Active substanceAzithromycinAzithromycin
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  • Dosage form: & nbspPowder for suspension for oral administration
    Composition:

    1 g of powder for the suspension for oral administration contains: active substance: azithromycin dihydrate * - 25.047 mg, in terms of azithromycin 23.895 mg;

    Excipients: sucrose * 929.753 mg, sodium phosphate 20.00 mg, giprolose 1.60 mg, xanthan gum 1.60 mg, strawberry flavor 10,000 mg, titanium dioxide 5,000 mg, silicon dioxide colloid 7,000 mg.

    * values ​​from the calculation of the theoretical activity of the substance 95.4%; The amount of sucrose can vary depending on the actual activity of azithromycin.

    Description:

    Powder from white to yellowish white with a characteristic smell of strawberries. After dissolution in water, a homogeneous suspension of yellowish-white color with a characteristic smell of strawberry.

    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 - the microbial cells. Communicating with 50Sthe subunit of the ribosome, depresses peptidranslokazu, at the stage of translation and suppresses protein synthesis, slowing the growth and multiplication of bacteria. In high concentrations has a bactericidal effect.

    It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.

    Microorganisms can initially be resistant to the action of an antibiotic or can acquire resistance to it.

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

    Microorganisms

    MIC, mg / l

    Sensitive

    Sustainable

    Staphylococcus

    <1

    >2

    Streptococcus A, B, C, G

    <0,25

    >0,5

    S. pneumoniae

    <0,25

    >0,5

    N. influenzae

    <0,12

    >4

    M. catarrhalis

    <0,5

    >0,5

    N. gonorrhoeae

    <0,25

    >0,5

    In most cases, sensitive microorganisms

    1. Gram-positive aerobes

    Staphylococcus aureus methicillin-sensitive

    Streptococcus pneumoniae penicillin-sensitive

    Streptococcus pyogenes

    2. Gram-negative aerobes

    Haemophilus influenzae

    Haemophilus parainfluenzae

    Legionella pneumophila

    Moraxella catarrhalis

    Pasteurella multocida

    Neisseria gonorrhoeae

    3. Anaerobes

    Clostridium perfringens

    Fusobacterium spp.

    Prevotella spp.

    Porphyriomonas spp.

    4. Other microorganisms

    Chlamydia trachomatis

    Chlamydia pneumoniae

    Chlamydia psittaci

    Mycoplasma pneumoniae

    Mycoplasma hominis

    Borrelia burgdorferi

    Microorganisms that can develop resistance to azithromycin Gram-positive aerobes

    Streptococcus pneumoniae penicillin-resistant

    Initially, resistant microorganisms

    Gram-positive aerobes

    Enterococcus faecalis

    Staphylococci (methicillin-resistant staphylococci with very high frequency have acquired resistance to macrolides)

    Gram-positive bacteria resistant to erythromycin.

    Anaerobes

    Bacteroides fragilis

    Pharmacokinetics:

    After oral administration azithromycin well absorbed and quickly distributed in the body. After a single dose of 500 mg bioavailability is 37% ("first pass" effect), the maximum concentration (0.4 mg / l) in the blood is created after 2-3 hours, the volume of distribution is 31.1 l / kg, protein binding back is proportional to the concentration in the blood and is 7-50%. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes the histohematological barriers and enters the tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection - by 24-34% more than in healthy tissues.

    In azithromycin, a very long half-life is 35-50 hours. The half-life of tissues is much longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is output, basically, in the unchanged form - 50% of the intestine, 6% of the kidneys. In the liver, demethylated, losing activity.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

    Infections of the upper respiratory tract and ENT organs (pharyngitis / tonsillitis, sinusitis, otitis media);

    Infections of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl. caused by atypical pathogens;

    Infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses);

    The initial stage of Lyme disease (borreliosis) - migrating erythema (erythema migrans).

    Contraindications:

    Hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides, or other components of the drug; impaired hepatic function; impaired renal function of severe degree (CC less than 40 ml / min); deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption; children's age up to 6 months; simultaneous reception of ergotamine and dihydroergotamine.

    Carefully:

    Myasthenia gravis; impaired liver function of mild to moderate severity; renal dysfunction of mild and moderate severity (QC more than 40 ml / min); 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), with disturbances of water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia, or severe heart failure; simultaneous use of digoxin, warfarin, cyclosporine, diabetes mellitus.

    Pregnancy and lactation:

    Azithromycin is used in pregnancy only if the benefit to the mother exceeds the possible risk to the fetus.During treatment with Sumamed® medication, breastfeeding is suspended.

