Cyclohexylamine

Basic toxicokinetics

Administrative data

Endpoint:

basic toxicokinetics in vivo

Type of information:

experimental study

Adequacy of study:

key study

Reliability:

2 (reliable with restrictions)

Data source

Reference

Reference Type:

publication

Title:

Pharmacokinetics, carciovascular and metabolic actions of cyclohexylamine in man

Author:

Eichelbaum M, Hengstmann JH, Rost HD, Brecht T, Dengler HJ

Year:

1974

Bibliographic source:

Arch Toxicol 31, 243-263

Materials and methods

Objective of study:

toxicokinetics

Principles of method if other than guideline:

Cyclohexylamine was administered orally in doses of 2.5, 5, amd 10 mg/kg bw to 11 healthy volunteers to determine absorption, plasma half lives, excretion, and biochemical effects

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

Cyclohexylamine

EC Number:

203-629-0

EC Name:

Cyclohexylamine

Cas Number:

108-91-8

Molecular formula:

C6H13N

IUPAC Name:

cyclohexanamine

Details on test material:

cyclohexylamine purissimum adjusted with hydrochloric acid to a pH of about 7 (no further data)

Radiolabelling:

no

Test animals

Species:

human

Strain:

other: medical or laboratory staff members familiar with Cyclamate/cyclohexylamine problem

Sex:

male

Administration / exposure

Route of administration:

other: oral (total dose at once)

Vehicle:

water

Duration and frequency of treatment / exposure:

once

Doses / concentrations

Remarks:

Doses / Concentrations:
2.5, 5, 10 mg/kg bw

No. of animals per sex per dose / concentration:

total number : 11 male healthy volunteers; they fasted over night and did not take any food or fluid during the first 4 hours of the experiment.
They were lying in a quiet room 30 min before and 4 hours after ingestion of the testsubstance

Control animals:

not specified

Results and discussion

Main ADME results

Main ADME results 1

Type:

absorption

Results:

Almost complete enteral absorption

Main ADME results 2

Type:

excretion

Results:

86 -95 % of the administered doses were excreted in the urine during 48 hours as unchanged compound

Toxicokinetic / pharmacokinetic studies

Details on absorption:

levels of cyclohexylamine could be observed already 15 min after the administration.
Peak levels were obtained 90-120 min after dosing; thereafter the falll in plasma cyclohexylamine was shown to be linear when plotted on a semilogarithmic scale

Details on distribution in tissues:

no data

Details on excretion:

no further data

Toxicokinetic parameters

Toxicokinetic parameters:

other: half life in plasma ranged from 3.5 -4.8 hours:clear dose dependency

Metabolite characterisation studies

Metabolites identified:

no

Any other information on results incl. tables

Cyclohexylamine caused a dose dependent rise in arterial blood pressure . A close correlation between plasma level of CHA and increase in mean arterial blood pressure could be established. A significant increase in fatty acids and cumulative urinary excretion of catecholamine was observed only after the administration of 10 mg/kg bw.