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. 1980 Dec;56(6):355–362. doi: 10.1136/sti.56.6.355

Kinetic study of serum penicillin concentrations after single doses of benzathine and benethamine penicillins in young and old people.

P Collart, M Poitevin, A Milovanovic, A Herlin, J Durel
PMCID: PMC1045831  PMID: 7448577

Abstract

In a comparative kinetic study of the serum concentrations of two penicillin complexes--medium-long-acting (benethamine penicillin) and long-acting (benzathine bipenicillin)--after a single injection in young adults and elderly people, the following results were confirmed statistically: (a) age was a major factor in the variations in serum penicillin concentrations and in their persistence in the serum; (b) the penicillin was absorbed faster in young than in elderly subjects even when a long-acting complex was used; (c) serum concentrations below the level regarded as lethal for treponemes appeared much earlier and more frequently in young than in old people; and (d) the bioequivalence between penicillin preparations could not be estimated solely for the number of units of the agent used but from the bioavailability of the chosen formulation. Thus a uniform and standard penicillin dosage allowing no safety margin may help in the superficial healing of a syphilitic chancre or the resolution of a roseola but it will certainly be insufficient to kill Treponema pallidum. It seems essential therefore to provide an antibiotic cover at high dosage over a long period of time.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. BROWN W. J. Syphilis and gonorrhea in general practice. Clin Med (Northfield) 1962 Jan;69:91–100. [PubMed] [Google Scholar]
  2. Bender A. D. Pharmacodynamic principles of drug therapy in the aged. J Am Geriatr Soc. 1974 Jul;22(7):296–303. doi: 10.1111/j.1532-5415.1974.tb05397.x. [DOI] [PubMed] [Google Scholar]
  3. Bennett J. V., Brodie J. L., Benner E. J., Kirby W. M. Simplified, accurate method for antibiotic assay of clinical specimens. Appl Microbiol. 1966 Mar;14(2):170–177. doi: 10.1128/am.14.2.170-177.1966. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. CHABBERT Y., BOULINGRE H. Modifications pratiques concernant le dosage des antibiotiques en clinique. Rev Fr Etud Clin Biol. 1957 Jun;2(6):636–640. [PubMed] [Google Scholar]
  5. Chan K., Kendall M. J., Mitchard M., Wells W. D. The effect of ageing on plasma pethidine concentration. Br J Clin Pharmacol. 1975 Aug;2(4):297–302. doi: 10.1111/j.1365-2125.1975.tb02773.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Collart P. Critique des éléments de base sur lesquels reposent certains traitements de la syphilis. Sem Hop. 1974 Feb 26;50(10):673–679. [PubMed] [Google Scholar]
  7. Collart P., Poitevin M. Données récentes sur le comportement biologique des tréponèmes pâles. Rev Prat. 1976 Dec 11;26(57):4065–4076. [PubMed] [Google Scholar]
  8. EAGLE H., FLEISCHMAN R., MUSSELMAN A. D. The effective concentrations of penicillin in vitro and in vivo for streptococci, pneumococci, and Treponema pallidum. J Bacteriol. 1950 May;59(5):625–643. doi: 10.1128/jb.59.5.625-643.1950. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Eben-Moussi E., van den Driessche J. Pharmaco-cinetique des antibiotiques dans l'organisme humain. Anesth Analg (Paris) 1971 Jul-Aug;28(4):671–687. [PubMed] [Google Scholar]
  10. Giles A. J., Lawrence A. G. Treatment failure with penicillin in early syphilis. Br J Vener Dis. 1979 Feb;55(1):62–64. doi: 10.1136/sti.55.1.62. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Gladtke E. Pharmacokinetics in relation to age. Boll Chim Farm. 1973 May;112(5):333–341. [PubMed] [Google Scholar]
  12. HEITE H. J. Beitrag zur Verteilung des Penicillins im Säugetierorganismus. Klin Wochenschr. 1952 Feb 15;30(7-8):174–175. doi: 10.1007/BF01478255. [DOI] [PubMed] [Google Scholar]
