Cesolin

The drug Cezolin belongs to antimicrobial β-lactam drugs, and, in particular, to the group of cephalosporin antibiotics of the first generation. The active component of the drug is a derivative of 7-aminocephalosporanic acid.

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Indications Cesolin

Cezolin is indicated for the following diseases:

• Infectious microbial lesions of the respiratory system and otolaryngological organs (tonsillitis, pharyngitis, pneumonia and bronchitis, empyema of the pleura, lung abscesses, otitis, sinusitis).
• Infectious diseases of the urinary and biliary systems.
• Infections of the abdominal organs, skin, musculoskeletal system (peritonitis, osteomyelitis, pyoderma, furuncles, abscesses).
• Syphilis, gonorrhea.
• Infectious complications after burns, wounds or surgeries.
• Preventive measures carried out before or after surgical interventions.

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Release form

The drug is produced in the form of a lyophilized mass for the preparation of solutions for injection. The mass is packaged in vials, which are placed in individual cardboard packages.

One vial with lyophilized mass may contain the active component cefazolin 0.5 g or 1 g.

The drug is manufactured in India by the pharmaceutical company Lupin Ltd.

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Pharmacodynamics

Cezolin is a representative of the cephalosporin group of first-generation antibiotics for internal use. Kills bacteria by preventing the process of synthesis of the microbial cell wall. Has a wide range of antimicrobial action. It is active against gram (+) staphylococci, streptococci, corynebacteria, as well as gram (-) shigella, salmonella, escherichia, klebsiella, treponema, leptospira, etc. It is effective in combating some strains of enterobacteria and enterococci.

It does not show activity against indole-positive strains of Proteus, mycobacteria, anaerobic bacteria, or methicillin-resistant strains of staphylococci.

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Pharmacokinetics

After intramuscular injection of Cezolin in the amount of 0.5 and 1 g, the maximum plasma concentration of the active substance can be 38 and 64 mcg/ml. The peak content of cefazolin is observed 60-120 minutes after injection.

After intravenous injection of the drug in an amount of 1 g, the peak concentration is 180 mcg/ml, which can be observed already 6 minutes after the injection.

The active substance is able to penetrate into the joint capsules (usually after one and a half to two hours, in newborns - after 4-5 hours, in patients with renal dysfunction - from 3 to 42 hours), into the vascular walls and cardiac tissue, into the abdominal organs, into the urinary system, placenta, skin and mucous membranes.

The drug is excreted through the urinary system in an intact form, mainly within six hours after administration (up to 90%). After 24 hours, the excreted amount of the drug reaches 95%.

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Dosing and administration

The drug can be administered by intramuscular or intravenous injections (both jet and drip methods).

The standard daily dosage for an adult patient is from 1 to 4 g, with a maximum daily dosage of up to 6 g. The drug is administered about 3-4 times a day. The course of therapy is 1-2 weeks.

As a preventive measure in the postoperative period, Cezolin is administered intravenously: in the amount of 1 g half an hour before the start of surgery, the same amount during the operation, and from 500 mg to 1 g during the first 24 hours after surgery, at 8-hour intervals.

For patients with functional renal disorders, the dosage of the drug is adjusted depending on creatinine clearance: the Cezolin dosage regimen does not require adjustment with clearance of 55 ml per minute or higher, or with a creatinine level in the blood serum of 1.5 mg% or less. If the clearance drops to 35 ml per minute and the creatinine level reaches 3 mg%, the dosage can be left unchanged, limited to lengthening the intervals between administrations (at least 8 hours). With clearance up to 11 ml per minute and a creatinine level of up to 4.5 mg%, half of the prescribed dosage is administered at intervals of 12 hours. If the clearance is 10 ml per minute or lower and the creatinine level in the blood serum increases to 4.6 mg% or higher, half of the prescribed amount of the drug is used with time intervals of administration from 18 to 24 hours.

Treatment usually begins with a trial injection of 500 mg of the drug. In pediatrics, 1 month and older, 25 to 50 mg per kilogram of body weight per day are prescribed. If complications occur, the dosage of the drug can be increased to 100 mg per kilogram of body weight per day. The frequency of injections is up to 3-4 times per day.

If a child is diagnosed with renal dysfunction, the amount of the administered drug is linked to the blood purification rate:

• with clearance from 70 to 40 ml per minute, only 60% of the previously prescribed dosage is used with a time interval of 12 hours;
• with a clearance of 40 to 20 ml per minute, only 25% of the previously prescribed dosage is left with a time interval of 12 hours;
• with clearance from 5 to 20 ml per minute, 10% of the previously prescribed dosage is used once a day.

All listed dosages are used after a single administration of a “shock” dosage.

To prepare injection and infusion solutions, 500 mg of lyophilisate is diluted in 2 ml of injection water, and 1 g of lyophilisate is diluted in 4 ml.

For intravenous administration, the resulting preparation should be diluted in 5 ml of injection water. Administer carefully, slowly, over 4-5 minutes.

For drip administration, the lyophilisate is diluted in 100 ml of dextrose solution, isotonic solution or Ringer's solution. The lyophilized mass should be completely dissolved in the liquid. If the solution contains insoluble elements, it is not recommended to use such a preparation.

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Use Cesolin during pregnancy

The use of Cezolin should be avoided during pregnancy. The facts of penetration of the active component of the drug through the placental barrier have been proven.

During lactation, the drug is found in small quantities in mother's milk.

The use of Cezolin by pregnant and lactating women is not encouraged and can only be prescribed when the expected benefit to the woman is significantly higher than the possible danger to the embryo or newborn baby.

Contraindications

The drug Cezolin is not used:

• if you are prone to allergies to cephalosporin antibiotics;
• in infants up to 1 month;
• in severe renal dysfunction and chronic colitis.

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Side effects Cesolin

Cezolin may cause the following side effects:

• Development of allergy: reddening of the skin, rashes, itchy rash, difficulty breathing, swelling, joint pain, anaphylaxis, signs of erythema multiforme exudative, eosinophilia.
• Convulsions.
• In case of renal dysfunction: deterioration of the condition.
• Dyspeptic symptoms, attacks of nausea and vomiting, epigastric pain, cholestasis, hepatitis.
• Blood test: signs of leukopenia, neutropenia, hemolytic anemia, decrease or increase in the level of platelets in the blood.
• Disruption of the microflora of the intestinal, vaginal and oral cavity.
• Hyperactivity of liver transaminases, presence of creatine in the blood, increased prothrombin index.
• Pain at the injection site, development of inflammation of the venous wall during intravenous injection.

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Overdose

In case of overdose, side effects may increase, allergic reactions and anaphylaxis may develop.

There is no special drug that neutralizes the effect of Cezolin. In cases of overdose, symptomatic therapy is used; in case of digestive disorders, milk is given every 3 hours.

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Interactions with other drugs

Combinations of Cezolin with anticoagulants and diuretics should not be used. When Cezolin is used simultaneously with loop diuretics, tubular secretion may be blocked.

Aminoglycoside groups increase the risk of pathological damage to the renal system. In addition, Cezolin and aminoglycosides mutually inhibit each other's action.

Medicines that can block tubular secretion can increase intoxication of the body and slow down the elimination of toxic substances and metabolic products.

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Storage conditions

The lyophilisate drug must be stored in dry, ventilated places with a temperature of up to 30°C, in the original packaging.

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Shelf life

Shelf life – up to 2 years. The prepared solution cannot be stored and should be used immediately after preparation.

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