Azitromitsin-OBL

General characteristics. Structure:

Active ingredient: 250 mg of azithromycin (in the form of a dihydrate) in 1 capsule.

Excipients: cellulose microcrystallic, povidone (polyvinylpirrolidone low-molecular medical), кросповидон, calcium stearate, sodium lauryl sulfate.

Capsules firm gelatinous No. 1: titanium dioxide, dye blue patent (patent blue V), diamond black, dye crimson [Ponso 4R], azoruby, gelatin.

Antibiotic of a broad spectrum of activity. Is also means of the first choice in therapy of diseases, sexually transmitted.

Pharmacological properties:

Pharmacodynamics. Azithromycin – a bacteriostatic antibiotic of a broad spectrum of activity from group of macroleads azaleads. Possesses a wide range of antimicrobic action. The mechanism of effect of azithromycin is connected with suppression of synthesis of protein of a microbic cell. Communicating with 50S – ribosome subunit, oppresses to a peptidtranslokaz at a stage of broadcasting and suppresses protein synthesis, slowing down growth and reproduction of bacteria. In high concentration has bactericidal effect.

Has activity concerning a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.

Microorganisms can be initial steady against action of an antibiotic or can gain resistance to it.

In most cases sensitive microorganisms

1. Gram-positive aerobes: Staphylococcusaureus Methicillinum-sensitive; Streptococcuspneumoniae Penicillin-sensitive; Streptococcus pyogenes.

2. Gram-negative aerobes: Haemophilus influenzae; Haemophilus parainfluenzae; Legionella pneumophila; Moraxella catarrhalis; Pasteurella multocida; Neisseria gonorrhoeae.

3. Anaerobe bacterias: Clostridium perfringens; Fusobacterium spp.; Prevotella spp.; Porphyriomonas spp.

4. Other microorganisms: Chlamydia trachomatis; Chlamydia pneumoniae; Chlamydia psittaci; Mycoplasma pneumoniae; Mycoplasma hominis; Borrelia burgdorferi.

The microorganisms capable to develop azithromycin resistance.

Gram-positive aerobes: Streptococcuspneumoniae Penicillin-sensitive.

Initially steady microorganisms.

Gram-positive aerobes: Enterococcusfaecalis; Staphylococci (Methicillinum - steady staphylococcus show very high degree of resistance to macroleads); gram-positive bacteria steady against erythromycin. 

Anaerobe bacterias: Bacteroidesfragilis.

Pharmacokinetics. Azithromycin is quickly soaked up from digestive tract that is caused by its stability in acid medium and lipophilicity. It is quickly distributed on all organism, at the same time in fabrics high concentration of an antibiotic are reached. After intake of 500 mg the maximum concentration of azithromycin in a blood plasma is reached in 2,5-2,9 h and makes 0,4 mg/l. Bioavailability makes 37,5%.

Azithromycin well gets into respiratory tracts, bodies and fabrics of an urogenital path (in particular, into a prostate), into skin and soft tissues. High concentration in fabrics (is 10-50 times higher, than in a blood plasma) and a long elimination half-life are caused by low linkng of azithromycin with proteins of a blood plasma, and also its ability to get into eukaryotic cells and to concentrate in the environment with a low rn, a surrounding lysosome. It, in turn, determines the large seeming distribution volume (31,1 l/kg) and high plasma clearance.

Ability of azithromycin to collect preferential in lysosomes, is especially important for elimination of intracellular activators. It is proved that phagocytes deliver azithromycin to places of localization of an infection where it is released in the course of phagocytosis. Concentration of azithromycin in the centers of an infection it is reliable above, than in healthy fabrics (on average for 24-34%) and correlates with degree of inflammatory hypostasis. Azithromycin remains in bactericidal concentration within 5-7 days after reception of the last dose that allowed to develop short (3-day and 5-day) courses of treatment.

In a liver it demetilirutsya, the formed metabolites are not active.

Removal of azithromycin from a blood plasma takes place in 2 stages: the elimination half-life makes 14-20 h in the range from 8 to 24 h after administration of drug and 41 h – in the range from 24 to 72 h that allows to use drug of 1 times/days.

Drug generally with bile in an invariable look is removed, a small part is removed by kidneys.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

· Infections of upper parts of respiratory tracts and ENT organs (pharyngitis/tonsillitis, sinusitis, average otitis);

· Infections of lower parts of respiratory tracts: an acute bronchitis, an exacerbation of chronic bronchitis, including caused by atypical activators;

· Infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis);

· An initial stage of a disease Laima (borreliosis) – the migrating erythema (Erythemamigrans);

· The infections of urinogenital ways caused by Chlamydiatrachomatis (an urethritis, a cervicitis).

Route of administration and doses:

Inside, 1 time a day, at least, for 1 h to or in 2 h after food.

The adult (including elderly people) and to children 12 years with body weight over 45 kg are more senior.

At infections of upper and lower respiratory tracts, ENT organs, skin and soft tissues of 500 mg (2 capsules) once a day 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 the migrating erythema. 1 time a day within 5 days: the 1st day – 1,0 g (4 capsules), then from the 2nd to the 5th day – on 500 mg (2 capsules) (a course dose of 3,0 g).

