Зоперцин®

General characteristics. Structure:

Active ingredient: 4 g of a piperatsillin (in the form of sodium salt), 500 mg of a tazobaktam (in the form of sodium salt).

Pharmacological properties:

Pharmacodynamics. The combined antibacterial drug which includes пиперацилин – a semi-synthetic antibiotic of a broad spectrum of activity and to tazobakta – inhibitor the majority β-лактамаз.

Pharmacodynamics. The mechanism of action of a piperatsilin of sodium is caused by inhibition of synthesis of a wall of a cell, drug shows bactericidal activity. Tazobaktam of sodium is inhibitor β-лактамаз Richmoyda Saykesa ΙΙΙ a class: penicillinases and tsefalosporinaza. Tazobaktam in the recommended doses not an incentive of a chromosome β-lactamelements.

Presence of a tazobaktam considerably expands an action spectrum of a piperatsilin. The most part of strains of microorganisms which produce β-lactamelements is sensitive to a piperatsilina / tazobaktam and is resistant to a piperatsilin. Drug active concerning a wide range of bacteria:

- are sensitive (aerobic gram-positive bacteria) – Brevibacterium spp., Corynebacterium xerosis, Corynebacterium spp., Enterococcus durans, Enterococcus faecalis, Enterococcus spp., Gemella haemolysans, Gemella morbillorum, Lactococcus lactis cremoris, Propionibacterium granulosum, Propionibacterium spp., Staphylococcus aureus, Methicillinum - are sensitive, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus sciuri, Staphylococcus xylosus, Staphylococcus spp. (coagulase negative), Streptococcus agalactiae, Streptococcus anginosus, Streptococcus

- β-not hemolitic groups A. Streptococcus beta hemolitic groups D, Streptococcus constellatus, Streptococcus gordonii, Streptococcus intermedius, Streptococcus milleri, Streptococcus milleri-group, Streptococcus mitis, Streptococcus morbillorum, Streptococcus oralis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus sanguis, Streptococcus viridans, Streptococcus viridans group, Streptococcus spp.;

- are sensitive (aerobic gram-negative bacteria) – Acinetobacter anitratus, Acinetobacter lwoffii, Aeromonas sobria, Alcaligenens spp., Branhamella catarrhalis, Burkholderia cepacia, Citrobacter diversus, Citrobacter farmeri, Citrobacter freundii, Citrobacter koseri, Citrobacter spp., Eikenella corrodens, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp., Escherichia coli, Escherichia hermannii, Escherichia vulneris, Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus spp., Klebsiella ornithinolytica, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp., Morganella morganii, Pasteurella multocida, Proteus, indole positive, Proteus mirabilis, Proteus vulgaris, Proteus spp., Providencia stuartii, Providencia species, Pseudomonas aeruginosa, Pseudomonas fluorescens, Pseudomonas putida, Pseudomonas spp. Salmonella arizonae, Salmonella species, Serratia liquefaciens, Serratia marcescens, Serratia odorifera, Serratia spp., Shigella boydii, Shigella dysenteriae, Shigella flexneri, Shigella sonnei;

- are sensitive (anaerobic gram-positive bacteria) – Bifidobacterium spp., Clostridium bifermentans, Clostridium butyricum, Clostridium cadaveris, Clostridium clostridiforme, Clostridium difficile, Clostridium hastiforme, Clostridium limosum, Clostridium perfringens, Clostridium ramosum, Clostridium tertium, Clostridium spp., Eubacterium aerofaciens, Eubacterium lentum, Eubacterium spp., Peptococcus asaccharolyticus, Peptococcus spp., Peptostreptococcus anaerobius, Peptostreptococcus magnus, Peptostreptococcus micros, Peptostreptococcus prevotii, Peptostreptococcus species;

- are sensitive (anaerobic gram-negative bacteria) – Bacteroides caccae, Bacteroides capillosus, Bacteroides distasonis, Bacteroides fragilis, Bacteroides fragilis group, Bacteroides ovatus, Bacteroides putredinis, Bacteroides stercoris, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides ureolyticus, Bacteroides vulgatus, Bacteroides spp., Fusobacterium necrophorum, Fusobacterium nucleatum, Fusobacterium varium, Fusobacterium spp., Porphyromonas asaccharolytica, Porphyromonas gingivalis, Porphyromonas species, Prevotella bivia, Prevotella disiens, Prevotella intermedia, Prevotella melaninogenica, Prevotella oralis, Prevotella spp.;

- with intermediate sensitivity (aerobic gram-positive bacteria) – Enterococcus avium, Enterococcus faecium, Propionibacterium acnes;

- with intermediate sensitivity (aerobic gram-negative bacteria) – Acinetobacter baumannii, Acinetobacter calcoaceticus, Acinetobacter spp., Enterobacter aerogenes, Pseudomonas stutzeri, Stenotrophomonas maltophilia;

- resistant (aerobic gram-positive bacteria) – Corynebacterium jeikeium, Staphylococcus

- aureus (methicillin resistant), Staphylococcus coagulase negative (methicillin resistant).

