Producer: JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Republic of Kazakhstan
Code of automatic telephone exchange: J01FA10
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 131 mg, 262 mg or 524 mg of azithromycin of a dihydrate that 500 mg, 250 mg and 125 mg of azithromycin respectively are equivalent.
Excipients: starch prezhelatinizirovanny, LHPC 21, sodium lauryl sulfate, sodium of a kroskarmelloz, calcium hydrophosphate dihydrate, aerosil 200, lactose anhydrous, magnesium stearate,
Structure of a cover: a gidroksipropilmetiltsellyuloza, cellulose microcrystallic, titanium dioxide, a macrogoal - 40 OE stearate.
Pharmacodynamics. Azithromycin is derivative erythromycin and belongs to ozalid group, a subclass of makrolidny antibiotics. Azithromycin works by means of linkng with ribosomalny subunit 50S at sensitive microorganisms and, thereby, interferes with protein synthesis of microorganisms. Does not influence synthesis of nucleic acids.
In comparison with ZITMAK® erythromycin is more active concerning gram-negative microorganisms, is steadier in acid medium of a stomach, it is more slowly allocated from an organism and works more for a long time, it is better to be transferred, to a lesser extent inhibits liver R-450 cytochrome.
Зитмак® possesses a wide range of antimicrobic action. It is highly effective concerning many strains below the listed microorganisms as in vitro, and at clinically expressed infections:
Chlamydia pneumonia, Chlamydia trachomatis, Mycoplasma pneumonia, Borrelia burgdorferi, Mycoplasma pneumonia, Treponema pallidum, Ureaplasma urealyticum.
Aerobic gram-positive microorganisms: Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pneumonia, Streptococcus pyogenes, streptococci (C, F groups, G), Viridans group streptococci.
Aerobic gram-negative microorganisms: Haemophilus influenzae, Moraxella catarrhalis, Bordatella pertussis, Campylobacter jejuni, Legionella pneumophila.
Anaerobic microorganisms: Bacteroides bivius, Clostridium perfringes, types of Peptostreptococcus.
Cross azithromycin resistance about erythromycin - resistant gram-positive strains was noted. The majority of strains of Enterococcus faecalis and Methicillinum - resistant staphylococcus are steady against azithromycin.
Pharmacokinetics. Azithromycin is quickly soaked up from digestive tract and widely distributed on all organism. Higher concentration of azithromycin in fabrics, than in plasma or serum is caused by its property of bystry distribution. At reception of a single dose of 500 mg inside the maximum concentration makes 0.5 mkg/ml and is reached within 2.5 - 3 hours (= Tmax).
The seeming constant volume of distribution (Vd) makes about 31.1 l/kg. The elimination half-life makes - 14-72 hours. The prolonged final elimination half-life is caused by big accumulation and the subsequent removal of drug from fabrics. Removal of azithromycin with bile, is preferential in not changed look, is the main way of elimination. At use of a course over a week, about 6% of the accepted dose are removed by urine in not changed look. At use of the mode of treatment of 500 mg in the first day and 250 mg daily within 4 days in cerebrospinal fluid only very low concentration (less than 0.01 mkg/ml) were found.
Indications to use:
• an exacerbation of the chronic obstructive pulmonary disease caused by Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumonia;
• the acute bacterial sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumonia;
• the community-acquired pneumonia caused by Chlamydia pneumonia, Haemophilus influenzae, Mycoplasma pneumonia or Streptococcus pneumonia;
• patients suitable for peroral therapy;
• pharyngitis/tonsillitis, the caused Streptococcus pyogenes;
• the uncomplicated infections of skin and soft tissues caused by Staphylococcus aureus, Streptococcus pyogenes or Streptococcus agalactiae;
• the urethritis and a cervicitis caused by Chlamydia trachomatis, Neisseria gonorrhoeae;
• ulcers of external genitals, the caused Haemophilus ducreyi (venereal ulcer);
• Lyme's disease;
• the diseases of a stomach and a duodenum associated with Helicobacter pylori (as a part of complex therapy).
Route of administration and doses:
Drug is accepted to 1 h to or in 2 h after food.
Adults and teenagers are more senior than 16 years:
The recommended therapy dose/Duration
Community-acquired pneumonia (easy degree), pharyngitis/tonsillitis, skin / soft tissues uncomplicated)
Single dose of 500 mg (1 tablet Зитмак® 500) in the first day, then from the second to the fifth day of 250 mg (1 tablet ЗИТМАК® 250) once a day
Exacerbations of chronic obstructive pulmonary diseases (from easy to moderate degree)
500 mg (1 tablet Зитмак® 500) once a day within 3 days or a single dose of 500 mg (1 tablet Зитмак® 500) in the first day, then from the second to the fifth day of 250 mg (1 tablet ЗИТМАК® 250) once a day.
Acute bacterial sinusitis
500 mg (1 tablet Зитмак® 500) once a day within 3 days
Ulcers of generative organs (venereal ulcer)
Single dose of 1 grams (2 tablets Зитмак® 500)
Not gonococcal urethritis and cervicitis
Single dose of 1 grams (2 tablets Зитмак® 500)
Gonococcal urethritis and cervicitis
Single dose 2 grams (4 tablets Зитмак® 500)
The first day - 1 g (2 tablets Зитмак® 500) once, from the second to the fifth day on 500 mg (1 tablet Zitmak 500) (a course of treatment - 5 days, a course dose - 3 g or 6 tablets ZITMAK 500)
At the diseases of a stomach and duodenum associated with Helicobacter pylori appoint 1 g (on 2 tablets Зитмак® 500) in days within 3 days as a part of a combination therapy.
