- Amikacin is a semisynthetic aminoglycoside antibiotic derived from kanamycin A, with a molecular formula of C22H43N5O13 and a molecular mass of 585.603 g/mol.
- Its structure features a central 2-deoxystreptamine ring with amino sugars attached at positions 4 and 6, and a unique L-hydroxyaminobuteroyl amide group that provides enhanced stability against aminoglycoside-modifying enzymes.
- The antibiotic functions by binding to the 30S ribosomal subunit of susceptible bacteria, specifically interacting with the 16S rRNA component. This interaction leads to misreading of the genetic code and inhibition of protein synthesis, resulting in bactericidal activity.
- The compound demonstrates concentration-dependent killing, with post-antibiotic effects that persist even after serum levels fall below the minimum inhibitory concentration.
- Amikacin exhibits potent activity against many aerobic gram-negative bacteria, including Pseudomonas aeruginosa, Acinetobacter species, and various Enterobacteriaceae.
- Its resistance to many bacterial aminoglycoside-modifying enzymes makes it particularly valuable against multidrug-resistant organisms.
- Pharmacokinetically, it demonstrates poor oral absorption, necessitating parenteral administration, undergoes minimal metabolism, and is primarily eliminated unchanged through glomerular filtration.
- The antibiotic’s distribution is primarily in extracellular fluid, with a half-life of approximately 2-3 hours in patients with normal renal function, requiring careful monitoring of serum levels and renal function during therapy.