Pharmacokinetics. All indicators of pharmacokinetics at separate and combined use of a piperatsilin and tazobaktam were odnotipn.

Adsorption. After intravenous administration peak concentration of a piperatsilin and tazobaktam in plasma arises immediately. After introduction of 4 g of a piperatsilin of sodium peak concentration in plasma makes 298 mkg/ml.

After introduction of 500 mg of a tazobaktam of sodium peak concentration in plasma – 34 mkg/ml.

Absorption. The maximum concentration in plasma (With max) is reached at once after intravenous (in/in) an injection.

Distribution. Linkng with proteins is inherent both for a piperatsilin and for a tazobaktam and is equal to about 30%. Piperatsilin and to tazobakta randomly extend, including in lungs, female reproductive organs (a uterus, ovaries, fallopian pipes), a gall bladder, bile, a mucous membrane of intestines, intersticial liquid. Concentration in fabrics in general makes from 50% to 100% compared with plasma. Distribution of a piperatsilin and tazobaktam in cerebrospinal liquid is low in a case absence an inflammation of covers of a brain.

Metabolism. Piperatsilin is metabolized to a dezetilovy metabolite which shows antimicrobic activity. Tazobaktam is metabolized to a single metabolite that shows pharmacological and antibacterial activity.

Removal. Time of semi-removal of a piperatsilin and tazobaktam from plasma makes from 0,7 hour to 1, 2 hours. Piperatsilin and to tazobakta are removed through kidneys by means of glomerular filtering and tubular secretion. Piperatsilin is brought quickly as is not exchange medicine. 68% of a dose are removed with urine. Tazobaktam and his metabolites are brought in the basic (to 80%) through kidneys. Half-life (T1/2) at healthy volunteers makes from 36 min. to 72 minutes.

At patients with cirrhosis half-life (T1/2) of a piperatsilin grows for 25% and a tazobaktam – for 8%.

Indications to use:

Moderately severe infections, the caused strains, sensitive to drug:

- lower respiratory tract infections;

- infections of an urinary system;

- not complicated and complicated infections of skin and soft tissues (abscess, the infected trophic ulcers);

- infectious and inflammatory diseases of a basin or puerperal infections (including endometritis);

- the appendicitis (complicated by a rupture of an appendix, peritonitis and/or

to abscessings);

- septicaemia.

Route of administration and doses:

The way and dose are defined individually in each case depending on a current and localization of an infection. It is applied only intravenously slowly struyno or kapelno. For adults and children 12 years an average daily dose are more senior makes 12 g of a piperatsilin and 1,5 g of a tazobaktam, that is 4, 5 g of Zopertsin each 8 hours.

For patients with a renal failure doses are recommended: at clearance of creatinine> 20-80 ml/min. - 4,5 g each 8 h, at clearance of creatinine <20 - 4,5 g each 12 h.

For patients who are on a hemodialysis the maximum dose of Zopertsin makes 2, 25 g every the 8th hour. As in the period of a hemodialysis 30% – 40% of Zopertsin in 4 hours are removed, apply one additional dose of 2 g of a piperatsilin and 0,25 g of a tazobaktam after everyone to dialysis session. (daily dose of 8 g of a piperatsilin and 1 g of a tazobaktam). For patients with a renal failure control Zopertsin's concentration in plasma that allows to regulate necessary a drug dose.

Duration of treatment makes from 7 to 10 days. The recommended duration of use of drug at hospital pneumonia makes from 7 to 14 days. In other conditions therapy is conducted depending on weight of an infection, clinical and bacteriological progress and efficiency of treatment.

For preparation of solution for intravenous administration as solvent 0, 9% use solution of sodium of chloride, 5% dextrose solution, sterile water for injections. For intravenous administration struyno bottle contents that includes 4, 5 g of drug, part in 20 ml of one of the solutions stated above. Stir up before full dissolution. Substance is dissolved completely, without leaving any unallotted rest. The dose should be entered within 3 – 5 minutes.

