Clioquinol

Basic toxicokinetics

Administrative data

Endpoint:

basic toxicokinetics in vivo

Type of information:

experimental study

Adequacy of study:

supporting study

Reliability:

4 (not assignable)

Data source

Reference

Reference Type:

publication

Title:

No information

Author:

Ellenhorn, M.J. and D.G. Barceloux.

Year:

1988

Bibliographic source:

Medical Toxicology - Diagnosis and Treatment of Human Poisoning.New York, NY: Elsevier Science Publishing Co., Inc. 1988.p. 363

Materials and methods

Objective of study:

absorption

excretion

Test guideline

Qualifier:

according to guideline

Guideline:

other:

Principles of method if other than guideline:

Data is from Medical Toxicology

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

Clioquinol

EC Number:

204-984-4

EC Name:

Clioquinol

Cas Number:

130-26-7

Molecular formula:

C9H5ClINO

IUPAC Name:

5-chloro-7-iodoquinolin-8-ol

Details on test material:

- Name of test material (as cited in study report): clioquinol
- Substance type: Organic
- Physical state: Solid

Radiolabelling:

not specified

Test animals

Species:

human

Sex:

not specified

Administration / exposure

Route of administration:

other: oral and dermal

Vehicle:

not specified

Details on exposure:

Patients with widespread dermatitis were treated with 15-20 g of 3% clioquinol ointment to 40% of the body area twice daily.

Duration and frequency of treatment / exposure:

twice daily

Doses / concentrations

Remarks:

Doses / Concentrations:
15-20 g of 3% clioquinol ointment

No. of animals per sex per dose / concentration:

Details not available

Control animals:

not specified

Details on study design:

Patients with widespread dermatitis were treated with 15-20 g of 3% clioquinol ointment to 40% of the body area twice daily. This skin treatment resulted in a urinary excretion somewhat less than is obtained after a daily oral dose of 25 mg (one tablet) of clioquinol.

Results and discussion

Preliminary studies:

Patients with widespread dermatitis were treated with 15-20 g of 3% clioquinol ointment to 40% of the body area twice daily. The serum concentration increased to 0.8-1.2 ug/ml within 4 hr of application. In one patient, 15-20 mg was excreted in the urine daily mainly in the form of conjugated metabolites. This skin treatment resulted in a urinary excretion somewhat less than is obtained after a daily oral dose of 25 mg (one tablet) of clioquinol. Thus, 3-4% of the applied clioquinol was absorbed. 25% was excreted in the urine.

Main ADME results

Main ADME results 1

Type:

absorption

Results:

3-4% of the applied clioquinol was absorbed

Main ADME results 2

Type:

excretion

Results:

25% was excreted in the urine

Toxicokinetic / pharmacokinetic studies

Details on absorption:

3-4% of the applied clioquinol was absorbed.

Details on excretion:

In one patient, 15-20 mg was excreted in the urine daily mainly in the form of conjugated metabolites.This skin treatment resulted in a urinary excretion somewhat less than is obtained after a daily oral dose of 25 mg (one tablet) of clioquinol.

Metabolite characterisation studies

Metabolites identified:

yes

Details on metabolites:

In the form of conjugated metabolites.

Applicant's summary and conclusion

Conclusions:

Interpretation of results (migrated information): low bioaccumulation potential based on study results
3-4% of the applied clioquinol was absorbed, while 25% was excreted in the urine.

Executive summary:

15-20 mg of test substance Clioquinolwas excreted in the urine daily mainly in the form of conjugated metabolites. This skin treatment resulted in a urinary excretion somewhat less than is obtained after a daily oral dose of 25 mg (one tablet) of Clioquinol. Thus, 3-4% of the applied Clioquinol was absorbed and 25% was excreted in the urine.