2010/09/17

Azicid

Composition, structure and packing Azicid

Coated tablets: white to almost white, round, biconvex.

1 tab. azithromycin (in the form of dihydrate) 250 mg.

Excipients: corn starch pregelatinized, sodium croscarmellose, calcium hydrophosphate, magnesium stearate, sodium lauryl sulfate. The composition of the shell membrane: gipromelloza 2910 / 5, titanium dioxide, macrogol 6000, talc, Simethicone Emulsion SE 4 (water, siloxanes and silicones, cellulose methylated, sorbic acid), polysorbate 80. Coated tablets: white to almost white, oblong.

1 tab. azithromycin (in the form of dihydrate) 500 mg.

Excipients: corn starch pregelatinized, sodium croscarmellose, calcium hydrophosphate, magnesium stearate, sodium lauryl sulfate. The composition of the shell membrane: gipromelloza 2910 / 5, titanium dioxide, macrogol 6000, talc, Simethicone Emulsion SE 4 (water, siloxanes and silicones, cellulose methylated, sorbic acid), polysorbate 80.

Clinico-pharmacological group: Antibiotic macrolide - azalid.

Pharmacological action Azicid

Broad-spectrum antibiotic, a representative subgroup of macrolide antibiotics - azalidov. When you create inflammation in high concentrations has a bactericidal effect.

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

Azithromycin is not active against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics Azicid

Absorption

After taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After oral administration 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 Azicid

Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (in particular, 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, defines a large apparent 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. Shown that phagocytes deliver azithromycin in place of 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 correlated with the degree 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. In the liver demethylates formed metabolites are inactive.

Withdrawal Azicid

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

Statement

Infectious-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;
Infection of lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis);
infections of urogenital tract (uncomplicated urethritis and / or cervicitis);
Lyme disease (Lyme disease) in the early stages (erythema migrans);
gastric and duodenal ulcers associated with Helicobacter pylori.

Dosage regimen

Azitsid ingest 1 times / day for 1 hour before or 2 hours after meals.

Adults with the infection of the upper and lower respiratory tract appoint 500 mg / day for 1 reception for 3 days (course dose -1.5 g). With infections of the skin and soft tissue administered in a dose of 1 g / day for 1 admission on the first day, then - on 500 mg daily from 2 to 5 days (course dose - 3 g). In uncomplicated urethritis or cervicitis designate a single g. When Lyme disease (Lyme disease) for the treatment of early stages (erythema migrans) appoint 1 g the first day and 500 mg daily from 2 to 5 days (course dose - 3 g). In gastric ulcer and duodenal ulcer associated with Helicobacter pylori appoint 1 g / day for 3 days in a combination therapy of H. pylori.

Children older than 3 years of drug prescribed at 10 mg / kg 1 time / day for 3 days or the first day - 10 mg / kg followed by 4 days - from 5-10 mg / kg / day for 3 days (course dose - 30 mg / kg). In the treatment of erythema migrans in children older than 3 years the dose is 20 mg / kg on the first day and 10 mg / kg from 2 to 5 day.

Side effect

On the part of the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%), 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increase in liver transaminases; children - constipation , anorexia, gastritis. Chance kandidomikoz oral mucosa.

Since the cardiovascular system: heart, chest pain (1% or less).

From the side of the central nervous system: dizziness, headache, drowsiness; in children - a headache (for the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorder (1% or less).

On the part of the reproductive system: 1% or less - vaginal candidiasis.

From the urinary system: 1% or less - jade.

Dermatological reactions: in some cases, rash, photosensitivity.

Allergic reactions: rash, itching, Quincke's edema.

Other: fatigue; children - conjunctivitis, pruritus, urticaria.

Contraindications
severe liver problems;
severe renal dysfunction;
lactation (breastfeeding);
Children under 3 years;
Children weighing up to 25 kg;
Hypersensitivity to the drug's components;
increased sensitivity to other macrolide antibiotics.

Precautions should use the drug during pregnancy, patients with arrhythmia (ventricular arrhythmias and possible lengthening of the interval QT), in children with severe disorders of the liver or kidneys.

Pregnancy and lactation

Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, use during lactation should stop breastfeeding.

Application for violations of liver function

The drug is contraindicated in violation of liver function.

Application for violations of renal function

The drug is contraindicated in violation of renal function.

Cautions

In the case of missing the next admission should take the missed dose as soon as possible, and follow - with an interval of 24 h.

Necessary to observe a break of at least 2 h at the same time.The Azitsida and antacid drugs.

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

Overdose

Symptoms: increased side effects - severe nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: gastric lavage, the appointment of activated carbon, conducting symptomatic therapy.

Drug Interactions

Antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin.

At a joint appointment of warfarin and azithromycin (at normal doses) changes in prothrombin time was not revealed. However, given that the interaction of macrolides and warfarin may be increased anticoagulant activity, patients need careful monitoring prothrombin time.

In a joint application with digoxin increases the concentration of digoxin.

When combined with the use of ergotamine and dihydroergotamine increasing their toxicity (vasospasm, dysesthesia).

In a joint application with triazolamom decreases clearance and increases the pharmacological effect triazolama.

Azithromycin slows excretion and increases plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina, as well as preparations exposed to microsomal oxidation (carbamazepine, terfenadin, cyclosporine, geksobarbital, ergot alkaloids, valproic acid, dizopiramid, bromocriptine, phenytoin, oral hypoglycemic tools , xanthine derivatives, including theophylline) by inhibition of microsomal oxidation of azithromycin in hepatocytes. Linkozaminy reduce the effectiveness of azithromycin.

Tetracycline and chloramphenicol enhance the effectiveness of azithromycin. .

Storage conditions and expiry dates

The drug should be stored out of reach of children below 25 ° C. Shelf life - 2 years.