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Title: Metronidazole as a radiosensitizer: a preliminary report on estimation in serum and saliva

Abstract

Some studies indicate the clinical benefit of hypoxic radiosensitizers in patients who are undergoing radiotherapy. Serum level of sensitizers are usualy advised; however they are very demanding on the patient. Saliva level of the sensitizers may be an alternative method. This study correlated serum level of metronidazole to the saliva level in 10 patients who were undergoing radiotherapy with the sensitizer. A change to the saliva level method appears to relieve the patients.

Authors:
; ; ; ;
Publication Date:
Research Org.:
Free Univ., Amsterdam, Netherlands
OSTI Identifier:
6879682
Alternate Identifier(s):
OSTI ID: 6879682
Resource Type:
Conference
Resource Relation:
Journal Name: Int. J. Radiat. Oncol., Biol. Phys.; (United States); Journal Volume: 6:9
Country of Publication:
United States
Language:
English
Subject:
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.; 62 RADIOLOGY AND NUCLEAR MEDICINE; BLOOD SERUM; COMPARATIVE EVALUATIONS; METRONIDAZOLE; SAMPLING; SALIVA; TIME DEPENDENCE; ANOXIA; LIQUID COLUMN CHROMATOGRAPHY; PATIENTS; RADIOTHERAPY; ALCOHOLS; AZOLES; BIOLOGICAL MATERIALS; BODY FLUIDS; CHROMATOGRAPHY; DRUGS; HETEROCYCLIC COMPOUNDS; HYDROXY COMPOUNDS; IMIDAZOLES; MATERIALS; MEDICINE; NITRO COMPOUNDS; NUCLEAR MEDICINE; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; RADIOLOGY; RADIOSENSITIZERS; RESPONSE MODIFYING FACTORS; SEPARATION PROCESSES; THERAPY 560306* -- Chemicals Metabolism & Toxicology-- Man-- (-1987); 550603 -- Medicine-- External Radiation in Therapy-- (1980-)

Citation Formats

Karim, A.B.M.F., Faber, D.B., Haas, R.E., Hoekstra, F.H., and Njo, K.H. Metronidazole as a radiosensitizer: a preliminary report on estimation in serum and saliva. United States: N. p., 1980. Web.
Karim, A.B.M.F., Faber, D.B., Haas, R.E., Hoekstra, F.H., & Njo, K.H. Metronidazole as a radiosensitizer: a preliminary report on estimation in serum and saliva. United States.
Karim, A.B.M.F., Faber, D.B., Haas, R.E., Hoekstra, F.H., and Njo, K.H. Mon . "Metronidazole as a radiosensitizer: a preliminary report on estimation in serum and saliva". United States. doi:.
@article{osti_6879682,
title = {Metronidazole as a radiosensitizer: a preliminary report on estimation in serum and saliva},
author = {Karim, A.B.M.F. and Faber, D.B. and Haas, R.E. and Hoekstra, F.H. and Njo, K.H.},
abstractNote = {Some studies indicate the clinical benefit of hypoxic radiosensitizers in patients who are undergoing radiotherapy. Serum level of sensitizers are usualy advised; however they are very demanding on the patient. Saliva level of the sensitizers may be an alternative method. This study correlated serum level of metronidazole to the saliva level in 10 patients who were undergoing radiotherapy with the sensitizer. A change to the saliva level method appears to relieve the patients.},
doi = {},
journal = {Int. J. Radiat. Oncol., Biol. Phys.; (United States)},
number = ,
volume = 6:9,
place = {United States},
year = {Mon Sep 01 00:00:00 EDT 1980},
month = {Mon Sep 01 00:00:00 EDT 1980}
}

Conference:
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  • Metronidazole was administered orally to 25 patients and its maximum concentration in blood and tumor tissues, its ability to cross the blood/brain barrier and concentrate in the cerebrospinal fluid and brain tumor tissue, its immediate and long-term toxicity, and its enhancement of irradiation in normal tissue were studied. Maximum blood concentrations of 700 to 1,200 $mu$M (120 to 220 $mu$g/ml) were obtained at four hours with doses of 6 g/m$sup 2$. Moderate and transient nausea and vomiting were the only immediate signs of toxicity. No long-term toxicity was found up to 18 months after administration of the drug. These datamore » indicate that metronidazole can feasibly be administered in clinical trials of fractionated radiotherapy using dosages ranging from 9.5 to 11 g three times a week for three to four weeks. (auth)« less
  • As an extension of studies on the clinical use of nitroimidazoles as radiosensitizers, single-dose pharmacokinetic studies of iv metronidazole (500 mg/100-ml vials) were performed in eight consenting patients. Single doses of 0.5, 1.0, 1.5, and 2.0 g (0.29 to 1.21 g/m2) were administered iv by a zero-order infusion pump. Serial timed blood and urine samples were assayed for metronidazole and its two metabolites (acetic acid and ethoxy compounds) using a high-pressure liquid chromatographic assay. Open two-compartment kinetic characteristics of metronidazole were computed from simultaneous plasma infusion and urine excretion-rate equations using a nonlinear least-squares regression analysis program (NONLIN). Means ofmore » the four kinetic parameters were (h-1): k12, 1.18; k21, 0.86; k10, 0.22; and k'e, 0.46 x 10(-4). Means of the apparent volumes of distribution were (liters/kg): Vc, 0.41; VB, 1.02; and Vss, 0.75. The mean (+- SD) for alpha-half-life was 1.2 +- 1.3 hours, and that for beta-half-life was 9.8 +- 5.9 hours. Seven of the eight patients received a second identical dose orally 1 week later, and the absolute bioavailability was estimated to approximate 100%. Unless the oral route is not feasible and if immediate high peak blood levels are not necessary, oral metronidazole is the preferred route of administration of metronidazole for its radiosensitizing effects.« less