Azithromycin Ecomed powder for oral suspension preparation 100mg/5ml 16.5g vial, 1pc

Composition

Composition of components in 5 ml suspension:

Active ingredient:

azithromycin dihydrate 104.82 mg (based on azithromycin) 100.00 mg

Auxiliary substances:

lactitol 200.00 mg

sodium carbonate anhydrous 83.00 mg

crospovidone (collidone CL-M) 65.00 mg

strawberry flavor 55.00 mg

sodium benzoate 16.50 mg

xanthan gum 15.00 mg

apple flavor 13.75 mg

cinnamon flavor 13.75 mg

titanium dioxide 10.00 mg

colloidal silicon dioxide 5.50 mg

mint flavor 0.50 mg

sucrose by weight 3.75 g

Pharmacological action

Broad-spectrum antibacterial drug from the group of macrolides-azalides, has a bacteriostatic effect.

Binding to the 50S subunit of ribosomes, it inhibits peptidtranslase at the translation stage, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and has a bactericidal effect in high concentrations.

It acts on extracellularly and intracellularly located pathogens.

Microorganisms may be initially resistant to the action of an antibiotic or may become resistant to it.

Scale of sensitivity of microorganisms to azithromycin (Minimum inhibitory concentration, mg / l):

Microorganisms Sensitive Resistant

Staphylococcus ≤ 1 > 2Streptococcus A, B, C, G ≤ 0,25 > 0,5 Streptococcus pneumoniae ≤ 0,25 > 0,5 Haemophilus influenzae ≤ 0,12 > 4Moraxella catarrhalis ≤ 0,5 > 0,5 Neisseria gonorrhoeae ≤ 0,25 > 0,5

Sensitive: aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), 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., Porphyromonas spp. ;others: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi. Moderately sensitive or insensitive: aerobic gram-positive microorganisms: Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).

Sustainable: aerobic gram-positive microorganisms: Enterococcus faecalis, Methicillin-resistant strains of Staphylococcus aureus. Anaerobes: the Bacteroides fragilis group. Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. group A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-sensitive strains), resistant to erythromycin and other macrolides, lincosamides, are also resistant to azithromycin.

PharmacokineticsAfter oral use, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose of 0.5 g – 37% (the effect of “first pass” through the liver), the maximum concentration (Cmax) after oral use of 0.5 g-0.4 mg / l, the time to reach the maximum concentration (TCmax) – 2-3 hours. The concentration in tissues and cells is 10-50 times higher than in serum. The volume of distribution is 31.1 l / kg, binding to plasma proteins is inversely proportional to the concentration in the blood and is 7-50%.

Azithromycin – acid-resistant, lipophilic. Easily passes through histohematic barriers, penetrates well into the respiratory tract, internal organs and tissues, including the prostate gland, skin and soft tissues. It is also transported to the site of infection by phagocytes, polymorphonuclear leukocytes and macrophages, where it is released in the presence of bacteria. It penetrates cell membranes and creates high concentrations in them, which is especially important for the eradication of intracellularly located pathogens.

In the foci of infection, the concentration is 24-34% higher than in healthy tissues and correlates with the severity of the inflammatory process. It remains in effective concentrations for 5-7 days after the last dose. It is demethylated in the liver, and the resulting metabolites are not active. The drug is metabolized by CYP3A4, CYP3A5, and CYP3A7 isoenzymes, of which it is an inhibitor. Plasma clearance – 630 ml / min: half-life between 8 and 24 hours after use-14-20 hours, half-life in the range from 24 to 72 hours-41 hours. More than 50% of the drug is excreted unchanged through the intestine,6% – by the kidneys.

Food intake significantly changes the pharmacokinetics: Cmax increases (by 31%), the area under the concentration-time curve (AUC) does not change. In elderly men (65-85 years), the pharmacokinetic parameters do not change; in women, Cmax increases (by 30-50%).

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin: * upper respiratory tract and ENT infections: pharyngitis, tonsillitis, sinusitis, otitis media;• lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including those caused by atypical pathogens;• skin and soft tissue infections: erysipelas, impetigo, secondary infected dermatoses;• The initial stage of Lyme disease (borreliosis)is erythema migrans.

