Roxithromycin

Roxithromycin

Basics

Roxithromycin is a semisynthetic macrolide antibiotic. It is used to treat infections of the respiratory tract, urinary tract, and soft tissues. Roxithromycin is derived from erythromycin and has an almost identical structure. Roxithromycin is most effective against certain Gram-negative bacteria, particularly Legionella pneumophila. It is also currently being tested in clinical trials for the treatment of male pattern hair loss. It is taken by mouth.

Effect

Pharmacodynamics

Roxithromycin prevents the growth of bacteria by interfering with their protein synthesis. Roxithromycin binds to the 50S subunit of the bacterial ribosome, inhibiting the synthesis of peptides. This prevents the bacteria from multiplying and dividing.

Pharmacokinetics

Roxithromycin is absorbed very rapidly in the intestine and is 96% bound to plasma proteins in the blood. Roxithromycin is only partially metabolized in the liver, and more than half of the parent compound is excreted unchanged. The elimination half-life is approximately 12 hours.

Drug Interactions

  • When combined with statins, there is a risk of serious side effects such as myopathy and rabdomyolysis.
  • When Roxithromycin is combined with other antibiotics, cross-resistance may develop. These include primarily lincosamides, clindamycin, and chloramphenicol.
  • Plasma levels of carbamazepine, theophylline, digoxin, and valproic acid may be increased when combined, resulting in a higher risk of adverse reactions.
  • Terfenadine, astemizole, and cisapride may cause life-threatening cardiac arrhythmias when taken concomitantly.
  • Methylprednisolone, triazolam, midazolam, alfentanil, felodipine, and coumarin-type anticoagulants may be metabolized more slowly, increasing duration and potency of action.

Toxicity

Side effects

The most common side effects are gastrointestinal;

  • diarrhea
  • Nausea
  • Abdominal pain
  • Vomiting

Less common side effects include central or peripheral nervous system events such as headache, dizziness, vertigo and also the rarely seen skin rashes, abnormal liver function values and alteration of the sense of smell and taste.

Toxicological Data

LD50 (rat, oral): 830 mg-kg-1

Chemical & physical properties

ATC Code J01FA06
Formula C41H76N2O15
Molar Mass (g·mol−1) 837,05
Physical State solid
Melting Point (°C) 110–125
CAS Number 80214-83-1
PUB Number 6915744
Drugbank ID DB00778

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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