Tseperon Dzh

General characteristics. Structure:

Active ingredient: 1 g or 2 g of a tsefoperazon of sodium in terms of цефоперазон.

Tsefoperazon - a semi-synthetic tsefalosporinovy antibiotic of the III generation with a wide range of antibacterial action for parenteral administration.

Pharmacological properties:

Pharmacodynamics. Has the bactericidal effect caused by inhibition of synthesis of a cell wall of bacteria. Tsefoperazon is active in vitro concerning a large number of clinically significant microorganisms. It is steady against action of many beta лактамаз.

Pharmacokinetics / Communication with proteins of plasma - 82-93%. Time of achievement of the maximum concentration (TCmax) after intramuscular introduction (in oil) - 1-2 h, after intravenous (in/in) - at the end of infusion.

Reaches therapeutic concentration in such fabrics and liquids of an organism as peritoneal, ascitic liquid and spinal (at meningitis), urine, bile, walls of a gall bladder, lungs, a phlegm, palatine tonsils and a mucous membrane of sine, auricles, kidneys, ureters, a prostate, testicles, a uterus, fallopian pipes, bones, blood of an umbilical cord and amniotic liquid.

Indications to use:

The bacterial infections caused by sensitive microorganisms:
• upper and lower respiratory tracts,
• urinary tract,
• abdominal infections (peritonitis, cholecystitis, cholangitis, etc.),
• sepsis, meningitis,
• infections of skin and soft tissues,
• infections of bones and joints,
• infectious and inflammatory diseases of bodies of a small pelvis (endometritis, gonorrhea, etc. infections of a genital tract).

Prevention of infectious complications after abdominal, gynecologic and orthopedic operations, and also in cardiovascular surgery.

Route of administration and doses:

The drug is administered in oil and in/in (slowly struyno or kapelno). The drug is administered deeply in oil in a big gluteus or in the front surface of a hip. At in slow jet introduction the maximum single dose of drug makes 2 g; introduction duration - not less than 3-5 min. Duration in/in drop introductions - 15-60 min.

The dose for adults makes 2-4 g/days, divided into 2 introductions, each 12 h. At heavy infections the dose can be increased to 8 g/days, divided into 2 introductions, each 12 h. Treatment by drug can be begun before obtaining results of a research of sensitivity of microorganisms.

At an uncomplicated gonococcal urethritis single introduction in oil in a dose of 500 mg is recommended.

Prevention of postoperative complications. Each 12 h apply 1 g or 2 g of drug in/in in 30-90 min. prior to operation, with the subsequent repeated introduction (in most cases during no more than 24 h). At operations with the increased risk of infection (for example, operations in colorectal area), at open heart operations or prosthetics of joints preventive use of drug can continue during 72 h after completion of operation.

Abnormal liver function. Dose adjustment in case of the heavy expressed obstruction of biliary tract, a serious illness of a liver can be required or at the accompanying abnormal liver function and kidneys. In this case the daily dose should not exceed 2 g.

Renal failure. As цефоперазон it is generally removed with bile, dose adjustment at a renal failure at use in the recommended doses (2-4 g/days) is not required. To patients at whom the glomerular filtration rate makes less than 18 ml/min. or concentration of creatinine in blood serum exceeds 3.5 mg/dl, the daily dose should not exceed 4 g.

At a hemodialysis of T1/2 of a tsefoperazon from blood serum decreases a little therefore the drug should be administered after the end of a session of dialysis.

Abnormal liver function and kidneys. It is recommended to carry out control of concentration of a tsefoperazon in blood serum and if necessary to adjust a dose. There is no need to control serumal concentration provided that the daily dose does not exceed 2 g.

Children. The dose for children makes 50-200 mg/kg/days, divided into the equal parts entered each 8-12 h. The maximum dose should not exceed 12 g/days.

At in slow jet introduction the maximum single dose makes 50 mg/kg of body weight; introduction duration – not less than 3-5 min.

