Мегасеф®

General characteristics. Structure:

Active ingredient: 300,72 mg or 601,44 mg of a tsefuroksim of an aksetil equivalent of 250 mg or 500 mg.

Excipients: starch prezhelatinizirovanny, кросповидон (Kollidon Cl), sodium of a kroskarmelloz, sodium lauryl sulfate, magnesium stearate, silicon dioxide colloid anhydrous (Aerosil 200).

Film cover No. 1 Sepifilm LP 770: gipromelloz (gidroksipropilmetiltsellyuloz) (Е 464), cellulose microcrystallic (Е 460), stearic acid (Е 570), titanium dioxide (Е 171).

Pharmacological properties:

Pharmacodynamics. Tsefuroksim – a tsefalosporinovy antibiotic of the second generation of a broad spectrum of activity. Has bactericidal effect at the expense of inhibition of synthesis of a cell wall of bacteria. Tsefuroksim acetylates membrane-bound transpeptidases, breaking, thus, the cross stitching of peptido-glycanes necessary for ensuring durability and rigidity of a cell wall. Tsefuroksim is steady against action of many bacterial beta лактамаз therefore he is active concerning the majority of the types steady against penicillin and amoxicillin.

Tsefuroksim is active concerning the following microorganisms:

- gram-negative bacteria: Escherichia coli, Haemophilus influenzae (including the types producing beta lactamelements), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis (including the types producing beta lactamelements), Neisseria gonorrhoeae (including the types producing beta lactamelements), Salmonella spp., Shigella spp., Proteus mirabilis, Enterobacter spp.

- gram-positive bacteria: Staphylococcus aureus (including the types producing beta lactamelements), Streptococcus pneumoniae, Streptococcus pyogenes.

- certain types of enterococci, for example Enterococcus faecalis, are steady against a tsefuroksim.

- anaerobe bacterias: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Fusobacterium spp.

Pharmacokinetics. Tsefuroksim aksetit quickly is soaked up from digestive tract and hydrolyzed by nonspecific esterases of a mucous membrane of intestines and blood to a tsefuroksim. Linkng with proteins of plasma makes 50%.

Tsefuroksim is distributed in fabrics and liquids of an organism. At administration of drug after food the maximum concentration in plasma for dosages of 125 mg, 250 mg and 500 mg makes respectively 2,1 mkg/ml, 4,1 mkg/ml, 7 mkg/ml. The maximum concentration is reached 3 hours later after administration of drug. Therapeutic concentration in cerebrospinal fluid are reached only at meningitis.

Gets through a placenta, it is allocated with breast milk. It is removed with urine in not changed look. Elimination half-life about 1,2 hours.

Indications to use:

- upper respiratory tract infection and ENT organs (otitis, sinusitis, tonsillitis, pharyngitis);

- lower respiratory tract infections (acute bronchitis, exacerbation of chronic bronchitis, pneumonia);

- infections of urinogenital system (pyelonephritis, cystitis, urethritis, including gynecologic infections);

- abdominal infections;

- infections of bones and joints;

- infections of skin and soft tissues.

Route of administration and doses:

The recommended dose for adults makes 250 mg 2 times a day. At heavier infections or infections caused by less sensitive microorganisms 500 mg 2 times a day are recommended.

At uncomplicated infections of uric ways the recommended dose makes 250 mg once a day. If necessary at some patients with infections of uric ways the dosage can be increased to 250 mg 2 times a day. To children 12 years the recommended dose are more senior makes 125 mg (1/2 tablets) 2 times a day.

Usually duration of treatment makes 7 days (from 5 to 10 days). The course of treatment has to be prolonged up to 10 days at patients with the infections caused by a beta and hemolitic streptococcus for avoidance of developing of acute rheumatic fever or an acute glomerulonephritis.

To patients with a renal failure the mode of dosing is set taking into account KK values.

For the best absorption drug should be accepted after food. Tablets should be swallowed entirely, without chewing.

Features of use:

With care appoint at a chronic renal failure, bleedings and diseases of digestive tract, to the weakened and exhausted patients. At long reception it is necessary to control a pattern of blood, function of kidneys and a liver.

At patients with hypersensitivity to penicillin allergic reactions to tsefalosporinovy antibiotics are possible. At emergence of considerable allergic reaction on tsefuroksy it is necessary to cancel drug and to appoint the corresponding treatment. Heavy reactions of hypersensitivity can demand use of adrenaline and acceptance of other urgent measures, including oxygen, infusional therapy, intravenous administration of antihistaminic drugs, corticosteroids, pressor amines and imposing of an air duct according to indications.

Aksetit long use of a tsefuroksim, as well as other antibiotics of a broad spectrum of activity, can lead to the strengthened reproduction of microorganisms, insensitive to drug (for example, Candida, Enterococci, Clostridium difficile) that can demand drug withdrawal. At use of antibiotics of a broad spectrum of activity pseudomembranous colitis therefore it must be kept in mind at patients this diagnosis when developing diarrhea in time or after use of antibiotics was observed. During treatment positive forward reaction of Koombs and false positive reaction of urine to glucose is possible.

Pregnancy and period of a lactation. Use in II and III trimesters of pregnancy, and also in the period of a lactation perhaps in cases when the estimated advantage of therapy for mother exceeds potential risk for a fruit. Tsefuroksim gets into breast milk therefore during treatment by drug it is necessary to stop breastfeeding.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Considering side effects of drug it is necessary to be careful when driving or potentially dangerous mechanisms.

Side effects:

Often (≥1/100, <1/10):

- eosinophilia;

- headache, dizziness;

- nausea, diarrhea, pain in a stomach;

- short-term increase in level of liver enzymes (ALT, nuclear heating plant, LDG).

Infrequently (≥1/1000, <1/100):

- vomiting;

- skin rash;

- positive take of the test of Koombs, thrombocytopenia, leukopenia (sometimes expressed).

Seldom (≥1/10000, <1/1000):

- pseudomembranous colitis;

- urticaria, itch.

Very seldom (<1/10000):

- hemolitic anemia;

- medicinal fever, serum disease, anaphylaxis, multiformny erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis;

- jaundice (generally cholestatic), hepatitis.

Interaction with other medicines:

Tsefuroksim aksetit, is not active in a GIT, has the minimum impact on an indestinal flora and synthesis of vitamin K. At a concomitant use anticoagulating effect of warfarin amplifies.

At simultaneous use with loopback diuretics the risk of development of nephrotoxic action increases.

Probenetsid competes with tsefuroksimy at renal canalicular secretion that leads to increase in concentration of a tsefuroksim in plasma.

For determination of level of glucose in a blood plasma at the patients accepting tsefuroksy aksetit, it is recommended to apply glyukozoksidazny or hexokinase methods.

Tsefuroksim does not influence creatinine level in serum and in urine.

Pharmaceutical it is incompatible with aminoglycosides, solution of Natrii hydrocarbonas of 2,74%.

Contraindications:

- hypersensitivity to a tsefuroksim and other cephalosporins;

- children's age up to 12 years;

- first trimester of pregnancy.

Overdose:

Symptoms: excitement of TsNS, spasm.

Treatment: hemodialysis and peritoneal dialysis.

Storage conditions:

To store at a temperature not above 25 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets place in a blister strip packaging from a film of white polyvinyl chloride and aluminum foil.

On 1 planimetric packaging together with the instruction on a medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.