Ceftriabol - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic III generation of a broad spectrum of action for parenteral administration. Bactericidal action is due to irreversible binding to bacterial transpeptidases, which leads to disruption of the final stages of cell wall synthesis of microorganisms. It is characterized by resistance to the action of most beta-lactamases of gram-negative and gram-positive microorganisms.

Ceftriaxone is active against the following microorganisms:

Gram-positive aerobes - Staphylococcus aureus (including strains producing penicillinases), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups viridans;

Gram-negative aerobes - Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including beta-lactamase resistant strains resistant to ampicillin), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae) Moraxella catarrhalis (including beta-lactamase producer strains), Morganella morganii, Neisseria gonorrhoeae (including strains producing and non-producing penicillinases), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens), Pseudomonas aeruginosa (individual strains);

anaerobes - Bacteroides fragilis, Clostridium spp. (Besides FROM. difficile), Peptostreptococcus spp.

Has activity in vitro for most strains of the following microorganisms, although the clinical significance of this is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp. (including Providencia rettgeri), Salmonella spp. (including S. typhi), Shigella spp., Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus. Many strains of the above gram-positive and gram-negative microorganisms resistant to cephalosporins I-II generations, natural and semisynthetic penicillins, aminoglycosides, are sensitive to ceftriaxone.

Resistant to ceftriaxone: methicillin-resistant Staphylococcus spp., Enterococcus faecalis and Enterococcus faecium, Listeria monocytogenes.

Pharmacokinetics:

The main pharmacokinetic parameters, except the half-life (T1 / 2), depend on the administered dose.After 1/2 hour after a single intravenous (iv) injection, 0.5 g, 1 g and 2 g of the preparation concentration in serum are 82 mg / l, 151 mg / l and 257 mg / l, respectively. After 2 hours, the concentrations decrease, respectively, to 48 mg / L, 67 mg / L and 154 mg / L. After 24 hours, the serum concentrations are 5 mg / L, 9 mg / L and 15 mg / L. After intramuscular (intramuscular) administration of ceftriaxone in a dose of 0.5 g and 1 g, the maximum concentrations were observed 2 hours after the injection and were 38 mg / L and 81 mg / L, respectively. Bioavailability with the / m introduction is 100%. With repeated intravenous or / m administration, cumulation of the drug in the blood plasma is observed. After IV or IM injections ceftriaxone quickly penetrates into various fluids and body tissues in concentrations exceeding the minimum inhibitory concentrations (MICs) for sensitive microorganisms. For a minimum of 24 hours after administration, concentrations above the MIC are observed in the lungs, heart, bile and biliary tract, liver, palatine tonsils, middle ear, nasal mucosa, bones, as well as cerebrospinal, synovial, pleural, peritoneal and prostatic secretions.Well penetrates into the cerebrospinal fluid with inflammation of the meninges. In small concentrations penetrates into breast milk. Ceftriaxone reversibly binds to plasma albumins, the binding rate decreasing with increasing concentration, reaching 95% with an antibiotic concentration of less than 25 mg / L and decreasing to 85% at a concentration of 300 mg / L.

Ceftriaxone has a double elimination route. From 33% to 67% of the administered dose is excreted by the kidneys in unchanged form. The rest is excreted unchanged with bile, is converted into the intestine into inactive metabolites and released through the intestine. Concentrations of ceftriaxone in bile are many times higher than serum. T1 / 2 ceftriaxone in adults with normal liver and kidney function is 5.8 to 6.7 hours. T1 / 2 from the middle ear fluid is 25 hours. In neonates, about 70% of the administered dose is excreted through the nights. If there is a violation of the liver and kidneys, the pharmacokinetics of ceftriaxone varies only slightly: if the kidney function is impaired, the drug increases with bile; on the contrary, if liver function is impaired, elimination through the kidneys increases.In patients older than 75 years, T1 / 2 increases by 2-3 times.

Indications:Bacterial infections caused by susceptible to ceftriaxone pathogens: bacterial septicemia, bacterial meningitis; infections of the abdominal cavity organs (including peritonitis, inflammatory diseases of the gastrointestinal tract and bile ducts, including cholecystitis, cholangitis, gallbladder empyema), infectious and inflammatory diseases of the pelvic organs (including salpingoophoritis, endometritis, parametritis, pelvioperitonitis); infections of the lower respiratory tract, including pneumonia, pleural empyema, lung abscess; acute otitis media; infection of bones and joints, including infectious (septic) arthritis, osteomyelitis; infections of the skin and soft tissues (including infected wounds and burns); uncomplicated and complicated infections of the kidneys and urinary tract (acute and exacerbation of chronic pyelonephritis, pyelitis); Uncomplicated gonorrhea, Lyme disease. Infectious diseases in persons with weakened immunity. It is indicated for perioperative antibiotic prophylaxis.

