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

Semisynthetic antibiotic group of third generation cephalosporins for parenteral use. Cefotaxime acts bactericidal due to disruption of bacterial wall synthesis. It is also resistant to the action of most β-lactamases.

TO cefotaxime are usually sensitive: Aeromonas hydrophila; Bacillus subtilis; Bordetella pertussis; Borrelia burgdorferi: Moraxella (Branhamella) catarrlialis; Citrobacter diversus *; Citrobacter freundii *; Clostridium perfringens; Corynebacterium diphtberiae; Escherichia coli: Enterobacter spp. *: Erysipelothrix insidiosa: Eubacterium spp .: Haemophilus spp. (producing and penicillinase-inducing strains, including ampicillin-resistant): Klebsiella pneumoniae: Klebsiella oxytoca; Staphylococcus spp. (methicillin-sensitive, including penicillinase-producing and non-producing penicillinase strains); Morganella morgatiii; Neisseria gonorrhoeae (including strains producing and not producing penicillinase); Neisseria meningitidis; Propionibacterium spp .; Proteus mirabilis, Proteus vulgaris; Providencia spp .; Streptococcus spp. (including Streptococcus pneumonia). Salmonella spp .: Serratia spp. *; Shigella spp .: Vicllonella spp .; Yersinia spp. *: Pseudomonas spp. (except Pseudomonas aeruginosa, Pseudomonas cepacia).

* - sensitivity depends on epidemiological data and on the level of resistance in each country. Cefotaxime is resistant to: Acinetobacter baumanii, Bacteroides lragilis: Clostridium difficile; Entcrococcus spp .: gram-negative anaerobes; Listeria monocytogenes, Staphylococcus spp.(methicillin-resistant strains); Pseudomonas aeruginosa, Pseudomonas cepacia; Stenotrophomonas maltophilia.

Pharmacokinetics:

In adults - 5 minutes after a single intravenous (iv) injection of 1 g of cefotaxime

the maximum concentration (C max) in blood plasma is 100 μg / ml.

After intramuscular (intramuscularly) administration of cefotaxime in the same dose of Cmax in blood plasma is achieved

after 0.5 hours and is from 20 to 30 μg / ml. Bioavailability of cefotaxime in the / in the introduction is 100%, with the / m introduction - 90-95%. The half-life (T1 / 2) of cefotaxime is 1 hour with an IV injection and 1-1.5 hours with an IM injection. The binding with plasma proteins (mainly albumins) averages 25-40%. Metabolised in the liver with the formation of an active metabolite deacetylcefotaxime (M1), which has antibacterial activity, and inactive metabolites (M2, M3). About 90% of the administered dose is excreted by the kidneys: 50% - unchanged, about 15-25% in the form of metabolite deacetylcefotaxime and 15-30% in the form of inactive metabolites

(M2 + M3). 10% of the administered dose is excreted by the intestine.

Have elderly patients over 80 years T1 / 2 cefotaxime increases to 2.5 hours. Volume distribution (Vd) does not change in comparison with young healthy

volunteers.

Have adults with impaired renal function Vd does not change, and T1 / 2 does not exceed 2.5 h even in the last stages of renal failure. Have children concentration of cefotaxime in the blood plasma and Vd are similar to those in adults receiving the same dose of the drug in mg / kg of body weight. T1 / 2 cefotaxime is from 0.75 to 1.5 h.

Have Newborns and prematurely born children concentration of cefotaxime in the blood plasma and Vd similar to those of children. The average T1 / 2 of cefotaxime ranges from 1.4 to 6.4 h.

Indications:

Apply Cefotaxime in infections caused by sensitive microorganisms (mainly gram-negative): infections of the respiratory and urinary tract, kidneys; infections of the ear, throat, nose, septicemia, endocarditis, meningitis; infections of bones and soft tissues, abdominal cavity; with infectious and inflammatory diseases of the pelvic organs, gonorrhea; wound and burn infections and others.

Contraindications:

- Increased sensitivity to cefotaxime, other cephalosporins.

- For forms containing lidocaine as a solvent:

- hypersensitivity to lidocaine or other local anesthetic of the amide type;

- intracardiac blockades without an established pacemaker;

- severe heart failure;

- intravenous administration;

- Children under the age of 2.5 years (intramuscular injection).

Carefully:

- Patients with a history of allergy to penicillins (risk of developing

cross-sectional allergic reactions, see section "Special instructions").

- With simultaneous use with aminoglycosides (see sections "Special instructions".

"Interaction with other drugs").

- In case of renal insufficiency (see section "Method of administration and dose").

