Duspatalin Retard Mechanism of Action

Pharmacotherapeutic group: Synthetic anticholinergics, esters with tertiary amino group. ATC-Code: A03AA04.
Pharmacology: Pharmacodynamics: The following is a detailed description of how the active ingredient of Duspatalin works. For further explanations consult a doctor.
Mechanism of action and pharmacodynamic effects: Mebeverine is a musculotropic antispasmodic with a direct effect on the smooth muscle of the gastro-intestinal tract, relieving spasm without affecting normal gut motility. Since this effect is not mediated by the autonomic nervous system, the typical anti-cholinergic side-effects are absent.
Pharmacokinetics: The following is a detailed description of how the active ingredient of Duspatalin is metabolized by the body. For further explanations consult a doctor.
Absorption: Mebeverine is rapidly and completely absorbed after oral administration of tablets. The modified release formulation permits a twice daily dosing scheme.
Distribution: No significant accumulation occurs after multiple doses.
Biotransformation: Mebeverine hydrochloride is mainly metabolized by esterases, which split the ester bonds into veratric acid and mebeverine alcohol firstly.
The main metabolite in plasma is DMAC (demethylated carboxylic acid). The steady state elimination half-life of DMAC is 5.77 h. During multiple dosing (200 mg b.i.d.) the C_max of DMAC is 804 ng/ml, and t_max is about 3 hrs. The relative bioavailability of the modified release capsule appears to be optimal with a mean ratio of 97%.
Elimination: Mebeverine is not excreted as such, but metabolized completely; the metabolites are excreted nearly completely. Veratric acid is excreted into the urine, mebeverine alcohol is also excreted into the urine, partly as the corresponding carboxylic acid (MAC) and partly as the demethylated carboxylic acid (DMAC).
Paediatric population: No pharmacokinetic studies have been conducted in children with any formulation of mebeverine.