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

Cefotaxime is a third generation cephalosporin antibiotic for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of antimicrobial action.

Active against gram-positive and gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (incl. Staphylococcus aureus, including penicillinase-forming strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus species, Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (incl. Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Acinetobacter species, Corynebacterium diphtheriae, Erysipelothrix insidiosa, Eubacterium spp., Propionibacterium spp., Bacillus subtilis, Clostridium spp. (incl. Clostridium perfringens), Citrobacter spp., Proteus mirabilis, Proteus indole, Proteus vulgaris, Providencia spp. (incl. Providencia rettgeri), Serratia spp., Pseudomonas aeruginosa, Neisseria meningitidis, Bacteroides spp. (including some strains Bacteroides fragilis), Fusobacterium spp. (incl. Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp.

Most strains Clostridium difficile - are stable.

Cefotaxime is resistant to most beta-lactamases of Gram-positive and Gram-negative microorganisms.

Pharmacokinetics:

After a single intravenous (iv) dose at 0.5, 1.0 and 2.0 g, the maximum concentration is reached after 5 minutes and is 39 μg / ml, 101.7 μg / ml and 214 μg / ml, respectively.

After intramuscular (IM) administration at doses of 0.5, 1.0, the maximum concentration is achieved after 0.5 hours and is 11 and 21 μg / ml, respectively. The connection with plasma proteins is 30-50%. Bioavailability is 90-95%.

Creates therapeutic concentrations in most tissues (myocardium, bones, gallbladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, sputum, bile, urine, cerebrospinal fluid) of the body. The volume of distribution is 0.25-0.39 l / kg. The half-life is 1 hour with IV injection and 1-1.5 hours with the IM injection.

It is excreted by the kidneys - 20-36% unchanged, the rest - in the form of metabolites (15-25% - in the form of pharmacologically active deacetylcefotaxime and 20-25% - in the form of inactive metabolites - M2 and M3).

In chronic renal failure and in the elderly the elimination half-life is doubled.

Half-life in newborns - 0,75-1,5 h; in preterm neonates (body weight less than 1500 g) increases to 4.6 h, in children weighing more than 1500 g - 3.4 h.

With repeated iv administration in a dose of 1 g every 6 hours for 14 days of cumulation is not observed.

Penetrates into breast milk.

Indications:

Bacterial infections of the severe course caused by sensitive microorganisms: infections of the central nervous system (meningitis), lower respiratory tract and ENT organs, urinary tract, bones, joints, skin and soft tissues, pelvic organs, infected wounds and burns, peritonitis, sepsis, abdominal infections, endocarditis, Lyme disease (borreliosis), salmonellosis, infections against the background of immunodeficiency, prevention of infections after surgery (including urological, obstetric-gynecological, on the gastrointestinal tract ones), gonorrhea.

Contraindications:

Hypersensitivity to cephalosporin antibiotics (including penicillins, other cephalosporins, carbapenems); In children under 2.5 years of intramuscular injection.

Carefully:

In the period of newborn; during pregnancy and lactation; patients with impaired renal and hepatic function; with nonspecific ulcerative colitis (including anamnesis).

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Cefotaxime excreted in breast milk, so if you need to prescribe the drug during lactation should stop breastfeeding.

Dosing and Administration:

Apply cefantral intramuscularly or intravenously.

Adults and children over 12 years of age: for uncomplicated infections, as well as for infections of the urinary tract - in / m or / in 1 g every 8-12 hours; with uncomplicated acute gonorrhea -1 g IM once; at infections of average gravity - in / m or iv in 1-2 g every 12 h; in severe infections, for example, with meningitis - iv 2 g every 4-8 hours, maximum daily dose - 12 g.

Duration of treatment is set individually.

With the purpose of preventing the development of infections before the surgical operation, enter 1 g during the initial general anesthesia. If necessary, the administration is repeated after 6-12 hours.

At caesarean section - at the time of application of the clamps on the umbilical vein - in / in 1 g, then 6 and 12 hours after the first dose - an additional 1 g.

In the case of violations of kidney function dose reduced. With a creatinine clearance of 20 ml / min / 1.73 m 2² and a less daily dose of the drug is reduced by a factor of 2.