Newborns (at the age of less than 8 days). 50-200 mg/kg of weight bodies/days equal parts each 12 h. At treatment of the infections caused by Streptococcus pyogenes, duration of therapy has to make not less than 10 days.

Features of use:

Use at pregnancy and a lactation. Adequate and controlled researches on influence of a tsefoperazon on the course of pregnancy were not conducted. Use at pregnancy is possible only in that case when the estimated advantage for mother surpasses potential risk for a fruit. The insignificant quantity of a tsefoperazon gets into breast milk. It is necessary to be careful at purpose of a tsefoperazon to nursing mothers.

Some patients have a treatment tsefoperazony, as well as treatment by other antibiotics, can result in deficit of vitamin K in an organism that is connected with suppression of the indestinal flora synthesizing this vitamin. Patients with a sprue (for example are subject to the greatest risk, at a mucoviscidosis), and also the patients who are adhering to a defective diet or being for an appreciable length of time on parenteral food. At such patients during treatment it is necessary to control a prothrombin time, and if necessary to appoint vitamin K.

At long therapy it is recommended to control periodically function of kidneys, a liver and bodies of a hemopoiesis.

It is especially important for newborns, first of all premature and small children.

Side effects:

Hypersensitivity: allergic reactions, including skin itch, makulopapulezny rash, small tortoiseshell, eosinophilia and medicinal fever, Stephens-Johnson's syndrome; anaphylactoid reactions (including shock). The risk of development of allergic reactions is increased at patients with tendency to allergic reactions (especially on penicillin) in the anamnesis.

From bodies of a hemopoiesis: a reversible neutropenia (at prolonged treatment), false positive direct test of Koombs, decrease in hemoglobin or a hematocrit, an eosinophilia and a prothrombinopenia, bleedings.

From digestive organs: diarrhea or ease of a chair, nausea, vomiting, moderate passing increase in activity of an alaniniaminotransferaza (ALT), aspartate aminotransferase (nuclear heating plant) and the alkaline phosphatase (AP), development of pseudomembranous colitis is possible.

Local reactions: morbidity (at introduction in oil), phlebitis in the place in/in an injection.

Interaction with other medicines:

Alcohol and alkogolsoderzhashchy drinks. At alcohol intake during treatment or within 5 days after use of a tsefoperazon it was reported about cases of development of disulfiramopodobny reaction, shown "inflows", the increased sweating, a headache and tachycardia. Patients should be warned about danger of reception of alcoholic beverages during use of a tsefoperazon. For the patients who are on peroral or parenteral artificial nutrition it is necessary to exclude the solutions containing alcohol.

Incompatibility. Aminoglycosides. Solutions of a tsefoperazon and aminoglycoside should not be mixed directly in one syringe (bottle) as between them there is a physical incompatibility. In need of carrying out a combination therapy tsefoperazony and aminoglycoside, it is carried out in the form of consecutive in drop infusion with use of two separate catheters on condition of adequate washing by their corresponding solvents between introduction of consecutive doses of drugs. Tsefoperazon it is necessary to enter before administration of aminoglycoside.

Contraindications:

Hypersensitivity to a tsefoperazon and other cephalosporins.

With care. A hyperbilirubinemia (at newborn and premature children), a renal liver failure, ulcer colitis.

Overdose:

Information on acute toxicity of a tsefoperazon is limited. It is supposed that the overdose of drug can be expressed by strengthening of side effects (except for allergic reactions). It is known that high concentration beta лактамных antibiotics in cerebrospinal fluid can cause neurologic effects therefore it is necessary to consider a possibility of development of spasms at overdose.

Treatment: symptomatic therapy (at spasms - diazepam).

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. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 1,0 g or 2,0 g. On 1,0 g and 2,0 g of active ingredient in the bottle of transparent glass corked by a stopper from the chlorbutyl rubber which is pressed out by the aluminum ring supplied with a plastic protective cap. On 1 bottle together with the application instruction in a cardboard pack. On 10, 25, 48 or 100 bottles with the equal number of instructions on a medical use in a cardboard box (for hospitals).