SOFEL [Cefazolin] 1 g Powder for solution for intramuscular administration

instructions for the medical use of the medicinal product

SOFEL

Tradename

Sofel, Софел

International non-proprietary name or generic name

Cefazolin, Цефазолин

Composition

Each vial contains: cefazolin sodium eq. cefazolin 1.0 g.

The solvent ampoule contains: novocaine* 0.5% 5 ml.

Dosage form

Powder for the preparation of solution for injection.

Pharmacotherapeutic group

Antibiotic cephalosporin.

ATX code – J01DB04.

Pharmacological properties

Pharmacodynamics

First generation cephalosporin antibiotic for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms.

Has a wide spectrum of action, active against gram-positive (Staphylococcus spp., Staphylococcus aureus (non-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.) microorganisms. Active regarding Haemophilus influenzae, some strains Enterobacter spp. и Enterococcus spp.

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

Pharmacokinetics

Cefazolin is rapidly absorbed when administered intramuscularly; peak plasma concentrations are reached 60 minutes after injection and amount to 37–64 mcg/ml. When administered intravenously, the Cmax of the drug is determined immediately after administration and is 185 mcg/ml. The bactericidal concentration in the blood persists for 8–12 hours. It penetrates well into the tissues and fluids of the body and is detected in therapeutic concentrations in mucous membranes, sputum, bone tissue, cerebrospinal fluid, penetrates the placental barrier and in very low concentrations into breast milk. 90% of the drug binds to blood plasma proteins. It is excreted from the body unchanged in urine (about 90%). The drug is metabolized in small quantities in the liver and excreted in the bile.

T½ - about 2 hours after IM administration, 1.8 hours - after IV administration. If renal function is impaired, T½ is 3–42 hours.

Indications for use

Infectious and inflammatory diseases caused by pathogens sensitive to the drug:

• sepsis;

• peritonitis;

• endocarditis;

• respiratory tract infections;

• genitourinary tract infections, including syphilis and gonorrhea;

• infectious lesions of bones and joints.

Prevention of surgical infections in the pre- and postoperative period.

Contraindications

Hypersensitivity to drugs of the cephalosporin group and other beta-lactam antibiotics, neonatal period (up to 1 month).

*procaine hydrochloride 0.5% 5 ml

Method of administration and dosage

Administer intramuscularly or intravenously (stream or drip).

The dose of the drug is set individually, taking into account the severity of the disease, the location of the infection and the sensitivity of the pathogen, as well as age and body weight, and kidney function.

The average daily dose for adults is 1 g; frequency of administration - 2 times a day. The maximum daily dose is 6 g; the frequency of administration can be increased to 3-4 times a day. The average duration of treatment is 7-10 days. For the prevention of postoperative infectious complications prescribe 1 g 30 minutes before surgery; 0.5-1 g during surgery and 0.5-1 g every 6-8 hours during the day after surgery.

In patients with impaired renal function, the dosage regimen is set taking into account the values of creatinine clearance (CC). When CC is more than 55 ml/min, the dosage regimen, as a rule, does not require correction. With a CC of 54-35 ml/min, a single dose can remain unchanged with an interval between administrations of 12 hours. When CC is 34-11 ml/min, the single dose should be reduced by 2 times with intervals between administrations of 11 hours. For CC less than 10 ml/min, half the usual dose is prescribed every 18-24 hours. All recommendations for adjusting the dosage regimen are applied after establishing the initial dose corresponding to the severity of the infection.

The average daily dose for children over 1 month is 25-50 mg/kg; in case of severe infection, the dose can be increased to 100 mg/kg per day. The frequency of administration is 3-4 times a day. In children with impaired renal function, the dosage regimen is adjusted depending on the CC values. With CC 70-40 ml/min - 60% of the average daily dose is administered after 12 hours. With CC 40-20 ml/min - 25% of the average daily dose with an interval of 12 hours. Children with CC 5-20 ml/min - 10 % of average daily dose every 24 hours.