    Dosing and Administration:

    Inside, 1 time per day, 1 hour before or 2 hours after meals. After taking Sumamed® the child must necessarily offer to drink a few sips of water so that he can swallow the remains of the suspension.

    Before each intake of the drug, the contents of the vial are shaken carefully until a homogeneous suspension is obtained. If the required volume of the suspension has not been removed from the vial within 20 minutes after shaking, the suspension should be shaken again, take the necessary volume and give the baby.

    The required dose is measured with a syringe for dosing with a 1 ml dividing rate and a nominal suspension capacity of 5 ml (100 mg azithromycin) or a measuring spoon with a nominal slurry capacity of 2.5 ml (50 mg azithromycin) or 5 ml (100 mg azithromycin), nested in a cardboard box together with a bottle.

    After use a syringe (after having disassembled it) and the measuring spoon was washed with running water, dried and stored in a dry place until the next dose of Sumamed®.

    In infections of the upper and lower respiratory tract. ENT-organs, skin and soft tissues

    At the rate of 10 mg / kg body weight 1 time per day for 3 days (course dose 30 mg / kg). To accurately dose Sumamed ® according to the body weight of the child, you should use see the table below.

    Body weight, kg

    The volume of suspension (ml) at 1 reception

    5

    2.5 ml (50 mg of azithromycin)

    6

    3.0 ml (60 mg of azithromycin)

    7

    3.5 ml (70 mg of azithromycin)

    8

    4.0 ml (80 mg)

    9

    4.5 ml (90 mg of azithromycin)

    10

    5 ml (100 mg of azithromycin)

    With pharyngitis / tonsillitis caused by Streptococcus pyogenes, Sumamed® preparation apply at a dose of 20 mg / kg / day for 3 days (exchange dose of 60 mg / kg). The maximum daily dose is 500 mg.

    With Lyme disease (the initial stage of borreliosis) - migratory erythema (erythema migrans): in the first day at a dose of 20 mg / kg / day, then from the 2nd to the 5th day in a dose 10 mg / kg / day (the course dose of 60 mg / kg).

    In case of impaired renal function: when used in patients with impaired renal function of mild and moderate severity (QC more than 40 ml / min) dose adjustment is not required.

    If the function is disturbed, bake, when used in patients with impaired liver function of mild to moderate severity, dose adjustment is not required.

    Elderly patients: correction of the dose is not required.

    Method of preparation and snoring of the suspension

    To the contents of the vial, intended for the preparation of 20 ml of suspension (nominal volume), 12 ml of water are added by means of a syringe for dosing. Shake until a homogeneous suspension is obtained. The volume of the resulting suspension is about 25 ml, which exceeds the nominal volume by approximately 5 ml. This is provided for compensation the inevitable loss of the suspension when the drug is dosed. The prepared suspension can be stored at a temperature of no higher than 25 ° C for not more than 5 days.


    Side effects:

    Frequency of side effects classified according to the recommendations of the World Organization health: very often - at least 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%; The unknown frequency can not be estimated from the available data.

    Infectious diseases: infrequently - candidiasis, including oral and genital mucosa, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; an unknown frequency is pseudomembranous colitis.

    From the side of the blood and lymphatic system: infrequently - leukopenia, neutropenia, eosinophilia; very rarely - thrombocytopenia, hemolytic anemia.

    From the side of metabolism and nutrition: infrequently - anorexia.

    Allergic reactions: infrequently - angioedema, hypersensitivity reaction; unknown frequency - anaphylactic reaction.

    From the nervous system: often - headache; infrequently - dizziness, dyspnoea, paresthesia, drowsiness, insomnia, nervousness; rarely - agitation; unknown frequency - hypesthesia, anxiety, aggression, fainting, seizures, psychomotor hyperactivity, loss of smell, perverted sense of smell, loss of taste sensations, myasthenia gravis, delirium, hallucinations.

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

    From the side of the hearing organ and labyrinthine disorders: infrequently - hearing disorder, vertigo; unknown frequency - hearing impairment, including deafness and / or tinnitus.

    From the cardiovascular system: infrequently - sensation palpitation, "tides" of blood to the face; unknown frequency - lowering blood pressure, increasing the interval QT on the electrocardiogram, arrhythmia of the type "pirouette", ventricular tachycardia.

    From the respiratory system: infrequently - shortness of breath, nosebleed.

    From the gastrointestinal tract: very often diarrhea; often - nausea, vomiting, abdominal pain; infrequent - meteorism, dyspepsia, constipation, gastritis, dysphagia, bloating, dryness of the oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - a discoloration of the tongue, pancreatitis.

