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| Trade names | Rulide, Biaxsig, others |
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| Metabolism | Liver, peak concentration averaging 2 hours after ingestion. |
| Eliminationhalf-life | 11 hours |
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| ECHA InfoCard | 100.121.308 |
| Chemical and physical data | |
| Formula | C41H76N2O15 |
| Molar mass | 837.058 g·mol−1 |
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Roxithromycin is a semi-syntheticmacrolideantibiotic used to treat respiratory tract, urinary and soft tissue infections. It is a derivative oferythromycin - comprising the same 14-membered lactone ring - with anoxime-basedside chain attached to the macrolide ring.
Roxithromycin was patented in 1980 and approved for medical use in 1987.[1] It is available under several brand names in Australia, France, Germany, Israel, South Korea and New Zealand, but not in the United States. Roxithromycin has also been shown to possess antimalarial activity.[citation needed]
The most common side effects are gastrointestinal: diarrhoea, nausea, abdominal pain and vomiting. Less common side effects include central or peripheral nervous system events such as headaches, dizziness, vertigo.Rarely seen side effects are rashes, abnormal liver function values and alteration in the senses of smell and taste.[citation needed]
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Roxithromycin has fewer interactions thanerythromycin as it has a lower affinity forcytochrome P450.
Roxithromycin is not known to interact withhormonal contraceptives,prednisolone,carbamazepine,ranitidine orantacids.
When roxithromycin is administered withtheophylline, some studies have shown an increase in theplasma concentration oftheophylline. A change in dosage is usually not required but patients with high levels oftheophylline at the start of thetreatment should have their plasma levels monitored.
Roxithromycin appears to interact withwarfarin. This is shown by an increase in prothrombin time and/or international normalised ratio (INR) in patients taking roxithromycin andwarfarin concurrently. As a consequence, severe bleeding episodes have occurred.
Roxithromycin is commonly available as tablets or oral suspension.[citation needed]
Roxithromycin preventsbacteria from growing, by interfering with theirprotein synthesis. Roxithromycin binds to the subunit 50S of the bacterialribosome, and thus inhibits the synthesis ofpeptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularlyLegionella pneumophila.[citation needed]
When taken before a meal, roxithromycin is very rapidly absorbed, and diffuses into most tissues andphagocytes. Due to the high concentration inphagocytes, roxithromycin is actively transported to the site of infection. During active phagocytosis, large concentrations of roxithromycin are released.[citation needed]
Only a small portion of roxithromycin is metabolised. Most of roxithromycin is secreted unchanged into the bile and some in expired air. Under 10% is excreted into the urine. Roxithromycin's half-life is 12 hours.
French pharmaceutical companyRoussel Uclaf first marketed roxithromycin in 1987.
