Sulbatsin

General characteristics. Structure:

Active ingredient: 0,5 g or 1 g of ampicillin of sodium salt in terms of anhydrous ampicillin, 0,25 g or 0,5 g of a sulbaktam of sodium salt in terms of anhydrous to sulbakta.

Polusinteticheky penicillinic antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Sulbatsin – the combined drug which has a wide range of antibacterial (bactericidal) action. Ampicillin – semi-synthetic penicillin of a broad spectrum of activity, is a bactericidal component of an ampisulbin, affects sensitive microorganisms in a phase of active reproduction by oppression of biosynthesis of a mukopeptid of a cell wall.

Sulbaktam has no the expressed antibacterial activity (it is active only concerning Neisseria spp., Acinetobacter calcoacet_cus, Bacteroides spp., Branhamella catarrhalis, Pseudomonas cepacia), is inhibitor beta лактамаз, the microorganisms causing resistance to effect of ampicillin.

Sulbaktam possesses an action synergism with penicillin. Thanks to a combination of a sulbaktam of sodium and ampicillin of sodium the range and expressiveness of antimicrobic action of components of drug extends. Drug is active concerning the majority of gram-positive and gram-negative microorganisms: Staphylococcus spp. (including the strains producing beta lactamazu), Streptococcus spp., including S. pyogenes, S. viridans, S. Pneumoniae, S. faecalis, Haemophilus influenzae and H. parainfluenzae (including the strains producing beta lactamelements), Branhamella catarralis, Neisseria meningitidis, N. gonorrhoeae, Escherichia coli, Klebsiella spp., Proteus spp. (indolpositive and indolnegative strains), Citrobacter spp., Enterobacter spp., Morganella morganii, Clostridium spp., asporous anaerobe bacterias – Peptococcus spp. and Peptostreptococcus spp., Bacteroides spp., including Bacteroides fragilis.

Pharmacokinetics. Pharmacokinetic parameters of a sulbaktam and ampicillin match. The maximum concentration in blood and an elimination half-life of ampicillin at its use in combination with sulbaktamy are similar to the corresponding indicators at administration of one ampicillin in an equivalent dose. Drug is well distributed in the majority of fabrics and liquids of an organism, well gets into bile, a phlegm, pus.

Penetration into liquids of a head and spinal cord low, however amplifies in the presence of an inflammation of a meninx. Concentration of components in pleural and peritoneal liquid corresponds to concentration which are observed in blood serum. In low concentration it is found in breast milk. Depending on a dose and a way of introduction амписульбин it is found in blood within 6 - 8 hours. The elimination half-life makes about 1 hour. It is removed preferential with urine (75 - 80%) in not changed look.

Indications to use:

The bacterial infections caused by microorganisms, sensitive to drug:

• infections of an ear, a throat, a nose (sinusitis, average otitis, epiglotit, tonsillitis, pharyngitis),
• respiratory infections (bronchitis, pneumonia),
• infections of an urinary system (cystitis, pyelonephritis),
• intraperitoneal infections (peritonitis, cholecystitis),
• infections in obstetrics and gynecology (an endometritis, a parametritis, a salpingo-oophoritis),
• sepsis,
• infections of skin and soft tissues,
• infections of bones and joints (osteomyelitis, arthritis),
• gonococcal infections,
• mephitic gangrenes.

Preoperative prevention of purulent complications in surgery, obstetrics and gynecology.

Route of administration and doses:

Before use of drug it is necessary to carry out skin tests on portability of drug.

Sulbatsin appoint intravenously and intramusculary. For adults the dose usually makes 1,5 - 3 which is entered for 3 - 4 receptions with an interval of 6 - 8 hours. At not heavy infections it is possible to enter drug each 12 hours in a daily dose to 3 g; at moderately severe infections – in a daily dose to 6 g each 6 or 8 hours. The maximum daily dose makes 12 g. To children drug appoint in a dose 150 mg/kg of body weight a day, having divided into 3 or 4 introductions with an interval of 6 - 8 hours. To premature children and children in the first week of life the drug is administered by each 12 hours in a dose of 75 mg/kg of body weight a day. Duration of treatment is defined individually and makes 5 - 14 days. After normalization of body temperature and disappearance of other pathological symptoms drug is used within 48 hours.

For prevention of surgical infections enter 1,5 - 3 of drug during an introduction anesthesia that is considered sufficient for achievement of effective concentration in serum and fabrics during operation. Administration of drug can be repeated in 6-8 hours, at the majority of surgical interventions use of an antibiotic is usually stopped in 24 h after operation.

For treatment of uncomplicated gonorrhea the drug is administered disposable in a dose of 1,5 g.

Solution Sulbatsin is prepared just before its use. At preparation of solution it is necessary to allow to it to be defended after addition of solvent before total disappearance of foam which is formed visually to estimate completeness of dissolution. For intravenous administration drug is dissolved in sterile water for injections or 0,9% solution of sodium of chloride or 5% glucose solution. To the bottle containing 0,75 g of drug add 5 ml of solvent, to the bottle containing 1,5 g – 10 ml. Enter slowly within 5 - 10 min.

