Dicetel Mechanism of Action

Pharmacotherapeutic Group: Other drugs for functional bowel disorders.
Pharmacology: Pharmacodynamics: The following is a detailed description of how the active ingredients of Dicetel work. For further explanations please consult a doctor.
Pinaverium bromide is an antispasmodic which selectively acts on the gastro-intestinal tract. It is a calcium antagonist which inhibits the influx of calcium into intestinal smooth muscle cells. In animal, pinaverium directly or indirectly reduces the effects of the stimulation of the sensitive afferences. It is free from anticholinergic effects. It is also devoid of effects on the cardiovascular system.
Paediatric Population: Pharmacodynamic and efficacy studies have mainly been conducted in adults. In one open, baseline-controlled clinical study the efficacy and safety have been assessed in 29 children aged 5 to 15 over a period of 7-15 days with a daily dose of 100-150 mg. The safety and tolerability was shown to be good. Efficacy was analyzed only for the subset of patients (N=17) suffering from abdominal pain associated to an organic lesion or to previous pathological symptomatology. Overall clinical responses were considered good in 9 patients (53%), partial in 6 patients (35%) and nil in 2 patients (12%).
Pharmacokinetics: The following is a detailed description of how the active ingredients of Dicetel are metabolized by the body. For further explanations please consult a doctor.
After oral administration pinaverium bromide is rapidly absorbed with peak plasma concentrations occurring within one hour. The drug is extensively metabolized and eliminated via the liver. The elimination half-life is 1.5 hours.
Absolute bioavailability for the oral formulation is very low (<1%). Major route of excretion is via the feces.
Plasma protein binding of pinaverium bromide is high (95-97%).
Toxicology: Preclinical safety data: Toxicity: Toxicity of pinaverium bromide after oral administration was low. Signs of toxicity were mostly limited to general signs of toxicity, gastrointestinal symptoms and CNS symptoms.
Genotoxicity, carcinogenic potential, teratogenicity: Pinaverium bromide did not display genotoxic or carcinogenic properties. At doses 2 fold the maximal recommended clinical dose pinaverium had no teratogenic potential.
Reproductive toxicity: At doses 2 fold the maximal recommended clinical dose pinaverium bromide decreased gravidity performance, but had no relevant effect on the pre- or post-natal development. Placental transfer of pinaverium bromide and transfer into the milk were not studied.