RANZOL 500 INJECTION

Indications

• Bacterial infections
• Surgical prophylaxis
• Skin infections
• Soft tissue infections
• Bone infections
• Joint infections
• Lower urinary tract infections

Dosage

Children: Child 3–11 months: 12.5 mg/kg twice daily, alternatively 125 mg twice daily for

Adults: 500 mg 2–3 times a day for 7 to 10 days; in severe infections, the dose may be increased to 1–1.5 g 3–4 times a day.

Mechanism of action

Cefazolin exerts its bactericidal effects by inhibiting cell wall synthesis in bacteria. It binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, inhibiting the third and final stage of cell wall synthesis. This action prevents the cross-linkage of peptidoglycan chains, which is essential for maintaining bacterial cell wall strength. The inhibition of cell wall synthesis leads to cell lysis, particularly in rapidly dividing bacteria, which are most susceptible to cefazolin's action.

Pharmacodynamics

Cefazolin demonstrates broad-spectrum antibiotic activity due to its ability to inhibit bacterial cell wall synthesis. It is effective against a variety of pathogens, including Staphylococcus aureus and Escherichia coli. Its rapid excretion via the urine contributes to its effectiveness, allowing for high serum levels shortly after administration.

Pharmacokinetics

Cefazolin is administered parenterally and achieves peak serum concentrations quickly. It is widely distributed in body tissues and fluids, including bones and joints. The drug is primarily eliminated through the kidneys, with a significant portion excreted unchanged in the urine. The half-life of cefazolin is approximately 1.8 to 2.2 hours in individuals with normal renal function.

Adverse effects

• anxiety
• asthenia
• bo.ne marrow disorders
• chest pain
• confusion
• cough
• drowsiness
• dyspnoea
• epileptogenic activity
• gastrointestinal discomfort
• hyperglycaemia
• hypersensitivity
• hypoglycaemia
• increased leucocytes
• increased risk of infection
• jaundice
• lymphopenia
• malaise
• nephropathy
• proteinuria
• sleep disorders
• tongue swelling
• vertigo

Precautions

• Reduce dose in moderate impairment
• Use with caution in patients with a history of hypersensitivity to beta-lactam antibiotics

Pregnancy

Not known to be harmful.

Breast-feeding

Present in milk in low concentration, but appropriate to use.

Storage

Store at room temperature, away from moisture and light.

Formulations

• Intravenous injection
• Intravenous infusion
• Deep intramuscular injection

Mechanism of action

In vitro tests demonstrate that the bactericidal action of cephalosporins results from inhibition of cell wall synthesis. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins. Bactericidal; action depends on ability to reach and bind penicillin-binding proteins located in bacterial cytoplasmic membranes; cephalosporins inhibit bacterial septum and cell wall synthesis, probably by acylation of membrane-bound transpeptidase enzymes. This prevents cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity. Also, cell division and growth are inhibited, and lysis and elongation of susceptible bacteria frequently occur. Rapidly dividing bacteria are those most susceptible to the action of cephalosporins. /Cephalosporins/

Pharmacodynamics

Cefazolin (also known as cefazoline or cephazolin) is a semi-synthetic first generation cephalosporin for parenteral administration. Cefazolin has broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.