AMIKACIN SULFATE IN SODIUM CHLORIDE 0.9% IN PLASTIC CONTAINER
Clinical safety rating
safeNo significant drug interactions Can cause hypernatremia and fluid overload.
Aminoglycoside antibiotic that irreversibly binds to the 30S ribosomal subunit, causing misreading of mRNA and inhibiting bacterial protein synthesis.
| Metabolism | Amikacin is minimally metabolized; primarily eliminated unchanged by glomerular filtration. |
| Excretion | Amikacin is eliminated primarily by glomerular filtration. Approximately 94-98% of an administered dose is excreted unchanged in the urine within 24 hours in patients with normal renal function. Less than 1% is excreted in bile or feces. |
| Half-life | The terminal elimination half-life is approximately 2-3 hours in adults with normal renal function. In neonates, it may be prolonged to 4-8 hours. In patients with impaired renal function, half-life can extend to 30-80 hours or more, necessitating dose adjustment based on creatinine clearance. |
| Protein binding | Amikacin has low protein binding, ranging from 0-11%. It binds primarily to albumin, but due to low binding, protein binding alterations do not significantly impact pharmacokinetics. |
| Volume of Distribution | The volume of distribution is approximately 0.25-0.4 L/kg in adults. It reflects distribution primarily into extracellular fluid. The Vd is increased in conditions such as edema, ascites, and sepsis, and is decreased in dehydration. In neonates, the Vd is larger (0.5-0.6 L/kg) due to higher extracellular fluid volume. |
| Bioavailability | Intramuscular: Nearly complete, with bioavailability >90%. Oral: Not bioavailable due to negligible gastrointestinal absorption (<1%). Intravenous: 100%. |
| Onset of Action | Intravenous infusion: Rapid, with peak serum concentrations achieved at the end of infusion. Intramuscular injection: Peak concentrations occur within 30-90 minutes. Clinical effect onset is typically within 1-2 hours for susceptible organisms. |
| Duration of Action | Duration of action is approximately 8-12 hours in patients with normal renal function when administered every 8-12 hours. The duration is prolonged in renal impairment, and trough levels should be monitored to avoid accumulation. |
| Molecular Weight | 585.6 |
15 mg/kg/day IV divided every 8-12 hours or 15-20 mg/kg IV once daily; typical adult dose: 500-1000 mg IV every 8-12 hours.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-60 mL/min: administer every 12-24 hours; CrCl 15-29 mL/min: administer every 24-48 hours; CrCl <15 mL/min: administer every 48-72 hours. Use therapeutic drug monitoring. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Neonates: 15-20 mg/kg IV every 24 hours; Infants and children: 15-20 mg/kg IV every 8-24 hours depending on age and renal function. Not to exceed 1.5 g/day. |
| Geriatric use | Reduce initial dose based on renal function; monitor serum creatinine and drug levels; typical starting dose: 7.5 mg/kg IV every 24 hours adjusted for CrCl. |
| 1st trimester | Amikacin crosses the placenta. Use only if clearly needed due to potential ototoxicity and nephrotoxicity. Avoid in first trimester unless no alternative. |
| 2nd trimester | Use with caution. Monitor maternal and fetal renal function. Association with fetal ototoxicity and nephrotoxicity if maternal plasma levels are high. |
| 3rd trimester | Use with caution. Risk of fetal ototoxicity and nephrotoxicity. Prolonged use may cause toxicity to the fetal eighth cranial nerve. |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Placental transfer | Amikacin crosses the placenta, achieving fetal serum levels approximately 30-50% of maternal levels. Reported amniotic fluid concentrations range from 16-100% of maternal levels. |
| Breastfeeding | Amikacin is excreted into breast milk in low concentrations. The amount is unlikely to cause adverse effects in nursing infants, but monitor infant for diarrhea, rash, or changes in bowel flora. The American Academy of Pediatrics considers amikacin compatible with breastfeeding. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Amikacin is an aminoglycoside antibiotic. There are no adequate and well-controlled studies in pregnant women. Aminoglycosides can cause fetal harm when administered to a pregnant woman. There is a potential for fetal ototoxicity and nephrotoxicity. First trimester: Risks unknown but avoid if possible. Second/Third trimester: Use only if clearly needed and if benefit outweighs risk; associated with irreversible bilateral congenital deafness when administered during pregnancy. |
| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN) and hearing (audiometry) before and during therapy. Monitor fetal heart rate and consider fetal growth ultrasound if prolonged use. Assess for signs of maternal ototoxicity and nephrotoxicity. In neonates exposed in utero, monitor auditory function and renal function. |
| Fertility Effects | No specific studies on fertility effects in humans. Animal studies: no evidence of impaired fertility at clinically relevant doses. However, aminoglycosides can cause testicular damage in animal models at high doses; relevance unknown. Reproductive toxicity is not well characterized. |
■ FDA Black Box Warning
Aminoglycosides, including amikacin, are associated with nephrotoxicity and ototoxicity (both auditory and vestibular), which can occur even at therapeutic doses. Risk is increased with prolonged use, higher doses, renal impairment, and concurrent use of other nephrotoxic or ototoxic drugs. Monitoring of renal function and serum drug levels is essential.
| Common Effects | fluid replacement |
| Serious Effects |
Hypersensitivity to amikacin or any aminoglycosideMyasthenia gravis (aminoglycosides can exacerbate neuromuscular blockade)Concurrent use of other nephrotoxic or ototoxic drugs (e.g., other aminoglycosides, vancomycin, loop diuretics) unless carefully monitored
| Precautions | Neurotoxicity (including ototoxicity and nephrotoxicity) may occur. Risk of neuromuscular blockade, especially in patients with neuromuscular disorders or receiving anesthetics. Monitor renal function, audiometric tests, and serum drug concentrations. Use with caution in elderly, dehydrated, or renally impaired patients. Avoid concomitant use of other nephrotoxic or ototoxic agents. |
| Food/Dietary | No significant food interactions. Maintain adequate hydration unless contraindicated. No specific dietary restrictions. |
| Clinical Pearls | Avoid concomitant use with other nephrotoxic or ototoxic drugs (e.g., loop diuretics, vancomycin). Monitor peak (25-35 mcg/mL) and trough (<8 mcg/mL) serum levels to guide dosing and reduce toxicity risk. Extended-interval (once-daily) dosing is preferred in many patients; adjust for renal function using ideal body weight. In obese patients, dose based on adjusted body weight. Rapid infusion can cause neuromuscular blockade; use with caution in myasthenia gravis or concurrent neuromuscular blocking agents. |
| Patient Advice | This medication is given intravenously and will be monitored closely by your healthcare team. · Report any new hearing loss, ringing in the ears, dizziness, or difficulty urinating immediately. · Do not skip or double doses; adhere to the prescribed schedule. · Inform your doctor if you are pregnant, breastfeeding, or have kidney disease. |
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