AzitRus - instructions for use, doses, side effects, contraindications

Excipients: sodium citrate (sodium citric acid trisubstituted) - 0.63 g, 0.63 g, 0.63 g; sodium saccharinate (saccharin soluble) 0.021 g, 0.021 g, 0.021 g; orange flavoring (orange food flavoring) 0.0074 g, 0.0074 g. 0.0074 g; sucrose (sugar) 3,1216 g, 3,0716 g, 2,971 g; crospovidone (collidine CML) 0.37 g, 0.37 g, 0.37 g

Description:The powder is white or almost white with an orange smell. The finished suspension is a homogeneous white suspension with a yellowish tinge.

Pharmacotherapeutic group:Antibiotic-azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Azithromycin is a bacteriostatic broad-spectrum antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of a microbial cell.By binding to the 50S subunit of the ribosome, it inhibits the peptidranslokase at the translation stage and suppresses protein synthesis, slowing the growth and multiplication of bacteria. In high concentrations has a bactericidal effect.

Has activity against a number of gram-positive. gram-negative, anaerobes, intracellular and other microorganisms.

Sensitive microorganisms:

aerobic gram-positive microorganisms - Staphylococcus aureus (methicillin-sensitive strains), Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes;

aerobic gram-negative microorganisms - Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;

anaerobic microorganisms Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp .;

others microorganisms - Chlamydia trachomatis, Chlamydia pneumoniae. Chlamydia psittaci. Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms, can develop resistance to azithromycin:

aerobic gram-positive microorganisms - Streptococcus pneumoniae (penicillin-resistant strains and strains with an average sensitivity to penicillin).

Microorganisms with initial resistance:

aerobic gram-positive microorganisms - Enterococcus faecalis; Staphylococci (methicillin-resistant strains);

anaerobic Gram-positive microorganisms - Bacteroides fragilis.

The sensitivity scale of microorganisms to azithromycin (Minimum inhibitory concentration (MIC), mg / l)

Microorganisms	MITO mg / l *
Microorganisms	Sensitive	Sustainable
Staphylococcus	no more 1	more than 2
Streptococcus A, B, C, G	not more than 0.25	more than 0.5
Streptococcus pneumoniae	not more than 0,25	more than 0.5
Haemophilus influenzae	not more than 0,12	more than 4
Moraxella catarrhalis	no more than 0.5	more than 0.5
Neisseria gonorrhoeae	not more than 0,25	more than 0.5

Pharmacokinetics:

After taking the drug inside the bioavailability is 37%, the maximum concentration in the blood plasma (C_max) is created after 2-3 hours, the volume of distribution is 31.1 l / kg. Binding to plasma proteins is inversely proportional to the concentration in the blood and is 12-52%. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. Easily passes through the histohematological barriers and enters the tissues. The concentration in tissues and cells is 50 times higher than in blood plasma, and in the focus of infection is 24-34% more than in healthy tissues.

It is slowly excreted from the tissues and has a long half-life period of 2-4 days.The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is deduced, basically, in the unchanged form of 50% of the intestine, 12% of the kidneys. In the liver, demethylated, losing activity.

In patients with severe renal failure (creatinine clearance less than 10 ml / min), the half-life of azithromycin increases by 33%.

Indications:

Infectious-inflammatory diseases caused by microorganisms susceptible to azithromycin: infections of the upper and lower respiratory tract (sinusitis, tonsillitis, pharyngitis, otitis media, acute bronchitis, exacerbation of chronic bronchitis and community-acquired pneumonia); infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses); urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis); Lyme disease (initial stage of borreliosis) migrating erythema (erythema migrans).

Contraindications:

Hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides, or other components of the drug; severe hepatic dysfunction (no data on efficacy and safety); impaired renal function (CC less than 40 ml / min) (no data on efficacy and safety); deficiency of sugar / isomaltase, intolerance to fructose,glucose-galactose malabsorption; children up to 6 months; breast-feeding; simultaneous reception of ergotamine and dihydroergotamine.

Carefully:

Pregnancy; myasthenia gravis; violations of liver function of mild and moderate severity; renal dysfunction of mild and moderate severity (SC more than 40 ml min): diabetes mellitus: in patients with pro-arrhythmic factors (especially in elderly patients): with congenital or acquired lengthening of the interval QT, in patients receiving antiarrhythmic drug therapy classes IA (quinidine, procainamide), III (dofetilide, amiodarone, sotalol), cisapride, terfenadine. antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances of the water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of warfarin, digoxin, cyclosporine.

Pregnancy and lactation:

The use of the drug in pregnancy is possible only if the intended benefit for the mother exceeds potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (azithromycin excreted in breast milk).

Dosing and Administration:

Inside the 1 h before meals or 2 hours after meals 1 time per day.

Adults:

In infections of the upper and lower respiratory tract 500 mg / day for 1 reception for 3 days (exchange dose 1,5 g).

With infections of the skin and soft tissues 500 mg / day for I reception for 3 days (exchange dose - 1.5 g).

In acute infections of the urogenital organs (notcomplicated urethritis or cervicitis) one time 1 g.