To children 6 years are more senior it is recommended to apply the tablets ЗИТМАК® 125 according to the following scheme: in the first day - 10 mg/kg, then 4 days - on 5 mg/kg a day or on 10 mg/kg a day within 3 days (a course dose - 30 mg/kg); at Lyme's disease in the first day - 20 mg/kg, from the 2nd to the 5th day - 10 mg/kg/days.
Features of use:
It is necessary to observe a break of 2 h at simultaneous use of antacids and the drug Zitmak®.
At the patients receiving treatment by azithromycin serious allergic reactions, including a Quincke's disease, an anaphylaxis and dermatological reactions, such as Stephens-Johnson's syndrome and a toxic epidermal necrolysis were in rare instances observed. These patients need more long period of observation and symptomatic therapy.
At treatment of pneumonia it was noted that only azithromycin is safe and effective at treatment of the community-acquired pneumonia caused by Chlamydia pneumonia, Haemophilus influenzae, Mycoplasma pneumonia or Streptococcus pneumonia in patients suitable for peroral therapy. At the pneumonia which is not subject to peroral therapy inefficient will appoint azithromycin for intake. Azithromycin should not be applied at patients with pneumonia at whom this disease was estimated improper for peroral therapy as the disease is characterized by moderate or heavy severity or is available some of the listed risk factors:
• patients with cystous fibrosis;
• patients with intrahospital infections;
• patients with suspicion or the revealed bacteremia;
• patients, needing hospitalization;
• the elderly or weakened patients, in a condition of the expressed immunodeficiency and a functional aspleniya.
Case of pseudomembranous colitis are reported at use of almost all antibacterial agents, and on weight can be from easy to life-threatening degree. Therefore, it is important to take into account this diagnosis at patients who have a diarrhea which followed after reception of antibacterial agent.
Because azithromycin is mainly removed through a liver, it is necessary to be careful at use of azithromycin for patients with insufficiency of functions of a liver. Owing to insufficient data at persons who have a glomerular filtration rate <10 ml/min. it is necessary to be careful at purpose of azithromycin. As usual at any kind of antibacterial therapy, it is reasonable to inspect the patient to define the consecutive infection having not bacterial origin, including fungi.
Use in pediatrics. Children up to 6 years are not recommended to apply a dosage form in the form of tablets, and it is recommended to apply mg ЗИТМАК® 100 suspension / 5 ml or ЗИТМАК® 200 mg / 5 ml according to the instruction.
Use for elderly patients. Patients of advanced age have no need for correction of a dose with normal renal and hepatic functions, receiving treatment.
Pregnancy and period of a lactation. Use of medicine is possible if the expected advantage for mother exceeds potential risk for a fruit.
It is unknown whether azithromycin with breast milk therefore at use of the drug Zitmak® for nursing mothers it is necessary to be careful is emitted.
Features of influence of medicine on ability to manage motor transport or moving mechanisms. Considering side effects of drug it is necessary to be careful at control of motor transport or moving mechanisms.
• nausea, vomiting, diarrhea, lock, meteorism, abdominal pains;
• cholestatic jaundice;
• stethalgia, heartbeat;
• weakness, headache, dizziness, drowsiness;
• pseudomembranous colitis;
• neutropenia or neutrophilia, eosinophilia;
• rash, a Quincke's disease at children;
• hyperkinesia, excitement, nervousness, sleeplessness, conjunctivitis.
Interaction with other medicines:
At simultaneous use of Zitmak® with:
• the antacids containing aluminum hydroxide and magnesium concentration of drug decreases;
• Cimetidinum, use of Cimetidinum (800 mg) in two hours prior to reception of azithromycin does not influence absorption of the last;
• theophylline, in therapeutic doses azithromycin moderately affects theophylline pharmacokinetics (intravenous and peroral);
• warfarin, azithromycin does not influence a prothrombin time at use of a single dose of warfarin. However, care of use in medical practice provides attentive observation of a prothrombin time at all patients receiving simultaneous treatment by azithromycin and warfarin;
• digoxin, azithromycin leads to increase in concentration of digoxin;
• the acute intoxication ergotaminovy drugs which is characterized by a peripheral vasospasm and a dizesteziya (sensitivity disturbance) can occur ergotamine or dihydroergotamine;
• ergot alkaloids, the effect of alkaloids of an ergot amplifies;
• tetracyclines and chloramphenicol, strengthen action (synergism);
• linkozamidam, lower effect of drug;
• antacids, ethanol, food slow down and lower absorption;
• Cycloserinum, indirect anticoagulants, Methylprednisolonum and felodipiny, azithromycin slows down excretion, increases concentration in blood serum and increases toxicity;
• carbamazepine, ergot alkaloids, valproyevy acid, hexobarbital, Phenytoinum, Disopyramidum, Bromocriptinum, theophylline and other ksantinovy derivatives, peroral hypoglycemic means, azithromycin inhibiting a microsomal oxidation in hepatocytes, extends an elimination half-life, slows down excretion, increases concentration and toxicity;
• heparin, pharmaceutical it is incompatible.
• hypersensitivity to azithromycin, erythromycin or any antibiotic from group of macroleads;
• heavy abnormal liver functions and kidneys;
• children's age up to 6 years.
Data concerning overdose are insufficient.
Treatment: to wash out a stomach and to appoint a symptomatic treatment.
To store at a temperature not above 25 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 4 years. Not to apply after a period of storage.
According to the recipe
Tablets, film coated, 500 mg, 250 mg, 125 mg
On 3 tablets (for a dosage of 500 mg), or on 6 tablets (for a dosage of 250 mg and 125 mg) in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.
1 packaging together with the instruction on a medical use in the state and Russian languages is placed in a pack cardboard with the hologram of manufacturing firm.