Azimed (Suspension)

General characteristics. Structure:

Active ingredient: azithromycin;

5 ml of suspension contain dihydrate azithromycin in terms of azithromycin 200 mg;

excipients: sucrose, sodium phosphate, hydroxypropyl cellulose, xanthane gum, silicon dioxide colloid anhydrous, fragrance cherry, fragrance banana, fragrance vanilla.

Pharmacological properties:

Pharmacodynamics. Azithromycin is the representative of group of makrolidny antibiotics – the azaleads having a wide range of antimicrobic action. The mechanism of effect of azithromycin consists in inhibition of synthesis of bacterial protein due to linkng with the 50th S-subunit of ribosomes and prevention of a translocation of peptides in the absence of influence on synthesis of polynucleotides.

Resistance mechanism

Resistance to azithromycin can be inborn or acquired. Full cross resistance exists among Streptococcus pneumoniae, beta and hemolitic streptococci of group A, Enterococcus faecalis and Staphylococcus aureus, including metitsillinrezistentny golden staphylococcus (MRSA), to erythromycin, azithromycin, other macroleads and linkozamida.

Range of antimicrobic effect of azithromycin

Sensitive

Aerobic gram-positive bacteria

Staphylococcus aureus - metitsillinchuvstvitelny, Streptococcus pneumoniae - penitsillinchuvstvitelny, Streptococcus pyogenes (гр. A)

Aerobic gram-negative bacteria

Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida

Anaerobic bacteria

Clostridium perfringens, Fusobacterium spp. (types), Prevotella spp., Porphyromonas spp.

Other bacteria

Chlamydia trachomatis

Types which gain resistance in isolated cases

Aerobic gram-positive bacteria

Streptococcus pneumoniae – with intermediate sensitivity to penicillin, penitsillinrezistentny

Vrozhdennorezistentny organisms

Aerobic gram-positive bacteria

Enterococcus faecalis

Stafilokokkimrsa, MRSE (metitsillinrezistentny golden staphylococcus)

Anaerobic bacteria

Group of Bacteroides fragilis bacteroids

Pharmacokinetics. Bioavailability after oral administration makes about 37%. The maximum concentration in blood serum is reached in 2-3 hours after administration of drug.

At intake azithromycin is distributed on all organism. Pharmacokinetic researches showed that concentration of azithromycin in fabrics are much higher (by 50 times), than in plasma that demonstrates strong linkng of drug with fabrics.

Linkng with proteins of serum varies depending on plasma concentration and makes from 12% at 0,5 mkg/ml to 52% at 0,05 mkg/ml in serum. The Predpologayemy volume of distribution in an equilibrium state (VVss) makes 31,1 l/kg.

The final period of plasma semi-removal completely reflects an elimination half-life from fabrics within 2-4 days. About 12% of an intravenous dose of azithromycin are allocated not changed with urine during the next three days. Especially high concentration of not changed azithromycin are found in bile of the person. Also in bile ten metabolites which are not microbiological active are revealed.

Pharmaceutical characteristics.

Main physical and chemical properties: powder from white till yellow-white color with a characteristic smell of banana, vanilla and cherry.

The recovered suspension represents homogeneous suspension from white till light yellow color with a characteristic smell of banana, vanilla and cherry.

Indications to use:

The infections caused by the microorganisms sensitive to azithromycin:

·        infections of ENT organs (bacterial pharyngitis / tonsillitis, sinusitis, average otitis);

·        respiratory infections (bacterial bronchitis, not hospital pneumonia);

·        infections of skin and soft tissues: the migrating erythema (an initial stage of a disease of Lyme), an ugly face, impetigo, secondary pyodermatoses.

Route of administration and doses:

Азимед® accept 1 time a day, it is obligatory in 1 hour prior to or in 2 hours after food. At infections of upper and lower respiratory tracts, skin and soft tissues (except for the chronic migrating erythema) accept 10 mg/kg of body weight of 1 times a day for 3 days.

Depending on the body weight of the child such scheme of dosing is recommended:

Body weight        Daily dose
15-24             kg 5 ml (200 mg)
25-34             kg 7,5 ml (300 mg)
35-44             kg 10 ml (400 mg)
 ³ 45 kg              appoint doses for adults

The migrating erythema (Lyme's disease): 1 time a day for 5 days in a dose of 20 mg/kg of body weight in the 1st day, then – on 10 mg/kg of body weight from the 2nd to the 5th day.

