| Identification | Back Directory | [Name]
ROKITAMYCIN | [CAS]
74014-51-0 | [Synonyms]
M-19-Q
Rokital
TMS 19Q
Rikamycin
Ricamycin
ROKITAMYCIN
T'urimyein H4
ROKITAMYCIN USP/EP/BP
3''-Propionylleucomycin A5
Leummycin V 4B-bu-tanoate 3 B-propanoate
Leucomycin V, 4B-butanoate 3B-propanoate
Leucomycin V, 4B-butanoate 3B-propanoate (9CI) | [Molecular Formula]
C42H69NO15 | [MDL Number]
MFCD00941397 | [MOL File]
74014-51-0.mol | [Molecular Weight]
827.99 |
| Chemical Properties | Back Directory | [Melting point ]
116° | [alpha ]
D20 -71° (c = 1.0 in chloroform) | [Boiling point ]
879.3±65.0 °C(Predicted) | [density ]
1.21±0.1 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [pka]
13.06±0.70(Predicted) | [CAS DataBase Reference]
74014-51-0 |
| Hazard Information | Back Directory | [Description]
Rokitamycin is a semisynthetic macrolide
antibiotic, closely related to miokamycin(2) both in structure and antimicrobial spectrum. | [Chemical Properties]
White to slightly yellowish powder, odorless, bitter. Very soluble in methanol, ethanol, ether, acetone, and ethyl acetate, practically insoluble in water or n-hexane. Melting point: 116°C. [α] D25-50° (C = 1, chloroform); [α] D20-71° (C = 1.0, chloroform) has also been reported. UV absorption maximum (ethanol): 232 nm (ε 28,000). | [Originator]
Toyo Jozo (Japan) | [Uses]
ROKITAMYCIN is a macrolide antibiotic with an antibacterial spectrum similar to erythromycin, exhibiting strong antimicrobial activity against Gram-positive bacteria, anaerobes, and Mycoplasma spp. Clinically, it is used for various infections caused by these susceptible bacteria, such as pneumonia, mycoplasmal pneumonia, otitis externa, otitis media, periodontitis, sinusitis, subcutaneous abscess, hidradenitis suppurativa, laryngitis, acute bronchitis, tonsillitis, boils, and erysipelas. | [Definition]
ChEBI: Rokitamycin is an organic molecular entity. | [Brand name]
RICAMYCIN | [Pharmaceutical Applications]
3″-Propionyl leucomycin A5. A semisynthetic macrolide. Unstable in acid media.
The antibacterial spectrum is identical to that of erythromycin, but it is less active against Gram-positive cocci. It is poorly active against H. influenzae (MIC50 8 mg/L) and Mor. catarrhalis (MIC50 4 mg/L). It displays good activity against Campylobacter spp. (MIC50 0.1 mg/L), L. pneumophila (MIC50 0.1 mg/L) and M. pneumoniae (MIC50 0.003 mg/L). It is active against anaerobes, including some Bacteroides spp. (MIC50 <0.05 mg/L).
After a single oral dose of 600 mg, the peak plasma concentration was 1.9 mg/L after 0.6 h. Oral doses of 5, 10 and 15 mg/kg of a syrup formulation given to children achieved plasma concentrations of 0.26, 0.55 and 0.79 mg/L, respectively, after about 40 min. The half-life is around 2 h.
It is mainly eliminated in the bile; only about 2% appears in the urine. Its major metabolites are leucomycin A7, 10″-OH-rokitamycin (which show some antibacterial activity) and leucomycin V. In healthy adult volunteers, the proportions of rokitamycin and its metabolites in serum 30 min after a single oral dose of 1200 mg were 18% (leucomycin A7), 33% (10″-OH-rokitamycin) and 9% (leucomycin V). The pharmacokinetic behavior is not altered in patients with liver cirrhosis. It is available in Italy and Japan. |
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