PINAVERIUM NOVAGENERICS

Pinaverium is a spasmolytic agent used for functional gastrointestinal disorders.

It is a quaternary ammonium compound that acts as an atypical calcium antagonist to restore normal bowel function.

It is shown to relieve

GI spasm and pain, transit disturbances and other symptoms related to motility disorders and may be considered as effective first-lline therapy for patients with irritable bowel syndrome (IBS) 5.

Pinaverium bromide is the common ingredient in formulations, mostly as oral tablets.

Although it is not a currently approved drug by the FDA, pinaverium is available in over 60 countries including Canada.

Pinaverium is indicated for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.

Pinaverium is a selective and specific voltage-dependent calcium channel blocker located on intestinal smooth muscle cells to inhibit calcium influx.

It mediates various effects on the

GI tract: it causes oesophageal, gastric and duodenal relaxation, relaxes the colon and intestines, inhibits colonic motility in response to food, hormonal or pharmacological stimuli, accelerates gastric emptying, and reduces contractions of the gallbladder and phasic contractions of sphincter of Oddi 10, 5.

At higher concentrations, pinaverium also exhibits very weak anticholinergic effects 10 but is not shown to display vasodilatory or anti-arrythmic actions 9.

After oral administration, pinaverium is poorly absorbed (5-10%) followed by uptake by liver.

Poor absorption is due to its highly polar quaternary ammonium group and high molecular weight 10, which limits extensive diffusion across all cell membranes and promotes its selectivity towards the gastrointestinal tracts.

Peak plasma concentration is reached within one hour after administration and the absolute oral bioavailability is reported to be less than 1%.

It is selectively distributed to the digestive tract due to poor absorption and marked hepatobiliary excretion 10.

Hepatic metabolism of pinaverium involves demethylation of one of the methoxy groups, hydroxylation of the norpinanyl ring and elimination of the benzyl group with subsequent opening of the morpholine ring 10.

Pinaverium is predominantly eliminated into feces 10.

The mean elimination half life is approximately 1.5 hours 10.

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Some minor

GI-related adverse effects include epigastric pain and/or fullness, nausea, constipation, heartburn, distension, and diarrhoea.

Other side effects are headache, dry mouth, drowsiness, vertigo and skin allergy.

LD50 in mice, rats and rabbits are 1531 mg/kg, 1145 mg/kg and 154 mg/kg, respectively 10.

Pinaverium displays no teratogenic, mutagenic or carcinogenic potential.