    From the liver and bile ducts: infrequently - hepatitis; rarely - Mr.the destruction of liver function, cholestatic jaundice; unknown frequency - hepatic insufficiency (in rare cases with a fatal outcome mainly on the background of a serious violation liver function); liver necrosis, fulminant hepatitis.

    From the skin and subcutaneous tissues: infrequently - skin rash, itching, hives, dermatitis, dry skin, sweating; rarely the reaction of photosensitization; unknown frequency - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.

    From the musculoskeletal system: infrequently - osteoarthritis, myalgia, back pain, neck pain; unknown frequency - arthralgia.

    From the side of the kidneys and urinary tract: infrequently - dysuria, pain in the kidney; unknown frequency interstitial nephritis, acute renal failure.

    From the genitals and the breast: infrequently - metrorrhagia, dysfunction of testicles.

    Other: infrequently - asthenia, malaise, fatigue, face swelling, chest pain, fever, peripheral edema.

    Laboratory data: often a decrease in the number of lymphocytes, an increase in the number of eosinophils, an increase in the number of basophils, an increase number of monocytes, increase number of neutrophils, decrease concentration of bicarbonates in the blood plasma; infrequently - increased activity of aspartate aminotransferase, alanine aminotransferase, increased concentration of bilirubin in blood plasma, increased urea concentration in the blood plasma, increased creatinine concentration in the blood plasma, a change in the potassium content in the blood plasma, increased 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, increase in the number platelets, increase of hematocrit, increase of bicarbonate concentration in blood plasma, change of sodium content in blood plasma.

    Overdose:

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

    Treatment: symptomatic.
    Interaction:

    Antacid preparations

    Antacid preparations do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and food.

    Cetirizine

    Simultaneous use of azithromycin with cetirizine (20 mg) in healthy volunteers for 5 days did not lead to pharmacokinetic interaction and significant change the interval QT.

    Didanosine (dideoxyinosine)

    Simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected patients showed no change in the pharmacokinetic indications of didanosine compared with the placebo group.

    Digoxin (substrates of P-glycoprotein)

    Simultaneous use of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates, such as digoxin, leads to an increase in the concentration of substrate P-glycoprotein in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

    Zidovudine

    Simultaneous use of azithromycin (a single dose of 1000 mg and repeated administration of 1200 mg or 600 mg) has a negligible effect on the pharmacokinetics,including the excretion of zidovudine or its glucuronide metabolite by the kidneys. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

    Azithromycin weakly interacts with isoenzymes of the cytochrome P450 system. It was not revealed that azithromycin participates in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin It is not an inhibitor and inducer of cytochrome P450 isoenzymes.

    Alkaloids of ergot

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

    Pharmacokinetic studies of the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of cytochrome P450 isoenzymes have been carried out.

    Atorvastatin

    The simultaneous use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause a change in the concentrations of atorvastatin in the blood plasma (based on the inhibition of GMA-CoA reductase).However, in the post-marketing period, separate reports were received on cases of rhabdomyolysis in patients receiving concomitantly azithromycin and statins.

    Carbamazepine

    In pharmacokinetic studies involving healthy volunteers, no significant effect on the concentration of carbamazepine and its active metabolite in blood plasma in patients receiving concomitantly azithromycin.

    Cimetidine

    In pharmacokinetic studies, the effects of a single dose of cimetidine on pharmacokinetics of azithromycin nc revealed changes in the pharmacokinetics of azithromycin, provided cimetidine is administered 2 hours before azithromycin.

    Anticoagulants of indirect action (coumarin derivatives)

    In pharmacokinetic studies azithromycin did not affect the anticoagulant effect of a single dose of 15 mg of warfarin taken by healthy volunteers. It was reported on the potentiation of anticoagulant effect after simultaneous use of azithromycin and anticoagulants of indirect action (coumarin derivatives). Despite the fact that a causal relationship has not been established, the need for frequent prothrombin time monitoring atthe use of azithromycin in patients who receive oral anticoagulants of indirect action (coumarin derivatives).

    Cyclosporin

    In a pharmacokinetic study involving healthy volunteers who within 3 days were ingested azithromycin (500 mg / day once), and then ciclosporin (10 mg / kg / day once), there was a significant increase in the maximum concentration in the blood plasma (Cmax) and the area under the "concentration-time" curve (AUC0-5) cyclosporine. Care should be taken when using these drugs at the same time. If necessary, simultaneous use of these drugs, it is necessary to monitor the concentration of cyclosporine in the blood plasma and, accordingly, adjust the dose.

