2010/06/24

Aziwok

Composition, structure and packing

Hard gelatin capsules, yellowish-white with markings "AZIWOK" and "WOCKHARDT" black; content caps - white or near white powder;

A capsule. azithromycin 250 mg.

Excipients: lactose, corn starch, magnesium stearate, sodium lauryl sulfate.

Clinico-pharmacological group: Antibiotic macrolide - azalid.

Pharmacological action

Macrolide antibiotic, a derivative azalida. It has a wide spectrum of antimicrobial action. When you create inflammation in high concentrations has a bactericidal effect.

The drug is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of CF and G, Streptococcus viridans, Staphylococcus aureus; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.; against other microorganisms: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

Azivok inactive against Gram-positive bacteria resistant to erythromycin.

Pharmacokinetics

Absorption

Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After receiving Azivoka oral dose of 500 mg of azithromycin Cmax plasma levels achieved after 2.5-2.96 h and is 0.4 mg / liter. Bioavailability is 37%.

Distribution

Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (particularly in the prostate gland), in skin and soft tissue. The high concentration in tissues (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 an environment with low pH, environmental lysosomes. This, in turn, determines a large Vd and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens.

Shown that phagocytes deliver azithromycin to the localization of infection sites, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissues (on average 24-34%) and correlated with severity of inflammatory edema. Despite the high concentration in phagocytes, azithromycin did not significantly affect their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after receiving the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.

Withdrawal

Derivation of azithromycin from plasma occurs in 2 stages: T1 / 2 is 14-20 h in the range from 8 hours to 24 hours after drug administration and 41 h - in the range from 24 h to 72 h, which allows you to use a drug once a day .

Statement

Infectious and inflammatory diseases caused by organisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (tonsillitis, sinusitis, tonsillitis, otitis media);
Infection of lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
scarlet fever;
infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis);
Uncomplicated urethritis and / or cervicitis;
Lyme disease (borreliosis) - for treatment of early stage (erythema migrans);
gastric and duodenal ulcers associated with Helicobacter pylori.

Dosage regimen

Drugs are taken 1 time per day is strictly for 1 hour before meals or 2 hours after meals.

With infections of the upper and lower respiratory tract infections, skin and soft tissue prescribe 500 mg / day for 3 days; course dose of 1.5 PM

In uncomplicated urethritis and / or cervicitis designate single 1 g (4 capsules. 250 mg).

When Lyme disease (borrelia) for the treatment of early stages (erythema migrans) appoint 1 g (4 capsules. 250 mg) in 1-day and 500 mg daily, from 2 to 5 Days (course dose - 3 g).

In gastric and duodenal ulcers associated with Helicobacter pylori, a drug prescribed for 1 g (4 capsules. 250 mg) daily for 3 days in a combination therapy. In the case of a missed dose missed dose should be taken as soon as possible, and follow-up - with a break in 24 hours

Side effect
From the digestive system: nausea, diarrhea, abdominal pain, rarely - vomiting, flatulence, transient increase in liver enzymes.
Dermatological reactions: in some cases - a rash.

Contraindications
severe renal dysfunction;
severe liver problems;
Pregnancy
Lactation (breastfeeding);
Children under 12 years
Hypersensitivity to azithromycin and other macrolide antibiotics.

Pregnancy and lactation

Azivok contraindicated in pregnancy. When you need to use during lactation breastfeeding should be interrupted for the duration of treatment.

Application for violations of liver function

Contraindicated in severe liver problems.

Application for violations of renal function

Contraindicated in severe renal dysfunction.

Cautions

Among the methods Azivoka and antacid drugs should be observed by a break of at least 2 hours

Overdose

Data on drug overdose Azivok not available.

Drug Interactions

Azivok intensifies the effect of ergot alkaloids, dihydroergotamine, tetracycline and chloramphenicol - Synergy effects; Lincosamides reduce the effectiveness of azithromycin. Antacids, ethanol, food slow down and reduce the absorption of azithromycin. Cycloserine, indirect anticoagulants, methylprednisolone, felodipin - slow excretion, increased concentration in the serum and increased toxicity of these drugs, while the use of azithromycin.

Inhibiting microsomal oxidation in hepatocytes, azithromycin increases T1 / 2, slow excretion, improves concentration and toxicity of medicines undergoing microsomal oxidation (including carbamazepine, ergot alkaloids, valproic acid, geksobarbital, phenytoin, dizopiramid, bromocriptine, theophylline and other xanthine derivatives, oral hypoglycemic agents).

Pharmaceutical incompatible with heparin.

Terms and Conditions of storage

The drug should be stored in a dark place at temperatures not above 30 ° C.

Shelf life - 2 years.