Description
Erythromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains. It is effective against a host of bacterial genera, including
Streptococcus,
Staphylococcus, and
Haemophilus (MIC
90s range from 0.015-2.0 mg/l). Erythromycin is known to potently inhibit the cytochrome P450 isoform CYP3A4, which can affect the metabolism of numerous clinically relevant medications. Erythromycin lactobionate is a soluble salt of erythromycin that is typically used for intraperitoneal or intravenous injections.
Chemical Properties
White or slightly yellow hygroscopic, powder.
Originator
Erythrocin,Abbott,US,1954
Uses
Erythromycin Lactobionate is an antibiotic used to reduce the prevalence of drug resistant bacteria as well as keeping constant the efficacy of other antibacterial drugs.
Uses
Macrolide antibacterial.
Manufacturing Process
A solution of erythromycin free base is prepared by dissolving 8.0 grams of
erythromycin in 25 cc of acetone. 4.0 grams of lactobiono-delta-lactone is
dissolved in 25 cc of water. The free lactobionic acid is formed in this solution
and it has the molecular formula C12H22O12. The two solutions are mixed and
evaporated to a gummy residue. This residue is dissolved in 60 cc of water
and the solution is frozen and dried in vacuum by lyophilization. The dried
residue of erythromycin lactobionate is a white amorphous powder and weighs
11.7 grams. The reaction product has an activity against B. subtilis of 420units per milligram. Its solubility in water is about 200 mg/cc and the melting
point of the white powdery reaction product is 145° to 150°C.
brand name
Erythrocin
(Abbott); Erythrocin (Hospira).
Therapeutic Function
Antibacterial
General Description
Erythromycin lactobionate is a water-soluble salt preparedby reacting erythromycin base with lactobiono-σ-lactone. Itoccurs as an amorphous powder that is freely soluble inwater and alcohol and slightly soluble in ether. It is intended,after reconstitution in sterile water, for intravenousadministration to achieve high plasma levels in the treatmentof serious infections.
References
[1] P PERITI. Clinical pharmacokinetic properties of the macrolide antibiotics. Effects of age and various pathophysiological states (Part I).[J]. Clinical Pharmacokinetics, 1989, 16 4: 193-214. DOI:
10.2165/00003088-198916040-00001[2] G. LEBEK G T. Effects in vitro of erythromycin, alone and in combination with penicillin, on staphylococci, pneumococci and streptococci[J]. Current Medical Research and Opinion, 1978, 5 1: 3-14. DOI:
10.1185/03007997809110242[3] E AZOULAY-DUPUIS. Antipneumococcal activity of ciprofloxacin, ofloxacin, and temafloxacin in an experimental mouse pneumonia model at various stages of the disease.[J]. Journal of Infectious Diseases, 1991, 163 2: 319-324. DOI:
10.1093/infdis/163.2.319[4] Y HIRAKATA. Efficacy of erythromycin lactobionate for treating Pseudomonas aeruginosa bacteremia in mice.[J]. Antimicrobial Agents and Chemotherapy, 1992, 36 6: 1198-1203. DOI:
10.1128/aac.36.6.1198
