Zitrolid FORTE
Active material: Azithromycin
When ATH: J01FA10
CCF: Macrolide antibiotics – azalid
ICD-10 codes (testimony): A31.0, A38, A46, A48.1, A56.0, A56.1, A56.4, A69.2, B96.0, H66, J01, J03, J15, J15.7, J16.0, J20, J32, J35.0, J42, K25, K26, L01, L30.3, N34, N72
When CSF: 06.07.01
Manufacturer: OAO Valenta PHARMACEUTICS (Russia)
Pharmaceutical form, composition and packaging
Capsules hard gelatin, size №00, with white body and orange cap; contents of capsules – Powder from white to white with a yellowish tint.
| 1 caps. | |
| azithromycin | 500 mg |
Excipients: microcrystalline cellulose, magnesium stearate.
The composition of the shell: gelatin, Titanium dioxide, yellow “sunset”.
3 PC. – packings Valium planimetric (1) – packs cardboard.
Pharmacological action
Macrolide antibiotics, a representative subgroup azalides. It has a wide spectrum of antimicrobial action. When you create inflammation in high concentrations has a bactericidal effect.
Preparation active against Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus Group C, F and G, Streptococcus viridans, Staphylococcus aureus; Gram negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; anaerobes: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.
It is also active against: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pale, Borrelia burgdorferi.
Zitrolid® forte activity against Gram-positive bacteria, erythromycin resistant.
Pharmacokinetics
Absorption
When administered azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic medium and lipophilicity. After taking the drug orally at a dose 500 mg Cmax azithromycin plasma levels achieved after 2.5-2.96 h and is 0.4 mg / l. Bioavailability is 37%.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (in particular, in prostate), in skin and soft tissue. High concentrations in tissues (in 10-50 times higher, than in blood plasma) and a long T1/2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in medium with low pH, environmental lysosomes. It, in turn, It defines a large Vd (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens. Proved, that phagocytes deliver azithromycin to the localization of infection, where it is released in the process of phagocytosis.
The concentration of azithromycin in the foci of infection was significantly higher, than in healthy tissues (on average 24-34%) and correlate with the severity of inflammation. Despite the high concentration in phagocytes, Azithromycin has no significant effect on their function.
Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatments.
Metabolism
Azithromycin demethylated in the liver into inactive metabolites.
Deduction
Derivation of azithromycin from plasma occurs in 2 Phase: T1/2 is 14-20 hours, ranging from 8 to 24 hours after dosing and 41 hours, ranging from 24 to 72 h after dosing, allowing you to take it 1 time / day.
Testimony
Infectious-inflammatory diseases, caused by susceptible to malaria infections:
- Infections of the upper respiratory tract and ENT (sore throat, pharyngitis, sinusitis, tonsillitis, otitis media);
- Infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
- Scarlet fever;
- Infections of the skin and soft tissues (mug, impetigo, secondarily infected dermatitis);
- Infections of the genitourinary system (uncomplicated urethritis and / or cervicitis);
- Lyme disease (ʙorrelioz) – for the treatment of early stage (Erythema migrans);
- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in a combination therapy).
Dosage regimen
The drug is taken orally 1 time / day for 1 hours before meals or 2 h postprandial.
Adults at infections of the upper and lower respiratory tract appointed 500 mg / day for 3 days; course dose is 1.5 g.
At infections of skin and soft tissue appointed 1 g in 1 day and 500 mg daily from the 2nd to the 5th day (kursovaya dose – 3 g).
At acute infections of the genitourinary system (uncomplicated urethritis or cervicitis) administered once 1 g.
At Lyme disease (ʙorrelioze) for the treatment of stage I (Erythema migrans) appointed 1 g in 1 day and 500 mg daily from the 2nd to the 5th day (kursovaya dose – 3 g).
At peptic ulcer stomach and duodenum, associated with Helicobacter pylori, the drug is prescribed for 1 g / day for 3 days in a combination therapy.
Children over 1 year the drug is prescribed on the basis of 10 mg / kg body weight 1 times / day for 3 days or 1 day – 10 mg / kg, then for 3-4 days – by 5-10 mg / kg / day (kursovaya dose – 30 mg / kg).
At Lyme disease (ʙorrelioze) for the treatment of stage I (Erythema migrans) children prescribed a dose 20 mg / kg on day 1 and 10 mg / kg from the 2nd to the 5th day.
Side effect
From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% less – dyspepsia, flatulence, vomiting, ground, cholestatic jaundice, increase in liver transaminases; children – constipation, anorexia, gastritis.
Cardio-vascular system: heartbeat, chest pain (1% less).
CNS: dizziness, headache, drowsiness; children – headache (for the treatment of otitis media), giperkineziya, anxiety, neurosis, sleep disturbance (1% less).
With the genitourinary system: vaginal candidiasis, jade (1% less).
Allergic reactions: rash, photosensitivity, angioedema; children – conjunctivitis, itch, hives.
Other: fatigue.
Contraindications
- Severe hepatic impairment;
- Severe renal insufficiency;
- Breastfeeding;
- Children up to age 1 year;
- Hypersensitivity to the drug;
- Hypersensitivity to other macrolides.
FROM caution drug use during pregnancy, Arrhythmia (may develop ventricular arrhythmias, QT prolongation), in children with severe hepatic or renal function.
Pregnancy and lactation
Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.
The drug is contraindicated during breast-feeding. If necessary, use Zitrolid® Fort lactation should decide the issue of termination of breastfeeding.
Cautions
Observe break 2 h, while the use of azithromycin with antacids.
After discontinuation of therapy in some patients hypersensitivity reactions may persist, which require a specific therapy under the supervision of a physician.
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Drug Interactions
Antacids (aluminum- and magnesium-), ethanol and food slows down and reduces the absorption of azithromycin.
When concomitant administration of warfarin and azithromycin (at conventional doses) changes in prothrombin time is not revealed, However, given the, that the interaction of macrolides and warfarin may increase the anticoagulant effect, Patients should be closely monitored prothrombin time.
With simultaneous use of azithromycin with digoxin increases the concentration of the latter.
With simultaneous use of azithromycin with ergotamine and dihydroergotamine amplified the toxic effect of the latter (vasospasm, dysesthesia).
With simultaneous use of azithromycin reduced triazolam clearance and enhanced pharmacological effects last.
Azithromycin slows down and increases the plasma concentration and toxicity of cycloserine, anticoagulants, methylprednisolone, Felodipine, as well as preparations, undergoing microsomal oxidation (Carbamazepine, terfenadine, cyclosporine, geksoʙarʙital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemics, xanthine derivatives, incl. theophylline) due to inhibition of azithromycin microsomal oxidation in hepatocytes.
Linkozaminy weaken the effectiveness of azithromycin.
Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.
Azithromycin pharmaceutically incompatible with heparin.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.
