Azitrus powder for the preparation of suspensions pac. 50mg N3
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Description
AzitRus is an antibacterial drug with a bacteriostatic action from the group of macrolides (azalide), active against gram-positive microorganisms, with the exception of bacteria that are resistant to erythromycin.
Active ingredients
Azithromycin
Composition
Solution for infusion 20% - albumin, obtained from plasma for fractionation, 20%, Excipients: sodium caprylic acid (5.7-6.4) g / l, sodium chloride (90-160) mmol / l, water for injection to 1 l.
Pharmacological effect
Acts bacteriostatic. Binding to the 50S-subunit of the ribosome, inhibits protein synthesis, slows the growth and reproduction of bacteria. In high concentrations has a bactericidal effect. It acts on extracellular and intracellular pathogens. It is active against gram-positive microorganisms: Streptococcus spp. (C), EF, EF, EF, GF, GF, GF, GF, EF, GF, GF, GF, EF Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis, some anaerobic bacteria: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp, as well as intracellular pathogens:. Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.Azithromycin is not active against gram-positive bacteria, erythromycin-tolerant.
Pharmacokinetics
AbsorptionAfter taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. After ingestion in a dose of 500 mg Cmax in plasma is reached in 2.5-2.9 hours and is 0.4 mg / l. Bioavailability - 37.5%. Distribution: Asitromycin is rapidly distributed throughout the body, while high concentrations of the antibiotic are achieved in the tissues. It penetrates the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland), skin and soft tissues. High tissue concentrations (10–50 times higher than in plasma) and prolonged T1 / 2 are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding the lysosomes. This, in turn, determines a large apparent 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 site of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (by an average of 24–34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin remains in bactericidal concentrations in the inflammatory focus for 5-7 days after the last dose, which allowed developing short (3-day and 5-day) courses of treatment Metabolism Azithromycin is metabolized in the liver by demethylation with the formation of inactive metabolites. Excretion Azithromycin is released from plasma 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, which allows you to use the drug 1 time / day. It is mainly excreted in the bile unchanged, a small part is excreted by the kidneys.
Indications
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug: - infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media), scarlet fever, - infections of the lower respiratory tract (bacterial, including caused by atypical pathogens of pneumonia, exacerbation of chronic pneumonia, bronchitis), - infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses), - infections of the urinary tract (gonorrheal and non-urethral urethritis), - infections Yonsky genital organs (cervicitis) - Lyme disease (Lyme disease) in the early stages (erythema migrans), - diseases of stomach and duodenal ulcers associated with Helicobacter pylori (in a combination therapy).
Contraindications
Hypersensitivity (including to other macrolides), severe violations of the liver and / or kidneys, age up to 16 years (infusion), up to 12 years with a body weight less than 45 kg (capsules, pills), up to 6 months (suspension for ingestion).
Use during pregnancy and lactation
In pregnancy, it is possible if the expected effect of therapy outweighs the potential risk to the fetus. Category of action on the fetus according to FDA - B. At the time of treatment, breastfeeding should be stopped.
Dosage and administration
AzitRus should be taken orally once a day, 1 hour before meals or 2 hours after meals.Recommended dosages for adults depending on the indications: - Infections of the respiratory tract: 500 mg / day for a 3-day course, - Infections of the skin and soft tissues, creeping erythema: Day 1 - 1000 mg, 2-5 days - 500 mg , - Uncomplicated urethritis and / or cervicitis: 1000 mg once, - Peptic ulcer and 12 duodenal ulcer caused by Helicobacter pylori (as part of combination therapy): 1000 mg / day for 3 days. Recommended doses for children: - Infections of the respiratory tract, soft tissues and skin: on the 1st day 10 mg / kg, over the next 4 days - 5-10 mg / kg / day or 10 mg / kg 1 time per day within 3 days, - Erythema creeping: 1st day - 20 mg / kg, 2-5 days - 10 mg / kg / day. For children over 6 months old, AzitRus is prescribed in the form of a suspension prepared from powder. Recommended daily (single) doses of the suspension, depending on the body weight of the child when using the powder in a dose of 100 mg / 5 ml - azithromycin (suspension): - 5 kg - 50 mg (2.5 ml), - 6 kg - 60 mg (3 ml), - 7 kg - 70 mg (3.5 ml), - 8 kg - 80 mg (4 ml), - 9 kg - 90 mg (4.5 ml), - 10-14 kg - 100 mg (5 ml) The recommended daily (single) doses of the suspension, depending on the body weight of the child when using the powder in a dose of 200 mg / 5 ml - azithromycin (suspension): - 15-24 kg - 200 mg (5 ml), - 25-34 kg - 300 mg (7.5 ml), - 35-44 kg - 400 mg (10 ml), - From 45 kg - doses for adults (from 500 to 1000 mg). Terms of preparation of the suspension for oral administration: pour a small amount of boiled and cooled water into a clean glass, pour the contents of 1 package and mix until a homogeneous suspension is obtained. After taking the medication, rinse the cup with clean water, dry it and store in a clean, dry place.
Side effects
From the nervous system and sensory organs: dizziness, vertigo, headache, paresthesia, agitation, increased fatigue, drowsiness, rarely - tinnitus, reversible hearing impairment up to deafness (when taken in high doses for a long time), in children - headache (in the treatment of otitis media), hyperkinesia, nervousness, anxiety, sleep disturbance, conjunctivitis. From the cardiovascular system and blood (hematopoiesis, hemostasis): chest pain, palpitations. From the side of the gastrointestinal tract: nausea, vomiting diarrhea , flatulence, abdominal pain, increased activity of ALT and AST, bilirubin level, cholestasis, jaundice, rarely - constipation, change in the color of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, liver failure (possibly fatal), in children - decreased appetite gastritisCandidomycosis of the oral mucosa. From the urogenital system: vaginal candidiasis, nephritis. Allergic reactions: rash, pruritus, urticaria, rarely - angioedema, anaphylactic shock. Others: photosensitization, eosinophilia, transient neutrophilia, in a w / in injection, in a / in injection - bronchospasm, pain and inflammation at the injection site.
Overdose
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea. Treatment: gastric lavage, conducting symptomatic therapy.
Interaction with other drugs
With simultaneous use of antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin. When combined with azithromycin in therapeutic doses with warfarin, there is no change in prothrombin time, however, when interacting with macrolides with warfarin, it is possible to enhance the anticoagulant effect. prescribing this combination to patients requires careful monitoring of prothrombin time. With simultaneous use, the concentration of digoxin in plasma increases krovi.Pri simultaneous application enhanced toxic effect (vasospasm, dysesthesia) and ergotamine digidroergotamina.Pri simultaneous application decreases clearance and enhanced pharmacological effect triazolama.Azitromitsin inhibits microsomal oxidation in hepatocytes, resulting in slower clearance and increase in the plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclo porin, hexobarbital, ergot alkaloids, valproate, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline). Lincosamines reduce the effectiveness of azithromycin. Tetracycline and chloramphenicol increase the effectiveness of azithromycin.
special instructions
The drug is not taken during the meal. In case of a missed dose, the missed dose should be taken as early as possible, and the next - with an interval of 24 hours. It is necessary to observe a break of at least 2 hours between taking AzitRus and antacid preparations.After discontinuation of the drug, hypersensitivity reactions in some patients may persist, in such cases, the prescription of specific therapy is recommended under medical supervision.