Before the use to shake up.

Directly after suspension reception the child needs to allow to drink several drinks of liquid to wash away and swallow the suspension which remained in an oral cavity.

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 – at an interval of the 24th hour.

Renal failure.

Patients with insignificant dysfunction of kidneys (clearance of creatinine> of 40 ml/min.) do not have need to change dosing. There are no data on drug use to patients with clearance of creatinine <40 ml/min. Therefore such patients should apply azithromycin with care.

Liver failure.

As azithromycin is metabolized in a liver and removed with bile, drug should not be used to patients with a serious illness of a liver.

For ensuring full dosing the bottle has to contain additional 5 ml of suspension.

Азимед®, powder for 30 ml of peroral suspension. For receiving 35 ml of homogeneous suspension it is necessary to add 14,5 ml of the distilled water to a bottle from 1200 mg of azithromycin.

Suspension preparation

By means of the syringe for dosing it is possible to measure the amount of water necessary for drug dissolution.

1. The bottle contains powder from which by the water addition (distilled or prokipyachenny and cooled) prepare suspension.

2. Press a cover of a bottle from top to bottom and rotate counterclockwise.

3. For receiving Azimed® suspension it is necessary to add 14,5 ml of water.

4. Carefully shake up bottle contents before receiving homogeneous suspension.

Application instruction

Packaging contains the syringe for dosing and a spoon. The spoon has marking of 2,5 ml and 5 ml.

Filling of the syringe with drug

1. Before use shake up suspension.

2. Press a cover from top to bottom and turn counterclockwise.

3. Ship the syringe in suspension and, extending the piston up, gain necessary amount of suspension.

4. If you noticed vials of air in the syringe, return drug to a bottle and repeat the procedure 3.

Drug use to the child

1. Arrange the child as for feeding.

2. You pokladit a tip of the syringe in a mouth to the child and slowly force out contents.

3. Give to the child the chance to gradually swallow all amount of drug.

4. After administration of drug let's the child drink a little tea or juice to wash away and swallow the suspension which remained in an oral cavity.

Washing and storage of the syringe

Disassemble the used syringe, wash out flowing water, dry up and you store in the dry and pure place together with drug.

After the child accepted the last dose of drug, the syringe and a bottle need to be destroyed.

Features of use:

Allergic реакции:в exceptional cases azithromycin causes serious allergic (seldom lethal) reactions, such as a Quincke's disease and an anaphylaxis.

The extended cordial repolarization and interval of QT increasing risk of development of cardiac arrhythmia and a torsade de pointes of ventricles that it is also observed at treatment by other makrolidny antibiotics. The similar effect of azithromycin cannot be excluded completely at patients with the increased risk of lengthening of cordial repolarization.

Streptococcal инфекции:азитромицин it is effective for treatment of a streptococcus in a stomatopharynx, however there are no data showing efficiency of azithromycin for prevention of acute rheumatic polyarthritis.

Superinfektsii:kak and at use of other antibacterial drugs, exists possibility of superinfection (for example mycosis).

Because drug contains sucrose, patients cannot appoint it with rare hereditary syndromes of an intolerantnost to fructose, glyukozo-galaktozny malabsorption or insufficiency of sucrose-isomaltase.

Ability to influence speed of response at control of motor transport or the robot with other mechanisms.

Drug is intended for use in pediatrics.

Side effects:

Assessment of by-effects is based on classification taking into account the frequency of reactions: very often> 10%; often> 1% - <10%; infrequently> 0,1% - <1%; seldom> 0,01% - <0,1%; very seldom <0,01%, including isolated cases.

From blood and lymphatic системы:редко – thrombocytopenia;

from outside психики:редко – aggression, a hyperactivity, alarm and nervousness;

from a nervous system: infrequently — dizziness / вертиго, drowsiness, a headache, a syncope, spasms (it was revealed that they are also called by other makrolidny antibiotics), distortion of taste and perception of smells; seldom – paresthesia, an adynamy, sleeplessness;

from bodies слуха:редко makrolidny antibiotics can cause the hearing disorder having reversible character;

from a cardiovascular sistemy:redko – strong heartbeat, arrhythmia, ventricular tachycardia (it was revealed that they are also called by other makrolidny antibiotics), and also lengthening of an interval of QT and a torsade de pointes of ventricles, arterial hypotension is possible;