With Lyme disease (borreliosis) for treatment of stage I (erythema migrans) 1 g on the first day and 500 mg daily from 2 to 5 days (course dose 3 g).

Children from 6 months:

In infections of the upper and lower respiratory puENT organs, skin and meg(with the exception of migrating erythema) prescribe children in a single (daily) dose at a rate of 10 mg / kg body weight 1 time per day for 3 consecutive days (exchange dose of 30 mg / kg body weight)

Depending on the body weight of the child, the following doses are recommended:

Body weight, kg	Single (daily) dose of azithromycin, mg / day
10-14	100
15-24	200
25-34	300
35-44	400
not less than 45	500

With pharyngitis and tonsillitis caused by Streptococcus pyogenes, the preparation AzitRus® is used in a dose of 20 mg / kg / day for 3 days (the course dose of 60mg / kg). The maximum daily dose is 500 mg.

With Lyme disease (the initial stage of borreliosis) migratory erythema (erythema migrans) the drug is prescribed to children once a day for 5 days: 20 mg / kg of body weight on the first day and 10 mg / kg of body weight from 2 to 5 days (exchange dose of 60 mg / kg).

Note:

a dose of 150 mg corresponds to: 1 packet of 100 mg - 1 package 50 mg or 3 packets of 50 mg:

dose 250 mg corresponds to: 1 packet of 200 mg + 1 packet of 50 mg or 2 packets of 100 mg - 1 package 50 mg;

a dose of 500 mg corresponds to: 1 packet of 200 mg + 1 packet of 100 mg or 3 packets of 100 mg; a dose of 400 mg corresponds to: 2 packages of 200 mg or 4 packets of 100 mg or 8 packets of 50 mg or 3 packets of 100 mg + 2 packs of 50 mg or 2 packets of 100 mg - 4 packets of 50 mg;

a dose of 500 mg corresponds to: 2 packets of 200 mg + 1 packet of 100 mg or 5 packets of 100 mg or 1 packet of 200 mg + 3 packets of 100 mg or 2 packets of 100 mg + 6 packets of 50 mg or 10 packets of 50 mg.

Immediately after taking the suspension, the child should be given a few sips of fluids (water, teas) in order to wash off and swallow the remaining suspension in the oral cavity.

Patients with impaired renal function

When used in patients with impaired renal function (QC more than 40 ml min) dose adjustment ns is required.

Patients with hepatic impairment and elderly patients

When used in patients with impaired liver function of mild and moderate severity, elderly patients do not need dose adjustment.

Cooking method.

In a clean cup, pour boiled and cooled to room temperature water in an amount of at least 10 ml (2 teaspoons) per package, then pour the contents of one or more packages and mix until a homogeneous suspension is obtained.

After taking the glass, rinse with water, dry and store in a dry and clean place.

Side effects:

Infectious diseases: pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis, candidiasis, including mucous membranes of the oral cavity and genitals, pseudomembranous colitis.

From the side of metabolism and nutrition: anorexia.

Allergic reactions: hypersensitivity reactions, angioedema, anaphylactic reaction.

From the side of the blood and lymphatic system: lymphocytopenia, eosinophilia, leukopenia, neutropenia. thrombocytopenia, hemolytic anemia.

From the nervous system: dizziness, headache, paresthesia, taste disorders, agitation, hypoesthesia, drowsiness, insomnia, nervousness. anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell (or anosmia), perversion of smell,taste sensations, myasthenia gravis, anxiety, wobble, hallucinations.

From the side of the organ of vision: impaired vision.

From the side of the hearing organ and labyrinthine disorders: deafness, noise in the ears, twists, hearing disorder.

From the cardiovascular system: palpitation, lowering blood pressure, increasing the interval QT. arrhythmia such as "pirouette", ventricular tachycardia, "tides" of blood to the face.

From the respiratory system: shortness of breath, nosebleed.

From the gastrointestinal tract: dysphagia, abdominal distension, nausea, diarrhea, abdominal pain, flatulence, dyspepsia, vomiting, gastritis, constipation, change the language of color, dryness of the oral mucosa, burping, ulcer oral mucosa, increased secretion of the salivary glands, pancreatitis.

From the liver and bile ducts: increased activity "liver" enzymes, increasing the concentration of bilirubin, hepatitis, liver dysfunction, cholestatic jaundice, hepatic failure (in rare cases, fatal mainly the presence of severe liver disorder), hepatic necrosis, fulminant hepatitis.

From the osteomuscular system and connective tissue: osteoarthritis, myalgia, back pain, neck pain, arthralgia.

From the skin and subcutaneous tissues: skin rash, itching. urticaria, dermatitis, dry skin, sweating, photosensitivity reaction, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.

From the side of the kidneys and urinary tract: dysuria, pain in the kidney, increased urea and creatinine in the blood plasma, interstitial nephritis, acute renal failure.

Other: metrorrhagia, dysfunction of testicles, weakness, facial edema, chest pain, fever, peripheral edema, asthenia, malaise, change in potassium concentration.