    Efavirenz

    Simultaneous application azithromycin (600 mg / day once) and efavirenz (400 mg / day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

    Fluconazole

    Simultaneous use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and the half-life of azithromycin did not change with the simultaneous use of fluconazole, but a decrease in Cmah azithromycin (by 18%), which had no clinical significance.

    Indinavir

    Simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg three times daily for 5 days).

    Methylprednisolone

    Azithromycin does not significantly affect the pharmacokinetics methylprednisolone.

    Nelfinavir

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

    Rifabutin

    Simultaneous use of azithromycin and rifabutin does not affect the concentration of each of the drugs in the blood serum. 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.

    Sildenafil

    When used in healthy volunteers, ns received evidence of the effect of azithromycin (500 mg / day daily in for 3 days) on AUC and Cmah sildenafil or its main circulating metabolite.

    Terfenadine

    In pharmacokinetic studies, no evidence was obtained interactions between azithromycin and terfenadine. It was reported about isolated cases, when the possibility of such interaction could not be excluded completely, but there was no concrete evidence that such an interaction took place.

    It was found that the simultaneous use of terfenadine and macrolides may cause arrhythmia and lengthening of the interval QT.

    Theophylline

    There was no interaction between azithromycin and theophylline.

    Triazolam / midazolam

    Significant changes in pharmacokinetic parameters with the simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses are not revealed.

    Trimethoprim / sulfamethoxazole

    Simultaneous application trimethoprim / sulfamethoxazole with azithromycin did not reveal significant impact on Cmah, total exposure or kidney excretion of trimethoprim or sulfamethoxazole.

    The concentrations of azithromycin in the serum corresponded to those detected in other studies.

    Special instructions:

    When using Sumamed ® in patients with diabetes mellitus, as well as with a low-calorie diet, it is necessary to take into account that the suspension contains sucrose (0.32 XE / 5 ml).

    If you miss a dose of Sumamed ®, the missed dose should be taken as soon as possible, and the subsequent dose should be taken with interruptions of 24 hours. Sumamed ® should be taken at least one hour before or two hours after taking antacid preparations.

    Sumamed ® should be taken with caution in patients with mild to moderate liver function disorder due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency.

    In the presence of symptoms of liver dysfunction, such as rapidly growing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy with Sumamed® should be stopped and a study of the functional state of the liver.

    For violations of kidney function of mild and moderate severity (CC more than 40 ml / min) therapy with Sumamed® should be conducted with caution under the control of the state of kidney function.

    As with the use of other antibacterial drugs, with the treatment with Sumamed®, patients should be regularly monitored for the presence of non-susceptible microorganisms and signs of development of superinfections, including fungal ones. Sumamed ® 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 simple dosing regimen.

    There is no data on the possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but because of the development of ergotism with the simultaneous use of macrolides with derivatives of ergotamine and dihydroergotamine, this combination is not recommended.

    With long-term use of Sumamed®, it is possible to develop pseudomembranous colitis caused by Clostridium difficile, as in the form of mild diarrhea, and severe colitis. In the development of antibiotic-associated diarrhea against the background of taking the drug Sumamed®, and also 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded.

    When treating macrolides, including azithromycin, prolonged cardiac repolarization and interval QT, increasing the risk of developing cardiac arrhythmias, including arrhythmias of the typhoid "pirouette", which can lead to cardiac arrest.

    Caution should be used when using Sumamed® in patients with pro-arrhythmic factors (especially in elderly patients), including congenital or acquired lengthening of the interval QT; in patients taking antiarrhythmic drugs classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances of water-electrolyte balance, especially in case of hypokalemia or hypomagnesemia, clinically significant bradycardia, cardiac arrhythmia or severe heart failure.

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

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

    When unwanted effects develop the sides of the nervous system and the organ of vision should be careful when performing actions that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Powder for the preparation of suspension for ingestion 100 mg / 5 ml.

    Packaging:

    By 20.925 g of powder is put into an opaque white bottle made of high density polyethylene with a volume of 50 ml with polypropylene resistant cover.

    1 bottle together with the instructions for use, a measuring spoon and / or a syringe for dosing is put in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    Powder for the preparation of suspension - 2 years.

    The prepared suspension is 5 days.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N015662 / 03
    Date of registration:15.07.2009
    The owner of the registration certificate:Pliva of Hrvatska dooPliva of Hrvatska doo Croatia
    Manufacturer: & nbsp
    Representation: & nbspPliva of Hvartska dooPliva of Hvartska doo
    Information update date: & nbsp22.09.2015
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