Macrolides: drugs of this group of antibiotics,list, titles, performance

Update: October 2018

Macrolides – a group of antibacterial drugs, the basis
the structures of which a macrocyclic lactone ring acts.
Thanks to the ability to disrupt the formation of bacteria proteins,
macrolide antibiotics stop their livelihoods. AT
high dosages drugs completely destroy
microorganisms.

Macrolide antibiotics show activity by
relation to:

  • gram-positive bacteria (streptococci, staphylococci,
    mycobacteria, etc.);
  • gram-negative bacilli (enterobacteria, Helicobacter
    pylori, hemophilus bacillus, etc.);
  • intracellular microorganisms (moraksella, legionella,
    mycoplasmas, chlamydia, etc.).

The action of macrolides is mainly aimed at therapy.
infectious diseases of the respiratory tract due to atypical and
gram-positive pathogens.

Popular drugs

AT списке антибиотиков группы макролиbeforeв выделяются два вещества,
most used at the moment:

  • clarithromycin;
  • azithromycin.

They are representatives of two different macrolide generations.
drugs. Из них позднее был получен azithromycin. Despite,
that they are united by the mechanism of action on microbes and belonging
To the same group, there are significant differences:

Comparison option Azithromycin Clarithromycin
Microbial spectrum of action
  • ATнутриклеточные организмы (хламидии, микоплазмы, уреаплазмы,
    legionella).
  • Streptococcus.
  • Staphylococcus (other than erythromycin-resistant – for
    azithromycin).
  • Anaerobic bacteria (clostridia, bacteroids).
  • Gram-negative bacteria (hemophilus bacillus, moraxella,
    meningococcus, pertussis bacillus).
  • Gonococcus
  • Spirochetes
  • Mycobacteria, incl. tuberculosis.
  • Toxoplasma.
  • Meningococcus.
  • Helicobacter pylori.
Effect speed AT течение 2-3 часов. Stable concentration of the drug in the blood
appears after 5-7 days of regular intake.
AT течение 2-3 часов. Stable concentration of the drug in the blood
– after 2-3 days of regular admission.
Efficiency Same efficacy in the treatment of Helicobacter gastritis.
Azithromycin лучше распространяется по тканям легкого при лечении
pulmonary infection, however, the effectiveness of the drug is similar to
clarithromycin in a similar case of appointment. Azithromycin
more effective with legionellosis.
Adverse reactions
  • Центральная и периферическая нервная система:
    systemic vertigo, headaches, nightmares, general
    excitability, hallucinations, disturbed rhythm of sleep-wakefulness.
  • Сердце и сосудистое русло: сердцебиение,
    tachycardia.
  • Пищеварительный тракт: тошнота, рвота, боли в
    diarrhea, short-term elevation of liver enzymes
    (alanine and aspartate aminotransferase), jaundice.
  • Аллергические проявления: сыпь (крапивница),
    itchiness
  • ATагинальный кандиbeforeз.
  • Anaphylactic shock (occasionally).
  • Increased UV sensitivity.
  • Candidiasis of the oral mucosa.
  • Violation of the electrical conductivity of the myocardium in the form of arrhythmias
    (seldom).
  • Снижение числа тромбоцитов (seldom).
  • Неbeforeстаточность почечной функции (seldom).
  • Anaphylactic shock.
  • Angioedema.
  • Malignant exudative erythema (syndrome
    Stevens-Johnson).
Safety for pregnant and lactating patients
  • Should refuse to lactation.
  • Use during pregnancy may be permitted if use
    from the drug supposedly higher risks to the fetus.

Thus, the benefits of azithromycin include
fewer adverse reactions in the form of severe hazardous
life states.

For clarithromycin, the advantages of use are a wider
spectrum of action and rapid achievement of stable blood levels
the patient.

The main minus for both macrolide antibiotics is undesirable
use for pregnant women, which complicates the choice of the drug in this
population groups.

Macrolide classification

ATсе поколения макролиbeforeв, появившиеся по мере продвижения
scientific studies are divided by their origin into natural
and semi-synthetic. The first are derivatives of natural
raw materials, the second – artificially derived medicinal substances.

