AMIKIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AMIKIN (AMIKIN).
Aminoglycoside antibiotic that binds to the 30S ribosomal subunit, causing misreading of mRNA and inhibition of protein synthesis.
| Metabolism | Amikacin is not metabolized; it is excreted unchanged primarily by glomerular filtration. |
| Excretion | Renal: >90% unchanged in urine via glomerular filtration; biliary/fecal: <1%. |
| Half-life | 2-3 hours in adults with normal renal function; prolonged to 30-90 hours in ESRD. |
| Protein binding | 0-10% (low binding to albumin). |
| Volume of Distribution | 0.25 L/kg in adults; higher in neonates and edema states (0.3-0.4 L/kg), indicating distribution into extracellular fluid. |
| Bioavailability | IM: 100% (complete absorption); oral: <1% (not absorbed). |
| Onset of Action | IM: 30-60 minutes; IV: immediate upon completion of infusion. |
| Duration of Action | Approximately 8-12 hours; prolonged in renal impairment. |
| Action Class | Aminoglycosides |
| Brand Substitutes | Amilab 500mg Injection, Acil 500mg Injection, Emica 500mg Injection, Mika Best 500mg Injection, Ivimicin 500mg Injection |
15 mg/kg/day IV or IM divided every 8 to 12 hours; usual adult dose: 15 mg/kg/day
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-59 mL/min: extend dosing interval to every 12-24 hours; GFR 15-29 mL/min: extend to every 24-48 hours; GFR <15 mL/min: extend to every 48-72 hours or consider peritonitis dosing; adjust based on serum levels |
| Liver impairment | No specific Child-Pugh based adjustments required; amikacin is minimally hepatically metabolized; monitor renal function as primary clearance route |
| Pediatric use | Neonates: 15-20 mg/kg/day IV/IM every 12-24 hours depending on gestational age; Infants and children: 15-22.5 mg/kg/day divided every 8-12 hours; maximum 1.5 g/day |
| Geriatric use | Start with lower initial doses based on renal function; monitor renal function and serum amikacin levels closely; usual initial dose reduction to 7.5 mg/kg every 12-24 hours based on estimated GFR |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AMIKIN (AMIKIN).
| Breastfeeding | Amikacin is excreted into human breast milk in low concentrations. The milk-to-plasma (M/P) ratio is approximately 0.1-0.2. After intramuscular administration of 500 mg, peak milk concentrations are about 1-2 mcg/mL. Because of low oral bioavailability (poorly absorbed from the GI tract), systemic effects in the nursing infant are unlikely. However, theoretical risk of alteration of infant gut flora and direct exposure. Use with caution, especially in premature infants or those with renal impairment. The American Academy of Pediatrics considers amikacin compatible with breastfeeding. |
| Teratogenic Risk | Amikacin is an aminoglycoside antibiotic. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown evidence of fetal harm (e.g., nephrotoxicity, ototoxicity) at doses similar to or lower than human doses. Amikacin crosses the placenta. First trimester: Risk cannot be excluded; use only if clearly needed. Second and third trimesters: Potential for fetal nephrotoxicity and ototoxicity; avoid use unless necessary for serious infections. Risk category D (positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience). |
■ FDA Black Box Warning
Amikacin can cause nephrotoxicity and ototoxicity. The risk of nephrotoxicity is greater in patients with impaired renal function and those receiving high doses or prolonged therapy. Ototoxicity (both vestibular and auditory) can occur in patients with pre-existing renal damage and in those with normal renal function treated with higher doses or for longer periods than recommended.
| Serious Effects |
Hypersensitivity to amikacin or any aminoglycoside; history of ototoxicity with prior aminoglycoside use.
| Precautions | Neurotoxicity (ototoxicity) and nephrotoxicity; neuromuscular blockade; respiratory paralysis; cross-allergenicity among aminoglycosides; monitoring of renal function and drug levels recommended. |
| Food/Dietary | No significant food interactions. Maintain adequate hydration. Avoid alcohol as it may worsen side effects. |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN, creatinine clearance) before and during therapy. Audiometric testing (baseline and periodic) in mother if prolonged therapy. Monitor serum amikacin peak and trough levels to avoid toxicity (therapeutic peak: 20-30 mcg/mL for serious infections; trough <5-10 mcg/mL). In neonates exposed in utero, monitor for signs of ototoxicity (hearing loss, balance issues) and nephrotoxicity (urine output, renal function tests). |
| Fertility Effects | No specific studies on human fertility. Animal studies have not shown impairment of fertility. Aminoglycosides, in general, are not associated with significant effects on fertility. |
| Clinical Pearls | Monitor peak (20-30 mcg/mL) and trough (1-8 mcg/mL) serum levels; adjust dose based on renal function. Avoid concurrent use with other ototoxic/nephrotoxic drugs. Use extended-interval dosing (e.g., 15-20 mg/kg IV once daily) when possible. Assess for vestibular toxicity (ataxia, vertigo) and cochlear toxicity (tinnitus, high-frequency hearing loss). |
| Patient Advice | Report any hearing loss, ringing in ears, dizziness, or unsteadiness immediately. · Drink plenty of fluids to help prevent kidney damage. · Avoid taking other aminoglycosides or strong diuretics unless prescribed. · Inform your doctor if you have kidney disease, myasthenia gravis, or are pregnant. |