Cefotaxime powder solution 1g vials, 1pc – Borisov

Composition

1 bottle contains: Active ingredient: cefotaxime sodium in terms of cefotaxime 1000 mg

Pharmacological action

Pharmacotherapy group: Antibiotic-Cephalosporin ATX code: J01DD01 Pharmacodynamics : Cephalosporin antibiotic of the third generation for parenteral use. It acts bactericidal. disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of action. Cefotaxime is usually susceptible to: Aeromonas hydrophila; Bacillus subtilis; Bordetella pertussis; Borrelia burgdorferi; Moraxella catarrhalis; Citrobacrer diversus; Curobacler freundii*; Clostridium perfringens; Corynebacterium diphtheriae Escherichia coli; Enterobacter spp. *; Erysipelothrix insidiosa; Eubacterium spp. ; Haemophilus spp. (penicillinase-producing and non-producing strains including ampicillin-resistant): Klebsiella pneumoniae; Klebsiella oxytoca; Staphylococcus spp. (methicillin-sensitive including peninillinase-producing and non-producing strains); Morganella morganii Neisseria gonorrhoea (including penicillinase-producing and non-producing strains); Neisseria meningitidis: Propionibacterium spp ; Proteus mirabilis; Proteus vulgaris: Providencia spp. ; Streptococcus spp (including Streptococcus pneumoniae): Salmonella spp. Serratia spp *; Shigella spp.. Veillonella spp*; Yersinia spp*; Pseudomonas spp. (except Pseudomonas aeruginosa Pseudomonas cepacia). * – sensitivity depends on epidemiological data and the level of resistance in each particular country. Cefotaxime is resistant to: Acinetobacter baumanii; Bacteroidcs fragilis; Clostridium difficile; Entcrococcus spp. ; gram-negative anaerobes: Listeria monocytogenes Staphylococcus spp. (methicillin-resistant strains); Pseudomonas aeruginosa; Pscudomonas cepacia; Stenotrophomonas maltophilia. Pharmacokinetics: After a single IV (intravenous) use in doses of 05 1 and 2 g, the time to reach the maximum concentration (Cmax) is 5 minutes, the maximum concentration (Cmax) is 39 1017 and 214 mcg / ml, respectively. After intravenous (intramuscular) use to the vines of 05 and 1 g, the Cmax is 05 h and the Cmax is 11 and 21 mcg / ml, respectively. Plasma protein binding is 30-50%. Bioavailability – 90-95%. Creates therapeutic concentrations in most tissues (myocardium bone gall bladder skin soft tissues) and fluids (synovial pericardial pleural sputum bile urine cerebrospinal fluid (CSF) of the body. The volume of distribution is 025-039 l / kg. The elimination half-life (T 1/2) is 1 h with intravenous use and 1-1.5 h with intramuscular use. Excreted by the kidneys-20-36% unchanged, the remaining amount in the form of metabolites (15-25% in the form of pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites of M2 and MH). In chronic renal failure and in elderly patients, T 1/2 increases 2-fold. In newborns T 1/2 ranges from 0.75 to 15 hours in premature newborns it increases to 64 hours

Indications

Severe bacterial infections caused by microorganisms sensitive to cefotaxime: infections of the central nervous system (meningitis) of the respiratory tract and ENT organs of the urinary tract bones joints skin and soft tissues of the pelvic organs gonorrhea infected wounds and burns peritonitis sepsis abdominal infections endocarditis Lyme disease infections against the background of immunodeficiency prevention of infections after surgical operations (including urological obstetric and gynecological on the gastrointestinal tract).

Use during pregnancy and lactation

Use during pregnancy and lactation is contraindicated. If it is necessary to prescribe the drug during breastfeeding, stop breastfeeding.

Contraindications

Hypersensitivity to cefotaxime (including penicillins, cephalosporins, carbapenems) pregnancy lactation children (iv use-up to 25 years when using lidocaine as a solvent). With caution: In patients with a history of allergy to penicillins (risk of cross-allergic reactions); with simultaneous use with aminoglycosides; with renal failure.