At infections of urinogenital ways, the caused Chlamydiatrachomatis (an urethritis, a cervicitis). An uncomplicated urethritis / cervicitis – 1 g (4 capsules) once.

Appointment to patients with a renal failure. For patients with moderate renal failures (clearance of creatinine> of 40 ml/min.) dose adjustment is not necessary.

Features of use:

Use at pregnancy and during breastfeeding: Use of drug at pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit.

In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding (it is allocated with breast milk).

Not to accept with food.

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 in 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.

Influence on ability to manage motor transport and mechanisms. Azithromycin does not exert impact on ability to manage motor transport and mechanisms.

Side effects:

Allergic reactions: an itch, skin rashes, a Quincke's disease, a small tortoiseshell, anaphylactic reaction, including hypostasis (in rare instances from the death), a mnogoformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrosis.

From circulatory and lymphatic systems: thrombocytopenia, neutropenia.

From the central nervous system: dizziness / вертиго, headache, spasms, drowsiness, paresthesia, adynamy, sleeplessness, hyperactivity, aggression, concern, nervousness.

From sense bodys: a sonitus, a reversible hearing disorder up to deafness (at reception of high doses for a long time), disturbance of perception of taste and a smell.

From cardiovascular system: seldom – heartbeat, arrhythmia, ventricular tachycardia, increase in an interval of QT, bidirectional ventricular tachycardia.

From the alimentary system: nausea, vomiting, diarrhea, abdominal pains / spasms, a liquid chair, a meteorism, a digestive disturbance, anorexia, a lock, language discoloration, pseudomembranous colitis, cholestatic jaundice, hepatitis, change of laboratory indicators of functions of a liver, liver dysfunction, a liver necrosis (it is possible from the death).

From a musculoskeletal system: arthralgia.

From urinogenital system: nephrite, acute renal failure.

Others: vaginitis, candidiasis, photosensitization.

Interaction with other medicines:

Antiacid means do not influence bioavailability of azithromycin, but reduce the maximum concentration in blood by 30% therefore drug should be accepted, at least, in one hour prior to or in two hours after reception of these drugs and food.

Azithromycin does not influence concentration of carbamazepine, a didanozin, rifabutin and Methylprednisolonum in blood when sharing.

At parenteral use azithromycin does not influence concentration of Cimetidinum, efavirenz, flukonazol, indinavir, midazolam, a triazolam, Trimethoprimum/sulfamethoxazole in blood when sharing, however it is not necessary to exclude possibilities of such interactions at purpose of azithromycin for intake.

Azithromycin does not influence theophylline pharmacokinetics, however at joint reception with other macroleads concentration of theophylline in a blood plasma can increase.

In need of combined use with cyclosporine, it is recommended to control the content of cyclosporine in blood. In spite of the fact that there are no data on influence of azithromycin on change of concentration of cyclosporine in blood, other representatives of a class of macroleads are capable to change its level in a blood plasma.

At joint reception of digoxin and azithromycin it is necessary to control digoxin level in blood as many macroleads increase absorption of digoxin in intestines, increasing that its concentration in a blood plasma.

At joint purpose of warfarin and azithromycin it is recommended to carry out careful control of a prothrombin time.

It was established that the concomitant use of a terfenadin and antibiotics of a class of macroleads causes arrhythmia and lengthening of QT of an interval. Proceeding from that, it is impossible to exclude the above-stated complications at joint reception of a terfenadin and azithromycin.

As there is a possibility of inhibition of CYP3A4 enzyme azithromycin in a parenteral form at joint appointment with cyclosporine, terfenadiny, ergot alkaloids, tsizapridy, Pimozidum, quinidine, astemizoly and other drugs which metabolism happens to participation of this enzyme it is necessary to consider a possibility of such interaction at purpose of azithromycin for intake.

At joint reception of azithromycin and a zidovudine, azithromycin does not influence pharmacokinetic parameters of a zidovudine in a blood plasma or on removal by kidneys of its and its metabolite of a glucuronide. Nevertheless, concentration of an active metabolite – a fosforilirovanny zidovudine in mononuclear cells of peripheral vessels increases. Clinical value of this fact is not clear.

At a concomitant use of macroleads with ergotamine and dihydroergotamine manifestation of their toxic action is possible.

Contraindications:

· Hypersensitivity to antibiotics of group of macroleads;

· Heavy abnormal liver functions and kidneys;

· Children's age up to 12 years with body weight less than 45 kg (for this dosage form);

· Breastfeeding;

· A concomitant use with ergotamine and dihydroergotamine.

With care:

– moderate abnormal liver functions and kidneys;

– at arrhythmias or predisposition to arrhythmias and lengthening of an interval of QT;

– at joint purpose of a terfenadin, warfarin, digoxin.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

Period of validity - 3 years. Not to apply after a period of validity. List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg. On 6 or 10 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1 blister strip packaging together with the application instruction in a pack from a cardboard.