An evaluation of tolerance of roxithromycin in adults

Abstract

This review deals with tolerance of a new macrolide, roxithromycin from data collected from a number of studies in adults. A total of 2917 adults, 2519 given roxithromycin 150 mg bid, were recruited into 17 multicentre comparative or non-comparative studies. Nine studies were double-blind, against doxycycline, erythromycin estolate (EES), lymecycline or cephradine. Overall the drug was well tolerated: side-effects possibly or probably related to roxithromycin were noted in only 4.1% (120/2917) of all patients, and in 3.1% (15/480) of elderly subjects. The gastrointestinal tolerance of roxithromycin was significantly better than that of doxycycline in four trials, and better than that of erythromycin ethylsuccinate in one study. The incidence of drug-related liver function test abnormalities following roxithromycin therapy was low and compared favourably with data published on erythromycin. Roxithromycin shows a satisfactory safety profile at the recommended daily dosage of 150 mg bid in adults.

The overall safety of oral roxithromycin in paediatric clinical studies

“…The particularly low incidence should be compared with that observed with roxithromycin in adults [8]. Nevertheless, it is clear that the incidence of drug-related adverse events is low (20/477 cases, 4%) and led to a dis-Continuation of treatment only in few patients (6/477,1%).…”

“…This macrolide, which is chemically an ether oxime derivative of erythromycin, has an antibacterial spectrum of activity similar to that of erythromycin [3,4]. Since the compound has proved to be effective and safe in adult patients, two large multicentre trials were conducted in children to assess whether roxithromycin offers clinical benefits to paediatric patients with respiratory tract and skin infections, and to evaluate its tolerance profile [8,9]. A long elimination half-life, high plasma levels and good diffusion into the tonsils and adenoids suggest that the mean daily dose of 2.5 mg/kg twice daily used in adults is also appropriate in paediatrics.…”

Prevention ofPneumocystis carinii pneumonia and of cerebral toxoplasmosis by roxithromycin in HIV-infected patients

“…These were expected, mainly gastrointestinal side effects, such as nausea, abdominal pain and raised liver transaminases [9]. Treatment with roxithromycin was discontinued when these events occurred because the dose of roxithromycin was high (three times the usual 300 mg daily dose); thereare no data on the effects of prolonged treatment in man.…”

“…Roxithromycin, an ether oxime derivative of erythromycin, was chosen on the basis of in vitro and in vivo efficacy in animal studies with Toxoplasma gondii infection [1][2][3][4][5] and of the clinical efficacy against PCP in patients intolerant of trimethoprim/sulphamethoxazole (TMP/SMX) and of pentamidine [6]. The pharmacokinetic properties of roxithromycin, namely high serum cerebral tissue concentrations [7], long half-life [8], and good tolerance [9] also favoured this choice.…”

Η Φαρμακοκινητική Της Κλαριθρομυκίνης Στον Προστατικό Ιστό

“…Η ομάδα των μακρολιδίων πλην της Ερυθρομυκίνης, η οποία αποτελεί τον κύριο εκπρόσωπο της ομάδος και ανακαλύφθηκε το 1952 σε ένα στέλεχος του Streptomyces erythreus που απομονώθηκε σε δείγμα εδάφους (χώμα) Με τις Μακρολίδες ,σε αντίθεση με τις αμινογλυκοσίδες και τα β-λακταμικά αντιβιοτικά, επιτυγχάνονται υψηλές συγκεντρώσεις στους ιστούς και ενδοκυττάρια, γεγονός που τους προσδίδει ιδιαίτερη θεραπευτική αξία255 . C, G είναι ευαίσθητοι με σπάνια εμφάνιση αντοχής263,267 . Εκ της ομάδος D, o Streptococcus faecalis είναι ανθεκτικός σε ποσοστό 50%, ενώ ο Streptococcus pneumoniae είναι ευαίσθητος ως και τα στελέχη Streptococcus viridans.…”