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

Cephalosporin antibiotic of the first generation for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide spectrum of action, is active against Gram-positive (Staphylococcus spp., Including Staphylococcus aureus (not producing and producing penicillinase strains), Streptococcus pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp ., Salmonella spp., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) Of microorganisms. It is active against Haemophilus influenzae, some strains of Enterobacter spp. and Enterococcus spp.

Ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.

Pharmacokinetics:

Time to reach the maximum concentration in plasma (TCmax) with intramuscular (IM) administration at a dose of 500 and 1000 mg, respectively - 2 and 1 hour. The maximum plasma concentration (Cmax) is 38 and 64 μg / ml, respectively; after intravenous (iv) administration of TCmax - at the end of infusion. With intravenous administration of cefazolinum in a dose of 1000 mg Cmax -180 mcg / ml. Penetrates into joints, tissues of the cardiovascular system, into the abdominal cavity, kidneys and urinary tract, placenta, middle ear, respiratory tract, skin and soft tissues. In small amounts excreted in breast milk. The concentration in the wall of the gallbladder and bile is much higher than in the blood plasma. With obstruction of the gallbladder, the concentration in the bile is less than in the plasma. The volume of distribution is -0.12 l / kg. The connection with plasma proteins is 85%. Half-life (T_1/2) with a / m introduction -1.8 h, with iv in the introduction -2 h. In case of a violation of the kidney function T_1/2 - 20-40 hours.

Excreted mainly by the kidneys in unchanged form: during the first 6 to 60-90%, after 24 hours - 70-95%. Stam in urine is 1000 μg / ml and 4000 μg / ml after IM injection at doses of 500 mg and 1000 mg, respectively.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to cefazolin: upper and lower respiratory tract, LOP-organs, urinary and biliary tract, pelvic organs, skin and soft tissues, bones and joints; endocarditis, sepsis, peritonitis, mastitis; wound, burn and postoperative infections; syphilis, gonorrhea.

Preventive maintenance of surgical infections in the pre- and postoperative period.

Contraindications:Hypersensitivity to cefazolin, cephalosporin group preparations and other beta-lactam antibiotics, neonatal period (up to 1 month).

Carefully:Renal / hepatic insufficiency, intestinal diseases (including colitis in the anamnesis), children's age from 1 month to 1 year.

Pregnancy and lactation:At pregnancy appoint or nominate only under vital indications. If you need to use the drug during lactation, breastfeeding is discontinued.

Dosing and Administration:

Intravenous (jet and drip), intramuscularly.

The average daily intake for adults is 1-4 g; the frequency of administration is 3-4 times a day. For infections of moderate severity caused by sensitive Gram-positive microorganisms, 0.25-0.5 g every 8 hours. With pneumococcal pneumonia - 0.5 g every 12 hours.In acute uncomplicated diseases of the urinary tract - 1 g every 12 hours. The maximum daily dose is 6 g (in rare cases - 12 g). The average duration of treatment is 7-10 days.

For prevention of postoperative infection - 1 z intravenously 30-60 minutes prior to surgery, 0.5-1 g - during surgery and at 0.5-1 g - every 6-8 hours during the first day after surgery.

Patients with impaired renal function require a change in the dosing regimen in accordance with the values of creatinine clearance (CK). When QA 55 ml / min or more or in a plasma creatinine concentration of 1.5 mg% or less can be administered a full dose. When QA 54-35 ml / min or plasma creatinine concentration 3-1,6% mg can be administered a full dose, but the interval between injections to increase up to 8 hours. When QA 34-11 ml / min, or a creatinine concentration in the plasma 4 5-3,1 mg% - 1A doses at intervals of 12 hours when QA 10 ml / min or less or plasma creatinine concentration 4.6 mg% or more -. 1/2 the average dose every 18-24 hours All recommended. doses are given after the initial dose corresponding to the severity of the infection.

The average daily dose for children older than 1 month is 25-50 mg / kg; with severe course of infection, the dose can be increased to 100 mg / kg / day. Multiplicity of administration - 3-4 times a day.

In children with impaired renal function, correction of the dosing regimen is performed depending on the values of the CC. At CC 70-40 ml / min - 60% of the average daily dose is administered every 12 hours. At KK 40-20 ml / min - 25% of the average daily dose with an interval of 12 hours. Children with KK 5-20 ml / min - 10 % of the average daily dose every 24 hours. All recommended doses are administered after the initial dose corresponding to the severity of the infection.

