AZARAN
Active material: Ceftriaxone
When ATH: J01DD04
CCF: III generation cephalosporins
ICD-10 codes (testimony): A02, A03, A39, A40, A41, A54, A69.2, G00, i33, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J85, J86, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M00, M86, N10, N11, N15.1, N30, N34, N41, N70, N71, N72, N73.0, Z29.2
Manufacturer: HEMOFARM A.D. (Serbia)
Pharmaceutical form, composition and packaging
Powder for solution for I / O, and the / m from white to white with a yellowish tint.
| 1 fl. | |
| ceftriaxone (sodium salt) | 1 g |
Bottles of colorless glass (1) – packs cardboard.
Bottles of colorless glass (10) – packs cardboard.
Bottles of colorless glass (50) – packs cardboard.
Pharmacological action
Cephalosporin antibiotic III generation broad-spectrum parenteral. Effective bactericidal, oppressing synthesis of cell walls of bacteria. Acetiliruet membrane-transpeptidaza, Turkey thus cross-lacing peptidoglikanov, necessary to ensure strength and rigidity of the cell wall. Resistant against β-lactamases, produced by most gram-positive and gram-negative bacteria.
It is active against gram-positive aerobic bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis; Gram-negative aerobic bacteria: Asinetobacter lwoffii, Asinetobacter anitratus, Aeromonas hydrophila, Alcaligenes faecalis, Alcaligenes odorans, Citrobacter spp., Enterobacter spp., (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (incl. strains, penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (incl. Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (incl. strains, penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus is wonderful, Proteus vulgaris, Providencia spp., Salmonella spp. (incl. Salmonella typhi), Serratia spp. (incl. Serratia marsescens), Shigella spp., Vibrio spp. (incl. Vibrio cholerae), Yersinia spp. (incl. Yersinia enterocolitica), Pseudomonas aeruginosa (Some strains of); Gram-negative anaerobic bacteria: Bacteroides spp. (incl. some strains of Bacteroides fragilis), Clostridium spp. (other than Clostridium difficile), Fusobacterium spp. (In addition to Fusobacterium mortiferum and Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.
C drug resistant Methicillin-resistant strains of Staphylococcus spp., strains of Enterococcus spp. (Enterococcus faecalis), Clostridium difficile, many strains of Bacteroides spp. (продуцирующие b-лактамазы).
Pharmacokinetics
Absorption and distribution
After the/m introduction ceftriaxone quickly and completely absorbed in the blood system. It penetrates the tissues and liquid body Wednesday: Airways, bones, joints, mochevyvodjashhij tract, skin, subcutaneous and abdominal organs. When nerve meningealnah membranes it penetrates into spinnomozgovu liquid. Ceftriaxone bioavailability with the/m introduction is 100%.
When the/m in a dose of ceftriaxone 500 mg 1 г Cmax in plasma is 38 ug / ml 76 ug / ml, respectively, at / in a dose 500 mg, 1 and g 2 g – 82 ug / ml, 151 ug / ml 257 ug / ml, respectively. In adults through 2-24 hours after administration at a dose 50 mg/kg concentration in cerebrospinal fluid is many times superior to the IPC for the most common causative agents of meningitis.
The equilibrium is established within 4 days of application.
Reversible binding to plasma proteins (albumin) is 83-95%.
Vd is 5.78-13.5 l (0.12-0.14 l / kg), children – 0.3 l / kg.
Penetrates through the placental barrier in small quantities.
Deduction
T1/2 is 6-9 no, allowing you to use the drug 1 time / day.
Plasma clearance- 0.58-1.45 l /, Kidney klirens- 0.32-0.73 l /.
In adult patients for 48 no 50-60% the drug is excreted by the kidneys unchanged, 40-50% excreted with jelchew in intestine, where biotransformiroetsa in the inactive metabolite.
Pharmacokinetics in special clinical situations
The baby's kidneys excreted about 70% product.
In newborns and the elderly (the age 75 years), as well as in patients with the human kidney and liver t1/2 significantly increased.
Patients, hemodialysis (CC 0-5 ml / min), T1/2 is 14.7 no; at CC 5-15 ml / min – 15.7 no; at CC 16-30 ml / min – 11.4 no; at CC 31-60 ml / min – 12.4 no.
In children with meningitis t1/2 after / in a dose of 50-75 mg/kg is 4.3-4.6 no.
Ceftriaxone is not displayed during hemodialysis.
Testimony
Treatment of infectious and inflammatory diseases, caused by susceptible microorganisms:
- Infections of the upper and lower respiratory tract (incl. pneumonia, lung abscess, empyema);
- Infections of the skin and soft tissues;
- Bone and joint infections;
- Urinary tract infections (incl. pyelonephritis);
-inflammatory diseases of the INTESTINE and biliary tract (incl. kholangit, gallbladder empyema);
- Pelvic infection;
- Peritonitis;
- Bacterial meningitis;
- Bacterial endocarditis;
- Sepsis;
acute uncomplicated gonorrhea;
- Lyme disease;
-Shigella;
-salmonellosis.
Prevention and treatment of infectious post-operative complications.
Dosage regimen
The drug is injected in/m or/in struino or drip.
To adults and children over 12 years the average daily dose is 1-2 g 1 time / day. The maximum daily dose for adults – 4 g.
To infants up to the age of 14 days dose of 20-50 mg / kg / day. The maximum daily dose 50 mg / kg.
To children aged 15 days and up to 12 years daily dose is 20-80 mg / kg.
Children weighing more 50 kg prescribed dose for adults.
The daily dose 50 mg/kg or more should be applied in the form of infusions over 30 m.
The course duration is typically less than 10 d. The introduction of the drug should continue for 2-3 days after the normalization of body temperature and symptoms disappear.
To Prevention of postoperative infections the drug is injected once per 30-90 minutes before the start of the operation in a dose 1-2 g (Depending on the degree of infection risk). When operating interventions on the colon and rectum are recommending additional introduction of the drug from a group 5-nitroimidazolov.
At bacterial meningitis in infants and young children dose of 100 mg / kg 1 time / day. The maximum daily dose - 4 g. Duration of therapy depends on the type of pathogen and can range from 4 days with meningitis, caused by Neisseria meningitidis, to 10-14 days with meningitis, caused by susceptible strains of Enterobacteriaceae.
At acute uncomplicated gonorrhea the drug is injected in/m one dose 250 mg.
At Lyme disease appointed adults and children dose 50 mg / kg 1 time / day, the maximum daily dose – 2 g. Length of treatment – 14 days.
In patients with impaired renal function dose adjustment is required only if severe renal insufficiency (CC less than 10 ml / min), in this case, the daily dose of ceftriaxone should not exceed 2 g.
In patients with impaired renal function no need for dose adjustment, If liver function remains normal.
In patients with impaired liver function no need for dose adjustment, If kidney function remains normal.
At combined renal failure and liver failure should regularly monitor the concentrations zeftriakson plasma and adjust his dose.
Patients, hemodialysis, additional introduction after dialysis is not required, tk. ceftriaxone is not removed with hemodialysis. Speed out of ceftriaxone in these patients may vary, Therefore, you should monitor the concentration of ceftriaxone in plasma for possible dose adjustment.
Rules of preparation and introduction solution for injection
Preparation of the solution for the on/m introduction
1 g of drug dissolved in 3.6 ml water for injection, 1 ml of the resulting solution contains about 250 mg of ceftriaxone. Optionally, you can use a more diluted solution.
1 g of drug dissolved in 3.5 ml 1% lidocaine solution of chloride. Enter deeply into relatively large muscle (in the gluteus muscle or the muscle of thigh). Do not enter more 1 g in one muscle. It should be remembered, that solution of lidocaine chloride/386/1989.
Preparation of the solution for the on/in the injection
1 g of drug dissolved in 9.6 ml of sterile water for injection, 1 ml of the resulting solution contains about 100 mg of ceftriaxone. Solution give/in slowly over 2-4 m.
Preparation of the solution for the on/in infusions
2 g of drug dissolved in 40 ml of one of the solutions, not containing calcium (0.9% sodium chloride solution; 0.45% sodium chloride solution + 2.5% Dextrose; 5% Dextrose; 10% Dextrose; 6% solution of dextran in 5% dextrose; 6-10% solution of the hydroxyethyl starch). The on/in infusion duration of not less than 30 m.
Freshly prepared solutions of zeftriakson stable during 6 hours at room temperature and during the 24 h when stored in the refrigerator at a temperature from 2° to 8° c.
