Azithromycin forte

General characteristics. Structure:

Active ingredient: 500 mg of azithromycin (in the form of a dihydrate) in 1 tablet.

Excipients: [cellulose microcrystallic, sodium lauryl sulfate, кросповидон, hypro rod (hydroxypropyl cellulose), magnesium stearate].

Excipients for a cover of Opadray II (series 85): [polyvinyl alcohol; macrogoal (polyethyleneglycol); talc; titanium dioxide; an aluminum varnish on the basis of indigo carmine dye; ferrous oxide yellow].

Bacteriostatic antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. The Makrolidny antibiotic of a broad spectrum of activity, an azalead, works bacteriostatically. Communicating with 50S – ribosome subunit, suppresses protein synthesis, slows down growth and reproduction of bacteria. In high concentration has bactericidal effect. Works on out of - and intracellular activators.

It is active concerning aerobic gram-positive microorganisms: Staphylococcusaureus (metitsillinchuvstvitelny), Streptococcuspneumonia (penitsillinchuvstvitelny), Streptococcuspyogenes;

aerobic gram-negative microorganisms: Haemophilusinfluenzae, Haemophilusparainfluenza, Legionellapneumophila, Moraxellacatarrhalis, Pasteurellamultocida, Neisseriagonorrhoeae;

some anaerobic microorganisms: Clostridiumperfringens, Fusobacteriumspp., Prevotellaspp., Porphyromonasspp.;

and also other activators: Chlamydiatrachomatis, Chlamydiapneumoniae, Chlamydiapsittaci, Mycoplasmapneumoniae, Mycoplasmahominis, Borreliaburgdorferi.

Aerobic gram-positive microorganisms - Streptococcuspneumonia are moderately sensitive or insensitive (moderately sensitive or resistant to penicillin).

It is not active concerning aerobic gram-positive microorganisms - Enterococcusfaecalis, Staphylococcusspp. (metitsillinustoychivy);

anaerobe bacterias of the Bacteroides fragilis group.

Streptococcus pneumonia, beta and hemolitic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including metitsillinustoychivy strains), resistant to erythromycin and other macroleads and linkozamida, are steady also against azithromycin.

Pharmacokinetics. Azithromycin is quickly soaked up from the digestive tract (DT) 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 (Cmax) 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), skin and soft tissues. High concentration in fabrics (is 10-50 times higher, than in a blood plasma) and a long elimination half-life (Т½) 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: Т½ 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 a day.

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:

Upper respiratory tract infection and ENT organs (sinusitis, tonsillitis, pharyngitis, average otitis);

Lower respiratory tract infections (bacterial, including caused by atypical activators, pneumonia, an exacerbation of chronic bronchitis);

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

Infections of mochevypolovy ways (gonorrheal and not gonorrheal urethritis, cervicitis);

initial stage of a disease Laima (borreliosis) – the migrating erythema.

Route of administration and doses:

Inside, for 1 h to or in 2 h after food of 1 times a day.

To adults and children 12 years at infections of upper and lower respiratory tracts, ENT organs, skin and soft tissues are more senior – 0,5 g/days for 1 reception within 3 days (a course dose – 1,5 g).

At infections of urinogenital ways (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).

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.

At the pharyngitis and tonsillitis caused by Streptococcuspyogenes, antibiotics of the choice is penicillin. Efficiency of azithromycin for prevention of rheumatic fever is unknown.

At azithromycin use, also as at use and other antibiotics, development of superinfection is possible (including fungal).

Influence on ability to driving or other mechanical means

It is necessary to refrain from the types of activity connected with need of high concentration of attention and bystry psychomotor reactions (including from driving of the car) at treatment the Sumametsiny fort.

Side effects:

Frequency of side reactions at use of azithromycin is specified below according to the standard classification: very often (≥1/10); often (≥1/100, <1/10); infrequently (≥1/1000, <1/100); seldom (≥1/10000, <1/1000); very seldom (<1/10000), including separate messages.

From a GIT: often - diarrhea, nausea, vomiting, pain or spasms in a stomach; infrequently – a meteorism, not properly executed chair, digestion disturbance, anorexia; seldom - a lock, language discoloration, pseudomembranous colitis, hepatitis, cholestatic jaundice, disturbance of functional trials of a liver (increase in activity of "hepatic" transaminases), a necrosis of a liver and a liver failure (up to a lethal outcome).

From a nervous system: infrequently - dizziness, вертиго, drowsiness, a headache, spasms, a food faddism and sense of smell; seldom – paresthesia, an adynamy, sleeplessness, a hyperactivity, aggression, concern, uneasiness, a nevroznost.

From urinogenital system: infrequently – a vaginitis; seldom – intersticial nephrite, an acute renal failure.

From a musculoskeletal system: infrequently – an arthralgia.

Allergic reactions: infrequently - rash, urticaria, a skin itch; seldom - a Quincke's disease, anafilaksichesky reactions, Stephens-Johnson's syndrome.

From sense bodys: seldom – a hearing disorder, deafness, a ring in ears.

From cardiovascular system (CCC): seldom – a heart consciousness, arrhythmia (including, ventricular tachycardia, piruetny tachycardia), lengthening of an interval of Q-T.

From integuments: seldom – a photosensitization, a mnogoformny erythema, a toxic epidermal necrolysis.

From bodies of a hemopoiesis: seldom – thrombocytopenia, it is very rare - a tranzitorny neutropenia.

Others: seldom – candidiasis.

Interaction with other medicines:

Antacids (aluminum and magniysoderzhashchy), ethanol and food slow down and reduce azithromycin absorption therefore azithromycin should be taken for 1 h to or in 2 h after reception of antacids.

At simultaneous use with cyclosporine it is necessary to control concentration in blood and to korrigirovat a dose of the last.

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 anticoagulating effect is possible, patients need to control a prothrombin time and the international normalized relation (INR) carefully.

Increases concentration of digoxin.

Ergotamine and dihydroergotamine: strengthening of toxic action (an ergotism - a vasospasm, a dizesteziya). Simultaneous use is contraindicated.

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

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

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

Simultaneous use with rifabutiny can lead to a neutropenia.

Contraindications:

Hypersensitivity (including to other macroleads); a heavy liver and/or renal failure, the lactation period, to children up to 12 years with body weight less than 45 kg, a concomitant use with ergotamine and dihydroergotamine.

With care:
- Arrhythmia (ventricular arrhythmias and lengthening of an interval of QT are possible);

- Moderate disturbances of functions of a liver or kidneys;

- Joint purpose of a terfenadin, warfarin, digoxin.

Overdose:

Overdose symptoms: deafness, nausea, vomiting, diarrhea.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 500 mg. On 2, 3 or 6 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4, 5 or 6 blister strip packagings together with the application instruction place in a pack from a cardboard.