Contraindications:Hypersensitivity (incl.to other cephalosporins, penicillins, carbapenem); Hyperbilirubinemia in newborns, newborns, which showed iv administration of solutions containing Ca2 +.

Carefully:In premature newborns; with renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy, lactation.

Pregnancy and lactation:

The use of ceftriaabol in pregnant women is possible in cases where the intended benefit to the mother exceeds the potential risk to the fetus, and should be monitored by a specialist. For the period of ceftriaxone treatment, breastfeeding should be discontinued.

Dosing and Administration:

Do not use solutions containing calcium ions for the dilution of Ceftriaabol®.

Ceftriabol® can be administered intravenously and intramuscularly. If necessary, single administration at a dose of more than 1 g, as well as for the treatment of severe infections in / in the route of administration is preferred. When administered intravenously at a dose of 50 mg / kg and above, an intravenous infusion of at least 30 minutes should be used.

In adults Ceftriabol® is administered at a dose of 1 to 2 grams once a day or divided into two doses (every 12 hours), depending on the shape and severity 4

infection. In severe cases, the dose may be increased, but should not exceed 4 g / day.

When Lyme disease (tick-borne borreliosis) daily dose in children and adults is 50 mg / kg (maximum daily dose - 2 g); duration of treatment - 14 days.

For treatment of uncomplicated gonorrhea ceftriaxone injected at a dose of 250 mg intramuscularly once.

For perioperative antibiotic prophylaxis of infectious complications, 1 g of ceftriaxone is given IV in 30-60 min before the operation. In operations on the colon and rectum, simultaneous (but separate!) Administration of 2.0 g of ceftriaxone and a drug from the group of 5-nitroimidazoles is recommended. The dose for newborns - 20-50 mg / kg / day.

For treatment skin and soft tissue infections the recommended daily intake in children is 50-75 mg / kg, once a day or divided into two doses (every 12 hours). The total daily dose should not exceed 2 g.

For treatment bacterial meningitis children are prescribed in a daily dose of 100 mg / kg (but not more than 4 g / day), which is administered / once a day, or the daily dose is divided into two intravenous infusions (every 12 hours). The recommended duration of therapy is 7-14 days.

When average otitis Ceftriabol® is administered once a day at a dose of 50 mg / kg (but not more than 1 g).

In the treatment of other infections in children, the recommended daily dose of ceftriaxone is 50-75 mg / kg body weight divided by two

and reception (every 12 hours). The total daily dose should not exceed 2 g.

Have children weighing more than 50 kg and above apply doses to adults.

Treatment with ceftriaabol® should continue for at least 2 more days after the disappearance of symptoms and signs of infection. The course of treatment is usually 4-14 days; with complicated infections, a longer administration may be required. In the treatment of infections caused by Streptococcus pyogenes, The duration of therapy should be at least 10 days.

When chronic renal failure (creatinine clearance less than 10 ml / min) - the daily dose should not exceed 2 g. Patients on hemodialysis do not need to enter an additional dose of ceftriaxone after a hemodialysis session. However, the concentration of ceftriaxone in the blood serum should be monitored for possible dose adjustment, as its excretion in such patients may be slowed down.

Have patients with renal-hepatic insufficiency a daily dose of Ceftriaabol® should not exceed 2 g without determining the concentration of the drug in the blood plasma.

Rules for the preparation of solutions

Intramuscular injection

For intramuscular injection, 2.0 g of the drug must be diluted in 7.0 ml of a 1% solution of lidocaine and inserted deep into the gluteal muscles.

It is recommended to inject no more than 1 g of the drug into one buttock. A solution of lidocaine can not be administered intravenously!

Intravenous administration

Ceftriabol® 2.0 g is given as an intravenous infusion. To do this, 2.0 g of the drug is dissolved in at least 50 ml of a calcium-free solution: a 0.9% solution of sodium chloride, in a 5% or 10% solution of dextrose. The resulting solution is introduced slowly, at least 30 minutes.

Side effects:

Allergic reactions: chills or fever, rash, itching.

From the nervous system: headache, dizziness.

From the digestive system: nausea, vomiting, diarrhea, pseudomembranous colitis.

On the part of the blood system and hemopoiesis: anemia (including hemolytic), eosinophilia, leukopenia, neutropenia, thrombocytopenia, lymphopenia, thrombocytosis.

