Erythromycin
 | |
| Material name by the IUPAC glossology | |
|---|---|
| (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R) -6-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyl oxane-2-yl] oxy}-14- ethyl-7,12,13-bird hydroxy -4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyl oxane-2-yl]oxy}-3,5,7,9,11,13- hexamethyl-1-oxa cyclo tetradecane-2,10-dione | |
| Clinical data | |
| Fetus degree of risk classification | |
| Legal regulation |
|
| Dosage method | Oral, intravenous feeding intravenous injection, intramuscular injection, local site |
| Pharmacokinetics data | |
| Bioavailability | 100% |
| Plasma protein combination | 90% |
| Metabolism | Liver (under 5% excreted unchanged) |
| Half-life | 1.5 Time |
| Excretion | Choler |
| Identification | |
| CAS number (MeSH) | 114-07-8 |
| ATC cord | D10AF02 (WHO) J01FA01 (WHO)S01AA17 (WHO) |
| PubChem | CID: 3255 |
| DrugBank | APRD00953 |
| ChemSpider | 12041 |
| KEGG | D00140 |
| Chemical data | |
| Chemical formula | C37H67NO13 |
| Molecular weight | 733.93 g/mol |
Erythromycin (erythromycin) is one of the macrolide derivative antibiotics. The product name "Erythrocin ®" (Mylan EPD joint company production sale). The antibacterial spectrum resembles penicillin, but is often used for a person having an allergy to penicillin slightly widely. About the infectious disease to a respiratory system, I have a high effect for the non-fixed form microbes such as mycoplasmal クラミドフィラ, but do not show antibacterial activity to the Haemophilus influenzae which is one of the pathogens of the community-acquired pneumonia. When I deal with chlamydia, syphilis, an outbreak of gonorrhea, I am used. I have structure with two sugar (L-クラジノース and D-デソアミン) in a 14-membered ring lactone ring. It is a compound said to that it is difficult that there is ten places of asymmetric center and composes it because structure is complicated.
I am created by Saccaropolyspora erythraea (former name Streptomyces erythraeus) of the actinomyces genus.
Table of contents
History
In 1949, Philippine scientist アベラルド アギュイラー (Abelardo Aguilar) sent a sample of a certain soil to Eli Lilly which employed him. I succeeded in the study team of Eli Lilly which McGwire (J. M. McGuire) led isolating erythromycin from a metabolism product of strain Streptomyces erythraeus included in the sample. I took place name Iloilo where a sample was gathered of Philippines, and the brand name was marketed in イロソン Ilosone® and christening られ, 1952. I was called イロチシン Ilotycin®. In 1981, Robert Barnes Woodward of the Nobel Prize in Chemistry prize winner and the study team reported the first stereoselective asymmetric composition of erythromycin A in chemical professors of Harvard University.
Formulation
It is available in 腸溶 coating tablet, a sustained release capsule, dry syrup, oral suspension, eye drops, ointment, jelly, the form of the injection agent. (in Japan only as for some formulations)
As a brand name Erythrocin, Robimycin, E-Mycin, E.E.S. Granules, E.E.S.-200, E.E.S.-400, E.E.S.-400 Filmtab, Erymax, Ery-Tab, Eryc, Erypar, EryPed, Eryped 200, Eryped 400, Erythrocin Stearate Filmtab, Erythrocot, E-Base, Ilosone, MY-E, Pediamycin, PCE Dispertab are known.
Action mechanism
I suppress the increase by obstructing the protein synthesis of bacteria. I obstruct transposition of the peptide by the erythromycin binding to the rRNA in the ribosome of bacteria for 23s of the 50S subunit, and blocking up the exit of the peptide to extend.
Pharmacokinetics
I give coating to deactivate it by gastric acid easily when I give it orally, or it is necessary to prescribe more stable salt and ester body. It is high in the speed to be absorbed and spreads to most organizations and phagocytes. Because the density in the phagocyte is easy to rise, it arrives at the infection part immediately, and highly-concentrated erythromycin is released while a phagocyte is active. There is not the shift to a cerebrospinal fluid. Bioavailability is around 50%.
Metabolism
Most get demethylating it for liver and are metabolized. In the main discharge course, a small quantity is exhausted in choler by urine. Half-life is 1.5 hours.
Side effect
Alimentary system disorders such as diarrhea, nausea, abdominal pain, vomiting are seen well. It is said that these symptoms occur because a material called ヘミケタル which occurs when erythromycin is broken down in stomach aggravates gastrointestinal peristalsis. Therefore there is not so that it is prescribed as a first-line drug. However, it is said that it is effective when I treat gastroparesis (gastroparesis) because I have an effect to cause such a kineticism. Intravenous erythromycin may be used to let you exhaust the contents of the stomach in the case of examination with esophagogastric duodenal mirror.
A more serious side effects such as hearing losses are rare. The allergic reaction is not common, but hives and anaphylaxis may be caused. Cholestasis、Stevens-Johnson syndrome、Toxic necrolysisなどもまれに is seen.
When mother takes in erythromycin late in the pregnancy, I am shown to increase possibility of the pyloric senosis of the child.
Contraindicated
Because an example of the sudden death was reported early, a large-scale cohort study was carried out, and the erythromycin in the patient who gave verapamil or diltiazem which inhibited CYP3A4 which was one of cytochrome P450, and delayed metabolism of the erythromycin at the same time and connection of tachycardia and the cardiac sudden death were clarified [1]. In other words, the erythromycin was concluded when you should avoid the dosage for the patient who used the drug which postponed those drugs and QT time. As another example, I include terfenadine (Seldane®, Seldane-D®), astemizole (Hismanal®), cisapride (the authorization is canceled for an effect to let you extend QT time in a country of a lot of Propulsid®,), pimozide (Orap®).
References
- ^ Ray, W.A.; Murray, K. T.; Meredith, S.; Narasimhulu, S. S.; Hall, K.; Stein, C. M. (2004). "Oral Erythromycin and the risk of sudden death from cardiac causes". NEJM. It is 1089–1096. 351 PMID 15356306
This article is taken from the Japanese Wikipedia Erythromycin
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