Цефабол®

General characteristics. Structure:

Active ingredient: 1 g of a tsefotaksin of sodium (in recalculation in tsefotaksy).
Tsefalosporinovy antibiotic of the III generation for parenteral use.

Pharmacological properties:

Pharmacodynamics. Tsefotaksim is a tsefalosporinovy antibiotic of the III generation for parenteral use. Works bakteritsidno: contacts transpeptidases and breaks the final stages of synthesis of a cell wall of bacteria. Possesses a wide range of antimicrobic action.

It is active concerning gram-positive and gram-negative microorganisms, including steady against penicillin and cephalosporins I-II of generations: Staphylococcus spp. (including Staphylococcus epidermidis, S. aureus, except the strains steady against Methicillinum), most Streptococcus spp. (including S. pneumoniae, S. pyogenes, S. agalactiae, S. bovis, Streptococcus spp. viridans groups, etc.), Enterococcus spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Acinetobacter spp., Bordetella pertussis, Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including the strains steady against ampicillin), H. parainfluenzae, Klebsiella spp. (including K. pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including the strains producing beta lactamelements), N. meningitidis, Proteus mirabilis, P. vulgaris, Providencia spp., Providencia rettgeri, P. stuartii, Serratia marcescens, Shigella spp. Salmonella spp. (including S.typhi), Yersinia spp. (including Y.enterocolitica), Borrelia burgdorferi, Bacteroides spp., (including some strains of Bacteroides fragilis), Clostridium spp. (except C. difficile), Fusobacterium spp., including F. nucleatum, Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp.

It is steady against the majority beta лактамаз gram-positive and gram-negative microorganisms, a penicillinase of stafilokokk.

Pharmacokinetics. After single intravenous (in/in) introductions of 1,0 g of Tsefabola®, the maximum serumal concentration (Cmax) is reached in 5 min. and makes 101,7 mg/l. In 30 min. after intramuscular introduction (in oil) in the same dose of Cmax makes 20,5 mg/l, respectively. At introduction in oil bioavailability of Tsefabola® makes 90-95%. Extent of linkng with proteins of a blood plasma of 25-40%.

Later in/in and introductions in oil therapeutic concentration are reached in the majority of fabrics (in lungs, a myocardium, mucous paranasal sine, abdominal organs, kidneys, skin and hypodermic cellulose, bones) and liquids (in liquor, synovial, pleural, ascitic and pericardiac liquids, liquid of a middle ear, etc.) an organism. In insignificant concentration it is excreted with breast milk, gets through a placenta (in small concentration). Distribution volume - 0,25-0,39 l/kg.

The elimination half-life of a tsefotaksim from blood serum later in/in and introductions in oil - about 1 hour, at newborns is 0,75-1,5 h. A part of a tsefotaksim is metabolized in a liver with formation of an active metabolite (M1) - a dezatsetiltsefotaksima, and two inactive - Sq.m and M3. About 80% of the entered dose of a tsefotaksim are removed with urine, and 44-61% in an invariable look, 13-24% in the form of a dezatsetiltsefotaksim and 7-16% - in the form of inactive metabolites (Sq.m and M3). At repeated in introductions in a dose of 1 g each 6 h during 14 days of cumulation it is not observed.

At the chronic renal failure (CRF) and at elderly people the elimination half-life increases twice; at premature newborns it is extended to 4,6 h.

Indications to use:

Treatments of medium-weight and heavy infections of various localizations caused by microorganisms, sensitive to a tsefotaksim, at children, since the neonatality period, and at adults:

- infections of the central nervous system (including meningitis),
- respiratory infection and ENT organs, including pneumonia,
- infections of urinary tract, including pyelonephritis,
- infections of bones, joints,
- infections of skin and soft tissues, including postoperative wound complications,
- infections of bodies of a small pelvis, including acute and aggravation of a chronic adnexitis, pelviperitonitis, endometritis,
- gonorrhea,
- Lyme's disease (tick-borne borreliosis),
- endokapdit,
- salmonellosis,
- sepsis,
- infections against the background of an immunodeficiency,
- prevention of infections after surgeries (including urological, obstetric and gynecologic, on digestive tract).

