Aziadzhio

General characteristics. Structure:

Active ingredient: 250 mg or 500 mg of azithromycin in the form of dihydrate azithromycin.

Excipients: cellulose microcrystallic, sodium lauryl sulfate, sodium krakhmalglikolit (type A), povidone, sodium of a kroskarmelloz, talc, magnesium stearate.

Cover: gipromelloza, talc, Ponso's dye 4R (Е 124), titanium dioxide (Е 171), macrogoal.

Pharmacological properties:

Pharmacodynamics. Azithromycin is the representative of group of makrolidny antibiotics – azaleads, possesses a wide range of antimicrobic action. The mechanism of action is caused by inhibition of biosynthesis of protein owing to linkng of azithromycin with SOS substance of a ribosome and oppression of a peptidiltranslokaza.

Azithromycin is active in the relation:

• gram-positive aerobic bacteria: Streptococcus pneumoniae, S. pyogenes, S. agalactiae, S. viridans, streptococci of the groups C, F and G, Staphylococcus aureus,
• gram-negative aerobic bacteria: Haemophilus ducreyi, H. influenzae, H. parainfluenzae, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Legionella pneumophila, Campylobacter jejuni, Helicobacter pylori, Neisseria gonorrhoeae, N. meningitides, Gardnerella vaginalis, Brucella melitensis,
• anaerobic bacteria: Bacteroides bivius, Clostridium spp., Peptostreptococcus spp., Peptococcus spp.

Drug is also active concerning intracellular and other microorganisms, including: Chlamydia trachomatis, C. pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum, Listeria monocitogenes, Treponema pallidum, Borrelia burgdorferi.

Does not influence the gram-positive microorganisms steady against erythromycin.

Pharmacokinetics. Azithromycin is quickly soaked up from a GIT that is caused by stability in acid medium and lipophilicity. Bioavailability makes 37%. The maximum concentration in blood serum is reached in 2,5-3 hours and makes 0,4 mg/l at intake of 0,5 g of azithromycin. Drug well gets into respiratory tracts, bodies and fabrics of an urogenital path, in particular, in a prostate gland, skin and soft tissues.

Concentration of drug in fabrics is 80-1000 times higher, than in blood serum. High concentration in fabrics and a long elimination half-life are caused by low linkng of azithromycin with serum proteins, and also ability to get into eukariotny cells and to concentrate in the environment with a low rn, a surrounding lysosome. It determines, in turn, the large volume of the seeming distribution (31,1 l/kg) and high plasma clearance. It is proved that phagocytes deliver drug to places of an infection where release it. Good penetration of azithromycin into cells and accumulation in phagocytes with which it is transported in the inflammation centers promotes antimicrobic activity of drug. Despite high concentration in phagocytes, azithromycin does not influence significantly their function.

In bactericidal concentration in the centers an inflammation drug remains within 5-7 days after reception of the last dose that allowed to develop short (3 - and 5-day) courses of treatment. The elimination half-life makes 2-4 days. On average 50% of drug are removed with bile in steady-state condition. Other 50% – in the form of metabolites which do not possess antibacterial activity. About 6% of drug are removed by kidneys. Meal can reduce azithromycin absorption.

Indications to use:

The infections caused by microorganisms, sensitive to azithromycin:

• respiratory infection and ENT organs (acute pharyngitis and tonsillitis, scarlet fever, acute average otitis, acute sinusitis, acute bronchitis, exacerbation of chronic bronchitis, intersticial and alveolar pneumonia),
• infections of skin and soft tissues (an ugly face, impetigo, the chronic migrating erythema (an initial stage of a disease of Lyme), secondary pyodermatoses, uncomplicated forms of the Acne вульгарис),
• infections of urinary tract and generative organs (acute nonspecific or gonococcal urethritis, cervicitis, colpitis),
• the infections of a stomach and duodenum caused by Helicobacter pylori (as a part of schemes of an eradikation).

Route of administration and doses:

Azithromycin is accepted in 1 hour prior to food or in 2 hours after food once a day.

Adults. The adult at infections of ENT organs, respiratory tracts, skin and soft tissues (except the chronic migrating erythema) appoint 500 mg (1 tablet on 500 mg or 2 tablets on 250 mg) in days once within 3 days (a course dose – 1,5 g).

