Quick Facts
| CAS Number | 39831-55-5 |
|---|---|
| Molecular Formula | C22H47N5O21S2 |
| Molecular Weight | 781.759 |
| Pharmacopoeia | USP, EP, CPV |
| Packaging | 25 KG/DRUM |
Product Overview
Amikacin was developed in 1972 by Kawaguchi and colleagues at Bristol-Banyu Research Institute (Japan) through the semisynthetic modification of kanamycin A. The discovery was driven by the growing clinical problem of aminoglycoside resistance: by the late 1960s, bacterial enzymes that acetylate, phosphorylate, or adenylylate aminoglycoside molecules were spreading among Gram-negative pathogens, rendering gentamicin and kanamycin ineffective against many hospital-acquired infections. The key innovation was acylating the 1-amino group of the 2-deoxystreptamine ring with L-(-)-gamma-amino-alpha-hydroxybutyric acid (L-HABA), creating a steric shield that blocks enzymatic attack at 14 of the 16 known aminoglycoside modification sites.
This structural modification gives amikacin the broadest resistance coverage among all aminoglycosides. While gentamicin and tobramycin are inactivated by a wide range of aminoglycoside-modifying enzymes (AMEs), only a handful of AAC(6')-type acetyltransferases can modify amikacin. This makes amikacin the aminoglycoside of last resort — reserved for serious, multidrug-resistant Gram-negative infections where other antibiotics have failed. Its indications include MDR Pseudomonas aeruginosa, Acinetobacter baumannii, extended-spectrum beta-lactamase (ESBL)-producing Enterobacteriaceae, and mycobacterial infections including Mycobacterium avium complex (MAC).
In veterinary medicine, amikacin sulphate is used for severe Gram-negative infections in livestock and companion animals, particularly ampicillin-resistant and gentamicin-resistant strains. It is administered parenterally (intramuscular or intravenous) due to negligible oral absorption. The compound requires therapeutic drug monitoring in both human and veterinary patients because of its narrow therapeutic window: trough concentrations above 10 mg/L are associated with nephrotoxicity, while peak concentrations below 20-25 mg/L risk treatment failure.
Global amikacin demand is sustained by rising rates of MDR Gram-negative infections and the shortage of new antibiotic classes. The API market is supplied primarily by manufacturers in China and India, with production concentrated in facilities holding both human-grade (USP/EP) and veterinary-grade (CPV) certifications. As antimicrobial resistance surveillance data continues to show amikacin retaining activity against a high proportion of MDR isolates, it remains an essential reserve antibiotic in both human and veterinary medicine.
Quality Specifications
| Potency (USP, anhydrous) | 674 - 786 µg/mg |
|---|---|
| Kanamycin Content | ≤ 5.0% (critical starting-material impurity) |
| Water Content (KF) | 4.0% - 8.0% |
| pH (1 in 10 solution) | 3.5 - 5.5 |
| Specific Optical Rotation | +76° to +84° |
| Bacterial Endotoxins (injectable) | ≤ 0.33 EU/mg |
| Heavy Metals | ≤ 20 ppm |
| Residual Solvents | Compliant with ICH Q3C |
| GMP Status | Manufactured under ICH Q7 GMP conditions |
Applications
- Serious Gram-negative infections in livestock: Injectable aminoglycoside for pneumonia, septicemia, and enteric infections resistant to first-line antibiotics including gentamicin.
- Respiratory infections in poultry: Administered parenterally for E. coli, Pasteurella, and Mycoplasma respiratory complex when oral antibiotics are inadequate.
- Human hospital-acquired infections: Reserved for MDR Gram-negative infections including ESBL-producing Enterobacteriaceae, P. aeruginosa, and Acinetobacter spp.
- Mycobacterial infections: Component of multi-drug regimens for MAC and M. abscessus infections, particularly in immunocompromised patients.
- Urinary tract infections: Effective against complicated UTIs caused by susceptible MDR Enterobacteriaceae when oral options have failed.
Sourcing Amikacin Sulphate: Key Checks
Documentation
Request CoA with potency assay (micrograms/mg), kanamycin content, and endotoxin data for injectable grade. Verify specific optical rotation and pH. For regulated markets, confirm DMF or CEP filing status.
Red Flags
Kanamycin content above 5% indicates incomplete acylation. Wide pH variation from 3.5-5.5 suggests inconsistent salt formation. Endotoxin levels above specification limit for injectable-grade API.
Packaging & Logistics
Standard: 25 KG/DRUM. Amikacin is hygroscopic — packaging must be airtight with desiccant. Store at controlled room temperature (15-25 degrees Celsius). Sterile API for injection requires validated aseptic processing documentation.
Market Context
Sustained demand driven by rising MDR Gram-negative infections globally. Amikacin retains activity against >85% of ESBL-producing Enterobacteriaceae where gentamicin resistance exceeds 30-50%. China and India dominate API production. Essential in both human reserve antibiotic and veterinary critical care settings.