Tseforal Solyutab

General characteristics. Structure:

Active agent: tsefiksy - 400 mg (in the form of a tsefiksim of trihydrate of 447,7 mg)
Excipients:
cellulose microcrystallic, the hypro rod low-replaced silicon dioxide colloid, povidone, magnesium stearate, saccharinate calcium трисесквигидрат, fragrance strawberry (FA 15757 and PV 4284), "yellow sunset" dye (E110).

Description
Oblong tablet of pale orange color with risky on both parties, with a strawberry smell.

Pharmacological properties:

Pharmacodynamics. Action mechanism. A semi-synthetic antibiotic from group of cephalosporins III of generation for intake. Has bactericidal effect. The mechanism of action is connected with oppression of synthesis of a cell wall of bacteria. Tsefiksim is steady against action (3-laktamaz, produced by many gram-positive and gram-negative bacteria.

Range of antimicrobic activity
In the conditions of clinical practice and in vitro efficiency of a tsefiksim is confirmed at the infections caused by Streptococcus pnewnoniae, Streptococcus pyogenes, Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Proteus mirahilis, Neisseria gonorrhoeae.

Tsefiksim also has activity of in vitro against gram-positive - Streptococcus agalactiae and gram-negative bacteria - Haemophilus paramfluenzae,   Proteus vulgaris,     Klebsiella pneumoniae,      Kiebsiella oxytoca,     Pasteurella multocida, Providencia spp., Salmonella spp., Shigella spp., Citrobacter amatonaticus, Citrobacter diversus.

Pseudomonas spp are steady against drug., Enterococcus spp., Listeria monocytogenes, majority of strains of Enterobacter spp., Staphylococcus spp. (including metitsillinorezistentny strains), Bacteroides fragilis, Clostridium spp.

Pharmacokinetics. Absorption. At intake bioavailability makes 40-50% and does not depend on meal. The maximum concentration in a blood plasma (Cmax) at adults after oral administration in a dose of 400 mg is reached in 3-4 h and makes 2,5-4,9 mkg/ml, after reception in a dose of 200 mg - 1,49-3,25 mkg/ml. Of significant effect does not accord meal on absorption of drug from a GIT.

Distribution
Distribution volume at introduction of 200 mg of a tsefiksim made 6,7 l, at achievement of equilibrium concentration - 16,8 h.p. proteins of plasma about 65% of a tsefiksim communicate. Tsefiksy creates the highest concentration in urine and bile. Tsefiksim gets through a placenta. Concentration of a tsefiksim in blood of an umbilical cord reached 1/6-1/2 concentration of drug in a blood plasma of mother; in breast milk drug is not defined.
Metabolism and removal
The elimination half-life at adults and children makes 3-4 h Tsefiksim is not metabolized in a liver; 50-55% of the accepted dose are removed with urine in not changed look during 24 h. About 10% of a tsefiksim are removed with bile.

Pharmacokinetics in special clinical situations
In the presence at the patient of a renal failure it is possible to expect increase in an elimination half-life and respectively, higher concentration of drug in plasma and delays of its elimination by kidneys.
At patients with clearance of creatinine of 30 ml/min. at reception of 400 mg of a tsefiksim the elimination half-life increases to 7-8 h, the maximum concentration in plasma averages 7,53 mkg/ml, and removal with urine for 24 h - 5,5%.
At patients with cirrhosis the elimination half-life increases up to 6,4 h, time of achievement of the maximum concentration (TCmax) - 5,2 h; at the same time the drug share, элиминирующегося kidneys increases. Cmax and the area under a pharmacokinetic curve does not change.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:
- streptococcal tonsillitis and pharyngitis;
- sinusitis;
- acute bronchitis;
- exacerbation of chronic bronchitis;
- acute average otitis;
- uncomplicated infections of urinary tract;
- uncomplicated gonorrhea;
- shigellosis.

Route of administration and doses:

For adults and children with body weight more than 50 kg the daily dose makes 400 mg in one or two receptions.

To children with the body weight of 25-50 kg drug is appointed in a dose of 200 mg a day in one step.
The tablet can be swallowed, washing down with enough water, or to part in water and to drink the received suspension right after preparation. Drug can be accepted irrespective of meal.

Duration of treatment depends on character of a course of a disease and a type of an infection.
After disappearance of symptoms of an infection and/or fever it is reasonable to continue administration of drug within, at least, 48-72 hours.

The course of treatment at respiratory infections and ENT organs makes 7-14 days.

At a tonzillofaringita, the caused Streptococcus pyogenes, duration of treatment has to be not less than 10 days.

At uncomplicated gonorrhea drug appoint in a dose 400 mg once.

At uncomplicated infections of the lower uric ways at women drug can be appointed within 3-7 days, at the neoput infections of uric ways at women – 14 days.

