Tsefzoksim J.

General characteristics. Structure:

Active ingredient: 1 g of a tseftizoksim of sodium in recalculation on anhydrous tseftizoksy.

Pharmacological properties:

Pharmakodiiamika. The Tsefalosporinovy antibiotic of the III generation for parenteral administration. Works bakteritsidno, breaking synthesis of a cell wall of microorganisms. It is steady against a wide range beta лактамаз (penicillinases and цефалоспориназ), including beta lactamelements of I, II, III and IV types on Richmond and THOSE type, produced by both gram-positive, and gram-negative aerobes, and also anaerobe bacterias.

Possesses a broad spectrum of activity which includes various aerobic and anaerobic gram-positive and gram-negative microorganisms.

Pharmacokinetics. The maximum concentration (Cmax) after intramuscular introduction (in oil) in doses of 0.5 and 1 g - 13.7 and 39 mkg/ml respectively. Time of achievement of the maximum concentration (Tstakh) is 1 h Stakh after intravenous administration (in/in) in doses of 2 and 3 g - 110.9 and 174 mkg/ml respectively, Tstakh - 10 min.

Elimination half-life (T1/2) after in oil and in/in introductions - 1.7 h. Communication with blood proteins - 30%. In 2 h later in/in introductions in urine concentration more than 6 mg/ml is reached. Therapeutic concentration are reached in various liquids and body tissues: bile, pleural, peritoneal, ascitic, etc. liquids, bones, gall bladder, heart, prostate, uterus; collects in saliva, bile and cerebrospinal fluid. In small amounts gets into breast milk.

It is removed by kidneys in not changed look, creating high concentration in urine.

Indications to use:

The bacterial infections caused by strains of microorganisms, sensitive to a tseftizoksim:
• lower respiratory tract infections;
• infections of urinary tract;
• gonorrhea;
• infectious and inflammatory diseases of bodies of a small pelvis; - intraabdominal infections (excepting the infections caused by enterococci);
• septicaemia;
• infections of skin and hypodermic fabrics (excepting the infections caused by enterococci);
• infections of bones and joints (excepting the infections caused by enterococci);
• meningitis.

Tseftizoksim is effective at treatment of heavy infections, including at the weakened patients, patients with reduced immunity, a neutropenia, the mixed aerobic-anaerobic infections steady against other cephalosporins and aminoglycosides.

Route of administration and doses:

In oil, in/in struyno (within 3-5 minutes) or kapelno. In/in a way of introduction it is preferable at patients with a bacterial septicaemia, limited parynchemal abscess (in particular intraabdominal abscess), peritonitis or other heavy or zhizneugrozhayushchy infections. The drug dose, a way of maintaining have to be defined depending on a condition of the patient, weight of a course of an infection and sensitivity of a microorganism.

Usually the drug dose at adults makes 1-2 g each 8-12 h.

At uncomplicated infections of urinary tract - 500 mg each 12 h in/in or in oil. At treatment of the infections caused by P. aeruginosa, the dose has to be increased as many strains of P. aeruginosa are moderately sensitive to a tseftizoksim. If the response to treatment does not come during the near future, it is necessary to begin other therapy.

At infections of other localizations - 1 g each 8-12 h in/in or in oil.

Heavy or refractory infections - 1 g each 8 h or 2 g each 8-12 h in/in or in oil. In need of introduction of 2 in oil the dose has to be divided and entered separately into different large muscles.

Infectious and inflammatory diseases of bodies of a small pelvis - 2 g each 8 h in / century. If as the activator S. is suspected by trachomatis, it is necessary to enter in addition antibiotics, effective concerning S. of trachomatis as tseftizoksy it is inactive concerning this activator.

Zhizneugrozhayushchy infections - 3-4 g each 8 h in / century. There is an experience of introduction of doses to 2 g each 4 h.

For treatment of uncomplicated gonorrhea - 1 in oil once.

At normal function of kidneys of a dose from 2 to 12 g in/in can daily be entered, at a bacterial septicaemia in a dose of 6-12 g carry usually out to introduction within several days then the dose is gradually reduced according to the clinical answer and laboratory indicators.

To children 6 months - 50 mg/kg/days each 6-8 h are more senior. If necessary the dose can be increased to the general daily dose of 200 mg/kg, but should not exceed the maximum recommended dose at adults at treatment of heavy infections.

