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Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
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Intermittent intravenous (IV) infusion is a method of drug administration where medications are delivered over short infusion periods followed by intervals of no drug delivery. This approach helps to prevent sustained high drug concentrations in the bloodstream, reducing the risk of adverse effects associated with prolonged exposure. Unlike continuous infusion, steady-state concentrations may not be achieved during a single dosing cycle but can be reached through repeated...
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Gentamicin, an aminoglycoside antibiotic, is commonly administered via intermittent intravenous infusion to treat severe infections. An intermittent one-hour infusion of gentamicin, administered at eight-hour intervals, allows for precise control of plasma drug concentrations, minimizing toxicity while ensuring therapeutic efficacy. Pharmacokinetic principles govern the dynamics of plasma concentrations and can be mathematically described using specific equations.The plasma drug concentration...
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Trans-Tympanic Drug Delivery for the Treatment of Ototoxicity
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Betahistine exacerbates amikacin ototoxicity.

Fadlullah Aksoy1, Remzi Dogan2, Orhan Ozturan1

  • 1Bezmialem Vakif University, Department of Otorhinolaryngology, Fatih, Istanbul, Turkey.

The Annals of Otology, Rhinology, and Laryngology
|November 1, 2014
PubMed
Summary

Betahistine may worsen amikacin-induced ototoxicity. Concurrent use of betahistine with amikacin led to greater hearing loss in rats, indicated by decreased distortion-product otoacoustic emissions and increased auditory brainstem response thresholds.

Keywords:
ABRDPOAEamikacinbetahistineototoxicity

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Area of Science:

  • Ototoxicity research
  • Pharmacology
  • Auditory neuroscience

Background:

  • Amikacin is an antibiotic with a broad spectrum of use, but its ototoxic side effects are a significant clinical concern.
  • Betahistine is known to enhance cochlear blood flow and is used therapeutically.
  • The potential interaction between betahistine and amikacin regarding ototoxicity has not been fully elucidated.

Purpose of the Study:

  • To investigate the effect of betahistine on amikacin-induced ototoxicity in a rat model.
  • To determine if betahistine mitigates or exacerbates the hearing damage caused by amikacin.

Main Methods:

  • Thirty-two rats were divided into four groups: amikacin, amikacin + betahistine, betahistine, and no treatment.
  • Amikacin was administered intramuscularly for 14 days, while betahistine was given orally for 21 days.
  • Auditory function was assessed using distortion-product otoacoustic emissions (DPOAE) and auditory brainstem response (ABR) tests.

Main Results:

  • Both amikacin and amikacin + betahistine groups showed significant decreases in DPOAE levels and increases in ABR thresholds compared to baseline.
  • The amikacin + betahistine group exhibited significantly greater decreases in DPOAE and increases in ABR thresholds on days 7, 14, and 21 compared to the amikacin-only group.
  • Betahistine alone did not show significant changes in auditory function tests.

Conclusions:

  • The concurrent administration of betahistine appears to augment the ototoxic effects of amikacin.
  • Further experimental and clinical studies, including histopathological analysis, are warranted to confirm these findings.
  • This suggests caution when using betahistine in patients treated with amikacin.