At uncomplicated infections of upper and lower uric ways at men duration of treatment makes 7-14 days.

At a renal failure the dose is established depending on an indicator of clearance of creatinine in blood serum. At clearance of creatinine of 21-60 ml/min. or at the patients who are on a hemodialysis it is recommended to use other dosage forms of drug due to the need of reduction of a daily dose by 25%. At clearance of creatinine of 20 ml/min. and less or at the patients who are on peritoneal dialysis, the daily dose should be reduced twice.

Features of use:

Due to the possibility of cross allergic reactions with penicillin, it is recommended to estimate the anamnesis of patients carefully. At emergence of allergic reaction use of drug has to be immediately stopped.

At long administration of drug disturbance of normal intestinal microflora is possible that can lead to excess reproduction of Clostridium difficile and development of pseudomembranous colitis. At emergence of easy forms the antibiotic - the associated diarrhea, as a rule, is enough to stop administration of drug. At more severe forms corrective treatment is recommended (for example, purpose of Vancomycinum inside on 250 mg 4 times a day). The antidiarrheal drugs inhibiting motility of a GIT at development of pseudomembranous colitis are contraindicated.

In case of drug use Tseforala Solyutab along with aminoglycosides, polymyxin B, kolistimetaty sodium, "loopback" diuretics (furosemide, Acidum etacrynicum) in high doses it is necessary to control function of kidneys especially carefully. After prolonged treatment by drug Tseforal Solyutab it is necessary to check a condition of function of a hemogenesis.

The dispersed tablets should be dissolved only in water. During treatment false positive forward reaction of Koombs and false positive reaction of urine to glucose when using some test systems for express diagnosis is possible.

Influence on ability to manage vehicles and to work with mechanisms.

Drug influence researches Tseforal Solyutab on ability to manage vehicles and mechanisms were not conducted. Due to the possible adverse effects (for example, dizziness), it is necessary to be careful.

Side effects:

Side effects are classified by the frequency of the registered cases:
Very often: (> 10%); often (1-10%); infrequently (0,1-1%); seldom (0,01-0,1%); very seldom (≤0,01%).

From system of blood and bodies of a hemopoiesis:
Very seldom: tranzitorny leukopenia, agranulocytosis, pancytopenia, thrombocytopenia or eosinophilia. Separate cases of disturbances of a blood coagulation were noted.

Allergic reactions:
Seldom: allergic reactions (for example, urticaria, skin itch).
Very seldom: a Lyell's disease (in this case drug should be cancelled immediately); other allergic reactions connected with a sensitization – medicinal fever, the syndrome reminding a serum disease, hemolitic anemia and intersticial nephrite. At development of an acute anaphylaxis Epinephrinum, system glucocorticosteroids and antihistaminic drugs are entered.

From a nervous system:
Infrequently: headaches, dizziness, dysphoria.

Reactions from the alimentary system:
Often: abdominal pains, digestion disturbances, nausea, vomiting and diarrhea.
Very seldom: pseudomembranous colitis.

From gepatobiliarny system:
Seldom: increase in level of an alkaline phosphatase and transaminases.
Very seldom: separate cases of hepatitis and cholestatic jaundice.

From urinogenital system:
Very seldom: small increase in concentration of creatinine in blood, a hamaturia.

Interaction with other medicines:

Blockers of canalicular secretion (пробенецид, etc.) slow down removal of a tsefiksim through kidneys that can lead to overdose symptoms.
Tsefiksim reduces a prothrombin ratio, strengthens effect of indirect anticoagulants.
At simultaneous use of a tsefiksim with carbamazepine increase in concentration of the last in plasma was observed; in such cases carrying out therapeutic medicinal monitoring is reasonable.

Contraindications:

- hypersensitivity to a tsefiksim or components of drug;
- hypersensitivity to cephalosporins or penicillin;
- less than 25 kg in this dosage form are not recommended for use for children with a chronic renal failure and at children with body weight

With care
Advanced age, renal failure, colitis (in the anamnesis), pregnancy.

Pregnancy and lactation
Drug use Tseforal Solyutab at pregnancy it is possible in that case when the estimated advantage for mother exceeds potential risk for a fruit. In need of use of drug in the period of a lactation breastfeeding should be stopped.

Overdose:

At reception in the dose exceeding the maximum daily increase in frequency of the dozozavisimy side effects described above is possible.

Treatment: gastric lavage; carry out a symptomatic and maintenance therapy. The hemodialysis and peritoneal dialysis are not effective.

Storage conditions:

To store at a temperature not above 25 °C. To store in the places unavailable to children. Period of validity 3 years. Not to use after the termination of the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets the dispersed 400 mg.
1, 5, 7 tablets in the blister from PVC-aluminum foil.
1 blister on 1, 5, 7 tablets or 2 blisters on 5 tablets instead of with the application instruction in a cardboard pack.