Journal of Antimicrobial Chemotherapy, Vol 40, 83-92, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
R Stahlmann and R Schwabe
Preclinical investigations with grepafloxacin showed that its toxicological
profile is similar to that of other fluoroquinolones. The photosensitizing
effect of grepafloxacin was relatively weak and similar to that of
ciprofloxacin. Grepafloxacin did not cause convulsions in mice when
administered in conjunction with the non- steroidal anti-inflammatory drug
fenbufen. Intravenous injection of grepafloxacin caused transient
dysrhythmias in rabbits at a dosage of 10 mg/kg and ventricular tachycardia
at 30 mg/kg iv. Joint cartilage lesions were found in juvenile dogs after
iv treatment with 100 mg/kg daily. Plasma concentrations (19-24 mg/L) under
these conditions were approximately ten times above a therapeutic level.
Data derived from patients who had been treated with grepafloxacin in phase
II and phase III multiple-dose studies (400 mg, n = 1069; 600 mg, n = 925)
were available for an analysis of the patients' tolerance of the drug. The
most common adverse events observed for the 400 mg and 600 mg treatments
during these studies were gastrointestinal reactions, such as nausea (11%
and 15%, respectively), vomiting (1% and 6%) and diarrhoea (3% and 4%). In
both groups a considerable number of patients (9% and 17%) reported an
unpleasant taste; this was less common in the pooled controls (1%) after
treatment with drugs such as doxycycline, ciprofloxacin, amoxycillin or
cefixime. Headache occurred in 4% (400 mg) and 5% (600 mg) and insomnia in
1% (400 mg) or 2% (600 mg) of the patients. Similar incidences were found
for photosensitivity (1% and 2%, respectively) and for rash (1% and 2%) in
the 400 mg and 600 mg groups. So far, tolerance of the new compound seems
to be similar to that of other fluoroquinolones. However, incidences of
nausea, vomiting and unpleasant taste were rather high during the first
clinical trials, particularly after treatment with 600 mg daily. Further
data are necessary for a sound evaluation of the tolerance of
grepafloxacin.
ORIGINAL ARTICLES
Safety profile of grepafloxacin compared with other fluoroquinolones
Institut fur Klinische Pharmakologie und Toxikologie, Universitatsklinikum Benjamin Franklin Freie Universitat Berlin, Germany.
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