What is the available comparative evidence regarding antibiotics and their effect on seizure incidence (e.g. penicillins vs. cephalosporins vs. fluoroquinolones, etc)?

Comment by InpharmD Researcher

The greatest amount of evidence of antibiotic-associated seizure risk seems to implicate beta-lactams but also includes other categories of antibiotics, such as fluoroquinolones. Overall, the comparative data is too limited to rank potential seizure thresholds of antibiotics, which doesn't include other patient and disease-related factors. The data available primarily stems from individual studies and is observed collectively in review articles.

Background

A 2015 systematic review analyzed 143 articles (N=25,712) studying various antibiotics from different classes to examine the current evidence for seizures associated with antibiotics. Studies were mainly classified as low to very low levels of evidence observing beta-lactam agents. Certain penicillins, fourth-generation cephalosporins, and imipenem have been studied the most and seem to be prevalent with use of high doses or in those with renal dysfunction. However, this does not preclude the potential seizure effects of other antibiotic regimens and there is no direct comparison data. The authors have summarized the known data with defined frequency, which is presented in Table 1. [1]

A 2020 review article discussed the available literature regarding antibiotics and epilepsy. Overall, the agents that have been shown to induce seizures include beta-lactams, macrolides, fluoroquinolones, metronidazole, and polymyxins. Among penicillins, penicillin G is described to have the highest epileptic potential without regards to concentration in the cerebrospinal fluid. Between penicillins and cephalosporins, cephalosporins with heterocyclic rings at position 7 and 3 and 3 of 7-aminocephalosporanic acid seem to have similar or greater potential for epilepsy (e.g. cefazolin). Fluoroquinolones with GABA-like structures at 7 positions seem to also have greater epilepsy potential, such as norfloxacin and ciprofloxacin. There are other factors that have seldom been explored such as co-administration with other agents, fever, electrolyte imbalances, metabolic disturbances, and type of infection treatment. More research is needed before comparative conclusions can be made. [2]

A 2014 review article provided similar insights regarding the clinical features and management of antibiotic neurotoxicity. The antibiotic classes most commonly associated with seizures included penicillins, cephalosporins, carbapenems, and fluoroquinolones. Other antibiotics that have been linked to seizures are metronidazole when taken for prolonged periods and isoniazid in overdose. Seizures from antibiotic use are rare, with reported incidence rates of 0.04% for cephalosporins and 0.1-0.5% for fluoroquinolones. However, seizure risk can differ based on patient factors like brain lesions. It also varies within antibiotic classes, as seizures have more often occurred with levofloxacin compared to other fluoroquinolones and with imipenem versus other carbapenems. [3]

References:

[1] Sutter R, Rüegg S, Tschudin-Sutter S. Seizures as adverse events of antibiotic drugs: A systematic review. Neurology. 2015;85(15):1332-1341. doi:10.1212/WNL.0000000000002023
[2] Wanleenuwat P, Suntharampillai N, Iwanowski P. Antibiotic-induced epileptic seizures: mechanisms of action and clinical considerations. Seizure. 2020;81:167-174. doi:10.1016/j.seizure.2020.08.012
[3] Bhattacharyya S, Darby R, Berkowitz AL. Antibiotic-induced neurotoxicity. Curr Infect Dis Rep. 2014;16(12):448. doi:10.1007/s11908-014-0448-3

Literature Review

A search of the published medical literature revealed 2 studies investigating the researchable question:

What is the available comparative evidence regarding antibiotics and their effect on seizure incidence (e.g. penicillins vs. cephalosporins vs. fluoroquinolones, etc)?

Please see Tables 1-2 for your response.


 

Compiled evidence of symptomatic seizures and status epilepticus related to antibiotic drugs in adults extrapolated from Sutter et al. (Only those with frequency defined were included in the table)

Antibiotics Frequency of events American Academy of Neurology classification Reported symptomatic seizures Contributing risk factors for symptomatic seizures
Penicillin G or oxacillin up to 5% Class IV

Generalized myoclonic seizures > convulsive seizures

Renal insufficiency; brain lesions

Cefazolin

80% with renal insufficiency Class IV

Generalized tonic-clonic seizure > NCSE

Renal insufficiency; intrathecal cefazolin injection

Cefepime 

Up to 11% Class III-IV NCSE > generalized seizures > myoclonus

Renal insufficiency; brain lesions

Imipenem

Up to 5% Class III-IV Generalized tonic-clonic seizures

Renal insufficiency; epilepsy; brain lesions; treatment with theophylline (3 cases)

Meropenem

Up to 1% Class III - IV Generalized convulsive seizures > tonic-clonic seizures

Renal insufficiency; epilepsy treated with valproic acid; brain lesions

Doripenem

Up to 1.2% Class III Generalized tonic-clonic seizures Epilepsy

 

References:

Sutter R, Rüegg S, Tschudin-Sutter S. Seizures as adverse events of antibiotic drugs: A systematic review. Neurology. 2015;85(15):1332-1341. doi:10.1212/WNL.0000000000002023

 

Comparison of the Prevalence of Convulsions Associated with the Use of Cefepime and Meropenem

Design

Single center, retrospective, chart review

N = 928

Objective

To investigate the prevalence of convulsions associated with the use of cefepime compared to meropenem

Study Groups

Cefepime group (n = 183)

Meropenem group (n = 745)

Inclusion Criteria

Patients over the age of 18 and treated with cefepime or meropenem

Exclusion Criteria

N/A

Methods

Data on the use of prescription drugs were collected from the medical records of patients treated with cefepime and patients treated with meropenem at Ehime University Hospital. The data was evaluated and the prevalence of convlusions between the two groups was assessed. 

Duration

N/A

Outcome Measures

Cefepime or meropenem-associated convulsion 

Baseline Characteristics

 

Cefepime (n = 183)

Meropenem (n = 745)

 

Age, years

 59 (19-87) 66 (19-90)  

eGFR

71 (9-147)  64 (7-158)  

Results

Endpoint

Cefepime (n = 183)

Meropenem (n = 745)

p-Value

Prevalence of convulsion

 0.54%  2.73%  <0.01

Adverse Events

Common Adverse Events: N/A

Serious Adverse Events: N/A

Percentage that Discontinued due to Adverse Events: N/A

Study Author Conclusions

The prevalence of convulsions is significantly higher in patients treated with cefepime than in patients treated with meropenem. Cefepime-associated convulsions should be recognized as potential complications even in patients with normal renal function. Brain disorders may increase the risk of cefepime-associated convulsions.

InpharmD Researcher Critique

The study was a retrospective analysis and the study design could have resulted in selection bias.



References:

Tanaka A, Takechi K, Watanabe S, Tanaka M, Suemaru K, Araki H. Comparison of the prevalence of convulsions associated with the use of cefepime and meropenem [published correction appears in Int J Clin Pharm. 2015 Jun;37(3):546-7]. Int J Clin Pharm. 2013;35(5):683-687