Sterile powder to Sulbatsin can be recovered in necessary concentration by the following parenteral solvents. Recovery given by solvents in the specified concentration gives to Sulbatsin solutions which stability remains during the time specified in the table. After this time any unused portion of solution has to be destroyed.

Solvent	Maximum concentration (mg/ml) Sulbatsin (Sulbaktam / Ampitsillin)	Period uses
Water for injections is sterile	45 (15/30)	8 hours at 25 °C
	45 (15/30)	48 hours at 4 °C
	30 (10/20)	72 hours at 4 °C
0.9% sodium chloride solution for injections	45 (15/30)	8 hours at 25 °C
	45 (15/30)	48 hours at 4 °C
	30 (10/20)	72 hours at 4 °C
5% glucose solution for injections	30 (10/20)	2 hours at 25 °C
	30 (10/20)	4 hours at 4 °C
Ringer's solution of a lactate	45 (15/30)	8 hours at 25 °C
	45 (15/30)	24 hours at 4 °C
M/6 sodium lactate for injections	45 (15/30)	8 hours at 25 °C
	45 (15/30)	8 hours at 4 °C
5% of glucose in 0,45% normal saline solution	15 (5/10)	4 hours at 4 °C
10% solution of the inverted sugar	30 (10/20)	3 hours at 4 °C

At first bottle contents to Sulbatsin can be dissolved in 3 - 5 ml of sterile water for injections. Solution has to be divorced further corresponding infusional with substance for obtaining final concentration about 15 - 30 mg/ml. The recovered solution to Sulbatsin has to be entered within 15 - 30 min.

For intramuscular introduction Sulbatsin dissolve in sterile water for injections. With a dosage of 0,75 g or 1,5 g of drug add 2 ml or 3 ml of solvent to a bottle respectively. Solution is entered deeply into an upper outside square of a buttock.

At the expressed renal failures it is necessary to increase intervals between each introduction: at clearance of creatinine from 15 to 29 ml/min. the interval makes 12 hours, at clearance of creatinine from 5 to 14 ml/min. – respectively 24 hours. To the patients who are on a hemodialysis, Sulbatsin enter right after dialysis session, and at long arter_ovenozny a hemodialysis – in 6 - 12 hours.

Features of use:

With care appoint the patient with renal failures and a liver, at digestive tract diseases in the anamnesis, especially at colitis. During all course of treatment it is necessary to control function of kidneys and a liver.

Sulbatsin can be also applied to treatment of the infections provoked ampicillin - sensitive organisms, thanks to the content of ampicillin. Thus, the polymicrobial infections provoked ampicillin - sensitive organisms and beta лактамазними the derivative organisms sensitive to Sulbatsin, do not demand use of an additional antibiotic. Therapy can be carried out before passing of bacteriological tests and tests for a susceptibility, when there is no the bases to consider that the infection can attract any beta лактамазные the derivative organisms which are listed above.

With care it is applied at allergic diseases in the anamnesis.

Pregnancy and feeding by a breast. Use of drug at pregnancy is possible only in case the estimated advantage for mother exceeds potential risk for a fruit. In need of use Sulbatsin should stop feeding by a breast.

Side effects:

Nausea, vomiting, diarrhea, rash, itch and other skin reactions, in exceptional cases – anemia, thrombocytopenia, an eosinophilia and a leukopenia, increase in alaninaminotranspherase (ALT) and aspartate aminotransferase (nuclear heating plant), a hyperbilirubinemia, pseudomembranous colitis are possible. Local reactions – pain in the place of injections are possible, at intravenous administration – phlebitis. Very seldom – an acute anaphylaxis.

Interaction with other medicines:

It is incompatible with aminoglycosides, tetracyclines, Amphotericinum, kl_ndom_tsiny, lincomycin, erythromycin, metronidazole, polymyxin B sulfate.

Aminoglycosides are inactivated when mixing with ampicillin therefore it is not necessary to mix them in one syringe.

At patients with gout at a concomitant use to Sulbatsin and Allopyrinolum the risk of development of skin reactions increases.

The concomitant use of a probenetsid leads to increase in concentration of ampicillin and a sulbaktam in blood and extends elimination half-lives of these drugs as a result of oppression of renal (canalicular) secretion.

Sulbatsin is unstable in the solutions containing a dextrose or other carbohydrates, it should not be mixed with blood preparations and hydrolyzates proteinaceous exactly.

Sulbatsin extends a prothrombin time and increases effect of coumarinic anticoagulants.

Contraindications:

Hypersensitivity to cephalosporins and penicillin, bronchial asthma, a lymphoid leukosis, an infectious mononucleosis.

Overdose:

It is shown by nausea, vomiting, diarrhea, spasms. Symptomatic therapy is recommended.

Storage conditions:

To store in the unavailable to children, dry and protected from light place, at a temperature not above 25 °C. A period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

0,75 g: each cardboard packaging contains 10 ml in the colourless bottle like I (USP) closed by a gray butylrubber stopper and sealed claret color by a protective aluminum cap with a cover.

1,5 g: each cardboard packaging contains 20 ml in the colourless bottle like I (USP) closed by a gray butylrubber stopper and sealed green color by a protective aluminum cap with a cover.