Sumatrolid Solyushn Tablets

General characteristics. Structure:

Active agent: azithromycin a dihydrate of 265,3 mg, in terms of azithromycin of 250,0 mg.

Excipients: cellulose of microcrystallic 225,9 mg, кросповидон 60,3 mg, starch of prezhelatinizirovanny 67,0 mg, fragrance of blackcurrant 5,0 mg, magnesium stearate of 6,0 mg, sodium saccharinate of 15,0 mg, vanillin of 1,5 mg, silicon dioxide of colloid 24,0 mg.

Pharmacological properties:

Pharmacodynamics. Azithromycin - a makrolidny antibiotic of group of azaleads. Reversibly contacting 50v-subunit of ribosomes of bacterial cells, breaks a translocation of the growing polypeptide chain from the aminoacylic site in peptidilny that leads to suppression of synthesis of protein in bacterial cells.
Are sensitive: aerobic gram-positive microorganisms - Staphylococcus aureus (metitsillinchuvstvitelny), Streptococcus
pneumoniae (penitsillinchuvstvitelny), Streptococcus pyogenes, Streptococcus of group 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.; others - Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi. Are moderately sensitive or insensitive: aerobic gram-positive microorganisms - Streptococcus pneumoniae (moderately sensitive or resistant to penicillin). Are steady: aerobic gram-positive microorganisms - Enterococcus faecalis, Staphylococcus spp. (metitsillinustoychivy); anaerobe bacterias: Bacteroides fragilis group.
Streptococcus pneumoniae, beta and hemolitic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including metitsillinustoychivy strains), resistant against erythromycin and other macroleads, linkozamida are steady also against azithromycin.

Pharmacokinetics. After intake bioavailability makes 37%, the maximum concentration in a blood plasma (With max) is created in 2-3 hours, the volume of distribution of-31 l/kg. Linkng with proteins of a blood plasma in inverse proportion to concentration in blood also makes 12-52%. Gets through membranes of cells (it is effective at the infections caused by intracellular activators). It is transported by phagocytes, polymorphonuclear leukocytes and macrophages to the place of an infection where it is released in the presence of bacteria. Easily passes through gistogematichesky barriers and comes to fabrics. Concentration in fabrics and cells 50 times higher, than in a blood plasma, and in the infection center - is 24-34% more, than in healthy fabrics. It is slowly brought out of fabrics and 2-4 days possess a long elimination half-life. Therapeutic concentration of azithromycin remains up to 5-7 days after reception of the last dose. Azithromycin is removed, generally in not changed look - 50% by intestines, 12% kidneys. In a liver it demetilirutsya, losing activity. At patients with a renal failure (the clearance of creatinine (CC) less than 10 ml/min.) the elimination half-life of azithromycin increases by 33%.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to azithromycin:
• Upper respiratory tract infection and ENT organs (pharyngitis, tonsillitis, sinusitis, average otitis);
• Lower respiratory tract infections (an acute bronchitis, an exacerbation of chronic bronchitis, community-acquired pneumonia, including caused by atypical activators);
• Infections of skin and soft tissues (eels ordinary moderate severity, the ugly face, impetigo for the second time infected a dermatosis);
• An initial stage of a disease Laima (borreliosis) - the migrating erythema (erythema migrans);
• The uncomplicated infections of urinogenital ways caused by Chlamidia trachomatis (an urethritis, a cervicitis).

Route of administration and doses:

