The present study was carried out to screen the anticholinergic
and cardiovascular side effects of tianeptine and to evaluate
its analgesic effects versus amitriptyline.
Data obtained in the present work pointed out those gradually
increasing doses of tianeptine induced non-significant inhibition
of rhythmic contractions of rabbit jejunum (P > 0.05).
While, gradually increasing doses of amitriptylene, however,
induced a significant inhibition of rhythmic contractions of
isolated rabbit jejunum (P < 0.05). Tianeptine had less inhibitory
effect on isolated rabbit intestine than amitriptyline when
added in the same concentrations. Moreover, the inhibitory effect
of tianeptine and amitriptyline were not affected by prior
addition of alpha- and beta-adrenoreceptor blockers (phentolamine
and propranolol, respectively) or the dopaminergic receptor
blocker (metoclopramide). In addition, tianeptine produced
a non-significant decrease in acetylcholine (A Ch)
induced intestinal contractions, while, amitriptyline significantly
attenuated A Ch- induced contractions of isolated rabbit
intestine.
Regarding the effect on cardiovascular system, the results
of the present work showed that, gradually increasing concentrations
of both tianeptine and amitraptyline produced a non-
significant decrease in the 'contractility of isolated rabbit bean
(P >0.05).
Gradually increasing concentrations of tianeptine produced
a non- significant decrease in norepinephrine-induced contraction
of isolated rabbit aortic strip while amitriptyline in a concentration
of 32 ug/ml produced significant decrease in norepinephrine-
induced contraction of isolated rabbit aortic strip.
The results of the present work showed that, acute administration
of tianeptine and amitriptyline produced a nonsignificant
decrease in mean systolic blood pressure and in the
bean rate of anaesthetized rats. Moreover, acute administration
of tianeptine and amitriptyline had a significant analgesic effect
(11/40.05) with no differences between the analgesic potency
of both drugs.
In conclusion, tianeptine had low incidence of anticholinergic
effects, postural hypotension and cardiotoxicity in comparison
with amitriptyline, which had moderate to marked anticholinergic
side effects. In addition, it produced an analgesic
effect which can be useful in depressed patients. |