ESB3

Indications

• Bacterial infections
• Urinary tract infections
• Respiratory tract infections
• Gastrointestinal infections

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines.

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Sulfaclozine exerts its antibacterial effect by competitively inhibiting the enzyme dihydropteroate synthase, which is involved in the synthesis of folate in bacteria. By blocking this enzyme, sulfaclozine prevents the formation of dihydropteroic acid, a precursor in the folate synthesis pathway, ultimately leading to impaired nucleic acid synthesis and bacterial cell growth.

Pharmacodynamics

Sulfaclozine shows bacteriostatic activity against a range of gram-positive and gram-negative bacteria. Its effectiveness is influenced by factors such as bacterial resistance mechanisms, and its action is most effective during the logarithmic phase of bacterial growth. The drug's efficacy is also dependent on the concentration achieved at the site of infection.

Pharmacokinetics

Sulfaclozine is absorbed from the gastrointestinal tract, with peak plasma concentrations achieved within a few hours of oral administration. It is widely distributed throughout the body and is metabolized in the liver, with metabolites being excreted primarily in the urine. The elimination half-life of sulfaclozine varies, but it is typically several hours, allowing for once or twice daily dosing in most regimens.

Contra-indications

• Hypersensitivity to sulfaclozine or any of its components
• Severe liver or kidney impairment
• Porphyria

Adverse effects

• Rash
• Nausea
• Vomiting
• Diarrhea
• Headache
• Dizziness
• Hypersensitivity reactions
• Hematological disorders such as agranulocytosis or thrombocytopenia

Interactions

• May enhance the effects of anticoagulants such as warfarin
• May interact with methotrexate, leading to increased toxicity
• May reduce the efficacy of certain antiepileptic drugs

Precautions

• Use with caution in patients with impaired renal function
• Monitor for signs of hematological reactions
• Caution in patients with a history of hypersensitivity to sulfonamides

Pregnancy

Sulfaclozine should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. Its safety in pregnancy has not been established.

Breast-feeding

Caution is advised when sulfaclozine is administered to a nursing woman. It is not known if the drug is excreted in breast milk.

Storage

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

Formulations

• Tablets
• Oral suspension