Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic group: psycholeptics, antipsychotics.
ATC code: N05AH06.

Entumin is a neuroleptic of the dibenzothiazepine group which acts by inhibiting the central dopaminergic receptors.
Its action manifests in three phases:
-     A rapid symptomatic effect which may appear from the very first day and concerns anxiety.
-     A predominant, progressive sedative action on psychomotor activity and vigilance.
-     An antipsychotic action that sets in more slowly, in stages; improvements do not involve any secondary depressive reactions, even after long-term treatment.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

Due to method-related difficulties, the pharmacokinetics and metabolism are not yet fully understood.
In animals, absorption of radioactively (tritium) labelled clotiapine is good and rapid, with elimination occurring within 24 to 140 hours, depending on the species, at a rate of 65 - 80% via the urine and faeces.
In humans, absorption of clotiapine after oral administration is good and its biotransformation is almost complete. The metabolites are, for the vast majority, glucuronides highly soluble in water which are eliminated via the urine. The main metabolite is N-dimethyl sulphoxide; 25 - 40% of the administered dose is recovered in the urine as unchanged substance (approx. 10%) or known metabolites.