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

Pharmacodynamics:Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide range of action. It is active against Gram-positive and Gram-negative microorganisms resistant to other antibiotics: Staphylococcus spp. (Including Staphylococcus aureus, including strains forming penicillinase), Staphylococcus epidermidis (except for Staphylococcus epidermidis and Staphylococcus aureus, methicillin-resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella spp. (including Klebsiella pneumoniae), Borrelia burgdorferi, Morganella morganii, Neisseria gonorrhoeae (incl.strains forming penicillinase), Acinetobacter spp., Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Eubacter spp., Propionibacterium spp., Clostridium spp. (including Clostridium perfringens), Citrobacter spp., Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri), Serratia spp., some strains of Pseudomonas aeruginosa, Neisseria meningitidis, Neisseria gonorrhoeae, Bacteroides spp. (including some strains of Bacteroides fragilis), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. Most strains of Clostridium difficile are stable. Resistant to most beta-lactamases of gram-positive and gram-negative microorganisms.

Pharmacokinetics:

After a single intravenous (IV) dose of 0.5 g, 1 g and 2 g, the maximum concentration in the blood plasma (C max) is determined after 5 minutes and is 39 μg / ml, 101.7 μg / ml and 214 μg / ml respectively. After intramuscular (IM) administration of the drug in doses of 0.5 g and 1 g of C max is determined after 30 minutes and is 11 μg / ml and 21 μg / ml, respectively. Communication with blood plasma proteins is 30-50%. Bioavailability is 90-95%.

Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, cerebrospinal fluid, sputum, bile, urine) of the body. The volume of distribution is 0.25-0.39 l / kg. The half-life (T1 / 2) is 1 hour with IV injection and 1-1.5 hours with the IM. It is excreted by the kidneys - 20-36% unchanged, the rest is in the form of metabolites (12-25% in the form of pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites - M2 and M3,deprived of antimicrobial action). In chronic renal failure (CRF) and in elderly people, T1 / 2 increases by 2 times. T1 / 2 in newborn - 0.75-1.5 hours in premature neonates (body weight less than 1500 g) was increased to 4.6 hours; in children with a body weight of more than 1500 g - 3.4 hours. With repeated iv administration in doses of 1 g every 6 hours for 14 days cumulation is not observed. Penetrates into breast milk, passes through the placental barrier.

Indications:

Infectious-inflammatory diseases caused by susceptible to cefotaxime microorganisms: central nervous system infections (meningitis), respiratory tract and LOP tract, urinary tract, bones, joints, skin and soft tissue of the pelvic organs, gonorrhea, infected wounds and burns, peritonitis , septicemia, abdominal infections, endocarditis, Lyme disease (Lyme disease), infections due to immune deficiency.

Prevention of infections after surgery (including urological, obstetric-gynecological, on the gastrointestinal tract).

Contraindications:Hypersensitivity to cefotaxime, penicillin, other cephalosporins, carbapenems, pregnancy,lactation period; in case of dissolution of the drug with lidocaine 1%: 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:Newborn period, chronic renal failure, ulcerative colitis (including in the anamnesis).

Pregnancy and lactation:The use of the drug during pregnancy is contraindicated. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

The drug is administered intravenously (jet or drip) and intramuscularly. Adults and children over 12 years of age (with a body weight of 50 kg or more):

- with uncomplicated infections - in / m or / in, 1 g every 12 h;

- with uncomplicated acute gonorrhea - in / m, 0.5-1 g once;

- at infections of average gravity - in / m or in / in, on 1-2 g every 8-12 h;

- with severe and life-threatening infections, for example, with meningitis-in / in, 2 g every 4-8 hours, the maximum daily dose is 12 g. The duration of treatment is set individually.

In order to prevent the development of infections before surgery, one is administered once during the initial general anesthesia. If necessary, the administration is repeated after 6-12 hours.

At caesarean section - at the time of imposition of the clamps on the umbilical vein-in / in, 1 g, then 6 and 12 hours after the first dose-additionally 1 g. When creatinine clearance is 20 ml / min / 1.73 m2 and less the daily dose is reduced by 2 times.

Premature and newborns under the age of 1 week. - IV 50 mg / kg every 12 hours; at the age of 1-4 weeks. - IV 50 mg / kg every 8 hours;

Children from 1 month. (with a body weight of up to 50 kg) - in / in or / m 50-180 mg / kg in 4 - 6 injections. In severe infections, incl. meningitis, the daily dose to children is increased to 100-200 mg / kg, IM or IV in 4-6 injections, the maximum daily dose is 12 g.

Rules for the preparation of injection solutions: for intravenous injection as a solvent used water for injection (1 g diluted in 10 ml of solvent), the drug is administered slowly for 3-5 minutes; for intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1-2 g diluted in 50-100 ml solvent); duration of infusion is 50-60 minutes; for the / m administration using water for injection or 1% lidocaine solution (for a dose of 1 g - 4 ml).

Side effects:

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

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

From the central nervous system: headache, dizziness, encephalopathy, motor disorders, convulsions.

From the gastrointestinal tract: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function, stomatitis, glossitis, pseudomembranous colitis, hepatitis, jaundice.

From the urinary system: disturbance of kidney function, oliguria, interstitial nephritis.

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

Laboratory indicators: azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia,hyperbilirubinemia,

false positive test of Coombs.

Local reactions: phlebitis, pain along the vein, tenderness and

infiltration at the site of intramuscular injection.

Other: Superinfection (in particular, candidal vaginitis).

Overdose:

Symptoms: seizures, encephalopathy (in the case of high doses, especially in patients with renal insufficiency), tremor, neuromuscular excitability.

Treatment: symptomatic, there is no specific antidote.

Interaction:

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

The probability of kidney damage increases with simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics. Drugs that block tubular secretion, increase the plasma concentrations of cefotaxime and slow down its excretion. 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.

Patients who had a history of allergic reactions to penicillins may have increased sensitivity to the antibiotics of the cephalosporin group.

When the drug is treated for more than 10 days, it is necessary to monitor the pattern of peripheral blood.

During treatment with cefotaxime, it is possible to obtain a false positive sample of Coombs and a false positive urine reaction to glucose. During treatment, use ethanol it is impossible because of the possibility of disulfiram-like reactions (facial hyperemia, abdominal and stomach cramps, nausea, vomiting, headache, lowering of blood pressure, tachycardia, dyspnea).

Effect on the ability to drive transp. cf. and fur:There is no data on the effect of the drug on the ability to drive transport and carry out work that requires increased concentration of attention. Given the likelihood of side effects from the central nervous system, care should be taken when driving vehicles or working with mechanisms.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.

Storage conditions:In 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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N011830 / 01

Date of registration:05.08.2011

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

Manufacturer: & nbsp

CADILA PHARMACEUTICALS, Ltd. India

Representation: & nbspCADILA PHARMACEUTICALS LTD. CADILA PHARMACEUTICALS LTD. India

Information update date: & nbsp01.11.2015

Illustrated instructions

Instructions

Ortaxime (Oritaxim)