Concentration of doxycycline in human gingival fluid

Abstract

Doxycycline is a synthetic tetracycline compound whose main advantages over tetracycline hydrochloride are increased oral absorption, prolonged serum half-life and decreased gastrointestinal side-effects. The purpose of this study was to measure the concentration of doxycycline in gingival fluid and blood after oral administration. 4 volunteers were given doses of 100 mg doxycycline every 12 h on the first day of antibiotic administration followed by a maintenance dose of 100 mg per day for an additional 4 days. 3 of these volunteers were also given tetracycline hydrochloride every 6 h for 5 days either 1 month before or after doxycycline administration to compare gingival fluid levels of these 2 tetracycline compounds. Gingival fluid was sampled from 4 gingival sites in each volunteer at hourly intervals from hours 0 to 6, 9, 24, 27, 48 to 54, 57, 72, 75, 96 to 102 and 105. Blood was sampled by finger puncture at hours 0, 3, 6, 24, 48, 54, 72, 96 and 102. Antibiotic levels in gingival fluid and blood were measured using an agar diffusion assay method. The results demonstrated that doxycycline achieved much higher levels in the gingival fluid than in blood and yielded comparable gingival fluid levels to those achieved by tetracycline hydrochloride. Doxycycline levels in gingival fluid ranged between 1.2 micrograms/ml and 8.1 micrograms/ml in the first 24 h and generally achieved 3-10 micrograms/ml after 48 h. Blood levels after 48 h ranged between 2.1 micrograms/ml and 2.9 micrograms/ml. Tetracycline hydrochloride in gingival fluid after 48 h was generally in the range of 4 micrograms/ml-10 micrograms/ml with blood levels between 2.2 micrograms/ml and 3.4 micrograms/ml.(ABSTRACT TRUNCATED AT 250 WORDS)

Modulation of Gingival Fibroblast Minocycline Accumulation by Biological Mediators

“…Interestingly, they appear to distribute preferentially to gingival crevicular fluid (GCF). When taken by the systemic route, tetracyclines attain GCF levels that are approximately 4-to 5-fold higher than serum levels (Ciancio et al, 1980;Pascale et al, 1986). Our recent work has shown that gingival fibroblasts express transporters that allow them to take up extracellular tetracyclines and sequester them in the gingiva (Yang et al, 2002).…”

Accumulation of Ciprofloxacin and Minocycline by Cultured Human Gingival Fibroblasts

“…Due to the unique architecture of the gingiva (Schroeder and Listgarten, 1997), much of the ciprofloxacin or minocycline in interstitial fluid is eventually washed through the junctional epithelium and into the gingival crevice. The existence of a drug reservoir in the gingiva could explain why tetracycline (Gordon et al, 1981), doxycycline (Pascale et al, 1986), minocycline (Ciancio et al, 1980) and ciprofloxacin (Conway et al, 2000) appear to reach higher levels in GF than in blood serum when sampled after blood levels have receded from their peak values. It could also account for the findings of Sakellari et al (2000), who found higher levels of tetracycline, doxycycline and minocycline in blood than in GF.…”

“…Interestingly, both classes of antibiotics appear to preferentially distribute in the gingival fluid (GF). When taken by the systemic route, tetracyclines attain GF levels that are approximately 4-5 fold higher than serum levels, while ciprofloxacin reaches GF levels that are about 4.5 fold higher (Pascale et al, 1986;Ciancio et al 1980;Conway et al, 2000).…”

Tetracycline and Its Analogues: a Therapeutic Paradigm in Periodontal Diseases

“…Tetracyclines have a distinctive property of concentrating in GCF at levels from two to 10 times greater than that of the serum after a single 250-mg dose (Gordon et al, 1981a (Gordon et al, 1981b). Doxycycline achieved gingival fluid levels of 4 to 10 Vg/mL after the administration of 100 mg every 12 hours for the first day, followed by 100 mg/day for 14 days (Pascale et al, 1986). GCF concentrations of minocycline are 5 times as high as serum when 150-200 mg/day are given for 8 days, and can remain bacteriostatic for at least one week after treatment is discontinued (Ciancio et al, 1980).…”