At disturbance of secretory function of kidneys correction of the mode of dosing depending on values of the clearance of creatinine (CC) is required. After an initial dose of 500 mg or 1 g in/in or in oil the dose decline according to the data provided in the table is necessary:

The patients who are on a hemodialysis have no need for introduction of an additional dose, however administration of drug should be carried out (according to the table above) at the end of a hemodialysis session.

For preparation of solution for injections in oil bottle contents (1 g) are dissolved by 3 ml of sterile water for injections.

For preparation of solution for in/in jet injections bottle contents (1 g) are dissolved by 10 ml of sterile water for injections. The prepared solution can be entered directly into a vein, or through a cannula for administration of parenteral liquids. For in/in drop introductions previously recovered solution dissolve further in 50-100 ml 0.9% of solution of sodium of chloride, 5% or 10% solution of a dextrose (glucose), 5% solution of a dextrose and 0.9%, 0.45% or 0.2% chloride sodium solution, in Ringer and Ringer's solution of a lactate, 5% Natrii hydrocarbonas solution.

Features of use:

Patients with an allergy to penicillin can have cross hypersensitivity to tsefalosporinovy antibiotics.

At emergence in time or after treatment of heavy and long diarrhea it is necessary to exclude the diagnosis of pseudomembranous colitis which demands immediate drug withdrawal and purpose of the corresponding treatment.

As well as other cephalosporins tseftizoksy it is inactive concerning Chlamydia trachomatis therefore in case of treatment of infectious and inflammatory diseases of bodies of a small pelvis when as one of activators Chlamydia trachomatis is suspected, it is necessary to add antibiotics, active concerning this activator.

During treatment it is necessary to exercise control of function of kidneys periodically.

Prior to treatment tseftizoksimy it is necessary to conduct a laboratory research for establishment of a type of the activator and its sensitivity; treatment tseftizoksimy can be begun before obtaining results of these researches, however in the subsequent has to be corrected according to the received results. In case of heavy infections by tseftizoksy it can be applied in a combination with aminoglycosides.

After cultivation drug can be stored at the room temperature during 7 h, in the refrigerator - 48 h.

The recovered solution can get yellowish coloring that does not influence its activity.

Influence on ability to manage vehicles and work with mechanisms. Researches on influence of drug on ability to manage vehicles and work with mechanisms were not conducted.

Side effects:

The most frequent (more than 1%, but less than 5%): Allergic reactions: rash, itch, fever.

From gepatobiliarny system: tranzitorny increase in activity of alaninaminotranspherase (ALT), aspartate aminotransferase (ACT) and alkaline phosphatase (AP).

From bodies of a hemopoiesis: tranzitorny eosinophilia, thrombocytosis, false positive test of Koombs.

Reactions in an injection site: burning, an inflammation of hypodermic cellulose, phlebitis (at in introduction), pain, consolidation, morbidity when pressing, paresthesia.

Less frequent (less than 1%): Allergic reactions: numbness and anaphylaxis.

From gepatobiliarny system: increase in bilirubin in blood. From urinogenital system: tranzitorny increase in blood of an urea nitrogen and creatinine; vaginitis.

From bodies of a hemopoiesis: anemia (including hemolitic), a leukopenia, a neutropenia, thrombocytopenia.

From the alimentary system: diarrhea, nausea, vomiting, pseudomembranous colitis.

Interaction with other medicines:

At simultaneous use with other cephalosporins and aminoglycosides the risk of nephrotoxic action increases.

Pharmaceutical it is incompatible with other medicines (for  recovery  of drug  it is necessary  to use only the solvents listed in the section "Route of Administration and Doses").

Contraindications:

Hypersensitivity (including to other beta лактамным to antibiotics), chest age (up to 6 months).

With care. A renal failure, the pseudomembranous colitis connected using antibacterial medicines, pregnancy, the lactation period.

Overdose:

Overdose cases are not registered so far.

Storage conditions:

To store in the dry place protected from light at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intramuscular and intravenous administration of 1.0 g. On 1.0 g of powder in the bottle of transparent glass corked by a stopper from the chlorbutyl rubber which is pressed out by an aluminum ring, and a plastic cap. On 1 bottle together with the application instruction in a pack cardboard.