Preparation of solutions:

For intramuscular injection, 0.5 g of the drug is dissolved in 2 ml of water for injection, 1 g is dissolved in 4 ml of water for injection, 0.25-0.5% solution of procaine, 0.9% solution of sodium chloride.

For intravenous fluid administration, a single dose of the drug is diluted in 10 ml of 0.9% sodium chloride solution and injected slowly for 3-5 minutes.

For intravenous drip injection, the drug is dissolved in 50-100 ml of 0.9% sodium chloride solution, 5-10% dextrose solution, Ringer's solution; infusion is carried out for 20-30 minutes (rate of administration of 60-80 drops per minute). During the dilution, the vials are vigorously shaken until completely dissolved.

Side effects:

Allergic reactions: hyperthermia, skin rashes, hives, itching, bronchospasm, eosinophilia, Quincke's edema,anaphylactic shock, erythema multiforme, toxic epidermal necrolysis, malignant exudative erythema (Stevens-Johnson syndrome).

From the nervous system: convulsions.

From the urinary system: in patients with kidney disease in the treatment of large doses (6 g) - renal dysfunction (in these cases - the dose is reduced, and the treatment is controlled by the dynamics of urea nitrogen and creatinine in the blood).

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, decrease appetite, pseudomembranous colitis, cholestatic jaundice, hepatitis.

From the hematopoiesis: leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, lymphocytosis, hemolytic anemia.

Other: fever, arthralgia, dysbacteriosis, superinfection caused by resistant to antibiotic strains, candidamycosis (including candidal stomatitis, candidiasis vaginitis).

Laboratory indicators: a positive test of Coombs, an increase in the activity of "liver" transaminases, hyperbilirubinemia, hypercreatininaemia, an increase in prothrombin time.

Local reactions: with the / m introduction - soreness (at the injection site), education infiltrates and abscesses, with / in the introduction - phlebitis, thrombophlebitis.

Overdose:

Symptoms: dizziness headache, paresthesia, possibly the development of seizures (especially in patients with kidney disease). Laboratory indicators: increased concentration of creatinine, blood urea nitrogen, increased activity of liver enzymes, hyperbilirubinemia, thrombocytosis.

Treatment: immediately stop the introduction of the drug, carefully monitor the vital functions of the body and the relevant laboratory indicators. Conduction of symptomatic therapy. In severe cases, hemodialysis is possible. Peritoneal dialysis is not effective.

Interaction:

It is not recommended simultaneous use with anticoagulants and diuretics. With the simultaneous use of cefazolin and loop diuretics, blockade of its tubular secretion occurs.

Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation). Drugs that block tubular secretion, increase concentration in the blood, slow down excretion and increase the risk of developing toxic reactions.

Special instructions:

Patients who had a history of allergic reactions to penicillins, carbapenems may have increased sensitivity to cephalosporin antibiotics. During treatment with cefazolinum, false positive and indirect Coombs probes can be obtained, as well as a false positive urine reaction to glucose.

When the drug is used, there may be an exacerbation of diseases of the gastrointestinal tract, especially colitis. When using cefazolin, pseudomembranous colitis may occur. Therefore, it is important to keep this diagnosis in mind when diarrhea occurs during treatment with the drug. Light forms of colitis do not require special treatment, it is enough to stop the introduction of the drug; mild or severe cases may require special treatment. The use of drugs that inhibit the intestinal peristalsis is contraindicated.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g.

Packaging:

0.5 g or 1.0 g of active substance is placed in a bottle of colorless transparent glass, sealed with a rubber stopper, rolled up with an aluminum cap and closed with a plastic lid.

Solvent - "Water for Injection", 2 ml or 5 ml produced by OJSC "Pharmasintez", Russia (RU No. LP-001844)

1. One bottle with 0.5 g of the drug together with instructions for use in a pack of cardboard.

2. One bottle with 1.0 g of the drug together with instructions for use in a pack of cardboard.

3. One vial with 0.5 g of preparation and one ampoule with 2 ml of solvent together with instructions for use are placed in a cardboard box with septums.

4. One bottle of 0.5 g of the drug and one ampoule with 5 ml of solvent together with the instruction for use are placed in a cardboard box with septums.

5. One vial with 1.0 g of preparation and one ampoule with 5 ml of solvent together with instructions for use are placed in a cardboard box with septums.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N016309 / 01

Date of registration:20.05.2005

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

LYKA LABS, Ltd. India

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp24.02.2018

Illustrated instructions

Instructions

Lizolin (Lyzolin)