Use during pregnancy and lactation

PregnancyDuring pregnancy, azithromycin is used only if the intended benefit to the mother exceeds the potential risk to the fetus.

Breast-feeding periodDuring breastfeeding, it is used only if the intended benefit to the mother exceeds the potential risk to the child. If it is necessary to use azithromycin during breastfeeding, it is recommended to suspend breastfeeding.

Contraindications

• hypersensitivity to azithromycin (including to other macrolides) or other components of the drug;
• severe renal insufficiency (creatinine clearance (CC) of less than 40 ml/min);
• severe liver failure (class C child-Pugh);
• breastfeeding;
• concomitant use with ergotamine and dihydroergotamine;
• children up to age 6 months;
• deficiency of sucrase/isomaltase, fructose intolerance, glucose-galactose malabsorption;
• hypersensitivity to erythromycin; ketolides.

With cautionPregnancy, myasthenia gravis, mild to moderate hepatic impairment, mild to moderate renal impairment (creatinine clearance greater than 40 ml / min), diabetes mellitus, in patients with proarrhythmogenic factors (especially in elderly patients): patients with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with impaired water-electrolyte balance balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of digoxin, warfarin, cyclosporine.

Side effects

Infectious and parasitic diseasesinfrequently: candidiasis, including oral mucosa, vaginal infection, pneumonia, fungal infection, bacterial infection, pharyngitis, gastroenteritis, respiratory diseases, rhinitis Unknown frequency: pseudomembranous colitisDisorders of the blood and lymphatic systeminfrequently: leukopenia, neutropenia, eosinophilia very rarely: thrombocytopenia, hemolytic anemiaMetabolic and nutritionaldisorders infrequently: anorexiaImmune system disordersare uncommon: angioedema, hypersensitivity reactionnotable frequency: anaphylactic reactionNervous system disorderscommon: headache frequent: dizziness, impaired taste, paresthesia, drowsiness, insomnia, nervousness Rare: agitation Unknown frequency: hypesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of sense of smell, perverted sense of smell, loss of taste, myasthenia gravis, delusions, hallucinationsDisorders of the visual organoften: visual impairmentHearing disorders and labyrinthine disordersuncommon: hearing disorder, vertigone Known frequency: hearing impairment, including deafness and / or tinnitusDisorders of the cardiovascular systeminfrequently: palpitation sensation very rare: arrhythmiaunknown frequency: increased QT interval on the electrocardiogram, pirouette-type arrhythmia, ventricular tachycardiaVascular disordersinfrequently: “hot flashes” of blood to the face unknown frequency: low blood pressureRespiratory, thoracic and mediastinal disorders often: shortness of breath, nosebleedsGastrointestinal disordersvery common: diarrhoea often: nausea, vomiting, abdominal pain often: flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased salivary gland secretion Very rare: discoloration of the tongue, pancreatitisLiver and biliary tractdisorders infrequently: hepatitis rare: impaired liver function, cholestatic jaundice Known frequency: liver failure (in rare cases-with a fatal outcome, mainly against the background of severe liver dysfunction); liver necrosis, fulminant hepatitisSkin and subcutaneous tissue disordersUncommon: skin rash, pruritus, urticaria, dermatitis, dry skin, sweating Rare: photosensitization reactionnotable frequency: Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS-syndrome)Musculoskeletal and connective tissuedisorders uncommon: osteoarthritis, myalgia, back pain, neck painnotable frequency: arthralgiaRenal and urinary tractdisorders uncommon: dysuria, renal painnotable frequency: interstitial nephritis, acute renal failureGenital and breast disordersinfrequently: metrorrhagia, testicular dysfunctionGeneral disorders and disorders at the injectionsite infrequently: edema, asthenia, malaise, fatigue, facial edema, chest pain, fever, peripheral edemaThe impact on the results of laboratory and instrumental studiesis often: decrease in the number of lymphocytes, increase in the number of eosinophils, increase in the number of basophils, increase in the number of monocytes, increase in the number of neutrophils, decrease in the concentration of bicarbonates in blood plasma frequently: the increase in the activity of aspartate aminotransferase, alanine aminotransferase, increased concentration of bilirubin in blood plasma, increasing the concentration of urea in blood plasma, increasing the concentration of creatinine in the blood plasma, a change in the content of potassium in the blood plasma, increased activity of alkaline phosphatase in blood plasma, increasing the chloride content in blood plasma, increasing the concentration of glucose in the blood, increasing the number of platelets, decrease in hematocrit, an increase in the concentration of bicarbonate in the blood plasma, changes in the sodium content of the blood plasma

Interaction

Antacids (containing aluminum and magnesium) they do not affect bioavailability, but reduce the concentration of azithromycin in the blood by 30%, so the interval between their intake should be 1 hour before or 2 hours after taking these drugs.