At the chronic migrating erythema drug is appointed 1 time a day within 5 days: the first day – 1 g (2 tablets on 500 mg or 4 tablets on 250 mg), then on 500 mg (1 tablet on 500 mg or 2 tablets on 250 mg) daily from the second to the fifth day (a course dose – 3 g).

At infections, sexually transmitted: 1 g (2 tablets on 500 mg or 4 tablets on 250 mg) once.

At the infections of a stomach and duodenum associated with Helicobacter pylori appoint 1 g (2 tablets on 500 mg or 4 tablets on 250 mg) in days within 3 days as a part of a combination therapy.

At an acne вульгарис the course dose makes 6 g. Such scheme of treatment is recommended: in the first 3 days appoint on 1 tablet on 500 mg of 1 times the day following 9 weeks – on 1 tablet on 500 mg once a week, and for the second week apply a tablet in 7 days after the previous reception.

Children. To children with the body weight from 25 to 45 kg Aziadzhio is recommended to apply tablets of 250 mg.

At treatment of infections of ENT organs, respiratory tracts, skin and soft tissues (except the chronic migrating erythema) the recommended dose makes 10 mg/kg of body weight of 1 times a day within 3 days.

At the chronic migrating erythema drug is appointed 1 time a day within 5 days on 20 mg/kg of body weight in the first day, then on 10 mg/kg of body weight daily from the second to the fifth day.

To children with body weight more than 45 kg appoint doses for adults.

To children with body weight less than 25 kg appoint azithromycin in the form of suspension for oral administration with the corresponding dosing.

In case of the admission of reception of 1 dose of drug it is necessary to accept the passed dose as soon as possible, and the following – bucketed at 24 o'clock.

Patients of advanced age and patients with a renal failure have no need to change a dosage.

Features of use:

Use during pregnancy or feeding by a breast. Use of drug during pregnancy or feeding is not recommended by a breast (unless the expected effect exceeds possible risk of use of drug for a fruit or the child).

Children. This dosage form is not intended for treatment of children with body weight to 25 kg.

Features of use. Drug should be used with care for treatment of patients with heavy abnormal liver functions and kidneys, and also at cardiac arrhythmias (ventricular arrhythmias and lengthening of an interval of QT are possible).

Ability to influence the speed of reactions at control of motor transport or work with other mechanisms. Considering that sensitive patients at Aziadzhio's use can have a drowsiness or dizziness, for the period of administration of drug it is better to refrain from control of vehicles and work with other mechanisms.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, meteorism, abdominal pain, lock, loss of appetite, tranzitorny increase in activity of liver enzymes, cholestatic jaundice, gastritis.

Allergic reactions: skin rashes, an itch, urticaria, it is rare – a Quincke's disease, an acute anaphylaxis.

From cardiovascular system: heartbeat, thorax pain.

From a nervous system: dizziness, headache, paresthesias, excitement, drowsiness, irritability, sleep disorder, hyperkinesia, feeling of alarm, neurosis.

From an urinary system: nephrite.

From a reproductive system: vaginal candidiasis.

Others: conjunctivitis, photosensitization, arthralgia, hyperglycemia, neutropenia, eosinophilia.

Interaction with other medicines:

Antiacid means (calciferous, aluminum, magnesium), and also blockers of H2-histamine receptors slow down the azithromycin absorption speed therefore the 2-hour interval between reception of azithromycin and these drugs is necessary.

Macroleads at simultaneous use with theophylline, terfenadiny, warfarin, carbamazepine, Phenytoinum, triazolamy, digoxin, ergotamine, cyclosporine, valproic acid slow down removal of these drugs, increase their concentration and toxicity.

Azithromycin, unlike other makrolidny antibiotics, does not contact isoenzymes of system of P450 cytochrome. By this time interaction with the specified drugs was not observed.

At simultaneous use with warfarin it is recommended to control a prothrombin time.

Contraindications:

Hypersensitivity to antibiotics of group of macroleads or to any of drug components. This dosage form is not intended for treatment of children with body weight to 25 kg.

Overdose:

Symptoms: a temporary hearing disorder, the expressed nausea, diarrhea, vomiting.

Treatment: gastric lavage, reception of absorbent carbon. The symptomatic therapy directed to maintenance of the vital functions of an organism.

Storage conditions:

Period of validity - 2 years. To store in dry, protected from light and the place, unavailable to children, at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg: on 6 tablets in the blister. On 1 blister in a cardboard box. Tablets on 500 mg: on 3 tablets in the blister. On 1 blister in a cardboard box.