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

Excipients: cellulose microcrystalline 225.9 mg, crospovidone 60.3 mg, pregelatinized starch 67.0, blackcurrant flavor 5.0 mg, magnesium stearate 6.0 mg, sodium saccharinate 15.0 mg, vanillin 1.5 mg, silicon dioxide colloidal 24 , 0 mg.

Description:Tablets of an oval biconvex form with a risk on one side, with the smell of vanillin and black currant. The surface of the tablets is white or white with a beige shade of color, with slight impregnations from beige to light brown.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Azithromycin is a macrolide antibiotic of the azalide group.Reversibly binding to the 508 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.

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.

Moderately sensitive or insensitive: aerobic Gram-positive microorganisms - Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).

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 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 plasma, and in the focus of infection - 24-34% more than in healthy tissues. Slowly removed from the tissues and has 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, 12% 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:

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

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

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

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

5) Uncomplicated urinary tract infections caused by Chlamidia trachomatis (urethritis, cervicitis).

Contraindications:

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

Carefully:

The syndrome of an elongated interval Q-T, chronic renal failure (CC greater than 40 ml / min), hepatic insufficiency (class A on the Child-Pugh scale), myasthenia gravis, simultaneous administration with terfenadine, warfarin, digoxin, drugs extending the interval Q-T.

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 (2 tablets) 1 time per day for 3 days (course dose 1.5 g)

The initial stage of Lyme disease:

1 time per day for 5 days: 1st day - 1.0 g (4 tablets), then from 2 to 5 days - 500 mg (2 tablets) (course dose 3.0 g)

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

1 g (4 tablets) once.

With acne:

the course dose is 6 g: 500 mg (2 tablets) once a day for 3 days, then 500 mg once a week for 9 weeks.

Children from 6 months to 12 years.

With infections of the 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).

With streptococcal pharyngitis:

At the rate of 10-20 mg / kg once a day for 3 days.

The initial stage of Lyme disease:

On the 1st day - at a dose of 20 mg / kg of body weight and then from 2 to 5 days - daily at a dose of 10 mg / kg of body weight (exchange dose of 60 mg / kg).

The appointment of patients with impaired renal function:

For patients with moderate impairment of kidney function (CK> 40 ml / min) dose adjustment is not needed.

Dispersible tablets can be taken in various ways; The tablet can be swallowed whole, washed down with water or beforehand, before taking it, dissolved in water. Tablets should be dissolved in at least 50 ml of water. Before taking, carefully mix the resulting suspension.

Side effects:

From the hematopoiesis: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, transient neutropenia, hemolytic anemia.

From the side of the nervous system, dizziness, vertigo, drowsiness, headache, seizures, paresthesia, hyposthenia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, anxiety, nervousness.

From the sense organs: hearing impairment, deafness, ringing in the ears, distortion of taste or smell, decreased visual acuity.

From the side of the cardiovascular system: palpitation, lowering of arterial pressure, arrhythmia (including ventricular tachycardia, pirouette tachycardia), lengthening of the interval Q-T.

From the digestive systemnausea, vomiting, diarrhea, abdominal pain or abdominal cramps, unformed stool, flatulence, digestive disorders, gastritis, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, hepatitis, cholestatic jaundice, impaired functional liver tests, liver necrosis and liver failure (up to the lethal outcome), pancreatitis, fulminant hepatitis.

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

From the side of the musculoskeletal system: arthralgia.

From the genitourinary system: vaginitis, interstitial nephritis, acute renal failure.

Laboratory indicators: increased serum levels of bilirubin, urea, creatinine, potassium ions, decreased serum bicarbonate concentrations.

Other: candidiasis, chest pain, peripheral edema, fainting, myasthenia exacerbation gravis, malaise, hyperglycemia.

Overdose:

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

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

Interaction:

Antacids reduce the maximum concentration of azithromycin by 30%, so azithromycin should be taken 1 hour before or 2 hours after taking antacids.

The possibility of inhibiting the isoenzyme should be considered CYP3A4 azithromycin with the simultaneous use of cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism occurs with the participation of this isoenzyme.

When used simultaneously with cyclosporine, the concentration of cyclosporin in the blood should be monitored.

When used simultaneously with indirect anticoagulants, the frequency of bleeding may increase, prothrombin time and the international normalized ratio (MNO) should be monitored.

With simultaneous use with digoxin, an increase in the concentration in the blood of the latter, therefore, the concentration of digoxin in the blood should be monitored.

With simultaneous use with ergotamine, ergotism can develop; simultaneous use is not recommended.

Care must be taken when using terfinadine and azithromycin concomitantly, since it has been established that simultaneous administration of terfinadine and macrolides causes arrhythmia and lengthening Q-T interval. Proceeding from this, it is impossible to exclude the aforementioned complications in the joint administration of azithromycin and terfenadine.

At simultaneous application with neofinavir it is possible to increase the incidence of adverse reactions of azithromycin (decrease in hearing, increase in activity of "liver" transaminases).

Azithromycin increases the content of zidovudine triphosphate (an active metabolite of zidovudine) in mononuclear cells, the clinical significance of this phenomenon is unknown.

Simultaneous use with rifabutin can lead to neutropenia.

Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin, methylprednisolone in the blood with simultaneous application.

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.

With pharyngitis and tonsillitis caused by Streptococcus pyogenes, antibiotics of choice are penicillins. The effectiveness of azithromycin for the prevention of rheumatic fever is unknown.

Take with caution patients with liver failure (class A on the Child-Pugh scale) because of the possibility of developing fulminant hepatitis and severe hepatic insufficiency in such patients. In the presence of symptoms of liver dysfunction (rapidly increasing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy) therapy with azithromycin should be discontinued and an examination of the functional state of the liver should be carried out.

With renal failure (CC greater than 40 ml / min), azithromycin should be administered under the control of kidney function.

With the use of azithromycin, as well as with the use of other antibiotics, there is a risk of developing superinfection (including fungal).

With prolonged use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile. 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.In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole is indicated. Do not use drugs that inhibit the intestinal motility.

Since it is possible to extend the interval Q-T in patients receiving macrolides, including azithromycin, with the use of azithromycin, caution should be exercised in patients with known risk factors for lengthening the interval Q-T: old age, electrolyte balance disorder (hypokalemia, hypomagnesemia), congenital lengthening interval syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), simultaneous use of drugs capable of lengthening the interval Q-T (including antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, fluoroquinolones).

With the use of azithromycin, the development of myasthenic syndrome or myasthenia exacerbation is possible.

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 250 mg.

Packaging:For 3, 6 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. By 6, 18, 24, 30, 36, 48, 60 or 100 tablets in cans of polymeric 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:

Store in a dry, 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 the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001161

Date of registration:11.11.2011

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

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Sumatrolide Solidshn Tablets (Sumatrolid Solution Tablets)