Pregnancy and lactation:

Cefotaxime penetrates the placental barrier. Research. conducted on animals, not

revealed a teratogenic or fetotoxic effect of the drug. However, security

the use of cefotaxime in pregnancy in humans is not established, so the drug should not be used during pregnancy.

Cefotaxime penetrates into breast milk, so if you need to prescribe the drug, breastfeeding should be interrupted.

Dosing and Administration:

Intramuscularly or intravenously. The dose, mode and frequency of administration should be determined by the severity of the infection, the sensitivity

the pathogen and the patient's condition. Treatment can be initiated before the results of the sensitivity test are obtained. Adults and children over 12 years of age and weighing 50 kg or more for infections of mild and moderate severity - I g every 12 h. The dose may vary depending on the severity of the infection, the sensitivity of the pathogen and the patient's condition. When severe infections the dose can be increased to 12 g per day, divided into 3-4 injections. When infections, diagnosed Pseudomonas spp.. the daily dose should be more than 6 g. For children under 12 years and with a body weight of up to 50 kg, the usual dose is 100-150 mg / kg of body weight per day, divided into 2-4 injections. When very serious infections the dose can be increased to 200 mg / kg of body weight per day. For newborns, the dose is 50 mg / kg of body weight per day, diluted in 2-4 injections. When severe infections - a dose of 150-200 mg / kg of body weight per day, divided into 2-4 injections.

When gonorrhea: 1 g once-intramuscularly or intravenously.

With the aim of prevention of infection before surgery (from 30 to 90 minutes before the operation) 1 g intramuscularly or intravenously. By doing cesarean section at the time of application of the clips to the umbilical vein, 1 g of the drug is intravenously injected, then 1 g intramuscularly or intravenously is reintroduced after 6-12 h.

Patients with renal disease insufficiency

In cases where creatinine clearance is less than 10 ml / min, it is necessary to reduce the dose. After the introduction of the initial single dose, the daily dose should be halved without changing the frequency of administration, that is, instead of 1 g every 12 hours - 0.5 g every 12 h instead of 1 g every 8 h - 0.5 g every 8 h, instead of 2 g every 8 h - 1 g every 8 hours, etc. Further dose adjustment may be required depending on the course infection and general condition patient.

Rules for the preparation of solutions

For intravenous injection in the solvent used water for injection (1 g diluted in 4 ml); with intravenous injection solution should be introduced in the current is from 3 to 5 minutes.

For intravenous infusion in the solvent used 0.9% solution of sodium chloride or 5% solution of dextrose (1-2 g diluted in 40-100 ml of solvent). Also a solution can be used Ringer's lactate. Duration Infusion - 20-60 minutes.

For intramuscular injection use water for injection or 1 % solution of lidocaine (1 g diluted in 4 ml of solvent).

Side effects:

The incidence of adverse events is classified according to the recommendations of the World Health Organization

health care organizations: very often - at least 10%; often - not less than 1%. but less than 10%: infrequently - not less than 0.1%. but less than 1%: rarely - not less than 0.01%, less than 0.1%; very rarely - less than 0.01%: unknown frequency - can not be estimated from the available data.

Infectious and parasitic diseases

The frequency is unknown: superinfection. As with the appointment of other antibiotics, the use of

cefotaxime, especially prolonged. can lead to excessive growth of insensitive microorganisms. Regular monitoring of the patient's condition should be made. If the development of superinfection occurs during therapy with cefotaxime, appropriate measures should be taken.

Violations of the blood and lymphatic system

Infrequently: leukopenia, eosinophilia. thrombocytopenia.

The frequency is unknown: failure of bone marrow hematopoiesis, pancytopenia, neutropenia,

agranulocytosis, hemolytic anemia.

Immune system disorders

Infrequently: the reaction of Yarisch-Gerxheimer. As with the use of other antibiotics, in the treatment

borreliosis during the first days of therapy, the development of the Yarisch-Gerxheimer reaction is possible. There are reports of the occurrence of one or more symptoms after a few weeks of treatment of borreliosis: skin rash, itching, fever, leukopenia, increased activity of "liver" enzymes, shortness of breath, discomfort in the joints.

It should be borne in mind that to some extent, these manifestations are consistent with the symptoms of the underlying

a disease for which the patient is receiving treatment.

The frequency is unknown: anaphylactic reactions, angioedema, bronchospasm, anaphylactic shock.

Disturbances from the nervous system

Infrequently: convulsions.

The frequency is unknown: encephalopathy (eg, impaired consciousness.

activity), headache, dizziness.