From the genitourinary system: candidiasis of the vagina, vaginitis.

Local reactions: with iv introduction - phlebitis, tenderness, compaction along the vein; Intramuscular injection - soreness, sensation of warmth, tightness or condensation at the injection site.

Laboratory indicators: increase (decrease) prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatinemia, increased urea concentration, the presence of sediment in the urine.

Other: increased sweating, "hot flashes" of blood.

Undesirable reactions with a frequency of less than 0.1%: abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, bronchospasm, colitis, dyspepsia, epistaxis, bloating, pseudocholithiasis with or without symptoms, which go away after the drug is discontinued, glucosuria , hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitation, convulsions, serum sickness.

Postmarketing experience: stomatitis, glossitis, oliguria, rash, allergic dermatitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

Overdose:Symptoms: nausea, vomiting, diarrhea, confusion, convulsions. In case of an overdose, a decrease in ceftriaxone concentration can not be achieved with hemo- and peritoneal dialysis. There is no specific antidote. Treatment, in general, is symptomatic.

Interaction:

Compatible with the following infusion solutions: 0.9% solution of sodium chloride, 5% and 10% solutions of dextrose, a solution containing 0.9% sodium chloride and 5% dextrose, a solution containing 0.45% sodium chloride and 5% dextrose, 6% dextran solution in 5% dextrose solution, 6-10% solutions of hydroxyethylated starch, 5% fructose solution. Do not use as a solvent and do not add ceftriaxone in solutions containing calcium ions (Ringer's and Hartman's solution). Pharmaceutically incompatible with vancomycin, fluconazole and aminoglycosides. When used simultaneously, they should not be mixed in one syringe or one infusion medium; with the / m introduction to enter into different parts of the body; when administered intravenously, it is recommended to administer separately, following the sequence, with as long a time interval between injections (infusions), or use separate intravenous catheters. In vitro, antagonism is observed between chloramphenicol and ceftriaxone.

The risk of bleeding increases with simultaneous administration of ceftriaxone with non-steroidal anti-inflammatory drugs and other inhibitors of platelet aggregation.

At simultaneous application with "loop" diuretics and aminoglycosides, the risk of renal dysfunction is minimal.

Special instructions:

In rare cases, on the background or after therapy with ceftriaxone, ultrasound examination of the gallbladder reveals acoustic shadows taken for concrements, and / or a clinic of cholelithiasis develops. The phenomena are caused by precipitation and the formation of a precipitate of ceftriaxone compounds with calcium in the gall bladder. It is necessary to cancel the antibiotic and carry out symptomatic treatment. In infections caused by aerobic anaerobic flora (peritonitis, abscess of the lungs, empyema of the pleura, infection of the pelvic organs), it is recommended to combine ceftriaxone with preparations used for anaerobic infection (for example, from the group of 5-nitroimidazoles). In mixed infections and the likely etiological role of chlamydia and mycoplasma, combinations of ceftriaxone with tetracyclines or macrolides are recommended.With simultaneous severe renal and hepatic insufficiency, the concentration of the drug in the plasma should be regularly determined. In patients with hepatic insufficiency, the recommended daily dose of ceftriaxone is no more than 2 g.

In patients with impaired metabolism of vitamin K (eg, liver failure), prothrombin time should be monitored regularly. In the case of prolonged prothrombin time before or during the administration of ceftriaxone, vitamin K should be given at a dose of 10 mg per week. Use caution when using ceftriaxone in people who have concomitant bowel disease, especially colitis. If diarrhea occurs during treatment with ceftriaxone, caution should be exercised because of the possible development of pseudomembranous colitis. If a diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis is established, ceftriaxone should be discontinued and appropriate treatment should be prescribed.

As with other antibiotics, the use of ceftriaxone may lead to colonization by an insensitive microflora and the development of superinfection.

With long-term treatment, it is necessary to regularly monitor the picture of peripheral blood, indicators of the functional state of the liver and kidneys.

Effect on the ability to drive transp. cf. and fur:

There is no evidence indicating a negative effect of ceftriaxone on the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

When using a lidocaine solution as a solvent, care must be taken when driving vehicles and engaging in other potentially hazardous activities.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 2.0 g.

Packaging:

2.0 g of active substance is placed in glass bottles with a capacity of 20 ml or 100 ml.

1 bottle with the drug, along with instructions for use, is placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008018/10

Date of registration:12.08.2010

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp21.11.2015

Illustrated instructions

Instructions

Ceftriabol® (Ceftriabol®)