Also important is the division of drugs according to their structural
features. AT зависимости от того, сколько углеродных атомов
contains macrolide ring matter, they are divided into 3 large
generations:

14-member

Representatives Tradename Method of use, price
Oleandomycin Oleandomycinа фосфат Byрошок-субстанция. Obsolete macrolide,
practically does not occur in pharmacies.
Clarithromycin Klacid Pills: 0,5 гр х 2 раза в день, прием 14
days 500-800 rubles
Granules for suspension preparation inside
флаконе
: медленно залить воду before отметки, встряхнуть
bottle, drink twice a day (the bottle contains 0.125 or 0.25 g
substances). 350-450 rub.
Раствор для внутривенного введения: 0,5 гр х 2
once a day (daily dose – 1.0 g), after mixing with
solvent. 650-700 rubles
Claritrosin Pills: 0,25 гр х 2 раза в сутки без
зависимости от приема пищи, курс 14 days 100-150
rub.
Fromilid Pills: 0,5 гр х 2 раза в день без
зависимости от приема пищи, курс 14 days 290-680
rub.
Clarithromycin-Тева Pills: 0,25 гр х 2 раза в день курсом 7 дней
or increase the dose to 0.5 g x 2 times a day course of 2 weeks.
380-530 rub.
Erythromycin Erythromycin Pills: по 0,2-0,4 гр четыре раза в сутки before
(for 30-60 minutes) or after eating (in 1.5-2 hours), drinking water,
курс 7-10 days 70-90 rub.
Глазная мазь: помещать за нижнее веко трижды в
день, курс 14 days 70-140 rub.
Мазь для наружного применения: на пораженную
skin with a small layer 2-3 times a day, the duration of the course
determined individually depending on the severity of the pathology.
80-100 rub.
Lyophilisate for the preparation of intravenous
раствора
: по 0,2 гр вещества, разведенного растворителем,
3 times a day. The maximum duration of use is 2 weeks.
550-590 rub.
Roxithromycin Esparoxy Pills: 0,15 гр х 2 раза в сутки за 15 минут
before приема пищи или 0,3 гр однократно, курс 10 days 330-350
rub.
Rulid Pills: 0,15 гр х 2 раза в сутки, курс 10
days 1000-1400 rub.
RoxGEKSAL Pills: 0,15 гр х 2 раза в сутки или 0,3 мг в
один прием, курс 10 days 100-170 rub.

15-member

Representatives Tradename Method of use, price
Azithromycin Sumamed Pills: 0,5 гр х 1 раз в сутки за час before или
2 hours after meals. 200-580 rub.
Powder for suspension inside
флаконах
: beforeбавить в содержимое флакона 11 мл воды,
shake up, take once a day, an hour before or in 1.5-2 hours
after meal. 200-570 rub.
Капсулы: по 0,5 гр (1 капсула) одиножды в день
one hour before or 2 hours after meals. 450-500
rub.
Azitral Капсулы: по 0,25/0,5 гр х 1 раз в день перед
или 2 hours after meals. 280-330 rub.
Nitrolide Капсулы: по 2 капсулы (0,5 гр) в один прием 1
once a day. 280-350 rub.
Azitrox Капсулы: по 0,25/0,5 гр х 1 раз в сутки.
280-330 rub.
Powder for suspension inside
флаконах
: beforeбавить 9,5 мл воды о флакон, взболтать,
take 2 times a day. 120-370 rub.

16 members

Representatives Tradename Method of use, price
Spiramycin Rovamycin Pills: по 2-3 таблетки (по 3 млн МЕ) или 4-6
tablets (6-9 million IU) in 2-3 doses per day.
1000-1700 rub.
Spiramycin-веро Pills: по 2-3 таблетки (по 3 млн МЕ) за 2-3
ingestion per day. 220-1700 rub.
Midecamycin Macropene Pills: 0,4 гр х 3 раза в сутки, курс 14
days 250-350 rub.
Josamycin ATильпрафен Pills: 0,5 гр х 2 раза в сутки, не
chewing, drinking plenty of water. 530-610
rub.
ATильпрафен солютаб Pills: 0,5 гр х 2 раза в сутки, не
chewing or dissolving in 20 ml of water. 670-750
rub.

The list of 14-membered macrolides differs by producing a pronounced
resistance of microorganisms to their action. That is why the first
A subgroup of macrolide antibiotics is not prescribed immediately, but only when
the ineffectiveness of other antibacterial agents.

