BETAKELFIN

Indications

• Urinary tract infections
• Respiratory tract infections
• Gastrointestinal infections
• Skin infections
• Certain types of pneumonia

Dosage

Children: Refer to clinical guidelines or specific product information for paediatric dosing.

Adults: Refer to clinical guidelines or specific product information for adult dosing.

Mechanism of action

Sulphamethoxypyridazime works by competitively inhibiting the enzyme dihydropteroate synthase, which is involved in the bacterial folate synthesis pathway. This inhibition prevents the formation of dihydropteroic acid from para-aminobenzoic acid (PABA) and pteridine, ultimately leading to a decrease in folate production, which is necessary for DNA and RNA synthesis in bacteria.

Pharmacodynamics

The pharmacodynamics of sulphamethoxypyridazime involves its role as a bacteriostatic agent. By inhibiting folate synthesis, it slows down bacterial growth and replication. The drug demonstrates time-dependent antimicrobial activity, meaning that its effectiveness is related to the duration of time that the drug concentration remains above the minimum inhibitory concentration (MIC) for the target bacteria.

Pharmacokinetics

Sulphamethoxypyridazime is absorbed well from the gastrointestinal tract, achieving peak plasma concentrations within a few hours after administration. It is widely distributed throughout the body tissues and fluids. The drug undergoes hepatic metabolism and is primarily excreted in the urine, both unchanged and as metabolites. The half-life of the drug varies but is generally around 10 to 12 hours in healthy adults.

Contra-indications

• Hypersensitivity to sulfonamides or any component of the formulation
• Severe hepatic or renal impairment
• Pregnancy (particularly near term)

Adverse effects

• Nausea
• Vomiting
• Rash
• Allergic reactions
• Hematological disorders (such as agranulocytosis, thrombocytopenia)
• Liver toxicity
• Kidney damage (nephrotoxicity)

Interactions

• May potentiate the effects of anticoagulants (e.g., warfarin)
• May interact with methotrexate leading to increased toxicity
• Potential interactions with oral hypoglycemics
• May enhance the effects of other sulfonamides

Precautions

• Use with caution in patients with glucose-6-phosphate dehydrogenase deficiency
• Monitor renal function during therapy
• Assess for sensitivity to sulfonamides
• Use with caution in patients with asthma or other respiratory conditions

Pregnancy

Use during pregnancy is not recommended due to potential harm to the fetus. Risk of kernicterus in newborns.

Breast-feeding

Use with caution during breastfeeding. Sulfamethoxypyridazime is excreted in breast milk and may cause adverse effects in nursing infants.

Storage

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

Formulations

• Tablets
• Oral suspension