DR BACTERIA 10000MG/100G SOLUBLE POWDER

Indications

• Bacterial infections caused by susceptible Gram-negative organisms
• Infections in veterinary medicine, particularly in livestock

Dosage

Children: Refer to BNF for Children for specific dosing information.

Adults: Refer to specific BNF guidelines for dosing information.

Mechanism of action

Apramycin exerts its antibacterial effect by binding to the bacterial ribosomal RNA, specifically blocking translocation during protein synthesis. It also binds to the eukaryotic decoding site, despite differences in key residues, which allows it to interact with human ribosomes, albeit with a distinct binding mode compared to bacterial targets. This unique binding leads to interference in the translation of proteins, contributing to its antimicrobial activity.

Pharmacodynamics

The pharmacodynamics of apramycin involve its bactericidal activity against susceptible strains of bacteria. It is effective at low concentrations and exhibits a concentration-dependent killing effect. The drug's ability to bind to both bacterial and eukaryotic ribosomes provides a dual mechanism of action, although its clinical relevance in humans needs further evaluation.

Pharmacokinetics

The pharmacokinetics of apramycin involve limited absorption from the gastrointestinal tract when administered orally, leading to its use primarily as a parenteral agent. It is distributed in body fluids and tissues, but its penetration into the central nervous system is minimal. The drug is primarily excreted unchanged via the kidneys, necessitating dose adjustments in patients with renal impairment.

Pregnancy

Apramycin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, as safety in pregnancy has not been established.

Breast-feeding

It is not known whether apramycin is excreted in human milk. Caution should be exercised when administering to breastfeeding women.

Storage

Store below 25 degrees Celsius. Protect from light and moisture.

Mechanism of action

Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria.