to heal. Sometimes a five-day intake is necessary, it is almost always enough to achieve a pronounced result.
Particularly noteworthy are patients using an antimicrobial drug in combination with antacids. At least two hours should elapse between taking these groups of drugs, otherwise the effectiveness of the antibacterial composition will be too low.
Negative effects: what to prepare for?
In general, the drug is tolerated quite well, therefore, its use is practiced even for the treatment of children. And yet, as can be seen from the responses to the drug (as well as from the text of the instructions for use), Azithromycin (suspension, tablets, capsules) can cause:
- vomiting
- nausea
- increased gas formation;
- activation of liver enzymes.
In a small percentage of patients, skin rashes were observed with the use of the composition.
If you feel sick and vomit very badly, stools are broken, hearing is impaired, the patient probably took too much “Azithromycin”. To alleviate the condition, urgent gastric lavage is required. Therapy is carried out, focusing on the disturbing symptoms. There is no specific antidote to the antimicrobial drug.
Requires attention!
As indicated for different dosage options (125, 500, 250) in the instructions for use, "Azithromycin" for children in the mother’s womb can be harmful, therefore, use of the product by pregnant women is allowed only in extremely rare cases. The doctor evaluates the obvious benefits of the medication, the possible dangers, notifies the woman, only after that they decide on the use of the medicine.
Since studies have shown that active components can pass into breast milk, in order to avoid the effect of Azithromycin on children, the instructions for use indicate the need to stop breast-feeding during treatment until the composition is completely removed from the mother's body.
In rare cases, the antimicrobial composition can cause side effects for vision, the nervous system. This forces you to be especially careful during the use of tablets, when driving vehicles and other units, devices that require increased care. At the same time, there are no strict restrictions on such activities, since the risk of developing negative side effects is estimated as low.
Mutual influence
Digoxin and azithromycin in combination can cause an increase in blood serum P-glycoprotein. In some cases, the number of cardiac glycosides in the blood plasma increases significantly, which means that the likelihood of glycoside poisoning increases.
The combination of zidovudine and azithromycin can cause the first compound to be poorly effective, since the kinetics may change with a single use of one gram of azithromycin or multiple doses of 0.6–1.2 g. It is known that the combination of azithromycin and zidovudine can cause an increase in mononuclear cells in the peripheral circulatory system of the active product of zidovudine processing. At the moment, it was not possible to establish the clinical significance of this phenomenon.
To a low degree, azithromycin reacts with cytochrome isoenzymes. The simultaneous use of the antimicrobial composition and ergot alkaloids is associated with a risk of ergotism, therefore, a combination of these groups of drugs should be avoided.
Daily use of 0.5 g of azithromycin and 10 mg of atorvastatin does not provoke changes in the concentration of the second substance in the circulatory system during the course, but it is known that in some patients rhabdomyolysis was fixed with a combination of antimicrobial composition and some statins.
Terfenadine and azithromycin in the complex can lead to a violation of the rhythm of the heartbeat, an increase in the QT interval. Ventricular fibrillation is possible with a combination of antibiotic and disopyramide. Rhabdomyolysis is possible with a combination with lovastatin, and in combination with rifabutin, the risk of neutro-leukopenia increases.
The simultaneous intake of cyclosporine and the drug in question leads to improper processing of the first compound, which means that the risk of poisoning, side effects inherent in cyclosporine, increases.
Antacids, which include aluminum, magnesium, ethanol, and food products, can reduce the absorption of antimicrobial substances.
What else to look for?
In the instructions, the manufacturer mentions that the combination of the drug with warfarin can provoke an adjustment of the prothrombin time if the compositions are used in doses higher than recommended by the manufacturers. At the moment, such cases have not been recorded, but the experience of combined use of warfarin, macrolides shows that patients require special monitoring and periodic verification of the quality of the circulatory system.
The combination of the drug in question and dihydroergotamine, ergotamine can cause the latter to be poisoned. The condition manifests itself as vasospasm, dysesthesia. When combined with triazolam, clearance decreases, which means that the pharmacological effect becomes more pronounced.
"Azithromycin" can cause slow elimination, an increase in the amount of substances in the plasma, as well as toxicity above the norm for the following drugs:
- cycloserine;
- coagulants that have an indirect effect on the body;
- methylprednisolone;
- felodipine;
- substances oxidized at the microsomal level.
Azithromycin acts more pronounced if you combine an antibiotic with tetracycline, chloramphenicol. A decrease in the effectiveness of the intake is observed with the simultaneous ingestion of the drug in question and lincosamides.
Analogs
The instructions for use of "Azithromycin" indicate that the active component of this drug is called the same as the medication itself - azithromycin. Medicines are based on it:
- Hemomycin;
- "Azimycin";
- "Sumamed."
It is possible to replace the medicine in question with Ekomed or Zitrocin.
Based on the diagnosis, the condition of the patient, the individual characteristics of the body, the doctor may advise as an alternative the drugs:
- "Fromilide";
- Lekoklar;
- "Rovamycin."
«» «». «» «». «» «».
. , , .
Will it help?
, «» , . «» , , . , , , , .
, , , . . «» (250 ) , . , , , – , . , .
«» , , . , , . , : «» .
Reviews of specialists
As can be seen from the responses, the Azithromycin doctors are in good standing - the drug is effective, rarely leads to unpleasant impressions in patients, it is used for a variety of diseases. The drug relieves inflammation, has certain qualities of an immunomodulator, is suitable for children and adults, therefore it is, if not universal, then close to it. Doctors highly appreciate the bactericidal qualities of this representative of macrolides, note the high efficiency.
The tool is indispensable for diseases of the respiratory system, as it can accumulate in this area, and also shows a pronounced effect against pathological microorganisms that are resistant to many other medicines available to modern people. The active substance has a post-antibiotic effect, which means that “Azithromycin” is effective even with short-term use. Using the composition according to the instructions helps to increase the sensitivity of bacteria to the immune system, and therefore, strengthen the body's own forces in the fight against the disease.
To some extent, the antimicrobial drug is similar to those based on erythromycin, but has a distinct advantage - it does not harm the acidic gastric environment. In addition, "Azithromycin" shows a rather weak effect on the gastrointestinal tract, which means that the risk of side effects is lower.
About pricing
The cost of the drug depends on the manufacturer, form of release, dosage of the active compound, the number of tablets in the package. A significant role is played by the pricing policy of a particular point of sale. On average, a cardboard box containing six capsules of Azithromycin and instructions for using the drug costs from 50 rubles and above. The dosage of the active compound is 250 mg. Double the amount of the drug in one dose with an equal number of copies in the package will cost the buyer a little more - the prices start at 55 rubles.
Among other antibiotics, Azithromycin is one of the most accessible and widespread.
About analogues: "Sumamed"
Both medicines belong to the class of macrolides, a group of azalides. Their feature is the chemical structure, which is very different from all other antimicrobial agents known to people. Both drugs have increased resistance to acidic environments, which is due to the peculiarities of the location in the molecules of carbon and nitrogen atoms.
If we evaluate modern medical practice, we can conclude that Sumamed is prescribed more often than Azithromycin. “Sumamed” for sale is represented by capsules, tablets, powder, on the basis of which it is possible to make a suspension - in a word, the release forms coincide with those described above for “Azithromycin”. Both drugs can be used as therapeutic if the child is sick, but it is permissible to apply strictly under the supervision of a doctor. Both drugs are based on azithromycin, have a bacteriostatic effect, strongly affect pathological microorganisms from the groups of gram-positive, gram-negative, anaerobic.
The manufacturer indicates that Sumamed is able to be rapidly absorbed when passing through the gastrointestinal tract, it soon accumulates in infectious foci, affecting microorganisms: inhibits growth and reproduction by suppressing protein synthesis. It is known that bacteria are able to obtain resistance to azithromycin, which imposes serious restrictions on the possibility of using both drugs. In order for the course to show a pronounced effect, tests should first be done to check the sensitivity of the bacteria to the antimicrobial substance.
Important Features
"Sumamed" is intended for use once a day. Between receptions stand exactly 24 hours. To maximize the effectiveness of the therapeutic course, rules and time limits should be followed. You can use the medication if the infection is localized in the organs of the ear, throat, nose, reproductive, urinary, respiratory. "Sumamed" is indicated at the initial stage of Lyme disease and in the treatment of genital infections.
Doctors note that, on average, Sumamed provokes side effects somewhat less frequently than the Azithromycin described above, although both of these medications are well tolerated by patients of different age groups. On the other hand, Sumamed costs much more, since the drug is imported. A package containing three 500 mg capsules, on average in pharmacies, costs 450-500 rubles.
Sumamed is slightly different in composition from Azithromycin, which allows the drug to be used for gastritis, duodenitis, intestinal ulcers, and stomach - Azithromycin is ineffective in these diseases. But both drugs are used if the patient suffers from severe acne.
Important aspects!
Azithromycin, as tests have shown, is more toxic than Sumamed. It is not used for the treatment of children under the age of twelve, they are not combined with alpha-blockers. "Sumamed" is considered safer, appointed from six months of age (in the form of a suspension). You can use the product during breastfeeding, if there is no effective alternative.