Skip to main content
PMC home page
Antimicrobial Agents and Chemotherapy logoLink to Antimicrobial Agents and Chemotherapy
. 1983 May;23(5):721–725. doi: 10.1128/aac.23.5.721

Comparative pharmacokinetics of metronidazole and tinidazole as influenced by administration route.

J Mattila, P T Männistö, R Mäntylä, S Nykänen, U Lamminsivu
PMCID: PMC184797  PMID: 6870221

Abstract

Serum kinetics of metronidazole and tinidazole were compared in four separate randomized crossover studies. Single doses of each drug were given to healthy volunteers through intravenous infusion (500 mg over 20 min, six persons), by mouth (500 mg, nine persons), by rectum (1,000 mg, six persons), or intravaginally (500 mg, six persons). Concentrations of the unchanged drugs in serum, measured by high-pressure liquid chromatography, were similar after oral and intravenous administration, with mean peaks of 9.0 and 9.4 micrograms/ml for metronidazole and 7.5 and 10.1 micrograms/ml for tinidazole. Concentrations of tinidazole were significantly higher than those of metronidazole from 4 h onwards after intravenous infusion, and from 3 h onwards after administration by mouth. After rectal administrations, a significant difference was seen only at 48 h. After vaginal dosing, however, concentrations of metronidazole were significantly higher than those of tinidazole between 1.5 and 12 h. Bioavailability of either drug, calculated according to the formula (area under the curve for oral administration)/(area under the curve for infusion), was practically complete after oral administration and was poorer after rectal and especially vaginal administration. Whenever the parameters were calculable, the elimination half-life of tinidazole (range of means, 14.0 to 14.7 h) was significantly longer and total clearance (40.3 to 47.6 ml/min) was lower than the corresponding values of metronidazole (7.9 to 8.8 h and 71.8 to 80.1 ml/min, respectively).

Full text

PDF
721

Selected References

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

  1. Bergan T., Arnold E. Pharmacokinetics of metronidazole in healthy adult volunteers after tablets and suppositories. Chemotherapy. 1980;26(4):231–241. doi: 10.1159/000237911. [DOI] [PubMed] [Google Scholar]
  2. Brogden R. N., Heel R. C., Speight T. M., Avery G. S. Metronidazole in anaerobic infections: a review of its activity, pharmacokinetics and therapeutic use. Drugs. 1978 Nov;16(5):387–417. doi: 10.2165/00003495-197816050-00002. [DOI] [PubMed] [Google Scholar]
  3. Carmine A. A., Brogden R. N., Heel R. C., Speight T. M., Avery G. S. Tinidazole in anaerobic infections: a review of its antibacterial activity, pharmacological properties and therapeutic efficacy. Drugs. 1982 Aug;24(2):85–117. doi: 10.2165/00003495-198224020-00001. [DOI] [PubMed] [Google Scholar]
  4. Charuel C., Nachbaur J., Monro A. M., De Palol J. The pharmacokinetics of intravenous tinidazole in man. J Antimicrob Chemother. 1981 Oct;8(4):343–344. doi: 10.1093/jac/8.4.343. [DOI] [PubMed] [Google Scholar]
  5. Gjerløff C., Arnold E. Pharmacokinetics of intravenous metronidazole in man. Acta Pharmacol Toxicol (Copenh) 1982 Aug;51(2):132–135. doi: 10.1111/j.1600-0773.1982.tb01003.x. [DOI] [PubMed] [Google Scholar]
  6. Houghton G. W., Thorne P. S., Smith J., Templeton R., Collier J. Comparison of the pharmacokinetics of metronidazole in healthy female volunteers following either a single oral or intravenous dose. Br J Clin Pharmacol. 1979 Oct;8(4):337–341. doi: 10.1111/j.1365-2125.1979.tb04715.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Ioannides L., Somogyi A., Spicer J., Heinzow B., Tong N., Franklin C., McLean A. Rectal administration of metronidazole provides therapeutic plasma levels in postoperative patients. N Engl J Med. 1981 Dec 24;305(26):1569–1570. doi: 10.1056/NEJM198112243052607. [DOI] [PubMed] [Google Scholar]
  8. Marques R. A., Stafford B., Flynn N., Sadée W. Determination of metronidazole and misonidazole and their metabolites in plasma and urine by high-performance liquid chromatography. J Chromatogr. 1978 Jul 1;146(1):163–166. doi: 10.1016/s0378-4347(00)81303-1. [DOI] [PubMed] [Google Scholar]
  9. Mattie H., Dijkmans B. A., van Gulpen C. The pharmacokinetics of metronidazole and tinidazole in patients with mixed aerobic--anaerobic infections. J Antimicrob Chemother. 1982 Aug;10 (Suppl A):59–64. doi: 10.1093/jac/10.suppl_a.59. [DOI] [PubMed] [Google Scholar]
  10. Ripa T., Weström L., Mårdh P. A., Andersson K. E. Concentrations of tinidazole in body fluids and tissues in gynaecological patients. Chemotherapy. 1977;23(4):227–235. doi: 10.1159/000221990. [DOI] [PubMed] [Google Scholar]
  11. Viitanen J., Auvinen O., Tunturi T. Serum and tissue tinidazole concentrations after intravenous infusion. Chemotherapy. 1983;29(1):13–17. doi: 10.1159/000238167. [DOI] [PubMed] [Google Scholar]
  12. Welling P. G., Monro A. M. The pharmacokinetics of metronidazole and tinidazole in man. Arzneimittelforschung. 1972 Dec;22(12):2128–2132. [PubMed] [Google Scholar]
  13. Wood B. A., Faulkner J. K., Monro A. M. The pharmacokinetics, metabolism and tissue distribution of tinidazole. J Antimicrob Chemother. 1982 Aug;10 (Suppl A):43–57. doi: 10.1093/jac/10.suppl_a.43. [DOI] [PubMed] [Google Scholar]
  14. Wood B. A., Monro A. M. Pharmacokinetics of tinidazole and metronidazole in women after single large oral doses. Br J Vener Dis. 1975 Feb;51(1):51–53. doi: 10.1136/sti.51.1.51. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES