Оритакс

General characteristics. Structure:

Active ingredient: 0,5 g or 1 g of a tsefotaksim of the sodium equivalent to a tsefotaksim.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the III generation for parenteral administration. Works bakteritsidno, breaking synthesis of a cell wall of microorganisms. Possesses a broad spectrum of activity.

It is active concerning the gram-positive and gram-negative microorganisms steady against other antibiotics

It is steady against the majority beta лактамаз gram-positive and gram-negative microorganisms.

Pharmacokinetics. After single intravenous administration in doses of 0,5 g, 1 g and 2 g the maximum concentration in a blood plasma (Cmax) is defined in 5 min. and makes about 40 mkg/ml, 102 mkg/ml and 215 mkg/ml respectively. After intramuscular administration of drug in doses of 0,5 g and 1 g of Cmax is defined in 30 minutes and makes about 10 mkg/ml and 23 mkg/ml respectively. Communication with proteins of a blood plasma of-30-50%. Bioavailability - 90-95%. Creates therapeutic concentration in the majority of fabrics (a myocardium, bones, a gall bladder, skin, soft tissues) and liquids (synovial, pericardiac, pleural, cerebrospinal fluid, a phlegm, bile, urine) of an organism. Distribution volume – 0,25–0,39 l/kg.

Elimination half-life (T1/2) – 1 hour at in introduction and 1-1,5 hours – at introduction in oil. It is removed by kidneys – 20-36% in not changed look, other quantity – in the form of metabolites (12-25% - in the form of pharmacological active dezatsetiltsefotaksim and 20-25% - in the form of 2 inactive metabolites – Sq.m and M3 deprived of antimicrobic action).

At the chronic renal failure (CRF) and at elderly people of T1/2 increases twice. T1/2 at newborns – 0,75-1,5 hours, at premature newborn children (body weight less than 1500) increases till 4,6 o'clock; children with body weight have more than 1500 – 3,4 hours. At repeated in introductions in doses of 1 g each 6 hours within 14 days of cumulation it is not observed. Gets into breast milk, passes through a placental barrier.

Indications to use:

The bacterial infections of a heavy current caused by sensitive microorganisms:
• infections of the central nervous system (meningitis);
• airways and ENT organs;
• urinary tract;
• bones and joints;
• skin and soft tissues, including contaminated wounds and burns;
• bodies of a small pelvis;
• clamidiosis, gonorrhea;
• peritonitis, abdominal infections;
• sepsis, endocarditis;
• Lyme's disease, salmonellezy
• 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:

Intravenously (in/in) or intramusculary (in oil).
To adults and children with the body weight of 50 kg and more
• at uncomplicated infections - in oil or in/in, on 1 g each 12 h;
• at moderately severe infections - in oil or in/in, on 1-2 g each 8 h;
• at zhizneugrozhayushchy infections (at meningitis) - in/in, on 2 g each 4 h, the maximum daily dose - 12 g;
• at uncomplicated acute gonorrhea - in oil, on 0.5-1 g once;
• at sepsis - in/in, on 2 g each 6-8 h.

Duration of treatment is established individually.

For the purpose of prevention of development of infections before surgery enter into time of introduction general anesthesia once 1 g. If necessary introduction is repeated in 6-12 h.

At Cesarean section (at the time of imposing of clips on an umbilical vein) - in/in 1 g, then in 6 and 12 h after the first dose - in addition on 1 g. At KK of 20 ml/min. / 1.73 the sq.m and less daily dose are reduced twice.

Premature and newborn to 1 week - in/in 50 mg/kg each 12 h; at the age of 1-4 weeks - in/in 50 mg/kg each 8 h; to children, with body weight to 50 kg - in/in or 50-180 mg/kg in oil in 4-6 introductions. At the heavy course of infections, including meningitis, in oil or in/in, in 4-6 receptions, the maximum daily dose - 12 g.

Rules of preparation of injection solutions: for in/in an injection as solvent use water for injections (0.5-1 g part in 4 ml of solvent, 2 g - in 10 ml); for in/in infusion as solvent use 0.9% solution of sodium of chloride or 5% dextrose solution (1-2 g part in 50-100 ml of solvent). Infusion duration - 50-60 min. For introduction in oil use water for injections or 1% lidocaine solution (for a dose of drug of 500 mg - 2 ml, for a dose of 1 g - 4 ml).

Features of use:

Use at pregnancy and in the period of a lactation. Use of drug during pregnancy is contraindicated. In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

In the first weeks of treatment there can be pseudomembranous colitis which is shown heavy long diarrhea. At the same time stop administration of drug and appoint adequate therapy, including Vancomycinum or metronidazole.

The patients who had allergic reactions to penicillin in the anamnesis can have hypersensitivity to antibiotics of group of cephalosporins.

At treatment by drug over 10 days control of a picture of peripheral blood is necessary.

During treatment tsefotaksimy receiving false positive test of Koombs and false positive reaction of urine to glucose is possible.

During treatment it is impossible to use ethanol because of possibility of disulfiramopodobny reactions (a hyperemia of the person, spastic abdominal pains and in epigastric area, nausea, vomiting, a headache, a lowering of arterial pressure, tachycardia, short wind).

Side effects:

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

From a nervous system: headache, dizziness.

From an urinary system: renal failure, oliguria, intersticial nephrite.

From the alimentary system: nausea, vomiting, diarrhea or locks, a meteorism, an abdominal pain, dysbacteriosis, an abnormal liver function, it is rare - stomatitis, a glossitis, a pseudomembranous coloenteritis.

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

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

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, positive test of Koombs.

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

Others: development of superinfection (in particular, mycotic vulvovaginitis).

Interaction with other medicines:

Increases risk of development of bleedings at a combination to antiagregant, non-steroidal anti-inflammatory drugs.

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

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

Pharmaceutical it is incompatible with solutions of other antibiotics in one syringe or a dropper.

Contraindications:

Hypersensitivity (including to penicillin, other cephalosporins, karbapenema), pregnancy, children's age up to 2,5 years (for an intramuscular way of introduction).

With care. The neonatality period (for intravenous administration), the lactation period, a chronic renal failure, nonspecific ulcer colitis (including in the anamnesis).

Overdose:

Symptoms: spasms, encephalopathy (in case of introduction of high doses, especially at patients with a renal failure), a tremor, nervously – muscular irritability.

Treatment: symptomatic, there is no specific antidote.

Storage conditions:

List B. To store in the dry place protected from light 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 a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 0,5 g and 1,0 g of drug in the bottle of transparent glass corked by a stopper from the chlorbutyl rubber which is pressed out by an aluminum ring with a safety plastic cap. On 1 bottle together with the application instruction in a pack cardboard.

For hospitals: 10, 25, 48 or 100 bottles  together with the equal number of application instructions in a cardboard box.