Spasmopinaver

Spasmopinaver Uses, Dosage, Side Effects, Food Interaction and all others data.

Spasmopinaver 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) . Spasmopinaver 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.

Spasmopinaver 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 .

Spasmopinaver
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Spasmopinaver
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

Spasmopinaver is a spasmolytic agent used for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.

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

Spasmopinaver is also used to associated treatment for these conditions: Flatulence, Irritable Bowel Syndrome (IBS), Functional disorders of the biliary tract, Stomach cramps

How Spasmopinaver works

Spasmopinaver 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 . Spasmopinaver 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 . Spasmopinaver 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%.