Preterm infants and newborns under 1 week of age - IV, 50 mg / kg body weight every 12 hours; at the age of 1-4 weeks - IV, 50 mg / kg body weight every 8 hours; children with body weight up to 50 kg - in / in or / m, 50-180 mg / kg of body weight per day (4-6 injections during the day). In severe infections, including meningitis, the daily dose is increased to 100-200 mg / kg in 4-6 injections, the maximum daily dose is 12 g.

Children under the age of 2.5 years of intramuscular injection of the drug is contraindicated.

Rules for the preparation and injection of injection solutions

For intramuscular injection, dissolve 0.5 g of the drug in 2 ml (respectively 1 g in 4 ml) of sterile water for injection, injected deeply into the gluteal muscle. As a solvent, intramuscular injection also uses a 1% solution of lidocaine (0.5 g - 2 ml, 1 g - 4 ml).

For intravenous administration, 0.5-1 g of the drug is dissolved in 10 ml of sterile water for injection. Enter slowly for 3-5 minutes.

For drip administration (within 50-60 minutes), dissolve 2 g of the drug in 100 ml of isotonic sodium chloride solution or 5% glucose solution.

Side effects:

Allergic reactions: urticaria, chills or fever, rash, itching; rarely - bronchospasm, eosinophilia, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), angioedema, anaphylactic shock.

From the gastrointestinal tract: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function; rarely - stomatitis, glossitis, pseudomembranous enterocolitis.

From the cardiovascular system: potentially life-threatening arrhythmias after a rapid bolus injection into the central vein.

From the hematopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolytic anemia, hypocoagulation.

From the urinary system: disturbance of kidney function (oliguria, anuria).

From the nervous system: headache, dizziness.

Local reactions: phlebitis, soreness along the vein, soreness and infiltration at the site of the / m introduction.

Laboratory indicators: an increase in the activity of "hepatic" transaminases, alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, azotemia, an increase in urea in the blood, a positive Coombs reaction.

Other: Superinfection (in particular, candidal vaginitis).

Overdose:

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

Treatment: symptomatic therapy.

Interaction:

Increases the risk of bleeding when combined with antiaggregants and non-steroidal anti-inflammatory drugs.

With the simultaneous use of cefotaxime with potentially nephrotoxic drugs (aminoglycosides, polymyxin In, "loop" diuretics) it is necessary to control the function of the kidneys (the risk of nephrotoxic action of the latter).

Drugs that block tubular secretion, increase the concentration of cefotaxime in the blood plasma and slow its elimination.

The cefotaxime solution is pharmaceutically incompatible with solutions of other antibiotics in one syringe or dropper.

Special instructions:

In the first weeks of treatment, pseudomembranous colitis can occur, which is manifested by severe prolonged diarrhea. At the same time, stop taking the drug and prescribe adequate therapy, including vancomycin or metronidazole.

Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. There is a cross-allergy between penicillins and cephalosporins.

When there are reactions of hypersensitivity (which are severe and even lead to death), the drug is canceled.

With a duration of treatment with the drug for more than 10 days, it is necessary to monitor the picture of peripheral blood.

When determining glucose in the urine by a non-enzymatic method (for example, by the method of Benedict), false-positive results are possible.

During treatment can not be used ethanol - possible effects similar to the action of disulfiram (facial hyperemia, stomach and stomach spasm, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

Form release / dosage:

Powder for solution for intravenous and intramuscular injection, 250 mg, 500 mg and 1.0 g.

Packaging:According to 0.25 g, 0.5 g or 1.0 g of active substance in a bottle of colorless glass, corked with a rubber stopper, rolled up with an aluminum cap and closed with a plastic lid with a logo and an inscription "LUPIN". A label is attached to the vial.

One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

Store in a dry 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014934 / 01

Date of registration:17.10.2007

Expiration Date:Unlimited

The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India

Manufacturer: & nbsp

LUPIN, Ltd. India

Representation: & nbspLUPIN LIMITEDLUPIN LIMITED

Information update date: & nbsp10.01.2017

Illustrated instructions

Instructions

Cefanthral (Cefantral)