from a digestive trakta:chasto – nausea, vomiting, diarrhea, discomfort in a stomach (pains/spasms); infrequently – diarrhea, a meteorism, digestion disturbance, anorexia; seldom – a lock, language discoloration. Pseudomembranous colitis, pancreatitis are possible;

from a liver and bilious пузыря:редко – hepatitis and cholestatic jaundice, including pathological changes of a functional trial of a liver, and also isolated cases of necrotic hepatitis and dysfunction of a liver which in rare instances lead to a lethal outcome;

from outside кожи:нечасто – allergic reactions, including an itch and rashes; seldom – allergic reactions, including a Quincke's disease, a small tortoiseshell and a photosensitivity; serious skin reactions, namely: polymorphic erythema, Stephens-Johnson's syndrome and toxic epidermal necrolysis;

from a skeletal and muscular sistemy:nechasto – an arthralgia;

from kidneys and urinary путей:редко – intersticial nephrite and an acute renal failure;

from a reproductive sistemy:nechasto – a vaginitis;

системныенарушения:редко – an anaphylaxis, including hypostasis, candidiasis.

Interaction with other medicines:

It is necessary to appoint with care azithromycin along with other drugs which can extend QT interval (for example with quinidine, cyclophosphamide, ketokonazoly, terfenadiny, a haloperidol, lithium).

Simultaneous use of antacids and azithromycin of change in bioavailability of the last were not observed by Antatsidy:pri though plasma peak concentration of azithromycin decrease by 30%. Azithromycin needs to be taken at least for 1 h to or in 2 h after reception of an antacid.

Karbamazepin:azitromitsin does not exert considerable impact on carbamazepine level in a blood plasma or on its active metabolites.

Tsiklosporin:nekotory makrolidny antibiotics influence cyclosporine metabolism. It is necessary to assess carefully a therapeutic situation before purpose of a concomitant use of azithromycin and cyclosporine. At expediency of a combination therapy it is necessary to carry out careful monitoring of level of cyclosporine and to respectively regulate dosing.

Coumarinic antikoagulyanty:vozmozhno increase in a tendency of a kkrovotecheniyampra simultaneous use of azithromycin and warfarin or cumarine-like peroral anticoagulants. Frequent monitoring of a prothrombin time is necessary.

Digoxin: in case of simultaneous use of azithromycin and digoxin it is necessary to remember a possibility of increase in concentration of digoxin and to carry out monitoring of level of digoxin.

Terfenadin:kak and in a case with other makrolidny antibiotics, it is necessary to appoint azithromycin with care in a combination with terfenadiny.

Teofillin:azitromitsin does not influence theophylline pharmacokinetics at simultaneous use of azithromycin and theophylline. The combined use of theophylline and other makrolidny antibiotics sometimes leads to increase in level of theophylline in blood serum.

Metilprednizolon:azitromitsin significantly does not influence Methylprednisolonum pharmacokinetics.

Zidovudin:azitromitsin does not influence plasma pharmacokinetics or removal with urine of a zidovudine or its glyukuronidny metabolites. However reception of azithromycin can increase concentration of a fosforilirovanny zidovudine, clinically active metabolite, in mononukleara in peripheric circulation.

Didanozin:pri simultaneous use of daily doses of 1200 mg of azithromycin with didanoziny did not reveal influence on pharmacokinetics of a didanozin.

Rifabutin:odnovremenny use of azithromycin and rifabutin does not influence plasma concentration of these drugs. The neutropenia can be observed at patients who accept at the same time azithromycin and рифабутин. Though the neutropenia is connected using a rifabutin, a causal relationship with a concomitant use of azithromycin is not established.

Contraindications:

Hypersensitivity to active ingredient, to any other component of drug or to other makrolidny antibiotics. In view of a theoretical possibility of an ergotism azithromycin should not be applied along with ergot derivatives.

Overdose:

Typical symptoms peredozirovki:obratimy hearing disorder, nausea, vomiting and diarrhea. In case of overdose it is necessary to accept absorbent carbon and to carry out the symptomatic therapy directed to maintenance of the vital functions of an organism.

Use during pregnancy or feeding by a breast.

Drug is intended for use in pediatrics.

Children.

To apply to children with body weight more than 15 kg.

Storage conditions:

Period of validity 2 years. A suspension period of validity – 10 days. To store in original packaging at a temperature not vyshe25 °C. To store suspension in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1200 mg of azithromycin in a bottle for preparation of 30 ml of suspension for oral use. On 1 bottle together with the calibration syringe and a measured spoon for dosing in a pack.