  13. HURIEZ C., DESMONS F., FOSSATI-DELESCLUSE R. ETUDE TH'ERAPEUTIQUE ET M'ETABOLIQUE DE LA B'ENETHAMINE-P'ENICILLINE. Bull Soc Fr Dermatol Syphiligr. 1964 Sep-Oct;71:643–644. [PubMed] [Google Scholar]
  14. Hansen J. M., Kampmann J., Laursen H. Renal excretion of drugs in the elderly. Lancet. 1970 May 30;1(7657):1170–1170. doi: 10.1016/s0140-6736(70)91236-5. [DOI] [PubMed] [Google Scholar]
  15. Hirtz J., Schoeller J. P. Intérêt clinique du doseage des médicaments dans le sang: un nouvel aspect de la pharmacocinétique. Nouv Presse Med. 1976 Mar 27;5(13):869–872. [PubMed] [Google Scholar]
  16. Kunin C. M. Clinical pharmacology of the new penicillins. 1. The importance of serum protein binding in determining antimicrobial activity and concentration in serum. Clin Pharmacol Ther. 1966 Mar-Apr;7(2):166–179. doi: 10.1002/cpt196672166. [DOI] [PubMed] [Google Scholar]
  17. LEIKOLA E., VARTIA K. O. On penicillin levels in young and geriatric subjects. J Gerontol. 1957 Jan;12(1):48–52. doi: 10.1093/geronj/12.1.48. [DOI] [PubMed] [Google Scholar]
  18. LIGHTBOWN J. W., SULITZEANU D. The assay of penicillin in blood-serum using Sarcina lutea. Bull World Health Organ. 1957;17(4-5):553–567. [PMC free article] [PubMed] [Google Scholar]
  19. Lanigan-O'Keeffe F. M. Monorecidive or chancre redux. Br J Clin Pract. 1978 Jul;32(7):206–207. [PubMed] [Google Scholar]
  20. MAGNUSON H. J. The use of antibiotics in spirochaetosis laboratory and general considerations. Ann N Y Acad Sci. 1952 Dec 30;55(6):1161–1167. doi: 10.1111/j.1749-6632.1952.tb22680.x. [DOI] [PubMed] [Google Scholar]
  21. NELSON M. G., TALBOT J. M., BINNS T. B. Benethamine penicillin: a new salt with a prolonged action. Br Med J. 1954 Aug 7;2(4883):339–341. doi: 10.1136/bmj.2.4883.339. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. REIN C. R., BUCKWALTER F. H., MANN C. H., LANDY S. E., FLAX S. Time-dosage relationship in the treatment of treponemal diseases with a new combination of three penicillin salts; laboratory and clinical basis for effective therapy. J Invest Dermatol. 1953 Dec;21(6):435-44; discussion, 444-6. doi: 10.1038/jid.1953.120. [DOI] [PubMed] [Google Scholar]
  23. Schumacher G. E. Practical pharmacokinetic techniques for drug consultation and evaluation. I. Use of dosage regimen calculations. Am J Hosp Pharm. 1972 Jun;29(6):474–484. [PubMed] [Google Scholar]
  24. Simon C., Malerczyk V., Müller U., Müller G. Zur Pharmakokinetik von Propicillin bei geriatrischen Patienten im Verglich zu jüngeren Erwachsenen. Dtsch Med Wochenschr. 1972 Dec 29;97(52):1999–2003. doi: 10.1055/s-0028-1107695. [DOI] [PubMed] [Google Scholar]
  25. Tinkler A. E., Shannon R. Daily penicillin serum concentrations following injection of 2.4 mega-units of "all purpose" penicillin. Bull World Health Organ. 1966;35(6):857–862. [PMC free article] [PubMed] [Google Scholar]
  26. Vignalou J. Généralités sur la thérapeutique en gériatrie. Cah Med. 1974 Sep;15(9):573–578. [PubMed] [Google Scholar]
  27. WILLCOX R. R. Treatment of early venereal syphilis with antibiotics. Br J Vener Dis. 1962 Sep;38:109–125. doi: 10.1136/sti.38.3.109. [DOI] [PMC free article] [PubMed] [Google Scholar]
  28. Wallace S., Whiting B. Factors affecting drug binding in plasma of elderly patients. Br J Clin Pharmacol. 1976 Apr;3(2):327–330. doi: 10.1111/j.1365-2125.1976.tb00611.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  29. de GRACIANSKY, GRUPPER C. [Results of the treatment of primo-secondary syphilis by single injection of long-delayed penicillin. (Apropos of 147 cases)]. Bull Soc Fr Dermatol Syphiligr. 1959 Nov-Dec;5:699–710. [PubMed] [Google Scholar]

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