Roxithromycin

Brand name: CADITHRO (Rulide, Roxithromycin)

CADITHRO (Rulide, Roxithromycin)
Systematic (IUPAC) name

Identifiers

Therapeutic considerations

CADITHRO (Rulide, Roxithromycin) is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. CADITHRO (Rulide, Roxithromycin) is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring.

CADITHRO (Rulide, Roxithromycin) is available under several brandnames, for example Surlid, Rulide, Biaxsig, Roxar and Roximycin.
Contents

* 1 History * 2 Available forms * * 3 Mechanism of action * 4 Pharmacokinetics * 5 Metabolism * 6 Side effects * 7 Drug interactions History

German pharmaceutical company Hoechst Uclaf brought out CADITHRO (Rulide, Roxithromycin) in 1987.

Available forms *

CADITHRO (Rulide, Roxithromycin) is commonly available as tablets or oral suspension.

Mechanism of action CADITHRO (Rulide, Roxithromycin)

CADITHRO (Rulide, Roxithromycin) prevents bacteria from growing, by interfering with their protein synthesis. CADITHRO (Rulide, Roxithromycin) binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. CADITHRO (Rulide, Roxithromycin) has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila.

Pharmacokinetics

When taken before a meal, CADITHRO (Rulide, Roxithromycin) is very rapidly absorbed, and diffused into most tissues and phagocytes. Due to the high concentration in phagocytes, CADITHRO (Rulide, Roxithromycin) is actively transported to the site of infection. During active phagocytosis, large concentrations of CADITHRO (Rulide, Roxithromycin) are released.

Metabolism

Only a small portion of CADITHRO (Rulide, Roxithromycin) is metabolised. Most of CADITHRO (Rulide, Roxithromycin) is secreted unchanged into the bile and some in expired air. Under 10% is excreted into the urine. CADITHRO (Rulide, Roxithromycin)'s half-life is 12 hours.

Side effects CADITHRO (Rulide, Roxithromycin)

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, and also the rarely seen rashes, abnormal liver function values and alteration in senses of smell and taste.

Drug interactions

CADITHRO (Rulide, Roxithromycin) has less interactions than erythromycin as it has a lower affinity for cytochrome P450.

CADITHRO (Rulide, Roxithromycin) does not interact with oral contraceptives, prednisolone, carbamazepine, ranitidine or antacids.

When CADITHRO (Rulide, Roxithromycin) is administered with theophylline, some studies have shown an increase in the plasma concentration of theophylline. A change in dosage is usually not required but patients with high levels of theophylline at the start of the treatment should have their plasma levels monitored.

CADITHRO (Rulide, Roxithromycin) appears to interact with warfarin. This is shown by an increase in prothrombin time (international normalised ratio (INR)) in patients taking CADITHRO (Rulide, Roxithromycin) and warfarin concurrently. As a consequence, severe bleeding episodes have occurred.