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Zithromax Azithromycin 100, 250, 500 mg
Most popular brand: Zithromax
Active ingredient: Azithromycin
Available dosage forms: 100, 250, 500 mg
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Azithromycin (Azithromycin): instruction, and the use of a formula

Code CAS

Feature substance Azithromycin

The white crystalline powder.

Pharmacology

Mode of action – antibacterial broad-spectrum.

Associated with the 50S subunit of the ribosome inhibits translation peptidtranslokazu on stage and inhibits protein biosynthesis by slowing the growth and reproduction of bacteria at high concentrations of bactericidal effect is possible.

The range of action is wide and includes gram (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus groups C, F, G, Streptococcus viridans) . besides resistant to erythromycin, and gram-negative (Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Campylobacter jejuni, Legionella pneumophila, Neisseria gonorrhoeae, Gardnerella vaginalis) bacteria, anaerobes (Bacteroides bivius, Peptostreptococcus spp. Peptococcus, Clostridium perfringens) . Chlamydia (Chlamydia trachomatis, Chlamydia pneumoniae) . Mycobacterium (Mycobacteria avium complex) . Mycoplasma (Mycoplasma pneumoniae) . ureaplasmas (Ureaplasma urealyticum) . spirochetes (Treponema pallidum, Borrelia burgdorferi) .

It is resistant to acid medium, lipophilic, when taken orally is rapidly absorbed from the gastrointestinal tract. After a single oral administration of 500 mg the bioavailability ; 37% (the effect of “first pass»), C max (0,4 mg / l) is created after 2 – 3 h, the apparent distribution volume ; 31.1 l / kg, protein binding is inversely proportional to the concentration in the blood and is 7 – 50%, T 1/2 ; . 68 h stable plasma levels achieved after 5 – 7 days. Gistogematicalkie barriers easily passes and enters the tissue. Dispatching also phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, which is released in the presence of bacteria. It penetrates through the cell membrane (effective for infections caused by intracellular pathogens). Concentration in the tissues and cells at 10 – 50 times higher than in plasma, and in the site of infection ; 24 – 34% more than in healthy tissues. The high level (an antibacterial) is retained in the tissue for 5 – 7 days after the last injection. Food intake was significantly alters the pharmacokinetics (depending on formulation) capsules ; reduced C max (52%) and AUC (43%); Suspension ; increases the C max (46%) and AUC (14%); Tablets ; increases C max (31%), does not change the AUC. The liver demethylated losing activity. The plasma clearance ; 630 ml / min. 50% is excreted in the bile in unchanged form, 6% ; urine. In older men (65 – 85 years) pharmacokinetic parameters are not changed, women ; increases C max (30 – 50%) in children aged 1 – 5 years ; reduced C max . T 1/2 . AUC.

Application of the substance Azithromycin

For intake: infections of the upper (streptococcal pharyngitis / tonsillitis) and lower (bacterial bronchitis, interstitial and alveolar pneumonia, exacerbation of chronic bronchitis) respiratory tract, ENT – organs (otitis media, laryngitis and sinusitis), urinary system (urethritis and cervicitis), skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis), chronic stage of erythema migrans (Lyme disease), diseases of the stomach and duodenal ulcers associated with Helicobacter pylori .

For the infusion: severe infections caused by susceptible strains microorganisms: community-acquired pneumonia, infectious – inflammatory diseases of the pelvic organs.

Contraindications

Hypersensitivity (including to other macrolides), severe liver and / or kidney disease, the age of 16 years (infusion), up to 12 years with a body weight less than 45 kg (capsules, tablets), up to 6 months (oral suspension).

Restrictions on the use

Violation of the liver and / or kidney disease, arrhythmia or predisposition to arrhythmias and prolongation of the QT interval.

Application of pregnancy and breastfeeding

When pregnancy is possible if the expected effect of therapy outweighs the potential risk to the fetus.

Category effects on the fetus by FDA ; B.

breast-feeding should be discontinued at the time of treatment.

Side effects of substance Azithromycin

From the nervous system and sensory organs: dizziness, vertigo, headache, paresthesia, agitation, fatigue, drowsiness; rare ; tinnitus, reversible hearing impairment including deafness (when taken in high doses for a long time); children ; headache (in the treatment of otitis media), hyperkinesia, nervousness, anxiety, insomnia, conjunctivitis.

From the cardio – vascular system and blood (blood, hemostasis): chest pain, palpitations.

From the digestive tract: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of ALT and AST. bilirubin, cholestasis, jaundice; rare ; constipation, a change in the language of color, pseudomembranous colitis, pancreatitis, hepatic necrosis, hepatic failure (possibly fatal); children ; loss of appetite, gastritis, candidiasis of the oral mucosa.

With the genitourinary system: vaginal candidiasis, jade.

Allergic reactions: rash, pruritus, urticaria; rare ; angioedema, anaphylactic shock.

Other: photosensitivity, eosinophilia, transient neutrophils; with a / in the introduction (optional) ; bronchoconstriction, inflammation and pain at the injection site.

Interaction

Antacids, ethanol, food slow down and reduce absorption (azithromycin should be taken 1 hour before or 2 hours after taking antacids, and food). Tetracycline and chloramphenicol enhance the effectiveness of azithromycin, lincosamides ; weaken. When used in therapeutic doses, azithromycin has little effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir sulfate, midazolam, rifabutin, Viagra, theophylline (w / w and inside), triazolam, co – trimoxazole, zidovudine. Efavirenz and fluconazole have little effect on the pharmacokinetics of azithromycin. Nelfinavir significantly increases the C max and AUC of azithromycin (by sharing a strict control over such side effects of azithromycin as a violation of liver function and hearing loss). It should be monitored closely while taking azithromycin with digoxin (may increase the concentration of digoxin in the blood), with ergot alkaloids (perhaps a manifestation of their toxic effect ; vasospasm, dysesthesia), with cyclosporine and phenytoin (necessary to monitor their concentrations in the blood). If necessary, co-administration with warfarin is recommended careful monitoring of PV (PV may increase and frequency of hemorrhage). Pharmaceutically compatible with heparin.

Overdose

Symptoms: nausea, vomiting, diarrhea, temporary hearing loss.

Treatment: gastric lavage (if swallowed), symptomatic therapy.

Dosing and Administration

Inside, intravenously. The mode set individually, taking into account indications, severity of disease susceptibility. Inside (1 hour before or 2 hours after meal), 1 times a day for adults ; 0,25 – 1 g, for children ; 5 – 10 mg / kg. B / in the form of an infusion, a drip (not less than 1 hour). You can not enter in / jet or / m!

Precautions substance Azithromycin

After discontinuation of treatment hypersensitivity reactions in some patients may persist, which requires specific therapy under the supervision of a physician.

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