Erythromycin succinate

A young woman developed severe cholestasis and jaundice after taking erythromycin stearate (47). A second severe episode of jaundice and malaise occurred after treatment with erythromycin succinate 2 years later pointing to erythromycin itself as the culprit. 

Horn S, Aglas F, Horina JH. Cholestasis and liver cell damage due to hypersensitivity to erythromycin stearate— recurrence following therapy with erythromycin succinate. Wien Klin Wochenschr 1999 lll(2) 76-7. 

A randomised, placebo-controlled trial of erythromycin succinate (400 mg twice daily) in noncystic fibrosis subjects recorded few adverse events. One subject with a baseline QTc of 470 ms was withdrawn from the trial at week 24 due to an increase in the QTc to 480 ms [117 ]. 

Ofloxacin 300 mg orally twice daily for 7 days, or levofloxacin 500 mg orally once daily for 7 days, or erythromycin base 500 mg orally four times daily for 7 days, or erythromycin ethyl succinate 800 mg orally four times daily for 7 days Erythromycin base 250 mg orally four times daily for 14 days, or erythromycin ethyl succinate 800 mg orally four times daily for 7 days (or 400 mg orally four times daily for 14 days... 

Semisynthetic Derivatives. Erythromycin has been the principal subject of modification of 14-membered macrolides some of the derivatives are being commercially launched. Derivatives of erythromycin and oleandomycin include 2-U-nee ly I erythromycin (C331129NO t. 2 -O-propionylerythromycin (QoHtiNOm), erythromycin ethyl carbonate (C/0H71NO15), erytliromydn ethyl succinate (C 3H75NOi2), tn-O-acetyloleandomycin (C4iHc7NOi5), erythromycin-11,12-carbonate... 

Decrease solubility Erythromycin Erythromycin30 Ethyl succinate... 

The oral dosage of erythromycin base, stearate, or estolate is 0.25-0.5 g every 6 hours (for children, 40 mg/kg/d). The dosage of erythromycin ethyl succinate is 0.4-0.6 g every 6 hours. Oral... 

Heparin and its salts are incompatible with many drugs including alteplase, amikacin sulfate, amiodarone hydrochloride, ampicillin sodium, aprotinin, benzylpenicillin potassium or sodium, cephalothin sodium, ciprofloxacin lactate, cytarabine, dacarbazine, daunorubicin hydrochloride, diazepam, dobutamine hydrochloride, doxorubicin hydrochloride, droperidol, erythromycin lactobionate, gentamicin sulfate, haloperidol lactate, hyaluronidase, hydrocortisone sodium succinate, kanamycin sulfate, methicillin sodium, netilmicin sulfate, some opioid analgesics, oxytetracycline hydrochloride, some phenothiazines, polymyxin B sulfate, streptomycin sulfate, tetracycline hydrochloride, tobramycin sulfate, vancomycin hydrochloride, vinblastine sulfate, cisatracurium besylate, labetalol hydrochloride, nicardipine hydrochloride, cefmetazole, sodium ions, and fat emulsion.110 112... 

Tablets (e.g., quinapril hydrochloride) Capsules (e.g., pancrease) Oral suspensions (e.g., cefuroxime axetil) Injectables (e.g., coumadin) Sterile powders (e.g., cefoxitin) Topicals (e.g., zinc oxide powder) Anti-infectives (e.g., erythromycin ethyl succinate) Anti-coagulants (e.g., warfarin sodium) Anti-asthmatics (e.g., montelukast sodium) Anti-psychotics and anxiolytics Hypnotics and anticonvulsants (e.g., barbiturates) Anti-hypertensives Anti-inflammatories (e.g., indomethacin) Analgesics (e.g., aspirin) Antacids (e.g., aluminum hydroxide) Diuretics Enzymes (e.g., pancreatin) Hormones...

MW 733), erythromycin estolate (Er-E, MW 789), and erythromycin ethyl succinate (Er-S, MW 789) was analyzed using HSCCC-ESI-MS with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (4 7 4 3). TIC showed, clearly, four peaks corresponding to Er-A, Er-E, Er-S, and an unknown substance. The mass spectra of Er-E and Er-S gave [M + H]+ at miz 862 and 789 and [M -i- H H2O... 

Ester derivatives of erythromycin, shown in Table 4, were synthesized soon after its discovery (124—126). They are readily prepared by acylation of the 2-hydroxyl group the neighboring 3r-dimethylamino group directs acylation to this site. Commonly used esters of erythromycin are propionate, acetate, ethyl succinate, and ethyl carbonate (30). 2r-Esters do not bind bacterial ribosomes, however, and consequently must be hydrolyzed back to the parent to exert antibacterial activity (127). Ester derivatives are still being prepared (128,129). 2,-0-Acetylerythromycin stearate, also known as erythromycin acistrate, is an example undergoing clinical trial (11,130,131). Two salts of 2,-0-propionyl-erythromycin, N-acetylcysteinate (erythromycin stinoprate) and mercaptosuccinate, were prepared to combine antibiotic and mucolytic properties in a single agent (132—134). 

Sample preparation Weigh out materied corresponding to ca. 250 mg erythromycin ethyl-succinate, add 10 mL acetone, sonicate 5 min, centrifuge at 2500 g for 5 min, dilute a 6 mL aliquot of supernatant to 10 mL with 200 mM pH 6.5 tetrabutylammonium hydrogen sulfate 200 mM pH 6.5 phosphate buffer. water 12.5 7.5 80. 

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