Laboratory data: an increase in the number of basophils, monocytes, neutrophils, a decrease or increase in the concentration of bicarbonates in the blood plasma, an increase in the activity of alkaline phosphatase in the blood plasma, an increase in the level of chlorine in the blood plasma, an increase in the concentration of glucose in the blood, an increase in the number of platelets, an increase in hematocrit, a change in the sodium content in the plasma blood.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Interaction:

Antacid drugs do not affect the bioavailability of azithromycin, but reduce the maximum concentration in blood plasma by 30%, so azithromycin should be taken at least one hour before or two hours after taking these drugs. Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and methylprednisolone in plasma.

Given the theoretical possibility of the emergence of ergotism, the simultaneous use of azithromycin with derivatives of ergot alkaloids is not recommended.

Separate reports of cases of rhabdomyolysis in patients concomitantly receiving azithromycin and statins.

With the simultaneous use of azithromycin and rifabutin, neutropenia was sometimes observed, despite the fact that neutropenia was associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established.

With the simultaneous use of azithromycin and cyclosporine, dose adjustments of cyclosporine are necessary.

Azithromycin weakly interacts with isoenzymes of the cytochrome system R₄₅₀. It was not revealed that azithromycin participates in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor and inducer of cytochrome isoenzymes R₄₅₀.

With the simultaneous use of digoxin and azithromycin, it is necessary to monitor the concentration of digoxin in the blood plasma, since many macrolides increase the absorption of digoxin in the intestine.

If it is necessary to use simultaneously with anticoagulant means of indirect action (warfarin, other anticoagulants of the coumarin type) it is recommended to carry out a thorough prothrombin time control.

It was found that simultaneous use of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening of the interval QT. Proceeding from this, it is impossible to exclude the aforementioned complications with concurrent administration of terfenadine and azithromycin.

Simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentration of azithromycin in the blood plasma. Clinically significant side effects were not observed and correction of the dose of azithromycin with its simultaneous application with nelfinavir is not required.

When combined with zidovudine azithromycin do not affect the pharmacokinetic parameters of zidovudine in the blood plasma or to excrete the kidneys of its and its metabolite glucuronide. Nevertheless, the concentration of the active metabolite of phosphorylated zidovudine in mononuclear cells of peripheral vessels increases. The clinical significance of this fact is not clear.

Special instructions:

When prescribing AzitRus® in patients with diabetes mellitus, as well as with a low-calorie diet, it is necessary to take into account that the preparation contains sucrose (about 0.3 XE in one package).

If you miss a dose of AzitRus®, the missed dose should be taken as soon as possible, and the subsequent dose with interruptions of 24 hours.

The drug AzitRus® should be used with caution in patients with mild liver function disorders due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency.

If there are symptoms of liver dysfunction, such as rapidly growing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy with AsitRus® should be discontinued and an examination of the functional state of the liver should be carried out.

For violations of the function of the kidneys of mild severity (CC more than 40 ml / min), therapy with AsitRus® should be performed with caution under the control of the state of kidney function.

It should be remembered that for the prevention of pharyngitis / tonsillitis caused by Streptococcus pyogenes, as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin.

As with the use of other antibacterial drugs, patients with AsitRus® should regularly examine patients for non-susceptible microorganisms and signs of development of superinfections, including fungal ones.

A drug AzitRus® should not be used with longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and convenient dosage regimen.

There is no data on the possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but because of the development of argotism with the simultaneous use of macrolides with derivatives of ergotamine and dihydroergotamine this combination is contraindicated. With the long-term administration of the drug AsitRus®, the development of pseudomembranous colitis, caused by Clostridium difficile, as in the form of mild diarrhea, and severe colitis. With the development of diarrhea against the background of taking azithromycin, and also 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. Drugs that inhibit the intestinal peristalsis are contraindicated.

Syndrome of delayed repolarization of the ventricles syndrome of lengthening the interval QT increases the risk of arrhythmias, including arrhythmias such as "pirouette" against the background of taking macrolides, as well as the drug AzitRus®. Caution should be exercised when using AzitRus® in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired lengthening of the interval QT, in patients receiving antiarrhythmic drug therapy classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), in patients with disturbances of water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure.

The use of the drug AzitRus® can provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Effect on the ability to drive transp. cf. and fur:

With the development of undesirable effects on the part of the nervous system and the organ of vision, care should be taken when performing actions requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Powder for the preparation of a suspension for oral administration of 50 mg, 100 mg, 200 mg.

Packaging:

According to 4.2 g (50 mg, 100 mg or 200 mg azithromycin) in heat-sealable single-dose bags from the material of a composite multilayer on the basis of a foil or the material of a combined multilayer bevel or paper with a polyethylene coating.

3 or 6 packets (50 mg, 100 mg or 200 mg of azithromycin) with instructions for use and a plastic cup or without a glass are placed in a pack of cardboard.

Storage conditions:

AT protected from light at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003268/07

Date of registration:17.10.2007 / 21.04.2015

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp22.06.2017

Illustrated instructions

Instructions

AzitrRus® (AzitRus®)