Sumatrolide Soluxtion Tablets - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline - 112.95 mg, pregelatinized starch - 33.50 mg, crospovidone - 30.15 mg, silicon dioxide colloid - 12.00 mg, sodium saccharinate - 7.50 mg, magnesium stearate - 3.00 mg, black currant flavor - 2.50 mg, vanillin 0.75 mg.

Composition per 1 tablet 500 mg:

Active substance: azithromycin dihydrate - 530,60 mg, in terms of azithromycin - 500 mg.

Excipients: cellulose microcrystalline - 451.80 mg, pregelatinized starch - 134.00 mg, crospovidone - 120.60 mg, silicon dioxide colloid - 48.00 mg, sodium saccharate - 30.00 mg, magnesium stearate - 12.00 mg, black currant flavor - 10,00 mg, vanillin - 3,00 mg.

Description:Oval biconvex tablets white or white with a beige shade of color,with minor impregnations from beige to light brown, with a risk on one side; with a characteristic odor.

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. Reversibly communicating with 50S subunit of ribosomes of bacterial cells, disrupts the translocation of the growing polypeptide chain from the aminoacyl region to the peptidyl, which leads to suppression of protein synthesis in bacterial cells, 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 may initially be resistant to the action of the antibiotic or may acquire resistance to it.

Sensitive: aerobic Gram-positive microorganisms - Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Streptococcus groups A, B, C, G; 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.; other - 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 strains).

Stable: aerobic Gram-positive microorganisms - Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant); anaerobes: group Bacteroides fragilis. Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains), resistant to erythromycin and other macrolides, and lincosamides are resistant to azithromycin.

Pharmacokinetics:

After oral administration, the bioavailability is 37%, the maximum concentration in the blood plasma (Cmax) is created in 2-3 hours, the volume of distribution is 31 l / kg. Binding to plasma proteins is inversely 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, polymorphically nuclear 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 the blood plasma, and in the focus of infection - 24-34% more than in healthy tissues. Slowly removed from tissues and possesses a long half-life of 2-4 days. 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. In patients with renal insufficiency (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 respiratory tract and ENT organs (pharyngitis, tonsillitis, sinusitis, otitis media);

- Infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia, including caused by atypical pathogens);

- Infections of the skin and soft tissues (acne vulgaris of medium severity, erysipelas, impetigo, secondarily infected dermatoses);

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

- Uncomplicated urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications:

Hypersensitivity to azithromycin, erythromycin, other macrolides or ketolides, or other components of the drug; simultaneous use with ergotamine and dihydroergotamine, severe hepatic insufficiency (class C on the Child-Pugh scale). Severe renal failure (CC less than 40 ml / min). Children up to 6 months.

Carefully:

Myasthenia gravis; impaired liver function of mild and moderate severity; disturbance of renal function of mild and moderate severity (QC more than 40 ml / min); arrhythmia, in the presence of proarrhythmogenic factors (especially in elderly patients), including congenital or acquired lengthening of the interval QT: in patients receiving therapy with antiarrhythmic drugs classes IA (quinidine, procainamide), III (dofetil, amiodarone, sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), in patients with disturbed water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia,clinically significant bradycardia, severe heart failure; simultaneous use of warfarin, digoxin, cyclosporine.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside, 1 time per day, at least 1 hour before or 2 hours after meals.

Adults (including the elderly) and children over 12 years of age with a body weight of over 45 kg.

With infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues:

500 mg once a day for 3 days (course dose of 1.5 g)

The initial stage of Lyme disease:

1 time per day in the treatment of 5 days: 1st day - 1.0 g, then from 2 to 5 days - 500 mg (course dose 3.0 g)

In uncomplicated infections of the genitourinary tract caused by Chlamydia trachomatis (urethritis, cervicitis):

1 g once.

Acne vulgaris of medium severity:

course dose 6_;0 g: 500 mg once a day for 3 days, then 500 mg once a week for 9 weeks.The first weekly tablet should be taken 7 days after taking the first daily tablet (the 8th day from the start of treatment), the subsequent 8 weekly tablets - with an interval of 7 days.

Children aged 6 months to 12 years with a body weight of less than 45 kg.

With 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).

For the convenience of dosing, it is recommended to use the table number 1.