When used simultaneously with derivatives of ergotamine and dihydroergotamine, it is possible to increase the toxic effect of the latter (vasospasm, dysesthesia).

When co-administered with coumarin-type indirect anticoagulants (warfarin), patients should be carefully monitored for prothrombin time.

Caution should be exercised when co-prescribing terfenadine and azithromycin, as simultaneous use of terfenadine and macrolides has been found to cause arrhythmia and prolongation of the Q-T interval. Based on this, the above-mentioned complications cannot be excluded when taking terfenadine and azithromycin together.

When used concomitantly with cyclosporine, it is necessary to monitor the concentration of cyclosporine in the blood. When azithromycin and cyclosporine are co-administered, a dose adjustment of cyclosporine is necessary. When used concomitantly with digoxin, it is necessary to control the concentration of digoxin in the blood (it is possible to increase the absorption of digoxin in the intestine). Concomitant use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the steady-state concentration of azithromycin in blood plasma, no clinically significant side effects were observed, and dose adjustment of azithromycin with its simultaneous use with nelfinavir is not required.

When co-administered with zidovudine, azithromycin has little effect on the pharmacokinetics, including renal excretion, of zidovudine or its glucuronide metabolite. Azithromycin weakly interacts with cytochrome P 450 isoenzymes, azithromycin was not found to participate in pharmacokinetic interactions similar to erythromycin and other macrolides, azithromycin is not an inducer or inhibitor of the cytochrome P 450 isoenzyme.

Neutropenia has sometimes been observed with concomitant use of azithromycin and rifabutin, although neutropenia has been 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.

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 the blood when used simultaneously.

There have been isolated reports of rhabdomyolysis in patients taking concomitant azithromycin and statins.

How to take, course of use and dosage

Inside (the method of application is determined by the form of release),1 time a day,1 hour before or 2 hours after meals. After taking the drug, the child must be offered to drink a few sips of water so that he can swallow the remains of the suspension. Before each dose of the drug, it must be thoroughly shaken until a homogeneous suspension is obtained. If the required volume of suspension has not been selected within 20 minutes after shaking, the suspension should be shaken again, the required volume should be selected and given to the child. For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissuesBased on 10 mg / kg of body weight once a day for 3 days (a course dose of 30 mg / kg).

The table below should be used for accurate dosing of azithromycin according to the child’s body weight.

Body weight, kg Dose of azithromycin, mg (the amount of suspension 200 mg/5 ml, ml) for 1 admission

10-14 kg 100 mg of azithromycin (2.5 ml suspension)15-24 kg 200 mg of azithromycin (5.0 ml suspension)25-34 kg 300 mg of azithromycin (7.5 ml suspension)35-44 kg 400 mg of azithromycin (10.0 ml suspension)at least 45 kg of 500 mg azithromycin (12.5 ml suspension) (corresponds to the dose for adult patients)

Children weighing less than 10 kg should take azithromycin in powder form to prepare an oral suspension with a concentration of 100 mg/5 ml. The table below should be used for accurate dosing of azithromycin according to the child’s body weight.

