Roxithromycin

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Roxithromycin

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Catalog Number	PR80214831
CAS	80214-83-1
Description	Roxithromycin is semisynthetic derivative of erythromycin A. It has a role as an antibacterial drug. It is an erythromycin derivative, a macrolide and a semisynthetic derivative. It is functionally related to an erythromycin A.
Synonyms	Rulide; Roxithromycinum; Roxithromycine
IUPAC Name	(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one
Molecular Weight	837.0
Molecular Formula	C41H76N2O15
InChI	RXZBMPWDPOLZGW-XMRMVWPWSA-N
InChI Key	InChI=1S/C41H76N2O15/c1-15-29-41(10,49)34(45)24(4)31(42-53-21-52-17-16-50-13)22(2)19-39(8,48)36(58-38-32(44)28(43(11)12)18-23(3)54-38)25(5)33(26(6)37(47)56-29)57-30-20-40(9,51-14)35(46)27(7)55-30/h22-30,32-36,38,44-46,48-49H,15-21H2,1-14H3/b42-31+/t22-,23-,24+,25+,26-,27+,28+,29-,30+,32-,33+,34-,35+,36-,38+,39-,40-,41-/m1/s1
Drug Categories	Anti-Bacterial Agents; Anti-Infective Agents; Antibacterials for Systemic Use; Antiinfectives for Systemic Use; Cytochrome P-450 CYP2B6 Inhibitors; Cytochrome P-450 CYP2B6 Inhibitors (strength unknown); Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 CYP3A Substrates; Cytochrome P-450 CYP3A4 Inhibitors; Cytochrome P-450 CYP3A4 Inhibitors (weak); Cytochrome P-450 CYP3A4 Substrates; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Substrates; Erythromycin and similars; Lactones; Macrolides; Macrolides, Lincosamides and Streptogramins; Moderate Risk QTc-Prolonging Agents; OATP1B1/SLCO1B1 Inhibitors; OATP1B3 inhibitors; Polyketides; QTc Prolonging Agents
Drug Interactions	Abametapir-The serum concentration of Roxithromycin can be increased when it is combined with Abametapir. Abemaciclib-The metabolism of Abemaciclib can be decreased when combined with Roxithromycin. Acalabrutinib-The metabolism of Acalabrutinib can be decreased when combined with Roxithromycin. Acenocoumarol-The serum concentration of Acenocoumarol can be increased when it is combined with Roxithromycin. Acrivastine-The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Roxithromycin.
Half-Life	12 hours
Isomeric SMILES	CC[C@@H]1[C@@]([C@@H]([C@H](/C(=N/OCOCCOC)/[C@@H](C[C@@]([C@@H]([C@H]([C@@H]([C@H](C(=O)O1)C)O[C@H]2C[C@@]([C@H]([C@@H](O2)C)O)(C)OC)C)O[C@H]3[C@@H]([C@H](C[C@H](O3)C)N(C)C)O)(C)O)C)C)O)(C)O
Type	Small Molecule
Therapeutic Category	Antibacterials

Pharmacology

Indications

Roxithromycin is indicated for the treatment of infections affecting the respiratory tract, urinary tract, and soft tissues. This antibiotic is specifically effective against a range of bacterial infections in these areas, making it a valuable option in clinical settings for managing such conditions.

Pharmacodynamics

Roxithromycin exhibits a broad antibacterial spectrum in vitro, which includes activity against pathogens such as Streptococcus agalactiae, Streptococcus pneumoniae (Pneumococcus), and Neisseria meningitides (Meningococcus). It is also effective against Listeria monocytogenes, Mycoplasma pneumoniae, Chlamydia trachomatis, Ureaplasma urealyticum, Legionella pneumophila, Helicobacter species, Gardnerella vaginalis, Bordetella pertussis, Moraxella catarrhalis (Branhamella catarrhalis), and Haemophilus ducreyi. Roxithromycin is concentrated within polymorphonuclear leukocytes and macrophages, achieving higher intracellular concentrations than extracellular ones. It enhances the adhesive and chemotactic functions of these cells, facilitating phagocytosis and the subsequent lysis of bacteria, while also demonstrating intracellular bactericidal activity.

Absorption

Roxithromycin is rapidly absorbed and distributed into most tissues and phagocytes, ensuring that therapeutic concentrations are reached quickly throughout the body. This rapid absorption aids in the effectiveness of the drug against targeted infections.

Metabolism

Roxithromycin undergoes partial metabolism in the liver, with more than half of the parent compound being excreted unchanged. Its metabolites are excreted via urine and feces, and include the major metabolite descladinose roxithromycin, alongside minor metabolites N-mono and N-di-demethyl roxithromycin. The distribution of the parent drug and its metabolites is similar across both urine and fecal excretions.

Mechanism of Action

Roxithromycin functions by inhibiting bacterial proliferation through disruption of protein synthesis. It achieves this by binding to the 50S subunit of the bacterial ribosome, thereby hindering the translocation of peptides and effectively preventing their assembly.

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