Chapter 29 : Central Nervous System Toxicity

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Central nervous system (CNS) reactions have been well known to occur sporadically with all nonfluorinated and fluorinated quinolone antibacterial agents. Studies using positron emission tomography have shown that fleroxacin is rapidly and equally distributed to the various parts of the brain and that lomefloxacin or ciprofloxacin do not affect cerebral blood flow or oxygen or glucose metabolism. Impaired excretory organ function, resulting in slower elimination of quinolones, may result in increased risks of accumulation of the drugs and subsequent CNS toxicity. Quinolones with a pyrrolidinyl side chain, like tosufloxacin and clinafloxacin, have intermediate binding, and those with alkylated side chains, such as temafloxacin and sparfloxacin, have low affinity. Interaction between ciprofloxacin and methadone has been described in one patient who developed confusion, sedation, and respiratory depression. Although serious reactions, seizures, and mental alterations occur, they are very rare. Risk factors for such reactions are high doses (including overdosing as a result of altered excretion, e.g., due to renal or hepatic failure or advanced age), previous epilepsy, and, probably, interactions with nonsteroidal anti-inflammatory drugs (NSAIDs) or theophylline.

Citation: Norby S. 2003. Central Nervous System Toxicity, p 461-465. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch29
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Table 1

In vitro binding of quinolones to GABA A receptors with or without anti-inflammatory drugs (10⁻⁴ M)

Citation: Norby S. 2003. Central Nervous System Toxicity, p 461-465. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch29
Generic image for table
Table 2

Potentiation of the CNS toxicity of quinolone antibiotics

Citation: Norby S. 2003. Central Nervous System Toxicity, p 461-465. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch29

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