Inside, 1 time a day, at least, in 1 hour prior to or in 2 hours after food.
The adult (including elderly people) and to children 12 years with body weight over 45 kg are more senior.
At infections of upper and lower respiratory tracts, ENT organs, skin and soft tissues:
500 mg (2 tablets) once a day within 3 days (a course dose of 1,5 g).
Initial stage of a disease of Lyme:
1 time a day within 5 days: the 1st day - 1,0 g (4 tablets), then from the 2nd to the 5th day - on 500 mg (2 tablets) (a course dose of 3,0 g).
At uncomplicated infections of the urinogenital ways caused by Chlamidia trachomatis (an urethritis, a cervicitis): 1 g (4 tablets) once. At acne rash:
the course dose makes 6 g: on 500 mg (2 tablets) once a day within 3 days, then on 500 mg once a week within 9 weeks. To children from 6 months to 12 years.
At respiratory infections, ENT organs, skin and soft tissues:
At the rate of 10 mg/kg of body weight once a day within 3 days (a course dose of 30 mg/kg).
At streptococcal pharyngitis:
At the rate of 10-20 mg/kg of 1 times a day within 3 days.
Initial stage of a disease of Lyme:
In the 1st day - in a dose of 20 mg/kg of body weight and then from 2 to the 5th day - daily in a dose of 10 mg/kg of body weight (a course dose of 60 mg/kg).
Appointment to patients with renal failures:
For patients with moderate renal failures (KK> of 40 ml/min.) dose adjustment is not necessary. The dispersed  pill  can    be taken in various ways: the tablet can be swallowed entirely, washing down with water or previously, before reception, to dissolve in water. Tablets should be dissolved at least in 50 ml of water. Before reception it is necessary to mix carefully formed suspension.

Features of use:

In case of the admission of reception of one dose of drug - it is necessary to accept the passed dose as soon as possible, and the subsequent - with breaks at 24 o'clock. At the pharyngitis and tonsillitis caused by Streptococcus pyogenes, antibiotics of the choice is penicillin. Efficiency of azithromycin for prevention of rheumatic fever is unknown.
To take with caution to patients with a liver failure (a class A on a scale of Chayld-Pyyu) because of a possibility of development of fulminantny hepatitis and a heavy liver failure at such patients. In the presence of symptoms of an abnormal liver function (quickly accruing adynamy, jaundice, urine darkening, tendency to bleedings, hepatic encephalopathy) therapy by azithromycin it is necessary to stop and conduct a research of a functional condition of a liver. At a renal failure (KK more than 40 ml/min.) use of azithromycin should be carried out under control of function of kidneys.
At azithromycin use, also as well as at use of other antibiotics there is a risk of development of superinfection (including fungal). At long reception of azithromycin development of the pseudomembranous colitis caused by Clostridium difficile is possible. At development of diarrhea against the background of azithromycin reception, and also in 2 months after the end of therapy, it is necessary to exclude klostridi-alny pseudomembranous colitis. In mild cases there is enough cancellation of treatment and use of ion-exchange resins (Colestyraminum, колестипол), in hard cases compensation of loss of liquid, electrolytes and protein, purpose of Vancomycinum, bacitracin or metronidazole is shown. It is impossible to apply the medicines braking an intestines peristaltics.
As lengthening of an interval of Q-T at the patients receiving macroleads including azithromycin is possible, at azithromycin use, it is necessary to be careful at patients with the known risk factors of lengthening of an interval of Q-T: advanced age, disturbance of electrolytic balance (a hypopotassemia, a hypomagnesiemia), a syndrome of inborn lengthening of an interval of Q-T, a heart disease (heart failure, a myocardial infarction, bradycardia), a concomitant use of medicines capable to extend Q-T interval (including antiarrhytmic IA and III medicines of classes, tricyclic and tetracyclic antidepressants, neuroleptics, ftorkhinolona). At use of azithromycin development of a myasthenic syndrome or an aggravation of a myasthenia is possible.

INFLUENCE  ON  ABILITY TO MANAGE MOTOR TRANSPORT AND TO WORK WITH MECHANISMS
In case of side reactions from a nervous system patients are recommended to refrain from driving and other mechanisms, and also to be careful at occupation the types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