Body weight, kg Azithromycin dose, mg (suspension volume 100 mg/5 ml, ml) per 1 dose

5 50 mg azithromycin (2.5 ml suspension)660 mg of azithromycin (3.0 ml suspension)770 mg of azithromycin (3.5 ml suspension)8 80 mg of azithromycin (4.0 ml suspension)9 90 mg of azithromycin (4.5 ml suspension)10,100 mg of azithromycin (5 ml suspension)

For pharyngitis / tonsillitiscaused by Streptococcus pyogenes, azithromycin is used at a dose of 20 mg / kg / day for 3 days (a course dose of 60 mg / kg). The maximum daily dose is 500 mg. Lyme disease (initial stage of borreliosis) – erythema migrans On day 1 at a dose of 20 mg / kg / day, then from day 2 to day 5 at a dose of 10 mg / kg/day (a course dose of 60 mg / kg). With impaired renal functionIn patients with GFR (glomerular filtration rate) of 10-80 ml/min, no dose adjustment is required. With impaired liver functionWhen used in patients with mild to moderate hepatic impairment, no dose adjustment is required. Elderly patientsNo dose adjustment is required. In elderly patients, special care should be taken when using azithromycin due to the possible presence of proarrhythmogenic factors that may increase the risk of developing cardiac arrhythmia and arrhythmia of the “pirouette”type.

Suspension preparation methodThe suspension is prepared immediately before use. The powder in the vial is pre-shaken, add 12 ml of boiled and cooled to room temperature water, using a syringe for dosing, mix to obtain a homogeneous suspension. For accurate dosage of the suspension, you should use a syringe, which should be rinsed well with water after each application. After dilution, the finished suspension should be stored for no more than 5 days in the refrigerator, but not frozen. When used in patients with mild to moderate renal impairment, no dose adjustment is required; when used in patients with mild to moderate hepatic impairment, no dose adjustment is required in elderly patients.

Overdose

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

Treatment is symptomatic.

Description

White or yellowish-white powder with a faint fruity smell. Finished suspension: white to light yellow in color, homogeneous with a faint fruity smell.

Special instructions

If one dose of azithromycin is missed, the missed dose should be taken as early as possible, and subsequent doses should be taken at intervals of 24 hours. Azithromycin should be taken at least one hour before or two hours after taking antacids. Azithromycin should be used with caution in patients with mild to moderate hepatic impairment due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency. In the presence of symptoms of impaired liver function, such as rapidly increasing asthenia, jaundice, darkening of the urine, tendency to bleeding, hepatic encephalopathy, azithromycin therapy should be discontinued and a study of the functional state of the liver should be conducted. With impaired renal function: in patients with GFR (glomerular filtration rate) of 10-80 ml/min, no dose adjustment is required, azithromycin therapy should be carried out with caution under the control of renal function, as with other antibacterial drugs, patients with azithromycin therapy should be regularly examined for the presence of non-susceptible microorganisms and signs of superinfections, including fungal ones. Azithromycin should not be used for longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.There are no data on a possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but due to the development of ergotism with the simultaneous use of macrolides with derivatives of ergotamine and dihydroergotamine, this combination is contraindicated. With prolonged use of azithromycin, pseudomembranous colitis caused by Clostridium difficile may develop, both in the form of mild diarrhea and severe colitis. If antibiotic-associated diarrhea develops while taking azithromycin, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. Do not use drugs that inhibit intestinal motility. Macrolide treatment, including azithromycin, has been associated with prolonged cardiac repolarization and QT interval, which increases the risk of cardiac arrhythmias, including pirouette-type arrhythmias that can lead to cardiac arrest. Caution should be exercised when using azithromycin in patients with proarrhythmogenic factors (especially in elderly patients), including those with congenital or acquired QT prolongation, in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with impaired water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure. The use of azithromycin can provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Influence on the ability to drive vehicles and mechanismsDuring the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Powder for preparing a suspension for oral use of 100 mg/5 ml,200 mg/5 ml. 16.5 g each in dark glass vials with a capacity of 60 ml with a screw-on plastic lid with a silica gel insert. 1 bottle together with a syringe for dosing and instructions for use is placed in a pack of cardboard.

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 °C. The finished suspension is stored at a temperature of 2 ° C to 8 ° C in a tightly closed bottle. Keep out of reach of children.

Shelf

life is 2 years. The finished suspension lasts for 5 days. Do not use after the expiration date.

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 6 months of age

Indications

Bronchitis, Sinusitis, Tonsillitis, Chlamydia, Pneumonia, Pharyngitis, Urinary Tract Infections, Respiratory Tract Infections, Pneumonia, Sore Throat, Infectious Diseases, Sinusitis, Skin Infections, Otitis Media, Urethritis