Orizolin (Powder) Instructions for Use

Marketing Authorization Holder

Cadila Healthcare Ltd. (India)

ATC Code

J01DB04 (Cefazolin)

Active Substance

Cefazolin (Rec.INN registered by WHO)

Dosage Form

Orizolin

Powder for solution for intravenous and intramuscular administration 1 g: vial. 1 pc.

Dosage Form, Packaging, and Composition

1 g – vials (1) – cardboard packs.

Clinical-Pharmacological Group

First generation cephalosporin

Pharmacotherapeutic Group

Antibiotic-cephalosporin

Pharmacological Action

Cephalosporin antibiotic of the first generation with a broad spectrum of action. It has a bactericidal effect.

It is active against gram-positive bacteria: Staphylococcus spp. (strains producing and not producing penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp., Escherichia coli, Klebsiella spp.

It is also active against Spirochaetoceae, Leptospira spp.

It is not active against Pseudomonas aeruginosa, indole-positive strains of Proteus spp., Mycobacterium tuberculosis, anaerobic bacteria.

Pharmacokinetics

Cefazolin is poorly absorbed from the gastrointestinal tract and is therefore administered intramuscularly or intravenously. After intramuscular administration of a 500 mg dose, the C_max in plasma is reached in 1-2 hours and is 30 µg/ml.

Plasma protein binding is about 85%.

Cefazolin penetrates into bone tissue, ascitic fluid, pleural and synovial fluids, but is not detected in the CNS.

The T_1/2 of cefazolin from plasma is about 1.8 hours.

Cefazolin is excreted in the urine unchanged, mainly by glomerular filtration and to a small extent by tubular secretion. After intramuscular administration, at least 80% of the dose is excreted within 24 hours. After intramuscular administration of 500 mg and 1 g doses, the C_max in urine is 1 mg/ml and 4 mg/ml, respectively.

There is evidence of high concentrations of cefazolin in bile, although it is excreted by this route in small amounts.

The T_1/2 from plasma is increased in patients with impaired renal function.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to cefazolin, including diseases of the upper and lower respiratory tract, urinary and biliary tract, pelvic organs, skin and soft tissues, bones and joints, endocarditis, sepsis, peritonitis, otitis media, osteomyelitis, mastitis, wound, burn and postoperative infections, syphilis, gonorrhea.

ICD codes

Dosage Regimen

The dosage is set individually, taking into account the severity and localization of the infection, and the sensitivity of the pathogen.

It is administered intramuscularly or intravenously (bolus or drip). The average daily dose for adults is 1 g, the frequency of administration is 2-4 times/day.

For the prevention of postoperative infection, it is administered at a dose of 1 g 30 minutes before surgery, 0.5-1 g during surgery, and 0.5-1 g every 6-8 hours for 24 hours after surgery.

Maximum dose 6 g/day.

For children, the average daily dose is 20-40 mg/kg; in severe infections, the dose can be increased to 100 mg/kg/day. The duration of treatment is 7-10 days.

Adverse Reactions

From the digestive system nausea, vomiting, diarrhea are possible; rarely – a transient increase in the activity of hepatic transaminases.

Allergic reactions urticaria, skin itching, eosinophilia, fever are possible; in isolated cases – angioedema, arthralgia, anaphylactic shock.

Effects due to chemotherapeutic action candidiasis, pseudomembranous colitis.

From the hematopoietic system rarely – reversible leukopenia, neutropenia, thrombocytopenia.

From the urinary system rarely – impaired renal function.

Local reactions pain at the intramuscular injection site is possible.

Contraindications

Children under 1 month of age, hypersensitivity to cephalosporins.

Use in Pregnancy and Lactation

It crosses the placental barrier.

Low concentrations of cefazolin are detected in breast milk.

Use during pregnancy and lactation is justified only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Contraindicated in children under 1 month of age.

Use in children over 1 month of age is possible according to the dosage regimen.

Special Precautions

Use with caution in patients with impaired renal function.

In patients with hypersensitivity to penicillins, allergic reactions to cephalosporin antibiotics are possible.

During treatment, a false-positive urine reaction for sugar is possible.

Cefazolin is removed by hemodialysis.

Drug Interactions

With simultaneous use with “loop” diuretics, tubular secretion of cefazolin is blocked (such a combination is not recommended).

Cefazolin can cause disulfiram-like reactions when used simultaneously with ethanol.

Probenecid impairs the excretion of cefazolin.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.