Side effect
CNS: headache, dizziness.
From the urinary system: impairment of renal function (azotemia, increasing urea in the blood, giperkreatininemiя, glycosuria, цilindrurija, hematuria, oligurija, anurija).
From the digestive system: nausea, vomiting, taste disturbance, flatulence, stomatitis, glossitis, diarrhea or constipation, pseudomembranous enterocolitis, psevdoholelitiaz (sludge syndrome), dysbiosis, abdominal pain, increase in liver transaminases and alkaline phosphatase, giperʙiliruʙinemija, cholestatic jaundice.
From the hematopoietic system: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytopenia, thrombocytosis, ʙazofilija, gemoliticheskaya anemia.
From the blood coagulation system: hypocoagulation, reduction of plasma clotting factors (II, VII, IX, X), nose bleed, increased prothrombin time.
Allergic reactions: hives, rash, itch, fever, chills; rarely – bronchospasm, swelling, eozinofilija, mnogoformnaya Erythema ekssoudatus (incl. Stevens-Johnson syndrome), anaphylactic shock, serum sickness.
Local reactions: at / in the introduction – phlebitis, pain along the vein; when i / m administration – tenderness at the injection site.
Other: superimposed infection (incl. candidiasis).
Contraindications
- Hypersensitivity to the drug;
- Hypersensitivity to other cephalosporins, penicillin and carbapenems.
FROM caution assign product in human liver and/or kidney disease, premature and newborn infants with hyperbilirubinemia, When NSU, as well as in jenterite or colitis, involving the use of antibacterial drugs.
Pregnancy and lactation
Use Azarana when pregnancy is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus (ceftriaxone penetrates through the placental barrier).
If necessary, the use of Azarana during lactation should decide on the termination of breastfeeding (ceftriaxone is secreted in breast milk).
Cautions
The drug is applied only in a hospital environment.
While severe kidney and liver failure in patients, hemodialysis, should regularly monitor the concentration of ceftriaxone in plasma.
Long-term treatment should be regularly monitored picture peripheral blood, the functional state of the liver and kidneys.
In rare cases, the gallbladder ultrasound marked blackout, that disappear after the drug (even if this phenomenon is accompanied by pain in the right hypochondrium, recommend to continue appointment of antibiotic and symptomatic treatment of conduction).
In applying the drug not to consume ethanol, tk. Perhaps the disul'firamopodobnyh effects (redness of the face, spasticskie pains in the abdomen and stomach, nausea, vomiting, headache, decrease in blood pressure, tachycardia, breathlessness).
Against the backdrop of Azarana elderly and immunocompromised patients may need a vitamin k.
Despite a detailed medical history, that is the rule and for other cephalosporin antibiotics, You cannot exclude the possibility of development of anafilaticheskogo shock, that requires immediate therapy: first give/epinephrine, then – GCS.
Studies in vitro have shown, that like other zefalosporynam, ceftriaxone is able to displace bilirubin, associated with serum albumin. Therefore, the newborn with hyperbilirubinemia and, especially in preterm infants, use of ceftriaxone requires even more care.
Overdose
Currently, the cases of drug overdose Azaran not reported.
Treatment: symptomatic therapy. No specific antidote. For deducing from an organism of ceftriaxone Hepatology and peritonealny dialysis is not effective.
Drug Interactions
Ceftriaxone and aminoglycosides have synergistic against many Gram-negative bacteria (incl. Pseudomonas aeruginosa), drugs should be entered separately in the recommended doses.
Ceftriaxone, suppressing intestinal flora, inhibits the synthesis of vitamin k. Therefore, while the use of drugs, reduces platelet aggregation (NSAIDs, salicilaty, sulfinpirazon), It increases the risk of bleeding.
Together with the use of anticoagulants increasing antikoaguljantnogo action.
Together with the application “loop” dioretikami and other nefrotoksicnami drugs increases the risk of nefrotoksicski action.
The drug is not compatible with ethanol.
Pharmaceutical interaction
Pharmaceutically compatible with solutions, containing other antibiotics (incl. Vancomycin and aminoglycosides) and solutions, containing fluconazole.
Ceftriaxone should not be confused with solutions, containing calcium (incl. with Ringer solution).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, dark place at a temperature of 15 ° to 25 ° C. Shelf life – 3 year.
