FUROXICLAV 156.25 SUSPENSION

Indications

• Bacterial infections due to susceptible organisms
• Complicated urinary tract infections
• Pyelonephritis
• Cellulitis
• Erysipelas
• Prophylaxis of infection from human bites
• Acute diverticulitis
• Superficial bacterial eye infections
• Endophthalmitis prophylaxis after cataract surgery

Mechanism of action

Cefuroxime, like other beta-lactam antibiotics, binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall. This binding inhibits the third and final stage of bacterial cell wall synthesis. The resultant disruption leads to cell lysis, aided by bacterial cell wall autolytic enzymes such as autolysins. Cefuroxime may also interfere with an autolysin inhibitor, enhancing its bactericidal effect.

Pharmacodynamics

Cefuroxime is a bactericidal agent that works by inhibiting the synthesis of peptidoglycan, an essential component of the bacterial cell wall. This inhibition occurs through the blockade of the transpeptidation process, which is required for cross-linking of the cell wall structure. Cefuroxime is effective against various organisms, including aerobic Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pneumoniae, as well as Gram-negative bacteria like Escherichia coli and Haemophilus influenzae, including strains that produce beta-lactamase.

Pharmacokinetics

Cefuroxime is well-absorbed after oral administration, with its bioavailability being enhanced when taken with food. The drug exhibits a volume of distribution indicating good tissue penetration. Cefuroxime is primarily eliminated by the kidneys, with renal clearance contributing significantly to its overall elimination. Dosage adjustments may be necessary in patients with renal impairment to prevent accumulation and toxicity.

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Allergic reactions
• Thrombophlebitis at the injection site
• Renal impairment

Interactions

• Probenecid may increase cefuroxime levels
• Other nephrotoxic drugs may enhance renal toxicity
• Anticoagulants may have increased effects

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of superinfection
• May cause allergic reactions in sensitive individuals
• Caution in patients with a history of gastrointestinal disease

Pregnancy

Not known to be harmful, but should be used only if clearly needed.

Breast-feeding

Present in low concentrations in breast milk; generally considered appropriate to use.

Storage

Store in a cool, dry place away from direct light. Reconstituted solutions should be used immediately or stored at 2–8°C for a short time.

Formulations

• Intravenous injection solution
• Powder for solution for injection
• Oral suspension
• Tablets

Indications

• Community-acquired pneumonia
• Acute exacerbations of chronic bronchitis
• Sinusitis
• Urinary tract infections
• Skin and soft tissue infections
• Gonorrhea

Dosage

Children: Refer to the BNF for Children

Adults: Refer to the BNF for specific dosing guidelines based on the infection being treated and patient characteristics.

Mechanism of action

Axetil exerts its antibacterial effect by inhibiting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, disrupting the cross-linking of peptidoglycan layers which is crucial for maintaining bacterial cell wall integrity. This leads to cell lysis and death of the bacteria. The action is generally bactericidal, particularly against actively dividing bacteria.

Pharmacodynamics

Axetil demonstrates a broad spectrum of activity against various bacteria, including Streptococcus pneumoniae, Haemophilus influenzae, and Escherichia coli. The efficacy of axetil may vary based on the susceptibility of the pathogen. It is important to consider local resistance patterns when prescribing this antibiotic. The time-dependent killing characteristic of axetil suggests that maintaining adequate serum levels is critical for its effectiveness.

Pharmacokinetics

Following oral administration, axetil is rapidly absorbed and converted to its active form, cefuroxime, in the gastrointestinal tract. Peak plasma concentrations are typically reached within 2 to 3 hours after ingestion. The bioavailability of axetil is approximately 50%, which can be enhanced when taken with food. Cefuroxime is primarily excreted unchanged in the urine, with a half-life of about 1 to 2 hours. Renal function can significantly influence the clearance of the drug, necessitating dose adjustments in patients with impaired renal function.

Pregnancy

The safety of axetil during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Axetil may pass into breast milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Indications

• Bacterial infections caused by beta-lactamase producing organisms
• Community-acquired pneumonia
• Respiratory tract infections
• Urinary tract infections
• Skin and soft tissue infections

Dosage

Children: Paediatric dosing of clavulanate should be determined based on the specific indication and the formulation used. Refer to the BNF for

Adults: The usual adult dose of clavulanate varies depending on the specific antibiotic it is combined with, generally ranging from 125 mg to 250 mg, taken every 8 hours when combined with amoxicillin.

Mechanism of action

Clavulanate works by irreversibly binding to the active site of beta-lactamase enzymes. By inhibiting these enzymes, clavulanate protects beta-lactam antibiotics from degradation, allowing them to exert their antibacterial effects effectively. This mechanism enhances the spectrum of activity of the co-administered antibiotic, thereby improving clinical outcomes in infections caused by beta-lactamase producing organisms.

Pharmacodynamics

Clavulanate exhibits a time-dependent antibacterial effect, characterized by its ability to maintain effective concentrations against beta-lactamase producing bacteria. Its pharmacodynamic properties are mainly influenced by its interaction with beta-lactam antibiotics, enhancing their efficacy in treating infections. The overall effect is a synergistic relationship that increases the potency of the antibiotic treatment.

Pharmacokinetics

Clavulanate is usually administered orally or parenterally, and it is rapidly absorbed from the gastrointestinal tract. It reaches peak plasma concentrations within 1 to 2 hours after administration. The drug is widely distributed in body tissues, with a volume of distribution indicative of good tissue penetration. Clavulanate undergoes hepatic metabolism, primarily by conjugation, and is excreted largely in the urine as metabolites. The elimination half-life is approximately 1 hour, necessitating frequent dosing for optimal therapeutic effect.

Contra-indications

• Hypersensitivity to clavulanate or any component of the formulation
• History of jaundice or hepatic impairment related to previous use of beta-lactam antibiotics

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Hepatic dysfunction
• Allergic reactions

Interactions

• Probenecid may increase concentrations of clavulanate
• Anticoagulants may have altered effects due to changes in gut flora

Precautions

• Monitor liver function during prolonged therapy
• Use cautiously in patients with renal impairment
• Assess for history of allergy to penicillins or cephalosporins

Pregnancy

Clavulanate is classified as category B. Animal studies have not shown teratogenic effects, but adequate and well-controlled studies in pregnant women are lacking.

Breast-feeding

Clavulanate is excreted in breast milk. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from direct light. Keep out of reach of children.

Formulations

• Clavulanate potassium 125 mg/5 mL
• Clavulanate potassium 250 mg/5 mL

Indications

• Infections caused by beta-lactamase-producing bacteria
• Acute bacterial sinusitis
• Acute otitis media
• Lower respiratory tract infections
• Urinary tract infections

Dosage

Children: Refer to the BNF for Children for specific dosing according to age and weight; adjustments may be necessary based on the clinical scenario.

Adults: Refer to specific product guidelines for dosing; typical regimens depend on the combination antibiotic used and the severity of the infection.

Mechanism of action

Clavulanic acid works by irreversibly binding to the active site of beta-lactamase enzymes that are produced by certain bacteria to inactivate beta-lactam antibiotics. By inhibiting these enzymes, clavulanic acid protects the penicillin antibiotic from degradation, allowing it to exert its antibacterial effects.

Pharmacodynamics

Clavulanic acid has a synergistic effect when combined with other antibiotics, particularly amoxicillin. The presence of clavulanic acid allows for the effective treatment of infections caused by bacteria that would otherwise be resistant to penicillins. Its antibacterial activity is generally weak on its own but significantly enhances the efficacy of other beta-lactam antibiotics.

Pharmacokinetics

Clavulanic acid is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 hour. It is widely distributed throughout the body and has a half-life of approximately 1 hour. The drug is primarily excreted unchanged in the urine. In the presence of renal impairment, dosage adjustment may be necessary, as the elimination of clavulanic acid can be affected.

Contra-indications

• Hypersensitivity to clavulanic acid or any of the excipients
• History of jaundice or hepatic impairment associated with previous use of penicillins or beta-lactam antibiotics

Adverse effects

• Nausea
• Diarrhea
• Rash
• Elevated liver enzymes
• Allergic reactions including anaphylaxis
• Superinfection

Interactions

• May enhance the effects of anticoagulants such as warfarin
• Probenecid may increase plasma concentrations of clavulanic acid
• May reduce the efficacy of oral contraceptives

Precautions

• Caution in patients with renal impairment
• Monitor liver function in patients receiving prolonged therapy
• Use with caution in patients with a history of allergic reactions to beta-lactams

Pregnancy

Clavulanic acid is categorized as pregnancy category B. Animal studies have not shown any harm to the fetus, but there are no adequate and well-controlled studies in pregnant women.

Breast-feeding

Clavulanic acid is excreted in breast milk, but it is generally considered safe for use during breastfeeding. Monitor for potential effects in the infant.

Storage

Store at room temperature, away from moisture and heat. Protect from light. Keep out of reach of children.

Formulations

• Oral tablets
• Oral suspension
• Injectable forms

Mechanism of action

Cefuroxime, like the penicillins, is a beta-lactam antibiotic. 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; it is possible that cefuroxime interferes with an autolysin inhibitor.

Pharmacodynamics

Cefuroxime is a &beta;-lactam type antibiotic. More specifically, it is a second-generation cephalosporin. Cephalosporins work the same way as penicillins: they interfere with the peptidoglycan synthesis of the bacterial wall by inhibiting the final transpeptidation needed for the cross-links. This effect is bactericidal. Cefuroxime is effective against the following organisms: Aerobic Gram-positive Microorganisms: <i>Staphylococcus aureus</i>, <i>Streptococcus pneumoniae</i>, <i>Streptococcus pyogenes</i>. Aerobic Gram-negative Microorganisms: <i>Escherichia coli</i>, <i>Haemophilus influenzae</i> (including beta-lactamase-producing strains), <i>Haemophilus parainfluenzae</i>, <i>Klebsiella pneumoniae</i>, <i>Moraxella catarrhalis</i> (including beta-lactamase-producing strains), <i>Neisseria gonorrhoeae</i> (including beta-lactamase-producing strains). Spirochetes: <i>Borrelia burgdorferi</i>. Cefuroxime axetil is the prodrug