For intravenous administration kapelno contents of a bottle which includes 4, 5 g of drug are parted in 20 ml 0, by 9% of solution of sodium of chloride, the solution further received is dissolved in 50 ml of one of the specified solutions, or in 5% dextrose solution in water, or in mix of 5% of solution of a dextrose and 0, 9% of sodium of chloride. Stir up before full dissolution. Substance is dissolved completely, without leaving any unallotted rest the Dose it is necessary to enter within 30 minutes.

Features of use:

At use of drugs of penicillinic group serious reactions of hypersensitivity of drugs were observed that demanded immediate medical care using Epinephrinum, oxygen, intravenous administration of steroids and an intubation of respiratory tracts.

In case of developing of heavy persistent diarrhea it is necessary to consider a possibility of development of the pseudomembranous coloenteritis caused by an aggressive strain of Clostridium difficile (NAP1/027) which expressed toxicity it is probably connected with raised by production of toxins A and B. In case of this complication it is necessary to cancel drug and to appoint orally тейкопланин or Vancomycinum.

At patients with a renal failure who applied beta лактамные antibiotics including пиперацилин, took place of a deviation of indicators of coagulation, such as hour of coagulation, aggregation of thrombocytes and formation of thrombin. It can precede emergence of bleedings.

At emergence of symptoms coagulation disturbance, use of drug has to be stopped and the picked-up corresponding therapy.

At prolonged treatment it is necessary periodically kontrolyuvavt function of kidneys, a liver.

When using penicillin, including the piperatsilina at patients with cystous fibrosis, can be observed temperature increase and a rash.

Pregnancy and lactation. During pregnancy Zopertsin it is possible to apply only when the expected advantage exceeds potential risk for a fruit.

Zopertsin in insignificant concentration is brought with breast milk therefore to use drug at women who nurse perhaps only when the expected advantage exceeds potential risk for the child, or to stop feeding by a breast.

Children's age. In sufficient a measure safety and efficiency of use is not established to piperatsilin/tazobakta at children 12 years are younger.

With care appoint Zopertsin to patients age is more senior than 65 years.

During treatment not to take alcohol.

Ability to influence directly speed of response when driving by motor transport or other mechanisms is not established so far. In case of side reactions – see. "Side effect" (dizzinesses, convulsion and another) should refrain from driving by motor transport or other mechanisms.

Side effects:

From a digestive tract – diarrhea, a lock, nausea, vomiting.

From the central nervous system – the alarm, concerns, sleeplessness, a headache, in isolated cases are possible a tremor, convulsions, dizziness.

From cardiovascular system – increase in arterial pressure, hypostases, a stethalgia, in isolated cases are possible hypotension, tachycardia, arrhythmia.

Allergic reactions – a rash, an itch;

From respiratory system – an asthma

Interaction with other medicines:

Simultaneous use of Zopertsin with heparin can cause disturbance of system of blood coagulation. Simultaneous use of Zopertsin with Tobramycinum reduces the area under a curve "concentration time" by 11%, renal clearance – for 32%.

Simultaneous use of a vankuronium together with Zopertsin leads to prolongation of neyromuskulyarny blockade. Probenetsid increases time drug semi-removal Zopertsin.

Zopertsin do not mix with other medicines in the syringe or an infusional bottle as their compatibility it is not finished. Zopertsin can be applied along with other antibiotics, but medicines have to be entered separately.

Results of bench tests at patients who apply piperatsilin/to tazobakta have to be interpreted carefully with confirmations by other diagnostic methods.

Contraindications:

Zopertsin of contraindications the patient with allergic reactions to any penicillin, cephalosporins or inhibitors β-lactamelements.

Overdose:

Zopertsin belongs to penicillinic group and can be the cause of neuromuscular excitement or convulsion, owing to intravenous administration of a high dose (especially at patients with a renal failure). In these cases therapy symptomatic. High concentration of a piperatsilin and tazobaktam can be reduced by means of a hemodialysis. There is no specific antidote.

Storage conditions:

To store at a temperature not above 25 °C in protected from light and the place, unavailable to children. A period of validity - 2 years. After dissolution of drug in sterile water for injections solution keeps the activity 24 hours at a temperature of 20 - 25 °C or 48 watch at a temperature of 2 - 8 °C.

Issue conditions:

According to the recipe

Packaging:

4.5 - bottles glass (1) - boxes cardboard.
4.5 - bottles glass (50) - boxes cardboard.