Table No. 1

Body mass	The dose of azithromycin in tablets 125 mg
10-17 kg	1 tablet (125 mg of azithromycin)
18-30 kg	2 tablets (250 mg of azithromycin)
31-44 kg	3 tablets (375 mg of azithromycin)
not less than 45 kg	apply doses recommended for adults

With pharyngitis / tonsillitis caused by Streptococcus pyogenes:

At the rate of 20 mg / kg once a 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:

At 20 mg / kg body weight 1 time per day on the 1st day, then at the rate of 10 mg / kg 1 time per day from 2 to 5 days.

The appointment of patients with impaired renal function:

For patients with mild to moderate severity of renal dysfunction (CK> 40 ml / min), dose adjustment is not necessary.

If there is a violation of the liver: if the liver function of mild and moderate severity, dose adjustment is not required.

Elderly patients: correction of the dose is not required. Since older people may have proarrhythmogenic conditions, caution should be exercised when using the drug, due to the high risk of developing cardiac arrhythmias, including pirouette-type arrhythmias.

Dispersible tablets can be taken in various ways: the tablet can be swallowed whole by washing with water or beforehand, before taking it, dissolve boiling room temperature in water. One tablet should be dissolved in 15 ml of water, 2-3 tablets in 30 ml of water. Before taking, carefully mix the resulting suspension.

Side effects:

Infectious diseases: candidiasis, including oral and genital mucosa, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis, pseudomembranous colitis.

On the part of the blood and lymphatic system: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, transient neutropenia, hemolytic anemia, basophilia, monocytosis, an increase in the number of neutrophils.

Allergic reactions: hypersensitivity reactions.

From the nervous system: dizziness, vertigo, drowsiness, headache, seizures, paresthesia, hyposthenia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, anxiety, nervousness, hypoesthesia, agitation, fainting, delirium, hallucinations.

From the sense organs: hearing impairment, deafness, ringing in the ears, perversion of taste or smell, impaired vision, disruption of taste, loss of smell (or anosmia) and taste sensations.

From the cardiovascular system: a feeling of heartbeat, lowering of arterial pressure, arrhythmia (including ventricular tachycardia, arrhythmia of the "pirouette" type), "tides" of blood to the face, lengthening of the interval QT on an electrocardiogram.

From the side of the digestive system, dysphagia, bloating, dryness of the oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands, nausea, vomiting, diarrhea, abdominal pain or cramps in the abdomen, flatulence, digestive disorders, gastritis, anorexia, constipation, discoloration language, hepatitis, cholestatic jaundice, increased activity of "liver" transaminases,liver necrosis and hepatic insufficiency (up to a lethal outcome), pancreatitis, impaired liver function, fulminant hepatitis.

From the respiratory system: shortness of breath, nosebleed.

From the skin: itching and rash, angioedema, hives, dermatitis, dry skin, sweating, photosensitization, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactic reactions.

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

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

From the genitals and mammary glands: metrorrhagia, dysfunction of testicles.

Laboratory indicators: increased serum levels of bilirubin, urea, creatinine, a change in the potassium concentration in the blood plasma, increased activity of alkaline phosphatase, an increase in the concentration of chlorine in the blood plasma, an increase in the number of platelets, an increase in hematocrit, an increase or decrease concentration of bicarbonates and changes in the concentration of sodium in the blood plasma.

Other: pain in the chest, peripheral edema, exacerbation of myasthenia gravis, malaise, hyperglycemia, fatigue, face swelling, fever.

Overdose:

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

Treatment: reception of activated carbon, maintenance of vital body functions.

Interaction:

Antacid preparations do not affect the bioavailability of azithromycin, but reduce the maximum concentration of azithromycin by 30%, so azithromycin should be taken 1 hour before or 2 hours after taking antacids.

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

Didanosine: simultaneous use of azithromycin (1200 mg / day) and didanosine (400 mg / day) in 6 HIV-infected patients showed no changes in the pharmacokinetic indices of didanosine compared with the placebo group.

Digoxin: simultaneous application of macrolide antibacterial drugs, including azithromycin, with substrates of P-glycoprotein, such as digoxin, leads to an increase in the concentration of the P-glycoprotein substrate in the blood plasma. Thus, with the simultaneous use of digoxin and azithromycin, it is necessary to consider the possibility of increasing the concentration of digoxin in the blood plasma.

Zidovudine: simultaneous use of azithromycin (a single dose of 1000 mg and repeated administration of 1200 mg or 600 mg) has little effect on the pharmacokinetics, including kidney excretion, zidovudine or its glucuronide metabolite. Nevertheless, the concentration of the active metabolite - phosphorylated zidovudine - increases 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: taking into account the theoretical possibility of developmentergotism. simultaneous use of azithromycin with derivatives of ergot alkaloids (ergotamine, dihydroergotamine) 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: simultaneous use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in the concentration of atorvastatin in the blood plasma (based on the inhibition of GMK-CoA reductase). However, reports were received of cases of rhabdomyolysis in patients receiving concomitantly azithromycin and statins.

Carbamazepine: in pharmacokinetic studies involving healthy Volunteers showed no significant effect on the concentration of carbamazepine and its active metabolite in blood plasma when used simultaneously with azithromycin.

Cimetidine: in pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were observed, provided cimetidine was administered 2 hours before azithromycin. Anticoagulants of indirect action (coumarin derivatives): in pharmacokinetic studies azithromycin did not affect the anticoagulant effect of warfarin in a single dose of 15 mg, taken by healthy volunteers. Potential anticoagulant effect was reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Despite the fact that a causal relationship has not been established, it is recommended to carefully monitor prothrombin time in patients, while using azithromycin and indirect anticoagulants (coumarin derivatives).

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

Efavirenz: simultaneous use of azithromycin (600 mg 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 half-life did not change with the simultaneous use of fluconazole, however, a decrease in the maximum concentration of azithromycin by 18% was noted, which was not clinically significant.

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

Methylprednisolone: azithromycin does not significantly affect pharmacokinetics of methylprednisolone.

Nelfinavir: simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg three times a day) causes an increase in the equilibrium concentrations 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.

Rifabutin: simultaneous use of azithromycin and rifabutin does not affect the concentration of each of the drugs in the blood plasma. 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, no evidence of the effect of azithromycin (500 mg / day daily for 3 days) on the maximum concentration in the blood plasma and the area under the concentration-time curve of sildenafil and its main metabolite was not obtained.

Terfenadine: in pharmacokinetic studies there was no evidence of interaction between azithromycin and terfenadine. Individual cases were reported where the possibility of such interaction could not be completely excluded, but there was no specific evidence that such an interaction took place. It was found that the simultaneous use of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening of the interval QT.

Theophylline: the interaction between azithromycin and theophylline has not been identified.

Triazolam / midazolam: no significant changes in pharmacokinetic parameters were observed with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses.

Trimethoprim / sulfamethoxazole: simultaneous application trimethoprim / sulfamethoxazole with azithromycin showed no significant effect on the maximum concentration, total exposure or excretion of trimethoprim or sulfamethoxazole by the kidneys. The concentration of azithromycin in the blood plasma was consistent with that found in other studies.

Special instructions:

If you miss a dose of the drug - the missed dose should be taken as soon as possible, and the next - with interruptions of 24 hours.

The drug should be taken at least 1 hour before or 2 hours after taking antacid medications.

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

In the presence of symptoms of impaired liver function, such as rapidly accruing asthenia, jaundice,darkening of the urine, a tendency to bleeding, hepatic encephalopathy, drug therapy should be discontinued and an examination of the functional state of the liver should be carried out.

For violations of kidney function of mild and moderate severity (QC more than 40 ml / min), the drug should be administered 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, the drug should be regularly monitored for susceptible microorganisms and signs of development of superinfection, including fungal ones.

The drug 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 convenient dosage regimen.

There is no evidence of a possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but due to the development of ergotism with simultaneous application of macrolides with derivatives of ergotamine and dihydroergotamine given the combination is contraindicated.

With long-term use of the drug may develop pseudomembranous colitis, caused by Clostridium difficile, both in the form of mild diarrhea, and severe colitis. When the development of diarrhea against the background of taking azithromycin, and also 2 months after the end therapy, clostridial pseudomembranous colitis should be excluded. In the lungs cases it is sufficient to abolish azithromycin and use ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole. You can not use drugs that inhibit intestinal motility.

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

The use of azithromycin may provoke the development of a myasthenic syndrome or cause an exacerbation of myasthenia gravis.

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

In case of adverse reactions from the nervous system, patients are advised to refrain from controlling the car and other mechanisms, as well as to be cautious when engaging in activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets are dispersible 125 mg, 500 mg.

Packaging:

By 3, 6, 10 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered.

By 3, 6, 9, 12, 15, 18, 20, 24, 30, 40, 50, 60 or 100 tablets in cans of polyethylene terephthalate or polymer cans made of polypropylene for medicines.

One jar or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002802

Date of registration:29.12.2014

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Sumatrolide Solidshn Tablets (Sumatrolid Solution Tablets)