This is a backup medication. Oleandomycin и эритромицин
low toxicity, almost never cause serious side
reactions. More often you can meet nausea, vomiting, general malaise,
allergies (urticaria, etc.). The first generation of macrolides should not
appoint pregnant and lactating patients.

Among the list of 14-membered drugs most active in
against Helicobacter pylori is clarithromycin, which
allowed to include it in one of the treatment regimens for chronic gastritis
in people infected with this microorganism. He is three times more active
erythromycin for coccal infections and lasts twice as long.
Oleandomycin, напротив, почти не применяется в настоящее время, так
as outdated and does not show high antimicrobial activity.

The latest generation macrolides are the most modern.
class representatives. AT частности, джозамицин за редким исключением
does not act on bacteria that have developed resistance. It is effective and
safe medicine that is permitted during the gestation period
baby and breastfeeding. Spiramycin также beforeпустим при
pregnancy, but is prohibited to lactating women, as it penetrates
breast milk. The drug midecamycin – macrolide reserve, not
recommended for expectant mothers and lactating women.

Use in childhood

The use of macrolides for children is a separate section:
not always drugs of this group are allowed for use without
restrictions. In addition, the recommended dosage of drugs
turn out to be lower than the adult population, and almost always
calculated on the body weight of the baby. 

Erythromycin solution for intravenous administration rarely can
cause acute toxic hepatitis in a child. Assigned substance
30-40 mg per kilogram of mass, this daily dose is divided by 2-4
reception. Course duration is unchanged (7-10 days).

Drugs, including macrolide clarithromycin, are limited to
appointment of newborns and infants up to 6 months. Children over 12
years they are discharged 250 mg twice a day.

Roxithromycin не рекоменbeforeван для малышей before 2 месяцев, другим
he is prescribed 5-8 mg per 1 kg of body weight. The dose is divided by 2
reception.

Azithromycin не применяют у детей:

  • up to 16 years (for infusion forms);
  • up to 12 years with a mass of less than 45 kg (for tablets and
    capsule form);
  • before half a year (for suspension).

При этом beforeзировка для детей старше 12 лет при массе тела более
45 кг совпадает с взрослой beforeзой. A child is 3-12 years old with a mass
less than 45 kg of the antibiotic is discharged at 10 mg per kilogram once a day.
day.

The dose of josamycin is 40-50 microns / kg. It is evenly divided by 2-3
приема в day. It is recommended to appoint 1-2 grams. Pills
спирамицина по 1,5 млн МЕ не дают детям before 3 лет, по 3 млн МЕ – before
18 years. Максимум beforeзы – 300 МЕ на килограмм в day.

Bacteria Resistance

Bacterial microorganisms are able to produce
resistance (immunity) to the action of antibiotics.
Macrolides are no exception. Bacteria in the spectrum
действия макролиbeforeв, «избегают» их влияния тремя путями:

  • Modification of cellular components.
  • Inactivation of the antibiotic.
  • Active “release” of an antibiotic from a cage.

AT последние годы ученые отмечают мировой рост невосприимчивости
bacterial organisms to macrolide row. AT США, а также
Центральной и Южной Европе резистентность beforeстигает 15-40%. By
data of the Consilium Medicum portal, in addition to macrolide stability
встречается неbeforeстаточная эффективность аминогликозиbeforeв и
метициллина (before 30% случаев). For Turkey, Italy and Japanese lands
bacteria immunity ranges from 30-50%.

AT России ситуация так же ухудшается с течением времени.
Результаты исслеbeforeвания под курацией Научно-исслеbeforeвательского
Clinical Institute of Otorhinolaryngology. L.I. Sverzhevsky
states: Stability of Staphylococcus pneumoniae (pneumococcus) in
15% of azithromycin in Moscow patients increased by 12.9%
(с 8,4% before 21,3%) в промежуток 2009-2016 гг. AT Ярославле отмечается
low resistance of S. pyogenes to erythromycin (7.5-8.4%). But for
Tomsk and Irkutsk, this figure was higher – 15.5% and 28.3%
respectively.

Группа макролиbeforeв – одна из самых безопасных в
present tense A wide range of drug activity allows
success in using them in treating infections of different severity, including
including as drugs “reserve”. But for профилактики развития
microbial resilience should not be self-drinking data
drugs without prior consultation with a specialist.

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