Heart Disease

The frequency is unknown: arrhythmias (due to rapid bolus administration through the central

venous catheter).

Disorders from the gastrointestinal tract

Infrequently: diarrhea.

The frequency is unknown: nausea, vomiting, abdominal pain, pseudomembranous colitis.

Disturbances from the liver and bile ducts

Infrequently: increased activity of "hepatic" enzymes (alanine aminotransferase [ALT],

aspartate aminotransferase [ACT], lactate dehydrogenase [LDH], gamma-glutamyltransferase [gamma-GT], alkaline phosphatase [AChF]) and / or bilirubin concentrations. These

deviations in laboratory indicators (which can also be explained by the presence of infection), in

rare cases exceed the upper limit of the norm 2 times and indicate liver damage,

manifested cholestasis and often asymptomatic.

The frequency is unknown: hepatitis (sometimes with jaundice).

Disturbances from the skin and subcutaneous tissues

Infrequent: rash, itching, hives.

The frequency is unknown: erythema multiforme, Stevens-Johnson syndrome, toxic

epidermal necrolysis, acute generalized exanthematous pustulosis.

Disorders from the kidneys and urinary tract

Infrequent: decreased kidney function / increased creatinine concentration, especially when

combined use with aminoglycosides.

Frequency unknown: acute renal failure, interstitial nephritis.

General disorders and disorders at the site of administration

Often: pain at the injection site (with intramuscular injection).

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

The frequency is unknown: when administered intramuscularly, if the solvent is used

lidocaine, possible development of systemic reactions associated with lidocaine, especially in cases

unintentional intravenous administration of the drug, injection into highly vascularized tissue or overdose.

Overdose:

Interaction:

Probenecid retards excretion and increases the concentration of cephalosporins in the blood plasma.

As with other cephalosporins, cefotaxime can enhance the nephrotoxic effect of drugs that have a nephrotoxic effect (such as furosmide, aminoglycosides).

Compatibility guidelines:

cefotaxime should not be mixed with other antibiotics (including aminoglycosides), as in one syringe, and in one infusion solution.

For infusions, the following solutions can be used (concentration of cefotaxime 1 g / 250

ml): water for injection, 0.9% sodium chloride solution, 5% dextrose solution, Ringer's lactate solution,

Ionostearyl.

Special instructions:

Anaphylactic reactions

The appointment of cephalosporins requires the collection of an allergic anamnesis (allergic diathesis, hypersensitivity reactions to β-lactam antibiotics).

If the patient develops a hypersensitivity reaction, then the treatment should be stopped.

The use of cefotaxime is contraindicated in patients with a history of reaction

immediate type hypersensitivity to cephalosporins. In case of any doubt, the presence of a physician at the first administration of the drug is necessary, in view of the possible anaphylactic reaction. There is a cross-allergy between cephalosporins and penicillins. which occurs in 5-10% of cases. Anaphylactic reactions that develop in this situation can be serious or even fatal. In patients who have a history of having an allergy to penicillins, the drug is applied from extreme caution. Care should be taken to monitor the patient's condition with the first administration of the drug due to a possible anaphylactic reaction.

In case of development of the first symptoms and signs of anaphylactic shock, the drug should be stopped immediately. The patient should remain in the "lying" position with raised legs.A slow intravenous injection of 0.1 mg (1 ml) of epinephrine (Epinephrine) solution under the control of pulse and arterial pressure, as well as intravenous administration of plasma substitutes, human albumin, or balanced electrolyte solutions was introduced: subsequently, intravenous glucocorticosteroids eg, 250-1000 mg hydrocortisone), once or, if necessary, repeatedly. A supporting therapeutic Events:

Effect on the ability to drive transp. cf. and fur:In the case of the development of such a side effect as dizziness, the ability to concentrate attention and reactions may be impaired. In this case, patients should refrain from driving

motor transport and work with mechanisms.

Form release / dosage:

Powder for solution for injection for 0.5 and 1.0 g.

Packaging:

Powder for solution for injection for 0.5 and 1.0 g in glass bottles with a volume of 10ml. One bottle together with the instruction for use is placed in a cardboard bundle

Storage conditions:

At a temperature not higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015272 / 01

Date of registration:15.12.2008

The owner of the registration certificate:Shraya Life Senses Pvt. Ltd.Shraya Life Senses Pvt. Ltd. India

Manufacturer: & nbsp

SERENA PHARMA, Pvt.Ltd. India

Representation: & nbspSHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India

Information update date: & nbsp04.11.2015

Illustrated instructions

Instructions

Cefotaxime (Cefotaxime)