Drug Detail

Amikacin

Last Updated June 10, 2016

Trade Names

Amikacin Fresenius, Kacinth-A Injection

Drug Classification

Semisynthetic aminoglycoside bacteriocidal antibiotic, kanamycin derivative

Formulations

100 mg/2 mL, 250 mg/2 mL, 500 mg/2 mL, 1 g/4 mL solutions for injection

Indications and Pharmacology

Indication: for treatment of infections caused by Gram-negative bacilli; particularly used in nosocomial infections.

Also used for treatment of tuberculosis in combination with other antituberculosis drugs, including multidrug-resistant tuberculosis.

Mechanism of action: inhibition of protein synthesis through binding 30S ribosomal unit, causing cell death.

Pharmacokinetics: rapidly absorbed and widely distributed throughout body; half-life 2-3 hours (prolonged with renal impairment).

Dosage

Adult Dose: 15 mg/kg/day, maximum 1.5 g/day.

Use in Renal or Hepatic Insufficiency: 

  • Renal impairment: glomerular filtration rate  < 60 mL/min, 10 mg/kg loading dose then guided by drug levels (target plasma levels for once-daily dosing: peak > 30 mg/L, trough < 1 mg/L).
  • No adjustments needed for hepatic impairment.

Use in Pregnancy and Breastfeeding: Pregnancy Category D. Can cross placenta, potential for foetal ototoxicity. Unknown whether excreted in breast milk.

Use in Children: 

  • Neonates: 15 mg/kg/day; measure trough levels before third dose and if > 5 mg/L, increase dose interval to 36-48 hours and measure after 2 further doses.
  • Infants and children 1 week to < 10 years: 25 mg/kg initial dose on first day, then 18 mg/kg/day, maximum 360 mg/day.
  • Children > 10 years: 20 mg/kg initial dose, then 15 mg/kg/day, maximum 360 mg/day

Warnings

Contraindicated in patients with hypersensitivity to amikacin, kanamycin, or other aminoglycosides, and patients with myasthenia gravis.

Not indicated for long-term therapy due to toxicity.

Can cause vestibular toxicity (heralded by headache, nausea, vomiting, disequilibrium) and cochlear toxicity (heralded by loss of high-frequency hearing); patients should be monitored to avoid irreversible damage.

Increased risk of severe neurotoxic reactions, including ototoxicity, optic nerve dysfunction, and peripheral neuritis, in patients with renal impairment.

May cause nephrotoxicity; risk higher in patients with renal impairment.

Renal and eighth nerve function should be monitored frequently during administration.

Use with caution in patients with Parkinsonism.

Respiratory paralysis due to neuromuscular blockade may occur, especially when used soon after anaesthesia or muscle relaxants.

Should not be given with concomitant diuretics due to increased toxicity.

Drug–Drug Interactions

Concomitant use of aminoglycosides and beta-lactam–type antibiotic may cause mutual inactivation.

Ototoxicity potentiated by concomitant administration of ethacrynic acid, furosemide, mannitol, and possibly other diuretics.

Avoid concurrent or sequential use of other neurotoxic and/or nephrotoxic drugs, including neomycin, kanamycin, gentamicin, cephaloridine, paromomycin, viomycin, polymyxin B, colistin, tobramycin, and cyclosporine.

Considerations for Special Populations

Renal impairment: increased risks of ototoxicity, nephrotoxicity, and neuromuscular blockade.

Geriatric: may require reduced dose due to renal impairment.

Infants: use with caution in premature and neonatal infants due to renal immaturity.

See above for pregnancy and lactation.

Adverse Effects

Ototoxicity (auditory and sometimes vestibular), nephrotoxicity, neuromuscular blockade, rash, drug fever, headache, paresthesia, tremor, nausea, vomiting, eosinophilia, arthralgia, anaemia, hypotension.