- From bodies of a hemopoiesis: lymphocytopenia, eosinophilia, leukopenia, thrombocytopenia, tranzitorny neutropenia, hemolitic anemia.
- From a nervous  system:  dizziness, вертиго, drowsiness, headache, spasms, paresthesia, giposteziya, adynamy, sleeplessness, hyperactivity, aggression, concern, alarm, nervousness.
- From sense bodys: a hearing disorder, deafness, a ring in ears, a food faddism or sense of smell, decrease in visual acuity.
- From cardiovascular system: heart consciousness, lowering of arterial pressure, arrhythmia (including ventricular tachycardia, piruetny tachycardia), lengthening of an interval of Q-T.
- From the alimentary system: nausea, vomiting, diarrhea, abdominal pain or spasms in a stomach, not properly executed chair, a meteorism, digestion disturbance, gastritis, anorexia, a lock, language discoloration, pseudomembranous colitis, hepatitis, cholestatic jaundice, disturbance of functional trials of a liver, a necrosis of a liver and a liver failure (up to a lethal outcome), pancreatitis, fulminantny hepatitis.
- From integuments: an itch and rash, a Quincke's disease, a small tortoiseshell, a photosensitization, a mnogoformny erythema, a syndrome Stephen - and - Johnson, a toxic epidermal necrolysis, anaphylactic reactions.
- From a musculoskeletal system: arthralgia.
- From urinogenital system: vaginitis, intersticial nephrite, acute renal failure.
- Laboratory indicators: increase in concentration in blood serum of bilirubin, urea, creatinine, potassium ions, decrease in concentration in blood serum of bicarbonates.
- Other: candidiasis, stethalgia, peripheral hypostases, faints, gravis myasthenia aggravation, indisposition, hyperglycemia.

Interaction with other medicines:

Antacids reduce the maximum concentration of azithromycin by 30% therefore azithromycin should be taken for 1 h to or in 2 h after reception of antacids.
It is necessary to consider a possibility of inhibition of an isoenzyme of CYP3A4 of azithromycin at simultaneous use of cyclosporine, a terfenadin, ergot alkaloids, tsizapridy, Pimozidum, quinidine, astemizoly and other medicines which metabolism happens to participation of this isoenzyme.
At simultaneous use with cyclosporine it is necessary to control concentration of cyclosporine in blood.
At simultaneous use with indirect anticoagulants the frequency of bleedings can increase, it is necessary to control a prothrombin time and the international normalized relation (MHO).
At simultaneous use with digoxin increase in concentration in blood of the last therefore it is necessary to control concentration of digoxin in blood is possible.
At simultaneous use with ergotamine the ergotism can develop; simultaneous use is not recommended.
It is necessary to be careful at combined use of a terfinadin and azithromycin as it was established that the concomitant use of a terfinadin and macroleads causes arrhythmia and lengthening of Q-T of an interval. Proceeding from it, it is impossible to exclude the above-stated complications at joint reception of azithromycin and a terfinadin. At simultaneous use with neofinaviry increase in frequency of side reactions of azithromycin (decrease in hearing, increase in activity of "hepatic" transaminases) is possible. Azithromycin increases the maintenance of a zidovudintrifosfat (an active metabolite of a zidovudine) in mononuclear cells, clinical value of this phenomenon is unknown.
Simultaneous use with rifabutiny can lead to a neutropenia.
Azithromycin does not influence concentration of carbamazepine, Cimetidinum, didanozin, efavirenz, flukonazol,  indinavir,  midazolam,  theophylline, a triazolam, Trimethoprimum/sulfamethoxazole, a tsetirizin, sildenafil, atorvastatin, rifabutin, methyldexamethazone in blood at simultaneous use.

Contraindications:

Hypersensitivity to azithromycin, other macroleads, drug components, simultaneous use with ergot derivatives, a heavy liver failure (a class B and C on a scale of Chayld-Pyyu). Heavy renal failure (KK less than 40 ml/min.). Children's age up to 6 months.

WITH CARE
Syndrome of the extended Q-T interval, chronic renal failure (KK more than 40 ml/min.), a liver failure (a class A on a scale of Chayld-Pyyu), a myasthenia, a concomitant use with terfenadiny, the warfarin, digoxin, medicines extending Q-T interval.

USE AT PREGNANCY AND IN THE PERIOD OF THE LACTATION
Use of drug during pregnancy is possible only when the estimated advantage for mother exceeds potential risk for a fruit. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

Symptoms: temporary hearing loss, nausea and vomiting, diarrhea.
Treatment: reception of absorbent carbon, maintenance of the vital functions of an organism.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets the dispersed 250 mg. On 3, 6 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 6, 18, 24, 30, 36, 48, 60 or 100 tablets in banks polymeric for medicines. To one bank or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 blister strip packagings together with the application instruction place in cardboard packaging (pack).