Azithromycin

General characteristics. Structure:

Active ingredient: 250 mg of azithromycin in 1 capsule.

Excipients: microcrystallic cellulose, potato starch, calcium stearate, lactoses monohydrate.

Structure of the capsule: gelatin, glycerin, methylparahydroxybenzoate, пропилпарагидроксибензоат, sodium lauryl sulfate, titanium E 171 dioxide, the water purified.

Pharmacological properties:

Pharmacodynamics. The antibacterial agent of a broad spectrum of activity, an azalead derivative of macroleads, works bacteriostatically. Communicating with 50S in subunit of ribosomes, oppresses to a peptidtranslokaz at a broadcasting stage, suppresses protein synthesis, slows down growth and reproduction of bacteria, in high concentration renders bactericidal effect. Works on out of - and intracellular activators.

It is active concerning gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except steady against erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; and also Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.

It is inactive concerning the gram-positive bacteria steady against erythromycin.

Pharmacokinetics. Absorption - high, кислотоустойчив, липофилен. Bioavailability after a single dose of 0,5 g – 37% (effect of "the first passing" through a liver), the maximum concentration of drug in a blood plasma (Cmax) after oral administration of 0,5 g – 0,4 mg/l, the period of achievement of Cmax – 2,5 - 2, in fabrics and cells concentration is 10 - 50 times higher, than in blood serum, distribution volume – 31,1 l/kg. Easily passes gistogematichesky barriers. Well gets into respiratory tracts, urinogenital bodies and fabrics, into a prostate, into skin and soft tissues; collects in the environment with low pH, in lysosomes (that is especially important for an eradikation of intracellularly located activators). It is transported also by phagocytes, polymorphonuclear leukocytes and macrophages. Gets through membranes of cells.

Concentration in the centers of an infection it is reliable above (for 24 - 34%), than in healthy fabrics, and correlates with expressiveness of inflammatory hypostasis. In the center of an inflammation remains in bactericidal concentration within 5 - 7 days after reception of the last dose. Communication with proteins of plasma - 7 - 50% (it is inversely proportional concentration in blood).

In a liver it demetilirutsya, the formed metabolites are not active. Plasma clearance – 630 ml/min.: Elimination from serum takes place in two stages: The elimination half-life of drug (T1/2) between 8 and 24 h after reception – 14 - 20 h, T1/2 in the range from 24 to 72 h - is removed with bile in not changed look, 6% 41 h 50% - kidneys.

Meal significantly changes pharmacokinetics (depending on a dosage form): capsules - Cmax decreases (by 52%) and AUC (for 43%); suspension - Cmax increases (by 46%) and AUC (for 14%); tablets - Cmax increases (by 31%), AUC does not change.

At elderly men (65-85 years) pharmacokinetic parameters do not change, at women Cmax increases (by 30–50%).

Indications to use:

The infections of upper parts of respiratory tracts and ENT organs caused by sensitive activators: pharyngitis, tonsillitis, laryngitis, sinusitis, average otitis; scarlet fever; infections of lower parts of respiratory tracts: pneumonia (including atypical), bronchitis; infections of skin and soft tissues: the erysipelatous inflammation, impetigo for the second time infected a dermatosis; infections of urinary tract: gonorrheal and not gonorrheal urethritis, cervicitis; Lyme's disease (an initial stage - erythema migrans), the peptic ulcer of a stomach and a 12-perstny gut associated with Helicobacter pylori (as a part of a combination therapy).

Route of administration and doses:

Inside, for 1 h to or in 2 h after food of 1 times a day. The adult at infections of upper and lower parts of respiratory tracts – 0,5 g/days for 1 reception within 3 days (a course dose – 1,5 g).

At infections of skin and soft tissues - 1 g/days in the first day for 1 reception, further on 0,5 g/days daily from 2 to 5 day (a course dose - 3 g).

At acute infections of urinogenital bodies (an uncomplicated urethritis or a cervicitis) - once 1 g.

At a disease Laima (borreliosis) for treatment of the I stage (erythema migrans) – 1 g in the first day and 0,5 g daily from 2 to 5 day (a course dose – 3 g).

At a peptic ulcer of a stomach and the duodenum associated with Helicobacter pylori - 1 g/days within 3 days as a part of the combined antikhelikobakterny therapy.

Features of use:

In case of the admission of reception of a dose it is necessary to accept the passed dose as soon as possible, and the subsequent - at an interval of 24 h. It is necessary to observe a break of 2 h at simultaneous use of antacids. After cancellation of treatment of reaction of hypersensitivity at some patients can remain that demands specific therapy under observation of the doctor.

At treatment of the first stage of a disease of Lyme, azithromycin as well as other drugs from group of macroleads considerably concedes to penicillin, cephalosporins and tetracyclines therefore azithromycin is appointed at contraindications of drugs from groups of penicillin, cephalosporins and tetracyclines.

Pregnancy and lactation. At pregnancy azithromycin can be applied only when the advantage of its use for mother considerably exceeds possible risk for a fruit, breastfeeding for the period of reception of azithromycin needs to be stopped.

With care apply at arrhythmia (ventricular arrhythmias and lengthening of an interval of Q-T are possible).

Side effects:

From the alimentary system: at intake - diarrhea (5%), nausea (3%), an abdominal pain (3%); 1% and less - a meteorism, vomiting, a melena, cholestatic jaundice, increase in activity of "hepatic" transaminases; besides, children have locks, a loss of appetite, gastritis.

From cardiovascular system: heartbeat, thorax pain (1% and less).

From a nervous system: dizziness, headache, вертиго, drowsiness; children have a headache (at therapy of average otitis), a hyperkinesia, uneasiness, neurosis, sleep disorders (1% and less).

From urinogenital system: vaginal candidiasis, nephrite (1% and less).

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

Others: increased fatigue; children have a conjunctivitis, an itch, urticaria.

Interaction with other medicines:

Antacids (aluminum - and magniysoderzhashchy), ethanol and food slow down and reduce azithromycin absorption. At joint purpose of warfarin and azithromycin (in usual doses) changes of a prothrombin time it is not revealed, however, considering that at interaction of macroleads and warfarin strengthening of anti-coagulative effect is possible, careful control of a prothrombin time is necessary for patients.

Increases concentration of digoxin due to weakening of its inactivation an indestinal flora.

Ergotamine and dihydroergotamine: strengthening of toxic action (vasospasm, dizesteziya).

To triazoles: decrease in clearance and increase in pharmacological action of a triazolam.

Slows down removal and increases concentration in plasma and toxicity of Cycloserinum, indirect anticoagulants, Methylprednisolonum, felodipin, and also the HP which are exposed to a microsomal oxidation (carbamazepine, терфенадин, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, Disopyramidum, Bromocriptinum, Phenytoinum, peroral hypoglycemic means, theophylline, etc. ksantinovy derivatives), at the expense of inhibition of a microsomal oxidation in hepatocytes azithromycin.

Linkozamida weaken, and tetracycline and chloramphenicol increase efficiency of azithromycin.

Contraindications:

Hypersensitivity (including to macroleads), the heavy liver and/or renal failure, pregnancy, the lactation period, children's age up to 12 years, to children up to 16 years appoint with care, according to indications.

Overdose:

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

Treatment: symptomatic therapy.

Storage conditions:

In the place protected from moisture and light, at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 2 years. Not to use medicine after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 6 capsules in a blister strip packaging No. 6х1. In banks No. 6 in packaging No. 1.