Side effects

Classification of adverse reactions by frequency according to the World Health Organization recommendations: very common (> 10%): common (>>1% and >>< 10%); infrequent (> 0.1% and < 10%); infrequent (>< 1%); rare (> 001% and < 1%); rare (>< 0.1%); very rare (

Infectious and parasitic diseases

Frequency unknown:  superinfections. As with other antibiotics, especially prolonged use of cefotaxime can lead to excessive growth of insensitive microorganisms. The patient’s condition should be monitored regularly If superinfection occurs during cefotaxime therapy, appropriate measures should be taken.

Disorders of the blood and lymphatic system

Infrequently:  leukopenia eosinophilia thrombocytopenia.

Frequency unknown:  insufficiency of bone marrow hematopoiesis pancytopenia neutropenia agranulocytosis hemolytic anemia.

Immune system disorders

Infrequently:  Jarisch-Herkegeimer’s reaction: As with other antibiotics, a Jarisch – Herkegeimer’s reaction may occur during the first days of therapy in the treatment of borreliosis. There are reports of one or more symptoms occurring after a few weeks of treatment for borreliosis: skin rash pruritus fever leukopenia increased activity of “liver” enzymes difficulty breathing joint discomfort. It should be borne in mind that to some extent these manifestations are consistent with the symptoms of the underlying disease for which the patient is receiving treatment.

Frequency unknown:  anaphylactic reactions angioedema bronchospasm anaphylactic shock.

Nervous system disorders

Infrequently:  convulsions.

Frequency unknown encephalopathy (e. g. impaired consciousness motor activity disorders) headache dizziness.

Cardiac disorders

Frequency unknown:  arrhythmias (due to rapid bolus insertion through a central venous catheter).

Disorders of the gastrointestinal tract

Infrequently:  Diarrhea

Frequency unknown:  nausea vomiting abdominal pain pseudomembranous colitis

Liver and biliary tract disorders

Infrequently:  increased activity of “liver” enzymes (alanine aminotransferase (ALT) aspartate aminotransferase (ACT) lactate dehydrogenase (LDH) gamma – glutamyltransferase (gamma – GT) alkaline phosphatase (ALP) and/or bilirubin concentration. These deviations in laboratory parameters (which can also be explained by the presence of infection) in rare cases exceed the upper limit of normal by 2 times and indicate liver damage manifested by cholestasis and often asymptomatic.

Frequency unknown:  hepatitis (sometimes with jaundice).

Skin and subcutaneous tissue disorders

Infrequently: rash pruritus urticaria.

Frequency unknown:  erythema multiforme Stevens-Johnson syndrome toxic epidermal necrolysis acute generalized exanthematous pustulosis.

Kidney and urinary tract disorders

Infrequently:  decreased renal function increased creatinine concentration especially when combined with aminoglycosides.

Frequency unknown:  acute renal failure interstitial nephritis.

General disorders and disorders at the data

collection site Often:  pain at the injection site (when administered intramuscularly).

Infrequently:  fever inflammatory reactions at the injection site including phlebitis / thrombophlebitis.

Frequency unknown:  when administered intramuscularly if lidocaine is used as a solvent it is possible to develop systemic reactions associated with lidocaine especially in cases of unintentional intravenous use of the drug injections into highly vascularized tissues or overdose.

Interaction

Increases the risk of bleeding when combined with antiplatelet agents, nonsteroidal anti-inflammatory drugs. The likelihood of kidney damage increases with simultaneous use with aminoglycosides polymyxin B and “loop” diuretics. Drugs that block tubular secretion increase plasma concentrations of Cefotaxime and slow its elimination Pharmacologically incompatible with solutions of other antibiotics in the same syringe or dropper.

