Zerpyco
Zerpyco Uses, Dosage, Side Effects, Food Interaction and all others data.
Zerpyco 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) . Zerpyco 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.
Zerpyco 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 . At higher concentrations, pinaverium also exhibits very weak anticholinergic effects but is not shown to display vasodilatory or anti-arrythmic actions .
Trade Name | Zerpyco |
Generic | Pinaverium |
Type | |
Formula | C26H41BrNO4 |
Weight | Average: 511.52 Monoisotopic: 510.221348 |
Protein binding | Pinaverium is highly bound to human plasma proteins with the ratio of 97% . |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zerpyco is a spasmolytic agent used for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.
Zerpyco is indicated for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.
Zerpyco is also used to associated treatment for these conditions: Flatulence, Irritable Bowel Syndrome (IBS), Functional disorders of the biliary tract, Stomach cramps
How Zerpyco works
Zerpyco interacts with the 1,4-dihydropyridine binding sites on voltage dependent L-type calcium channels located on GI smooth muscle cells in a competitve manner . The binding site is located in the alpha 1S subunit and pinaverium most likely antagonizes the action of calcium ions by stabilizing a non-conducting channel state . Zerpyco inhibits smooth muscle contractions of the GI tract by inhibiting inward calcium current and calcium influx. It is suggested that pinaverium may be able to bind to both closed or inactivates states of the calcium channel with similar affinity .
Toxicity
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. Oral LD50 in mice, rats and rabbits are 1531 mg/kg, 1145 mg/kg and 154 mg/kg, respectively . Zerpyco displays no teratogenic, mutagenic or carcinogenic potential.
Food Interaction
- Take with a full glass of water.
- Take with food. This helps prevent pinaverium from irritating the esophagus.
Volume of Distribution
It is selectively distributed to the digestive tract due to poor absorption and marked hepatobiliary excretion .
Elimination Route
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 , 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%.
Half Life
The mean elimination half life is approximately 1.5 hours .
Elimination Route
Zerpyco is predominantly eliminated into feces .
Innovators Monograph
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