Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Mechanism of action (MOA)
The mechanism of action of carbamazepine, the active substance of Tegretol, has only been partially elucidated. Carbamazepine stabilizes hyperexcited nerve membranes, inhibits repetitive neuronal discharges, and reduces synaptic propagation of excitatory impulses. It is conceivable that prevention of repetitive firing of sodium-dependent action potentials in depolarized neurons via use- and voltage-dependent blockade of sodium channels may be its main mechanism of action.

Whereas reduction of glutamate release and stabilization of neuronal membranes may account mainly for the antiepileptic effects, the depressant effect on dopamine and noradrenaline turnover could be responsible for the antimanic properties of carbamazepine.


Pharmacotherapeutic group, ATC
Therapeutic class: antiepileptic, neurotropic, and psychotropic agent; (ATC Code: N03 AF01).
Dibenzazepine derivative.

Pharmacodynamics (PD)As an antiepileptic agent its spectrum of activity embraces: partial seizures (simple and complex) with and without secondary generalization; generalized tonic- clonic seizures, as well as combinations of these types of seizures.

In clinical studies Tegretol given as monotherapy to patients with epilepsy - in particular children and adolescents - has been reported to exert a psychotropic action, including a positive effect on symptoms of anxiety and depression as well as a decrease in irritability and aggressiveness. As regards cognitive and psychomotor performance, in some studies equivocal or negative effects, depending also upon dosages administered, were reported. In other studies, a beneficial effect on attentiveness, cognitive performance/memory was observed.

As a neurotropic agent Tegretol is clinically effective in a number of neurological disorders, e.g. it prevents paroxysmal attacks of pain in idiopathic and secondary trigeminal neuralgia; in addition, it is used for the relief of neurogenic pain in a variety of conditions, including tabes dorsalis, post-traumatic paresthesia, and post-herpetic neuralgia; in diabetes insipidus centralis, Tegretol reduces the urinary volume and relieves the feeling of thirst.

As a psychotropic agent Tegretol proved to have clinical efficacy in affective disorders, i.e. as treatment for acute mania as well as for maintenance treatment of (manic-depressive) bipolar affective disorders, when given either as monotherapy or in combination with neuroleptics, antidepressants, or lithium, in excited schizo-affective disorder and excited mania in combination with other neuroleptics, and in rapid cycling episodes.

Clinical efficacy and safety
No recent clinical trials have been conducted with Tegretol.

Pharmacokinetic Properties