How to take it, course of use and dosage

Either intravenously or intramuscularly. The dose method and frequency of use should be determined by the severity of the infection the sensitivity of the pathogen and the patient’s condition. Treatment can be initiated before receiving the results of a sensitivity test. Adults and children over 12 years of age and weighing 50 kg or more: – for mild and moderate infections – 1 g every 12 hours. The dose may vary depending on the severity of the infection, the sensitivity of the pathogen and the patient’s condition. – for severe infections, the dose can be increased to 12 g per day divided into 3 or 4 injections. – for infections caused by Pseudomonas spp. the daily dose should be more than 6 g.

Children under 12 years of age and weighing up to 50 kg: – the usual dose is 100-150 mg / ct / day. divided pa 2-4 introductions. – for very severe infections, the dose can be increased to 200 mg / kg / day.

Newborns: 50 mg / ct / day divided into 2 – 4 injections. – for severe infections-a dose of 150-200 mg / kg / day divided into 2-4 injections.

With gonorrhea: 1 g once intravenously or intramuscularly.

For the purpose of prevention,1 g is administered intramuscularly or intravenously before surgery (from 30 to 90 minutes before the operation).

When performing a caesarean section at the time of applying clamps to the umbilical vein,1 g of the drug is administered intravenously, then after 6 and 12 hours,1 g is re-administered intravenously or intramuscularly.

In patients with renal insufficiency: in cases where the creatinine clearance is less than 10 ml/min, the dose should be reduced. After use of the initial single dose, the daily dose should be halved without changing the frequency of use, i. e. instead of 1 g every 12 hours -05 g every 12 hours instead of 1 g every 8 hours-05 g every 8 hours instead of 2 g every 8 hours-1 g every 8 hours, etc. Further dose adjustment may be required depending on the course of infection and the general condition of the patient.

Rules for preparing solutions: for intravenous injection, water for injection is used as a solvent (250 mg is diluted in 2 ml of solvent: 500 mg is diluted in 2 ml of solvent; 1 g is diluted in 4 ml: 2 g in 10 ml); for intravenous injection, the solution should be administered within 3 to 5 minutes. For intravenous infusion,0.9% sodium chloride solution or 5% dextrose solution is used as a solvent (1-2 g is diluted in 40-100 ml of solvent). Ringer’s lactate solution can also be used. Duration of infusions -20 – 60 min. For intramuscular use, use water for injection or 1% lidocaine solution (250 mg diluted in 2 ml of solvent; 500 mg-in 2 ml; 1 g-in 4 ml; 2 g-in 10 ml).

Overdose

Symptoms of convulsions encephalopathy (in the case of large doses, especially in patients with renal insufficiency) tremor neuromuscular excitability Treatment: symptomatic.

Special instructions

Pseudomembranous colitis may occur in the first weeks of treatment, with severe prolonged diarrhea. At the same time, stop taking the drug and prescribe adequate therapy, including vancomycin or metronidazole. Patients with a history of allergic reactions to penicillins may be hypersensitive to cephalosporin antibiotics. When treating with the drug for more than 10 days, it is necessary to control the number of formed blood elements. During treatment with cefotaxime, a false-positive Coombs test and a false-positive urine glucose response may be obtained. With simultaneous use of cephalosporin antibiotics and ethanol, disulfiram-like reactions may develop; however, in clinical studies of cefotaxime (Claforan), no similar effect was recorded when it was used simultaneously with ethanol. Caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions. During treatment with cefotaxime, leukopenia neutropenia may develop and, more rarely, bone marrow hematopoiesis insufficiency pancytopenia and agranulocytosis If the course of treatment lasts more than 10 days, the number of formed blood elements should be monitored. If these blood parameters deviate from the norm, the drug should be discontinued. Influence on the ability to drive vehicles and mechanisms:If a side effect such as dizziness develops, the ability to concentrate and react may be impaired. In this case, patients should refrain from driving vehicles and working with mechanisms.

Form of production

Powder for solution preparation for intravenous and intramuscular use

Storage conditions

In a dark place at a temperature not exceeding 25 °C. The freshly prepared solution is suitable for use for 12 hours at room temperature no higher than 25 °C. Keep out of reach of children.

Shelf

life is 2 years. It is recommended to use it before the period indicated on the package.

Active ingredient

Cefotaxime

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion