INJTAX 500

Indications

• Acute infections due to sensitive Gram-positive and Gram-negative bacteria
• Severe susceptible infections
• Surgical prophylaxis
• Meningitis
• Uncomplicated gonorrhoea
• Disseminated gonococcal infection

Dosage

Children: For children aged 1 month to 11 years, 50 mg/kg for a single dose; for children aged 12 to 17 years, 1 g for a single

Adults: 1 g every 12 hours for acute infections; 400 mg for a single dose in uncomplicated gonorrhoea; 200-400 mg daily in 1-2 divided doses for meningitis.

Mechanism of action

Cefotaxime exerts its bactericidal effect by inhibiting cell wall synthesis through a high affinity for penicillin-binding proteins (PBPs), particularly PBP Ib and PBP III. This inhibition disrupts the integrity of the bacterial cell wall, leading to cell lysis and death.

Pharmacodynamics

Cefotaxime has a broad spectrum of activity against a variety of pathogens, including both Gram-positive and Gram-negative bacteria. It is not effective against Pseudomonas aeruginosa. The drug's resistance to penicillinases enables it to treat infections that other antibiotics, including penicillins, cannot address. Its pharmacodynamic profile allows for effective treatment of various infections, including those of the respiratory tract, skin, and central nervous system.

Pharmacokinetics

Cefotaxime is administered via intramuscular or intravenous routes, with rapid absorption and distribution in bodily tissues. The drug is metabolized in the liver and excreted primarily through the kidneys. Dosage adjustments are necessary in patients with renal impairment, particularly when glomerular filtration rate is significantly reduced. The half-life of cefotaxime is approximately 1 hour, necessitating frequent dosing in severe infections.

Adverse effects

• Acute kidney injury
• Arthralgia
• Drug fever
• Dyspepsia
• Dyspnoea
• Facial edema
• Flatulence
• Genital pruritus
• Hypereosinophilia
• Jaundice
• Serum sickness-like reaction
• Thrombocytosis

Precautions

• Caution in severe renal impairment
• Dose adjustments required for renal function
• Consult local guidelines for intravenous use

Pregnancy

Not known to be harmful.

Breast-feeding

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

Storage

Store in a cool, dry place, protected from light.

Formulations

• Intravenous injection
• Intramuscular injection
• Intravenous infusion
• Tablet

Indications

• Bacterial meningitis
• Severe bacterial infections
• Pneumonia
• Sepsis
• Intra-abdominal infections
• Skin and soft tissue infections
• Urinary tract infections

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on the child's weight and age.

Adults: Refer to the BNF for specific dosing recommendations based on the type and severity of infection.

Mechanism of action

Cefotaxime exerts its antibacterial effects by inhibiting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, disrupting the peptidoglycan cross-linking necessary for cell wall integrity, leading to cell lysis and death.

Pharmacodynamics

Cefotaxime demonstrates time-dependent bactericidal activity. Its effectiveness is influenced by the duration of time the drug concentration remains above the minimum inhibitory concentration (MIC) of the target organism. It has a broad spectrum of activity against many strains of Escherichia coli, Klebsiella, and several other Enterobacteriaceae, as well as some gram-positive bacteria.

Pharmacokinetics

Cefotaxime is administered parenterally, typically via intravenous or intramuscular routes. It is rapidly absorbed, with peak plasma concentrations achieved shortly after administration. The drug is widely distributed in body tissues and fluids, including the central nervous system. Cefotaxime is primarily eliminated by the kidneys, with a half-life of about 1 hour in individuals with normal renal function. Dosage adjustments may be necessary in patients with renal impairment.

Contra-indications

• Hypersensitivity to cefotaxime or any cephalosporins
• History of severe allergic reactions to penicillins
• Severe renal impairment (when dose adjustment is not possible)

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Pruritus
• Severe allergic reactions (anaphylaxis)
• Nephrotoxicity
• Hematological reactions (e.g., leukopenia, thrombocytopenia)
• Clostridium difficile-associated diarrhea

Interactions

• Probenecid may increase cefotaxime levels
• Concurrent use with aminoglycosides may increase nephrotoxicity
• Oral contraceptives may have reduced efficacy

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of superinfection
• Caution in patients with a history of gastrointestinal disease, particularly colitis
• Monitor renal function during prolonged therapy

Pregnancy

Cefotaxime is classified as category B; animal studies have not shown an adverse effect on the fetus, but there are no adequate and well-controlled studies in pregnant women.

Breast-feeding

Cefotaxime is excreted in breast milk; caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, protect from light. Reconstituted solutions should be used promptly; if stored, they should be kept refrigerated and used within 24 hours.

Formulations

• Cefotaxime sodium injection
• Cefotaxime powder for injection

Indications

• Surgical procedures
• Injection of medications
• Preparation of sterile pharmaceutical products
• Management of open wounds
• Use in controlled environments such as hospitals and laboratories

Dosage

Children: Refer to specific drug monographs for dosage information as sterile itself is not a pharmacological agent.

Adults: Refer to specific drug monographs for dosage information as sterile itself is not a pharmacological agent.

Mechanism of action

Sterility itself does not have a mechanism of action as it is a state of cleanliness and does not interact with biological systems. However, the methods used to achieve sterility, such as heat or chemical agents, act by denaturing proteins, disrupting cellular structures, or damaging nucleic acids in microorganisms, leading to their inactivation or destruction.

Pharmacodynamics

The pharmacodynamics of sterile techniques primarily involves the prevention of microbial infection and contamination when administering medications. By ensuring that products are sterile, the risk of adverse effects related to infections is minimized. The effectiveness of sterilization methods can be influenced by factors such as temperature, duration of exposure, and the type of microorganisms present.

Pharmacokinetics

As sterility does not pertain to a specific drug, pharmacokinetics is not applicable. However, the pharmacokinetics of a drug will depend on its formulation, route of administration, and the presence of preservatives or stabilizers that may be used alongside sterile preparations.

Pregnancy

Sterile preparations are generally considered safe during pregnancy as they are used to provide hydration, nutrition, or medications in a controlled manner, but specific formulations should be assessed individually.

Breast-feeding

Sterile solutions used for hydration or nutritional support are typically safe during breastfeeding, but any specific additives or medications within the solutions should be evaluated for safety.

Storage

Sterile solutions should be stored in a cool, dry place, protected from light, and should be used before the expiration date. Once opened, they may have specific storage requirements based on the formulation.

Formulations

• Sterile saline solution
• Sterile water for injection
• Sterile dextrose solution
• Sterile electrolyte solutions

Mechanism of action

The bactericidal activity of cefotaxime results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cefotaxime shows high affinity for penicillin-binding proteins in the cell wall including PBP Ib and PBP III.

Pharmacodynamics

Cefotaxime is a third generation intravenous cephalosporin antibiotic. It has broad spectrum activity against Gram positive and Gram negative bacteria. It does not have activity against <i>Pseudomonas aeruginosa</i>. Cefotaxime works by inhibiting bacterial cell wall biosynthesis. A positive feature of cefotaxime is that it display a resistance to penicillinases and is useful to treat infections that are resistant to penicillin derivatives.