Azlocillin 2 g.

QUALITATIVE AND QUANTITATIVE COMPOSITION
azlocillin sodium l, 048 g Eq. of AZLOCILLIN lg azlocillin sodium 2,096 g Eq. of AZLOCILLIN 2g azlocillin sodium 5,240 g Eq. of AZLOCILLIN 5g
 
3 PHARMACEUTICAL FORM
powder for injection
 
 
4 CLINICAL DATA
4.1 Indications
AZLOCILLIN be used to treat infections caused by Pseudomonas aeruginosa and other infections caused by microorganisms susceptible to the antibiotic of the following location:
♦ airway - bronchitis, pneumonia, lung abscess, etc. .;
♦ urogenital infections - cystitis, cystopyelitis, pyelonephritis, prostatitis, epididymitis, etc. .;
♦ infections of the bone and joints - osteomyelitis, osteitis, etc..
♦ serositis -meningit; peritonitis; endocarditis; pleurisy;
♦ infections of skin and soft tissue;
♦ infected extensive burns;
♦ biliary infections;
♦ brain abscess; abdominal abscesses, etc. .;
♦ infections in patients with immunodeficiency;
♦ septic conditions.
 
 
4.2. DOSAGE AND RANK OF USE
AZLOCILLIN given intravenously - such as direct injection or infusion. Rarely resorted to because of the high intramuscular single dose, solubility and restrictions on the size of the injection volume.
Adults - usual dose for moderate and urinary infections 2g 6-8 hours. In life-threatening infections 5g every 6-8 hours. The maximum daily dose is 24g.
 
Children - 1-14 years - 75 mg / kg every 8 hours; 2-12 months - 100 mg / kg per 8 hours;
newborns - 100 mg / kg per 12 hours;
Premature - 50 mg / kg per 12 hours;
 
In patients with impaired renal function, a dose reduction as follows:
- If creatinine clearance 10-30 ml / min - 1.5g of 8-12 hours at a UTI and 2g of 8 hours when other serious infections;
- If creatinine clearance less than 10 ml / min - 1.5g of 12 hours at UTI and 2 g per 12 hours in other serious infections,
- In hemodialysis patients - 3g after each dialysis, then every 12 hours for 3g.
The duration of treatment depends on the severity of the infection, and at least 3 days following the disappearance of clinical symptoms of the disease.
 
 
4.3. CONTRAINDICATIONS
Known hypersensitivity to the antibiotic penicillin.
 
 
4.4. SPECIAL WARNINGS AND SPECIAL PRECAUTIONS FOR USE
Before any new course of treatment AZLOCILLIN, the patient should be carefully examined to determine whether he had previous hypersensitivity reactions to AZLOCILLIN, other penicillins, cephalosporins, or other drugs.
In the absence of an allergic history should be done scarification skin sample solution preparation, and for a history of allergy initially performed epicutaneous test and if it is negative is done scarification sample. Samples were read after 30 minutes.
In case of severe acute hypersensitivity reactions require application of epinephrine or 0,1 mg - 0,5mg subcutaneous adrenaline, intravenous infusion of corticosteroid preparations antihistamine (parenteral) novphylline and selective beta-mimetic in bronchospasm, oxygen, respiration if necessary and intubation.
Caution is advised and medical surveillance after the first injection in patients hypersensitive to cephalosporins, griseofulvin, penicillamine (cross-allergy). In patients with allergic diathesis napr.bronhialna asthma, hay fever, urticaria AZLOCILLIN (like all penicillins) should be used with caution.
If there is a form of allergy nyakakva- recommended to stop the use of the drug.
AZLOCILLIN should not be administered less than 5 minutes as an intravenous infusion was accompanied by a transient discomfort in the chest area.
AZLOCILLIN, as all antibacterial agents, increasing the risk of excessively developed a sensitivity to microorganisms and the development of fungal infections (candidiasis), usually during prolonged therapy. In the presence of such infection Appropriate therapy.
Be considered quantitative sodium (»50 mg / g) in preparation when applying to patients with restriction of sodium in the diet. Recommended verified electrolyte balance, especially in renal failure, liver cirrhosis and in the neonatal period.
During treatment with AZLOCILLIN may be a transient increase in serum aminotransferase, lactate dehydrogenase, alkaline phosphatase, bilirubin, creatinine, and a reduction in serum uric acid (probenecid-like effect). May be falsely positive for the reactions of sugar in the urine (using reduction methods), protein in the urine and direct test of Coombs.
 