Route of administration and doses:

Intramusculary and intravenously (struyno and kapelno), depending on the chosen dose, the mode of dosing and weight of an infection.

Adults and children are more senior than 12 years, or with the body weight of 50 kg and more. At uncomplicated infections each 12 h enter in oil or in/in, 1 g. At uncomplicated acute gonorrhea - 0.5-1 in oil once. At moderately severe infections appoint 1-2 in oil or in/in each 8 h. In cases when high doses of an antibiotic are required (including, for treatment of sepsis), enter in/in in a dose of 2 g with an interval of 6-8 hours. At life-threatening infections intervals between introductions can be reduced till 4 o'clock (the maximum dose - 12 g/days).

For antimicrobic prevention of postoperative it is purulent - septic complications enter 1,0 g ^{of Tsefabola®} in 30 min. prior to operation once. If necessary, introduction is repeated in 6 and 12 h. At the patients who are exposed to Cesarean section, 1,0 g ^{of Tsefabola®} enter in/in at once after crossclamping of an umbilical cord, then, if necessary, in addition on 1 in about 6 g and 12 h after the first dose.

The patient with a heavy renal failure (clearance of creatinine of 20 ml/min. / 1,73 ^sq.m) the daily dose ^{of Tsefabola®} is reduced twice.

Children of the first month have lives, irrespective of gestational age, use the following dosages: the newborn of the first week of life each 12 h enter in/in in a dose of 50 mg/kg; at the age of 1-4 weeks - in/in on 50 mg/kg each 8 h.

At children from 1 month to 12 years, or with body weight less than 50 kg, the daily dose ^{of Tsefabola®} making from 50 to 180 mg/kg are shared on 4-6 in oil or in/in introductions. At the heavy course of infections, including meningitis, the daily dose to children is increased to 200 mg/kg, intramusculary or intravenously, in 4-6 introductions. At children with body weight more than 50 kg use the dosages specified for adults.

Rules of preparation of solutions
For preparation of solution for an injection in oil 1,0 g of the dry sterile ^{powder Tsefabola®} dissolve in 3-4 ml of sterile water for injections or 1% of solution of lidocaine. Enter deeply intramusculary into body parts with the expressed muscular layer (an upper outside quadrant of a buttock or the lateral surface of a hip).

It is recommended to carry out the test for aspiration to avoid undesirable administration of solution in a blood vessel. For preparation of solution for in/in jet introductions of 1,0 g ^{of Tsefabola®} part in 10 ml of sterile water for injections. Enter in/in slowly, within 3-5 min.; introduction through a special node or port for system injections for in/in infusions is possible if the patient receives liquids parenterally.

For in/in drop introductions of 1,0 g ^{of Tsefabola®} part in 4-5 ml of sterile water for injections. The received solution is added to the bottle containing 50 or 100 ml of 5% of solution of a dextrose or 0,9% of solution of sodium of chloride.

Features of use:

When developing diarrhea during treatment of Tsefabolom® it is necessary to show vigilance in view of possible development of pseudomembranous colitis. If the diagnosis an antibiotic - the associated diarrhea or pseudomembranous colitis is established, it is necessary to stop immediately introduction of Tsefabola® and to appoint the corresponding treatment, including Vancomycinum or metronidazole inside.

Before purpose of drug it is necessary to collect the allergological anamnesis. The cross allergy between penicillin and cephalosporins is known. At persons in whose anamnesis there are instructions on an allergy to penicillin drug is used with extreme care (it is necessary to consider a possibility of development of heavy anaphylactic reactions).

At treatment duration drug over 10 days control of number of uniform elements of blood is necessary.

When determining sugar in urine by not euzymatic method (for example, Benedict's method) false positive results are possible.

Side effects:

Therapy of Tsefabolom® is well transferred, undesirable medicinal reactions are observed seldom, and quickly take place after drug withdrawal.

Allergic reactions: small tortoiseshell, fever or fever, rash, itch, bronchospasm, eosinophilia, malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), Quincke's disease, acute anaphylaxis.

From the alimentary system: nausea, vomiting, diarrhea or a lock, a meteorism, an abdominal pain, dysbacteriosis, stomatitis, a glossitis, an antibiotic - the associated diarrhea and pseudomembranous colitis.

From bodies of a hemopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolitic anemia.

From an urinary system: oliguria, intersticial nephrite.

From a nervous system: headache, dizziness. Laboratory indicators: an azotemia, increase in concentration of urea in blood, increase in activity of "hepatic" transaminases and an alkaline phosphatase, a giperkreatininemiya, a hyperbilirubinemia.

From cardiovascular system: potentially life-threatening arrhythmias after bystry bolyusny introduction to the central vein.

Local reactions: phlebitis, morbidity on the vein course, morbidity and infiltrate in the place in oil of introduction.

Others: superinfection (in particular, mycotic vulvovaginitis).

Interaction with other medicines:

At co-administration of Tsefabola® with aminoglycosides sinergidny and additive effects are observed.

In solution pharmaceutical it is incompatible with aminoglycosides and Vancomycinum.

At simultaneous use it is not necessary to mix them in one syringe or one infusional environment; at introduction in oil to enter into different body parts; at intravenous administration to enter separately, observing a certain sequence with as it is possible a big time interval between injections (infusions), or to use separate intravenous catheters.

It is impossible to use bicarbonate sodium solution as solvent.

At a combination to antiagregant, non-steroidal anti-inflammatory drugs the risk of development of bleedings increases.

The medicines blocking canalicular secretion increase plasma concentration of a tsefotaksim and slow down its removal.

The probability of a renal failure increases at a concomitant use with aminoglycosides, polymyxin B and "loopback" diuretics.

Does not lead to development of disulfiramopodobny reactions at combined use with ethanol.

Contraindications:

Hypersensitivity to a tsefotaksim and other tsefalosporinovy antibiotics. At use as lidocaine solution solvent:
- endocardiac blockade without the established pacemaker;
- cardiogenic shock;
- intravenous administration;
- children's age up to 2,5 years;
- hypersensitivity to lidocaine or other local anesthetic of amide type.

With care appoint at a chronic renal failure, nonspecific ulcer colitis (including in the anamnesis), allergic reactions to penicillin in the anamnesis.

Use of Tsefabola® during pregnancy perhaps in cases when the estimated advantage for mother exceeds potential risk for a fruit.
 
Tsefotaksim gets into breast milk therefore in need of use of drug in the period of a lactation it is necessary to stop breastfeeding.

Overdose:

Symptoms: spasms, encephalopathy (in case of introduction of high doses, especially at patients with a renal failure), a tremor, the increased neuromuscular excitability, cyanosis.
Treatment: symptomatic and maintenance therapy.

Storage conditions:

List B. In protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

1,0 g of active agent place in glass bottles with a capacity of 10 ml.

1 bottle with drug and the application instruction is placed in a pack from a cardboard. Solvent - "Water for injections" in glass ampoules of 5 ml.

1 bottle with drug and the application instruction is placed in a pack from a cardboard.

1 bottle with drug and 1 ampoule with solvent is packed into a blister strip packaging. One blister strip packaging and the application instruction are put in a pack cardboard.

5 bottles with drug pack into blister strip packagings. One blister strip packaging and the application instruction are put in a pack cardboard.

5 bottles with drug complete with 5 ampoules of solvent pack into blister strip packagings. One blister strip packaging with drug, one blister strip packaging with solvent and the application instruction is put in a pack cardboard.