A/T/S - Erythromycin

Dibucaine (Nupercainal) Doxepin, Topical (Zonalon, Prudoxin) Econazole (Spectazole) Efalizumab (Raptiva) Erythromycin, Topical (A/T/S, Eryderm, Erycette, T-Stat) Erythromycin Benzoyl Peroxide (Benzamycin) Finasteride (Propecia) Fluorouracil, Topical [5-FU] (Efudex) Gentamicin, Topical (Garamycin, G-Mycitin)... 

Trade names A/T/S, Bristsmycin, E.E.S., E-Mycin, Eryc, EryDerm, EryPed, Erythrocin, llotycin, Pediamycin, Pediazole, Pfizer-E, Robimycin, SK-Erythromycin, Staticin, Wyamycin Use Antibacterial HPLC ... 

Figure 1.2 Impurities in a sample of erythromycin A. Reproduced from [11]. Reproduced by permission from the publisher and authors. (Column 250 X 4.6 mm i.d. 8 pm 1000 A PLRP-S mobile-phase acetonitrile t-butanol 200 mM pH 9.0 phosphate buffer water 3 16.5 5 75.5 flowrate 2 mL/min column temperature 70°C injection 100 pi of a4 mg/ml solution detector UV 215 nm.)...

Antibiotics a, chiortetracyciine b, erythromycin c, gentamicin d, neomycin e, oxytetracycline t, penicillins g, streptomycin h, tetracycline i, tylosin j, chloramphenicol. Sulfonamides k, sulfabromomethazine I, sulta-chlorpyridazine m, sulfadiazine n, sulfadimethoxine o, sulfaethoxypyridazine p, sulfamethoxypyridazine q, sulfapyridine r, sulfamethazine s, sulfaquinoxaline t, sulfathiazole... 

Anderson, G., Esmonde, T. S., Coles, S., Macklin, J., and Carnegie, C. (1991). A comparative safety and efficacy study of clarithromycin and erythromycin stearate in community-acquired pneumonia. J. Antimicrob. Chemother. 27, 117-124. 

Assuming that the major accumulation of erythromycin in S. aureus cells is determined by uptake dependent on the amounts of ribosome present in the cells, these observations of drug accumulation can be easily accounted for. As described in a previous section, erythromycin molecules can bind to ribosome at a certain equilibrium state expressed as a dissociation constant [39]. For example, on the supposition that an intracellular concentration of erythromycin increases by 30 times the level of that in an extracellular medium (1 pg/ml), the nonprotonated molecules of erythromycin (p T = 8.8) are able to occupy no more than 1% of a drug concentration present in S. aureus cell. That is why it is expected that intracellular pH would be 6.8 or less [200] and that erythromycin (even as a free base) with p T = 8.8 is one of the most water-soluble (i.e., deposition-resisting) drugs in the macrolide antibiotics (Table I). 

Scheme 11.38. A representation of the polyketide synthase that is found to produce 3-deoxyerythronolyde B on the way to erythromycin A. See Pfeifer, B. A. Admiraal, S. J. Gramago, H. Cane, D. Khosia, C. Science, 2001, 291, 1790 for a leading reference to this elegant work and Chen, A. Y. Schnarr, N. A. Kim, C.-Y. Cane, D. E. Khosia, C. T. Am. Chem. Soc., 2006,128, 3067.

Tateishi, T., Graham, S. G., Krivoruk, Y., and Wood, A. J. J. (1995) Omeprazole does not affect measured CYP3A4 activity using the erythromycin breath test. Bn J. Clin. Pharmacol. 40, 411-412. 

Nakagawa, Y., Itai, S., Yoshida, T., and Nagai,T. (1992), Physicochemical properties and stability in the acidic solution of a new macrolide antibiotic, clarithromycin, In comparison with erythromycin, Chem. Pharm. Bull., 40,725-728. 

Hagg S, Spigset O, Mjorndal T, Granberg K, Persbo-Lundqvist G, Dahlqvist R. Absence of interaction between erythromycin and a single dose of clozapine. Eur J Clin Pharmacol 1999 55(3) 221-6. 

Sande, M.A. Mandell, G.L. Antimicrobial agents tetra-cyline, chloramphenicol, erythromycin, and miscellaneous antibacterial agents. In Pharmacological Basis of Therapeutics, 8th Ed. Gilman, A.G., Rail, T.W., Nies, A.S., Taylor, P., Eds. Pergamon Press New York, 1991 1117-1145. 

Thiboutot D, Jarratt M, Rich P, Rist T, Rodriguez D, Levy S. A randomized, parallel, vehicle-controlled comparison of two erythromycin/benzoyl peroxide preparations for acne vulgaris. Qin Ther 2002 24(5) 773-85. 

Pesco-Koplowitz L, Hassell A, Lee P, Zhou H, HaU N, Wiesinger B, Mechlinski W, Grover M, Hunt T, Smith R, Travers S. Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of steady-state intranasal levocabastine. J Qin Pharmacol 1999 39(l) 76-85. 

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