Description
Latin name
ZITROLID
Release form
Capsules.
Packing
In a blister pack of 6 capsules. In a cardboard box 1 blister.
Pharmacological action
Pharmacodynamics
Antibiotic macrolide group, is a representative of the azalide subgroup. It has a wide range of antimicrobial effects. When creating high concentrations of inflammation in the focus, it has a bactericidal effect.
The drug is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci groups C, F and G, Streptococcus viridans, Staphylococcus aureus gram-negative bacteria, Haemophilus influenzaeffrellella pheradeltella pheradeltella refellaella pheradeltaella pheradeltaella pheradeltaella pheradeltaella pheradeltaella straina , Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis of anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.
Also active in relation to: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Zitrolide is not active against gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
Absorption
When administered orally, azithromycin is rapidly absorbed from the digestive tract, due to its stability in an acidic environment and lipophilicity. After ingestion of the drug in a dose of 500 mg Cmax, azithromycin in plasma is reached after 2.5-2.96 hours and is 0.4 mg / L. Bioavailability is 37%.
Distribution of
Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland), into the skin and soft tissues. A high concentration in tissues (10-50 times higher than in blood plasma) and a long T1 / 2 are due to the low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding lysosomes.
This, in turn, defines a large Vd (31, 1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate primarily in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to the sites of localization of the infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the severity of the inflammatory process. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function.
Azithromycin persists in bactericidal concentrations in the focus of inflammation for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
Metabolism
Azithromycin demethylates in the liver to form inactive metabolites.
Excretion of
Excretion of azithromycin from blood plasma occurs in 2 stages: T1 / 2 is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours after taking the drug, which allows you to use it times / day
Indications
Infectious and inflammatory diseases caused by susceptible microorganisms:
infections of the upper respiratory tract and ENT organs (including tonsillitis, pharyngitis, sinusitis, tonsillitis, otitis media)
infections of the lower respiratory tract ( including bacterial and atypical pneumonia, bronchitis)
scarlet fever
infections of the skin and soft tissues (including erysipelas, impetigo, secondarily infected dermatoses)
infections of the genitourinary system (including uncomplicated urethritis and / or cervicitis)
Lyme disease (borreliosis) – for treatment initial stage (erythema migrans)
diseases of the stomach and duodenum associated with Helicobacter pylori (as part of combination therapy).
Contraindications
Severe liver failure
severe renal failure
lactation (breastfeeding)
children under 3 years of age
hypersensitivity to azithromycin or other macrolides.
Precautions: use the drug during pregnancy, arrhythmias (possibly developing ventricular arrhythmias and lengthening the QT interval), in children with severe impaired liver or kidney function.
Use during pregnancy and lactation
During pregnancy, Zitrolide and Zitrolide Forte should be used with caution and in cases where the expected benefits of therapy to the mother significantly exceed the potential risk to the fetus.
The drug is contraindicated for use during lactation (breastfeeding). If necessary, the use of Zitrolide and Zitrolide Forte during lactation during treatment, it is recommended to stop breastfeeding.
Composition
1 capsule contains:
Active substances:
azithromycin 250 mg.
Excipients:
magnesium stearate,
microcrystalline cellulose.
Capsule shell composition:
gelatin,
titanium dioxide,
quinoline yellow,
azorubine,
ponso 4R.
Dosage and Administration
Zitrolide and Zitrolide Forte are taken orally 1 time / day 1 hour before meals or 2 hours after meals.
Adults with upper and lower respiratory tract infections are prescribed 500 mg / day for 3 days, the course dose is 1.5 g.
For infections of the skin and soft tissues, 1 g is prescribed on the 1st day and 500 mg daily from 2- go on the 5th day (course dose – 3 g).
In acute infections of the genitourinary system (uncomplicated urethritis or cervicitis), 1 g is prescribed once.
For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on the 1st day and 500 mg daily from the 2nd to 5th day (course dose – 3 g).
For gastric and duodenal ulcer associated with Helicobacter pylori, the drug is prescribed 1 g / day for 3 days as part of combination therapy.
Children Zitrolide and Zitrolide Forte are prescribed at a rate of 10 mg / kg body weight 1 time / day for 3 days or on the 1st day – 10 mg / kg, then for 4 days – 5-10 mg / kg / day within 3 days (course dose – 30 mg / kg).
In Lyme disease (borreliosis), children are prescribed 20 mg / kg on day 1 and 10 mg / kg from day 2 to day 5 to treat the initial stage of erythema migrans.
Side effects of the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%) 1% – dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases in children – constipation, anorexia, gastritis, taste change ( 1%).
From the cardiovascular system: palpitations, chest pain ( 1%).
From the side of the central nervous system: dizziness, headache,otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance ( 1%).
From the genitourinary system: vaginal candidiasis, nephritis ( 1%).
Allergic reactions: rash, photosensitivity, Quincke’s edema in children ( 1%) – conjunctivitis, pruritus, urticaria.
Drug Interactions
Antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin.
No changes in prothrombin time have been observed with warfarin and azithromycin (in normal doses), but given that macrolides and warfarin interact with the anticoagulant effect, patients need careful monitoring of prothrombin time.
Digoxin concentrations are increased when co-administered with digoxin.
When used with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) is increased.
When used with triazolam, clearance is reduced and the pharmacological action of triazolam is increased.
Azithromycin slows excretion and increases plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and drugs, subjected to microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthosine derivatives, including.
Linkosamines impair the efficacy of azithromycin.
Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: withdrawal of the drug, carrying out symptomatic therapy.
Storage conditions
Keep out of the reach of children, in a dry, dark place at a temperature not exceeding 25 ° C.
Expiration
3 years.
Deystvuyuschee substances
Azithromycin
Conditions of supply of pharmacies
Prescription
Dosage form sr dlkp Dosage form
capsules
Valenta Pharmaceuticals, Russia