 
4.5. DRUG INTERACTIONS AND OTHER
Probenecid increases and prolong the plasma concentration of AZLOCILLIN.
Concomitant use of AZLOCILLIN and cefotaxime, the total body clearance of the latter is reduced in patients with normal and reduced renal function, which requires a reduction in the dose of cefotaxime, due to the risk of developing metabolic encephalopathy or seizures, especially in patients treated with high doses AZLOCILLIN and impaired renal function. In some patients receiving beta-lactam antibiotics occurs bleeding and coagulation tests were abnormal. More likely is that to occur in patients with renal impairment.
Co-administration of ciprofloxacin AZLOCILLIN parenterally, resulting in higher plasma concentrations and prolonging of ciprofloxacin.
In the combined administration of AZLOCILLIN and heparin and other anticoagulants observed prolongation of bleeding time. Avoid concomitant use of potentially hepatotoxic drugs.
 
 
4.6. Pregnancy and lactation
Safety of AZLOCILLIN pregnant has not been established, so it is recommended to avoid its use during pregnancy unless urgent indications. Caution should be exercised when applying AZLOCILLIN lactating women, as is excreted in low concentrations in human milk.
 
 
4.7. EFFECTS ON THE ABILITY TO DRIVE AND USE MACHINES
Application of AZLOCILLIN not affect the ability to drive or operate machinery.
 
4.8. SIDE EFFECTS
♦ allergic reactions - skin rash, pruritus, urticaria, arthralgia, myalgia, drug fever, rhinitis, bronchospasm, angioedema, anaphylactic shock (see PRECAUTIONS) and serum sickness;
♦ gastrointestinal effects - nausea, vomiting, diarrhea, oral candidiasis;
♦ haematological - are rarely observed transient haematopoietic disorders, reversible neutropenia (most often in patients treated over 2 weeks), thrombocytopenia, leukopenia, eosinophilia, reduction of hemoglobin or hematocrit prolonged prothrombin time or bleeding;
♦ local - rarely thrombophlebitis, pain, erythema, irritation -Short on veins (at concentrations of solutions greater than 10%).
 



4.9. OVERDOSE
When an overdose of antibiotics can be observed convulsions and other signs of toxicity (dizziness, paresthesia, headache) of the central nervous system. In case of overdose (especially in the application of high doses in patients with renal failure) use of the preparation is interrupted. If necessary, appoint anticonvulsant therapy. AZLOCILLIN removed by hemodialysis and less by peritoneal dialysis.
 
 
5 Pharmacological
ATC code: J01CA09.
Anti-infective agents for systemic use. Beta-lactam antibacterial agents, penicillins. Penicillins with a broad spectrum of action.
 
 
5.2. FARMLKODINLMICHNI PROPERTIES
AZLOCILLIN is a semisynthetic broad-spectrum penicillin group atsilureidopenitsilinite. Exhibits bactericidal activity against proliferating microorganisms, by suppressing the biosynthesis of the cell wall level transpeptidase enzymes. The antibacterial spectrum of AZLOCILLIN includes a large number of Gram-negative microorganisms, such as especially active is against Pseudomonas aeruginosa, including to some carbenicillin resistant strains.
Sensitive to the effects of the antibiotic from the groups of microorganisms Klebsiella, Enterobacter, Citrobacter, Serratia (Bkl..S.marcescens), Escherichia coli, Haemophilus influenzae, Bacteroides, some strains of Proteus (P.mirabilis, P.vulgaris, P.rettgeri, P.morganii), Neisseria gonorrhoeae, Neisseria meningitidis. A large number of Gram-positive micro - Streptococcus sp., Staphylococcus sp., Pneumococcus sp., Enterococcus sp., Corynebacterium sp. and Clostridium sp. are sensitive to AZLOCILLIN.
AZLOCILLIN inactivated by most beta-lactamases, and a large number of beta-laktmazoprodutsirashti microorganisms are resistant. Cross-resistance with some of the other antipseudomonal penicillins.
 
