Zolin - instructions for use, doses, side effects, contraindications

Cephalosporin antibiotic of the first generation for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. It has a wide spectrum of antimicrobial action. It is active both against Gram-positive (Staphylococcus spp., Bp Staphylococcus aureus (not producing and producing penicillinase), 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 also active against Haemophilus influenzae, some strains of Enterobacter spp. and Enterococcus spp.

The drug is ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.

Pharmacokinetics:

With intramuscular (intramuscular) and intravenous (intravenous) administration, the drug is rapidly absorbed and distributed in tissues and body fluids. Time to reach the maximum concentration in the blood (TCam) with a / m dose of 0.5 g and 1 g is 2 hours and 1 hour; the maximum concentration (C max) is 38 and 64 μg / ml; after intravenous administration of TCmax - at the end of infusion, after intravenous administration of 1 g of Cmax -180 μg / 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. Concentration in the tissue of the gallbladder and bile is much higher than in 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%. The half-life period (T1 / 2) with a / m introduction is -1.8 h, with an iv injection of -2 hours. If the renal function T1 / 2-20-40 h is disturbed,

It is excreted mainly by the kidneys in an unchanged form: within the first 6 hours, 60-90%, after 24 hours, 70-95%. Stam in the urine is 1000 μg / ml and 4000 μg / ml after IM in doses of 0.5 g and 1 g, respectively.

Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation: JIOP-organs (incl.otitis media); infections of the upper and lower respiratory tract, urinary and bile ducts, 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 cephalosporins and other beta-lactam antibiotics.

Pregnancy and lactation.

Children up to 1 month.

Carefully:Renal / hepatic insufficiency, pseudomembranous colitis, intestinal diseases, children under 1 year.

Dosing and Administration:

The dosage regimen is set individually, taking into account the severity of the course and localization of the infection, the sensitivity of the pathogen, the age of the patient. The drug can be administered intramuscularly, intravenously (struino or drip). The average daily intake for adults is 1-4 g; the frequency of administration is 3-4 times a day. The maximum daily dose is 6 g. The average duration of treatment is 7-10 days.

For the prevention of postoperative infection, 1 g intravenously is administered 0.5-1 h before the operation, 0.5-1 g during the operation and 0.5-1 g every 8 h during the first day after the operation.

In patients with impaired renal function, a change in the dosing regimen is required, taking into account the values of creatinine clearance (CC): at a CS of 55 ml / min or more, or with a plasma creatinine concentration of 1.5 mg% or less, a full dose can be administered; with SC 54-35 ml / min or creatinine concentration in plasma of 3-1.6 mg%, a full dose can be administered, however, the intervals between injections should be increased to 8 hours; with SC 34-11 ml / min or creatinine concentration in plasma 4.5-3.1 mg% - 1/2 dose at intervals of 12 hours; with CC 10 ml / min or less, or with a plasma creatinine concentration of 4.6 mg% or more - 1/2 of the usual dose every 18-24 hours. All recommended doses are administered after the administration of an initial dose corresponding to the severity of the infection. Children 1 month and older - 20-50 mg / kg / day; In severe 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, the correction of the dosing regimen is performed depending on the values of the CC: at a CC of 70-40 ml / min - 60% of the average daily dose and injected every 12 hours; with KK 40-20 ml / min - 25% of the average daily dose with an interval of 12 hours; with KK 5-20 ml / min - 10% of the average daily dose every 24 hours. All recommended doses are applied after the introduction of an initial dose corresponding to the severity of the infection.

Preparation of solutions

For intramuscular injection: 0.25 g of the drug is dissolved in 1 ml of water for injection, 0.5 g in 2 ml of water for injection, 1 g in 4 ml of water for injection or in 0.9% solution of sodium chloride, or 0.25 - 0.5% solution of procaine. For intravenous drip injection, the drug is dissolved in 50-100 ml of a 0.9% solution of sodium chloride or 5-10% solution of dextrose, depending on the dose of the drug; infusion is carried out for 20-30 minutes (rate of administration of 60-80 drops per minute).

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.

During the dilution, the vials are vigorously shaken until completely dissolved.

Side effects:

Allergic reactions: hyperthermia, skin rash, urticaria, skin itch, bronchospasm, eosinophilia, Quincke's edema, arthralgia, anaphylactic shock. erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome).

From the nervous system: convulsions

From the urinary system: In patients with kidney disease when treating large doses of cefazolin (6 g), renal dysfunction may occur. In these cases, the dose of the drug 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, pseudomembranous colitis, in rare cases - cholestatic jaundice, hepatitis.

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

With long-term treatment - Dysbacteriosis, superinfection caused by resistant to antibiotic strains, candidiasis (including candidiasis stomatitis).

Laboratory indicators: positive Coombs reaction, increased activity of "liver" transaminases, hypercreatininaemia, an increase in prothrombin time.

Local reactions: with intramuscular administration of the drug in rare cases - soreness at the injection site, with intravenous injection - phlebitis.

Overdose:

Symptoms: pain, inflammatory reactions and phlebitis at the site of administration; dizziness, headache, paresthesia, possibly the development of seizures (especially in patients with kidney disease).

Laboratory indicators: increased concentration of creatinine, blood urea nitrogen, activity of liver enzymes and bilirubin; thrombocytosis.

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

Interaction:

Do not use cefazolin together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, macrolides, lincosamides, chloramphenicol), since in vitro studies have shown that antagonism exists between them.

With the simultaneous use of oral anticoagulants or high doses of heparin, it is necessary to monitor the parameters of blood coagulability. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs that block tubular secretion, including probenecid, slow excretion, increases concentration in the blood and increase the risk of 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 prescribing the drug may exacerbate diseases of the gastrointestinal tract, especially colitis. In the presence of severe persistent diarrhea, it is necessary to consider the likelihood of developing pseudomembranous colitis associated with the use of an antibiotic. In this case, immediately cefazolin treatment is stopped and appropriate treatment is prescribed (use of drugs that affect peristalsis is contraindicated).

Safety of use in preterm infants and children of the first month of life is not established.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection of 250 mg, 500 mg and 1000 mg.

Packaging:The amount of the preparation, equivalent to 250 mg, 500 mg or 1000 mg of cefazolinum, to a vial of colorless glass, sealed with a rubber stopper, crimped with an aluminum cap and closed with a plastic lid. One bottle together with the instruction for use is placed in a cardboard box; 5, 20 or 50 bottles along with the instruction for use are placed in a cardboard box (for hospitals).

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Do not freeze. List B.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012534 / 01

Date of registration:04.03.2010

Expiration Date:Unlimited

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

Manufacturer: & nbsp

AUROBINDO PHARMA, Ltd. India

Representation: & nbspAurobindo Pharma, ZAOAurobindo Pharma, ZAO

Information update date: & nbsp15.10.2017

Illustrated instructions

Instructions

Zolin (Zolin)