Effect of cephalosporins on gamma-aminobutyric acid receptor binding with or without non-steroidal anti-inflammatory drugs.

  title={Effect of cephalosporins on gamma-aminobutyric acid receptor binding with or without non-steroidal anti-inflammatory drugs.},
  author={Seiji Hori and Keiji Kanemitsu and Jingoro Shimada},
  journal={The Journal of antibiotics},
  volume={46 7},
Cephalosporins have been well known to have potent convulsant activity. We studied the mechanism of the convulsions induced by cephalosporins. Cefazolin, cephaloridine, cefpirome and cefmetazole inhibited the receptor binding of gamma-aminobutyric acid (GABA), an inhibitory transmitter in the mammalian central nervous system. As fluoroquinolones also inhibited GABA receptor binding and this inhibition was enhanced in the presence of non-steroidal anti-inflammatory drugs (NSAIDs), we studied the… 
6 Citations
The Art of Fusion: From Penams and Cephems to Penems
Several investigational penems exhibit interesting antibacterial spectra, encompassing methicillin resistant staphylococci, enterococci and even P. aeruginosa due to their improved binding affinity to both wild-type and modified low-affinity penicillin binding proteins.
Neuropsychiatric Effects of Antimicrobial Agents
A number of antimicrobial drugs have the potential to exert CNS effects and many are associated with stimulant, psychotomimetic and epileptogenic properties, mediated by GABA antagonism, NMDA agonism, and more exotic mechanisms.
How epileptogenic are the recent antibiotics?
OBJECTIVE To review the clinical and experimental data concerning the serious neurologic adverse events, and more particularly seizures, which could be related to the administration of recent
From ion currents to genomic analysis: Recent advances in GABAA receptor research
The description of a receptor gene superfamily comprising the subunits of the GABAA, nicotinic acetylcholine, and glycine receptors has led to a new way of thinking about gene expression and receptor assembly in the nervous system.


Inhibitory effect of cephalosporins on gamma-aminobutyric acid receptor binding in rat synaptic membranes
Cephalosporins inhibited gamma-aminobutyric acid receptor binding in a concentration-dependent manner in vitro. Scatchard analysis revealed that cefazolin decreased the binding capacity but did not
Effects of drugs on γ-aminobutyric acid receptors, uptake, release and synthesis in vitro
The effects of various convulsant and anticonvulsant drugs have been studied using in vitro assays for the postsynaptic action of the neurotransmitter γ-aminobutyric acid (GABA). GABA caused a
Neurotoxicity of β-lactam antibiotics: predisposing factors and pathogenesis
There is now strong evidence that the concentration of beta-lactam in the brain, and not that in the cerebrospinal fluid, is the decisive factor for the risk of neurotoxic reactions.
Epileptogenic Activity of Cephalosporins in Rats and Their Structure‐Activity Relationship
Compounds such as eeftizoxime, cephalexin, and cephradine, substituted at R2 with small groups, were almost incapable of producing epileptogenic activity, which may indicate that the substitution of a heterocyclic ring at position 3 will provoke the convulsive actions.
Inhibition of GABA and benzodiazepine receptor binding by penicillins
The results are consistent with the assumption that penicillins are weak GABA receptor antagonists, and their potencies as inhibitors of specific [3H]GABA binding to rat brain membranes were investigated.
Gamma-aminobutyric acid binding to receptor sites in the rat central nervous system.
Gamma-aminobutyric acid binds to synaptic membrane fractions of rat brain in a selective fashion representing an interaction with postsynaptic GABA receptors, with intermediate values in the thalamus, hippocampus, hypothalamus, cerebral cortex, midbrain, and corpus striatum.
Epilepsy and γ-Aminobutyric Acid-Mediated Inhibition
This chapter discusses epilepsy and γ-aminobutyric acid (GABA) mediated inhibition and the principal sites where GABA produces hyperpolarization of the neuronal membrane, which resembles the physiologically induced inhibitory postsynaptic potential (IPSP).
Seizures associated with high cerebrospinal fluid concentrations of cefazolin.
Three cases of generalized seizures in patients with high cerebrospinal fluid (CSF) concentrations of cefazolin are reported and cefzolin doses should be adjusted in these patients to avoid seizures.
Convulsions associated with sodium cefazolin: a case report.
Although a cause and effect relationship between high cefazolin levels and neurotoxicity cannot be proven conclusively, the implication of this relationship exists is that the clinician should be aware of the potential neurotoxicity of this commonly used drug.