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Pharmacology of amikacin in humans
Abstract:
Amikacin is a new aminoglycoside antibiotic which is active in vitro against most isolates of gram-negative bacilli. A dose of 300 mg/m(2) intramuscularly produced a highest mean serum concentration of 25.4 mug/ml with a mean serum concentration of 3.1 mug/ml at 8 h. The same dose intravenously produced a highest mean serum concentration of 52.4 mug/ml with a mean serum concentration of 2.1 mug/ml at 8 h. The mean urinary excretion during the first 6 h was 75 and 66%, respectively. When amikacin was administered at a dose of 150 mg/m(2) every 6 h, there was evidence of some drug accumulation. A loading dose of 150 mg/m(2) administered intravenously over 30 min followed by 200 mg/m(2) administered as a continuous infusion every 6 h maintained serum concentrations of 8 mug/ml. No major toxicity was observed with any of these drug regimens.
Insights
Amikacin, a novel aminoglycoside antibiotic, demonstrates broad-spectrum activity against gram-negative bacilli. Pharmacokinetic studies show favorable serum concentrations and minimal toxicity across various dosing regimens.
Area of Science:
- Pharmacology
- Microbiology
- Clinical Therapeutics
Background:
- Amikacin is a new aminoglycoside antibiotic.
- It exhibits in vitro activity against most gram-negative bacilli isolates.
Purpose of the Study:
- To evaluate the pharmacokinetics and safety of amikacin in humans.
- To determine optimal dosing strategies for amikacin therapy.
Main Methods:
- Administered amikacin at doses of 300 mg/m(2) intramuscularly and intravenously.
- Evaluated serum concentrations and urinary excretion over time.
- Investigated alternative dosing regimens including loading and continuous infusion.
- Monitored for adverse events.
Main Results:
- Intramuscular and intravenous administration of 300 mg/m(2) yielded peak serum concentrations of 25.4 and 52.4 mug/ml, respectively.
- Mean serum concentrations at 8 hours were 3.1 mug/ml (IM) and 2.1 mug/ml (IV).
- Urinary excretion was high (75% IM, 66% IV in 6 hours).
- A regimen of 150 mg/m(2) every 6 hours showed potential for accumulation.
- A loading dose followed by continuous infusion maintained serum concentrations of 8 mug/ml.
- No major toxicity was observed.
Conclusions:
- Amikacin exhibits favorable pharmacokinetic properties and a good safety profile.
- Different dosing strategies can achieve therapeutic serum concentrations.
- Amikacin is a promising antibiotic for treating gram-negative bacterial infections.