Preparation of the solution

For intramuscular administration, 1 g of the drug is dissolved in 3-4 ml of 0.5% novocaine solution. For intravenous jet administration, a single dose of the drug is diluted in 5-10 ml of water for injection, then administered slowly over 3-5 minutes. For intravenous drip administration, the drug is diluted in 50 - 100 ml of 5% or 10% glucose solution, 0.9% sodium chloride solution, Ringer's solution, 5% sodium bicarbonate solution. During dilution, the bottle must be shaken vigorously until completely dissolved. The maximum single dose for intramuscular administration is 1 g; the drug should be administered only into large muscles. A solution containing novocaine cannot be administered intravenously. Only freshly prepared solutions should be used.

Special instructions and precautions

Before using the drug, consult your doctor.

Patients with impaired renal excretory function require adjustment of the cefazolin dosage regimen.

In patients with a history of allergic reactions to penicillins, cross-hypersensitivity to cephalosporins is observed.

During treatment with the drug, it is possible to obtain false-positive direct and indirect Coombs tests, as well as a false-positive urine reaction to sugar.

When prescribing the drug, exacerbation of diseases of the gastrointestinal tract, especially colitis, is possible. In the presence of severe persistent diarrhea, the possibility of developing antibiotic-associated pseudomembranous colitis must be considered. In this case, immediately stop therapy with Sofel and prescribe appropriate treatment (the use of drugs that affect peristalsis is contraindicated).

Prescribed with caution for renal failure, intestinal diseases (including a history of colitis) and children aged 1-12 months.

Influence on the ability to drive vehicles and mechanisms

Patients should be careful when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Use during pregnancy or lactation

Use during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Interaction with other medicinal products

Cefazolin should not be used together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, macrolides, lincosamides, chloramphenicol), since in vitro studies have shown that there is antagonism between them.

With the simultaneous use of oral anticoagulants or high doses of heparin, it is necessary to monitor blood clotting parameters.

There is a synergistic antibacterial effect when combined with aminoglycoside antibiotics, vancomycin, rifampicin. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).

Drugs that block tubular secretion, including probenecid, slow down the elimination of cefazolin, increase its concentration in the blood and increase the risk of developing toxic reactions.

When used simultaneously with loop diuretics (furosemide, ethacrynic acid), tubular secretion of cefazolin is blocked (co-administration should be avoided).

Cefazolin may cause disulfiram-like reactions when used concomitantly with ethanol.

Cefazolin, by suppressing intestinal flora, interferes with the synthesis of vitamin K. Therefore, when used simultaneously with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs (NSAIDs), salicylates), the risk of bleeding increases. For the same reason, when used simultaneously with anticoagulants, an increase in the anticoagulant effect is observed.

Side effect

Allergic reactions: hyperthermia, skin rash, urticaria, itching, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, erythema multiforme, Stevens-Johnson syndrome.

From the nervous system: dizziness, convulsions.

From the respiratory system: suffocation, shortness of breath.

From the urinary system: an increase in the concentration of blood urea nitrogen, hypercreatininemia (usually in patients with impaired renal function when treated with large doses (6 g) - in these cases the dose is reduced and treatment is carried out under the control of the dynamics of the concentration of urea nitrogen and creatinine in the blood).

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, rarely - pseudomembranous colitis, cholestatic jaundice, hepatitis.

From the hematopoietic organs: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia.

Laboratory indicators: false-positive Coombs test, increased activity of “liver” transaminases, hypercreatininemia, increased prothrombin time.

Local reactions: with intramuscular injection - pain at the injection site, with intravenous injection - phlebitis.

Other: dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidal stomatitis).

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

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

Laboratory indicators: increased concentrations of creatinine, blood urea nitrogen, liver enzyme activity and bilirubin; false-positive Coombs reaction; thrombocytosis and thrombocytopenia, eosinophilia, leukopenia, as well as an increase in prothrombin time.

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

Storage conditions

Store at a temperature not exceeding 25°C.

Keep out of the reach of children!

Shelf life

3 years. Do not use after the expiry date stated on the package.

Vacation conditions

Released by prescription.

Release form

1 bottle of powder and 1 ampoule of solvent, 5 ml each, along with instructions for medical use in a cardboard box.

Manufacturer

The holder of trade mark and Marketing Authorization is:

«LIVE MEDICINE ILAÇ VE TIC. LTD. ŞTI.», Gökevler Mah.2312. Sk. Burc Istanbul 18 Esenyurt, ISTANBUL, TURKEY.