 
5.2. Pharmacokinetic properties
AZLOCILLIN exhibits nonlinear dose-dependent pharmacokinetics. Upon intravenous administration of doubling. dose plasma concentrations were more than twice. Approximately 20-40% of the antibiotic is bound to plasma proteins. The biological half-life of about 1 hour.
In neonates and patients with renal insufficiency it is extended and can reach 2 to 6 hours. The plasma concentration of AZLOCILLIN increases and prolong the concomitant use of probenecid.
AZLOCILLIN is well distributed in body tissues and fluids, bile, surgical wound and bronchial secretions, urine, sputum, accumulates in the bones. In small amounts penetrate the CSF, except for cases of inflamed meninges. Crosses the placental barrier. Metbolizira a very small extent. About 50-70% of AZLOCILLIN is excreted unchanged by the kidneys by glomerular filtration and tubular secretion to 24 hours after administration.
In normal liver function, approximately 20-25% of applications AZLOCILLIN is excreted unchanged in the bile. At low concentrations excreted in breast milk. AZLOCILLIN removed by hemodialysis.
 
 
5 3 Preclinical safety data
Single dose (LD5o) was studied on white mice and rats for a period of observation of 20 days. For a single intramuscular administration to mice LD50> 5000 mg / kg and rats LD5o>! 0000 mg / kg. When administered intravenously to mice LD50 = 3452 mg / kg and rat - 1375 mg / kg. Species have been identified differences between experimental animals as rats showed a higher sensitivity.
Sexually pronounced differences have not been established. In rabbits (ivprilagane) LD50> 5000 mg / kg for dogs and -LD50> 2000 mg / kg.
The data show that AZLOCILLIN has low toxicity. Subacute toxicity was studied after intravenous 15 - day treatment of dogs "Beagle" with a dose of 800 mg / kg. Results showed no abnormalities in the studied clinical hematological and histological parameters.
Experiments on rats teratogenicity and embryotoxicity treated from 4th to 19th day of gestation with intramuscular AZLOCILLIN indicate that doses up to 1500 mg / kg did not result in teratogenic and embryotoxic effect.
Due to insufficient information on the effects of pregnancy, antibiotic recommended for reservation only in severe infections such as sepsis.
No evidence of mutagenic activity of the antibiotic.
 
 
6 PHARMACEUTICAL PARTICULARS
6.1. LIST OF OTHER SUBSTANCES AND THEIR QUANTITIES:
Finished dosage form contains no excipients.
 
 
6.2. Incompatibilities
Incompatibility was observed in in vitro mixing between AZLOCILLIN and aminoglycosides, ciprofloxacin, metronidazole, and tetracyclines.
Due to possible interactions with other AZLOCILLIN preparations in vitro is not desirable to mix them in the same syringe.
The combination of AZLOCILLIN with aminoglycoside antibiotics with administration, they should not be mixed in the same syringe or infusion because of the risk of inactivation and need to bring in different places in 1 hour intervals.
 
 
6.3. SHELF LIFE
Three (3) years from date of manufacture.
 
 
6.4. STORAGE CONDITIONS
Dry and protected from light, at temperatures below 25 ° C. Keep out of reach of children!
 
 
6.5. PHARMACEUTICAL FORM AND CONTENTS
Colorless glass vials of 30 ml in lg and 2g and 50 ml in 5g.
 
 
6.6. RECOMMENDATIONS FOR USE
The product subject to medical prescription and dosage, dosing interval and duration of treatment prescribed by the doctor.
 
 
Preparation of solutions
- For direct intravenous injection - per gram AZLOCILLIN dissolves at least 10ml of sterile water for injection, 5% dextrose or 0.9% sodium chloride. Shake vigorously to dissolve. To avoid irritating effect on veins, the final concentration of the antibiotic may not be greater than 10%). Injected slowly over no less than 5 minutes per gram AZLOCILLIN. Solutions of AZLOCILLIN are clear, colorless to pale yellow, and retain its activity for 6 hours at a single-acting, and if necessary by simultaneous RT. It is recommended, however, the reconstituted solution can be administered as soon as possible.

- Intravenous Infusion - prepared for direct intravenous injection solution was diluted with 50 to 100ml infusion -0.9% sodium chloride solution, 10% dextrose solution, Ringer's solution or 5% solution of laevulose. Time entry for 20-30 minutes. The preparation should not be used after the expiry date stated on the packaging.